公开(公告)号：US20210130301A1

公开(公告)日：2021-05-06

申请号：US17142586

申请日：2021-01-06

申请人： Vectus Biosystems Limited

发明人： Karen Annette DUGGAN

IPC分类号： C07D239/26 ,  A61P11/00 ,  C07C39/15 ,  C07C215/54 ,  C07C233/11 ,  C07D207/408 ,  C07D213/56 ,  C07D237/08 ,  C07D261/14 ,  C07D263/44 ,  C07D277/30 ,  C07D401/10 ,  C07D403/10 ,  C07D333/24 ,  C07C233/07 ,  C07D231/56 ,  C07D235/26 ,  C07D235/06 ,  C07C59/52 ,  C07C275/42 ,  C07D213/73 ,  C07D277/68 ,  A61P11/06 ,  C07D231/12 ,  C07C211/29 ,  C07D207/38 ,  C07C255/00 ,  C07C271/28 ,  C07C217/48 ,  C07C261/04 ,  C07D241/12 ,  C07D309/10 ,  C07D233/78 ,  C07D261/08 ,  C07D209/48 ,  C07C237/20 ,  C07D207/327 ,  C07C237/22 ,  C07D307/54 ,  C07D249/18 ,  C07D209/34 ,  C07D263/38 ,  C07C307/10 ,  C07D207/26 ,  C07D207/444 ,  C07C235/34 ,  C07C311/03 ,  C07C311/08 ,  C07C239/20 ,  C07C235/78 ,  C07D209/18 ,  C07D263/58 ,  C07D215/14 ,  C07D207/40

摘要： The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

公开(公告)号：US10258602B2

公开(公告)日：2019-04-16

申请号：US15938038

申请日：2018-03-28

申请人： Ocera Therapeutics, Inc.

发明人： Hamid Hoveyda ,  Graeme Fraser ,  Kamel Benakli ,  Eric Marsault ,  Mark L. Peterson

IPC分类号： A61K38/00 ,  A61K31/395 ,  C07D273/00 ,  C07C271/16 ,  C07C215/42 ,  C07C215/54 ,  C07D413/06 ,  C07D498/04 ,  C07D498/16

摘要： The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

公开(公告)号：US09949949B2

公开(公告)日：2018-04-24

申请号：US15178303

申请日：2016-06-09

申请人： OCERA THERAPEUTICS, INC.

发明人： Hamid Hoveyda ,  Graeme Fraser ,  Kamel Benakli ,  Eric Marsault ,  Mark L. Peterson

IPC分类号： C07K5/12 ,  A61K31/395 ,  C07D273/00 ,  C07C271/16 ,  C07C215/42 ,  C07C215/54 ,  C07D413/06 ,  C07D498/04 ,  C07D498/16

CPC分类号： A61K31/395 ,  C07C215/42 ,  C07C215/54 ,  C07C271/16 ,  C07C2601/14 ,  C07D273/00 ,  C07D413/06 ,  C07D498/04 ,  C07D498/16

摘要： The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone sceretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

公开(公告)号：US20180072682A1

公开(公告)日：2018-03-15

申请号：US15557762

申请日：2016-03-18

申请人： VECTUS BIOSYSTEMS LIMITED

发明人： KAREN ANNETTE DUGGAN

IPC分类号： C07D233/78 ,  C07C215/54 ,  C07D207/26 ,  C07D207/38 ,  C07D233/96 ,  C07D261/14 ,  C07D263/38 ,  C07C239/20 ,  C07D263/44 ,  C07D209/48 ,  C07C59/54 ,  C07C39/12

CPC分类号： C07D233/78 ,  C07C39/12 ,  C07C39/15 ,  C07C47/575 ,  C07C59/52 ,  C07C59/54 ,  C07C215/48 ,  C07C215/54 ,  C07C239/20 ,  C07D207/26 ,  C07D207/267 ,  C07D207/36 ,  C07D207/38 ,  C07D207/408 ,  C07D207/448 ,  C07D209/48 ,  C07D233/96 ,  C07D261/14 ,  C07D263/38 ,  C07D263/44

摘要： The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions.

公开(公告)号：US09371297B2

公开(公告)日：2016-06-21

申请号：US12028611

申请日：2008-02-08

申请人： Hamid Hoveyda ,  Graeme L. Fraser ,  Kamel Benakli ,  Sophie Beauchemin ,  Martin Brassard ,  Eric Marsault ,  Luc Oullet ,  Mark L. Peterson ,  Zhigang Wang

发明人： Hamid Hoveyda ,  Graeme L. Fraser ,  Kamel Benakli ,  Sophie Beauchemin ,  Martin Brassard ,  Eric Marsault ,  Luc Oullet ,  Mark L. Peterson ,  Zhigang Wang

IPC分类号： C07K5/12 ,  C07D273/00 ,  C07C271/16 ,  C07C215/42 ,  C07C215/54 ,  C07D413/06 ,  C07D498/04 ,  C07D498/16

CPC分类号： A61K31/395 ,  C07C215/42 ,  C07C215/54 ,  C07C271/16 ,  C07C2601/14 ,  C07D273/00 ,  C07D413/06 ,  C07D498/04 ,  C07D498/16

摘要： The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

摘要翻译： 本发明提供新的构象定义的大环化合物，其可以作为生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的选择性调节剂。 本文还描述了合成新化合物的方法。 这些化合物可用作生长素释放肽受体的激动剂，并且用作治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病，胃肠道疾病，心血管疾病，肥胖症和肥胖相关疾病， 中枢神经系统疾病，骨骼疾病，遗传疾病，过度增殖性疾病和炎症性疾病。

公开(公告)号：US20150152044A1

公开(公告)日：2015-06-04

申请号：US14406649

申请日：2013-06-14

申请人： ratiopharm GmbH

发明人： Simone Eichner ,  Wolfgang Albrecht

IPC分类号： C07C215/54 ,  C07C59/245 ,  C07C55/10

CPC分类号： C07C215/54 ,  C07C55/10 ,  C07C59/245

摘要： The invention relates to substantially pure Desfesoterodine salts, Desfesoterodine salts, solid state forms thereof and pharmaceutical compositions comprising one or more of the Desfesoterodine salts and/or solid state forms thereof.

摘要翻译： 本发明涉及基本上纯的Desfesoterodine盐，Desfesoterodine盐，其固态形式和包含一种或多种Desfesoterodine盐和/或固态形式的药物组合物。

公开(公告)号：US20140228380A1

公开(公告)日：2014-08-14

申请号：US13957861

申请日：2013-08-02

申请人： University of Medicine and Dentistry New Jersey Medical School ,  Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine

发明人： Sandhya Kortagere ,  Eldo V. Kuzhikandahil

IPC分类号： C07D471/04 ,  C07D235/16 ,  C07C211/29 ,  C07D209/14 ,  C07C215/08 ,  C07C215/54

CPC分类号： A61K31/137 ,  A61K31/198 ,  A61K31/4045 ,  A61K31/4184 ,  A61K31/428 ,  A61K31/473 ,  A61K31/48 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5513 ,  A61K45/06 ,  C07C211/29 ,  C07C215/08 ,  C07C215/54 ,  C07C217/62 ,  C07D209/14 ,  C07D235/16 ,  C07D471/04 ,  A61K2300/00

摘要： The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.

公开(公告)号：US20130022654A1

公开(公告)日：2013-01-24

申请号：US13638239

申请日：2011-02-07

申请人： Ashish Ashokrao Deshmukh ,  Pravin Meghrajji Bhutada ,  Sajeev Chandran ,  Shirishkumar Kulkarni

发明人： Ashish Ashokrao Deshmukh ,  Pravin Meghrajji Bhutada ,  Sajeev Chandran ,  Shirishkumar Kulkarni

IPC分类号： A61K31/137 ,  A61K9/00 ,  A61P25/00 ,  C07C215/54

CPC分类号： A61K9/209 ,  A61K9/0004 ,  A61K9/0065 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/5026 ,  A61K9/5042 ,  A61K31/137 ,  A61K45/06 ,  A61K2300/00

摘要： A once daily controlled release pharmaceutical compositions comprising tapentadol, wherein preferably the mean Tmax of tapentadol is reached after 10 hours of administration of the composition. The composition comprises tapentadol, such that it maintains serum concentration of tapentadol of at least about 20 ng/ml for at least about 17 hours after oral administration of the composition. According to one embodiment the controlled release pharmaceutical composition comprises tapentadol, which is gastroretentive.

摘要翻译： 包含他喷他多的每日一次的控释药物组合物，其中优选在施用组合物10小时后达到他喷他多的平均T max。 组合物包含他喷他多，使得其在口服给药组合物后至少约17小时维持至少约20ng / ml的他喷他多的血清浓度。 根据一个实施方案，控释药物组合物包含胃酸滞留的他喷他多。

公开(公告)号：US08067594B2

公开(公告)日：2011-11-29

申请号：US12302228

申请日：2007-05-21

申请人： Jens Bertil Ahman ,  Barry Richard Dillon ,  Alan John Pettman

发明人： Jens Bertil Ahman ,  Barry Richard Dillon ,  Alan John Pettman

IPC分类号： C07D311/20 ,  C07D311/58 ,  C07C215/54 ,  C07C213/02 ,  C07C219/28

CPC分类号： C07D311/20 ,  C07C45/69 ,  C07C213/02 ,  C07D311/58 ,  C07C47/27 ,  C07C215/54 ,  C07C219/28

摘要： The invention provides a process for producing a compound of formula (I), wherein Y is selected from the group consisting of CH3, CH2OH, CH2CH2OH, CH2Br and Br; comprising the steps of: (i) reacting a compound of formula (II), wherein OX represents hydroxy or O−M+, in which M+ is a cation selected from Li+, Na+ and K+, and Y is as defined above; with trans-cinnamaldehyde (III), in the presence of a secondary amine compound; then (ii) treating the product of the preceding step with acid to afford the compound of formula (I). The above process may also be used in the production of tolterodine and fesoterodine, which are useful in the treatment of overactive bladder.

摘要翻译： 本发明提供了制备式（I）化合物的方法，其中Y选自CH 3，CH 2 OH，CH 2 CH 2 OH，CH 2 Br和Br; 包括以下步骤：（i）使式（II）化合物其中OX表示羟基或O-M +，其中M +是选自Li +，Na +和K +的阳离子，Y如上定义; 在仲胺化合物的存在下反式肉桂醛（III）; 然后（ii）用酸处理前述步骤的产物，得到式（I）化合物。 上述方法也可用于生产托特罗定和非索罗定，其可用于治疗膀胱过动症。

公开(公告)号：US20110281952A1

公开(公告)日：2011-11-17

申请号：US12944560

申请日：2010-11-11

申请人： Anthony W. Czarnik

发明人： Anthony W. Czarnik

IPC分类号： C07C215/54 ,  A61P13/00 ,  A61K31/135

CPC分类号： C07B59/001

摘要： The present application describes deuterium-enriched tolterodine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

摘要翻译： 本申请描述了富含氘的托特罗定，其药学上可接受的盐形式，以及使用它们的治疗方法。