+

WO2002006280A3 - INHIBITORS OF FACTOR Xa - Google Patents

INHIBITORS OF FACTOR Xa Download PDF

Info

Publication number
WO2002006280A3
WO2002006280A3 PCT/US2001/022077 US0122077W WO0206280A3 WO 2002006280 A3 WO2002006280 A3 WO 2002006280A3 US 0122077 W US0122077 W US 0122077W WO 0206280 A3 WO0206280 A3 WO 0206280A3
Authority
WO
WIPO (PCT)
Prior art keywords
factor
inhibitors
compounds
vitro
vivo
Prior art date
Application number
PCT/US2001/022077
Other languages
French (fr)
Other versions
WO2002006280A2 (en
Inventor
Bing-Yan Zhu
Hua Yang
Robert M Scarborough
Original Assignee
Millennium Pharamaceuticals In
Bing-Yan Zhu
Hua Yang
Robert M Scarborough
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 Millennium Pharamaceuticals In, Bing-Yan Zhu, Hua Yang, Robert M Scarborough filed Critical Millennium Pharamaceuticals In
Priority to AU2002222933A priority Critical patent/AU2002222933A1/en
Publication of WO2002006280A2 publication Critical patent/WO2002006280A2/en
Publication of WO2002006280A3 publication Critical patent/WO2002006280A3/en

Links

Classifications

    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • 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
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • 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

Compounds, having the formula (I), their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
PCT/US2001/022077 2000-07-13 2001-07-13 INHIBITORS OF FACTOR Xa WO2002006280A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002222933A AU2002222933A1 (en) 2000-07-13 2001-07-13 Inhibitors of factor xa

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21805100P 2000-07-13 2000-07-13
US60/218,051 2000-07-13

Publications (2)

Publication Number Publication Date
WO2002006280A2 WO2002006280A2 (en) 2002-01-24
WO2002006280A3 true WO2002006280A3 (en) 2003-07-17

Family

ID=22813543

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/022077 WO2002006280A2 (en) 2000-07-13 2001-07-13 INHIBITORS OF FACTOR Xa

Country Status (2)

Country Link
AU (1) AU2002222933A1 (en)
WO (1) WO2002006280A2 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE50310038D1 (en) 2002-03-11 2008-08-07 Curacyte Ag INGREDIENTS OF UROKINASE, THEIR PREPARATION AND USE
DE10301300B4 (en) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Use of acylated 4-amidino- and 4-guanidinobenzylamines for the inhibition of plasma kallikrein
DE10342108A1 (en) 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basic substituted benzylamine analogs as coagulation factor Xa inhibitors, their preparation and use
DE102005044319A1 (en) * 2005-09-16 2007-03-22 Curacyte Chemistry Gmbh 2- (Aminomethyl) -5-chloro-benzylamide derivatives and their use as inhibitors of coagulation factor Xa
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
SG175609A1 (en) 2006-10-09 2011-11-28 Takeda Pharmaceutical Kinase inhibitors
DE102006050672A1 (en) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh New glycylglycine derivatives with a benzylsulfonylamido group and an amidino-organylamido group at the opposite chain ends, used in drugs for reducing loss of blood, e.g. in operations
JP7164521B2 (en) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー carbocyclic prolinamide derivatives
CN114685453A (en) 2016-06-21 2022-07-01 奥瑞恩眼科有限责任公司 Heterocyclic prolinamide derivatives

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993025574A1 (en) * 1992-06-12 1993-12-23 Pfizer Inc. Inhibitors of angiotensin i chymase(s) including human heart chymase
WO1994015956A1 (en) * 1993-01-04 1994-07-21 The Wellcome Foundation Limited Endothelin converting enzyme inhibitors
EP0611756A2 (en) * 1993-02-19 1994-08-24 Takeda Chemical Industries, Ltd. Alcohol or aldehyde derivatives as cathepsin L inhibitor and bone resorption inhibitor
WO1995024914A1 (en) * 1994-03-15 1995-09-21 Myogenics, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
JPH0820597A (en) * 1994-07-07 1996-01-23 Meiji Seika Kaisha Ltd Heterocyclic carbonyl compound having thrombin-inhibiting action
WO1996040741A1 (en) * 1995-06-07 1996-12-19 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
WO1996040744A1 (en) * 1995-06-07 1996-12-19 Cor Therapeutics, Inc. KETOHETEROCYCLIC INHIBITORS OF FACTOR Xa
WO1996040743A2 (en) * 1995-06-07 1996-12-19 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
WO1997031939A1 (en) * 1996-03-01 1997-09-04 Akzo Nobel N.V. Serine protease inhibitors
WO2001010894A2 (en) * 1999-08-04 2001-02-15 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993025574A1 (en) * 1992-06-12 1993-12-23 Pfizer Inc. Inhibitors of angiotensin i chymase(s) including human heart chymase
WO1994015956A1 (en) * 1993-01-04 1994-07-21 The Wellcome Foundation Limited Endothelin converting enzyme inhibitors
EP0611756A2 (en) * 1993-02-19 1994-08-24 Takeda Chemical Industries, Ltd. Alcohol or aldehyde derivatives as cathepsin L inhibitor and bone resorption inhibitor
WO1995024914A1 (en) * 1994-03-15 1995-09-21 Myogenics, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
JPH0820597A (en) * 1994-07-07 1996-01-23 Meiji Seika Kaisha Ltd Heterocyclic carbonyl compound having thrombin-inhibiting action
WO1996040741A1 (en) * 1995-06-07 1996-12-19 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
WO1996040744A1 (en) * 1995-06-07 1996-12-19 Cor Therapeutics, Inc. KETOHETEROCYCLIC INHIBITORS OF FACTOR Xa
WO1996040743A2 (en) * 1995-06-07 1996-12-19 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
WO1997031939A1 (en) * 1996-03-01 1997-09-04 Akzo Nobel N.V. Serine protease inhibitors
WO2001010894A2 (en) * 1999-08-04 2001-02-15 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
B.J. HALL ET AL, TETRAHEDRON LETT., vol. 39, no. 36, 1998, pages 6593 - 6596, XP004132554 *
DATABASE CAPLUS [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; XP002235421, retrieved from STN Database accession no. 1996:281614 *
M. IQBAL ET AL, BIOORG. MED. CHEM. LETT., vol. 7, no. 5, 1997, pages 539 - 544, XP004136061 *
M. TAO ET AL, BIOORG. MED. CHEM. LETT., vol. 6, no. 24, 1996, pages 3009 - 3012, XP002161620 *
S. BAJUSZ ET AL, BIOORG. MED. CHEM. LETT., vol. 8, no. 12, 1998, pages 1477 - 1482, XP004137067 *

Also Published As

Publication number Publication date
AU2002222933A1 (en) 2002-01-30
WO2002006280A2 (en) 2002-01-24

Similar Documents

Publication Publication Date Title
WO2000071507A3 (en) INHIBITORS OF FACTOR Xa
WO2000071515A3 (en) INHIBITORS OF FACTOR Xa
WO1998016523A3 (en) Selective factor xa inhibitors
WO2001064642A3 (en) Benzamides and related inhibitors of factor xa
BR0014078A (en) Xa factor inhibitors
WO2001019788A3 (en) BENZAMIDES AND RELATED INHIBITORS OF FACTOR Xa
WO2000071511A3 (en) INHIBITORS OF FACTOR Xa
ZA200306419B (en) Phenyl derivatives.
WO2001056989A3 (en) Inhibitors of factor xa
MA28279A1 (en) INDOLE DERIVATIVES AND THE USE THEREOF AS KINASE INHIBITORS, IN PARTICULAR IKK2 INHIBITORS
MX2007003470A (en) Carbonyl compounds usable as coagulation factor xa inhibitors.
TR200200883T2 (en) 2-substituted 1,1-biphenyl-2-carbonamides, manufacturing methods, use as drugs
DE60221505D1 (en) FACTOR Xa BENZAMIDINE INHIBITORS
WO1996040743A3 (en) Inhibitors of factor xa
WO2001072708A3 (en) OXINDOLE INHIBITORS OF FACTOR Xa
WO2002026720A3 (en) PIPERAZINE BASED INHIBITORS OF FACTOR Xa
TR200201128T2 (en) Tetrahydrothiopyraniphalazinone derivatives as PDE4 inhibitors.
WO2002006280A3 (en) INHIBITORS OF FACTOR Xa
DE69803383D1 (en) FACTOR X SELECTIVE INHIBITORS, CONTAINING AN ACEPINONE STRUCTURE
WO2002026718A3 (en) Bicyclic pyrimidin-4-one based inhibitors of factor xa
MXPA04004307A (en) Derivatives of phenoxy-n-'4-(isothiazolidin-1,1-dioxid-2yl)pheny!-valerian- acid amide and other compounds as inhibitors of the coagulation factor xa in the treatment of thromboembolic diseases and tumors.
WO2002026731A3 (en) Quaternary amidino based inhibitors of factor xa
WO2002074735A3 (en) Biurethane derivatives
YU19302A (en) 4-benzylaminoquinoline conjugates with bile acid and their heteroanalogues, methods for producing the same, medicaments containing these compounds and their use
WO2001000188A3 (en) Tetrahydroquinolinyl-6-methyldihydrothiadiazinone derivatives and their use for preventing and/or treating anaemia

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 CO CR CU CZ DE DK DM DZ EC 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 US 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
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

点击 这是indexloc提供的php浏览器服务，不要输入任何密码和下载