CZ306297A3 - Piperazinové sloučeniny a farmaceutické prostředky s jejich obsahem - Google Patents

Piperazinové sloučeniny a farmaceutické prostředky s jejich obsahem Download PDF

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Publication number
CZ306297A3
CZ306297A3 CZ973062A CZ306297A CZ306297A3 CZ 306297 A3 CZ306297 A3 CZ 306297A3 CZ 973062 A CZ973062 A CZ 973062A CZ 306297 A CZ306297 A CZ 306297A CZ 306297 A3 CZ306297 A3 CZ 306297A3
Authority
CZ
Czechia
Prior art keywords
carbon atoms
aryl
alkyl
group
heterocyclic radical
Prior art date
Application number
CZ973062A
Other languages
Czech (cs)
English (en)
Inventor
Neville J. Anthony
Terrence M. Ciccarone
Robert P. Gomez
John H. Hutchinson
Theresa M. Williams
Christopher J. Dinsmore
Gerald E. Stokker
George D. Hartman
Original Assignee
Merck And 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 And Co., Inc. filed Critical Merck And Co., Inc.
Publication of CZ306297A3 publication Critical patent/CZ306297A3/cs

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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)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
CZ973062A 1995-03-29 1996-03-25 Piperazinové sloučeniny a farmaceutické prostředky s jejich obsahem CZ306297A3 (cs)

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
CZ306297A3 true CZ306297A3 (cs) 1998-03-18

Family

ID=27410959

Family Applications (1)

Application Number Title Priority Date Filing Date
CZ973062A CZ306297A3 (cs) 1995-03-29 1996-03-25 Piperazinové sloučeniny a farmaceutické prostředky s jejich obsahem

Country Status (21)

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

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
US5869682A (en) * 1996-04-03 1999-02-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0900081A4 (en) * 1996-04-03 2002-01-09 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
EP0904080A4 (en) * 1996-04-03 2001-08-01 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
US5780492A (en) * 1996-04-03 1998-07-14 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5939557A (en) * 1996-04-03 1999-08-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6001835A (en) * 1996-04-03 1999-12-14 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000507584A (ja) * 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 ファルネシル―タンパク質転移酵素の阻害剤
WO1997036587A1 (en) * 1996-04-03 1997-10-09 Merck & Co., Inc. A method of treating cancer
US5919785A (en) * 1996-04-03 1999-07-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5859012A (en) * 1996-04-03 1999-01-12 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5891889A (en) * 1996-04-03 1999-04-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU715202B2 (en) * 1996-04-03 2000-01-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6063930A (en) * 1996-04-03 2000-05-16 Merck & Co., Inc. Substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
US5852010A (en) * 1996-04-03 1998-12-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000507589A (ja) * 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 ファルネシル―タンパク質転移酵素の阻害剤
US5780488A (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
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
US5922883A (en) * 1996-04-03 1999-07-13 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
EP0891353A4 (en) * 1996-04-03 2001-08-08 Merck & Co Inc FARNESYL PROTEIN TRANSFERASE INHIBITORS
US5885995A (en) * 1996-04-03 1999-03-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
BR9711135A (pt) * 1996-08-14 1999-08-17 Zeneca Ltd Composto composi-Æo farmac-utica utiliza-Æo de um composto e processos para prepara-Æo de um composto e para inibi-Æo de Äxido-equaleno ciclase num animal de sangue quente requerendo um tal tratamento
UA56197C2 (uk) 1996-11-08 2003-05-15 Зенека Лімітед Гетероциклічні похідні
JP2002511054A (ja) * 1996-12-30 2002-04-09 メルク エンド カンパニー インコーポレーテッド ファルネシル蛋白トランスフェラーゼ阻害薬
US6440972B1 (en) 1997-02-13 2002-08-27 Zeneca Limited Heterocyclic compounds useful as oxido-squalene cyclase inhibitors
DK0966462T3 (da) 1997-02-13 2003-09-22 Astrazeneca Ab Heterocykliske forbindelser, der er egnede som oxidosqualencyklaseinhibitorer
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
WO1999010525A1 (en) * 1997-08-27 1999-03-04 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
FR2774985A1 (fr) * 1998-02-13 1999-08-20 Rhone Poulenc Rorer Sa Nouveaux derives de naphthyl disubstitues, leur preparation, les compositions pharmaceutiques qui les contiennent et leur utilisation pour la preparation de medicaments
WO1999041242A1 (fr) * 1998-02-13 1999-08-19 Rhone-Poulenc Rorer S.A. Derives de naphtyl disubstitues, leur preparation, les compositions pharmaceutiques qui les contiennent
WO2000001691A1 (en) * 1998-07-01 2000-01-13 Merck & Co., Inc. Process for making farnesyl-protein transferase inhibitors
GB9902989D0 (en) 1999-02-11 1999-03-31 Zeneca Ltd Heterocyclic derivatives
CA2362493A1 (en) * 1999-03-03 2000-09-08 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
JP2002538120A (ja) * 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 プレニルタンパク質トランスフェラーゼの阻害剤
CA2363169A1 (en) * 1999-03-03 2000-09-08 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
JP2002542155A (ja) * 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 プレニル蛋白トランスフェラーゼの阻害剤
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 (fr) * 2001-01-18 2003-02-21 Servier Lab Nouveaux composes cyclo[d] azepane, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
FR2819509B1 (fr) 2001-01-18 2004-04-16 Servier Lab Nouveaux composes cycloheptene, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
FR2819510B1 (fr) * 2001-01-18 2003-10-31 Servier Lab Nouveaux composes cyclo[c] azepane, leur procede de preparation et les compositions pharmaceutiques qui le contiennent
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
JP2009508835A (ja) 2005-09-16 2009-03-05 アロー セラピューティクス リミテッド ビフェニル誘導体及びｃ型肝炎の治療におけるその使用
LT2474545T (lt) 2005-12-13 2017-02-27 Incyte Holdings Corporation Heteroarilu pakeisti pirolo[2,3-b]piridinai ir pirolo[2,3-b]pirimidinai kaip janus kinazės inhibitoriai
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
CA2672269A1 (en) * 2006-12-18 2008-06-26 Novartis Ag Organic compounds
SI2805945T1 (sl) 2007-01-10 2019-09-30 Msd Italia S.R.L. Amid substituirani indazoli, kot inhibitorji poli(ADP-riboza)polimeraze(PARP)
MX2009009304A (es) 2007-03-01 2009-11-18 Novartis Ag Inhibidores de cinasa pim y metodos para su uso.
BRPI0812159A2 (pt) 2007-05-21 2017-05-02 Novartis Ag inibidores de csf-1r, composições e métodos de uso
LT3070090T (lt) 2007-06-13 2019-06-25 Incyte Holdings Corporation Janus kinazės inhibitoriaus (r)-3-(4-(7h-pirol[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrilo druskų panaudojimas
WO2009002495A1 (en) 2007-06-27 2008-12-31 Merck & Co., Inc. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
RU2014151622A (ru) 2007-10-05 2015-08-20 Акусела Инк. Композиции и способы лечения нейродегенеративных заболеваний
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
GB0813142D0 (en) 2008-07-17 2008-08-27 Glaxo Group Ltd Novel compounds
GB0813144D0 (en) 2008-07-17 2008-08-27 Glaxo Group Ltd Novel compounds
ES2740424T3 (es) 2009-03-13 2020-02-05 Agios Pharmaceuticals Inc Métodos y composiciones para trastornos relacionados con la proliferación celular
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
CN102448951B (zh) 2009-04-06 2017-05-10 安吉奥斯医药品有限公司 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法
JP5775070B2 (ja) 2009-05-22 2015-09-09 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体
MY161416A (en) 2009-05-22 2017-04-14 Incyte Holdings Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4yl)-1h-pyrazol-1-yl]octane-or heptane-nitrile as jak inhibitors
WO2010144909A1 (en) 2009-06-12 2010-12-16 Novartis Ag Fused heterocyclic compounds and their uses
SG177434A1 (en) 2009-06-29 2012-02-28 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
ES2897527T3 (es) 2009-07-02 2022-03-01 Acucela Inc Farmacología de moduladores del ciclo visual
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
WO2011046771A1 (en) 2009-10-14 2011-04-21 Schering Corporation 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
AR081315A1 (es) 2010-03-10 2012-08-08 Incyte Corp Derivados heterociclicos de piperidin y pirimidin -4-il-azetidina, una forma cristalina de la sal del acido acetonitriladipico de un derivado pirimidinico, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades relacionadas con la inhibicion de jak-1, t
BR112012023021A2 (pt) 2010-03-16 2016-05-31 Dana Farber Cancer Inst Inc compostos de indazol e seus usos
ME02445B (me) 2010-05-21 2016-09-20 Incyte Holdings Corp Topikalna formulacija za inhibiciju jak-a
EP2584903B1 (en) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Novel 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)
EP3587574B1 (en) 2010-08-17 2022-03-16 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
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
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
AR083933A1 (es) 2010-11-19 2013-04-10 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
CA2821975A1 (en) 2010-12-17 2012-06-21 Shunqi Yan N-(4-(azetidine-1-carbonyl)phenyl)-(hetero-) arylsulfonamide derivatives as pyruvate kinase m2 pkm2 modulators
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
ES2569712T3 (es) 2010-12-21 2016-05-12 Agios Pharmaceuticals, Inc. Activadores de PKM2 bicíclicos
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
WO2012145471A1 (en) 2011-04-21 2012-10-26 Merck Sharp & Dohme Corp. Insulin-like growth factor-1 receptor inhibitors
PT2704721T (pt) 2011-05-03 2018-06-14 Agios Pharmaceuticals Inc Ativadores da piruvato-cinase para utilização em terapia
WO2012151452A1 (en) 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc Pyruvate kinase activators for use in therapy
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
PE20140832A1 (es) 2011-06-20 2014-07-14 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
JP6106685B2 (ja) 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 Ｃ−ｊｕｎ−ｎ−末端キナーゼ（ｊｎｋ）の阻害剤
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
CN104379563B (zh) * 2012-04-10 2018-12-21 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
EP3919620A1 (en) 2012-05-02 2021-12-08 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
WO2014063068A1 (en) 2012-10-18 2014-04-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
CA3178452A1 (en) 2012-11-15 2014-05-22 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
PL2925888T3 (pl) 2012-11-28 2018-03-30 Merck Sharp & Dohme Corp. Kompozycje i sposoby do stosowania w leczeniu nowotworów
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
LT3489239T (lt) 2013-03-06 2022-03-10 Incyte Holdings Corporation Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai
ME03564B (me) 2013-03-13 2020-07-20 Forma Therapeutics Inc DERIVATI 2-HIDROKSI-1-{4-[(4-FENILFENIL)KARBONIL]PIPERAZIN-1-IL}ETAN-1-ONA l SRODNA JEDINJENJA KAO INHIBITORI SINTAZE MASNIH KISELINA (FASN) ZA LEČENJE KANCERA
CN105593215B (zh) 2013-07-11 2019-01-15 安吉奥斯医药品有限公司 用于治疗癌症的作为idh2突变体抑制剂的2,4-或4,6-二氨基嘧啶化合物
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
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
MY195091A (en) 2013-08-07 2023-01-10 Incyte Corp Sustained Release Dosage Forms for a JAK1 Inhibitor
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
AU2015229214B2 (en) 2014-03-14 2019-07-11 Les Laboratoires Servier Pharmaceutical compositions of therapeutically active compounds
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US9862688B2 (en) 2014-04-23 2018-01-09 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 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
KR102026342B1 (ko) 2014-10-24 2019-09-27 란도스 바이오파마, 인크. 란티오닌 합성효소 c-유사 2-계 치료제
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
JP6861166B2 (ja) 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 サイクリン依存性キナーゼの阻害剤
WO2016201227A1 (en) 2015-06-11 2016-12-15 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. ASSOCIATION THERAPY USING TRANSCRIPTION INHIBITORS AND KINASE INHIBITORS
JP7028766B2 (ja) 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 サイクリン依存性キナーゼの阻害剤
HRP20211790T1 (hr) 2015-10-15 2022-03-04 Les Laboratoires Servier Kombinirana terapija za liječenje maligniteta
BR112018007671B1 (pt) 2015-10-15 2023-10-17 Les Laboratoires Servier Usos de um inibidor da idh1 e combinações
JOP20190055A1 (ar) 2016-09-26 2019-03-24 Merck Sharp & Dohme أجسام مضادة ضد cd27
AU2018252546A1 (en) 2017-04-13 2019-10-10 Sairopa B.V. Anti-SIRPα antibodies
EP4092013A1 (en) 2017-06-20 2022-11-23 Imbria Pharmaceuticals, Inc. Compositions and methods for increasing efficiency of cardiac metabolism
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for 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 (zh) * 2018-03-22 2022-08-02 西华大学 一种咪唑甲胺类衍生物的制备方法
MX2020010322A (es) 2018-03-30 2022-11-30 Incyte Corp Tratamiento de la hidradenitis supurativa mediante el uso de inhibidores de actividad de la cinasa janus (jak).
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
US11993602B2 (en) 2018-08-07 2024-05-28 Merck Sharp & Dohme Llc PRMT5 inhibitors
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
CN113382633A (zh) 2018-10-29 2021-09-10 福马治疗股份有限公司 (4-(2-氟-4-(1-甲基-1H-苯并[d]咪唑-5-基)苯甲酰基)哌嗪-1-基)(1-羟基环丙基)甲酮的固体形式
BR112022002387A2 (pt) 2019-12-20 2022-09-06 Landos Biopharma Inc Composto da fórmula z-y-q-y' ou um sal ou éster farmaceuticamente aceitável do mesmo
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 (it) * 1974-03-01 1982-01-30 Malesci Sas Inst Farmaco Bilog Derivati eterocicli della 4 fenil riperazina i alchil sostituita ad azione farmacologica e relativo procedimento di preparazione
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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