BR112017017135A2 - inibidores de tgf-beta - Google Patents
inibidores de tgf-betaInfo
- Publication number
- BR112017017135A2 BR112017017135A2 BR112017017135-0A BR112017017135A BR112017017135A2 BR 112017017135 A2 BR112017017135 A2 BR 112017017135A2 BR 112017017135 A BR112017017135 A BR 112017017135A BR 112017017135 A2 BR112017017135 A2 BR 112017017135A2
- Authority
- BR
- Brazil
- Prior art keywords
- tgf
- beta inhibitors
- compound
- prodrugs
- solvates
- Prior art date
Links
- 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
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000000903 blocking effect Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000011664 signaling Effects 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 150000003557 thiazoles Chemical class 0.000 abstract 1
Classifications
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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
-
- 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
-
- 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
-
- 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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- 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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- A61P9/12—Antihypertensives
-
- 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
-
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Biochemistry (AREA)
- Ophthalmology & Optometry (AREA)
- Reproductive Health (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562127109P | 2015-03-02 | 2015-03-02 | |
| US62/127,109 | 2015-03-02 | ||
| PCT/US2016/019830 WO2016140884A1 (en) | 2015-03-02 | 2016-02-26 | TGF-β INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112017017135A2 true BR112017017135A2 (pt) | 2018-04-03 |
Family
ID=55543068
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112017017135-0A BR112017017135A2 (pt) | 2015-03-02 | 2016-02-26 | inibidores de tgf-beta |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US9884868B2 (enExample) |
| EP (1) | EP3265454B1 (enExample) |
| JP (1) | JP6836998B2 (enExample) |
| KR (1) | KR20170122799A (enExample) |
| CN (1) | CN107406412B (enExample) |
| AR (1) | AR103828A1 (enExample) |
| AU (1) | AU2016226468B2 (enExample) |
| BR (1) | BR112017017135A2 (enExample) |
| CA (1) | CA2973602A1 (enExample) |
| CL (1) | CL2017002207A1 (enExample) |
| CO (1) | CO2017009891A2 (enExample) |
| EA (1) | EA037112B1 (enExample) |
| ES (1) | ES2789331T3 (enExample) |
| IL (1) | IL254187A0 (enExample) |
| MX (1) | MX371167B (enExample) |
| MY (1) | MY186133A (enExample) |
| PE (1) | PE20171789A1 (enExample) |
| PH (1) | PH12017501326A1 (enExample) |
| SG (1) | SG11201705821XA (enExample) |
| TN (1) | TN2017000374A1 (enExample) |
| TW (1) | TW201639827A (enExample) |
| WO (1) | WO2016140884A1 (enExample) |
| ZA (1) | ZA201705527B (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112017017135A2 (pt) | 2015-03-02 | 2018-04-03 | Rigel Pharmaceuticals, Inc. | inibidores de tgf-beta |
| 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 |
| EA201991375A1 (ru) | 2016-12-08 | 2020-01-20 | Боард Оф Регентс, Зе Юниверсити Оф Тексас Систем | Бицикло[1.1.1]пентановые ингибиторы киназы, содержащей домен с двумя лейциновыми "застежками-молниями" (dlk), для лечения заболевания |
| WO2018132279A1 (en) | 2017-01-05 | 2018-07-19 | Bristol-Myers Squibb Company | Tgf beta receptor antagonists |
| US11040027B2 (en) | 2017-01-17 | 2021-06-22 | 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 |
| WO2019185631A1 (en) | 2018-03-29 | 2019-10-03 | Masarykova Univerzita | 4—(1h— imidazol— 5— yl) -1h-pyrrolo [2, 3-b] pyridines for use in the treatment of leukaemias, lymphomas and solid tumors |
| US12252531B2 (en) | 2018-07-11 | 2025-03-18 | Scholar Rock, Inc. | Methods of screening for high-affinity, isoform-selective TGFβ1 inhibitors |
| WO2020041562A1 (en) | 2018-08-22 | 2020-02-27 | Clavius Pharmaceuticals, Llc | Substituted imidazoles for the inhibition of tgf-beta and methods of treatment |
| EP3894401A2 (en) * | 2018-12-11 | 2021-10-20 | Theravance Biopharma R&D IP, LLC | Naphthyridine and quinoline derivatives useful as alk5 inhibitors |
| 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 |
| WO2021102468A1 (en) * | 2019-11-22 | 2021-05-27 | Theravance Biopharma R&D Ip, Llc | Substituted 1,5-naphthyridines or quinolines as alk5 inhibitors |
| 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 |
| 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 |
| CA3227334A1 (en) * | 2021-07-28 | 2023-02-02 | Tiumbio Co., Ltd. | Pharmaceutical composition for preventing or treating tumor, and use thereof |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| 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 |
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| WO2025063820A1 (ko) * | 2023-09-21 | 2025-03-27 | 오토텔릭바이오 주식회사 | 티아졸 유도체 화합물을 포함하는 폐섬유화증 치료용 조성물 |
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