公开(公告)号：US09492457B2

公开(公告)日：2016-11-15

申请号：US14626978

申请日：2015-02-20

申请人： Concert Pharmaceuticals, Inc.

发明人： Roger D. Tung ,  Julie F. Liu ,  Scott L. Harbeson

IPC分类号： A61K31/555 ,  C07D473/06 ,  A61K31/522

CPC分类号： A61K31/522 ,  C07D473/06

摘要： This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.

公开(公告)号：US09422295B2

公开(公告)日：2016-08-23

申请号：US14418831

申请日：2013-07-30

申请人： Concert Pharmaceuticals, Inc.

发明人： Roger D. Tung ,  Adam J. Morgan

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04 ,  C07B59/00

CPC分类号： C07D487/04 ,  C07B59/002 ,  C07B2200/05

摘要： The present invention in one embodiment provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula (I) are as defined in the specification.

摘要翻译： 本发明在一个实施方案中提供式（I）的化合物; 或其药学上可接受的盐，其中式（I）所示的变量如说明书中所定义。

公开(公告)号：US09340512B2

公开(公告)日：2016-05-17

申请号：US14726758

申请日：2015-06-01

申请人： Concert Pharmaceuticals, Inc.

发明人： Philip B. Graham ,  I. Robert Silverman

IPC分类号： A61K31/485 ,  C07D221/28 ,  A61K45/06

CPC分类号： A61K31/485 ,  A61K31/195 ,  A61K31/4709 ,  A61K45/06 ,  C07D221/28

摘要： This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ1 receptor agonist that also has NMDA antagonist activity.

摘要翻译： 本发明涉及新的吗啡喃化合物及其药学上可接受的盐。 本发明还提供包含本发明化合物的组合物以及这些组合物在治疗通过施用也具有NMDA拮抗剂活性的1受体激动剂有益治疗的疾病和病症的方法中的用途。

公开(公告)号：US20160068519A1

公开(公告)日：2016-03-10

申请号：US14853900

申请日：2015-09-14

申请人： Concert Pharmaceuticals, Inc.

发明人： Scott L. Harbeson

IPC分类号： C07D405/10

CPC分类号： C07D405/10 ,  C07B59/002 ,  C07B2200/05 ,  C07D403/06

摘要： This invention relates to novel inhibitors of UDP-glucose: N-acyl-sphingosine glucosyltransferase and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of UDP-glucose: N-acyl-sphingosine glucosyltransferase.

摘要翻译： 本发明涉及新型UDP-葡萄糖抑制剂：N-酰基鞘氨醇葡糖基转移酶及其药学上可接受的盐。 本发明还提供了包含本发明化合物的组合物和这些组合物在治疗通过施用UDP-葡萄糖：N-酰基鞘氨醇葡糖基转移酶的抑制剂有益治疗的疾病和病症的方法中的用途。

公开(公告)号：US20160031801A1

公开(公告)日：2016-02-04

申请号：US14817876

申请日：2015-08-04

申请人： Concert Pharmaceuticals, Inc.

发明人： Craig E. Masse

IPC分类号： C07C233/18

CPC分类号： C07C233/18 ,  C07B59/001 ,  C07C235/34 ,  C07C237/06

摘要： This invention relates to novel 2-amino-3-hydroxypropanoic acid derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an NMDA glycine-site antagonist.

摘要翻译： 本发明涉及新的2-氨基-3-羟基丙酸衍生物及其药学上可接受的盐。 本发明还提供了包含本发明化合物的组合物和这些组合物在治疗通过施用NMDA甘氨酸位点拮抗剂有益治疗的疾病和病症的方法中的用途。

公开(公告)号：US20160009732A1

公开(公告)日：2016-01-14

申请号：US14772972

申请日：2014-03-12

申请人： CONCERT PHARMACEUTICALS, INC.

发明人： Scott L. Harbeson

IPC分类号： C07D498/08

CPC分类号： C07D498/08 ,  A61K31/519

摘要： The present invention in one embodiment provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification.

摘要翻译： 本发明在一个实施方案中提供式I化合物或其药学上可接受的盐，其中式I所示的变量如说明书中所定义。

公开(公告)号：US20150366853A1

公开(公告)日：2015-12-24

申请号：US14840952

申请日：2015-08-31

申请人： Concert Pharmaceuticals, Inc.

发明人： Bhaumik A. Pandya ,  Craig E. Masse ,  Ian Robert Silverman ,  Roger D. Tung

IPC分类号： A61K31/4545 ,  A61K31/44 ,  A61K31/517

CPC分类号： A61K31/4545 ,  A61K31/44 ,  A61K31/517 ,  A61K45/06 ,  C07D401/14 ,  A61K2300/00

摘要： This invention relates to novel pyrazole-substituted amino-heteroaryl compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of anaplastic lymphoma kinase (ALK).

摘要翻译： 本发明涉及式I的新型吡唑取代的氨基 - 杂芳基化合物及其药学上可接受的盐。 本发明还提供了包含本发明化合物的组合物和这种组合物在治疗通过施用间变性淋巴瘤激酶（ALK）的抑制剂有益治疗的疾病和病症的方法中的用途。

公开(公告)号：US09206179B2

公开(公告)日：2015-12-08

申请号：US14518254

申请日：2014-10-20

申请人： Concert Pharmaceuticals, Inc.

发明人： Julie F. Liu ,  Scott L. Harbeson ,  Roger D. Tung

IPC分类号： C07D241/38 ,  C07D471/04 ,  C07B59/00 ,  A61K31/4184 ,  A61K31/4985

CPC分类号： C07D471/04 ,  A61K31/4184 ,  A61K31/4985 ,  C07B59/002 ,  Y02A50/411 ,  Y02A50/423

摘要： This invention in one embodiment is directed to a compound of Formula Ia; where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Z1 is hydrogen or fluorine; Z2 is hydrogen, deuterium, or fluorine; Z3 is deuterium; Z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both Z1 and Z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.

摘要翻译： 本发明在一个实施方案中涉及式Ia化合物; 其中指定（R）表示指定的碳具有（R）立体化学; 并且其中Z1是氢或氟; Z2是氢，氘或氟; Z3是氘; Z4是氟; m为0〜10的整数; n为0〜2的整数; 条件是：m + n的和不超过10; 并且当Z1和Z2均为氢时，m + n的和大于0，以及其药学上可接受的盐。 本发明还提供包含一种或多种本发明化合物和载体的组合物，以及所述化合物和组合物在治疗通过施用抗栓剂如吡喹酮有益治疗的疾病和病症的方法中的用途。

公开(公告)号：US09085788B2

公开(公告)日：2015-07-21

申请号：US13820003

申请日：2011-09-01

申请人： Ramanaiah C. Kanamarlapudi ,  Steven A. Weissman ,  Emerich Eisenreich ,  Xuejun Liu

发明人： Ramanaiah C. Kanamarlapudi ,  Steven A. Weissman ,  Emerich Eisenreich ,  Xuejun Liu

IPC分类号： C12P17/18 ,  C07B59/00 ,  C07D473/04

CPC分类号： C12P17/182 ,  C07B59/002 ,  C07D473/04 ,  C12Y101/01184

摘要： The present invention provides a convenient and efficient process for the preparation of enantiomerically enriched, deuterated secondary alcohols without reducing deuterium incorporation.

摘要翻译： 本发明提供了用于制备对映体富集的氘化仲醇而不减少氘掺入的方便和有效的方法。

公开(公告)号：US09072711B2

公开(公告)日：2015-07-07

申请号：US14141694

申请日：2013-12-27

申请人： Concert Pharmaceuticals, Inc.

发明人： Roger Tung

IPC分类号： A61K31/4748 ,  A61K31/195 ,  C07B59/00 ,  A61K31/4709 ,  A61K31/485 ,  C07D221/28 ,  C07D471/08 ,  A61K31/49

CPC分类号： A61K31/195 ,  A61K31/4709 ,  A61K31/485 ,  A61K31/49 ,  C07B59/002 ,  C07D221/28 ,  C07D471/08

摘要： This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ1 receptor agonist that also has NMDA antagonist activity.

摘要翻译： 本公开涉及新的吗啡喃化合物及其衍生物，其药学上可接受的盐，溶剂合物和水合物。 本公开还提供了包含本公开的化合物的组合物以及这些组合物在治疗通过施用也具有NMDA拮抗剂活性的1受体激动剂有益治疗的疾病和病症的方法中的用途。