HUP9801883A3 - Piperazine-derivatives for inhibiting of farnesyl-protein transferase, preparation and use thereof, pharmaceutical compositions containing these compounds - Google Patents

Piperazine-derivatives for inhibiting of farnesyl-protein transferase, preparation and use thereof, pharmaceutical compositions containing these compounds

Info

Publication number
HUP9801883A3
HUP9801883A3 HU9801883A HUP9801883A HUP9801883A3 HU P9801883 A3 HUP9801883 A3 HU P9801883A3 HU 9801883 A HU9801883 A HU 9801883A HU P9801883 A HUP9801883 A HU P9801883A HU P9801883 A3 HUP9801883 A3 HU P9801883A3
Authority
HU
Hungary
Prior art keywords
farnesyl
piperazine
inhibiting
derivatives
compounds
Prior art date
Application number
HU9801883A
Other languages
Hungarian (hu)
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 HUP9801883A2 publication Critical patent/HUP9801883A2/en
Publication of HUP9801883A3 publication Critical patent/HUP9801883A3/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
HU9801883A 1995-03-29 1996-03-25 Piperazine-derivatives for inhibiting of farnesyl-protein transferase, preparation and use thereof, pharmaceutical compositions containing these compounds HUP9801883A3 (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 (2)

Publication Number Publication Date
HUP9801883A2 HUP9801883A2 (en) 1999-06-28
HUP9801883A3 true HUP9801883A3 (en) 2000-09-28

Family

ID=27410959

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9801883A HUP9801883A3 (en) 1995-03-29 1996-03-25 Piperazine-derivatives for inhibiting of farnesyl-protein transferase, preparation and use thereof, pharmaceutical compositions containing these compounds

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 (163)

* 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
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
AU707416B2 (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
US6080870A (en) * 1996-04-03 2000-06-27 Merck & Co., Inc. Biaryl 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
WO1997036592A1 (en) * 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5922883A (en) * 1996-04-03 1999-07-13 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
US5919785A (en) * 1996-04-03 1999-07-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU715202B2 (en) * 1996-04-03 2000-01-20 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
US5859012A (en) * 1996-04-03 1999-01-12 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2250192A1 (en) * 1996-04-03 1997-10-09 Chrisopher J. Dinsmore Inhibitors of farnesyl-protein transferase
JP2000504023A (en) * 1996-04-03 2000-04-04 メルク エンド カンパニー インコーポレーテッド Cancer treatment methods
US5939557A (en) * 1996-04-03 1999-08-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5925651A (en) * 1996-04-03 1999-07-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5885995A (en) * 1996-04-03 1999-03-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5780492A (en) * 1996-04-03 1998-07-14 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU707347B2 (en) * 1996-04-03 1999-07-08 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5869682A (en) * 1996-04-03 1999-02-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5883105A (en) * 1996-04-03 1999-03-16 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5852010A (en) * 1996-04-03 1998-12-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
TR199900303T2 (en) * 1996-08-14 1999-06-21 Zeneca Limited 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
JP2001511798A (en) 1997-02-13 2001-08-14 ゼネカ・リミテッド Heterocyclic compounds useful as oxide-squalene cyclase inhibitors
EP0966462B1 (en) 1997-02-13 2003-06-11 AstraZeneca AB 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
EP1019529A4 (en) * 1997-08-27 2002-09-11 Merck & Co Inc A method of treating cancer
US6387903B1 (en) 1997-08-27 2002-05-14 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
US6103487A (en) * 1997-08-27 2000-08-15 Merck & Co., Inc. Method of treating cancer
WO1999041242A1 (en) * 1998-02-13 1999-08-19 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
EP1165082A4 (en) * 1999-03-03 2002-06-12 Merck & Co Inc Inhibitors of prenyl-protein transferase
US6335343B1 (en) * 1999-03-03 2002-01-01 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
WO2000051612A1 (en) * 1999-03-03 2000-09-08 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
EP1158982A4 (en) * 1999-03-03 2002-06-12 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
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
FR2819512B1 (en) * 2001-01-18 2003-02-21 Servier Lab NOVEL CYCLO [D] AZEPANE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
US8362075B2 (en) 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
JP2009508835A (en) 2005-09-16 2009-03-05 アロー セラピューティクス リミテッド Biphenyl derivatives and their use in the treatment of hepatitis C
DK2455382T3 (en) 2005-12-13 2017-01-02 Incyte Holdings Corp Heteroberl 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
WO2008039327A2 (en) 2006-09-22 2008-04-03 Merck & Co., Inc. 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
AU2007334416A1 (en) * 2006-12-18 2008-06-26 Novartis Ag Imidazoles as aldosterone synthase inhibitors
PL2336120T3 (en) 2007-01-10 2014-12-31 Msd Italia Srl Combinations containing amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors
MX2009009304A (en) 2007-03-01 2009-11-18 Novartis Ag Pim kinase inhibitors and methods of their use.
CA2685967A1 (en) 2007-05-21 2008-11-21 Novartis Ag Csf-1r inhibitors, compositions, and methods of use
PT3070090T (en) 2007-06-13 2019-03-20 Incyte Holdings Corp Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
CA2690191C (en) 2007-06-27 2015-07-28 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
US7982071B2 (en) 2007-10-05 2011-07-19 Acucela Inc. Alkoxy compounds for disease treatment
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
CN102985557B (en) 2009-03-13 2018-06-15 安吉奥斯医药品有限公司 For the method and composition of cell Proliferation associated disease
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 Therapeutic compositions and related methods of use
NZ596479A (en) 2009-05-22 2014-01-31 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
CA2761954C (en) 2009-05-22 2018-07-31 Incyte Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
US8765747B2 (en) 2009-06-12 2014-07-01 Dana-Farber Cancer Institute, Inc. Fused 2-aminothiazole compounds
NZ622505A (en) 2009-06-29 2015-12-24 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
EP2448569B1 (en) 2009-07-02 2021-10-27 Acucela, Inc. Pharmacology of visual cycle modulators
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
PE20121172A1 (en) 2009-10-14 2012-09-05 Merck Sharp & Dohme PIPERIDINS SUBSTITUTED WITH ACTIVITY IN HDM2
EP2491145B1 (en) 2009-10-21 2016-03-09 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
SG183551A1 (en) 2010-03-10 2012-10-30 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
BR112012023021A2 (en) 2010-03-16 2016-05-31 Dana Farber Cancer Inst Inc indazole compounds and their uses
SG185567A1 (en) 2010-05-21 2012-12-28 Incyte Corp Topical formulation for a jak inhibitor
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CA2805265A1 (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)
CA2807307C (en) 2010-08-17 2021-02-09 Merck Sharp & Dohme Corp. 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
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. 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
EP2632472B1 (en) 2010-10-29 2017-12-13 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acids (sina)
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
UA113156C2 (en) 2010-11-19 2016-12-26 CYCLOBUTYL-SUBSTITUTED PYROLOPYRIDINE AND PYROLOPYRIMIDINE 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)
JP6092118B2 (en) 2010-12-21 2017-03-08 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 Bicyclic PKM2 activator
US9351965B2 (en) 2010-12-21 2016-05-31 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
IN2013MN02170A (en) 2011-04-21 2015-06-12 Piramal Entpr Ltd
CN103764147B (en) 2011-05-03 2018-05-22 安吉奥斯医药品有限公司 For the pyruvate kinase activator for the treatment of
CA2834692A1 (en) 2011-05-03 2012-11-08 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
JP5876146B2 (en) 2011-06-20 2016-03-02 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Azetidinylphenyl, pyridyl, or pyrazinylcarboxamide 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
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP3569598A1 (en) 2011-11-17 2019-11-20 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
JP6399660B2 (en) * 2012-04-10 2018-10-03 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア Cancer treatment compositions and methods
EP2844261B1 (en) 2012-05-02 2018-10-17 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
TW201406761A (en) 2012-05-18 2014-02-16 Incyte Corp Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 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
EP2919766B1 (en) 2012-11-15 2021-05-26 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
MX363243B (en) 2012-11-28 2019-03-14 Merck Sharp & Dohme Compositions and methods for treating cancer.
BR112015013611A2 (en) 2012-12-20 2017-11-14 Merck Sharp & Dohme compound and pharmaceutical composition
EP2951180B1 (en) 2013-01-30 2018-05-02 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
UA121532C2 (en) 2013-03-06 2020-06-10 Інсайт Холдінгс Корпорейшн METHODS AND INTERMEDIATES IN THE PREPARATION OF JAK INHIBITOR
ES2861180T3 (en) 2013-03-13 2021-10-05 Forma Therapeutics Inc Derivatives of 2-hydroxy-1- {4 - [(4-phenyl) phenyl] carbonyl} piperazin-1-yl} ethan-1-one and related compounds such as fatty acid synthase inhibitors (FASN) for the treatment of cancer
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
CN105593215B (en) 2013-07-11 2019-01-15 安吉奥斯医药品有限公司 2,4- the or 4,6- diaminopyrimidine compounds as IDH2 mutant inhibitor for treating cancer
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
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
US9655854B2 (en) 2013-08-07 2017-05-23 Incyte Corporation Sustained release dosage forms for a JAK1 inhibitor
EP3041938A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Circular polynucleotides
ES2676734T3 (en) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Heteroatomic compounds useful for the treatment of proliferative diseases
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
EA036325B1 (en) 2014-03-14 2020-10-27 Аджиос Фармасьютикалз, Инк. Pharmaceutical composition comprising solid dispersion of idh1 inhibitor
US10017477B2 (en) 2014-04-23 2018-07-10 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
RU2688677C2 (en) 2014-10-24 2019-05-22 Лэндос Байофарма, Инк. Drug preparations based on lanthionine synthetase of c-like protein
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)
JP6861166B2 (en) 2015-03-27 2021-04-21 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
WO2016201227A1 (en) 2015-06-11 2016-12-15 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
CA2996978A1 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
KR20180061372A (en) 2015-10-15 2018-06-07 아지오스 파마슈티컬스 아이엔씨. Combination Therapy for the Treatment of Malignant Tumors
LT3362066T (en) 2015-10-15 2022-02-10 Les Laboratoires Servier Sas Combination therapy for treating malignancies
JOP20190055A1 (en) 2016-09-26 2019-03-24 Merck Sharp & Dohme Anti-cd27 antibodies
MX2019012233A (en) 2017-04-13 2020-01-14 Aduro Biotech Holdings Europe Bv Anti-sirp alpha antibodies.
EP3641769B1 (en) 2017-06-20 2022-06-08 Imbria Pharmaceuticals, Inc. 1-[(2,3,4-trimethoxyphenyl)methyl]-piperazine derivative, compositions thereof and methods for increasing efficiency of cardiac metabolism
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
CR20200379A (en) 2018-01-30 2021-03-05 Incyte Corp 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 Preparation method of imidazole methylamine derivative
IL302865A (en) 2018-03-30 2023-07-01 Incyte Corp Treatment of hidradenitis suppurativa using jak inhibitors
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US20210277009A1 (en) 2018-08-07 2021-09-09 Merck Sharp & Dohme Corp. Prmt5 inhibitors
TWI767148B (en) 2018-10-10 2022-06-11 美商弗瑪治療公司 Inhibiting fatty acid synthase (fasn)
CN113382633A (en) 2018-10-29 2021-09-10 福马治疗股份有限公司 Solid forms of (4- (2-fluoro-4- (1-methyl-1H-benzo [ d ] imidazol-5-yl) benzoyl) piperazin-1-yl) (1-hydroxycyclopropyl) methanone
WO2021127472A1 (en) 2019-12-20 2021-06-24 Landos 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

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
EP0703905A1 (en) * 1993-06-18 1996-04-03 Merck & Co. Inc. 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
TR199701056T1 (en) 1998-02-21
EE9700314A (en) 1998-06-15
CA2216707A1 (en) 1996-10-03
SK129297A3 (en) 1998-05-06
IS4568A (en) 1997-09-24
AU5322396A (en) 1996-10-16
HUP9801883A2 (en) 1999-06-28
WO1996030343A1 (en) 1996-10-03
CZ306297A3 (en) 1998-03-18
AU710672B2 (en) 1999-09-23
NO974457D0 (en) 1997-09-26
IL117580A0 (en) 1996-07-23
NZ305254A (en) 1999-03-29
CN1195340A (en) 1998-10-07
BG101973A (en) 1998-05-29
JPH10511098A (en) 1998-10-27
MX9707459A (en) 1997-12-31
HRP960143A2 (en) 1998-04-30
JP3043815B2 (en) 2000-05-22
BR9607953A (en) 1998-07-14
AR002726A1 (en) 1998-04-29
PL322549A1 (en) 1998-02-02
EP0820445A1 (en) 1998-01-28
NO974457L (en) 1997-11-28

Similar Documents

Publication Publication Date Title
HUP9801883A3 (en) Piperazine-derivatives for inhibiting of farnesyl-protein transferase, preparation and use thereof, pharmaceutical compositions containing these compounds
HUP9901159A3 (en) Substituted benzylaminopiperidine derivatives and use thereof, pharmaceutical compositions containing these compounds
HUP0001607A3 (en) Thienopyrimidine derivatives, pharmaceutical compositions containing them, process for their preparation and use of the compounds
HUP9901037A3 (en) Piperazine derivatives,preparation and use thereof, pharmaceutical compositions containing these compounds
SI1156049T1 (en) Substituted heterocyclic compounds, their process of preparation and pharmaceutical compositions containing them
AU4543696A (en) Novel farnesyl transferase inhibitors, preparation thereof and pharmaceutical compositions containing same
AU4722796A (en) Novel farnesyl transferase inhibitors, preparation thereof, and pharmaceutical compositions containing same
AU4722896A (en) Novel farnesyl transferase inhibitors, preparation thereof, and pharmaceutical compositions containing same
HUP0001498A3 (en) Farnesyl transferase inhibiting 1,8-annelated imidazolyl-quinolinone derivatives, their intermediates, pharmaceutical compositions thereof and process for their preparation
AU6523396A (en) Novel farnesyl transferase inhibitors, preparation thereof and pharmaceutical compositions containing said inhibitors
HUP9901243A3 (en) Quinazoline derivatives, preparation and use thereof, pharmaceutical compositions containing these compounds
EP0811595A4 (en) Hydrochalcone derivatives, comestic compositions containing the same, and processes for the preparation of both
IL118369A0 (en) Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same
HRP960558B1 (en) New crystalline modifications of cdch, processes for the preparation thereof and pharmaceutical compositions containing them
HUP0002037A3 (en) Hydroximic acid derivatives, use of them for producing pharmaceutical compositions suitable for inhibiting matrix metalloproteinas and pharmaceutical compositions containing the compounds
HUP9701194A3 (en) 4-hydroxy-piperidine derivatives, preparation and use thereof, pharmaceutical compositions containing these compounds
IL123094A0 (en) Pharmaceutical compositions containing griseofulvin for inhibiting the growth of cancers
IL112443A0 (en) Heterocyclic compounds, their preparation and pharmaceutical compositions containing them
HUP9901326A3 (en) Benzopyran derivatives having leukotriene-antagonistic action, pharmaceutical compositions containing these compounds, process for the preparation and use of these compounds and compositions
IL117620A0 (en) Heterocyclic compounds processes for the preparation thereof and pharmaceutical compositions containing the same
HUP9801993A3 (en) Ascomycin derivatives and their use for preparation of pharmaceutical compositions, process for their preparation and pharmaceutical compositions containing them
HUP9801386A3 (en) Indazolecarboxamide derivatives, preparation thereof and pharmaceutical compositions containing them
IL117817A0 (en) N-subsituted azaheterocyclic compounds their preparation and pharmaceutical compositions containing them
CZ346595A3 (en) Substituted derivatives of 4-phenylthiazoles, process of their preparation and pharmaceutical compositions containing thereof
HUP9601680A3 (en) Benzisothiazolyl-substituted aminomethyl-chromanes, pharmaceutical compositions containing the same, process for their preparation and use of the compounds