EA201190237A1 - Аналоги изоксазол-3(2н)-она в качестве терапевтических агентов - Google Patents
Аналоги изоксазол-3(2н)-она в качестве терапевтических агентовInfo
- Publication number
- EA201190237A1 EA201190237A1 EA201190237A EA201190237A EA201190237A1 EA 201190237 A1 EA201190237 A1 EA 201190237A1 EA 201190237 A EA201190237 A EA 201190237A EA 201190237 A EA201190237 A EA 201190237A EA 201190237 A1 EA201190237 A1 EA 201190237A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- optionally substituted
- deuterium
- heteroaryl
- aryl
- Prior art date
Links
Classifications
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
-
- 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
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
-
- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Pregnancy & Childbirth (AREA)
- Gastroenterology & Hepatology (AREA)
- Gynecology & Obstetrics (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Соединение I или его фармацевтически приемлемая соль, где R1 и R2 независимо представляют собой водород, дейтерий, арил, гетероарил, C-C-алкил, возможно замещенный одним или более заместителями, независимо представляющими собой R3, R3 представляет собой арил, гетероарил, фтор, C-C-алкил, содержащий один или более чем один фтор, C-C-алкил, содержащий один или более чем один дейтерий, C-C-алкил, содержащий гидрокси, где арил и гетероарил возможно замещены одним или более чем одним галогеном, фторированным алкокси, фторированным алкилом, сульфонилом, одним или более чем одним дейтерием, Cалкилом, Cалкокси, нитрилом, или R3 представляет собой C-алкил, возможно замещенный одной или более из следующих групп: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; где R4 представляет собой Cалкил, возможно замещенный одним или более чем одним фтором, дейтерием, алкокси, арилкарбоксилатом, алкилкарбоксилатом; R5 и R6 независимо выбраны из водорода, алкила или они могут вместе образовывать 4-8-членное углеродное кольцо; или R1 и R2 образуют 3-10-членное углеродное кольцо, возможно содержащее О или N и возможно замещенное Cалкилом или арилом, гетероарилом, возможно замещенным R3.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16722409P | 2009-04-07 | 2009-04-07 | |
| US17195609P | 2009-04-23 | 2009-04-23 | |
| PCT/SE2010/050375 WO2010117323A1 (en) | 2009-04-07 | 2010-04-06 | Method and apparatus for producing heat energy and carbon dioxide |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201190237A1 true EA201190237A1 (ru) | 2012-04-30 |
| EA020825B1 EA020825B1 (ru) | 2015-02-27 |
Family
ID=42934883
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201190237A EA020825B1 (ru) | 2009-04-07 | 2010-04-06 | Аналоги изоксазол-3(2h)-она в качестве терапевтических агентов |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8415378B2 (ru) |
| EP (1) | EP2417131A4 (ru) |
| JP (1) | JP5711723B2 (ru) |
| KR (1) | KR101675607B1 (ru) |
| CN (1) | CN102459246B (ru) |
| AR (1) | AR076219A1 (ru) |
| AU (1) | AU2010235236B2 (ru) |
| BR (1) | BRPI1013984A2 (ru) |
| CA (1) | CA2757879C (ru) |
| CO (1) | CO6440580A2 (ru) |
| CU (1) | CU20110190A7 (ru) |
| EA (1) | EA020825B1 (ru) |
| EC (1) | ECSP11011385A (ru) |
| IL (1) | IL215336A0 (ru) |
| MX (1) | MX2011010647A (ru) |
| NI (1) | NI201100181A (ru) |
| SG (1) | SG174463A1 (ru) |
| TW (1) | TW201040166A (ru) |
| UY (1) | UY32543A (ru) |
| WO (1) | WO2010117323A1 (ru) |
| ZA (1) | ZA201108119B (ru) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2009279787B2 (en) | 2008-08-04 | 2014-05-29 | Chdi Foundation, Inc. | Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| MX2012008346A (es) | 2010-01-25 | 2012-11-12 | Chdi Foundation Inc | Determinados inhibidores de cinurenina-3-monooxigenasa, composiciones farmceuticas y metodos de uso de los mismos. |
| WO2012047156A1 (en) * | 2010-10-04 | 2012-04-12 | Astrazeneca Ab | Isoxazol-3(2h)-one analogs as plasminogen inhibitors and their use in the treatment of fibrinolysis related diseases |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| SG2014012926A (en) * | 2011-08-30 | 2014-06-27 | Chdi Foundation Inc | Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| AU2012300246A1 (en) | 2011-08-30 | 2014-03-06 | Chdi Foundation, Inc. | Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| US9073881B2 (en) | 2011-09-23 | 2015-07-07 | Hoffmann-La Roche Inc. | Benzoic acid derivatives |
| CN107652289B (zh) | 2012-06-13 | 2020-07-21 | 因塞特控股公司 | 作为fgfr抑制剂的取代的三环化合物 |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| CN102977040B (zh) * | 2012-11-20 | 2015-06-03 | 浙江工业大学 | 一种2-喹喔啉基二甲缩醛和2-喹喔啉基甲醛的合成方法 |
| CN102977050B (zh) * | 2012-11-20 | 2015-04-22 | 浙江工业大学 | 一种2-苯并噻唑二甲缩醛和2-苯并噻唑甲醛的合成方法 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| JP6449244B2 (ja) | 2013-04-19 | 2019-01-09 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｆｇｆｒ抑制剤としての二環式複素環 |
| UY35809A (es) | 2013-11-05 | 2015-05-29 | Bayer Pharma AG | (aza)piridopirazolopirimidinonas e indazolopirimidinonas y sus usos |
| US10258621B2 (en) | 2014-07-17 | 2019-04-16 | Chdi Foundation, Inc. | Methods and compositions for treating HIV-related disorders |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| US10118930B2 (en) | 2014-11-03 | 2018-11-06 | Bayer Pharma Aktiengesellschaft | Piperidinylpyrazolopyrimidinones and their use |
| WO2016099397A1 (en) | 2014-12-19 | 2016-06-23 | Emeriti Pharma Ab | 3-(piperidin-4-yl)-isoxazol-3(2h)-ones for treatment of dermatologic disorders |
| WO2016134320A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CN104725300A (zh) * | 2015-02-28 | 2015-06-24 | 宁波九胜创新医药科技有限公司 | 一种1-(6-甲基吡啶-3-基)-2-(4-甲磺酰基苯基)乙酮的制备方法 |
| WO2016173948A1 (en) | 2015-04-30 | 2016-11-03 | Bayer Pharma Aktiengesellschaft | Indazolopyrimidinones as fibrinolysis inhibitors |
| CN107459514B (zh) * | 2016-06-06 | 2020-10-23 | 南开大学 | 一类手性哌啶衍生物及其制备方法和用途 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CN107857725A (zh) * | 2017-12-19 | 2018-03-30 | 苏州艾缇克药物化学有限公司 | 一种2‑氨基吡啶‑4‑甲醇的合成方法 |
| SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
| DK3788047T3 (da) | 2018-05-04 | 2024-09-16 | Incyte Corp | Faste former af en FGFR-inhibitor og fremgangsmåder til fremstilling deraf |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| MX2022004513A (es) | 2019-10-14 | 2022-07-19 | Incyte Corp | Heterociclos biciclicos como inhibidores de los receptores del factor de crecimiento de fibroblastos (fgfr). |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP2023505258A (ja) | 2019-12-04 | 2023-02-08 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式複素環 |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2022166845A1 (zh) * | 2021-02-05 | 2022-08-11 | 赛诺哈勃药业（成都）有限公司 | 一种纤溶酶抑制剂、其制备方法及应用 |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUT74690A (en) * | 1993-11-24 | 1997-01-28 | Du Pont Merck Pharma | Novel isoxazoline and isoxazole fibrinogen receptor antagonists process for producing them and pharmaceutical compositions containing them |
| WO2000029406A2 (en) | 1998-11-18 | 2000-05-25 | Du Pont Pharmaceuticals Company | Novel isoxazoline fibrinogen receptor antagonists |
| US20030207873A1 (en) * | 2002-04-10 | 2003-11-06 | Edmund Harrington | Inhibitors of Src and other protein kinases |
| PT1615699E (pt) * | 2003-04-15 | 2010-05-21 | Merck Sharp & Dohme | Moduladores benzoxazinil-amidociclopentil-heterocíclicos dos receptores de quemoquina |
| US7598243B2 (en) * | 2003-04-17 | 2009-10-06 | Merck & Co., Inc. | Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity |
| CN101328173B (zh) * | 2008-07-31 | 2010-12-15 | 石药集团欧意药业有限公司 | 一种制备6-氟-3-(4-哌啶基)-1,2-苯并异噁唑盐酸盐的方法 |
-
2010
- 2010-04-06 JP JP2012504655A patent/JP5711723B2/ja not_active Expired - Fee Related
- 2010-04-06 CA CA2757879A patent/CA2757879C/en not_active Expired - Fee Related
- 2010-04-06 US US12/755,010 patent/US8415378B2/en not_active Expired - Fee Related
- 2010-04-06 EA EA201190237A patent/EA020825B1/ru not_active IP Right Cessation
- 2010-04-06 SG SG2011067568A patent/SG174463A1/en unknown
- 2010-04-06 MX MX2011010647A patent/MX2011010647A/es active IP Right Grant
- 2010-04-06 TW TW099110636A patent/TW201040166A/zh unknown
- 2010-04-06 EP EP10761933.0A patent/EP2417131A4/en not_active Withdrawn
- 2010-04-06 CN CN201080025847.5A patent/CN102459246B/zh not_active Expired - Fee Related
- 2010-04-06 WO PCT/SE2010/050375 patent/WO2010117323A1/en active Application Filing
- 2010-04-06 UY UY0001032543A patent/UY32543A/es not_active Application Discontinuation
- 2010-04-06 KR KR1020117026407A patent/KR101675607B1/ko active IP Right Grant
- 2010-04-06 BR BRPI1013984A patent/BRPI1013984A2/pt not_active Application Discontinuation
- 2010-04-06 AU AU2010235236A patent/AU2010235236B2/en not_active Ceased
- 2010-04-07 AR ARP100101162A patent/AR076219A1/es unknown
-
2011
- 2011-09-22 IL IL215336A patent/IL215336A0/en unknown
- 2011-10-06 CO CO11132448A patent/CO6440580A2/es not_active Application Discontinuation
- 2011-10-07 CU CU20110190A patent/CU20110190A7/es unknown
- 2011-10-07 EC EC2011011385A patent/ECSP11011385A/es unknown
- 2011-10-07 NI NI201100181A patent/NI201100181A/es unknown
- 2011-11-04 ZA ZA2011/08119A patent/ZA201108119B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2012522836A (ja) | 2012-09-27 |
| NI201100181A (es) | 2012-06-14 |
| UY32543A (es) | 2010-11-30 |
| WO2010117323A1 (en) | 2010-10-14 |
| ECSP11011385A (es) | 2011-11-30 |
| KR101675607B1 (ko) | 2016-11-11 |
| KR20120034611A (ko) | 2012-04-12 |
| IL215336A0 (en) | 2011-12-29 |
| MX2011010647A (es) | 2012-02-21 |
| BRPI1013984A2 (pt) | 2018-06-19 |
| AR076219A1 (es) | 2011-05-26 |
| AU2010235236A1 (en) | 2011-10-20 |
| CN102459246B (zh) | 2014-05-07 |
| TW201040166A (en) | 2010-11-16 |
| CN102459246A (zh) | 2012-05-16 |
| CU20110190A7 (es) | 2012-02-15 |
| JP5711723B2 (ja) | 2015-05-07 |
| EA020825B1 (ru) | 2015-02-27 |
| US20100261755A1 (en) | 2010-10-14 |
| AU2010235236B2 (en) | 2013-10-24 |
| EP2417131A1 (en) | 2012-02-15 |
| EP2417131A4 (en) | 2014-08-27 |
| SG174463A1 (en) | 2011-10-28 |
| US8415378B2 (en) | 2013-04-09 |
| CA2757879A1 (en) | 2010-10-14 |
| CA2757879C (en) | 2017-06-06 |
| CO6440580A2 (es) | 2012-05-15 |
| WO2010117323A8 (en) | 2010-11-18 |
| ZA201108119B (en) | 2012-07-25 |
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