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 (enExample) 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 (enExample)
EP (2) EP3010918B1 (enExample)
JP (3) JP6461118B2 (enExample)
CN (2) CN105473581B (enExample)
CA (2) CA2915622C (enExample)
ES (1) ES2661437T3 (enExample)
WO (2) WO2015004533A2 (enExample)

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
JP2016507496A (ja) 2012-12-21 2016-03-10 ゼニス・エピジェネティクス・コーポレイションZenith Epigenetics Corp. ブロモドメイン阻害剤としての新規複素環式化合物
EA035469B1 (ru) 2013-03-15 2020-06-22 Инсайт Холдингс Корпорейшн Трициклические гетероциклы как ингибиторы белков бэт
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
CN105073747B (zh) 2013-03-15 2017-06-06 普莱希科公司 杂环化合物及其应用
CN105473581B (zh) * 2013-06-21 2019-04-23 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新取代的双环化合物
KR102307566B1 (ko) 2013-06-21 2021-10-05 제니쓰 에피제네틱스 리미티드 신규한 바이사이클릭 브로모도메인 억제제
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain 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
US9315501B2 (en) 2013-11-26 2016-04-19 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
SMT202000133T1 (it) 2014-04-23 2020-05-08 Incyte Corp 1h-pirrolo[2,3-c]piridin-7(6h)-oni e pirazolo[3,4-c]piridin-7(6h)-oni come inibitori di proteine 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
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
HK1245246A1 (zh) 2014-12-01 2018-08-24 恒翼生物医药科技(上海)有限公司 作为溴域抑制剂的取代吡啶酮
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
CA2966452A1 (en) * 2014-12-17 2016-06-23 Samuel David Brown Substituted bicyclic compounds as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
EP3265453B1 (en) * 2015-03-05 2022-06-29 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
EP3328839A1 (en) * 2015-07-30 2018-06-06 Bristol-Myers Squibb Company Aryl substituted bicyclic heteroaryl compounds
HK1256753A1 (zh) 2015-08-11 2019-10-04 Neomed Institute 芳基-取代的二氢喹诺酮、它们的制备和它们作为药物的用途
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
CN114605387A (zh) 2015-08-12 2022-06-10 埃皮吉纳提克斯股份有限公司 取代的苯并咪唑、它们的制备和它们作为药物的用途
US10501459B2 (en) 2015-10-21 2019-12-10 Neomed Institute Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
EP3380469B1 (en) * 2015-11-25 2022-03-16 Convergene Llc Bicyclic bet bromodomain inhibitors and uses thereof
US20190263799A1 (en) * 2015-12-14 2019-08-29 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
RU2749025C2 (ru) * 2016-03-24 2021-06-03 Трагара Фармасьютикалз, Инк. Лечение рака при помощи tg02
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
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
CN109715625B (zh) 2016-06-20 2022-04-19 因赛特公司 Bet抑制剂的结晶固体形式
EP3490552B1 (en) 2016-07-26 2022-11-23 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
WO2018085069A1 (en) * 2016-11-03 2018-05-11 Gilead Sciences, Inc. Combination of a bcl-2 inhibitor and a bromodomain inhibitor for treating cancer
US11040027B2 (en) 2017-01-17 2021-06-22 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
WO2018219309A1 (zh) * 2017-06-02 2018-12-06 沈阳化工研究院有限公司 一种芳乙烯衍生物及其应用
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
IL279734B2 (en) 2018-06-29 2024-11-01 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
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
TW202102494A (zh) 2019-03-15 2021-01-16 美商弗瑪治療公司 抑制環amp-反應元件-結合蛋白(creb)
US11919904B2 (en) 2019-03-29 2024-03-05 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
WO2020223558A1 (en) 2019-05-01 2020-11-05 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
EP4010328A1 (en) * 2019-08-06 2022-06-15 Domain Therapeutics 5-heteroaryl-pyridin-2-amine confounds as neuropeptide ff receptor antagonists
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
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
WO2021030537A1 (en) 2019-08-14 2021-02-18 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
CR20220170A (es) 2019-10-11 2022-10-10 Incyte Corp Aminas bicíclicas 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
EP4192826A4 (en) * 2020-08-07 2024-09-04 Athos Therapeutics, Inc. SMALL MOLECULES FOR THE TREATMENT OF AUTOIMMUNE DISEASES AND CANCER
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
WO2022072783A1 (en) 2020-10-02 2022-04-07 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
US20240158355A1 (en) * 2021-01-20 2024-05-16 Baylor College Of Medicine Bet subfamily inhibitors and methods using same
US20240174662A1 (en) * 2021-02-01 2024-05-30 Janssen Biotech, Inc. Small molecule inhibitors of salt inducible kinases
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
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
CN117645603A (zh) * 2022-09-05 2024-03-05 复旦大学 p300溴结构域抑制剂及其药用组合物及其应用
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
AU2024253757A1 (en) * 2023-04-07 2025-10-16 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
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
DE4023369A1 (de) 1990-07-23 1992-01-30 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
DE4224752A1 (de) 1992-04-11 1994-02-03 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
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
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
EP0804434A1 (en) 1994-08-02 1997-11-05 MERCK SHARP & DOHME LTD. Azetidine, pyrrolidine and piperidine derivatives
CA2218493C (en) 1995-04-21 2005-02-22 Neurosearch A/S Benzimidazole compounds and their use as modulators of the gabaa receptor complex
JP2000072675A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd 医薬組成物
EP1144387A1 (en) 1998-12-04 2001-10-17 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
AU2001234705A1 (en) 2000-02-01 2001-08-14 Cor Therapeutics, Inc. Indalone and benzimidazolone inhibitors of factor xa
US20120028912A1 (en) 2000-02-22 2012-02-02 J.David Gladstone Institute Methods of modulating bromodomains
AU2001297622A1 (en) 2000-10-27 2002-09-12 Dow Agrosciences Llc Substituted 4,5-dihydro-1,2,4-triazin-6-ones, 1,2,4-triazin-6-ones, and their use as fungicides and insecticides
BR0115847A (pt) * 2000-12-01 2004-02-25 Osi Pharm Inc Compostos especìficos para receptor para adenosina a1, a2a, e a3 e usos dos mesmos
CN1659143A (zh) 2001-03-01 2005-08-24 盐野义制药株式会社 具有hiv整合酶抑制活性的含氮杂芳基化合物
WO2002072576A1 (en) * 2001-03-09 2002-09-19 Pfizer Products Inc. Benzimidazole anti-inflammatory compounds
EP1370265B8 (en) 2001-03-15 2013-10-30 Janssen Pharmaceutica NV Hiv inhibiting pyrazinone derivatives
HN2002000067A (es) * 2001-03-23 2003-10-24 Bayer Healthcare Llc Inhibidores de la rho - quinasa.
US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
CA2442428A1 (en) 2001-03-28 2002-10-10 Mark D. Wittman Novel tyrosine kinase inhibitors
EP1475408B1 (en) 2002-02-15 2011-04-06 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
WO2005013950A2 (en) 2003-08-08 2005-02-17 Avanir Pharmaceuticals 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.
US7863310B2 (en) 2004-02-03 2011-01-04 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
EP1730120A1 (en) 2004-03-23 2006-12-13 F.Hoffmann-La Roche Ag Non-nucleoside reverse transcriptase inhibitors
EP1734820A4 (en) 2004-04-16 2008-01-23 Neurogen Corp Imidazopyrrazine, imidazopyridine, and imidazo-pyrimidine as CRF1 receptor ligands
WO2005117876A1 (en) 2004-06-01 2005-12-15 University Of Virginia Patent Foundation Dual small molecule inhibitors of cancer and angiogenesis
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
EP1786777A1 (en) 2004-08-26 2007-05-23 Pfizer, Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
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
US7846915B2 (en) 2004-10-20 2010-12-07 Resverlogix Corporation Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
WO2006084281A1 (en) 2005-02-04 2006-08-10 Millennium Pharmaceuticals, Inc. Inhibitors of e1 activating enzymes
US20060223849A1 (en) * 2005-03-14 2006-10-05 Mjalli Adnan M Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors
EP1881966A2 (en) 2005-05-03 2008-01-30 Dow AgroSciences LLC Substituted 4,5-dihydro-1,2,4-triazin-6-ones, 1,2,4-trianzin-6-ones, and their use as fungicides
WO2007016525A2 (en) 2005-07-29 2007-02-08 Resverlogix Corp. Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices
WO2007040208A1 (ja) 2005-10-03 2007-04-12 Ono Pharmaceutical Co., Ltd. 含窒素複素環化合物およびその医薬用途
WO2007061923A2 (en) 2005-11-18 2007-05-31 Takeda San Diego, Inc. Glucokinase activators
DE602006011363D1 (de) * 2005-12-01 2010-02-04 Hoffmann La Roche Heteroaryl-substituierte piperidin-derivate als l-cpt1-hemmer
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
US8008481B2 (en) * 2006-03-31 2011-08-30 Ericsson Anna M Indazole compounds
EA200870404A1 (ru) 2006-04-03 2009-04-28 Глэксо Груп Лимитед Производные азабицикло[3.1.0.]гексила в качестве модуляторов рецепторов допамина d3
CA2700988A1 (en) 2006-09-27 2008-05-08 Surface Logix, Inc. Rho kinase inhibitors
EP2094662B1 (en) 2006-12-14 2012-04-11 Astellas Pharma Inc. Polycyclic acid compounds useful as crth2 antagonists and antiallergic agents
SG144809A1 (en) * 2007-01-11 2008-08-28 Millipore U K Ltd Benzimidazole compounds and their use as chromatographic ligands
PT2118074E (pt) 2007-02-01 2014-03-20 Resverlogix Corp Compostos para a prevenção e tratamento de doenças cardiovasculares
WO2008153701A1 (en) 2007-05-24 2008-12-18 Schering Corporation Compounds for inhibiting ksp kinesin activity
CN101790526A (zh) * 2007-06-08 2010-07-28 雅培制药有限公司 用作激酶抑制剂的5-杂芳基取代的吲唑化合物
WO2009000413A1 (en) 2007-06-26 2008-12-31 Sanofi-Aventis A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
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
US8084466B2 (en) 2007-12-18 2011-12-27 Janssen Pharmaceutica Nv 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
TW200942537A (en) * 2008-02-01 2009-10-16 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
US9643922B2 (en) 2008-08-18 2017-05-09 Yale University MIF modulators
US9540322B2 (en) * 2008-08-18 2017-01-10 Yale University MIF modulators
MX2011001872A (es) * 2008-08-18 2011-05-23 Univ Yale Moduladores de mif.
CN102264743B (zh) 2008-11-25 2015-02-11 罗彻斯特大学 Mlk抑制剂及其使用方法
PT2370413E (pt) 2008-12-08 2015-10-23 Arena Pharm Inc Moduladores do recetor da prostaciclina (pgi2) úteis para o tratamento de distúrbios relacionados com o mesmo
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
MX2011009568A (es) 2009-03-09 2011-12-06 Surface Logix Inc Inhibidores de la rho cinasa.
NZ617779A (en) 2009-03-18 2015-08-28 Resverlogix Corp Novel anti-inflammatory agents
CN102448458B (zh) 2009-03-18 2015-07-22 小利兰·斯坦福大学理事会 治疗黄病毒科病毒感染的方法和组合物
US9757368B2 (en) 2009-04-22 2017-09-12 Resverlogix Corp. Anti-inflammatory agents
US8415379B2 (en) 2009-05-05 2013-04-09 Hoffmann-La Roche Inc. Pyridines
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919423D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
CA2779355C (en) 2009-11-05 2018-01-16 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
AU2010317096B2 (en) 2009-11-05 2015-03-26 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
JP5757956B2 (ja) 2009-11-20 2015-08-05 エスケー ケミカルス シーオー., エルティーディー.Sk Chemicals Co., Ltd. ゴナドトロピン放出ホルモン受容体拮抗剤、その製造方法及びそれを含む医薬組成物
EP2507231A1 (en) * 2009-12-03 2012-10-10 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
ES2606958T3 (es) 2010-05-14 2017-03-28 Dana-Farber Cancer Institute, Inc. Compuestos de tienotriazolodiazepina para tratar una 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
US8933096B2 (en) 2010-06-09 2015-01-13 Rugers, 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
EP2603079B1 (en) 2010-08-12 2018-09-19 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
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
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
WO2012174487A2 (en) * 2011-06-17 2012-12-20 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
WO2013047813A1 (ja) * 2011-09-30 2013-04-04 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
PT2773354T (pt) 2011-11-01 2019-07-17 Resverlogix Corp Formulações orais de libertação imediata para quinazolinonas substituídas
KR102031846B1 (ko) 2011-12-01 2019-10-14 케모센트릭스, 인크. Ccr(4) 길항제로서의 치환된 벤즈이미다졸 및 벤조피라졸
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20130281398A1 (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
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
WO2013155695A1 (en) 2012-04-20 2013-10-24 Abbott Laboratories Isoindolone derivatives
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
CA2874303C (en) 2012-06-11 2020-10-13 Ucb Biopharma Sprl Tnf -alpha modulating benz imidazoles
WO2014031928A2 (en) 2012-08-24 2014-02-27 Philip Jones Heterocyclic modulators of hif activity for treatment of disease
WO2014037340A1 (de) 2012-09-05 2014-03-13 Bayer Cropscience Ag Verwendung substituierter 2-amidobenzimidazole, 2-amidobenzoxazole und 2-amidobenzothiazole oder deren salze als wirkstoffe gegen abiotischen pflanzenstress
WO2014043246A1 (en) 2012-09-11 2014-03-20 The Board Of Trustees Of The University Of Illinois Enoyl reductase inhibitors with antibacterial activity
US9663533B2 (en) 2012-11-14 2017-05-30 Glaxosmithkline Llc Thieno[3,2-C]pyridin-4(5H)-ones as BET inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
HK1211033A1 (en) 2012-12-20 2016-05-13 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydroquinoxalinones
JP2016507496A (ja) 2012-12-21 2016-03-10 ゼニス・エピジェネティクス・コーポレイションZenith Epigenetics Corp. ブロモドメイン阻害剤としての新規複素環式化合物
HK1212972A1 (zh) 2013-02-22 2016-06-24 Bayer Pharma Aktiengesellschaft 作爲bet-蛋白抑制剂用於治疗过度增殖性疾病的吡咯并-和吡唑并-三唑并二氮杂卓
CA2901805A1 (en) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft 4-substituted pyrrolo- and pyrazolo-diazepines
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
EP2961747B1 (en) 2013-02-27 2017-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2970285B1 (en) 2013-03-11 2019-04-17 AbbVie Inc. Fused tetracyclic bromodomain inhibitors
BR112015022861A8 (pt) 2013-03-11 2019-11-26 Abbvie Inc inibidores de bromodomínio
EP2970312B1 (en) 2013-03-11 2017-11-15 The Regents of The University of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
CN105164113B (zh) 2013-03-12 2018-03-02 艾伯维公司 吡咯酰胺抑制剂
JP2016512543A (ja) 2013-03-12 2016-04-28 アッヴィ・インコーポレイテッド ジヒドロ−ピロロピリジノンブロモドメイン阻害剤
CN105189461B (zh) 2013-03-14 2018-05-15 葛兰素史克知识产权第二有限公司 2,3-二取代的1-酰基-4-氨基-1,2,3,4-四氢喹啉衍生物和它们作为溴结构域抑制剂的用途
US9670221B2 (en) 2013-03-14 2017-06-06 Glaxosmithkline Intellectual Property (No. 2) Limited Furopyridines as bromodomain inhibitors
EA201591746A1 (ru) 2013-03-14 2016-08-31 КОНВЕРДЖЕН ЭлЭлСи Способы и композиции для ингибирования бромодомен-содержащих белков
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
WO2014152029A2 (en) 2013-03-15 2014-09-25 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
CN105073747B (zh) 2013-03-15 2017-06-06 普莱希科公司 杂环化合物及其应用
EA035469B1 (ru) 2013-03-15 2020-06-22 Инсайт Холдингс Корпорейшн Трициклические гетероциклы как ингибиторы белков бэт
US9199988B2 (en) 2013-03-27 2015-12-01 Boehringer Ingelheim International Gmbh Dihydroquinazolinone analogues
EP2978757B1 (en) 2013-03-27 2017-02-08 Boehringer Ingelheim International GmbH Indolinone analogues as brd4 inhibitors
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
EP2996689A1 (en) 2013-04-17 2016-03-23 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
EA027139B1 (ru) 2013-04-26 2017-06-30 Бейджин, Лтд. Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны
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
CN105209467B (zh) 2013-05-27 2018-06-08 诺华股份有限公司 咪唑并吡咯烷酮衍生物及其在治疗疾病中的用途
CA2915419A1 (en) 2013-06-17 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted phenyl-2,3-benzodiazepines
CN105473581B (zh) 2013-06-21 2019-04-23 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新取代的双环化合物
KR102307566B1 (ko) 2013-06-21 2021-10-05 제니쓰 에피제네틱스 리미티드 신규한 바이사이클릭 브로모도메인 억제제
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
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
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
US20150051208A1 (en) 2013-08-14 2015-02-19 Boehringer Ingelheim International Gmbh Pyridinones
RU2720237C2 (ru) 2013-11-18 2020-04-28 Форма Терапеутикс, Инк. Композиции, содержащие бензопиперазин, в качестве ингибиторов бромодоменов вет
BR122019007990B1 (pt) 2013-11-18 2021-05-04 Forma Therapeutics, Inc Composto, e, composição farmacêutica
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
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
HK1245246A1 (zh) 2014-12-01 2018-08-24 恒翼生物医药科技(上海)有限公司 作为溴域抑制剂的取代吡啶酮
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
CA2966452A1 (en) 2014-12-17 2016-06-23 Samuel David Brown Substituted bicyclic compounds as bromodomain inhibitors

Similar Documents

Publication Publication Date Title
JP2016525078A5 (enExample)
JP2016527263A5 (enExample)
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
JP2017538721A5 (enExample)
JP2017537946A5 (enExample)
JP2007510689A5 (enExample)
HRP20200854T1 (hr) Novi biciklički inhibitori bromodomene
AU2013365926A2 (en) Novel heterocyclic compounds as bromodomain inhibitors
WO2015015318A4 (en) Novel quinazolinones as bromodomain inhibitors
JP2017532360A5 (enExample)
JP2019504009A5 (enExample)
JP2012507566A5 (enExample)
AU2018233402A1 (en) Pyrimidinyl-pyridyloxy-naphthyl compounds and methods of treating ire1-related diseases and disorders
TW200536851A (en) Compounds and methods of use
JP2010510319A5 (enExample)
CN101743241A (zh) 哒嗪酮衍生物
BRPI0418082B1 (pt) Derivados de tiazol úteis como antagonistas de receptor de adenosina A2A
JP2020512401A5 (enExample)
KR20210058277A (ko) 피롤로피리미딘, 피롤로피리딘, 인다졸 화합물 유도체 및 이를 포함하는 치료용 약학 조성물
RU2025105237A (ru) Бициклические производные тетрагидроазепина
HK1224658A1 (en) Novel substituted bicyclic compounds as bromodomain inhibitors