[go: up one dir, main page]

WO2002000651A3 - Factor xa inhibitors - Google Patents

Factor xa inhibitors Download PDF

Info

Publication number
WO2002000651A3
WO2002000651A3 PCT/US2001/020538 US0120538W WO0200651A3 WO 2002000651 A3 WO2002000651 A3 WO 2002000651A3 US 0120538 W US0120538 W US 0120538W WO 0200651 A3 WO0200651 A3 WO 0200651A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
factor
same
trypsin
prevention
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2001/020538
Other languages
French (fr)
Other versions
WO2002000651A2 (en
Inventor
Mimi L Quan
Patrick Y Lam
Yunlong Li
Donald J P Pinto
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Pharma Co
Original Assignee
Bristol Myers Squibb Pharma Co
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
Application filed by Bristol Myers Squibb Pharma Co filed Critical Bristol Myers Squibb Pharma Co
Priority to AU2001273040A priority Critical patent/AU2001273040A1/en
Publication of WO2002000651A2 publication Critical patent/WO2002000651A2/en
Publication of WO2002000651A3 publication Critical patent/WO2002000651A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

This invention relates generally to compounds of formula (Ia) or (Ia) (Ib) that are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
PCT/US2001/020538 2000-06-27 2001-06-27 Factor xa inhibitors Ceased WO2002000651A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2001273040A AU2001273040A1 (en) 2000-06-27 2001-06-27 Factor xa inhibitors

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US21475800P 2000-06-27 2000-06-27
US60/214,758 2000-06-27
US24612400P 2000-11-06 2000-11-06
US60/246,124 2000-11-06

Publications (2)

Publication Number Publication Date
WO2002000651A2 WO2002000651A2 (en) 2002-01-03
WO2002000651A3 true WO2002000651A3 (en) 2002-06-13

Family

ID=26909329

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/020538 Ceased WO2002000651A2 (en) 2000-06-27 2001-06-27 Factor xa inhibitors

Country Status (2)

Country Link
AU (1) AU2001273040A1 (en)
WO (1) WO2002000651A2 (en)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7427616B2 (en) 2002-08-06 2008-09-23 Astrazeneca Ab Condensed pyridines and pyrimidines with tie2 (TEK) activity
US7612094B2 (en) 2002-04-04 2009-11-03 Biogen Idec Ma Inc. Tri-substituted heteroaryls and methods of making and using the same
US8710232B2 (en) 2004-04-22 2014-04-29 Sanofi-Aventis Deutschland Gmbh Imidazole derivatives used as TAFIa inhibitors
US8916554B2 (en) 2002-03-13 2014-12-23 Janssen Pharmaceutica, N.V. Amino-derivatives as novel inhibitors of histone deacetylase
US9150543B2 (en) 2004-07-28 2015-10-06 Janssen Pharmaceutica N. V. Substituted indolyl alkyl amino derivatives as inhibitors of histone deacetylase
US10214519B2 (en) 2016-09-23 2019-02-26 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US10227350B2 (en) 2016-09-23 2019-03-12 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US10479770B2 (en) 2016-09-23 2019-11-19 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US10532051B2 (en) 2014-10-06 2020-01-14 Chemocentryx, Inc. Compositions and methods for treating inflammatory bowel disease using a combination therapy of small molecule inhibitors of C-C chemokine receptor 9 (CCR9) and anti-α4β7 integrin blocking antibodies
US12054477B2 (en) 2021-09-15 2024-08-06 Hua Medicine (Shanghai) Ltd. Prodrug of pyrrolidone derivatives as glucokinase activator

Families Citing this family (146)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
DE60321548D1 (en) 2002-03-13 2008-07-24 Janssen Pharmaceutica Nv CARBONYLAMIN DERIVATIVES AS NEW INHIBITORS OF HISTONE DEACETYLASE
TW200307667A (en) * 2002-05-06 2003-12-16 Bristol Myers Squibb Co Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
CA2486376A1 (en) 2002-05-22 2003-12-04 Amgen Inc. Amino-pyridine, -pyridine and pyridazine derivatives for use as vanilloid receptor ligands for the treatment of pain
US7144888B2 (en) 2002-08-08 2006-12-05 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7358268B2 (en) 2002-12-04 2008-04-15 Sanofi-Aventis Deutschland Gmbh Imidazole derivatives as factor Xa inhibitors
ATE401322T1 (en) * 2002-12-04 2008-08-15 Sanofi Aventis Deutschland IMIDAZOLE DERIVATIVES AS FACTOR XA INHIBITORS
EP1479674A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Imidiazole-derivatives as factor xa inhibitors
UA80171C2 (en) 2002-12-19 2007-08-27 Pfizer Prod Inc Pyrrolopyrimidine derivatives
US7429581B2 (en) 2002-12-23 2008-09-30 Sanofi-Aventis Deutschland Gmbh Pyrazole-derivatives as factor Xa inhibitors
EP1479678A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Pyrazole-derivatives as factor xa inhibitors
EP1581523B1 (en) * 2002-12-23 2009-09-30 Sanofi-Aventis Deutschland GmbH Pyrazole-derivatives as factor xa inhibitors
US7696225B2 (en) 2003-01-06 2010-04-13 Osi Pharmaceuticals, Inc. (2-carboxamido)(3-Amino) thiophene compounds
TWI299664B (en) 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds
EP1479679A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Triazole-derivatives as factor Xa inhibitors
EP1479680A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Azaindole derivatives as Factor Xa inhibitors
US7223780B2 (en) 2003-05-19 2007-05-29 Sanofi-Aventis Deutschland Gmbh Triazole-derivatives as blood clotting enzyme factor Xa inhibitors
US7317027B2 (en) 2003-05-19 2008-01-08 Sanofi-Aventis Deutschland Gmbh Azaindole-derivatives as factor Xa inhibitors
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
CA2532965C (en) 2003-07-22 2013-05-14 Astex Therapeutics Limited 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
SE0302573D0 (en) 2003-09-26 2003-09-26 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
MY139645A (en) 2004-02-11 2009-10-30 Amgen Inc Vanilloid receptor ligands and their use in treatments
EP1745034A1 (en) 2004-02-11 2007-01-24 Amgen Inc. Vanilloid receptor ligands and their use in treatments
EP1568698A1 (en) * 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrole-derivatives as factor Xa inhibitors
ZA200607637B (en) 2004-03-05 2008-05-28 Nissan Chemical Ind Ltd Isoxazoline-substituted benzamide compound and noxious organism control agent
MXPA06013960A (en) 2004-06-18 2007-03-15 Millennium Pharm Inc Factor xa inhibitors.
US7696352B2 (en) 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
SE0401653D0 (en) * 2004-06-24 2004-06-24 Astrazeneca Ab New compounds
CA2573185A1 (en) 2004-07-14 2006-02-23 Ptc Therapeutics, Inc. Methods for treating hepatitis c
US7868037B2 (en) 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7772271B2 (en) 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
CA2578636A1 (en) 2004-07-22 2006-02-23 Ptc Therapeutics, Inc. Thienopyridines for treating hepatitis c
KR20070045226A (en) 2004-08-03 2007-05-02 와이어쓰 Indazole useful for treating cardiovascular disease
ATE545644T1 (en) 2004-09-24 2012-03-15 Astrazeneca Ab BENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME, PRODUCTION THEREOF AND USES THEREOF I
EP1817292B1 (en) 2004-11-16 2015-04-08 Janssen Pharmaceutica NV Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms)
DE102004058062A1 (en) * 2004-12-02 2006-06-08 Bayer Healthcare Ag Cyclic iminocarbamates and their use
DE602005009252D1 (en) 2004-12-08 2008-10-02 Bristol Myers Squibb Co Heterocyclic Compounds as Inhibitors of Factor VIIA
DE102004059219A1 (en) * 2004-12-09 2006-06-14 Bayer Healthcare Ag Pyrazine dicarboxylic acid amides and their use
DE102004061751A1 (en) * 2004-12-22 2006-07-06 Bayer Healthcare Ag Cyanoguanidine-substituted pyrazolines
DE102004061747A1 (en) * 2004-12-22 2006-07-06 Bayer Healthcare Ag Thiophene-substituted pyrazolines
EP1833819A1 (en) 2004-12-30 2007-09-19 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
AR054425A1 (en) 2005-01-21 2007-06-27 Astex Therapeutics Ltd PIPERIDIN ADDITION SALTS 4-IL-ACID AMID 4- (2,6-DICLORO-BENZOILAMINO) 1H-PIRAZOL-3-CARBOXILICO.
JP5475234B2 (en) 2005-01-21 2014-04-16 アステックス・セラピューティクス・リミテッド Pharmaceutical compounds
US20090036435A1 (en) 2005-01-21 2009-02-05 Astex Therapeutics Limited Pharmaceutical Compounds
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
US7301022B2 (en) 2005-02-15 2007-11-27 Amgen Inc. Vanilloid receptor ligands and their use in treatments
NZ560712A (en) 2005-02-17 2010-12-24 Synta Pharmaceuticals Corp (3,4,5-trisubstituted-phenyl)isoxazole combretastin derivatives for the treatment of disorders
EP1757290A1 (en) 2005-08-16 2007-02-28 Zentaris GmbH Novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors
DE102005042583A1 (en) * 2005-09-08 2007-03-15 Bayer Healthcare Ag Iminooxazolidine derivatives and their use
TWI385169B (en) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd Heterocyclic substituted pyridine derivatives and antifungal agent containing same
KR20080080214A (en) * 2005-12-23 2008-09-02 아스트라제네카 아베 Heterocyclic BAA-V Modulators
CN101341130A (en) 2005-12-23 2009-01-07 阿斯利康(瑞典)有限公司 Imidazole derivatives for the treatment of gastrointestinal disorders
CN101384558A (en) 2005-12-23 2009-03-11 阿斯利康(瑞典)有限公司 Gaba-b receptor modulators
PL1984344T3 (en) 2005-12-29 2013-03-29 Lexicon Pharmaceuticals Inc Multicyclic amino acid derivatives and methods of their use
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
DK1979326T3 (en) 2006-01-19 2013-01-07 Janssen Pharmaceutica Nv PYRIDINE AND PYRIMIDINE DERIVATIVES AS INHIBITORS OF HISTONDEACETYLASE
EP2460793A1 (en) 2006-02-03 2012-06-06 Bionomics Limited Substituted Benzofurans, Benzothiophenes, Benzoselenophenes and Indoles And Their Use as Tubulin Polymerisation Inhibitors
TW200745049A (en) 2006-03-23 2007-12-16 Astrazeneca Ab New crystalline forms
TW200808769A (en) 2006-04-18 2008-02-16 Astrazeneca Ab Therapeutic compounds
CN101490036B (en) 2006-05-05 2013-07-17 米伦纽姆医药公司 Factor xa inhibitors
EP2049119A2 (en) 2006-06-29 2009-04-22 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-urea
WO2008024724A1 (en) 2006-08-21 2008-02-28 Genentech, Inc. Aza-benzothiophenyl compounds and methods of use
WO2008059370A2 (en) 2006-11-17 2008-05-22 Pfizer Japan Inc. Substituted bicyclocarboxyamide compounds
UA99270C2 (en) 2006-12-12 2012-08-10 Лексикон Фармасьютикалз, Инк. 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use
SG182961A1 (en) 2007-06-28 2012-08-30 Novartis Ag Kallikrein 7 modulators
US8119809B2 (en) 2007-11-16 2012-02-21 Rigel Pharmaceuticals, Inc. AMPK-activating heterocycloalkyloxy(hetero)aryl carboxamide, sulfonamide and amine compounds and methods for using the same
JP5650540B2 (en) 2007-12-12 2015-01-07 ライジェル ファーマシューティカルズ， インコーポレイテッド Carboxamide, sulfonamide, and amine compounds for metabolic disorders
US8513287B2 (en) 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
AU2009240643B2 (en) 2008-04-23 2014-03-06 Rigel Pharmaceuticals, Inc. Carboxamide compounds for the treatment of metabolic disorders
AR072297A1 (en) 2008-06-27 2010-08-18 Novartis Ag DERIVATIVES OF INDOL-2-IL-PIRIDIN-3-ILO, PHARMACEUTICAL COMPOSITION THAT INCLUDES THEM AND ITS USE IN MEDICINES FOR THE TREATMENT OF DISEASES MEDIATED BY THE SYNTHESIS ALDOSTERONE.
AU2009271019A1 (en) 2008-07-14 2010-01-21 Gilead Sciences, Inc. Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases
WO2010009139A2 (en) 2008-07-14 2010-01-21 Gilead Colorado, Inc. Imidazolyl pyrimidine inhibitor compounds
CA2728228A1 (en) 2008-07-14 2010-01-21 Gilead Sciences, Inc. Oxindolyl inhibitor compounds
CN102123987A (en) 2008-07-28 2011-07-13 吉里德科学公司 Cycloalkylidene and heterocycloalkylidene histone deacetylase inhibitor compounds
US8455499B2 (en) 2008-12-11 2013-06-04 Amira Pharmaceuticals, Inc. Alkyne antagonists of lysophosphatidic acid receptors
GB2466121B (en) 2008-12-15 2010-12-08 Amira Pharmaceuticals Inc Antagonists of lysophosphatidic acid receptors
US9149465B2 (en) 2009-05-18 2015-10-06 Infinity Pharmaceuticals, Inc. Isoxazolines as inhibitors of fatty acid amide hydrolase
US8927551B2 (en) 2009-05-18 2015-01-06 Infinity Pharmaceuticals, Inc. Isoxazolines as inhibitors of fatty acid amide hydrolase
US8765735B2 (en) 2009-05-18 2014-07-01 Infinity Pharmaceuticals, Inc. Isoxazolines as inhibitors of fatty acid amide hydrolase
GB2470833B (en) 2009-06-03 2011-06-01 Amira Pharmaceuticals Inc Polycyclic antagonists of lysophosphatidic acid receptors
CA2764387A1 (en) 2009-06-05 2010-12-09 Link Medicine Corporation Aminopyrrolidinone derivatives and uses thereof
JP2012529514A (en) 2009-06-08 2012-11-22 ギリアード サイエンシーズ， インコーポレイテッド Cycloalkylcarbamate benzamide aniline HDAC inhibitor compound
BRPI1010884A2 (en) 2009-06-08 2016-03-15 Gilead Sciences Inc hdac alkanoylamino benzamide aniline inhibitors compound
JP2013501064A (en) 2009-08-04 2013-01-10 アミラ ファーマシューティカルス，インコーポレーテッド Compounds as lysophosphatidic acid receptor antagonists
GB2474748B (en) 2009-10-01 2011-10-12 Amira Pharmaceuticals Inc Polycyclic compounds as lysophosphatidic acid receptor antagonists
GB2474120B (en) 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists
EP2513094B1 (en) 2009-12-17 2015-12-16 Millennium Pharmaceuticals, Inc. Crystalline salts of a factor xa inhibitor
WO2011075602A1 (en) 2009-12-17 2011-06-23 Millennium Pharmaceuticals, Inc. Methods of preparing factor xa inhibitors and salts thereof
SG10201502484SA (en) 2010-03-30 2015-05-28 Verseon Corp Multisubstituted aromatic compounds as inhibitors of thrombin
US9290485B2 (en) 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
EP2431035A1 (en) 2010-09-16 2012-03-21 Æterna Zentaris GmbH Novel Triazole Derivatives with Improved Receptor Activity and Bioavailability Properties as Ghrelin Antagonists of Growth Hormone Secretagogue Receptors
CN103201269A (en) 2010-11-11 2013-07-10 赛诺菲 Process for the preparation of 3-(6-amino-pyridin-3yl)-2-acrylic acid derivatives
JP2014513077A (en) 2011-04-05 2014-05-29 アミラ ファーマシューティカルス，インコーポレーテッド Compounds based on 3- or 5-biphenyl-4-ylisoxazole useful for the treatment of fibrosis, pain, cancer, and respiratory, allergic, nervous system or cardiovascular disease
AU2012296662A1 (en) 2011-08-15 2014-03-27 Intermune, Inc. Lysophosphatidic acid receptor antagonists
US9056867B2 (en) 2011-09-16 2015-06-16 Novartis Ag N-substituted heterocyclyl carboxamides
US9199975B2 (en) 2011-09-30 2015-12-01 Asana Biosciences, Llc Biaryl imidazole derivatives for regulating CYP17
KR101093102B1 (en) 2011-10-04 2011-12-13 (주)목우연구소 Phenylisoxazolin-based compound having herbicidal activity and use thereof
KR102083693B1 (en) 2012-02-29 2020-03-02 케모센트릭스, 인크. Pyrazol-1-YL Benzene Sulfonamideas CCR9 Antagonists
WO2014007228A1 (en) * 2012-07-03 2014-01-09 小野薬品工業株式会社 Compound having agonistic activity on somatostatin receptor, and use thereof for medical purposes
AU2013348167A1 (en) 2012-11-20 2015-05-28 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of indoleamine 2,3-dioxygenase
CN105102448B (en) 2013-02-28 2018-03-06 百时美施贵宝公司 Phenylpyrazole derivatives as ROCK1 and ROCK2 inhibitor
TW201444798A (en) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors
SG11201506757TA (en) 2013-03-15 2015-09-29 Verseon Corp Halogenopyrazoles as inhibitors of thrombin
US9834542B2 (en) 2013-03-15 2017-12-05 Bristo-Myers Squibb Company LXR modulators
NZ711064A (en) 2013-03-15 2019-06-28 Verseon Corp Pyridone-substituted pyrazolyl compounds as serine protease inhibitors
AU2014352875B2 (en) 2013-11-22 2019-10-24 CL BioSciences LLC Gastrin antagonists (eg YF476, netazepide) for treatment and prevention of osteoporosis
WO2015089800A1 (en) 2013-12-19 2015-06-25 Eli Lilly And Company Fluorophenyl pyrazol compounds
CA2941380C (en) * 2014-03-07 2022-09-06 Biocryst Pharmaceuticals, Inc. Human plasma kallikrein inhibitors
AU2015229188A1 (en) 2014-03-13 2016-09-29 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing CFTR activity
AU2015229117A1 (en) 2014-03-13 2016-09-29 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing CFTR activity
MX376481B (en) 2014-06-03 2025-03-07 Idorsia Pharmaceuticals Ltd PYRAZOLE COMPOUNDS AND THEIR USE AS T-TYPE CALCIUM CHANNEL BLOCKERS.
WO2015196071A1 (en) 2014-06-19 2015-12-23 Proteostasis Therapeutics, Inc. Compounds, compositions and methods of increasing cftr activity
SG11201701998XA (en) 2014-09-15 2017-04-27 Actelion Pharmaceuticals Ltd Triazole compounds as t-type calcium channel blockers
CN106687445A (en) 2014-09-17 2017-05-17 维颂公司 Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
WO2016105484A1 (en) 2014-12-23 2016-06-30 Proteostasis Therapeutics, Inc. Derivatives of 5-(hetero)arylpyrazol-3-carboxylic amide or 1-(hetero)aryltriazol-4-carboxylic amide useful for the treatment of inter alia cystic fibrosis
MA41253A (en) 2014-12-23 2017-10-31 Proteostasis Therapeutics Inc COMPOUNDS, COMPOSITIONS AND PROCESSES TO INCREASE THE ACTIVITY OF CFTR
US10344023B2 (en) 2014-12-23 2019-07-09 Proteostasis Therapeutics, Inc. Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis
CA2971850A1 (en) 2014-12-23 2016-06-30 Proteostasis Therapeutics, Inc. Derivatives of 5-phenyl- or 5-heteroarylthiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis
SG10201907699YA (en) 2015-02-27 2019-09-27 Verseon Corp Substituted pyrazole compounds as serine protease inhibitors
TWI681956B (en) 2015-06-23 2020-01-11 日商橘生藥品工業股份有限公司 Pyrazole derivatives or their pharmacologically acceptable salts
EP3325474A1 (en) 2015-07-24 2018-05-30 Proteostasis Therapeutics, Inc. Compounds, compositions and methods of increasing cftr activity
MA43313B1 (en) 2015-09-02 2022-06-30 Trevena Inc 6-membered heterocyclic aza containing delta opioid receptor modulating compounds, and methods of making and using the same
MX382725B (en) 2015-10-06 2025-03-13 Proteostasis Therapeutics Inc COMPOUNDS, COMPOSITIONS AND METHODS FOR MODULATING THE TRANSMEMBRANE CONDUCTANCE REGULATOR OF CYSTIC FIBROSIS.
BR112018070747B1 (en) 2016-04-07 2024-01-09 Proteostasis Therapeutics, Inc SILICONE ATOMS CONTAINING IVACAFTOR ANALOGS, PHARMACEUTICAL COMPOSITIONS AND THERAPEUTIC USES
WO2017223188A1 (en) 2016-06-21 2017-12-28 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
CN110072521B (en) 2016-12-16 2022-11-29 爱杜西亚药品有限公司 Pharmaceutical combination comprising a T-type calcium channel blocker
EP3577099B1 (en) 2017-02-06 2024-01-24 Idorsia Pharmaceuticals Ltd A novel process for the synthesis of 1-aryl-1-trifluoromethylcyclopropanes
WO2018152286A1 (en) 2017-02-17 2018-08-23 Trevena, Inc. 7-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same
WO2018152293A1 (en) 2017-02-17 2018-08-23 Trevena, Inc. 5-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same
MX2020000576A (en) 2017-07-21 2020-09-10 Antabio Sas Chemical compounds.
JP7590183B2 (en) 2018-03-13 2024-11-26 武田薬品工業株式会社 Substituted imidazopyridines as inhibitors of plasma kallikrein and their uses
EP3587416A1 (en) 2018-06-29 2020-01-01 Institut Univ. de Ciència i Tecnologia, S.A. 2-oxopiperidin-3-yl derivatives and use thereof
CN112996795B (en) 2018-09-18 2024-11-12 尼坎治疗公司 Fused tricyclic derivatives as SRC homolog-2 phosphatase inhibitors
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
KR102135106B1 (en) * 2018-12-11 2020-07-17 재단법인 경기도경제과학진흥원 Antiviral Composition for Middle East Respiratory Syndrome Coronavirus
JP7695232B2 (en) 2019-09-18 2025-06-18 武田薬品工業株式会社 Heteroaryl plasma kallikrein inhibitors
CN114728962B (en) 2019-09-18 2025-09-19 武田药品工业有限公司 Plasma kallikrein inhibitors and uses thereof
US10792360B1 (en) 2019-11-21 2020-10-06 Chemocentryx, Inc. Compositions and methods for treating inflammatory bowel disease using CCR9 inhibitor and anti-TNF-alpha blocking antibodies
US11752149B2 (en) 2019-12-02 2023-09-12 Pipeline Therapeutics, Inc. Muscarinic acetylcholine M1 receptor antagonists
US12441707B2 (en) 2019-12-30 2025-10-14 Tyra Biosciences, Inc. Indazole compounds
EP4085056A1 (en) 2020-01-03 2022-11-09 Berg LLC Polycyclic amides as ube2k modulators for treating cancer
KR20230152654A (en) 2020-12-30 2023-11-03 타이라 바이오사이언시스, 인크. Indazole Compounds as Kinase Inhibitors
MA63501B1 (en) 2021-06-14 2024-07-31 Scorpion Therapeutics, Inc. Urea Derivatives for Cancer Treatment
EP4356909A1 (en) 2022-10-17 2024-04-24 Selabtec Sciences, SLU 1-(sulfonyl)-n-phenylpyrrolidine-2-carboxamides derivatives and use thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997023212A1 (en) * 1995-12-21 1997-07-03 The Du Pont Merck Pharmaceutical Company ISOXAZOLINE, ISOTHIAZOLINE AND PYRAZOLINE FACTOR Xa INHIBITORS

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997023212A1 (en) * 1995-12-21 1997-07-03 The Du Pont Merck Pharmaceutical Company ISOXAZOLINE, ISOTHIAZOLINE AND PYRAZOLINE FACTOR Xa INHIBITORS

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
M. L. QUAN: "Design and Synthesis of Isoxazoline Derivatives as Factor Xa Inhibitors", J. MED. CHEM., vol. 42, no. 15, - 7 July 1999 (1999-07-07), pages 2752 - 2759, XP002186000 *
QUAN M L ET AL: "Bisbenzamidine isoxazoline derivatives as factor Xa inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 7, no. 21, 4 November 1997 (1997-11-04), pages 2813 - 2818, XP004136536, ISSN: 0960-894X *

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8916554B2 (en) 2002-03-13 2014-12-23 Janssen Pharmaceutica, N.V. Amino-derivatives as novel inhibitors of histone deacetylase
US9533979B2 (en) 2002-03-13 2017-01-03 Janssen Pharmaceutica Nv Amino-derivatives as novel inhibitors of histone deacetylase
US7612094B2 (en) 2002-04-04 2009-11-03 Biogen Idec Ma Inc. Tri-substituted heteroaryls and methods of making and using the same
US7427616B2 (en) 2002-08-06 2008-09-23 Astrazeneca Ab Condensed pyridines and pyrimidines with tie2 (TEK) activity
US8710232B2 (en) 2004-04-22 2014-04-29 Sanofi-Aventis Deutschland Gmbh Imidazole derivatives used as TAFIa inhibitors
US9150543B2 (en) 2004-07-28 2015-10-06 Janssen Pharmaceutica N. V. Substituted indolyl alkyl amino derivatives as inhibitors of histone deacetylase
US10532051B2 (en) 2014-10-06 2020-01-14 Chemocentryx, Inc. Compositions and methods for treating inflammatory bowel disease using a combination therapy of small molecule inhibitors of C-C chemokine receptor 9 (CCR9) and anti-α4β7 integrin blocking antibodies
US10214519B2 (en) 2016-09-23 2019-02-26 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US10227350B2 (en) 2016-09-23 2019-03-12 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US10479770B2 (en) 2016-09-23 2019-11-19 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US12054477B2 (en) 2021-09-15 2024-08-06 Hua Medicine (Shanghai) Ltd. Prodrug of pyrrolidone derivatives as glucokinase activator

Also Published As

Publication number Publication date
WO2002000651A2 (en) 2002-01-03
AU2001273040A1 (en) 2002-01-08

Similar Documents

Publication Publication Date Title
WO2002000651A3 (en) Factor xa inhibitors
IL147317A0 (en) NITROGEN CONTAINING HETEROBICYCLES AS FACTOR Xa INHIBITORS
IL157652A (en) Metalloproteinase inhibitors, compositions comprising them and uses thereof for the preparation of medicaments for treating diseases or conditions mediated by metalloproteinase enzymes
WO2000055124A3 (en) Novel compounds and compositions as protease inhibitors
WO2005032472A3 (en) Pyrrolidine and piperidine derivatives as factor xa inhibitors
WO2004080971A8 (en) Tetrahydroquinoline derivatives useful as serine protease inhibitors
AP1744A (en) Inhibitors of factor XA and other serine proteases involved in the coagulation cascade
WO2004094372A3 (en) Compounds useful as serine protease inhibitors
WO2005099709A3 (en) Bicyclic heterocycles useful as serine protease inhibitors
WO2002080853A3 (en) Fused heterocyclic inhibitors of factor xa
NO20025601L (en) Arylmethylamine derivatives for use as tryptase inhibitors
WO2002020475A3 (en) Inhibitors of serine protease activity of matriptase or mtsp1
GEP20074098B (en) Lactam-containing compounds and derivatives thereof as factor xa inhibitors
WO2002048116A3 (en) Inhibitors of hepatitis c virus ns3 protease
WO1999043654A3 (en) Inhibitors of phospholipase enzymes
UA74372C2 (en) inhibitors of the serine proteaseS, pharmaceutical composition based thereon
NO983688L (en) Serine protease inhibitors
WO2004002405A3 (en) Amino-bicyclic pyrazinones and pyridinones
MY138303A (en) Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
WO2006047528A3 (en) Pyrazolobenzamides and derivatives as factor xa inhibitors
WO2004113278A3 (en) Acylsulfamide inhibitors of factor viia
WO2002002519A3 (en) THROMBIN OR FACTOR Xa INHIBITORS
WO2002098850A3 (en) Chemical compounds and pharmaceutical compositions as cathepsin s inhibitors
WO2004032908A3 (en) Method of inhibiting angiogenesis
WO2003015715A3 (en) Tetrahydroquinoline derivatives as antithrombotic agents

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CR CU CZ DE DK DM DZ EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
AK Designated states

Kind code of ref document: A3

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CR CU CZ DE DK DM DZ EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP

DPE2 Request for preliminary examination filed before expiration of 19th month from priority date (pct application filed from 20040101)