EA026894B1 - ИНГИБИТОРЫ БРОМОДОМЕНА НА ОСНОВЕ БЕНЗО[c]ИЗОКСАЗОЛАЗЕПИНА И ИХ ПРИМЕНЕНИЕ - Google Patents
ИНГИБИТОРЫ БРОМОДОМЕНА НА ОСНОВЕ БЕНЗО[c]ИЗОКСАЗОЛАЗЕПИНА И ИХ ПРИМЕНЕНИЕ Download PDFInfo
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- EA026894B1 EA026894B1 EA201492216A EA201492216A EA026894B1 EA 026894 B1 EA026894 B1 EA 026894B1 EA 201492216 A EA201492216 A EA 201492216A EA 201492216 A EA201492216 A EA 201492216A EA 026894 B1 EA026894 B1 EA 026894B1
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- Prior art keywords
- cancer
- compound
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- methyl
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- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 description 1
- AQTQHPDCURKLKT-JKDPCDLQSA-N vincristine sulfate Chemical compound OS(O)(=O)=O.C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C=O)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 AQTQHPDCURKLKT-JKDPCDLQSA-N 0.000 description 1
- 229960002110 vincristine sulfate Drugs 0.000 description 1
- GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 description 1
- 229960002066 vinorelbine Drugs 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 210000001260 vocal cord Anatomy 0.000 description 1
- WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 description 1
- 229960000237 vorinostat Drugs 0.000 description 1
- XLMPPFTZALNBFS-INIZCTEOSA-N vorozole Chemical compound C1([C@@H](C2=CC=C3N=NN(C3=C2)C)N2N=CN=C2)=CC=C(Cl)C=C1 XLMPPFTZALNBFS-INIZCTEOSA-N 0.000 description 1
- 201000005102 vulva cancer Diseases 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 239000010497 wheat germ oil Substances 0.000 description 1
- 235000021119 whey protein Nutrition 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
- 229960004276 zoledronic acid Drugs 0.000 description 1
- XRASPMIURGNCCH-UHFFFAOYSA-N zoledronic acid Chemical compound OP(=O)(O)C(P(O)(O)=O)(O)CN1C=CN=C1 XRASPMIURGNCCH-UHFFFAOYSA-N 0.000 description 1
- CGTADGCBEXYWNE-JUKNQOCSSA-N zotarolimus Chemical compound N1([C@H]2CC[C@@H](C[C@@H](C)[C@H]3OC(=O)[C@@H]4CCCCN4C(=O)C(=O)[C@@]4(O)[C@H](C)CC[C@H](O4)C[C@@H](/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C3)OC)C[C@H]2OC)C=NN=N1 CGTADGCBEXYWNE-JUKNQOCSSA-N 0.000 description 1
- 229950009819 zotarolimus Drugs 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Classifications
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/42—Oxazoles
- A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Virology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261656205P | 2012-06-06 | 2012-06-06 | |
| PCT/US2013/044444 WO2013184876A1 (en) | 2012-06-06 | 2013-06-06 | Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201492216A1 EA201492216A1 (ru) | 2015-03-31 |
| EA026894B1 true EA026894B1 (ru) | 2017-05-31 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201492216A EA026894B1 (ru) | 2012-06-06 | 2013-06-06 | ИНГИБИТОРЫ БРОМОДОМЕНА НА ОСНОВЕ БЕНЗО[c]ИЗОКСАЗОЛАЗЕПИНА И ИХ ПРИМЕНЕНИЕ |
Country Status (19)
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|---|---|
| US (2) | US9493483B2 (Direct) |
| EP (1) | EP2859000B1 (Direct) |
| JP (1) | JP6154004B2 (Direct) |
| KR (1) | KR20150023562A (Direct) |
| CN (1) | CN104428304B (Direct) |
| AR (1) | AR091285A1 (Direct) |
| AU (1) | AU2013271569B2 (Direct) |
| BR (1) | BR112014030165A2 (Direct) |
| CA (1) | CA2874774C (Direct) |
| EA (1) | EA026894B1 (Direct) |
| ES (1) | ES2632774T3 (Direct) |
| IL (1) | IL235844A (Direct) |
| IN (1) | IN2014DN10386A (Direct) |
| MX (1) | MX360598B (Direct) |
| NZ (1) | NZ702458A (Direct) |
| SG (1) | SG11201407900WA (Direct) |
| TW (1) | TWI602820B (Direct) |
| WO (1) | WO2013184876A1 (Direct) |
| ZA (1) | ZA201408720B (Direct) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11629152B2 (en) | 2018-03-30 | 2023-04-18 | Kyowa Kirin Co., Ltd. | Compound with anticancer activity |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR084070A1 (es) * | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| EP2864336B1 (en) | 2012-06-06 | 2016-11-23 | Constellation Pharmaceuticals, Inc. | Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof |
| AP2015008673A0 (en) | 2013-02-19 | 2015-08-31 | Bayer Pharma Aktiengesellchaft | Bicyclo 2,3-benzodiazepines and spirocyclically substituted 2,3-benzodiazepines |
| CA2901799A1 (en) | 2013-02-22 | 2014-08-28 | Bayer Pharma Aktiengesellschaft | Pyrrolo- and pyrazolo-triazolodiazepines as bet-protein inhibitors for treating hyperproliferative diseases |
| HK1212345A1 (en) | 2013-02-22 | 2016-06-10 | Bayer Pharma Aktiengesellschaft | 4-substituted pyrrolo- and pyrazolo-diazepines |
| AR095326A1 (es) | 2013-03-15 | 2015-10-07 | Incyte Corp | Heterociclos tricíclicos como inhibidores de la proteína bet |
| CA2917319A1 (en) | 2013-07-08 | 2015-01-15 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| EP3125896A2 (en) * | 2014-04-04 | 2017-02-08 | Constellation Pharmaceuticals, Inc. | EXPRESSION LEVELS OF BCL-xL, BCL2, BCL-w, AND BAD AND CANCER THERAPIES |
| KR102430144B1 (ko) | 2014-04-23 | 2022-08-08 | 인사이트 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| WO2015195863A1 (en) * | 2014-06-20 | 2015-12-23 | Constellation Pharmaceuticals, Inc. | Hydrated 2-((4s)-6-(4-chlorophenyl)-1 -methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide |
| WO2016044130A1 (en) | 2014-09-15 | 2016-03-24 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| MX2017016337A (es) | 2015-06-26 | 2018-11-22 | Tensha Therapeutics Inc | Tratamiento de carcinoma de linea media nut. |
| KR102759651B1 (ko) * | 2015-09-09 | 2025-02-03 | 주빌란트 바이오시스 리미티드 | 삼환식 축합피리딘-2－온 유도체 및 이들의 brd4 저해제로서의 용도 |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| US11225481B2 (en) | 2015-12-29 | 2022-01-18 | Centre National De La Recherche Scientifique | Xanthine derivative inhibitors of BET proteins |
| TWI830533B (zh) | 2016-06-20 | 2024-01-21 | 美商英塞特公司 | Ｂｅｔ抑制劑之結晶固體形式 |
| JP6827113B2 (ja) | 2017-01-21 | 2021-02-10 | 広州白雲山漢方現代薬業有限公司Ｇｕａｎｇｚｈｏｕ Ｈａｎｆａｎｇ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｃｏ．，Ｌｔｄ． | シェーグレン症候群の治療におけるペオニフロリン−６’−ｏ−ベンゼンスルホン酸の使用 |
| EP3707139B1 (en) | 2017-11-06 | 2022-02-16 | Centre National de la Recherche Scientifique | Xanthine derivatives and uses thereof as inhibitors of bromodomains of bet proteins |
| KR102026243B1 (ko) * | 2018-01-19 | 2019-09-27 | 연세대학교 산학협력단 | 백혈병 치료용 약학적 조성물 |
| CN111518045A (zh) * | 2019-02-02 | 2020-08-11 | 博诺康源(北京)药业科技有限公司 | 一种具有苯并七元环结构的化合物、其制备方法及用途 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
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| WO2011161031A1 (en) * | 2010-06-22 | 2011-12-29 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| WO2012075383A2 (en) * | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
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Also Published As
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| CN104428304B (zh) | 2016-09-21 |
| US20150148337A1 (en) | 2015-05-28 |
| IL235844A0 (en) | 2015-02-01 |
| US9493483B2 (en) | 2016-11-15 |
| TWI602820B (zh) | 2017-10-21 |
| CN104428304A (zh) | 2015-03-18 |
| SG11201407900WA (en) | 2014-12-30 |
| MX360598B (es) | 2018-11-08 |
| US9925197B2 (en) | 2018-03-27 |
| CA2874774C (en) | 2022-10-04 |
| AU2013271569A1 (en) | 2014-12-18 |
| HK1207372A1 (en) | 2016-01-29 |
| BR112014030165A2 (pt) | 2017-06-27 |
| EA201492216A1 (ru) | 2015-03-31 |
| CA2874774A1 (en) | 2013-12-12 |
| KR20150023562A (ko) | 2015-03-05 |
| EP2859000B1 (en) | 2017-04-26 |
| MX2014015004A (es) | 2015-03-05 |
| EP2859000A1 (en) | 2015-04-15 |
| JP2015518899A (ja) | 2015-07-06 |
| TW201402580A (zh) | 2014-01-16 |
| ES2632774T3 (es) | 2017-09-15 |
| AR091285A1 (es) | 2015-01-21 |
| WO2013184876A1 (en) | 2013-12-12 |
| JP6154004B2 (ja) | 2017-06-28 |
| US20170079984A1 (en) | 2017-03-23 |
| IN2014DN10386A (Direct) | 2015-08-14 |
| AU2013271569B2 (en) | 2017-09-14 |
| ZA201408720B (en) | 2018-05-30 |
| IL235844A (en) | 2017-04-30 |
| WO2013184876A8 (en) | 2014-11-27 |
| NZ702458A (en) | 2016-11-25 |
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