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91. 发明申请

WO2019173327A1 IMIDAZODIAZEPINEDIONES AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2019173327A1
公开(公告)日：2019-09-12
申请号：PCT/US2019/020732
申请日：2019-03-05
申请人： GOLDFINCH BIO, INC.
发明人： DANIELS, Matthew, H. , YU, Maolin , HARMANGE, Jean-Christophe, P. , TIBBITTS, Thomas, T. , LEDEBOER, Mark, W. , CASTLE, Neil, A. , MALOJCIC, Goran
IPC分类号： A61K31/551 , A61K31/5513 , A61K31/5517 , C07D243/06 , C07D243/10 , C07D243/12
摘要： Disclosed are compounds according to Formula (I) or (II), and pharmaceutical compositions comprising them. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (I) or (II).

92. 发明申请

WO2019056950A1 噻吩并二氮杂卓衍生物及其应用审中-公开
公开(公告)号：WO2019056950A1
公开(公告)日：2019-03-28
申请号：PCT/CN2018/104345
申请日：2018-09-06
申请人：南京明德新药研发股份有限公司
发明人：沈春莉 , 吴成德 , 刘勇 , 龚珍 , 黎健 , 陈曙辉
IPC分类号： C07D495/14 , C07D243/06 , A61K31/55 , A61K45/00 , A61P35/00 , A61P43/00
摘要：本发明涉及一类噻吩并二氮杂卓衍生物，及其在制备治疗与BET Bromodomain抑制剂相关疾病的药物中的应用。具体涉及式(Ⅰ)、(Ⅱ)所示化合物及其药学上可接受的盐。

93. 发明申请

WO2017215600A1 SUBSTITUTED TRICYCLIC HERTEOCYCLIC COMPOUNDS AND USE THEREOF 审中-公开
标题翻译：取代的三环杂环化合物及其用途
公开(公告)号：WO2017215600A1
公开(公告)日：2017-12-21
申请号：PCT/CN2017/088137
申请日：2017-06-13
申请人： SUZHOU YABAO PHARMACEUTICAL R&D CO., LTD. , LifeArc
发明人： XIA, Yan , MCIVER, Edward, Giles , SONG, Yang , XU, Yuanyuan , ZHU, Lin , CHU, Chunjun , WU, Ling , LIU, Miao , BRYANS, Justin, Stephen
IPC分类号： C07D491/14 , C07D267/04 , C07D487/04 , C07D243/06 , C07D498/04 , C07D519/00 , A61P35/00 , A61P25/00 , A61K31/437 , A61K31/4162
摘要： Provided are a substituted tricyclic herteocyclic compound of formula I or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt, ester or a prodrug thereof, a pharmaceutical composition including the same and uses thereof. The substituted tricyclic herteocyclic compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be used for treating a disorder caused by at least one of cancer and neurodegenerative diseases. Further the compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be also used for preventing or treating a disorder caused by, associated with or accompanied by any abnormal kinase activity.
摘要翻译：提供式I的取代的三环式并环化合物或其立体异构体，互变异构体，N-氧化物，水合物，溶剂合物，代谢物，药学上可接受的盐，酯或前药，包含其的药物组合物及其用途。取代的三环式脱环化合物和包含本文公开的化合物的药物组合物可用于治疗由癌症和神经变性疾病中的至少一种引起的病症。此外，包含本文公开的化合物的化合物和药物组合物还可以用于预防或治疗由任何异常激酶活性引起的，伴随或伴随的异常。

94. 发明申请

WO2004089313A3 NOVEL OLANZAPINE FORMS AND RELATED METHODS OF TREATMENT 审中-公开
标题翻译：新型奥兰波星形式及相关治疗方法
公开(公告)号：WO2004089313A3
公开(公告)日：2005-11-24
申请号：PCT/US2004009947
申请日：2004-03-31
申请人： TRANSFORM PHARMACEUTICALS INC , HICKEY MAGALI BOURGHOL , REMENAR JULIUS
发明人： HICKEY MAGALI BOURGHOL , REMENAR JULIUS
IPC分类号： A01N43/62 , A61K20060101 , A61K9/64 , A61K31/55 , A61P25/00 , C07D233/74 , C07D243/06 , C07D243/10
CPC分类号： A61K31/5513 , C07D513/04
摘要： The invention provides novel soluble olanzapine forms. These forms include salts, co-crystals, and solvates of olanzapine. The invention also provides novel pharmaceutical compositions comprising these novel soluble forms and related methods of treatment. Compositions and methods of the invention of the invention are useful in the treatment of psychosis and functional bowel disorders.
摘要翻译：本发明提供新的可溶性奥氮平形式。这些形式包括奥氮平的盐，共晶体和溶剂合物。本发明还提供包含这些新型可溶形式和相关治疗方法的新型药物组合物。本发明的组合物和方法可用于治疗精神病和功能性肠病。

95. 发明申请

WO9009092A3 NOVEL POTENT INDUCERS OF TERMINAL DIFFERENTIATION AND METHOD OF USE THEREOF 审中-公开
标题翻译：终末分化的新型感受器及其使用方法
公开(公告)号：WO9009092A3
公开(公告)日：1990-10-04
申请号：PCT/US8905203
申请日：1989-11-14
申请人： UNIV COLUMBIA , SLOAN KETTERING INST CANCER
发明人： MARKS PAUL A , RIFKIND RICHARD A , BRESLOW RONALD
IPC分类号： C07D243/06 , A61K31/415 , A61K31/505 , A61P35/00 , C07C233/05 , C07C233/36 , C07C235/74 , C07C243/28 , C07C259/06 , C07D231/32 , C07D231/36 , C07D239/62 , C07D243/08
CPC分类号： C07C233/05 , C07C233/36 , C07C235/74 , C07C243/28 , C07C259/06 , C07D231/32 , C07D239/62 , C07D243/08
摘要： The invention provides a class of compounds having two or more nonpolar components connected by a polar group and having polar groups on the termini of the compound. The invention also concerns a method of selectively inducing termini differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable condition with an amount of the compound effect to selectively induce terminal differentiation. Moreover, the invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells, thereby inhibiting their proliferation and suppressing oncogenicity. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound in an amount effective less than an amount which would cause toxicity in the patient.

96. 发明申请

WO1990009092A2 NOVEL POTENT INDUCERS OF TERMINAL DIFFERENTIATION AND METHOD OF USE THEREOF 审中-公开
标题翻译：终末分化的新型感受器及其使用方法
公开(公告)号：WO1990009092A2
公开(公告)日：1990-08-23
申请号：PCT/US1989005203
申请日：1989-11-14
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY ... , SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , MARKS, Paul, A. , RIFKIND, Richard, A. , BRESLOW, Ronald
发明人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY ... , SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
IPC分类号： C07D243/06 , A61K31/415 , A61K31/505 , A61P35/00 , C07C233/05 , C07C233/36 , C07C235/74 , C07C243/28 , C07C259/06 , C07D231/32 , C07D231/36 , C07D239/62 , C07D243/08
CPC分类号： C07C233/05 , C07C233/36 , C07C235/74 , C07C243/28 , C07C259/06 , C07D231/32 , C07D239/62 , C07D243/08
摘要： The invention provides a class of compounds having two or more nonpolar components connected by a polar group and having polar groups on the termini of the compound. The invention also concerns a method of selectively inducing termini differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable condition with an amount of the compound effect to selectively induce terminal differentiation. Moreover, the invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells, thereby inhibiting their proliferation and suppressing oncogenicity. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound in an amount effective less than an amount which would cause toxicity in the patient.
摘要翻译：本发明提供一类具有两个或更多个非极性组分的化合物，其通过极性基团连接并且在化合物的末端具有极性基团。本发明还涉及选择性诱导肿瘤细胞的终末分化并由此抑制这些细胞增殖的方法，其包括在合适的条件下将细胞与一定量的化合物作用接触以选择性诱导终末分化。此外，本发明提供了一种治疗肿瘤特征在于肿瘤细胞增殖的患者的方法，其包括给予患者一定量的有效选择性诱导这些肿瘤细胞的终末分化，从而抑制其增殖并抑制致癌性的化合物。最后，本发明提供了药物组合物，其包含药学上可接受的载体和化合物，其量有效量小于在患者中引起毒性的量。

97. 发明申请

WO2016022902A1 DIAZEPANE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： DIAZEPANE衍生物及其用途
公开(公告)号：WO2016022902A1
公开(公告)日：2016-02-11
申请号：PCT/US2015/044180
申请日：2015-08-07
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： BRADNER, James, E. , BUCKLEY, Dennis
IPC分类号： C07D487/04 , C07D243/06
CPC分类号： C07D487/04
摘要： The present disclosure provides compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) have been found to bind bromodomains and/or bromodomain-containing proteins ( e.g. , bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits of the compounds and pharmaceutical compositions for inhibiting the activity ( e.g. , increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins ( e.g. , proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, neurological diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
摘要翻译：本公开内容提供式（I）的化合物及其药学组合物。已经发现式（I）的化合物结合溴结构域和/或含溴结构域的蛋白质（例如溴和额外末端（BET）蛋白））。还提供了用于抑制溴结构域和/或含溴结构域的蛋白质的活性（例如，增加的活性）以及用于治疗和/或预防与溴结构域或溴结构域相关的疾病的化合物和药物组合物的方法，用途和试剂盒（例如，增殖性疾病，心血管疾病，病毒感染，纤维化疾病，神经疾病，代谢疾病，内分泌疾病和放射线中毒）。化合物，药物组合物和试剂盒也可用于男性避孕。

98. 发明申请

WO2009058238A1 SUBSTITUTED DIAZEPAN OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：取代的DIAZEPAN OREXIN受体拮抗剂
公开(公告)号：WO2009058238A1
公开(公告)日：2009-05-07
申请号：PCT/US2008/012182
申请日：2008-10-27
申请人： MERCK & CO., INC. , BERGMAN, Jeffrey, M. , COLEMAN, Paul, J. , COX, Christopher, D. , ROECKER, Anthony, J.
发明人： BERGMAN, Jeffrey, M. , COLEMAN, Paul, J. , COX, Christopher, D. , ROECKER, Anthony, J.
IPC分类号： A61K31/551 , A61P43/00 , C07D243/06
CPC分类号： C07D403/14 , C07D403/04 , C07D413/14 , C07D417/14
摘要： The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲素受体的拮抗剂的二氮杂环庚烷化合物，其可用于治疗神经性和精神疾病以及食欲素受体参与的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗其中涉及食欲素受体的疾病中的用途。

99. 发明申请

WO2007117180A1 АЗАГЕТЕРОЦИКЛЫ, КОМБИНАТОРНАЯ БИБЛИОТЕКА, ФОКУСИРОВАННАЯ БИБЛИОТЕКА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ 审中-公开
标题翻译： AZAHETEROCYCLES，组合图书馆，聚焦图书馆，药物组合物及其生产方法
公开(公告)号：WO2007117180A1
公开(公告)日：2007-10-18
申请号：PCT/RU2007/000163
申请日：2007-04-06
申请人： ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ «ИССЛЕДОВАТЕЛЬСКИЙ ИНСТИТУТ ХИМИЧЕСКОГО РАЗНООБРАЗИЯ» , ИВАЩЕНКО Александр Васильевич , ИЛЬИН Алексей Петрович , КИСЕЛЬ Владимир Михайлович , ТРИФИЛЕНКОВ Андрей Сергеевич , ЦИРУЛЬНИКОВ Сергей Александрович , ШКИРАНДО Александр Михайлович , ЧУРАКОВА Марина Васильевна , ЛОМАКИНА Ирина Олеговна , ПОТАПОВ Виктор Владимирович , ЗАМАЛЕТДИНОВА Анастасия Ильясовна , ТКАЧЕНКО Сергей Евгеньевич , КРАВЧЕНКО Дмитрий Владимирович , ХВАТ Александр Викторович , ОКУНЬ Илья Матусович , КИСЕЛЕВ Александр Сергеевич
发明人： ИВАЩЕНКО Александр Васильевич , ИЛЬИН Алексей Петрович , КИСЕЛЬ Владимир Михайлович , ТРИФИЛЕНКОВ Андрей Сергеевич , ЦИРУЛЬНИКОВ Сергей Александрович , ШКИРАНДО Александр Михайлович , ЧУРАКОВА Марина Васильевна , ЛОМАКИНА Ирина Олеговна , ПОТАПОВ Виктор Владимирович , ЗАМАЛЕТДИНОВА Анастасия Ильясовна , ТКАЧЕНКО Сергей Евгеньевич , КРАВЧЕНКО Дмитрий Владимирович , ХВАТ Александр Викторович , ОКУНЬ Илья Матусович , КИСЕЛЕВ Александр Сергеевич
IPC分类号： C07D223/10 , C07D223/16 , C07D241/06 , C07D241/08 , C07D241/36 , C07D243/06 , C07D243/08 , C07D243/10 , C07D243/12 , C07D245/04 , C07D245/06 , C07D255/02 , C07D255/04 , C07D493/10 , C07D495/04 , C07D495/10 , C07D495/14 , C07D498/04 , C07D498/14 , C07D507/02 , C07D513/04 , C07D513/14 , C40B40/04 , C07D267/00 , C07D267/22 , C07D267/14 , C07D281/06 , C07D281/08 , C07D283/00 , C07D285/38 , C07D321/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/06 , C07D417/04 , A61K31/381 , A61K31/395 , A61K31/444 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/4985 , C07D417/06 , C07D471/04 , C07D471/10 , C07D471/20 , C07D487/04 , C07D487/14 , C07D491/04 , C07D491/048 , C07D491/056 , C07D491/107 , C07D491/14 , C07D491/147 , C07D491/153 , C07D491/18 , A61K31/519 , A61K31/5395 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , A61P35/00
CPC分类号： C07D487/04 , C07D223/10 , C07D223/16 , C07D223/20 , C07D241/08 , C07D243/08 , C07D243/10 , C07D243/14 , C07D243/24 , C07D245/04 , C07D245/06 , C07D255/04 , C07D267/14 , C07D267/22 , C07D281/10 , C07D285/00 , C07D285/38 , C07D321/00 , C07D401/12 , C07D403/06 , C07D471/04 , C07D471/14 , C07D487/14 , C07D491/04 , C07D491/048 , C07D491/14 , C07D491/18 , C07D495/04 , C07D495/14 , C07D498/04 , C07D498/14 , C07D498/16 , C07D513/04 , C07D513/14
摘要： Изобретение относится к новым азагетероциклам, представляющим интерес как потенциальные физиологически активные вещества ( агонисты, антагонисты и модуляторы рецепторов, ингибиторы ферментов, онколитики, антибактериальные и противопаразитарные агенты и т.д. ), к комбинаторной и фокусированной библиотекам, включающим новые азагетероциклы, фармацевтической композиции, содержащей в качестве активной субстанции новые азагетероциклы, к способам их получения и применения. Предложены новые азагетероциклы общей формулы 1, где: W представляет собой азогетероцикл, включающий 6-12 атомов, необязательно аннелированный, по крайней мере, с одним С 5 – С 7 карбоциклом и/или гетероциклом, включающий, по крайней мере, один из гетероатомов, выбранный из группы О, S или N; R 1 a представляет собой заместитель аминогруппы, исключая водород, предпочтительно, C 1 – C 6 алкил, арил или гетероциклил, включающий, по крайней мере, один из гетероатомов, выбранных из группы О, S или N; R b представляют собой карбамоильную группу – С (О) NHR a , в которой R a представляет собой заместитель аминогруппы, исключая водород; R с представляют собой заместитель циклической системы, предпочтительно, C 1 – C 6 алкил, арил или гетероциклил, включающий, по крайней мере, один из гетероатомов, выбранных из группы О, S, или N, или R b и R с вместе образуют амино – циано – метиленовую группу [( = С(NH 2 )CN].
摘要翻译：本发明涉及作为潜在的生理活性物质（激动剂，拮抗剂，受体调节剂，发酵抑制剂，溶瘤剂，抗细菌剂和抗寄生虫剂等）的新型氮杂杂环化合物，其包含含有所述新型氮杂环的药物组合物的新型氮杂杂环以活性物质的形式，以及生产和使用方法。所述新型氮杂环是通式（1），其中W是包含6-12个原子的氮杂环，任选地被延长，具有至少一个C 5 -C 7 - 并且还包含杂原子中的至少一个并且选自O，S或N基团; [R ₁

100. 发明申请

WO99066934A1 CYCLIC AMINO ACID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING beta -AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS 审中-公开
标题翻译：包含氨基酸的化合物，包含其的药物组合物，以及用于抑制β-亚氨基肽释放和/或通过使用这些化合物合成的方法
公开(公告)号：WO99066934A1
公开(公告)日：1999-12-29
申请号：PCT/US1999/014211
申请日：1999-06-22
IPC分类号： A61K38/00 , A61K31/55 , A61P25/28 , A61P43/00 , C07D223/14 , C07D223/16 , C07D223/18 , C07D243/06 , C07D243/10 , C07D243/12 , C07D243/14 , C07D243/24 , C07D267/02 , C07D267/14 , C07D281/02 , C07D281/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07D471/04 , C07D471/06 , C07D471/08 , C07D487/02 , C07D487/04 , C07D487/12 , C07D498/02 , C07D513/02 , C07K4/00
CPC分类号： A61K31/55 , A61K38/00 , C07D223/14 , C07D223/16 , C07D223/18 , C07D243/06 , C07D243/10 , C07D243/12 , C07D243/14 , C07D243/24 , C07D267/02 , C07D267/14 , C07D281/02 , C07D281/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07D471/04 , C07D471/06 , C07D471/08 , C07D487/02 , C07D487/04 , C07D487/12 , C07D498/02 , C07D513/02 , C07K4/00
摘要： Disclosed are compounds which inhibit beta -amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta -amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要翻译：公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物，因此具有治疗阿尔茨海默氏病的效用。还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及预防和治疗这些药物组合物的阿尔茨海默氏病的方法。

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