-
公开(公告)号：US20230167132A1
公开(公告)日：2023-06-01
申请号：US17919212
申请日：2021-04-16
发明人： Suresh Kumar Tipparaju , Jeffrey Scott DePue , Helge Alfred Reisch , Samuel Alexander Stratford , Joseph Stephen Harris , Nikolaos Papaioannou , Sarah Jocelyn Fink
IPC分类号： C07D519/00 , C07C59/245 , C07C55/07 , C07C55/10 , C07C59/255 , C07C309/04 , C07C57/15 , C07C69/84
CPC分类号： C07D519/00 , C07C59/245 , C07C55/07 , C07C55/10 , C07C59/255 , C07C309/04 , C07C57/15 , C07C69/84 , C07B2200/13
摘要： The present invention provides solid forms of compound (1) and compositions thereof which are useful as inhibitors of Plasma Kallikrein (pKal) and which exhibit desirable characteristics for the same.
-
公开(公告)号：US10913705B2
公开(公告)日：2021-02-09
申请号：US15524587
申请日：2015-11-05
IPC分类号： C07C229/76 , A61K31/295 , C07C229/08 , C07C321/14 , C07C229/24 , C07C59/255 , C07C59/245 , C07C59/265 , C07C59/08 , C07D207/16 , A23L33/165 , A23L33/175 , A23C9/13 , A23C9/152 , A23G3/44 , A23L2/52
摘要： The invention describes hydrosoluble iron (III) oxyhydroxide complexes prepared from different sources of iron, amino acids and carboxylic acids. The iron (III) complexes have no undesirable residual taste and can be used as supplementation forms for the prevention or treatment of iron deficiency anemia in humans or animals and pharmaceutical or food compositions containing them.
-
3.发明申请公开(公告)号：US20200323836A1
公开(公告)日：2020-10-15
申请号：US16687467
申请日：2019-11-18
IPC分类号： A61K31/4468 , A61K45/06 , C07D211/58 , A61K31/194 , C07C59/255 , A61K9/20
摘要： Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonist may confer antipsychotic and ant dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
-
4.发明授权公开(公告)号：US10525046B2
公开(公告)日：2020-01-07
申请号：US16019485
申请日：2018-06-26
IPC分类号： A61K31/4468 , A61K31/194 , A61K45/06 , C07D211/58 , C07C59/255 , A61K9/20
摘要： Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
-
公开(公告)号：US10519150B2
公开(公告)日：2019-12-31
申请号：US16066490
申请日：2016-12-29
发明人： Guangxin Xia , Jianshu Xie , Guohui Jia , Jiansheng Han , Naoko Ueda , Toru Iijima
IPC分类号： C07D471/04 , A61K31/5377 , C07C51/41 , C07C53/10 , C07C59/245 , C07C59/255 , C07C309/35 , C07C51/43
摘要： The present invention provides novel pharmaceutically acceptable salts of a morpholine derivative, including a malate, a tartrate, a hydrochloride, an acetate, and a naphthalene disulfonate thereof, wherein the tartrate has 3 crystal salt forms: crystal form A, crystal form B and dihydrate; the malate, the hydrochloride, and the acetate each have one crystal salt form; the naphthalene disulfonate is amorphous. When compared to the known morpholine derivative free base, the present invention has one or more improved properties, e.g., a better crystalline state, greatly improved water solubility, light stability and thermal stability, etc. The present invention further provides preparation methods for the salts of morpholine derivative and the crystal forms thereof, pharmaceutical compositions and use thereof.
-
公开(公告)号：US20180228753A1
公开(公告)日：2018-08-16
申请号：US15866303
申请日：2018-01-09
IPC分类号： A61K31/198 , C07D307/62 , C07C57/15 , C07C229/12 , A61K47/12 , C07C59/255
CPC分类号： A61K31/198 , A61K47/12 , C07B2200/13 , C07C57/15 , C07C59/255 , C07C229/12 , C07D307/62
摘要： The present disclosure provides co-crystals of a substituted glycine compound and a co-former compound of Formula (I): compositions comprising such, and uses thereof in treating and/or reducing the risk for a neuropsychiatric disorder (e.g., schizophrenia, psychotic disorders, depressive disorders, suicidal ideation and/or behavior, obsessive compulsive disorder or Alzheimer's disease). Also provided herein are methods for preparing the co-crystals.
-
公开(公告)号：US09994515B2
公开(公告)日：2018-06-12
申请号：US14915194
申请日：2014-08-29
发明人： Sabyasachi Sanyal , Atul Kumar , Naibedya Chattopadhyay , Jawahar Lal , Arun Kumar Trivedi , Dipak Datta , Srikanta Kumar Rath , Tahseen Akhtar , Shailendra Kumar Dhar Dwivedi , Manisha Yadav , Bandana Chakravarti , Abhishek Kumar Singh , Jay Sharan Mishra , Nidhi Singh , Anil Kumar Tripathi
IPC分类号： C07C251/48 , C07C251/58 , C07C251/60 , C07C55/07 , C07C57/15 , C07C59/255 , C07C59/265 , C07C249/08 , C07C319/02 , C07C321/26 , C07D295/088
CPC分类号： C07C251/48 , C07C55/07 , C07C57/15 , C07C59/255 , C07C59/265 , C07C249/08 , C07C251/58 , C07C251/60 , C07C319/02 , C07C321/26 , C07D295/088
摘要： The present invention relates to substituted aryl naphthyl methanone oximes of general formula (I), their process for preparation and their derivatives, salts, pharmaceutical composition thereof and their use in treatment of chronic myelogenous leukemia, acute myelogenous leukemia, lymphoma, multiple myeloma, solid tumor forming cell-lines including such as breast cancer, endometrial cancer colon cancer, prostate cancer and killing of drug resistant cancer stem cells, as subject in need thereof.
-
公开(公告)号：US09862719B2
公开(公告)日：2018-01-09
申请号：US14804847
申请日：2015-07-21
申请人： Gruenenthal GmbH
发明人： Claudia Hinze , Otto Aulenbacher , Bernd Sundermann , Stefan Oberboersch , Elmar Friderichs , Werner Englberger , Babette-Yvonne Koegel , Klaus Linz , Hans Schick , Helmut Sonnenschein , Birgitta Henkel , Valerie Sarah Rose , Michael Jonathan Lipkin
IPC分类号： C07D209/58 , C07D471/10 , C07C59/265 , C07C59/255 , C07C309/06 , C07C309/04 , C07D491/107 , C07D491/10 , C07D493/10 , C07D495/10
CPC分类号： C07D471/10 , C07C59/255 , C07C59/265 , C07C309/04 , C07C309/06 , C07D491/10 , C07D491/107 , C07D493/10 , C07D495/10
摘要： Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.
-
公开(公告)号：US09745264B2
公开(公告)日：2017-08-29
申请号：US15103195
申请日：2014-10-20
发明人： Hong Gu , Jian Cao , Liushan Chen , Luning Huang
IPC分类号： C07D209/08 , C07C51/41 , C07C59/255 , C07C303/32 , C07C309/25
CPC分类号： C07D209/08 , C07C51/41 , C07C59/255 , C07C303/32 , C07C309/25 , C07C2602/42
摘要： Provided is a method for preparing silodosin. Also provided is a method for preparing an organic acid salt of a new intermediate 3-(7-cyano-5-((R)-2-((R)-1-phenylethylamino)propyl)-1-hydrogen-indolyl) propyl alcohol (ester or ether), and a new intermediate 3-(7-cyano-5-((R)-2-(((R)-1-phenethyl)(2-(2-(trifluoroethoxy)phenoxy) ethyl)amino)propyl)1-hydrogen-indolyl)propyl alcohol (ester or ether) and a salt thereof. The method has the following advantages: raw materials are cheap and easy to obtain, the operation is simple, the intermediate and product are easy to purify, the yield is high, and the method is applicable to industrial production.
-
10.发明申请公开(公告)号：US20170144989A1
公开(公告)日：2017-05-25
申请号：US15367808
申请日：2016-12-02
申请人： AMPLIO PHARMA, LLC
IPC分类号： C07D401/04 , C07C59/255 , C07C55/07 , C07C55/08 , C07C65/03 , C07C69/84
CPC分类号： C07D401/04 , A61K31/4035 , C07B2200/13 , C07C55/07 , C07C55/08 , C07C59/255 , C07C65/03 , C07C69/84 , C07C275/02
摘要： The invention relates to novel crystalline forms of 3-(4-amino-l-oxo-l,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione, including a novel urea cocrystal of 3-(4-amino-l-oxo-l,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel gallic acid cocrystal of 3-(4-amino-l-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel propyl gallate cocrystal of 3-(4-amino-l-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; and a novel L-tartaric acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention are described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, and the therapeutic use of the novel crystalline forms.
-
-
-
-
-
-
-
-
-
搜索结果
215 条记录 (耗时 0.027 秒)
