JP2016522246A5 - - Google Patents

Download PDF

Info

Publication number
JP2016522246A5
JP2016522246A5 JP2016520759A JP2016520759A JP2016522246A5 JP 2016522246 A5 JP2016522246 A5 JP 2016522246A5 JP 2016520759 A JP2016520759 A JP 2016520759A JP 2016520759 A JP2016520759 A JP 2016520759A JP 2016522246 A5 JP2016522246 A5 JP 2016522246A5
Authority
JP
Japan
Prior art keywords
benzo
imidazol
methyl
dimethylisoxazol
dimethyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
JP2016520759A
Other languages
English (en)
Japanese (ja)
Other versions
JP6461118B2 (ja
JP2016522246A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/IB2014/002238 external-priority patent/WO2015004533A2/en
Publication of JP2016522246A publication Critical patent/JP2016522246A/ja
Publication of JP2016522246A5 publication Critical patent/JP2016522246A5/ja
Application granted granted Critical
Publication of JP6461118B2 publication Critical patent/JP6461118B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2016520759A 2013-06-21 2014-06-20 ブロモドメイン阻害剤としての新規の置換された二環式化合物 Active JP6461118B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361837830P 2013-06-21 2013-06-21
US61/837,830 2013-06-21
US201361911668P 2013-12-04 2013-12-04
US61/911,668 2013-12-04
PCT/IB2014/002238 WO2015004533A2 (en) 2013-06-21 2014-06-20 Novel substituted bicyclic compounds as bromodomain inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2018228291A Division JP2019052178A (ja) 2013-06-21 2018-12-05 ブロモドメイン阻害剤としての新規の置換された二環式化合物

Publications (3)

Publication Number Publication Date
JP2016522246A JP2016522246A (ja) 2016-07-28
JP2016522246A5 true JP2016522246A5 (OSRAM) 2017-08-03
JP6461118B2 JP6461118B2 (ja) 2019-01-30

Family

ID=52280673

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2016520759A Active JP6461118B2 (ja) 2013-06-21 2014-06-20 ブロモドメイン阻害剤としての新規の置換された二環式化合物
JP2016520760A Active JP6599852B2 (ja) 2013-06-21 2014-06-20 ブロモドメイン阻害剤としての新規の置換された二環式化合物
JP2018228291A Pending JP2019052178A (ja) 2013-06-21 2018-12-05 ブロモドメイン阻害剤としての新規の置換された二環式化合物

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2016520760A Active JP6599852B2 (ja) 2013-06-21 2014-06-20 ブロモドメイン阻害剤としての新規の置換された二環式化合物
JP2018228291A Pending JP2019052178A (ja) 2013-06-21 2018-12-05 ブロモドメイン阻害剤としての新規の置換された二環式化合物

Country Status (7)

Country Link
US (5) US9636328B2 (OSRAM)
EP (2) EP3010918B1 (OSRAM)
JP (3) JP6461118B2 (OSRAM)
CN (2) CN105473581B (OSRAM)
CA (2) CA2915561C (OSRAM)
ES (1) ES2661437T3 (OSRAM)
WO (2) WO2015004534A2 (OSRAM)

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
AU2013365926B9 (en) 2012-12-21 2019-01-17 Zenith Epigenetics Ltd. Novel heterocyclic compounds as bromodomain inhibitors
RU2680100C9 (ru) 2013-03-15 2019-04-18 Плексксикон Инк. Гетероциклические соединения и их применения
TWI719464B (zh) 2013-03-15 2021-02-21 美商英塞特控股公司 作為bet蛋白抑制劑之三環雜環
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
SI3010503T1 (sl) 2013-06-21 2020-07-31 Zenith Epigenetics Ltd. Novi biciklični inhibitorji bromodomene
ES2661437T3 (es) * 2013-06-21 2018-04-02 Zenith Epigenetics Corp. Nuevos compuestos bicíclicos sustituidos como inhibidores de bromodominio
JP2016523964A (ja) 2013-07-08 2016-08-12 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Betタンパク質阻害剤としての三環式複素環
CN105593224B (zh) 2013-07-31 2021-05-25 恒元生物医药科技(苏州)有限公司 作为溴结构域抑制剂的新型喹唑啉酮类化合物
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles 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
EP2913330A1 (en) * 2014-02-27 2015-09-02 Laboratoire Biodim Condensed derivatives of imidazole useful as pharmaceuticals
KR20240134245A (ko) 2014-04-23 2024-09-06 인사이트 홀딩스 코포레이션 BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
CA2966452A1 (en) * 2014-12-17 2016-06-23 Samuel David Brown Substituted bicyclic compounds as bromodomain inhibitors
CA2966450A1 (en) 2014-12-17 2016-06-23 Olesya KHARENKO Inhibitors of bromodomains
WO2016139361A1 (en) * 2015-03-05 2016-09-09 Boehringer Ingelheim International Gmbh New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9
GB201504689D0 (en) * 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Chemical compounds
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
AR104259A1 (es) 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
GB201506658D0 (en) * 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
JP2018525371A (ja) * 2015-07-30 2018-09-06 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company アリール置換された二環式ヘテロアリール化合物
WO2017024406A1 (en) 2015-08-11 2017-02-16 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
EP3334717B1 (en) 2015-08-11 2020-07-01 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
WO2017024412A1 (en) 2015-08-12 2017-02-16 Neomed Institute Substituted benzimidazoles, their preparation and their use as pharmaceuticals
US10501459B2 (en) 2015-10-21 2019-12-10 Neomed Institute Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN109641886B (zh) * 2015-11-25 2022-11-18 康威基内有限公司 双环bet布罗莫结构域抑制剂及其用途
CA3007168A1 (en) * 2015-12-14 2017-06-22 Zenith Epigenetics Ltd. 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
CN107021963A (zh) * 2016-01-29 2017-08-08 北京诺诚健华医药科技有限公司 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用
SG11201808306PA (en) * 2016-03-24 2018-10-30 Tragara Pharmaceuticals Inc Treatment of cancer with tg02
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
EP4234554A3 (en) 2016-06-20 2023-12-27 Incyte Corporation Crystalline solid forms of a bet inhibitor
WO2018022802A1 (en) 2016-07-26 2018-02-01 University Of Southern California Selective bromodomain inhibition of fungal bdf1
GB201617630D0 (en) 2016-10-18 2016-11-30 Cellcentric Ltd Pharmaceutical compounds
GB201617627D0 (en) * 2016-10-18 2016-11-30 Cellcentric Ltd Pharmaceutical compounds
US20180133212A1 (en) * 2016-11-03 2018-05-17 Gilead Sciences, Inc. Combination of a bcl-2 inhibitor and a bromodomain inhibitor for treating cancer
WO2018134254A1 (en) 2017-01-17 2018-07-26 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
CN107141282B (zh) * 2017-03-29 2019-11-05 重庆文理学院 一种苯并咪唑杂氮环丁酮衍生物及其在抗肿瘤药物中的应用
JP6850911B2 (ja) * 2017-06-02 2021-03-31 瀋陽化工研究院有限公司Shenyang Research Institute Of Chemical Industry Co.,Ltd. ビニルアレーン誘導体およびその使用
GB201709456D0 (en) 2017-06-14 2017-07-26 Ucb Biopharma Sprl Therapeutic agents
CN107540616B (zh) * 2017-08-29 2020-07-31 河南大学 一种高对映选择性吡唑胺化合物的制备方法
WO2019055877A1 (en) 2017-09-15 2019-03-21 Forma Therapeutics, Inc. TETRAHYDROIMIDAZO QUINOLINE COMPOSITIONS AS INHIBITORS OF CBP / P300
US10717735B2 (en) 2017-10-13 2020-07-21 Plexxikon Inc. Solid forms of a compound for modulating kinases
GB201806320D0 (en) * 2018-04-18 2018-05-30 Cellcentric Ltd Process
AU2019295790B2 (en) 2018-06-29 2023-07-13 Forma Therapeutics, Inc. Inhibiting creb binding protein (CBP)
TWI882964B (zh) 2018-09-13 2025-05-11 大陸商恒翼生物醫藥(上海)股份有限公司 Bet 溴結構域(bromodomain)抑制劑之固體形式之製備方法
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
CN111484497B (zh) * 2019-01-25 2021-07-02 江苏恒瑞医药股份有限公司 咪唑并[1,5-a]吡嗪类衍生物的可药用盐、晶型及其制备方法
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020190791A1 (en) 2019-03-15 2020-09-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (creb)
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
CN112174945B (zh) * 2019-07-02 2022-06-07 四川大学 具有抗癌作用的吲唑类化合物及其制备方法和用途
CA3144527A1 (en) * 2019-08-06 2021-02-11 Domain Therapeutics 5-heteroaryl-pyridin-2-amine confounds as neuropeptide ff receptor antagonists
CN112341451B (zh) * 2019-08-09 2022-06-17 成都先导药物开发股份有限公司 一种免疫调节剂
CN112341450B (zh) * 2019-08-09 2022-05-17 成都先导药物开发股份有限公司 一种免疫调节剂
PH12022550361A1 (en) 2019-08-14 2023-02-27 Incyte Corp Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
PE20221905A1 (es) 2019-10-11 2022-12-23 Incyte Corp Aminas biciclicas como inhibidoras de la cdk2
CN111303131B (zh) * 2020-03-19 2021-06-04 江苏慧聚药业有限公司 特戈拉赞(Tegoprazan)类似物及其合成方法
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
JP2023536634A (ja) * 2020-08-07 2023-08-28 アトス セラピューティクス,インコーポレイテッド 自己免疫疾患および癌の処置のための小分子
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers
US11767320B2 (en) 2020-10-02 2023-09-26 Incyte Corporation Bicyclic dione compounds as inhibitors of KRAS
CN114369097B (zh) * 2020-10-15 2023-07-14 山东轩竹医药科技有限公司 杂芳环类AhR抑制剂
WO2022159454A1 (en) * 2021-01-20 2022-07-28 Baylor College Of Medicine Bet subfamily inhibitors and methods using same
WO2022165530A1 (en) * 2021-02-01 2022-08-04 Janssen Biotech, Inc. Small molecule inhibitors of salt inducible kinases
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
WO2023274418A1 (zh) * 2021-07-02 2023-01-05 南京明德新药研发有限公司 蛋白降解靶向嵌合体类化合物
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
CN116496266A (zh) * 2022-07-08 2023-07-28 歌礼生物科技(杭州)有限公司 三嗪衍生物
CN116425721B (zh) * 2022-12-19 2024-02-02 艾立康药业股份有限公司 作为mat2a抑制剂的双环类化合物
KR102638900B1 (ko) * 2023-01-27 2024-02-21 스마트바이오팜 주식회사 테고프라잔 중간체를 제조하는 방법 및 이에 사용되는 신규 중간체
WO2024211696A1 (en) * 2023-04-07 2024-10-10 Biogen Ma Inc. 1h-pyrrolo[2,3-b]pyridin-4-yl]-2-oxopyrrolidine-3-carbonitrile derivatives as tyrosine kinase 2 (tyk2) inhibitors for the treatment of inflammatory diseases
CN117800875B (zh) * 2023-12-21 2024-10-22 泰州精英化成医药科技有限公司 一种反式-(N-Boc-4-氨基环己基)乙酸的制备方法

Family Cites Families (183)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3508258A1 (de) * 1985-03-08 1986-09-18 Bayer Ag, 5090 Leverkusen Ss-lactamantibiotika, verfahren zur herstellung und ihre verwendung als und in arzneimitteln
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
DE4023369A1 (de) 1990-07-23 1992-01-30 Thomae Gmbh Dr K Benzimidazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
RU1836357C (ru) 1990-07-23 1993-08-23 Др.Карл Томэ ГмбХ Производные бензимидазола, их изомеры, смеси изомеров, гидраты или их физиологически переносимые соли, обладающие антагонистическими в отношении ангиотензина свойствами
US5614519A (en) 1991-02-06 1997-03-25 Karl Thomae Gmbh (1-(2,3 or 4-N-morpholinoalkyl)-imidazol-4-yl)-benizimidazol-1-yl-methyl]-biphenyls useful as angiotensin-II antagonists
DE4224752A1 (de) 1992-04-11 1994-02-03 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE4225756A1 (de) 1992-01-22 1994-03-10 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
SI9210098B (sl) 1991-02-06 2000-06-30 Dr. Karl Thomae Benzimidazoli, zdravila, ki te spojine vsebujejo, in postopek za njihovo pripravo
US5125961A (en) 1991-08-12 1992-06-30 Monsanto Company Substituted pyridine compounds
DE4219534A1 (de) 1992-02-19 1993-12-16 Thomae Gmbh Dr K Substituierte Biphenylylderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE4408497A1 (de) 1994-03-14 1995-09-21 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
JPH10503768A (ja) 1994-08-02 1998-04-07 メルク シヤープ エンド ドーム リミテツド アゼチジン、ピロリジンおよびピペリジン誘導体
CN1072669C (zh) 1995-04-21 2001-10-10 纽罗研究公司 苯并咪唑化合物及其用作gabaa受体复合物调节器的用途
JP2000072675A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd 医薬組成物
AU760250B2 (en) 1998-12-04 2003-05-08 Neurosearch A/S New benzimidazolone-, benzoxazolone-, or benzothiazolone derivatives as ion channel modulating agents
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
US6664252B2 (en) 1999-12-02 2003-12-16 Osi Pharmaceuticals, Inc. 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof
GB0002100D0 (en) 2000-01-28 2000-03-22 Novartis Ag Organic compounds
EP1263754A1 (en) 2000-02-01 2002-12-11 Millennium Pharmaceuticals, Inc. INDALONE AND BENZIMIDAZOLONE INHIBITORS OF FACTOR Xa
US20120028912A1 (en) 2000-02-22 2012-02-02 J.David Gladstone Institute Methods of modulating bromodomains
MXPA03004672A (es) 2000-10-27 2004-04-20 Dow Agrosciences Llc 4,5-dihidro-1,2,4-triazin-6-onas sustituidas, 1,2,4-triazin-6-onas sustituidas, y su uso como fungicidas e insecticidas.
EA007254B1 (ru) * 2000-12-01 2006-08-25 Оси Фармасьютикалз, Инк. Соединения, специфические к аденозиновому а, аи арецептору, и их применение
WO2002070486A1 (en) 2001-03-01 2002-09-12 Shionogi & Co., Ltd. Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
CA2440211A1 (en) * 2001-03-09 2002-09-19 Pfizer Products Inc. Benzimidazole anti-inflammatory compounds
DE60221368T2 (de) 2001-03-15 2008-04-17 Janssen Pharmaceutica N.V. Hiv hemmende pyrazinon-derivate
MXPA03008658A (es) 2001-03-23 2005-04-11 Bayer Ag Inhibidores de rho-cinasa.
US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
EP1381598A4 (en) 2001-03-28 2008-03-19 Bristol Myers Squibb Co NEW INHIBITORS OF TYROSINE KINASE
US20050176858A1 (en) 2002-02-15 2005-08-11 Bridgestone Corporation Rubber composition and pneumatic tire made therefrom
TWI276631B (en) 2002-09-12 2007-03-21 Avanir Pharmaceuticals Phenyl-aza-benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
US20040166137A1 (en) 2002-11-08 2004-08-26 Lackey John William Hetero-substituted benzimidazole compounds and antiviral uses thereof
AR043063A1 (es) 2002-12-13 2005-07-13 Altana Pharma Ag Bencimidazoles 6-sustituidos y su uso como inhibidores de secreciones gastricas
AR042956A1 (es) * 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
CL2004000409A1 (es) * 2003-03-03 2005-01-07 Vertex Pharma Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu
WO2004098494A2 (en) 2003-04-30 2004-11-18 Cytokinetics, Inc. Compounds, compositions, and methods
AU2003902860A0 (en) 2003-06-06 2003-06-26 Daicel Chemical Industries, Ltd Benzimidazole compounds
US20050256179A1 (en) 2003-08-08 2005-11-17 Sircar Jagadish C Selective pharmacologic inhibition of protein trafficking and related methods of treating human diseases
CL2004002050A1 (es) 2003-08-13 2005-06-03 Pharmacia Corp Sa Organizada B Compuestos derivados de piridinonas sustituidas; su uso en el tratamiento de afecciones causadas o exacerbadas por actividad p38 map kinasa y/o tnf no regulada, tales como inflamaciones, tumores, sida y otros.
WO2005080380A1 (en) 2004-02-03 2005-09-01 Eli Lilly And Company Kinase inhibitors
WO2005075432A1 (ja) 2004-02-06 2005-08-18 Chugai Seiyaku Kabushiki Kaisha 1−(2h)−イソキノロン誘導体およびその抗ガン剤としての使用
CN1285590C (zh) 2004-02-23 2006-11-22 上海医药工业研究院 伊曲康唑盐酸盐口服固体组合物和制备方法
CA2559552A1 (en) 2004-03-23 2005-09-29 F. Hoffmann-La Roche Ag Benzyl-pyridazinone derivatives as non-nucleoside reverse transcriptase inhibitors
US20080015196A1 (en) 2004-04-16 2008-01-17 Neurogen Corporation Imidazopyrazines, Imidazopyridines, and Imidazopyrimidines as Crf1 Receptor Ligands
KR101258298B1 (ko) 2004-06-01 2013-04-25 유니버시티 오브 버지니아 페이턴트 파운데이션 암 및 혈관형성의 이중 소분자 억제제
WO2005121132A1 (ja) 2004-06-11 2005-12-22 Shionogi & Co., Ltd. 抗hcv作用を有する縮合ヘテロ環化合物
MX2007001986A (es) 2004-08-26 2007-05-10 Pfizer Compuestos de aminoheteroarilo como inhibidores de proteina quinasa.
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006038734A1 (en) 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
CA2584485C (en) 2004-10-20 2013-12-31 Resverlogix Corp. Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
DK1848718T3 (da) 2005-02-04 2012-08-27 Millennium Pharm Inc E1 aktiveringsenzymhæmmere
US7893267B2 (en) 2005-03-14 2011-02-22 High Point Pharmaceuticals, Llc Benzazole derivatives, compositions, and methods of use as β-secretase inhibitors
WO2006119400A2 (en) 2005-05-03 2006-11-09 Dow Agrosciences Llc Substituted 4,5-dihydro-1,2,4-triazin-6-ones, 1,2,4-trianzin-6-ones, and their use as fungicides
CN101365446B (zh) 2005-07-29 2013-05-22 雷斯弗洛吉克斯公司 预防和治疗复杂疾病的药物组合物及其经由可植入医药装置的递送
CA2623813A1 (en) 2005-10-03 2007-04-12 Ono Pharmaceutical Co., Ltd. Nitrogen-containing heterocyclic compound and pharmaceutical application thereof
WO2007061923A2 (en) 2005-11-18 2007-05-31 Takeda San Diego, Inc. Glucokinase activators
PL1959951T3 (pl) * 2005-12-01 2010-06-30 Hoffmann La Roche Heteroarylo-podstawione pochodne piperydyny jako inhibitory l-cpt1
CN101384593A (zh) * 2006-02-17 2009-03-11 辉瑞有限公司 用作tlr7调节剂的3-脱氮嘌呤衍生物
AU2007216247A1 (en) * 2006-02-17 2007-08-23 Pfizer Limited 3 -deazapurine derivatives as TLR7 modulators
EP2001480A4 (en) * 2006-03-31 2011-06-15 Abbott Lab Indazole CONNECTIONS
BRPI0709660A2 (pt) 2006-04-03 2011-07-19 Glaxo Group Limided derivados de azabiciclo [3,1,0] hexila como moduladores dos receptores de dopamina d3
CA2700988A1 (en) 2006-09-27 2008-05-08 Surface Logix, Inc. Rho kinase inhibitors
PL2094662T3 (pl) 2006-12-14 2012-09-28 Astellas Pharma Inc Związki oparte na policyklicznych kwasach użyteczne jako antagoniści rCRTH2 oraz jako środki przeciwalergiczne
SG144809A1 (en) * 2007-01-11 2008-08-28 Millipore U K Ltd Benzimidazole compounds and their use as chromatographic ligands
DK2118074T3 (en) 2007-02-01 2014-03-10 Resverlogix Corp Compounds for the prevention and treatment of cardiovascular diseases
WO2008153701A1 (en) 2007-05-24 2008-12-18 Schering Corporation Compounds for inhibiting ksp kinesin activity
WO2008154241A1 (en) * 2007-06-08 2008-12-18 Abbott Laboratories 5-heteroaryl substituted indazoles as kinase inhibitors
JP5492770B2 (ja) 2007-06-26 2014-05-14 サノフイ ベンゾイミダゾール及びアザベンゾイミダゾールの位置選択的銅触媒合成
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
DE102007038957A1 (de) 2007-08-17 2009-02-19 Merck Patent Gmbh 6-Thioxo-pyridazinderivate
GB0719235D0 (en) 2007-10-02 2007-11-14 Glaxo Group Ltd Novel compounds
WO2009054790A1 (en) 2007-10-26 2009-04-30 Astrazeneca Ab Amide linked heteroaromatic derivatives as modulators of mglur5
CA2708262A1 (en) 2007-12-07 2009-06-18 Elan Pharmaceuticals, Inc. Methods and compositions for treating liquid tumors
WO2009079001A1 (en) 2007-12-18 2009-06-25 Janssen Pharmaceutica N.V. Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine h4 receptor
CN101910182B (zh) 2007-12-28 2013-07-17 田边三菱制药株式会社 抗癌剂
TW200938542A (en) * 2008-02-01 2009-09-16 Irm Llc Compounds and compositions as kinase inhibitors
WO2009158258A1 (en) 2008-06-25 2009-12-30 E. I. Du Pont De Nemours And Company Herbicidal dihydro oxo six-membered azinyl isoxazolines
JP2012500260A (ja) 2008-08-18 2012-01-05 イェール・ユニヴァーシティー Mifモジュレーター
US9643922B2 (en) 2008-08-18 2017-05-09 Yale University MIF modulators
US9540322B2 (en) * 2008-08-18 2017-01-10 Yale University MIF modulators
EP2379561B1 (en) 2008-11-25 2015-11-04 University Of Rochester Mlk inhibitors and methods of use
US8940891B2 (en) 2008-12-08 2015-01-27 Arena Pharmaceuticals, Inc. Modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
EP2196465A1 (en) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
DE102008062826A1 (de) 2008-12-23 2010-07-01 Merck Patent Gmbh Pyridazinonderivate
US8389550B2 (en) 2009-02-25 2013-03-05 Hoffmann-La Roche Inc. Isoxazoles / O-pyridines with ethyl and ethenyl linker
JP2012519732A (ja) 2009-03-09 2012-08-30 サーフェイス ロジックス,インコーポレイティド Rhoキナーゼ阻害剤
CN105859639A (zh) 2009-03-18 2016-08-17 雷斯韦洛吉克斯公司 新的抗炎剂
EP2408449A4 (en) 2009-03-18 2012-08-08 Univ Leland Stanford Junior METHOD AND COMPOSITIONS FOR TREATING FLAVIVIRIDAE VIRUS INFECTIONS
CN107252429B (zh) 2009-04-22 2023-06-16 雷斯韦洛吉克斯公司 新抗炎剂
JP5466292B2 (ja) 2009-05-05 2014-04-09 エフ.ホフマン−ラ ロシュ アーゲー イソオキサゾール−ピリジン誘導体
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ES2652304T3 (es) 2009-11-05 2018-02-01 Glaxosmithkline Llc Compuesto de benzodiacepina novedoso
GB0919432D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
EP3050885B1 (en) 2009-11-05 2017-10-18 GlaxoSmithKline LLC Benzodiazepine bromodomain inhibitor
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US9034850B2 (en) 2009-11-20 2015-05-19 Sk Chemicals Co., Ltd. Gonadotropin releasing hormone receptor antagonist, preparation method thereof and pharmaceutical composition comprising the same
WO2011067366A1 (en) * 2009-12-03 2011-06-09 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
WO2011097607A1 (en) 2010-02-08 2011-08-11 Southern Research Institute Anti-viral treatment and assay to screen for anti-viral agent
KR101165996B1 (ko) 2010-04-23 2012-07-18 주식회사 녹십자 프탈라지논 유도체, 이의 제조방법 및 이를 함유하는 약학적 조성물
HUE031073T2 (en) 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
JP2011246389A (ja) * 2010-05-26 2011-12-08 Oncotherapy Science Ltd Ttk阻害作用を有する縮環ピラゾール誘導体
CA2810162A1 (en) 2010-06-09 2011-12-15 Rutgers, The State University Of New Jersey Antimicrobial agents
WO2011159926A1 (en) 2010-06-16 2011-12-22 Rutgers, The State University Of New Jersey Antimicrobial agents
CA2803448A1 (en) 2010-07-06 2012-01-12 Universite De Montreal Imidazopyridine, imidazopyrimidine and imidazopyrazine derivatives as melanocortin-4 receptor modulators
WO2012009258A2 (en) 2010-07-13 2012-01-19 Edward Roberts Peptidomimetic galanin receptor modulators
US8993779B2 (en) 2010-08-12 2015-03-31 Merck Sharp & Dohme Corp. Positive allosteric modulators of MGLUR2
WO2012040499A2 (en) 2010-09-22 2012-03-29 Surface Logix, Inc. Metabolic inhibitors
KR101242572B1 (ko) 2010-10-12 2013-03-19 한국화학연구원 5-환 헤테로 아릴로 치환된 프탈라지논 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 약학적 조성물
GB201018147D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Method of treatment
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
CN102731409A (zh) 2011-04-08 2012-10-17 中国科学院上海药物研究所 一类哒嗪酮类化合物,其药物组合物、制备方法及用途
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106799D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
EP2721031B1 (en) 2011-06-17 2016-01-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
JP5878178B2 (ja) * 2011-09-30 2016-03-08 大鵬薬品工業株式会社 1,2,4−トリアジン−6−カルボキサミド誘導体
JP5992049B2 (ja) 2011-11-01 2016-09-14 レスバーロジックス コーポレイション 置換されたキナゾリノンのための経口速放性製剤
JP6141863B2 (ja) 2011-12-01 2017-06-07 ケモセントリックス,インコーポレイティド Ccr(4)アンタゴニストとしての置換ベンズイミダゾール及びベンゾピラゾール
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281396A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
HK1206744A1 (en) 2012-04-20 2016-01-15 Abbvie Inc. Isoindolone derivatives
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
CN104428293B (zh) 2012-06-11 2018-06-08 Ucb生物制药私人有限公司 调节TNFα的苯并咪唑类
EP2888256A4 (en) 2012-08-24 2016-02-17 Univ Texas HETEROCYCLIC HIF ACTIVITY MODULATORS FOR THE TREATMENT OF DISEASES
CN104780764A (zh) 2012-09-05 2015-07-15 拜尔农作物科学股份公司 取代的2-酰氨基苯并咪唑、2-酰氨基苯并噁唑和2-酰氨基苯并噻唑或其盐作为活性物质对抗非生物植物胁迫的用途
US20150246888A1 (en) 2012-09-11 2015-09-03 Michael Johnson Enoyl reductase inhibitors with antibacterial activity
EP2920183B1 (en) 2012-11-14 2017-03-08 Glaxosmithkline LLC Thieno[3,2-c]pyridin-4(5h)-ones as bet inhibitors
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
WO2014095775A1 (de) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydrochinoxalinone
AU2013365926B9 (en) 2012-12-21 2019-01-17 Zenith Epigenetics Ltd. Novel heterocyclic compounds as bromodomain inhibitors
HK1212345A1 (en) 2013-02-22 2016-06-10 Bayer Pharma Aktiengesellschaft 4-substituted pyrrolo- and pyrazolo-diazepines
WO2014128070A1 (de) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft Pyrrolo- und pyrazolo-triazolodiazepine als bet-proteininhibitoren zur behandlung von hyper-proliferativen erkrankungen
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
CN105189488B (zh) 2013-02-27 2018-07-24 百时美施贵宝公司 用作溴区结构域抑制剂的咔唑化合物
BR112015022674A2 (pt) 2013-03-11 2017-07-18 Abbvie Inc inibidores de bromodomínio
CN105377851B (zh) 2013-03-11 2018-07-20 密执安州立大学董事会 Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法
CA2904048A1 (en) 2013-03-11 2014-10-09 Abbvie Inc. Bromodomain inhibitors
KR20150126696A (ko) 2013-03-12 2015-11-12 애브비 인코포레이티드 디하이드로-피롤로피리디논 브로모도메인 억제제
US9493411B2 (en) 2013-03-12 2016-11-15 Abbvie Inc. Pyrrole-3-carboxamide bromodomain inhibitors
WO2014140077A1 (en) 2013-03-14 2014-09-18 Glaxosmithkline Intellectual Property (No.2) Limited Furopyridines as bromodomain inhibitors
ES2704048T3 (es) 2013-03-14 2019-03-14 Glaxosmithkline Ip No 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina-2,3-disustituida y su uso como inhibidores de bromodominio
BR112015022417A2 (pt) 2013-03-14 2017-07-18 Convergene Llc métodos e composições para inibição de proteínas contendo bromodomínio
US20160039842A1 (en) 2013-03-15 2016-02-11 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
RU2680100C9 (ru) 2013-03-15 2019-04-18 Плексксикон Инк. Гетероциклические соединения и их применения
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
TWI719464B (zh) 2013-03-15 2021-02-21 美商英塞特控股公司 作為bet蛋白抑制劑之三環雜環
US9199988B2 (en) 2013-03-27 2015-12-01 Boehringer Ingelheim International Gmbh Dihydroquinazolinone analogues
JP6370368B2 (ja) 2013-03-27 2018-08-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Brd4阻害剤としてのインドリノン類似体
TWI530499B (zh) * 2013-03-28 2016-04-21 吉李德科學股份有限公司 作為溴結構域(bromodomain)抑制劑之苯並咪唑酮衍生物類
EP2792355A1 (en) 2013-04-17 2014-10-22 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
US10435364B2 (en) 2013-04-17 2019-10-08 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
WO2014173241A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
TWI527811B (zh) 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
MX2015016344A (es) 2013-05-27 2016-03-01 Novartis Ag Derivados de imidazo-pirrolidinona y su uso en el tratamiento de enfermedades.
CA2915419A1 (en) 2013-06-17 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted phenyl-2,3-benzodiazepines
SI3010503T1 (sl) 2013-06-21 2020-07-31 Zenith Epigenetics Ltd. Novi biciklični inhibitorji bromodomene
ES2661437T3 (es) * 2013-06-21 2018-04-02 Zenith Epigenetics Corp. Nuevos compuestos bicíclicos sustituidos como inhibidores de bromodominio
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
JP2016523964A (ja) 2013-07-08 2016-08-12 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Betタンパク質阻害剤としての三環式複素環
WO2015011084A1 (de) 2013-07-23 2015-01-29 Bayer Pharma Aktiengesellschaft Substituierte dihydropyrido[3,4-b]pyrazinone als duale inhibitoren von bet-proteinen und polo-like kinasen
KR20160034379A (ko) 2013-07-25 2016-03-29 다나-파버 캔서 인스티튜트 인크. 전사 인자의 억제제 및 그의 용도
CN105593224B (zh) 2013-07-31 2021-05-25 恒元生物医药科技(苏州)有限公司 作为溴结构域抑制剂的新型喹唑啉酮类化合物
US20150051208A1 (en) 2013-08-14 2015-02-19 Boehringer Ingelheim International Gmbh Pyridinones
DK3071203T3 (da) 2013-11-18 2021-03-15 Forma Therapeutics Inc Tetrahydroquinolinsammensætninger som bet-bromdomæne-inhibitorer
RU2720237C2 (ru) 2013-11-18 2020-04-28 Форма Терапеутикс, Инк. Композиции, содержащие бензопиперазин, в качестве ингибиторов бромодоменов вет
GB201321739D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
US9458156B2 (en) 2014-12-23 2016-10-04 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
CA2966452A1 (en) 2014-12-17 2016-06-23 Samuel David Brown Substituted bicyclic compounds as bromodomain inhibitors
CA2966450A1 (en) 2014-12-17 2016-06-23 Olesya KHARENKO Inhibitors of bromodomains

Similar Documents

Publication Publication Date Title
JP2016522246A5 (OSRAM)
JP2016525078A5 (OSRAM)
JP2016527263A5 (OSRAM)
JP7216682B2 (ja) Usp30阻害剤としての1-シアノ-ピロリジン化合物
JP5055136B2 (ja) Vegf−r2阻害剤としてのイミダゾ(1,2−a)ピリジン化合物
EP3010918B1 (en) Novel substituted bicyclic compounds as bromodomain inhibitors
JP5925394B2 (ja) 抗レトロウイルス剤としての(ヘテロ)アリールアセトアミド誘導体
TWI579284B (zh) 咪唑并吡咯啶酮化合物
US10968203B2 (en) Pyrimidinyl-pyridyloxy-naphthyl compounds and methods of treating IRE1-related diseases and disorders
JP2017538721A5 (OSRAM)
JP2017537946A5 (OSRAM)
JP2007510689A5 (OSRAM)
HRP20200854T1 (hr) Novi biciklički inhibitori bromodomene
AU2013365926A2 (en) Novel heterocyclic compounds as bromodomain inhibitors
WO2015015318A4 (en) Novel quinazolinones as bromodomain inhibitors
JP2019504009A5 (OSRAM)
JP2012507566A5 (OSRAM)
JP2017532360A5 (OSRAM)
CN101605540A (zh) 使用mek抑制剂的方法
SK12002003A3 (en) Novel tyrosine kinase inhibitors
TW200536851A (en) Compounds and methods of use
CN101743241A (zh) 哒嗪酮衍生物
JP2010510319A5 (OSRAM)
BRPI0418082B1 (pt) Derivados de tiazol úteis como antagonistas de receptor de adenosina A2A
KR20210058277A (ko) 피롤로피리미딘, 피롤로피리딘, 인다졸 화합물 유도체 및 이를 포함하는 치료용 약학 조성물