SG11201705821XA - TGF-ß INHIBITORS - Google Patents
TGF-ß INHIBITORSInfo
- Publication number
- SG11201705821XA SG11201705821XA SG11201705821XA SG11201705821XA SG11201705821XA SG 11201705821X A SG11201705821X A SG 11201705821XA SG 11201705821X A SG11201705821X A SG 11201705821XA SG 11201705821X A SG11201705821X A SG 11201705821XA SG 11201705821X A SG11201705821X A SG 11201705821XA
- Authority
- SG
- Singapore
- Prior art keywords
- tgf
- inhibitors
- Prior art date
Links
- 102000004887 Transforming Growth Factor beta Human genes 0.000 title 1
- 108090001012 Transforming Growth Factor beta Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 title 1
Classifications
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- A—HUMAN NECESSITIES
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- 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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- 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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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
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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
- 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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- C—CHEMISTRY; METALLURGY
- 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
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Biochemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Vascular Medicine (AREA)
- Oncology (AREA)
- Reproductive Health (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
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 (1)
| Publication Number | Publication Date |
|---|---|
| SG11201705821XA true SG11201705821XA (en) | 2017-08-30 |
Family
ID=55543068
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201705821XA SG11201705821XA (en) | 2015-03-02 | 2016-02-26 | TGF-ß INHIBITORS |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US9884868B2 (https=) |
| EP (1) | EP3265454B1 (https=) |
| JP (1) | JP6836998B2 (https=) |
| KR (1) | KR20170122799A (https=) |
| CN (1) | CN107406412B (https=) |
| AR (1) | AR103828A1 (https=) |
| AU (1) | AU2016226468B2 (https=) |
| BR (1) | BR112017017135A2 (https=) |
| CA (1) | CA2973602A1 (https=) |
| CL (1) | CL2017002207A1 (https=) |
| CO (1) | CO2017009891A2 (https=) |
| EA (1) | EA037112B1 (https=) |
| ES (1) | ES2789331T3 (https=) |
| IL (1) | IL254187A0 (https=) |
| MX (1) | MX371167B (https=) |
| MY (1) | MY186133A (https=) |
| PE (1) | PE20171789A1 (https=) |
| PH (1) | PH12017501326A1 (https=) |
| SG (1) | SG11201705821XA (https=) |
| TN (1) | TN2017000374A1 (https=) |
| TW (1) | TW201639827A (https=) |
| WO (1) | WO2016140884A1 (https=) |
| ZA (1) | ZA201705527B (https=) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA037112B1 (ru) | 2015-03-02 | 2021-02-08 | Ригель Фармасьютикалс, Инк. | Ингибиторы tgf- |
| 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 |
| 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 |
| KR20190087622A (ko) | 2016-12-08 | 2019-07-24 | 보드 오브 리전츠 더 유니버시티 오브 텍사스 시스템 | 질환 치료를 위한 이중 류신 지퍼 (dlk) 키나아제의 바이시클로[1.1.1]펜탄 억제제 |
| WO2018132279A1 (en) | 2017-01-05 | 2018-07-19 | Bristol-Myers Squibb Company | Tgf beta receptor antagonists |
| ES2928773T3 (es) | 2017-01-17 | 2022-11-22 | Heparegenix Gmbh | Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos |
| WO2019005241A1 (en) | 2017-03-23 | 2019-01-03 | Clavius Pharmaceuticals, Llc | TRI-SUBSTITUTED IMIDAZOLES FOR INHIBITION OF TGF-BETA AND METHODS OF TREATMENT |
| 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 |
| CA3085967C (en) | 2018-03-29 | 2022-10-18 | Masarykova Univerzita | 4-(1h-imidazol-5-yl)-1h-pyrrolo[2,3-b]pyridines for use in the treatment of leukaemias, lymphomas and solid tumors |
| MA53125A (fr) | 2018-07-11 | 2021-05-19 | Scholar Rock Inc | Inhibiteurs de tgf?1 sélectifs selon l'isoforme à affinité élevée |
| WO2020041562A1 (en) * | 2018-08-22 | 2020-02-27 | Clavius Pharmaceuticals, Llc | Substituted imidazoles for the inhibition of tgf-beta and methods of treatment |
| BR112021011224A2 (pt) * | 2018-12-11 | 2021-08-24 | Theravance Biopharma R&D Ip, Llc | Inibidores de alk5 |
| CN111825658B (zh) * | 2019-04-18 | 2024-11-08 | 华东理工大学 | 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 |
| KR20220104208A (ko) * | 2019-11-22 | 2022-07-26 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | Alk5 억제제로서 치환된 1,5-나프티리딘 또는 퀴놀린 |
| CN118767143A (zh) | 2019-12-12 | 2024-10-15 | 听治疗有限责任公司 | 用于预防和治疗听力损失的组合物和方法 |
| US12441707B2 (en) | 2019-12-30 | 2025-10-14 | Tyra Biosciences, Inc. | Indazole compounds |
| EP4165041A1 (en) * | 2020-06-10 | 2023-04-19 | Theravance Biopharma R&D IP, LLC | Naphthyridine derivatives useful as alk5 inhibitors |
| 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 |
| CA3227334A1 (en) * | 2021-07-28 | 2023-02-02 | Tiumbio Co., Ltd. | Pharmaceutical composition for preventing or treating tumor, and use thereof |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2024239186A1 (zh) * | 2023-05-22 | 2024-11-28 | 睿健医药科技(苏州)有限公司 | 吡唑甲酰基哌嗪酮类化合物、药物组合物及其应用 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025063820A1 (ko) * | 2023-09-21 | 2025-03-27 | 오토텔릭바이오 주식회사 | 티아졸 유도체 화합물을 포함하는 폐섬유화증 치료용 조성물 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
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