MX2012015260A - Imidazoles 2-piridil-sustituidos como inhibidores terapeuticos de alk5 y/o alk4. - Google Patents
Imidazoles 2-piridil-sustituidos como inhibidores terapeuticos de alk5 y/o alk4.Info
- Publication number
- MX2012015260A MX2012015260A MX2012015260A MX2012015260A MX2012015260A MX 2012015260 A MX2012015260 A MX 2012015260A MX 2012015260 A MX2012015260 A MX 2012015260A MX 2012015260 A MX2012015260 A MX 2012015260A MX 2012015260 A MX2012015260 A MX 2012015260A
- Authority
- MX
- Mexico
- Prior art keywords
- pyridyl substituted
- substituted imidazoles
- alk5
- alk4
- inhibitors
- Prior art date
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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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- 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)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
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- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Virology (AREA)
- Reproductive Health (AREA)
- Hospice & Palliative Care (AREA)
- AIDS & HIV (AREA)
- Gastroenterology & Hepatology (AREA)
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- Tropical Medicine & Parasitology (AREA)
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- Vascular Medicine (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 I 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 (2)
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 |
PCT/KR2011/004631 WO2012002680A2 (en) | 2010-06-29 | 2011-06-24 | 2-pyridyl substituted imidazoles as therapeutic alk5 and/or alk4 inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2012015260A true MX2012015260A (es) | 2013-04-03 |
Family
ID=45219191
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2012015260A MX2012015260A (es) | 2010-06-29 | 2011-06-24 | Imidazoles 2-piridil-sustituidos como inhibidores terapeuticos de alk5 y/o alk4. |
Country Status (24)
Country | Link |
---|---|
US (2) | US8080568B1 (es) |
EP (2) | EP2947081B1 (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) | DK2947081T3 (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) |
Families Citing this family (34)
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EP3036262A4 (en) | 2013-08-22 | 2017-03-01 | Acceleron Pharma Inc. | Tgf-beta receptor type ii variants and uses thereof |
EP3685848B1 (en) | 2013-11-21 | 2021-09-15 | 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 |
JP6626094B2 (ja) * | 2014-05-16 | 2019-12-25 | ウェルヘッド バイオロジカル テクノロジー コーポレイション | 腎線維症を抑制するためのジンセノサイドm1の使用 |
EP3174550B1 (en) | 2014-08-01 | 2020-01-29 | 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 |
WO2016126028A1 (en) * | 2015-02-04 | 2016-08-11 | Medpacto Inc. | Pharmaceutical composition for preventing or treating chronic myeloid leukemia and method using the same |
WO2016163754A1 (en) * | 2015-04-07 | 2016-10-13 | Medpacto Inc. | Pharmaceutical composition for preventing or treating cancer and method using thereof |
KR20160120157A (ko) * | 2015-04-07 | 2016-10-17 | 주식회사 메드팩토 | 암 예방 또는 치료용 약학적 조성물 및 이를 이용한 방법 |
CN108348578B (zh) | 2015-08-04 | 2022-08-09 | 阿塞勒隆制药公司 | 用于治疗骨髓增生性病症的方法 |
EP3390406A1 (en) | 2015-12-15 | 2018-10-24 | Bristol-Myers Squibb Company | Cxcr4 receptor antagonists |
US11583593B2 (en) | 2016-01-14 | 2023-02-21 | Synthis Therapeutics, Inc. | Antibody-ALK5 inhibitor conjugates and their uses |
AU2017284124B2 (en) * | 2016-06-13 | 2021-06-03 | Genfleet Therapeutics (Shanghai) Inc. | Benzotriazole-derived α and β unsaturated amide compound used as TGF-βR1 inhibitor |
KR102434226B1 (ko) | 2016-06-30 | 2022-08-19 | 한미약품 주식회사 | Alk5 억제제로서의 신규 피라졸 유도체 및 이의 용도 |
EP3492461A4 (en) | 2016-07-29 | 2020-02-12 | Shanghai Yingli Pharmaceutical Co. Ltd. | NITROGEN HETEROCYCLIC AROMATIC COMPOUND, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION THEREOF AND APPLICATION THEREOF |
EP3527570A4 (en) * | 2016-10-14 | 2020-04-15 | Jiangsu Hengrui Medicine Co., Ltd. | FIVE-LINKED HETERARYARYLE CYCLE BRIDGE DERIVATIVE, METHOD FOR PREPARING SAME, AND MEDICAL USE THEREOF |
CA3043383A1 (en) | 2016-11-14 | 2018-05-17 | Jiangsu Hengrui Medicine Co., Ltd. | 3,4-bipyridyl pyrazole derivative, and preparation method therefor and medical application thereof |
CN109983015B (zh) * | 2017-03-22 | 2021-09-03 | 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 |
US11124509B2 (en) | 2017-03-23 | 2021-09-21 | Clavius Pharmaceuticals, LLC. | Tri-substituted imidazoles for the inhibition of TGF beta and methods of treatment |
EP4241848A3 (en) | 2017-05-04 | 2023-11-01 | Acceleron Pharma Inc. | Tgf-beta receptor type ii fusion proteins and uses thereof |
RU2750702C1 (ru) * | 2017-12-13 | 2021-07-01 | Джинфлит Терапьютикс (Шанхай) Инк. | КРИСТАЛЛИЧЕСКАЯ ФОРМА И СОЛЕВАЯ ФОРМА ИНГИБИТОРА TGF-βRI И СПОСОБ ИХ ПОЛУЧЕНИЯ |
EP3725313A4 (en) * | 2017-12-13 | 2021-11-24 | The Doshisha | COMPOSITION OR PROCESS INCLUDING (T) EW-7197 FOR THE PROPHYLACTIC OR THERAPEUTIC TREATMENT OF CORNEAL ENDOTHELIAL DISEASES |
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 |
BR112021007006A2 (pt) | 2018-12-27 | 2021-08-10 | Nexys Therapeutics, Inc. | derivados de (piridin-2-il)amina como inibidores de tgf-beta r1(alk5) para o tratamento de câncer |
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 |
KR102035481B1 (ko) | 2019-04-12 | 2019-10-23 | 한국지질자원연구원 | 점토광물 복합체를 포함하는 염증성 대장염의 예방, 개선 및 치료용 조성물 |
EP3999501A1 (en) * | 2019-07-16 | 2022-05-25 | Silverback Therapeutics, Inc. | Alk5 inhibitors, conjugates, and uses thereof |
AU2021223336A1 (en) | 2020-02-19 | 2022-10-06 | Nammi Therapeutics, Inc. | Formulated and/or co-formulated liposome compositions containing TGFB antagonist prodrugs useful in the treatment of cancer and methods thereof |
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 |
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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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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 | 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 |
JPWO2002096875A1 (ja) | 2001-05-25 | 2004-09-09 | 持田製薬株式会社 | 鎮痛作用を有する4−ヒドロキシピペリジン誘導体 |
US6514989B1 (en) * | 2001-07-20 | 2003-02-04 | Hoffmann-La Roche Inc. | Aromatic and heteroaromatic substituted 1,2,4-triazolo pyridine derivatives |
AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
MY139563A (en) * | 2002-09-04 | 2009-10-30 | Bristol Myers Squibb Co | Heterocyclic aromatic compounds useful as growth hormone secretagogues |
PL375980A1 (en) * | 2002-09-18 | 2005-12-12 | Pfizer Products Inc. | Novel imidazole compounds as transforming growth factor (tgf) inhibitors |
EA008881B1 (ru) * | 2003-10-24 | 2007-08-31 | Эли Лилли Энд Компани | Новые кристаллические формы {2-[1-(3,5-бис-трифторметилбензил)-5-пиридин-4-ил-1h-[1,2,3]триазол-4-ил]пиридин-3-ил}-(2-хлорфенил)метанона |
US20080319012A1 (en) * | 2004-04-21 | 2008-12-25 | In2Gen Co., Ltd. | 2-Pyridyl substituted imidazoles as ALK5 and/or ALK4 inhibitors |
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 |
KR20080082618A (ko) | 2005-12-16 | 2008-09-11 | 알콘, 인코퍼레이티드 | Alk5 조절제를 사용한 안압의 조절 |
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2010
- 2010-06-29 US US12/826,338 patent/US8080568B1/en not_active Ceased
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2011
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- 2011-06-24 EP EP15157476.1A patent/EP2947081B1/en active Active
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