PE20160200A1 - Inhibidores de bromodominios - Google Patents
Inhibidores de bromodominiosInfo
- Publication number
- PE20160200A1 PE20160200A1 PE2015002684A PE2015002684A PE20160200A1 PE 20160200 A1 PE20160200 A1 PE 20160200A1 PE 2015002684 A PE2015002684 A PE 2015002684A PE 2015002684 A PE2015002684 A PE 2015002684A PE 20160200 A1 PE20160200 A1 PE 20160200A1
- Authority
- PE
- Peru
- Prior art keywords
- bromodomines
- inhibitors
- compounds
- formula
- diseases
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 208000030507 AIDS Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
Classifications
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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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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract
Referida a compuestos de formula (I), done Rx y Ry son H; Rx1 es -CN, A1, A2, A3, y A4 son N, L1 es O, NH, entre otros y G1 es fenilo, C3-C6 cicloalquilo, entre otros. Dichos compuestos son utiles como agentes en el tratamiento de enfermedades y estados clinicos, incluyendo enfermedades inflamatorias, cancer, y SIDA. Tambien se proveen composiciones farmaceuticas que comprenden uno o mas compuestos de formula (I)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361840559P | 2013-06-28 | 2013-06-28 | |
| PCT/CN2014/077395 WO2014206150A1 (en) | 2013-06-28 | 2014-05-13 | Bromodomain inhibitors |
Publications (1)
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| PE2015002684A PE20160200A1 (es) | 2013-06-28 | 2014-06-27 | Inhibidores de bromodominios |
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| EP (2) | EP3013828A4 (es) |
| JP (2) | JP2016525503A (es) |
| KR (2) | KR20160027062A (es) |
| CN (2) | CN105518007A (es) |
| AR (1) | AR096757A1 (es) |
| AU (2) | AU2014303193A1 (es) |
| BR (2) | BR112015032710A2 (es) |
| CA (2) | CA2916542A1 (es) |
| CL (1) | CL2015003731A1 (es) |
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| MX (2) | MX2015017963A (es) |
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| TW (1) | TW201536780A (es) |
| UY (1) | UY35633A (es) |
| WO (2) | WO2014206150A1 (es) |
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| CA2903881C (en) | 2013-03-15 | 2021-05-18 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| EP3013828A4 (en) * | 2013-06-28 | 2016-11-23 | Abbvie Inc | BROMDOMÄNENINHIBITOREN |
| AR096837A1 (es) | 2013-07-08 | 2016-02-03 | Incyte Corp | Heterociclos tricíclicos como inhibidores de proteínas bet |
| PT3290407T (pt) | 2013-10-18 | 2020-04-06 | Celgene Quanticel Res Inc | Inibidores de bromodomínio |
| 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 |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| PT3674302T (pt) | 2014-04-23 | 2023-05-10 | Incyte Corp | 1h-pirrolo[2,3-c]piridin-7(6h)-onas e pirazolo[3,4-c]piridin-7(6h)-onas como inibidores das proteínas bet |
| JP6599979B2 (ja) | 2014-09-15 | 2019-10-30 | インサイト・コーポレイション | Betタンパク質阻害剤として用いるための三環式複素環化合物 |
| MA40940A (fr) | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| MA40943A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| EP3218376B1 (en) | 2014-11-10 | 2019-12-25 | Genentech, Inc. | Bromodomain inhibitors and uses thereof |
| CN107531692B (zh) | 2015-01-29 | 2020-12-25 | 基因泰克公司 | 治疗化合物及其用途 |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| UA124764C2 (uk) * | 2016-04-15 | 2021-11-17 | Еббві Інк. | Інгібітори бромодомену |
| CN105924671A (zh) * | 2016-06-02 | 2016-09-07 | 扬州兰都塑料科技有限公司 | 一种电力电缆用增韧剂 |
| CN105924841A (zh) * | 2016-06-02 | 2016-09-07 | 扬州兰都塑料科技有限公司 | 一种力学性能改善的电力电缆的制备方法 |
| CN105924842A (zh) * | 2016-06-02 | 2016-09-07 | 扬州兰都塑料科技有限公司 | 一种力学性能改善的电力电缆 |
| EP3472157B1 (en) | 2016-06-20 | 2023-04-12 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| CN108069958A (zh) * | 2016-11-10 | 2018-05-25 | 凯惠科技发展(上海)有限公司 | 一种含氮杂环类化合物、其制备方法、药物组合物及应用 |
| CN110167939B (zh) * | 2017-01-11 | 2021-12-31 | 江苏豪森药业集团有限公司 | 吡咯并[2,3-c]吡啶类衍生物、其制备方法及其在医药上的应用 |
| CN109384784B (zh) * | 2017-08-10 | 2021-01-12 | 浙江海正药业股份有限公司 | 磺酰胺类衍生物、其制备方法及其在医药上的用途 |
| KR102026243B1 (ko) * | 2018-01-19 | 2019-09-27 | 연세대학교 산학협력단 | 백혈병 치료용 약학적 조성물 |
| WO2019184919A1 (zh) * | 2018-03-27 | 2019-10-03 | 成都海创药业有限公司 | 一种含有金刚烷的化合物及其在治疗癌症中的用途 |
| WO2019191667A1 (en) * | 2018-03-29 | 2019-10-03 | Board Of Regents, The University Of Texas System | Imidazopiperazine inhibitors of transcription activating proteins |
| US10442799B1 (en) | 2018-04-07 | 2019-10-15 | Fuqiang Ruan | Heterocyclic compounds and uses thereof |
| CN112424200B (zh) | 2018-07-25 | 2022-09-20 | 正大天晴药业集团股份有限公司 | 作为溴区结构域蛋白抑制剂的亚氨基砜类化合物、药物组合物及其医药用途 |
| CN110776508B (zh) | 2018-07-27 | 2021-07-16 | 海创药业股份有限公司 | 一种brd4抑制剂及其制备方法和用途 |
| CA3116931A1 (en) | 2018-10-30 | 2020-05-07 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
| WO2020132004A1 (en) * | 2018-12-20 | 2020-06-25 | Saint Louis University | Bet inhibitors for modulating dux4 expression in fshd |
| KR20210139378A (ko) * | 2019-03-17 | 2021-11-22 | 상하이 린진 바이오파마 씨오., 엘티디. | 피롤아미드피리돈계 화합물, 제조방법 및 용도 |
| GB201905721D0 (en) | 2019-04-24 | 2019-06-05 | Univ Dundee | Compounds |
| CN112094266B (zh) * | 2019-06-17 | 2023-03-21 | 中国科学院上海药物研究所 | 一种吡咯并吡啶酮类化合物、其制备方法、其组合物和用途 |
| MX2022000050A (es) | 2019-07-02 | 2022-05-24 | Nuvation Bio Inc | Compuestos heterocíclicos como inhibidores de bromodominio extraterminal (bet). |
| CN114502534A (zh) | 2019-09-30 | 2022-05-13 | 协和麒麟株式会社 | Bet降解剂 |
| CN112625036A (zh) * | 2019-10-08 | 2021-04-09 | 上海海和药物研究开发股份有限公司 | 一类具有brd4抑制活性的化合物、其制备方法及用途 |
| CN113387879B (zh) * | 2020-03-14 | 2023-05-30 | 成都先导药物开发股份有限公司 | 一种胺类衍生物、其制备方法及其在医药上的应用 |
| WO2021206316A1 (ko) * | 2020-04-08 | 2021-10-14 | 압타바이오 주식회사 | 조영제 유발 급성 신부전 치료제 |
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| GB202016977D0 (en) | 2020-10-26 | 2020-12-09 | In4Derm Ltd | Compounds |
| US12527741B2 (en) | 2021-06-17 | 2026-01-20 | Wisconsin Alumni Research Foundation | Modular dendron micelles for treatment of pulmonary diseases related to fibrosis and viral infection including COVID-19 |
| EP4363417A1 (en) | 2021-06-29 | 2024-05-08 | Tay Therapeutics Limited | Pyrrolopyridone derivatives useful in the treatment of cancer |
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| TW263498B (es) | 1993-11-10 | 1995-11-21 | Takeda Pharm Industry Co Ltd | |
| JPH08337583A (ja) | 1995-04-13 | 1996-12-24 | Takeda Chem Ind Ltd | 複素環化合物およびその製造法 |
| US6271380B1 (en) * | 1998-12-30 | 2001-08-07 | Dupont Pharmaceuticals Company | 1H-imidazo[4,5-d]pyridazin-7-ones, 3H-imidazo-[4,5-c]pyridin-4-ones and corresponding thiones as corticotropin releasing factor (CRF) receptor ligands |
| US8044042B2 (en) | 2005-05-30 | 2011-10-25 | Mitsubishi Tanabe Pharma Corporation | Thienotriazolodiazepine compound and medicinal use thereof |
| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| US20130252331A1 (en) | 2010-05-14 | 2013-09-26 | James Elliott Bradner | Compositions and methods for modulating metabolism |
| CN104311562B (zh) | 2010-05-14 | 2017-07-04 | 达那-法伯癌症研究所 | 用于治疗瘤形成、炎性疾病和其他失调的组合物和方法 |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| EP3013828A4 (en) * | 2013-06-28 | 2016-11-23 | Abbvie Inc | BROMDOMÄNENINHIBITOREN |
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2014
- 2014-05-13 EP EP14818258.7A patent/EP3013828A4/en not_active Withdrawn
- 2014-05-13 KR KR1020167002406A patent/KR20160027062A/ko not_active Withdrawn
- 2014-05-13 CN CN201480047385.5A patent/CN105518007A/zh active Pending
- 2014-05-13 CA CA2916542A patent/CA2916542A1/en not_active Abandoned
- 2014-05-13 RU RU2016102647A patent/RU2016102647A/ru not_active Application Discontinuation
- 2014-05-13 WO PCT/CN2014/077395 patent/WO2014206150A1/en not_active Ceased
- 2014-05-13 HK HK16111612.7A patent/HK1223364A1/zh unknown
- 2014-05-13 HK HK16112710.6A patent/HK1224297A1/zh unknown
- 2014-05-13 BR BR112015032710A patent/BR112015032710A2/pt not_active IP Right Cessation
- 2014-05-13 PE PE2015002662A patent/PE20160540A1/es not_active Application Discontinuation
- 2014-05-13 AU AU2014303193A patent/AU2014303193A1/en not_active Abandoned
- 2014-05-13 US US14/392,200 patent/US10131657B2/en active Active
- 2014-05-13 MX MX2015017963A patent/MX2015017963A/es unknown
- 2014-05-13 JP JP2016522200A patent/JP2016525503A/ja active Pending
- 2014-05-13 SG SG11201510678TA patent/SG11201510678TA/en unknown
- 2014-06-26 AR ARP140102430A patent/AR096757A1/es unknown
- 2014-06-27 RU RU2016102648A patent/RU2016102648A/ru not_active Application Discontinuation
- 2014-06-27 WO PCT/CN2014/080991 patent/WO2014206345A1/en not_active Ceased
- 2014-06-27 TW TW103122420A patent/TW201536780A/zh unknown
- 2014-06-27 CA CA2916744A patent/CA2916744A1/en not_active Abandoned
- 2014-06-27 PE PE2015002684A patent/PE20160200A1/es not_active Application Discontinuation
- 2014-06-27 JP JP2016522234A patent/JP2016523271A/ja active Pending
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- 2014-06-27 UY UY0001035633A patent/UY35633A/es not_active Application Discontinuation
- 2014-06-27 US US14/392,201 patent/US9957263B2/en active Active
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- 2014-06-27 MX MX2015017964A patent/MX2015017964A/es unknown
- 2014-06-27 NZ NZ631062A patent/NZ631062A/en not_active IP Right Cessation
- 2014-06-27 SG SG11201510677VA patent/SG11201510677VA/en unknown
- 2014-06-27 HK HK16112709.9A patent/HK1224296A1/zh unknown
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- 2014-06-27 KR KR1020167002583A patent/KR20160027107A/ko not_active Withdrawn
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2015
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- 2015-12-22 DO DO2015000305A patent/DOP2015000305A/es unknown
- 2015-12-24 CL CL2015003731A patent/CL2015003731A1/es unknown
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2016
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- 2016-01-19 CR CR20160035A patent/CR20160035A/es unknown
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2018
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