[go: up one dir, main page]

MX9707459A - Inhibitors of farnesyl-protein transferase. - Google Patents

Inhibitors of farnesyl-protein transferase.

Info

Publication number
MX9707459A
MX9707459A MX9707459A MX9707459A MX9707459A MX 9707459 A MX9707459 A MX 9707459A MX 9707459 A MX9707459 A MX 9707459A MX 9707459 A MX9707459 A MX 9707459A MX 9707459 A MX9707459 A MX 9707459A
Authority
MX
Mexico
Prior art keywords
farnesyl
protein transferase
inhibitors
protein
farnesylation
Prior art date
Application number
MX9707459A
Other languages
Spanish (es)
Inventor
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 MX9707459A publication Critical patent/MX9707459A/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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (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)

Abstract

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
MX9707459A 1995-03-29 1996-03-25 Inhibitors of farnesyl-protein transferase. MX9707459A (en)

Applications Claiming Priority (4)

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
PCT/US1996/004019 WO1996030343A1 (en) 1995-03-29 1996-03-25 Inhibitors of farnesyl-protein transferase

Publications (1)

Publication Number Publication Date
MX9707459A true MX9707459A (en) 1997-12-31

Family

ID=27410959

Family Applications (1)

Application Number Title Priority Date Filing Date
MX9707459A MX9707459A (en) 1995-03-29 1996-03-25 Inhibitors of farnesyl-protein transferase.

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 (174)

* 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
US6313127B1 (en) 1996-02-02 2001-11-06 Zeneca Limited Heterocyclic compounds useful as pharmaceutical agents
US5891889A (en) * 1996-04-03 1999-04-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5965578A (en) * 1996-04-03 1999-10-12 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5922883A (en) * 1996-04-03 1999-07-13 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5885995A (en) * 1996-04-03 1999-03-23 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
US5919785A (en) * 1996-04-03 1999-07-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU716153B2 (en) * 1996-04-03 2000-02-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0906099A4 (en) * 1996-04-03 2001-02-07 Merck & Co Inc CANCER TREATMENT METHOD
EP0944388A4 (en) * 1996-04-03 2001-08-16 Merck & Co Inc FARNESYL PROTEIN TRANSFERASE INHIBITORS
US5869682A (en) * 1996-04-03 1999-02-09 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
US5939557A (en) * 1996-04-03 1999-08-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU707416B2 (en) * 1996-04-03 1999-07-08 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5852010A (en) * 1996-04-03 1998-12-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997036592A1 (en) * 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5780488A (en) * 1996-04-03 1998-07-14 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
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
JP2000507584A (en) * 1996-04-03 2000-06-20 メルク エンド カンパニー インコーポレーテッド Farnesyl-protein transferase inhibitor
CA2250587A1 (en) * 1996-04-03 1997-10-09 Christopher J. Dinsmore Inhibitors of farnesyl-protein transferase
US5859012A (en) * 1996-04-03 1999-01-12 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5780492A (en) * 1996-04-03 1998-07-14 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6001835A (en) * 1996-04-03 1999-12-14 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
KR20000029984A (en) * 1996-08-14 2000-05-25 사라 엔 람베쓰 Substituted pyrimidine derivatives and their pharmaceutical use
UA56197C2 (en) 1996-11-08 2003-05-15 Зенека Лімітед Heterocyclic derivatives
WO1998028980A1 (en) * 1996-12-30 1998-07-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1998035959A1 (en) 1997-02-13 1998-08-20 Zeneca Limited Heterocyclic compounds useful as oxido-squalene cyclase inhibitors
US6440972B1 (en) 1997-02-13 2002-08-27 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
AU8921398A (en) * 1997-08-27 1999-03-16 Merck & Co., Inc. A method of 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
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
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
JP2002542155A (en) * 1999-03-03 2002-12-10 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
WO2000051611A1 (en) * 1999-03-03 2000-09-08 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
US6376496B1 (en) * 1999-03-03 2002-04-23 Merck & Co., Inc. 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
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
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
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
TW200804345A (en) 2005-08-30 2008-01-16 Novartis Ag Substituted benzimidazoles and methods of preparation
ES2348332T3 (en) 2005-09-16 2010-12-02 Arrow Therapeutics Limited DERIVATIVES OF BIFENYL AND ITS USE IN THE TREATMENT OF HEPATITIS C.
PT1966202E (en) 2005-12-13 2012-01-03 Incyte Corp PYRIDOLES [2,3-B] PYRIDOLES AND PYRROLE [2,3-B] PYRIDINES SUBSTITUTED WITH HETEROARYLO AS JANUS KINASE INHIBITORS
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
DK2010528T3 (en) 2006-04-19 2018-01-15 Novartis Ag 6-O-Substituted Benzoxazole and Benzothiazole Compounds and Methods for Inhibiting CSF-1R Signaling
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
JP2010513482A (en) * 2006-12-18 2010-04-30 ノバルティス アーゲー Imidazoles as aldosterone synthase inhibitors
DK2805945T3 (en) 2007-01-10 2019-07-15 Msd Italia Srl AMID-SUBSTITUTED INDAZOLS AS POLY (ADP-RIBOSE) POLYMERASE (PARP) REQUESTS
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
AU2008254425A1 (en) 2007-05-21 2008-11-27 Novartis Ag CSF-1R inhibitors, compositions, and methods of use
RS53245B2 (en) 2007-06-13 2022-10-31 Incyte Holdings Corp JANUS KINASE INHIBITOR SALTS (R)-3-(4-(7H-PYROLO(2,3-D) PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANE-NITRILE
EP3103791B1 (en) 2007-06-27 2018-01-31 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
RU2541430C2 (en) * 2007-10-05 2015-02-10 Акусела Инк. Compositions and methods of treating neurodegenerative diseases
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
AU2010223919B2 (en) 2009-03-13 2016-03-31 Les Laboratoires Servier Methods and compositions for cell-proliferation-related disorders
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
CN102448951B (en) 2009-04-06 2017-05-10 安吉奥斯医药品有限公司 Pyruvate kinase M2 modulators, therapeutic compositions, and related methods of use
TW201100429A (en) 2009-05-22 2011-01-01 Incyte Corp 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
PL2432472T3 (en) 2009-05-22 2020-03-31 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
JP6073677B2 (en) 2009-06-12 2017-02-01 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Fused heterocyclic compounds and their use
NZ597379A (en) 2009-06-29 2014-04-30 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
EP4000610A1 (en) 2009-07-02 2022-05-25 Acucela Inc. Pharmacology of visual cycle modulators
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
PH12012500713A1 (en) 2009-10-14 2012-11-26 Merck Sharp & Dohme Substituted piperidines that increase p53 activity and the uses thereof
EP3064595B1 (en) 2009-10-21 2019-02-27 Agios Pharmaceuticals, Inc. Methods for cell-proliferation-related disorders
EP2519517B1 (en) 2009-12-29 2015-03-25 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
MX354212B (en) 2010-03-10 2018-02-19 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors.
EP2547661A2 (en) 2010-03-16 2013-01-23 Dana-Farber Cancer Institute, Inc. Indazole compounds and their uses
EA202091303A3 (en) 2010-05-21 2021-05-31 Инсайт Холдингс Корпорейшн JAK INHIBITOR COMPOSITION FOR LOCAL APPLICATION
EP2584903B1 (en) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
US8518907B2 (en) 2010-08-02 2013-08-27 Merck Sharp & Dohme Corp. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
RU2624045C2 (en) 2010-08-17 2017-06-30 Сирна Терапьютикс,Инк RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
EP2608669B1 (en) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
EP3327125B1 (en) 2010-10-29 2020-08-05 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acids (sina)
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
EP2651898B1 (en) 2010-12-17 2015-12-09 Agios Pharmaceuticals, Inc. Novel n-(4-(azetidine-1-carbonyl)phenyl)-(hetero-)arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators
CA2822432C (en) 2010-12-21 2019-09-24 Agios Pharmaceuticals, Inc. Bicyclic pkm2 activators
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
TWI549947B (en) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 Therapeutic compounds and compositions
JP2014514321A (en) 2011-04-21 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション Insulin-like growth factor 1 receptor inhibitor
WO2012151452A1 (en) 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc Pyruvate kinase activators for use in therapy
PH12017501176B1 (en) 2011-05-03 2023-03-08 Agios Pharmaceuticals Inc Pyruvate kinase activators for use in therapy
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
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
CN103797010B (en) 2011-06-20 2016-02-24 因塞特控股公司 As the azetidinyl phenyl of JAK inhibitor, pyridyl or pyrazinyl carboxamides derivatives
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
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
JP6106685B2 (en) 2011-11-17 2017-04-05 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 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
WO2013155223A1 (en) * 2012-04-10 2013-10-17 The Regents Of The University Of California Compositions and methods for treating cancer
EP3358013B1 (en) 2012-05-02 2020-06-24 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
US9233979B2 (en) 2012-09-28 2016-01-12 Merck Sharp & Dohme Corp. 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)
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
NZ708157A (en) 2012-11-15 2019-07-26 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
ME02925B (en) 2012-11-28 2018-04-20 Merck Sharp & Dohme COMPOSITIONS AND METHOD FOR THE TREATMENT OF CANCER
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
TWI634121B (en) 2013-03-06 2018-09-01 英塞特控股公司 Method and intermediate for preparing JAK inhibitor
WO2014164749A1 (en) 2013-03-13 2014-10-09 Forma Therapeutics, Inc. Novel compounds and compositions for inhibition of fasn
US9579324B2 (en) 2013-07-11 2017-02-28 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
CA2917671A1 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. 2,4-or 4,6-diaminopyrimidine compounds as idh2 mutants 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
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
MX394928B (en) 2013-08-07 2025-03-24 Incyte Holdings Corp EXTENDED-RELEASE DOSAGE FORMS FOR A JAK 1 (JANUS KINASE 1) INHIBITOR.
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
AU2014337122B2 (en) 2013-10-18 2019-01-03 Dana-Farber Cancer Institute, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
KR20220070066A (en) 2014-03-14 2022-05-27 아지오스 파마슈티컬스 아이엔씨. Pharmaceutical compositions of therapeutically active compounds
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US9498467B2 (en) 2014-05-30 2016-11-22 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
AU2015337091B2 (en) 2014-10-24 2018-11-22 Nimmune 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)
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
SI3307271T1 (en) 2015-06-11 2023-11-30 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP7028766B2 (en) 2015-09-09 2022-03-02 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
US10653710B2 (en) 2015-10-15 2020-05-19 Agios Pharmaceuticals, Inc. Combination therapy for treating malignancies
PT3362065T (en) 2015-10-15 2024-06-21 Servier Lab COMBINATION THERAPY COMPRISING IVOSIDENIB, CYTARABINE AND DAUNORUBICIN OR IDARUBICIN FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA
JOP20190055A1 (en) 2016-09-26 2019-03-24 Merck Sharp & Dohme Anti-cd27 antibodies
WO2018071283A1 (en) 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
CA3058134A1 (en) 2017-04-13 2018-10-18 Aduro Biotech Holdings, Europe B.V. Anti-sirp alpha antibodies
CN117100751A (en) 2017-06-20 2023-11-24 安布里亚制药公司 Compositions and methods for improving cardiometabolic efficiency
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
AR113922A1 (en) 2017-12-08 2020-07-01 Incyte Corp LOW DOSE COMBINATION THERAPY FOR THE TREATMENT OF MYELOPROLIFERATIVE NEOPLASMS
WO2019152374A1 (en) 2018-01-30 2019-08-08 Incyte Corporation Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
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
HUE067471T2 (en) 2018-03-30 2024-10-28 Incyte Corp Treatment of hidradenitis suppurativa using jak inhibitors
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE KINA INHIBITORS AND THEIR USES
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
AU2019317549A1 (en) 2018-08-07 2021-02-25 Msd International Gmbh PRMT5 inhibitors
EP3833667B1 (en) 2018-08-07 2024-03-13 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)
EP3866794B1 (en) 2018-10-17 2024-12-04 Imbria Pharmaceuticals, Inc. Methods of treating rheumatic diseases using trimetazidine-based compounds
US10793554B2 (en) 2018-10-29 2020-10-06 Forma Therapeutics, Inc. Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone
AU2019413694B2 (en) 2018-12-28 2025-03-20 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
WO2021126729A1 (en) 2019-12-17 2021-06-24 Merck Sharp & Dohme Corp. Prmt5 inhibitors
BR112022002387A2 (en) 2019-12-20 2022-09-06 Landos Biopharma Inc COMPOUND OF FORMULA Z-Y-Q-Y' OR A PHARMACEUTICALLY ACCEPTABLE SALT OR ESTER THEREOF
US12234578B2 (en) 2020-01-29 2025-02-25 Wisconsin Alumni Research Foundation Tannin composite fibers
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
IL322769A (en) 2023-03-02 2025-10-01 Carcimun Biotech Gmbh Means and methods for diagnosing cancer and/or an acute inflammatory disease

Family Cites Families (6)

* 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
US5182141A (en) 1990-02-13 1993-01-26 Co-Ex-Tec Industries Bilaminate polymer coated metal strip and method for manufacture thereof
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

Also Published As

Publication number Publication date
HRP960143A2 (en) 1998-04-30
EP0820445A1 (en) 1998-01-28
NO974457L (en) 1997-11-28
EE9700314A (en) 1998-06-15
IL117580A0 (en) 1996-07-23
HUP9801883A2 (en) 1999-06-28
PL322549A1 (en) 1998-02-02
IS4568A (en) 1997-09-24
CN1195340A (en) 1998-10-07
CZ306297A3 (en) 1998-03-18
WO1996030343A1 (en) 1996-10-03
AU5322396A (en) 1996-10-16
JP3043815B2 (en) 2000-05-22
SK129297A3 (en) 1998-05-06
JPH10511098A (en) 1998-10-27
AR002726A1 (en) 1998-04-29
HUP9801883A3 (en) 2000-09-28
BR9607953A (en) 1998-07-14
CA2216707A1 (en) 1996-10-03
NO974457D0 (en) 1997-09-26
AU710672B2 (en) 1999-09-23
NZ305254A (en) 1999-03-29
BG101973A (en) 1998-05-29
TR199701056T1 (en) 1998-02-21

Similar Documents

Publication Publication Date Title
MX9707459A (en) Inhibitors of farnesyl-protein transferase.
GR3030445T3 (en) Inhibitors of farnesyl-protein transferase.
HU9501238D0 (en) Inhibitors of farnesyl-protein transferase
WO1997038665A3 (en) Inhibitors of farnesyl-protein transferase
NO951647L (en) Inhibitors for farnesyl protein transferase
YU19296A (en) Inhibitors of farnesyl-protein transferase
MX9705273A (en) Inhibitors of prenyl transferases.
WO2000034437A3 (en) Inhibitors of prenyl-protein transferase
MY117961A (en) Inhibitors of farnesyl protein transferase
EP0664789A4 (en) Inhibitors of farnesyl protein transferase.
NZ330287A (en) Substituted 1,4-benzodiazepine inhibitors of farnesyl protein transferase
EP0820287A4 (en) THROMBINE INHIBITORS
EP0772590A1 (en) Thrombin inhibitors
FR2787327B1 (en) COMPOSITIONS CONTAINING FARNESYL TRANSFERASE INHIBITORS
EP0730467A4 (en) Inhibitors of farnesyl-protein transferase
EP0547669A3 (en) Inhibitors of farnesyl protein transferase
HUP0000073A3 (en) Substituted benzocycloheptapyridine useful as inhibitors of farnesyl-protein transferase
EP0547670A3 (en) Inhibitors of farnesyl protein transferase
EP0547672A3 (en) Inhibitors of farnesyl protein transferase
WO2002060868A3 (en) Inhibitors of prenyl-protein transferase
WO2000034239A3 (en) Inhibitors of prenyl-protein transferase
WO2002079147A3 (en) Inhibitors of prenyl-protein transferase
EP0547671A3 (en) Inhibitors of farnesyl protein transferase
CA2154871A1 (en) Farnesyl:protein transferase inhibitors as anticancer agents
GB9223246D0 (en) Inhibitors of farnesyl protein transferase