CO6620028A2 - Imidazoles 2-piridil sustituidos como inhibidores terapéuticos de alk5 y/o alk 4 - Google Patents
Imidazoles 2-piridil sustituidos como inhibidores terapéuticos de alk5 y/o alk 4Info
- Publication number
- CO6620028A2 CO6620028A2 CO13010451A CO13010451A CO6620028A2 CO 6620028 A2 CO6620028 A2 CO 6620028A2 CO 13010451 A CO13010451 A CO 13010451A CO 13010451 A CO13010451 A CO 13010451A CO 6620028 A2 CO6620028 A2 CO 6620028A2
- Authority
- CO
- Colombia
- Prior art keywords
- alk5
- alk
- pyridyl
- therapeutic inhibitors
- imidazoles substituted
- Prior art date
Links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—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
- 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
- C07D471/04—Ortho-condensed systems
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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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61P9/12—Antihypertensives
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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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
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- Engineering & Computer Science (AREA)
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- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
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- Rheumatology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
- Virology (AREA)
- Dermatology (AREA)
- Hospice & Palliative Care (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Molecular Biology (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Pulmonology (AREA)
Abstract
Esta invención se refiere a imidazoles 2-piridil-sustituidos, que son inhibidores del receptor de tipo I (ALK5) del factor beta de desarrollo transformante (TGF-ß) y/o del receptor tipo 1 de activina (ALK4); a métodos para su preparación y a su uso en medicina, específicamente en el tratamiento y la prevención de un estado de enfermedad mediado por esos receptores.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12/826,338 US8080568B1 (en) | 2010-06-29 | 2010-06-29 | 2-pyridyl substituted imidazoles as therapeutic ALK5 and/or ALK4 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6620028A2 true CO6620028A2 (es) | 2013-02-15 |
Family
ID=45219191
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO13010451A CO6620028A2 (es) | 2010-06-29 | 2013-01-21 | Imidazoles 2-piridil sustituidos como inhibidores terapéuticos de alk5 y/o alk 4 |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US8080568B1 (es) |
| EP (2) | EP2588479B3 (es) |
| JP (1) | JP5732131B2 (es) |
| KR (1) | KR101500665B1 (es) |
| CN (1) | CN103025731B (es) |
| AU (1) | AU2011272149B2 (es) |
| BR (1) | BR112012033334B1 (es) |
| CA (1) | CA2803577C (es) |
| CO (1) | CO6620028A2 (es) |
| DK (2) | DK2588479T6 (es) |
| ES (2) | ES2535876T7 (es) |
| HK (1) | HK1183307A1 (es) |
| HR (1) | HRP20171829T1 (es) |
| HU (1) | HUE036385T2 (es) |
| IL (1) | IL223744A (es) |
| MX (1) | MX2012015260A (es) |
| PL (1) | PL2588479T6 (es) |
| PT (2) | PT2588479E (es) |
| RS (1) | RS56710B1 (es) |
| RU (1) | RU2518069C1 (es) |
| SG (1) | SG186773A1 (es) |
| UA (1) | UA106136C2 (es) |
| WO (1) | WO2012002680A2 (es) |
| ZA (1) | ZA201208662B (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016528295A (ja) | 2013-08-22 | 2016-09-15 | アクセルロン ファーマ， インコーポレイテッド | Ｔｇｆ−ベータ受容体ｉｉ型変異体およびその使用 |
| EP3071215B1 (en) | 2013-11-21 | 2020-01-08 | The Brigham and Women's Hospital, Inc. | Compositions and methods for treating pulmonary hypertension |
| ES2704027T3 (es) * | 2014-05-02 | 2019-03-13 | Lee Sheau Long | Uso de ginsenósido M1 para el tratamiento de nefritis lúpica |
| DK3146062T3 (da) * | 2014-05-16 | 2019-08-12 | Wellhead Biological Tech Corp | Anvendelse af ginsenosid m1 til inhibering af nyrefibrose |
| AU2015296037B2 (en) | 2014-08-01 | 2021-04-29 | The Brigham And Women's Hospital, Inc. | Methods and compositions relating to treatment of pulmonary arterial hypertension |
| JP6631865B2 (ja) * | 2014-08-11 | 2020-01-15 | 日本化薬株式会社 | ＴＧＦβ阻害機能を持つキメラタンパク質 |
| TWI582083B (zh) | 2014-10-07 | 2017-05-11 | 美國禮來大藥廠 | 胺基吡啶基氧基吡唑化合物 |
| JP6581213B2 (ja) * | 2015-02-04 | 2019-09-25 | メドパクト インコーポレイテッド | 慢性骨髄性白血病の予防用または治療用の薬学的組成物、及びそれを利用した方法 |
| KR20160120157A (ko) | 2015-04-07 | 2016-10-17 | 주식회사 메드팩토 | 암 예방 또는 치료용 약학적 조성물 및 이를 이용한 방법 |
| WO2016163754A1 (en) * | 2015-04-07 | 2016-10-13 | Medpacto Inc. | Pharmaceutical composition for preventing or treating cancer and method using thereof |
| JP7320350B2 (ja) | 2015-08-04 | 2023-08-03 | アクセルロン ファーマ インコーポレイテッド | 骨髄増殖性障害を処置するための方法 |
| KR20180094036A (ko) | 2015-12-15 | 2018-08-22 | 브리스톨-마이어스 스큅 컴퍼니 | Cxcr4 수용체 길항제 |
| US11583593B2 (en) | 2016-01-14 | 2023-02-21 | Synthis Therapeutics, Inc. | Antibody-ALK5 inhibitor conjugates and their uses |
| JP6954932B2 (ja) * | 2016-06-13 | 2021-10-27 | ジェンフリート セラピューティクス（シャンハイ）インコーポレイテッド | ＴＧＦ−βＲＩ阻害剤としてのベンゾトリアゾール由来のα、β−不飽和アミド系化合物 |
| KR102434226B1 (ko) | 2016-06-30 | 2022-08-19 | 한미약품 주식회사 | Alk5 억제제로서의 신규 피라졸 유도체 및 이의 용도 |
| CN107663206B (zh) * | 2016-07-29 | 2021-06-18 | 上海璎黎药业有限公司 | 含氮芳香杂环化合物、其制备方法、药物组合物和应用 |
| JP2019534266A (ja) | 2016-10-14 | 2019-11-28 | 江蘇恒瑞医薬股▲ふん▼有限公司 | ５員ヘテロアリール環の架橋した環誘導体、その製造方法およびその医学的使用 |
| MX2019004822A (es) | 2016-11-14 | 2019-09-11 | Jiangsu Hengrui Medicine Co | Derivado del pirazol 3,4-bipiridilo y metodo de preparacion del mismo y aplicacion medica del mismo. |
| WO2018171611A1 (zh) * | 2017-03-22 | 2018-09-27 | 江苏恒瑞医药股份有限公司 | 6-吡唑-[1,2,4]三唑并[4,3-a]吡啶-3-酰胺类衍生物、其制备方法及其在医药上的应用 |
| EP3600294A4 (en) * | 2017-03-23 | 2020-08-26 | Clavius Pharmaceuticals, LLC | TRI-SUBSTITUTED IMIDAZOLES FOR INHIBITION OF TGF-BETA AND TREATMENT METHODS |
| PL3628049T3 (pl) | 2017-05-04 | 2023-09-25 | Acceleron Pharma Inc. | Białka fuzyjne receptora TGF-beta typu II i ich zastosowania |
| US11236112B2 (en) * | 2017-12-13 | 2022-02-01 | Genfleet Therapeutics (Shanghai) Inc. | Crystal form and salt form of TGF-βRI inhibitor and preparation method therefor |
| CN111712244A (zh) * | 2017-12-13 | 2020-09-25 | 学校法人同志社 | 包含(t)ew-7197的治疗或预防角膜内皮疾患的组合物或方法 |
| CN110066277B (zh) | 2018-01-24 | 2021-07-23 | 上海璎黎药业有限公司 | 芳香杂环取代烯烃化合物、其制备方法、药物组合物和应用 |
| CN110066276B (zh) | 2018-01-24 | 2020-09-18 | 上海璎黎药业有限公司 | 芳香杂环化合物、其中间体、制备方法、药物组合物和应用 |
| JP7147048B2 (ja) | 2018-08-22 | 2022-10-04 | クラヴィウス ファーマシューティカルズ，エルエルシー | Ｔｇｆ－ベータを阻害するための置換イミダゾールおよび処置方法 |
| CA3117838A1 (en) | 2018-12-27 | 2020-07-02 | Nexys Therapeutics, Inc. | (pyridin-2-yl)amine derivatives as tgf-beta r1 (alk5) inhibitors for the treatment of cancer |
| JP7335344B2 (ja) * | 2019-01-22 | 2023-08-29 | ビシケム カンパニー リミテッド | Ａｌｋ４／５阻害剤としての縮合環ヘテロアリール化合物 |
| KR102035479B1 (ko) | 2019-04-12 | 2019-10-23 | 한국지질자원연구원 | 점토광물 복합체를 포함하는 방출성이 제어된 경구투여용 조성물 |
| WO2021011834A1 (en) * | 2019-07-16 | 2021-01-21 | Silverback Therapeutics, Inc. | Alk5 inhibitors, conjugates, and uses thereof |
| JP2023514324A (ja) | 2020-02-19 | 2023-04-05 | ナミ セラピューティクス， インコーポレイテッド | がんの処置において有用なＴＦＧβアンタゴニストプロドラッグを含有する製剤化および／または共製剤化リポソーム組成物ならびにその方法 |
| CN114437061B (zh) * | 2020-10-30 | 2023-09-12 | 陕西莱特光电材料股份有限公司 | 双酮类化合物的制备方法和咪唑类衍生物的制备方法 |
| CN112266378B (zh) * | 2020-11-09 | 2021-10-12 | 延边大学 | 含吲唑结构的咪唑类衍生物及其制备方法和应用 |
| US20230047393A1 (en) * | 2021-08-02 | 2023-02-16 | EWHA DrugDesignHouse Co.,Ltd. | Composition containing an alk5 inhibitor, ew-7197 |
| KR102509625B1 (ko) * | 2022-03-25 | 2023-03-14 | 주식회사 메드팩토 | TGF-β 저해제의 합성에 유용한 중간체 및 이를 이용한 TGF-β 저해제 제조방법 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4775762A (en) * | 1987-05-11 | 1988-10-04 | The Dow Chemical Company | Novel (1H-1,2,3-triazol-1-yl)pyridines |
| DE60001229T2 (de) | 1999-04-09 | 2003-10-30 | Smithkline Beecham Corp., Philadelphia | Triarylimidazole |
| AR029803A1 (es) * | 2000-02-21 | 2003-07-16 | Smithkline Beecham Plc | Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden |
| GB0007405D0 (en) | 2000-03-27 | 2000-05-17 | Smithkline Beecham Corp | Compounds |
| GB0100762D0 (en) | 2001-01-11 | 2001-02-21 | Smithkline Beecham Plc | Novel use |
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| JP4959336B2 (ja) * | 2003-10-24 | 2012-06-20 | イーライ リリー アンド カンパニー | ｛２−［１−（３，５−ビストリフルオロメチルベンジル）−５−ピリジン−４−イル−１ｈ−［１，２，３］トリアゾル−４−イル］−ピリジン−３−イル｝−（２−クロロフェニル）−メタノンの新規の結晶形態 |
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| KR100749566B1 (ko) * | 2004-04-21 | 2007-08-16 | 이화여자대학교 산학협력단 | Ａｌｋ5 및/또는 ａｌｋ4 억제제로 유효한 2-피리딜이치환된 이미다졸 유도체 |
| GT200600381A (es) | 2005-08-25 | 2007-03-28 | Compuestos organicos | |
| AR058807A1 (es) * | 2005-09-29 | 2008-02-27 | Astrazeneca Ab | 5-(fenilisoxazoletoxi)-triazol-3-il piridinas sustituidas, para el tratamiento de trastornos mediados por el receptor mglur5 |
| WO2007070866A2 (en) | 2005-12-16 | 2007-06-21 | Alcon, Inc. | Control of intraocular pressure using alk5 modulation agents |
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2010
- 2010-06-29 US US12/826,338 patent/US8080568B1/en not_active Ceased
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2011
- 2011-06-24 RS RS20171245A patent/RS56710B1/sr unknown
- 2011-06-24 ES ES11801087.5T patent/ES2535876T7/es active Active
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- 2011-06-24 DK DK11801087.5T patent/DK2588479T6/en active
- 2011-06-24 AU AU2011272149A patent/AU2011272149B2/en active Active
- 2011-06-24 RU RU2012156261/04A patent/RU2518069C1/ru active
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