WO2009038157A1 - 2,3-ジヒドロ-イミノイソインドール誘導体 - Google Patents
2,3-ジヒドロ-イミノイソインドール誘導体 Download PDFInfo
- Publication number
- WO2009038157A1 WO2009038157A1 PCT/JP2008/066944 JP2008066944W WO2009038157A1 WO 2009038157 A1 WO2009038157 A1 WO 2009038157A1 JP 2008066944 W JP2008066944 W JP 2008066944W WO 2009038157 A1 WO2009038157 A1 WO 2009038157A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- compound
- salt
- optionally substituted
- inhibitory activity
- dihydroiminoisoindole
- Prior art date
Links
- MTKKGHVQPVOXIL-UHFFFAOYSA-N 3h-isoindol-1-amine Chemical class C1=CC=C2C(N)=NCC2=C1 MTKKGHVQPVOXIL-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 108010039209 Blood Coagulation Factors Proteins 0.000 abstract 1
- 102000015081 Blood Coagulation Factors Human genes 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 108010022999 Serine Proteases Proteins 0.000 abstract 1
- 102000012479 Serine Proteases Human genes 0.000 abstract 1
- 239000003114 blood coagulation factor Substances 0.000 abstract 1
- 229940019700 blood coagulation factors Drugs 0.000 abstract 1
- 230000035602 clotting Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 230000003449 preventive effect Effects 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- 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
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
-
- 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
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- C07D413/14—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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
Abstract
一般式(1) [式中、R1は、水素原子を意味する。R2は、置換基を有していてもよいフェニル基等を意味する。R3は、置換基を有していてもよいC6-10アリール基等を意味する。]で表される化合物またはその塩は、セリンプロテアーゼ阻害活性を有しており、特に血液凝固第VIIa因子に対する阻害活性に優れる。この化合物またはその塩は、血栓形成に起因する疾患の治療剤および/または予防剤として有用である。
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP08832347A EP2202231A4 (en) | 2007-09-21 | 2008-09-19 | 2,3-DIHYDROIMINOISOINDOLE DERIVATIVE |
JP2009533188A JPWO2009038157A1 (ja) | 2007-09-21 | 2008-09-19 | 2,3−ジヒドロ−イミノイソインドール誘導体 |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2007245988 | 2007-09-21 | ||
JP2007-245988 | 2007-09-21 | ||
US97505507P | 2007-09-25 | 2007-09-25 | |
US60/975,055 | 2007-09-25 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2009038157A1 true WO2009038157A1 (ja) | 2009-03-26 |
Family
ID=40467966
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/JP2008/066944 WO2009038157A1 (ja) | 2007-09-21 | 2008-09-19 | 2,3-ジヒドロ-イミノイソインドール誘導体 |
Country Status (4)
Country | Link |
---|---|
US (2) | US7807690B2 (ja) |
EP (1) | EP2202231A4 (ja) |
JP (1) | JPWO2009038157A1 (ja) |
WO (1) | WO2009038157A1 (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1810965A4 (en) * | 2004-10-13 | 2009-10-28 | Eisai R&D Man Co Ltd | HYDRAZIDE DERIVATIVES |
ITMI20051085A1 (it) * | 2005-06-10 | 2006-12-11 | Acs Dobfar Spa | Metodo di purificazione del cefotetan |
KR101362024B1 (ko) * | 2006-03-24 | 2014-02-11 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 트리아졸론 유도체 |
US7807690B2 (en) | 2007-09-21 | 2010-10-05 | Eisai R&D Management Co., Ltd. | 2,3-dihydro-iminoisoindole derivatives |
TW201206905A (en) | 2010-05-20 | 2012-02-16 | Eisai R & Amp D Man Co Ltd | Prodrug of triazolone compound |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2002509924A (ja) * | 1998-03-27 | 2002-04-02 | デュポン ファーマシューティカルズ カンパニー | 第Xa因子阻害剤としてのジ置換ピラゾリン類およびトリアゾリン類 |
WO2002085855A1 (fr) * | 2001-04-19 | 2002-10-31 | Eisai Co., Ltd. | Derives de 2-iminopyrrolidine |
JP2002543176A (ja) * | 1999-05-04 | 2002-12-17 | サノフィ−サンテラボ | 6−[[(アリールおよびヘテロアリール)オキシ]メチル]ナフタレン−2−カルボキシイミドアミド誘導体、それらの製造法およびそれらの治療的適用 |
WO2007111212A1 (ja) * | 2006-03-24 | 2007-10-04 | Eisai R & D Management Co., Ltd. | トリアゾロン誘導体 |
Family Cites Families (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0019586A1 (de) | 1979-05-11 | 1980-11-26 | Ciba-Geigy Ag | Neue antithrombotische Kombinationspräparate |
SU1512055A1 (ru) | 1987-12-04 | 1992-07-23 | Пермский фармацевтический институт | Дигидрохлорид гидразида N-ацетил-N-аллилантраниловой кислоты, про вл ющий антиагрегатную активность по отношению к тромбоцитам плазмы крови |
CA2301559A1 (en) | 1997-08-27 | 1999-03-04 | Norihiko Kikuchi | 3-amidinoaniline derivatives, activated blood coagulation factor x inhibitors, and intermediates for producing both |
AU2300699A (en) | 1998-02-17 | 1999-08-30 | Ono Pharmaceutical Co. Ltd. | Amidino derivatives and drugs containing the same as the active ingredient |
HUP0104421A3 (en) | 1998-12-14 | 2003-05-28 | Hoffmann La Roche | Phenylglycine derivatives |
ATE307111T1 (de) | 1999-01-13 | 2005-11-15 | Genentech Inc | Serinprotease-inhibitoren |
FR2791683A1 (fr) | 1999-03-30 | 2000-10-06 | Synthelabo | Derives de n-sulfonyl-dipeptides, leur preparation et leur application en therapeutique |
US6548694B2 (en) | 2000-05-23 | 2003-04-15 | Hoffman-La Roche Inc. | N-(4-carbamimidoyl-phenyl)-glycine derivatives |
EP1162194A1 (en) | 2000-06-06 | 2001-12-12 | Aventis Pharma Deutschland GmbH | Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use |
EP1312602A1 (en) | 2001-11-15 | 2003-05-21 | Eisai Co., Ltd. | Amidino derivatives, and anticoagulants and thrombosis therapeutic agents containing them |
JP4209659B2 (ja) | 2001-11-15 | 2009-01-14 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | アミジノ誘導体並びにそれを用いた抗血液凝固剤および血栓症治療剤 |
AU2003284001A1 (en) | 2002-10-07 | 2004-05-04 | Bristol-Myers Squibb Company | Triazolone and triazolethione derivatives |
EP1479679A1 (en) | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | Triazole-derivatives as factor Xa inhibitors |
EP1810965A4 (en) | 2004-10-13 | 2009-10-28 | Eisai R&D Man Co Ltd | HYDRAZIDE DERIVATIVES |
ES2310861T3 (es) | 2004-12-08 | 2009-01-16 | Bristol-Myers Squibb Company | Compuestos heterociclicos como inhibidores del factor viia. |
US7807690B2 (en) | 2007-09-21 | 2010-10-05 | Eisai R&D Management Co., Ltd. | 2,3-dihydro-iminoisoindole derivatives |
-
2008
- 2008-09-19 US US12/234,116 patent/US7807690B2/en not_active Expired - Fee Related
- 2008-09-19 WO PCT/JP2008/066944 patent/WO2009038157A1/ja active Application Filing
- 2008-09-19 JP JP2009533188A patent/JPWO2009038157A1/ja not_active Withdrawn
- 2008-09-19 EP EP08832347A patent/EP2202231A4/en not_active Withdrawn
-
2010
- 2010-01-15 US US12/688,756 patent/US20100184981A1/en not_active Abandoned
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2002509924A (ja) * | 1998-03-27 | 2002-04-02 | デュポン ファーマシューティカルズ カンパニー | 第Xa因子阻害剤としてのジ置換ピラゾリン類およびトリアゾリン類 |
JP2002543176A (ja) * | 1999-05-04 | 2002-12-17 | サノフィ−サンテラボ | 6−[[(アリールおよびヘテロアリール)オキシ]メチル]ナフタレン−2−カルボキシイミドアミド誘導体、それらの製造法およびそれらの治療的適用 |
WO2002085855A1 (fr) * | 2001-04-19 | 2002-10-31 | Eisai Co., Ltd. | Derives de 2-iminopyrrolidine |
WO2007111212A1 (ja) * | 2006-03-24 | 2007-10-04 | Eisai R & D Management Co., Ltd. | トリアゾロン誘導体 |
Non-Patent Citations (1)
Title |
---|
See also references of EP2202231A4 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
Also Published As
Publication number | Publication date |
---|---|
US7807690B2 (en) | 2010-10-05 |
JPWO2009038157A1 (ja) | 2011-01-06 |
US20090270433A1 (en) | 2009-10-29 |
EP2202231A1 (en) | 2010-06-30 |
EP2202231A4 (en) | 2011-09-28 |
US20100184981A1 (en) | 2010-07-22 |
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