PL322549A1 - Inhibitors of proteinous farnesiltransferase - Google Patents

Inhibitors of proteinous farnesiltransferase

Info

Publication number
PL322549A1
PL322549A1 PL96322549A PL32254996A PL322549A1 PL 322549 A1 PL322549 A1 PL 322549A1 PL 96322549 A PL96322549 A PL 96322549A PL 32254996 A PL32254996 A PL 32254996A PL 322549 A1 PL322549 A1 PL 322549A1
Authority
PL
Poland
Prior art keywords
farnesiltransferase
proteinous
inhibitors
proteinous farnesiltransferase
Prior art date
Application number
PL96322549A
Inventor
George D Hartman
Neville J Anthony
Terrence M Ciccarone
Robert P Gomez
John H Hutchinson
Theresa M Williams
Christopher J Dinsmore
Gerald E Stokker
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US08/600,728 external-priority patent/US5856326A/en
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of PL322549A1 publication Critical patent/PL322549A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
PL96322549A 1995-03-29 1996-03-25 Inhibitors of proteinous farnesiltransferase PL322549A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41282995A 1995-03-29 1995-03-29
US47069095A 1995-06-06 1995-06-06
US08/600,728 US5856326A (en) 1995-03-29 1996-03-01 Inhibitors of farnesyl-protein transferase

Publications (1)

Publication Number Publication Date
PL322549A1 true PL322549A1 (en) 1998-02-02

Family

ID=27410959

Family Applications (1)

Application Number Title Priority Date Filing Date
PL96322549A PL322549A1 (en) 1995-03-29 1996-03-25 Inhibitors of proteinous farnesiltransferase

Country Status (21)

Country Link
EP (1) EP0820445A1 (en)
JP (1) JP3043815B2 (en)
CN (1) CN1195340A (en)
AR (1) AR002726A1 (en)
AU (1) AU710672B2 (en)
BG (1) BG101973A (en)
BR (1) BR9607953A (en)
CA (1) CA2216707A1 (en)
CZ (1) CZ306297A3 (en)
EE (1) EE9700314A (en)
HR (1) HRP960143A2 (en)
HU (1) HUP9801883A3 (en)
IL (1) IL117580A0 (en)
IS (1) IS4568A (en)
MX (1) MX9707459A (en)
NO (1) NO974457L (en)
NZ (1) NZ305254A (en)
PL (1) PL322549A1 (en)
SK (1) SK129297A3 (en)
TR (1) TR199701056T1 (en)
WO (1) WO1996030343A1 (en)

Families Citing this family (168)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL115420A0 (en) 1994-09-26 1995-12-31 Zeneca Ltd Aminoheterocyclic derivatives
GB9516709D0 (en) * 1995-08-15 1995-10-18 Zeneca Ltd Medicament
US6083949A (en) * 1995-10-06 2000-07-04 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
GB9602166D0 (en) 1996-02-02 1996-04-03 Zeneca Ltd Aminoheterocyclic derivatives
EP0880501A1 (en) 1996-02-02 1998-12-02 Zeneca Limited Heterocyclic compounds useful as pharmaceutical agents
US5885995A (en) * 1996-04-03 1999-03-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997036592A1 (en) * 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU707347B2 (en) * 1996-04-03 1999-07-08 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6063930A (en) * 1996-04-03 2000-05-16 Merck & Co., Inc. Substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
US5891889A (en) * 1996-04-03 1999-04-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5780488A (en) * 1996-04-03 1998-07-14 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2250460A1 (en) * 1996-04-03 1997-10-09 John H. Hutchinson Inhibitors of farnesyl-protein transferase
US5922883A (en) * 1996-04-03 1999-07-13 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU716153B2 (en) * 1996-04-03 2000-02-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU727939B2 (en) * 1996-04-03 2001-01-04 Merck & Co., Inc. A method of treating cancer
US5869682A (en) * 1996-04-03 1999-02-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5859012A (en) * 1996-04-03 1999-01-12 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5919785A (en) * 1996-04-03 1999-07-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5939557A (en) * 1996-04-03 1999-08-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5852010A (en) * 1996-04-03 1998-12-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5780492A (en) * 1996-04-03 1998-07-14 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5965578A (en) * 1996-04-03 1999-10-12 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6001835A (en) * 1996-04-03 1999-12-14 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5925651A (en) * 1996-04-03 1999-07-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6080870A (en) * 1996-04-03 2000-06-27 Merck & Co., Inc. Biaryl substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
US5874452A (en) * 1996-04-03 1999-02-23 Merck & Co., Inc. Biheteroaryl inhibitors of farnesyl-protein transferase
US5883105A (en) * 1996-04-03 1999-03-16 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997038665A2 (en) * 1996-04-03 1997-10-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0959883A4 (en) * 1996-04-03 2001-05-09 Merck & Co Inc Inhibitors of farnesyl-protein transferase
SK18499A3 (en) * 1996-08-14 1999-07-12 Zeneca Ltd Substituted pyrimidine derivatives and their pharmaceutical use
UA56197C2 (en) 1996-11-08 2003-05-15 Зенека Лімітед Heterocyclic derivatives
EP1003374A1 (en) * 1996-12-30 2000-05-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2001511799A (en) 1997-02-13 2001-08-14 ゼネカ・リミテッド Heterocyclic compounds useful as oxide-squalene cyclase inhibitors
EP0966460A1 (en) 1997-02-13 1999-12-29 Zeneca Limited Heterocyclic compounds useful as oxido-squalene cyclase inhibitors
US5972942A (en) * 1997-03-27 1999-10-26 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6060038A (en) * 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
AUPO735997A0 (en) 1997-06-17 1997-07-10 Fujisawa Pharmaceutical Co., Ltd. Piperazine derivatives
GB9715895D0 (en) 1997-07-29 1997-10-01 Zeneca Ltd Heterocyclic compounds
US6103487A (en) * 1997-08-27 2000-08-15 Merck & Co., Inc. Method of treating cancer
US6387903B1 (en) 1997-08-27 2002-05-14 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
WO1999010525A1 (en) * 1997-08-27 1999-03-04 Merck & Co., Inc. A method of treating cancer
FR2774985A1 (en) * 1998-02-13 1999-08-20 Rhone Poulenc Rorer Sa New naphthyl carbonyl or sulfonyl oxopiperazine farnesyl transferase inhibitors, used as antiproliferative agents, e.g. for treating cancer
AU2286099A (en) * 1998-02-13 1999-08-30 Rhone-Poulenc Rorer S.A. Di-substituted naphthyl derivatives, preparation thereof, pharmaceutical compositions containing them
AU5086499A (en) * 1998-07-01 2000-01-24 Merck & Co., Inc. Process for making farnesyl-protein transferase inhibitors
GB9902989D0 (en) 1999-02-11 1999-03-31 Zeneca Ltd Heterocyclic derivatives
AU4005300A (en) * 1999-03-03 2000-09-21 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
EP1158982A4 (en) * 1999-03-03 2002-06-12 Merck & Co Inc Inhibitors of prenyl-protein transferase
US6358956B1 (en) * 1999-03-03 2002-03-19 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
JP2002538120A (en) * 1999-03-03 2002-11-12 メルク エンド カムパニー インコーポレーテッド Inhibitors of prenyl protein transferase
US6211182B1 (en) * 1999-03-08 2001-04-03 Schering Corporation Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms
US6458935B1 (en) 1999-06-23 2002-10-01 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
FR2819510B1 (en) * 2001-01-18 2003-10-31 Servier Lab NOVEL CYCLO [C] AZEPANE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
FR2819512B1 (en) * 2001-01-18 2003-02-21 Servier Lab NOVEL CYCLO [D] AZEPANE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
FR2819509B1 (en) 2001-01-18 2004-04-16 Servier Lab NOVEL CYCLOHEPTENE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
ES2382814T3 (en) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Cis-4 - [(4-chlorophenyl) sulfonyl] -4- (2,5-difluorophenyl) cyclohexanopropanoic acid for cancer treatment
ES2348332T3 (en) 2005-09-16 2010-12-02 Arrow Therapeutics Limited DERIVATIVES OF BIFENYL AND ITS USE IN THE TREATMENT OF HEPATITIS C.
LT2426129T (en) 2005-12-13 2017-02-10 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
EP2083831B1 (en) 2006-09-22 2013-12-25 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
EP2094680A2 (en) * 2006-12-18 2009-09-02 Novartis AG Imidazoles as aldosterone synthase inhibitors
AU2008204380B2 (en) 2007-01-10 2013-08-15 Msd Italia S.R.L. Amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors
WO2008106692A1 (en) 2007-03-01 2008-09-04 Novartis Vaccines And Diagnostics, Inc. Pim kinase inhibitors and methods of their use
KR20100017866A (en) 2007-05-21 2010-02-16 노파르티스 아게 Csf-1r inhibitors, compositions, and methods of use
RS54878B1 (en) 2007-06-13 2016-10-31 Incyte Holdings Corp Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
JP5501227B2 (en) 2007-06-27 2014-05-21 メルク・シャープ・アンド・ドーム・コーポレーション 4-Carboxybenzylamino derivatives as histone deacetylase inhibitors
ES2615389T3 (en) 2007-10-05 2017-06-06 Acucela, Inc. Alkoxyphenylpropylamines for the treatment of age-related macular degeneration
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
GB0813144D0 (en) 2008-07-17 2008-08-27 Glaxo Group Ltd Novel compounds
GB0813142D0 (en) 2008-07-17 2008-08-27 Glaxo Group Ltd Novel compounds
ES2740424T3 (en) 2009-03-13 2020-02-05 Agios Pharmaceuticals Inc Methods and compositions for disorders related to cell proliferation
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
JP5756457B2 (en) 2009-04-06 2015-07-29 アジオス ファーマシューティカルズ， インコーポレイテッド Pyruvate kinase M2 modulators, therapeutic compositions and related methods of use
UA106078C2 (en) 2009-05-22 2014-07-25 Інсайт Корпорейшн 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptanenitrile as jak inhibitors
WO2010135650A1 (en) 2009-05-22 2010-11-25 Incyte Corporation N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
US8765747B2 (en) 2009-06-12 2014-07-01 Dana-Farber Cancer Institute, Inc. Fused 2-aminothiazole compounds
SG177434A1 (en) 2009-06-29 2012-02-28 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
WO2011003103A2 (en) 2009-07-02 2011-01-06 Acucela, Inc. Pharmacology of visual cycle modulators
WO2011028685A1 (en) 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
MY174452A (en) 2009-10-14 2020-04-19 Schering Corp Substituted piperidines that increase p53 activity and the uses thereof
ES2594402T3 (en) 2009-10-21 2016-12-20 Agios Pharmaceuticals, Inc. Methods and compositions for disorders related to cell proliferation
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
MX364636B (en) 2010-03-10 2019-05-03 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors.
KR20130006664A (en) 2010-03-16 2013-01-17 다나-파버 캔서 인스티튜트 인크. Indazole compounds and their uses
SI2574168T1 (en) 2010-05-21 2016-07-29 Incyte Holdings Corporation Topical formulation for a jak inhibitor
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
WO2012018754A2 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF CATENIN (CADHERIN-ASSOCIATED PROTEIN), BETA 1 (CTNNB1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
AU2011292261B2 (en) 2010-08-17 2015-05-14 Sirna Therapeutics, Inc. RNA interference mediated inhibition of Hepatitis B virus (HBV) gene expression using short interfering nucleic acid (siNA)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
EP2613782B1 (en) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
WO2012036997A1 (en) 2010-09-16 2012-03-22 Schering Corporation Fused pyrazole derivatives as novel erk inhibitors
DK2632472T3 (en) 2010-10-29 2018-03-19 Sirna Therapeutics Inc RNA INTERFERENCE-MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERRING NUCLEIC ACIDS (SINA)
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
SG190839A1 (en) 2010-11-19 2013-07-31 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
JP5837091B2 (en) 2010-12-17 2015-12-24 アジオス ファーマシューティカルズ， インコーポレイテッド Novel N- (4- (azetidine-1-carbonyl) phenyl)-(hetero-) arylsulfonamide derivatives as modulators of pyruvate kinase M2 (PKM2)
US9351965B2 (en) 2010-12-21 2016-05-31 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
EP2655350B1 (en) 2010-12-21 2016-03-09 Agios Pharmaceuticals, Inc. Bicyclic pkm2 activators
TWI549947B (en) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 Therapeutic compounds and compositions
IN2013MN02170A (en) 2011-04-21 2015-06-12 Piramal Entpr Ltd
CA2834692A1 (en) 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy
PH12013502241A1 (en) 2011-05-03 2014-01-06 Agios Pharmaceuticals Inc Pyruvate kinase activators for use in therapy
CN102827073A (en) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 Therapeutically active compositions and application methods thereof
CN102827170A (en) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 Active treatment compositions and use method thereof
AU2012273164B2 (en) 2011-06-20 2015-05-28 Incyte Holdings Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
TW201313721A (en) 2011-08-18 2013-04-01 Incyte Corp Cyclohexyl azetidine derivatives as JAK inhibitors
UA111854C2 (en) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн METHODS AND INTERMEDIATE COMPOUNDS FOR JAK INHIBITORS
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP2822935B1 (en) 2011-11-17 2019-05-15 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
US20150087628A1 (en) * 2012-04-10 2015-03-26 The Regents Of The University Of California Compositions and methods for treating cancer
EP2844261B1 (en) 2012-05-02 2018-10-17 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
AR091079A1 (en) 2012-05-18 2014-12-30 Incyte Corp DERIVATIVES OF PIRROLOPIRIMIDINA AND PIRROLOPIRIDINA REPLACED WITH PIPERIDINILCICLOBUTILO AS JAK INHIBITORS
AU2013323508B2 (en) 2012-09-28 2017-11-02 Merck Sharp & Dohme Corp. Novel compounds that are ERK inhibitors
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
JP2015537030A (en) 2012-11-15 2015-12-24 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Sustained release dosage form of ruxolitinib
AU2013352568B2 (en) 2012-11-28 2019-09-19 Merck Sharp & Dohme Llc Compositions and methods for treating cancer
US8846657B2 (en) 2012-12-20 2014-09-30 Merck Sharp & Dohme Corp. Substituted imidazopyridines as HDM2 inhibitors
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
KR102366356B1 (en) 2013-03-06 2022-02-23 인사이트 홀딩스 코포레이션 Processes and intermediates for making a jak inhibitor
RS59411B1 (en) 2013-03-13 2019-11-29 Forma Therapeutics Inc 2-hydroxy-1-{4-[(4-phenylphenyl)carbonyl]piperazin-1-yl}ethan-1-one derivatives and related compounds as fatty acid synthase (fasn) inhibitors for the treatment of cancer
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
AU2014287121B2 (en) 2013-07-11 2018-11-15 Agios Pharmaceuticals, Inc. 2,4- or 4,6-diaminopyrimidine compounds as IDH2 mutants inhibitors for the treatment of cancer
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
EP3721873A1 (en) 2013-08-07 2020-10-14 Incyte Corporation Sustained release dosage forms for a jak1 inhibitor
WO2015034925A1 (en) 2013-09-03 2015-03-12 Moderna Therapeutics, Inc. Circular polynucleotides
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
WO2015138839A1 (en) 2014-03-14 2015-09-17 Agios Pharmaceuticals, Inc. Pharmaceutical compositions of therapeutically active compounds
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
JO3589B1 (en) 2014-08-06 2020-07-05 Novartis Ag Protein kinase c inhibitors and methods of their use
PL3209655T3 (en) 2014-10-24 2020-12-28 Landos Biopharma, Inc. Lanthionine synthetase c-like 2-based therapeutics
JP6854762B2 (en) 2014-12-23 2021-04-07 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド Inhibitor of cyclin-dependent kinase 7 (CDK7)
CA2978518C (en) 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
EP4344703A1 (en) 2015-06-11 2024-04-03 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
US11142507B2 (en) 2015-09-09 2021-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
PT3362066T (en) 2015-10-15 2021-11-16 Celgene Corp Combination therapy for treating malignancies
MD3362065T2 (en) 2015-10-15 2024-08-31 Servier Lab Combination therapy comprising ivosidenib, cytarabine and daunorubicin or idarubicin for treating acute myelogenous leukemia
JOP20190055A1 (en) 2016-09-26 2019-03-24 Merck Sharp & Dohme Anti-cd27 antibodies
EP3525785A4 (en) 2016-10-12 2020-03-25 Merck Sharp & Dohme Corp. KDM5 INHIBITORS
IL315837A (en) 2017-04-13 2024-11-01 Sairopa B V Anti-sirp alpha antibodies
US10556013B2 (en) 2017-06-20 2020-02-11 Imbria Pharmaceuticals, Inc. Compositions and methods for increasing efficiency of cardiac metabolism
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2019094312A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
TW201924683A (en) 2017-12-08 2019-07-01 美商英塞特公司 Low dose combination therapy for treatment of myeloproliferative neoplasms
AR114810A1 (en) 2018-01-30 2020-10-21 Incyte Corp PROCESSES AND INTERMEDIATES TO DEVELOP A JAK INHIBITOR
WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
CN110294713B (en) * 2018-03-22 2022-08-02 西华大学 A kind of preparation method of imidazole methylamine derivatives
CN113768934A (en) 2018-03-30 2021-12-10 因赛特公司 Treatment of hidradenitis suppurativa with JAK inhibitors
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
US12187701B2 (en) 2018-06-25 2025-01-07 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US12173026B2 (en) 2018-08-07 2024-12-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
TWI767148B (en) 2018-10-10 2022-06-11 美商弗瑪治療公司 Inhibiting fatty acid synthase (fasn)
WO2020092395A1 (en) 2018-10-29 2020-05-07 Forma Therapeutics, Inc. SOLID FORMS OF (4-(2-FLUORO-4-(1-METHYL-1 H-BENZO[d]IMIDAZOL-5-YL)BENZOYL) PIPERAZIN-1-YL)(1-HYDROXYCYCLOPROPYL)METHANONE
AU2020407645B2 (en) 2019-12-20 2022-10-06 Nimmune Biopharma, Inc. Lanthionine C-like protein 2 ligands, cells prepared therewith, and therapies using same
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11780811B2 (en) 2020-06-30 2023-10-10 Imbria Pharmaceuticals, Inc. Methods of synthesizing 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate
US11530184B2 (en) 2020-06-30 2022-12-20 Imbria Pharmaceuticals, Inc. Crystal forms of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate
US11883396B2 (en) 2021-05-03 2024-01-30 Imbria Pharmaceuticals, Inc. Methods of treating kidney conditions using modified forms of trimetazidine
WO2024180169A1 (en) 2023-03-02 2024-09-06 Carcimun Biotech Gmbh Means and methods for diagnosing cancer and/or an acute inflammatory disease

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1056055B (en) * 1974-03-01 1982-01-30 Malesci Sas Inst Farmaco Bilog Substd 1-alkyl 4-phenylpiperazines - with anti-hypertensive, vasodilating, alpha-inhibiting, anti-histamine and anti-bradykinin activity
US4371737A (en) * 1981-05-04 1983-02-01 Merrell Dow Pharmaceuticals Inc. 5-Aminomethyl-2,3-dihydro-2-oxo-1H-imidazole-4-carboxylic acid derivatives
US5159083A (en) * 1990-12-28 1992-10-27 Neurogen Corporation Certain aminomethyl phenylimidazole derivatives; a class of dopamine receptor subtype specific ligands
CA2165176A1 (en) * 1993-06-18 1995-01-05 Samuel L. Graham Inhibitors of farnesyl-protein transferase
US5478934A (en) * 1994-11-23 1995-12-26 Yuan; Jun Certain 1-substituted aminomethyl imidazole and pyrrole derivatives: novel dopamine receptor subtype specific ligands

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