JP2013510159A - ピラジノントロンビン阻害剤およびその中間体の製造方法 - Google Patents

ピラジノントロンビン阻害剤およびその中間体の製造方法 Download PDF

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Publication number
JP2013510159A
JP2013510159A JP2012537955A JP2012537955A JP2013510159A JP 2013510159 A JP2013510159 A JP 2013510159A JP 2012537955 A JP2012537955 A JP 2012537955A JP 2012537955 A JP2012537955 A JP 2012537955A JP 2013510159 A JP2013510159 A JP 2013510159A
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JP
Japan
Prior art keywords
compound
difluoro
formula
fluoropyridine
salt
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JP2012537955A
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English (en)
Japanese (ja)
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JP2013510159A5 (enExample
Inventor
レグリ・ブチ・レディ
ウッパラパリ・サンパスクマール
ニラム・サフ
ジャヴァジ・カルナカラ・ラオ
ゲイド・ブラフマ・レディ
Original Assignee
ダイアクロン・ファーマシューティカルズ・インコーポレイテッド
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Publication of JP2013510159A publication Critical patent/JP2013510159A/ja
Publication of JP2013510159A5 publication Critical patent/JP2013510159A5/ja
Pending legal-status Critical Current

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B61/00—Other general methods

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pyridine Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Catalysts (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
JP2012537955A 2009-11-03 2010-11-02 ピラジノントロンビン阻害剤およびその中間体の製造方法 Pending JP2013510159A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN2663CH2009 2009-11-03
IN2663/CHE/2009 2009-11-03
PCT/US2010/055176 WO2011056806A1 (en) 2009-11-03 2010-11-02 Process for the preparation of pyrazinone thrombin inhibitor and its intermediates

Publications (2)

Publication Number Publication Date
JP2013510159A true JP2013510159A (ja) 2013-03-21
JP2013510159A5 JP2013510159A5 (enExample) 2013-12-19

Family

ID=43926105

Family Applications (1)

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JP2012537955A Pending JP2013510159A (ja) 2009-11-03 2010-11-02 ピラジノントロンビン阻害剤およびその中間体の製造方法

Country Status (10)

Country Link
US (1) US8541580B2 (enExample)
EP (1) EP2496087A4 (enExample)
JP (1) JP2013510159A (enExample)
KR (1) KR20120106727A (enExample)
CN (1) CN102711481A (enExample)
AU (1) AU2010315338A1 (enExample)
CA (1) CA2778922A1 (enExample)
MX (1) MX2012005165A (enExample)
RU (1) RU2012118499A (enExample)
WO (1) WO2011056806A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10016417B2 (en) 2011-11-07 2018-07-10 Diakron Pharmaceuticals, Inc. Extended release formulation of a direct thrombin inhibitor
KR102666624B1 (ko) 2015-10-26 2024-05-16 바이엘 크롭사이언스 악티엔게젤샤프트 농약으로서의 융합된 비사이클릭 헤테로사이클 유도체
AU2020229979B2 (en) 2019-02-26 2025-03-06 Bayer Aktiengesellschaft Fused bicyclic heterocycle derivatives as pesticides
PH12021552065A1 (en) 2019-02-26 2022-05-23 Bayer Ag Condensed bicyclic heterocyclic derivatives as pest control agents

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003501426A (ja) * 1999-06-04 2003-01-14 メルク エンド カムパニー インコーポレーテッド ピラジノントロンビン阻害剤
JP2004518643A (ja) * 2000-12-06 2004-06-24 メルク　エンド　カムパニー　インコーポレーテッド トロンビン阻害剤の製造方法
JP2006508143A (ja) * 2002-11-20 2006-03-09 バイエル・クロツプサイエンス・エス・アー ２−アミノメチルピリジン誘導体の新規製造方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6147078A (en) * 1998-05-19 2000-11-14 Merck & Co., Inc. Pyrazinone thrombin inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003501426A (ja) * 1999-06-04 2003-01-14 メルク エンド カムパニー インコーポレーテッド ピラジノントロンビン阻害剤
JP2004518643A (ja) * 2000-12-06 2004-06-24 メルク　エンド　カムパニー　インコーポレーテッド トロンビン阻害剤の製造方法
JP2006508143A (ja) * 2002-11-20 2006-03-09 バイエル・クロツプサイエンス・エス・アー ２−アミノメチルピリジン誘導体の新規製造方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JPN6014041855; Ｃａｔａｌｏｇ　Ｈａｎｄｂｏｏｋ　ｏｆ　Ｆｉｎｅ　Ｃｈｅｍｉｃａｌｓ　１９９６-１９９７ , 1997, Ｓｉｇｍａ-Ａｌｄｒｉｃｈ　Ｊａｐａｎ　Ｋ．Ｋ． *

Also Published As

Publication number Publication date
CA2778922A1 (en) 2011-05-12
US8541580B2 (en) 2013-09-24
MX2012005165A (es) 2012-08-08
AU2010315338A1 (en) 2012-05-24
WO2011056806A1 (en) 2011-05-12
US20110105753A1 (en) 2011-05-05
EP2496087A4 (en) 2013-06-19
EP2496087A1 (en) 2012-09-12
CN102711481A (zh) 2012-10-03
RU2012118499A (ru) 2013-12-10
KR20120106727A (ko) 2012-09-26

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