MX2017010735A - Inhibidores de inhibidores del factor beta de crecimiento de transformacion (tgf-beta). - Google Patents
Inhibidores de inhibidores del factor beta de crecimiento de transformacion (tgf-beta).Info
- Publication number
- MX2017010735A MX2017010735A MX2017010735A MX2017010735A MX2017010735A MX 2017010735 A MX2017010735 A MX 2017010735A MX 2017010735 A MX2017010735 A MX 2017010735A MX 2017010735 A MX2017010735 A MX 2017010735A MX 2017010735 A MX2017010735 A MX 2017010735A
- Authority
- MX
- Mexico
- Prior art keywords
- tgf
- inhibitors
- compound
- disclosed
- prodrugs
- Prior art date
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- 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
- C07D401/02—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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—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
- C07D417/02—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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
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- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
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- Gastroenterology & Hepatology (AREA)
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Abstract
La presente invención se refiere a compuestos de imidazol y tiazol, así como también a composiciones farmacéuticas y métodos de uso de los mismos. Una modalidad es un compuesto que tiene la estructura de Fórmula (I) y sales, profármacos y N-óxidos de los mismos farmacéuticamente aceptables (y solvatos e hidratos de los mismos), en donde X, A, Z, R1 y R´ son como se describen en la presente. En ciertas modalidades, un compuesto descrito en la presente inhibe a TGF-ß, y puede ser usado para tratar enfermedades bloqueando la señalización del TGF-ß.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562127109P | 2015-03-02 | 2015-03-02 | |
| PCT/US2016/019830 WO2016140884A1 (en) | 2015-03-02 | 2016-02-26 | TGF-β INHIBITORS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2017010735A true MX2017010735A (es) | 2017-12-04 |
| MX371167B MX371167B (es) | 2020-01-21 |
Family
ID=55543068
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017010735A MX371167B (es) | 2015-03-02 | 2016-02-26 | Inhibidores de inhibidores del factor beta de crecimiento de transformacion (tgf-beta). |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US9884868B2 (es) |
| EP (1) | EP3265454B1 (es) |
| JP (1) | JP6836998B2 (es) |
| KR (1) | KR20170122799A (es) |
| CN (1) | CN107406412B (es) |
| AR (1) | AR103828A1 (es) |
| AU (1) | AU2016226468B2 (es) |
| BR (1) | BR112017017135A2 (es) |
| CA (1) | CA2973602A1 (es) |
| CL (1) | CL2017002207A1 (es) |
| CO (1) | CO2017009891A2 (es) |
| EA (1) | EA037112B1 (es) |
| ES (1) | ES2789331T3 (es) |
| HK (1) | HK1244785A1 (es) |
| IL (1) | IL254187A0 (es) |
| MX (1) | MX371167B (es) |
| MY (1) | MY186133A (es) |
| PE (1) | PE20171789A1 (es) |
| PH (1) | PH12017501326A1 (es) |
| SG (1) | SG11201705821XA (es) |
| TN (1) | TN2017000374A1 (es) |
| TW (1) | TW201639827A (es) |
| WO (1) | WO2016140884A1 (es) |
| ZA (1) | ZA201705527B (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2789331T3 (es) | 2015-03-02 | 2020-10-26 | Rigel Pharmaceuticals Inc | Inhibidores de TGF-beta |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療 |
| CA3045947A1 (en) | 2016-12-08 | 2018-06-14 | Michael J. Soth | Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (dlk) kinase for the treatment of disease |
| US10961239B2 (en) | 2017-01-05 | 2021-03-30 | Bristol-Myers Squibb Company | TGF beta receptor antagonists |
| NZ755835A (en) | 2017-01-17 | 2023-12-22 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| JP2020512400A (ja) * | 2017-03-23 | 2020-04-23 | クラヴィウス ファーマシューティカルズ，エルエルシー | ＴＧＦβの阻害のための三置換イミダゾールおよび治療方法 |
| CN109293652B (zh) * | 2017-07-24 | 2021-10-22 | 四川科伦博泰生物医药股份有限公司 | 一种取代的噻唑衍生物及其用途 |
| GB201718285D0 (en) | 2017-11-03 | 2017-12-20 | Discuva Ltd | Antibacterial Compounds |
| AU2019246220B2 (en) | 2018-03-29 | 2020-10-08 | Masarykova Univerzita | 4—(1h— imidazol— 5— yl) -1h-pyrrolo (2, 3-b) pyridines for use in the treatment of leukaemias, lymphomas and solid tumors |
| EP3840748A4 (en) | 2018-08-22 | 2022-06-29 | Clavius Pharmaceuticals, LLC | Substituted imidazoles for the inhibition of tgf-beta and methods of treatment |
| AU2019396360A1 (en) * | 2018-12-11 | 2021-05-27 | Theravance Biopharma R&D Ip, Llc | Naphthyridine and quinoline derivatives useful as ALK5 inhibitors |
| CN111825658A (zh) * | 2019-04-18 | 2020-10-27 | 华东理工大学 | 新型egfr三突变抑制剂及其应用 |
| US11560366B2 (en) | 2019-10-21 | 2023-01-24 | Board Of Regents, The University Of Texas System | Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease |
| TW202132297A (zh) * | 2019-11-22 | 2021-09-01 | 美商施萬生物製藥研發Ｉｐ有限責任公司 | 經取代吡啶及使用方法 |
| JP2023506768A (ja) | 2019-12-12 | 2023-02-20 | ティン セラピューティックス エルエルシー | 聴覚損失の予防及び治療のための組成物及び方法 |
| TW202214623A (zh) * | 2020-06-10 | 2022-04-16 | 美商施萬生物製藥研發 Ip有限責任公司 | 結晶型alk5抑制劑及其用途 |
| CN112321592B (zh) * | 2020-11-12 | 2022-03-04 | 山东省科学院菏泽分院 | 一种6-氯咪唑并[1,2-b]哒嗪-3-甲腈的合成方法 |
| WO2022251359A1 (en) * | 2021-05-26 | 2022-12-01 | Theravance Biopharma R&D Ip, Llc | Bicyclic inhibitors of alk5 and methods of use |
| CN117999077A (zh) * | 2021-07-28 | 2024-05-07 | 株式会社蒂奥姆生物 | 用于预防或治疗肿瘤的药物组合物及其用途 |
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| NZ513642A (en) | 1999-01-21 | 2004-02-27 | Metamorphix Inc | Growth differentiation factor inhibitors and uses therefor |
| AU2002225730A1 (en) * | 2000-11-16 | 2002-05-27 | Smith Kline Beecham Corporation | Compounds |
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| US7320789B2 (en) | 2001-09-26 | 2008-01-22 | Wyeth | Antibody inhibitors of GDF-8 and uses thereof |
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| TWI380996B (zh) | 2004-09-17 | 2013-01-01 | Hoffmann La Roche | 抗ｏｘ４０ｌ抗體 |
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| WO2008036642A2 (en) | 2006-09-19 | 2008-03-27 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
| CL2007002650A1 (es) | 2006-09-19 | 2008-02-08 | Incyte Corp | Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras. |
| EP1987839A1 (en) | 2007-04-30 | 2008-11-05 | I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale | Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease |
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