CO2022000422A2 - Inhibidores de enzimas - Google Patents
Inhibidores de enzimasInfo
- Publication number
- CO2022000422A2 CO2022000422A2 CONC2022/0000422A CO2022000422A CO2022000422A2 CO 2022000422 A2 CO2022000422 A2 CO 2022000422A2 CO 2022000422 A CO2022000422 A CO 2022000422A CO 2022000422 A2 CO2022000422 A2 CO 2022000422A2
- Authority
- CO
- Colombia
- Prior art keywords
- enzyme inhibitors
- compounds
- formula
- compositions
- methods
- Prior art date
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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
- C07D401/02—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
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P25/06—Antimigraine agents
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- A—HUMAN NECESSITIES
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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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- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
- C07C233/35—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/37—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a saturated carbon skeleton containing rings
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- 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
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- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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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
- C07D213/60—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 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
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
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- C07D213/02—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
- 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
- C07D213/60—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 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
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- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
- C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
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- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
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- C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
- C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
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- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D333/58—Radicals substituted by nitrogen atoms
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- 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
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- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invención proporciona compuestos de la Fórmula (I): Fórmula (I) composiciones que comprenden dichos compuestos; el uso te-rapéutico de cada uno de dichos compuestos; y métodos de tratamiento en pacientes con cada uno de dichos compues-tos; en donde A, Y, n, R1, R2A, R2B, R3 y *1 son definidos anteriormente en el presente documento.
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PCT/GB2019/052356 WO2021032933A1 (en) | 2019-08-21 | 2019-08-21 | Enzyme inhibitors |
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EP (1) | EP4017586A1 (es) |
JP (1) | JP2022552048A (es) |
KR (1) | KR20220050942A (es) |
CN (1) | CN114269431A (es) |
AR (1) | AR118082A1 (es) |
AU (1) | AU2019462669A1 (es) |
BR (1) | BR112022001054A2 (es) |
CA (1) | CA3147564A1 (es) |
CO (1) | CO2022000422A2 (es) |
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MX (1) | MX2022001933A (es) |
TW (1) | TW202115007A (es) |
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GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
EP4010333A1 (en) | 2019-08-09 | 2022-06-15 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
WO2022255399A1 (ja) * | 2021-06-01 | 2022-12-08 | 国立研究開発法人理化学研究所 | G9a阻害剤 |
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EP0442878A4 (en) * | 1988-04-05 | 1991-10-23 | Abbott Laboratories | Derivatives of tryptophan as cck antagonists |
EP1124822A4 (en) | 1998-10-30 | 2002-04-03 | Merck & Co Inc | THROMBIN INHIBITORS |
EA005031B1 (ru) | 1999-05-19 | 2004-10-28 | Фармация Корпорейшн | Замещенные полициклические арил- и гетероарилпиразиноны, которые могут использоваться при селективном ингибировании системы свертывания крови |
GB0030305D0 (en) * | 2000-12-13 | 2001-01-24 | Lilly Co Eli | Compounds |
EP1808440B1 (en) * | 2000-08-11 | 2011-07-27 | Wilex AG | Non-covalent inhibitors of urokinase and blood vessel formation |
DE10301300B4 (de) * | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
NZ617083A (en) | 2003-08-27 | 2015-04-24 | Ophthotech Corp | Combination therapy for the treatment of ocular neovascular disorders |
WO2008141010A2 (en) * | 2007-05-11 | 2008-11-20 | Mpex Pharmaceuticals, Inc. | Polybasic bacterial efflux pump inhibitors and therapeutic uses thereof |
GB0807828D0 (en) * | 2008-04-29 | 2008-06-04 | Vantia Ltd | Aminopyridine derivatives |
GB0918924D0 (en) * | 2009-10-28 | 2009-12-16 | Vantia Ltd | Azaindole derivatives |
US8598206B2 (en) * | 2010-01-28 | 2013-12-03 | The Medicines Company (Leipzig) Gmbh | Trypsin-like serine protease inhibitors, and their preparation and use |
EP2621893A1 (en) * | 2010-10-01 | 2013-08-07 | UCB Pharma GmbH | Process for the preparation of amino acid derivatives |
CA2829037C (en) | 2011-03-09 | 2022-05-17 | Csl Behring Gmbh | Factor xii inhibitors for the administration with medical procedures comprising contact with artificial surfaces |
JP6581774B2 (ja) * | 2011-05-27 | 2019-09-25 | アンブルックス, インコーポレイテッドAmbrx, Inc. | 非天然アミノ酸結合ドラスタチン誘導体を含有する化合物またはその化合物の溶媒和物、およびドラスタチンアナログを誘導体化するための方法 |
GB201421088D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
WO2017027967A1 (en) * | 2015-08-17 | 2017-02-23 | University Health Network | Inhibitors of peptidyl arginine deiminase (pad) enzymes and uses thereof |
WO2017123518A1 (en) | 2016-01-11 | 2017-07-20 | The Rockefeller University | Aminotriazole immunomodulators for treating autoimmune diseases |
EP3463341A4 (en) | 2016-05-23 | 2019-11-13 | The Rockefeller University | AMINOCYLINDAZOLE IMMUNOMODULATORS FOR THE TREATMENT OF AUTOIMMUNE DISEASES |
US11014920B2 (en) | 2016-11-18 | 2021-05-25 | Merck Sharp & Dohme Corp. | Factor XIIa inhibitors |
US10875851B2 (en) | 2016-11-18 | 2020-12-29 | Merck Sharp & Dohme Corp. | Factor XIIa inhibitors |
CN108239081B (zh) * | 2016-12-26 | 2020-07-28 | 成都先导药物开发股份有限公司 | 一种抑制rock的化合物及其应用 |
CA3083938A1 (en) | 2017-11-29 | 2019-06-06 | The Rockefeller University | Pyranopyrazole and pyrazolopyridine immunomodulators for treatment of autoimmune diseases |
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JP2022552048A (ja) | 2022-12-15 |
IL289863A (en) | 2022-03-01 |
TW202115007A (zh) | 2021-04-16 |
WO2021032933A1 (en) | 2021-02-25 |
MX2022001933A (es) | 2022-03-11 |
CN114269431A (zh) | 2022-04-01 |
AR118082A1 (es) | 2021-09-15 |
KR20220050942A (ko) | 2022-04-25 |
EP4017586A1 (en) | 2022-06-29 |
BR112022001054A2 (pt) | 2022-03-15 |
AU2019462669A1 (en) | 2022-02-24 |
US20220298138A1 (en) | 2022-09-22 |
CA3147564A1 (en) | 2021-02-25 |
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