EA201791955A1 - ИНГИБИТОРЫ TGF-β - Google Patents
ИНГИБИТОРЫ TGF-βInfo
- Publication number
- EA201791955A1 EA201791955A1 EA201791955A EA201791955A EA201791955A1 EA 201791955 A1 EA201791955 A1 EA 201791955A1 EA 201791955 A EA201791955 A EA 201791955A EA 201791955 A EA201791955 A EA 201791955A EA 201791955 A1 EA201791955 A1 EA 201791955A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- tgf
- present
- inhibitors
- compound
- prodrugs
- Prior art date
Links
- 102000004887 Transforming Growth Factor beta Human genes 0.000 title abstract 3
- 108090001012 Transforming Growth Factor beta Proteins 0.000 title abstract 3
- 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 abstract 3
- 239000003112 inhibitor Substances 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
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 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
- 239000012453 solvate Substances 0.000 abstract 1
- 150000003557 thiazoles Chemical class 0.000 abstract 1
Classifications
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- 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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- 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
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- 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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- 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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- 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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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Dermatology (AREA)
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- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
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Abstract
В настоящем изобретении раскрыты соединения имидазола и тиазола, а также фармацевтические композиции и способы их применения. Один вариант осуществления относится к соединению структурыи к его фармацевтически приемлемым солям, пролекарствам и N-оксидам (и его сольватам и гидратам), где X, A, Z, Rи R' описаны в настоящем изобретении. Согласно определенным вариантам осуществления раскрытое в настоящем изобретении соединение ингибирует TGF-β и может быть использовано для лечения заболевания путем блокирования сигнала TGF-β.
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 |
|---|---|
| EA201791955A1 true EA201791955A1 (ru) | 2018-01-31 |
| EA037112B1 EA037112B1 (ru) | 2021-02-08 |
Family
ID=55543068
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201791955A EA037112B1 (ru) | 2015-03-02 | 2016-02-26 | Ингибиторы tgf- |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US9884868B2 (ru) |
| EP (1) | EP3265454B1 (ru) |
| JP (1) | JP6836998B2 (ru) |
| KR (1) | KR20170122799A (ru) |
| CN (1) | CN107406412B (ru) |
| AR (1) | AR103828A1 (ru) |
| AU (1) | AU2016226468B2 (ru) |
| BR (1) | BR112017017135A2 (ru) |
| CA (1) | CA2973602A1 (ru) |
| CL (1) | CL2017002207A1 (ru) |
| CO (1) | CO2017009891A2 (ru) |
| EA (1) | EA037112B1 (ru) |
| ES (1) | ES2789331T3 (ru) |
| IL (1) | IL254187A0 (ru) |
| MX (1) | MX371167B (ru) |
| MY (1) | MY186133A (ru) |
| PE (1) | PE20171789A1 (ru) |
| PH (1) | PH12017501326A1 (ru) |
| SG (1) | SG11201705821XA (ru) |
| TN (1) | TN2017000374A1 (ru) |
| TW (1) | TW201639827A (ru) |
| WO (1) | WO2016140884A1 (ru) |
| ZA (1) | ZA201705527B (ru) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2016226468B2 (en) | 2015-03-02 | 2020-10-22 | Bristol-Myers Squibb Company | TGF-beta inhibitors |
| 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 |
| 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 |
| SI3774795T1 (sl) | 2018-03-29 | 2022-07-29 | Masarykova Univerzita | 4-(1H-imidazol-5-il)-1H-pirolo (2,3-B) piridini za uporabo pri zdravljenju levkemij, limfomov in trdnih tumorjev |
| AU2019302679A1 (en) | 2018-07-11 | 2021-02-11 | Scholar Rock, Inc. | High-affinity, isoform-selective TGFbeta1 inhibitors and use thereof |
| 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 |
| MA54448A (fr) | 2018-12-11 | 2021-10-20 | Theravance Biopharma R&D Ip Llc | Dérivés naphthyridine et quinoléine en tant qu'inhibiteurs 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 |
| CA3160307A1 (en) | 2019-11-22 | 2021-05-27 | Theravance Biopharma R&D Ip, Llc | Substituted 1,5-naphthyridines or quinolines as alk5 inhibitors |
| WO2021118924A2 (en) | 2019-12-12 | 2021-06-17 | Ting Therapeutics Llc | Compositions and methods for the prevention and treatment of hearing loss |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | 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 |
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