-
公开(公告)号：US11986481B2
公开(公告)日：2024-05-21
申请号：US18393813
申请日：2023-12-22
IPC分类号： A61K31/53 , A61K31/50 , A61P5/14 , A61P9/00 , C07D237/16 , C07D403/02 , C07D403/12
CPC分类号： A61K31/53 , A61K31/50 , A61P5/14 , A61P9/00 , C07D237/16 , C07D403/02 , C07D403/12 , C07B2200/13 , Y02P20/55
摘要： The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.
-
公开(公告)号：US11773064B2
公开(公告)日：2023-10-03
申请号：US17863941
申请日：2022-07-13
发明人： Gianluca Mariano Enrico Papeo , Mikhail Yurievitch Krasavin , Paolo Orsini , Alessandra Scolaro
IPC分类号： A61K31/4035 , C07D209/44 , C07D401/06 , C07D209/46 , C07D401/14 , C07D403/02 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/14 , A61K31/4188 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/5377
CPC分类号： C07D209/44 , A61K31/4035 , A61K31/4188 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/5377 , C07D209/46 , C07D401/06 , C07D401/14 , C07D403/02 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/14
摘要： There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-I with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
-
公开(公告)号：US20170275272A1
公开(公告)日：2017-09-28
申请号：US15468230
申请日：2017-03-24
发明人： Zulan Pi , Donna M. Bilder , Robert Paul Brigance , Heather Finlay , Wen Jiang , James A. Johnson , R. Michael Lawrence , Wei Meng , Michael C. Myers , Monique Phillips , George O. Tora , Xiaojun Zhang
IPC分类号： C07D403/06 , C07D471/04 , C07D417/14 , C07D401/14
CPC分类号： C07D403/06 , A61K31/505 , C07D239/54 , C07D239/545 , C07D239/557 , C07D401/06 , C07D401/14 , C07D403/02 , C07D403/14 , C07D417/14 , C07D471/04
摘要： The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
-
公开(公告)号：US09717713B2
公开(公告)日：2017-08-01
申请号：US15178742
申请日：2016-06-10
申请人： MEI Pharma, Inc.
发明人： DiZhong Chen , Hong Yan Song , Eric T. Sun , Niefang Yu , Yong Zou
IPC分类号： A61K31/4184 , A61K31/4439 , A61K31/496 , A61K31/444 , A61K31/506 , C04B35/632 , C07D235/06 , C07D235/08 , C07D235/14 , C07D235/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/02 , C07D409/04 , C07D413/02 , G01N33/50 , G01N33/68 , C07D403/06 , A61K31/454 , A61K31/4709 , A61K31/5377
CPC分类号： A61K31/4184 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , C04B35/632 , C07D235/06 , C07D235/08 , C07D235/14 , C07D235/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/02 , C07D403/06 , C07D409/04 , C07D413/02 , G01N33/5011 , G01N33/6875 , Y02A50/409 , Y02A50/411 , Y02A50/414
摘要： The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).
-
公开(公告)号：US20170197915A9
公开(公告)日：2017-07-13
申请号：US14972333
申请日：2015-12-17
申请人： Genentech, Inc.
发明人： Jun Liang , Daniel Fred Ortwine , Xiaojing Wang , Steven P. Govek , Mehmet Kahraman , Johnny Y. Nagasawa , Nicholas D. Smith , Simon Charles Goodacre , Nicholas Charles Ray
IPC分类号： C07D205/04 , A61K31/404 , A61K45/06 , A61K31/397 , C07D207/04 , A61K31/40 , C07D409/12 , A61K31/4025 , C07D413/12 , A61K31/422 , C07D417/12 , A61K31/427 , C07D401/14 , A61K31/4439 , C07D411/12 , C07D403/12
CPC分类号： C07D205/04 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/416 , A61K31/422 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/5415 , A61K45/06 , C07D207/04 , C07D207/08 , C07D401/14 , C07D403/02 , C07D403/12 , C07D403/14 , C07D409/02 , C07D409/12 , C07D411/02 , C07D411/12 , C07D413/02 , C07D413/12 , C07D417/02 , C07D417/12 , C07D417/14 , C07D493/04 , A61K2300/00
摘要： Described herein are compounds that are estrogen receptor modulators of Formula (I): and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
-
公开(公告)号：US20160279102A1
公开(公告)日：2016-09-29
申请号：US15178742
申请日：2016-06-10
申请人： MEI Pharma, Inc.
发明人： DiZhong Chen , Hong Yan Song , Eric T. Sun , Niefang Yu , Yong Zou
IPC分类号： A61K31/4184 , A61K31/5377 , A61K31/506 , A61K31/496 , A61K31/4709 , A61K31/4439 , A61K31/454
CPC分类号： A61K31/4184 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , C04B35/632 , C07D235/06 , C07D235/08 , C07D235/14 , C07D235/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/02 , C07D403/06 , C07D409/04 , C07D413/02 , G01N33/5011 , G01N33/6875 , Y02A50/409 , Y02A50/411 , Y02A50/414
摘要： The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).
-
公开(公告)号：US20160122307A1
公开(公告)日：2016-05-05
申请号：US14890183
申请日：2014-05-16
发明人： CHRISTOPH ABELS , ULRICH KNIE , MICHAEL SOEBERDT
IPC分类号： C07D241/42 , C07D405/14 , C07D409/14 , A61K31/506 , C07D401/14 , A61K45/06 , A61K31/498 , C07D403/02 , C07D403/14
CPC分类号： C07D241/42 , A61K31/498 , A61K31/506 , A61K45/06 , C07B2200/07 , C07D401/06 , C07D401/14 , C07D403/02 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/14
摘要： The present invention relates to perhydroquinoxaline compounds according to the general formula (1), their use as a medicament, in particular as analgesic, antipruritic and anti-inflammatory agents, and their preparation.
摘要翻译： 本发明涉及根据通式（1）的全氢化喹喔啉化合物，其用作药物，特别是镇痛，止痒和抗炎剂及其制备。
-
公开(公告)号：US09266861B2
公开(公告)日：2016-02-23
申请号：US14660720
申请日：2015-03-17
发明人： D. Keith Hester, II , Robert J. Duguid , Martha J. Kelly , Anna Chasnoff , Gang Dong , Edwin L. Crow , Duk Soon Choi , Lianhe Shu , Ping Wang
IPC分类号： C07D403/12 , C07D403/02 , C07D237/16 , A61K31/53 , A61K31/50
CPC分类号： A61K31/53 , A61K31/50 , C07B2200/13 , C07D237/16 , C07D403/02 , C07D403/12
摘要： The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.
摘要翻译： 本公开描述了合成哒嗪酮化合物作为甲状腺激素类似物及其前药的方法。 根据本公开的优选方法允许大规模制备具有高纯度的哒嗪酮化合物。 在一些实施方案中，根据本公开的优选方法还允许以比以前使用的制备这些化合物的方法更好地制备哒嗪酮化合物。 还公开了哒嗪酮化合物的形态。 进一步公开的是在具有至少一种TR＆bgr的受试者中治疗对甲状腺激素的抗性的方法; 突变。
-
9.发明申请公开(公告)号：US20160039840A1
公开(公告)日：2016-02-11
申请号：US14820725
申请日：2015-08-07
发明人： Aleem Gangjee
IPC分类号： C07D495/04 , C07D487/04
CPC分类号： C07D495/04 , A61K31/343 , A61K31/4709 , A61K31/505 , C07D239/48 , C07D403/02 , C07D405/02 , C07D487/04
摘要： The present invention discloses a compound comprising the formula: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH2, and optionally comprising a pharmaceutically acceptable salt, hydrate, or solvate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof.
摘要翻译： 本发明公开了一种包含下式的化合物：其中R是氢或具有1-10个碳原子的烷基，或下式化合物其中S被CH 2取代，并且任选地包含药学上可接受的盐，水合物， 或其溶剂合物。 一种治疗患有癌症或疾病的患者的方法，包括向患者施用有效量的化合物或其药学上可接受的盐，水合物或溶剂合物。
-
10.发明申请PYRIDINE DERIVATIVES AS PIM KINASE INHIBITORS AND PREPARATION METHODS AND USE IN MEDICINAL MANUFACTURE THEREOF 有权吡啶衍生物作为PIM激酶抑制剂及其制备方法及其在医药制造中的应用公开(公告)号：US20150284363A1
公开(公告)日：2015-10-08
申请号：US14746773
申请日：2015-06-22
发明人： Yu GE
IPC分类号： C07D401/12 , C07D405/12 , C07D401/14
CPC分类号： C07D401/12 , A61K31/444 , C07D213/81 , C07D401/14 , C07D403/02 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/02 , C07D451/06 , C07D453/02 , C07D471/08 , C07D487/08
摘要： PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, multi drug resistance, and inflammatory bowel disease. Also provided are methods for preparing and using the compounds represented by Formula I.
摘要翻译： 具有式I所示结构的PIM激酶抑制剂化合物及其异构体，非对映体，对映体，互变异构体及其药学上可接受的盐。 这些化合物显着抑制Pim激酶活性，并用于制备药物以治疗PIM激酶介导的疾病，如癌症，多药耐药和炎症性肠病。 还提供了制备和使用由式I表示的化合物的方法。
-
-
-
-
-
-
-
-
-
搜索结果
226 条记录 (耗时 0.044 秒)
