BRPI0515140A - derivados de benzamidina de 4-aminometila e seu emprego como inibidores do fator viia - Google Patents
derivados de benzamidina de 4-aminometila e seu emprego como inibidores do fator viiaInfo
- Publication number
- BRPI0515140A BRPI0515140A BRPI0515140-6A BRPI0515140A BRPI0515140A BR PI0515140 A BRPI0515140 A BR PI0515140A BR PI0515140 A BRPI0515140 A BR PI0515140A BR PI0515140 A BRPI0515140 A BR PI0515140A
- Authority
- BR
- Brazil
- Prior art keywords
- aminomethyl
- benzamidine derivatives
- factor inhibitors
- factor
- derivatives
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/58—Carboxylic 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
- C07C255/60—Carboxylic 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 at least one of the singly-bound nitrogen atoms being acylated
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- C07C257/00—Compounds 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
- C07C257/10—Compounds 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
- C07C257/18—Compounds 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
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
- C07C259/12—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
- C07C259/18—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxamidine groups bound to carbon atoms of six-membered aromatic rings
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/62—Compounds containing any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylcarbamates
- C07C271/64—Y being a hydrogen or a carbon atom, e.g. benzoylcarbamates
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- C07C311/00—Amides 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
- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C311/04—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
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- C07C311/00—Amides 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
- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
- C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
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- C07C311/00—Amides 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
- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
- C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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- 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
- C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic 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
- C07D211/36—Heterocyclic 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
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
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- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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Abstract
DERIVADOS DE BENZAMIDINA DE 4-AMINOMETILA E SEU EMPREGO COMO INIBIDORES DO FATOR VIIA. A invenção está relacionada com novos derivados de benzamidina de 4-aminometila de fórmula (I) em que Ar e X são tais como definidos na descrição e nas reivindicações, assim como pró-drogas e sais farmaceuticamente aceitáveis destes. Estes compostos inibem a formação dos fatores de coagulação Xa, Ixa e trombina induzida pelo fator Vila e fator tecidual e podem ser empregados como medicamentos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04104292 | 2004-09-06 | ||
PCT/EP2005/009280 WO2006027135A1 (en) | 2004-09-06 | 2005-08-29 | 4-aminomethyl benzamidine derivatives and their use as factor viiia inhibitors |
Publications (1)
Publication Number | Publication Date |
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BRPI0515140A true BRPI0515140A (pt) | 2008-07-08 |
Family
ID=35238064
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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BRPI0515140-6A BRPI0515140A (pt) | 2004-09-06 | 2005-08-29 | derivados de benzamidina de 4-aminometila e seu emprego como inibidores do fator viia |
Country Status (11)
Country | Link |
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US (1) | US20060116410A1 (pt) |
EP (1) | EP1791810A1 (pt) |
JP (1) | JP2008512364A (pt) |
KR (1) | KR20070047338A (pt) |
CN (1) | CN101031541A (pt) |
AU (1) | AU2005281934A1 (pt) |
BR (1) | BRPI0515140A (pt) |
CA (1) | CA2577608A1 (pt) |
MX (1) | MX2007002391A (pt) |
RU (1) | RU2007112688A (pt) |
WO (1) | WO2006027135A1 (pt) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
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JP5322935B2 (ja) * | 2006-07-31 | 2013-10-23 | アクティベサイト ファーマシューティカルズ インコーポレイティッド | 血漿カリクレインの阻害薬 |
EP2259679A4 (en) * | 2008-01-31 | 2011-09-14 | Joslin Diabetes Ct | METHOD FOR THE TREATMENT OF CALLIQUE CLEANING DISORDERS |
GB0815784D0 (en) | 2008-08-29 | 2008-10-08 | Xention Ltd | Novel potassium channel blockers |
GB0815781D0 (en) * | 2008-08-29 | 2008-10-08 | Xention Ltd | Novel potassium channel blockers |
GB0815782D0 (en) * | 2008-08-29 | 2008-10-08 | Xention Ltd | Novel potassium channel blockers |
US9206123B2 (en) | 2009-12-18 | 2015-12-08 | Activesite Pharmaceuticals, Inc. | Prodrugs of inhibitors of plasma kallikrein |
SG10201408429UA (en) | 2009-12-18 | 2015-02-27 | Activesite Pharmaceuticals Inc | Prodrugs of inhibitors of plasma kallikrein |
WO2012142308A1 (en) | 2011-04-13 | 2012-10-18 | Activesite Pharmaceuticals, Inc. | Prodrugs of inhibitors of plasma kallikrein |
EP2981522A4 (en) | 2013-04-05 | 2016-08-31 | Salk Inst For Biological Studi | ANTAGONISTS OF PPAR |
WO2016057322A1 (en) | 2014-10-08 | 2016-04-14 | Salk Institute For Biological Studies | Ppar agonists and methods of use thereof |
US10188627B2 (en) | 2014-10-08 | 2019-01-29 | Mitobridge, Inc. | PPAR agonists, compounds, pharmaceutical compositions, and methods of use thereof |
ES2949852T3 (es) | 2015-10-07 | 2023-10-03 | Mitobridge Inc | Agonistas de PPAR, compuestos, composiciones farmacéuticas y métodos de uso de los mismos |
CN109071459B (zh) | 2016-04-13 | 2022-08-16 | 米托布里奇公司 | Ppar激动剂、化合物、药物组合物以及它们的使用方法 |
AU2020310859A1 (en) * | 2019-07-08 | 2022-01-27 | Activesite Pharmaceuticals, Inc. | Crystalline forms of plasma kallikrein inhibitors |
CN114502531B (zh) * | 2019-07-08 | 2024-05-24 | 雷佐鲁特公司 | 制备血浆激肽释放酶抑制剂的方法 |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
HUP0003906A2 (hu) * | 1997-06-19 | 2001-05-28 | Du Pont Pharmaceuticals Co. | Xa faktort gátló hatású heterociklusos vegyületek és ezeket tartalmazó gyógyszerkészítmények |
US5998424A (en) * | 1997-06-19 | 1999-12-07 | Dupont Pharmaceuticals Company | Inhibitors of factor Xa with a neutral P1 specificity group |
DE19753522A1 (de) * | 1997-12-03 | 1999-06-10 | Boehringer Ingelheim Pharma | Substituierte Indole, ihre Herstellung und ihre Verwendung als Arzneimittel |
DE19754490A1 (de) * | 1997-12-09 | 1999-06-10 | Boehringer Ingelheim Pharma | Durch einen Aminocarbonylrest substituierte Bicyclen, ihre Herstellung und ihre Verwendung als Arzneimittel |
PT1042287E (pt) * | 1997-12-24 | 2005-08-31 | Aventis Pharma Gmbh | Derivados de indole como inibidores do factor xa |
US20020151534A1 (en) * | 2001-02-02 | 2002-10-17 | Ries Uwe Joerg | Antithrombotic compounds |
JP2004522759A (ja) * | 2001-02-02 | 2004-07-29 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | 抗血栓性化合物、その製法及び医薬組成物としての使用 |
DE10111842A1 (de) * | 2001-03-13 | 2002-09-19 | Boehringer Ingelheim Pharma | Antithrombotische Carbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel |
TW200410921A (en) * | 2002-11-25 | 2004-07-01 | Hoffmann La Roche | Mandelic acid derivatives |
US7247654B2 (en) * | 2003-06-04 | 2007-07-24 | Bristol-Myers Squibb Company | 3,4-disubstituted benzamidines and benzylamines, and analogues thereof, useful as serine protease inhibitors |
ATE538650T1 (de) * | 2006-03-10 | 2012-01-15 | Jenrin Discovery | Cannabinoid-rezeptor-antagonisten / inverse agonisten zur behandlung von übergewicht |
JP5322935B2 (ja) * | 2006-07-31 | 2013-10-23 | アクティベサイト ファーマシューティカルズ インコーポレイティッド | 血漿カリクレインの阻害薬 |
-
2005
- 2005-08-29 JP JP2007529330A patent/JP2008512364A/ja active Pending
- 2005-08-29 CN CNA2005800330246A patent/CN101031541A/zh active Pending
- 2005-08-29 EP EP05783728A patent/EP1791810A1/en not_active Withdrawn
- 2005-08-29 BR BRPI0515140-6A patent/BRPI0515140A/pt not_active IP Right Cessation
- 2005-08-29 MX MX2007002391A patent/MX2007002391A/es not_active Application Discontinuation
- 2005-08-29 WO PCT/EP2005/009280 patent/WO2006027135A1/en active Application Filing
- 2005-08-29 AU AU2005281934A patent/AU2005281934A1/en not_active Abandoned
- 2005-08-29 RU RU2007112688/04A patent/RU2007112688A/ru unknown
- 2005-08-29 CA CA002577608A patent/CA2577608A1/en not_active Abandoned
- 2005-08-29 KR KR1020077005304A patent/KR20070047338A/ko active IP Right Grant
- 2005-09-01 US US11/217,860 patent/US20060116410A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
KR20070047338A (ko) | 2007-05-04 |
US20060116410A1 (en) | 2006-06-01 |
EP1791810A1 (en) | 2007-06-06 |
AU2005281934A1 (en) | 2006-03-16 |
MX2007002391A (es) | 2007-04-23 |
WO2006027135A1 (en) | 2006-03-16 |
RU2007112688A (ru) | 2008-10-20 |
JP2008512364A (ja) | 2008-04-24 |
CA2577608A1 (en) | 2006-03-16 |
CN101031541A (zh) | 2007-09-05 |
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