ZA987676B - 3-amidinoaniline derivatives activated blood coagulation factor X inhibitors and intermediates thereof - Google Patents

3-amidinoaniline derivatives activated blood coagulation factor X inhibitors and intermediates thereof

Info

Publication number
ZA987676B
ZA987676B ZA987676A ZA987676A ZA987676B ZA 987676 B ZA987676 B ZA 987676B ZA 987676 A ZA987676 A ZA 987676A ZA 987676 A ZA987676 A ZA 987676A ZA 987676 B ZA987676 B ZA 987676B
Authority
ZA
South Africa
Prior art keywords
intermediates
inhibitors
blood coagulation
coagulation factor
activated blood
Prior art date
Application number
ZA987676A
Other languages
English (en)
Inventor
Satoshi Akahane
Masahiko Uchida
Hidetoshi Isawa
Norihiko Kikuchi
Tomonaga Ozawa
Horiaki Kobayashi
Yuichiro Kai
Kenji Akahane
Original Assignee
Kissei Pharmaceutical
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 Kissei Pharmaceutical filed Critical Kissei Pharmaceutical
Publication of ZA987676B publication Critical patent/ZA987676B/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • C07C317/26Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/64Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/16Heterocyclic 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
    • C07D295/18Heterocyclic 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
    • C07D295/195Radicals derived from nitrogen analogues of carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/22Heterocyclic 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 with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/24Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
ZA987676A 1997-08-27 1998-08-25 3-amidinoaniline derivatives activated blood coagulation factor X inhibitors and intermediates thereof ZA987676B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP27185397 1997-08-27

Publications (1)

Publication Number Publication Date
ZA987676B true ZA987676B (en) 1999-02-25

Family

ID=17505799

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA987676A ZA987676B (en) 1997-08-27 1998-08-25 3-amidinoaniline derivatives activated blood coagulation factor X inhibitors and intermediates thereof

Country Status (11)

Country Link
EP (1) EP1020434A4 (xx)
KR (1) KR20010023364A (xx)
CN (1) CN1268116A (xx)
AR (1) AR016868A1 (xx)
AU (1) AU8747598A (xx)
CA (1) CA2301559A1 (xx)
CO (1) CO4970693A1 (xx)
IL (1) IL134394A0 (xx)
PE (1) PE107999A1 (xx)
WO (1) WO1999010316A1 (xx)
ZA (1) ZA987676B (xx)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003500376A (ja) 1999-05-24 2003-01-07 シーオーアール セラピューティクス インコーポレイテッド Xa因子の阻害剤
WO2000071510A2 (en) 1999-05-24 2000-11-30 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
DE10041402A1 (de) 2000-08-23 2002-03-14 Morphochem Ag Neue Verbindungen, die Faktor Xa-Aktivität inhibieren
EP1095933A1 (en) * 1999-10-30 2001-05-02 Aventis Pharma Deutschland GmbH Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
WO2001056989A2 (en) * 2000-02-01 2001-08-09 Cor Therapeutics, Inc. Inhibitors of factor xa
US6376515B2 (en) 2000-02-29 2002-04-23 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor Xa
DE10027025A1 (de) * 2000-05-31 2001-12-06 Merck Patent Gmbh Clycinamide
DE10036121A1 (de) * 2000-07-25 2002-02-07 Merck Patent Gmbh N-Substituierte-1-amino-1,1-dialkyl-carbonsäurederivate
DE10040783A1 (de) 2000-08-21 2002-03-07 Merck Patent Gmbh AZA-Aminosäurederivate (Faktor X¶a¶-Inhibitoren 15)
DE10050723A1 (de) * 2000-10-13 2002-04-25 Merck Patent Gmbh N-Substituierte Aminosäurederivate (Faktor Xa Inhibitoren 12)
US7312235B2 (en) 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
DE10130374A1 (de) * 2001-06-23 2003-01-02 Boehringer Ingelheim Pharma Substituierte N-Acyl-anilinderivate, deren Herstellung und deren Verwendung als Arzneimittel
EP1443041A4 (en) * 2001-11-09 2006-06-07 Kissei Pharmaceutical 5-AMIDINO-2-HYDROXYBENZENE-SULFONAMIDE DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THEM, THEIR MEDICAL USE AND INTERMEDIATE PRODUCTS USED IN THEIR PRODUCTION
CN100341496C (zh) * 2002-03-22 2007-10-10 橘生药品工业株式会社 预防或治疗肾脏疾病的药剂
DE10220048A1 (de) * 2002-05-04 2003-11-13 Merck Patent Gmbh Semicarbazidderivate
PT1569912E (pt) 2002-12-03 2015-09-15 Pharmacyclics Llc Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia
WO2005034867A2 (en) 2003-10-09 2005-04-21 Millennium Pharmaceuticals, Inc. Thioether-substituted benzamides as inhibitors of factor xa
JP5020073B2 (ja) 2004-06-18 2012-09-05 ミレニアム ファーマシューティカルズ インク. 第Xa因子阻害剤
US7329656B2 (en) 2004-10-08 2008-02-12 H. Lundbeck A/S Arylthiobenzylpiperidine derivatives
US7446204B2 (en) 2004-10-08 2008-11-04 H. Lundbeck A/S Amino substituted aryloxybenzylpiperidine derivatives
WO2006041119A1 (ja) * 2004-10-13 2006-04-20 Eisai R & D Management Co., Ltd. ヒドラジド誘導体
US7612089B2 (en) 2004-11-19 2009-11-03 Portola Pharmaceuticals, Inc. Tetrahydroisoquinolines as factor Xa inhibitors
US7678913B2 (en) 2004-12-07 2010-03-16 Portola Pharmaceuticals, Inc. Ureas as factor Xa inhibitors
JP4900238B2 (ja) 2005-02-02 2012-03-21 味の素株式会社 新規ベンズアミジン化合物
JP5227178B2 (ja) 2005-11-08 2013-07-03 ミレニアム ファーマシューティカルズ, インコーポレイテッド N−(5−クロロ−2−ピリジニル)−2−[[4−[(ジメチルアミノ)イミノメチル]ベンゾイル]アミノ]−5−メトキシ−ベンズアミド、第Xa因子阻害剤の薬学的な塩および多形体
SI2000465T1 (sl) 2006-03-24 2011-04-29 Eisai R&D Man Co Ltd Derivat triazolona
EP2077995B1 (en) 2006-11-02 2012-02-08 Millennium Pharmaceuticals, Inc. Methods of synthesizing pharmaceutical salts of a factor xa inhibitor
EP2202231A4 (en) 2007-09-21 2011-09-28 Eisai R&D Man Co Ltd 2,3-DIHYDROIMINOISOINDOLE DERIVATIVE
WO2010005087A1 (ja) 2008-07-11 2010-01-14 味の素株式会社 アミジン誘導体
EA015918B1 (ru) 2010-03-03 2011-12-30 Дмитрий Геннадьевич ТОВБИН УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2606643B2 (ja) * 1992-04-01 1997-05-07 日東紡績株式会社 安息香酸アミジノフェニルエステル誘導体
JPH07330695A (ja) * 1994-04-11 1995-12-19 Green Cross Corp:The 新規カルボン酸誘導体またはその塩、およびその医薬用途
DK0892780T3 (da) * 1996-02-22 2003-03-03 Bristol Myers Squibb Pharma Co m-Amidinophenylanaloger som faktor Xa-inhibitorer
JPH101467A (ja) * 1996-06-13 1998-01-06 Banyu Pharmaceut Co Ltd ビフェニルアミジン誘導体

Also Published As

Publication number Publication date
IL134394A0 (en) 2001-04-30
CN1268116A (zh) 2000-09-27
CA2301559A1 (en) 1999-03-04
EP1020434A1 (en) 2000-07-19
WO1999010316A1 (fr) 1999-03-04
CO4970693A1 (es) 2000-11-07
PE107999A1 (es) 1999-11-24
EP1020434A4 (en) 2000-11-15
AR016868A1 (es) 2001-08-01
AU8747598A (en) 1999-03-16
KR20010023364A (ko) 2001-03-26

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