公开(公告)号：US07919490B2

公开(公告)日：2011-04-05

申请号：US11867562

申请日：2007-10-04

申请人： Irina Neagu ,  David Diller ,  Celia Kingsbury ,  Adolph C. Bohnstedt ,  Michael J. Ohlmeyer ,  Vidyadhar Paradkar ,  Nasrin Ansari

发明人： Irina Neagu ,  David Diller ,  Celia Kingsbury ,  Adolph C. Bohnstedt ,  Michael J. Ohlmeyer ,  Vidyadhar Paradkar ,  Nasrin Ansari

IPC分类号： C07D473/32 ,  C07D473/18 ,  A61K31/52 ,  A61K31/522 ,  A61P37/06 ,  A61P11/06 ,  A61P35/02 ,  C07D239/48 ,  C07D239/50 ,  C07D405/12 ,  C07D405/14

CPC分类号： C07D473/32 ,  C07D473/16 ,  C07D473/18 ,  C07D473/40

摘要： The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II shown below, in which Q is selected from the group consisting of CX and nitrogen; and A is chosen from the group consisting of H, (C1-C6) alkyl, heteroaryl, and aryl:

摘要翻译： 本发明提供了可用于预防和治疗自身免疫性疾病，炎性疾病，肥大细胞介导的疾病和移植排斥的新型嘌呤酮和嘌呤。 该化合物具有下列通式I和II，其中Q选自CX和氮; 并且A选自H，（C 1 -C 6）烷基，杂芳基和芳基：

公开(公告)号：US07902187B2

公开(公告)日：2011-03-08

申请号：US12196516

申请日：2008-08-22

申请人： Irina Neagu ,  David Diller ,  Celia Kingsbury ,  Adolph C. Bohnstedt ,  Michael J. Ohlmeyer ,  Vidyadhar Paradkar ,  Nasrin Ansari

发明人： Irina Neagu ,  David Diller ,  Celia Kingsbury ,  Adolph C. Bohnstedt ,  Michael J. Ohlmeyer ,  Vidyadhar Paradkar ,  Nasrin Ansari

IPC分类号： C07D473/32 ,  C07D473/18 ,  A61K31/52 ,  A61K31/522 ,  A61P37/06 ,  A61P11/06 ,  A61P35/02 ,  C07D239/48 ,  C07D239/50 ,  C07D405/12 ,  C07D405/14

CPC分类号： C07D473/16 ,  C07D473/18 ,  C07D473/32 ,  C07D473/40

摘要： The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II shown below, in which Q is selected from the group consisting of CX and nitrogen; and A is chosen from the group consisting of H, (C1-C6) alkyl, heteroaryl, and aryl:

公开(公告)号：US20080214580A1

公开(公告)日：2008-09-04

申请号：US11867562

申请日：2007-10-04

申请人： Irina Neagu ,  David Diller ,  Celia Kingsbury ,  Adolph C. Bohnstedt ,  Michael J. Ohlmeyer ,  Vidyadhar Paradkar ,  Nasrin Ansari

发明人： Irina Neagu ,  David Diller ,  Celia Kingsbury ,  Adolph C. Bohnstedt ,  Michael J. Ohlmeyer ,  Vidyadhar Paradkar ,  Nasrin Ansari

IPC分类号： A61K31/522 ,  C07D473/16

CPC分类号： C07D473/32 ,  C07D473/16 ,  C07D473/18 ,  C07D473/40

摘要： The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II:

摘要翻译： 本发明提供了可用于预防和治疗自身免疫性疾病，炎性疾病，肥大细胞介导的疾病和移植排斥的新型嘌呤酮和嘌呤。 该化合物具有通式I和II：

公开(公告)号：US20090069289A1

公开(公告)日：2009-03-12

申请号：US12196516

申请日：2008-08-22

申请人： Irina Neagu ,  David Diller ,  Celia Kingsbury ,  Adolph C. Bohnstedt ,  Michael J. Ohlmeyer ,  Vidyadhar Paradkar ,  Ansari Nasrin

发明人： Irina Neagu ,  David Diller ,  Celia Kingsbury ,  Adolph C. Bohnstedt ,  Michael J. Ohlmeyer ,  Vidyadhar Paradkar ,  Ansari Nasrin

IPC分类号： C07D473/28 ,  A61K31/522 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/551

CPC分类号： C07D473/16 ,  C07D473/18 ,  C07D473/32 ,  C07D473/40

摘要： The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II:

摘要翻译： 本发明提供了可用于预防和治疗自身免疫性疾病，炎性疾病，肥大细胞介导的疾病和移植排斥的新型嘌呤酮和嘌呤。 该化合物具有通式I和II：

公开(公告)号：US20110218189A1

公开(公告)日：2011-09-08

申请号：US12936604

申请日：2009-04-08

申请人： Andrew Laird Roughton ,  Koc-kan Ho ,  Michael Ohlmeyer ,  David Diller ,  Irina Neagu ,  Celia Kingsbury ,  Jui-Hsiang Chan ,  Johannes Petrus, Mmaria Lommerse ,  Neeltje Miranda Teerhuis ,  Jacobus Comelis Henricus Maria Wijkmans ,  Ralf Plate

发明人： Andrew Laird Roughton ,  Koc-kan Ho ,  Michael Ohlmeyer ,  David Diller ,  Irina Neagu ,  Celia Kingsbury ,  Jui-Hsiang Chan ,  Johannes Petrus, Mmaria Lommerse ,  Neeltje Miranda Teerhuis ,  Jacobus Comelis Henricus Maria Wijkmans ,  Ralf Plate

IPC分类号： A61K31/55 ,  C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61P29/00 ,  A61P43/00

CPC分类号： C07D487/04

摘要： The present invention relates to a pyrrolo[2,3-d]pyrimidin-2-yl-amine derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said pyrrolo[2,3-d]pyrimidine-2-ylamine derivatives and to their use in therapy, for instance in the treatment of PKCθ mediated disorders.

摘要翻译： 本发明涉及式（I）的吡咯并[2,3-d]嘧啶-2-基 - 胺衍生物，其中变量如说明书中所定义，或其药学上可接受的盐或溶剂合物。 本发明还涉及包含一种或多种所述吡咯并[2,3-d]嘧啶-2-基胺衍生物的药物组合物及其在治疗中的用途，例如用于治疗PKC和血栓; 介导的疾病。

公开(公告)号：US20110046131A1

公开(公告)日：2011-02-24

申请号：US12445862

申请日：2007-10-19

申请人： Irina Neagu ,  Andrew Laird Roughton ,  Koc-Kan Ho ,  David Diller ,  Jui-Hsiang Chan ,  Michael Ohlmeyer ,  Celia Kingsbury ,  Johannes Petrus Maria Lommerse ,  Neeltje Miranda ,  Jacobus Cornelis Henricus Maria Wijkmans

发明人： Irina Neagu ,  Andrew Laird Roughton ,  Koc-Kan Ho ,  David Diller ,  Jui-Hsiang Chan ,  Michael Ohlmeyer ,  Celia Kingsbury ,  Johannes Petrus Maria Lommerse ,  Neeltje Miranda ,  Jacobus Cornelis Henricus Maria Wijkmans

IPC分类号： A61K31/5377 ,  C07D473/32 ,  A61K31/52 ,  A61P11/06 ,  A61P29/00 ,  A61P37/06 ,  A61P25/00 ,  A61P19/02 ,  A61P35/00 ,  A61P3/10

CPC分类号： C07D473/32

摘要： A chemical genus of purines, which are useful as PKCθ inhibitors, is disclosed. The genus is represented by the formula (I); A representative example is: (II)

摘要翻译： 嘌呤的化学属，可用作PKC和原子; 抑制剂。 该属由式（I）表示; 一个代表性的例子是：（二）

公开(公告)号：US20120015958A1

公开(公告)日：2012-01-19

申请号：US13060730

申请日：2009-08-26

申请人： Andrew John Cooke ,  David Jonathan Bennett ,  Andrew Stanley Edwards ,  Andrew Laird Roughton ,  Irina Neagu ,  Jui-Hsiang Chan ,  Koc Kan Ho ,  Nasrin Ansari ,  Michelle Lee Morris ,  Yajing Rong ,  Michael Ohlmeyer

发明人： Andrew John Cooke ,  David Jonathan Bennett ,  Andrew Stanley Edwards ,  Andrew Laird Roughton ,  Irina Neagu ,  Jui-Hsiang Chan ,  Koc Kan Ho ,  Nasrin Ansari ,  Michelle Lee Morris ,  Yajing Rong ,  Michael Ohlmeyer

IPC分类号： A61K31/496 ,  C07D417/06 ,  C07D405/06 ,  C07D409/06 ,  C07D403/06 ,  A61P3/04 ,  A61P9/10 ,  A61P7/00 ,  A61P1/00 ,  A61P3/06 ,  A61P3/10 ,  C07D413/06 ,  C07D401/06

CPC分类号： C07D263/34 ,  C07D213/56 ,  C07D277/56 ,  C07D307/68 ,  C07D333/38

摘要： The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.

摘要翻译： 本发明涉及具有通式I的1-（4-脲基苯甲酰基）哌嗪衍生物（我们提请您注意，该电子版本没有提供式I，如在本文摘要中提供的）。其中R1是 （C 1-8）烷基，（C 3-8）环烷基或（C 3-8）环烷基（C 1-3）烷基，其各自可被羟基，氰基或卤素取代; R2表示1或2个任选的卤素; R3是（C 1-6）烷基，（C 3-6）环烷基或（C 3-6）环烷基（C 1-3）烷基，其各自可被一个或多个卤素取代; A表示包含1-3个选自N，O和S的杂原子的杂芳基环系统，当X是C时，该环系统是5-或6-元，当X是N时，该环系是5元; n为1或2; 或其药学上可接受的盐; 涉及包含其的药物组合物，以及这些1-（4-脲基苯甲酰基）哌嗪衍生物在制备用于治疗或预防动脉粥样硬化和与胆汁酸和胆汁酸运输和代谢相关的相关疾病的药物中的用途。

公开(公告)号：US08211927B2

公开(公告)日：2012-07-03

申请号：US12671113

申请日：2008-07-31

申请人： Andrew Laird Roughton ,  Koc-Kan Ho ,  Michael Ohlmeyer ,  Irina Neagu ,  Steven G. Kultgen ,  Nasrin Ansari ,  Yajing Rong ,  Paul David Ratcliffe ,  Ronald Palin

发明人： Andrew Laird Roughton ,  Koc-Kan Ho ,  Michael Ohlmeyer ,  Irina Neagu ,  Steven G. Kultgen ,  Nasrin Ansari ,  Yajing Rong ,  Paul David Ratcliffe ,  Ronald Palin

IPC分类号： A61K31/42 ,  C07D261/18

CPC分类号： C07D413/12 ,  C07D261/18

摘要： The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.

摘要翻译： 本发明涉及具有通式（I）的异恶唑-3-甲酰胺衍生物或其药学上可接受的盐，涉及含有该异构体的异恶唑-3-甲酰胺衍生物用于治疗的药物组合物 的TRPV1介导的疾病，例如急性和慢性疼痛障碍，急性和慢性神经性疼痛，急性和慢性炎症性疼痛，呼吸系统疾病和下尿路疾病。

公开(公告)号：US20090264416A1

公开(公告)日：2009-10-22

申请号：US12194146

申请日：2008-08-19

申请人： Koc-Kan Ho ,  Andrew Laird Roughton ,  Irina Neagu ,  Jui-Hsiang Chan ,  Nasrin Ansari ,  Michelle Lee Morris ,  Yajing Rong ,  Michael Ohlmeyer ,  Andrew John Cooke ,  Andrew Stanley Edwards ,  David Jonathan Bennett

发明人： Koc-Kan Ho ,  Andrew Laird Roughton ,  Irina Neagu ,  Jui-Hsiang Chan ,  Nasrin Ansari ,  Michelle Lee Morris ,  Yajing Rong ,  Michael Ohlmeyer ,  Andrew John Cooke ,  Andrew Stanley Edwards ,  David Jonathan Bennett

IPC分类号： A61K31/551 ,  C07D241/04 ,  C07D413/12 ,  A61K31/496 ,  C07D413/14 ,  C07D401/12 ,  A61K31/5377 ,  A61K31/535 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/497 ,  C07D243/08

CPC分类号： C07D295/192 ,  C07D241/04 ,  C07D243/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to N-benzyl,N′-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N′-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.

摘要翻译： 本发明涉及具有通式I的N-苄基，N'-芳基羰基哌嗪衍生物，其包含其的药物组合物，以及这些N-苄基，N'-芳基羰基哌嗪衍生物在制备用于治疗 或预防与胆固醇和胆汁酸运输和代谢相关的动脉粥样硬化和相关疾病。

公开(公告)号：US08759352B2

公开(公告)日：2014-06-24

申请号：US13060730

申请日：2009-08-26

申请人： Andrew John Cooke ,  David Jonathan Bennett ,  Andrew Stanley Edwards ,  Andrew Laird Roughton ,  Irina Neagu ,  Jui-Hsiang Chan ,  Koc-Kan Ho ,  Nasrin Ansari ,  Michelle Lee Morris ,  Yajing Rong ,  Michael Ohlmeyer

发明人： Andrew John Cooke ,  David Jonathan Bennett ,  Andrew Stanley Edwards ,  Andrew Laird Roughton ,  Irina Neagu ,  Jui-Hsiang Chan ,  Koc-Kan Ho ,  Nasrin Ansari ,  Michelle Lee Morris ,  Yajing Rong ,  Michael Ohlmeyer

IPC分类号： A61K31/496 ,  C07D213/56 ,  C07D263/34 ,  C07D277/56 ,  C07D307/68

CPC分类号： C07D263/34 ,  C07D213/56 ,  C07D277/56 ,  C07D307/68 ,  C07D333/38

摘要： The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.

摘要翻译： 本发明涉及具有通式I的1-（4-脲基苯甲酰基）哌嗪衍生物（我们提请您注意，该电子版本没有提供式I，如在本文摘要中提供的）。其中R1是 （C 1-8）烷基，（C 3-8）环烷基或（C 3-8）环烷基（C 1-3）烷基，其各自可被羟基，氰基或卤素取代; R2表示1或2个任选的卤素; R3是（C 1-6）烷基，（C 3-6）环烷基或（C 3-6）环烷基（C 1-3）烷基，其各自可被一个或多个卤素取代; A表示包含1-3个选自N，O和S的杂原子的杂芳基环系统，当X是C时，该环系统是5-或6-元，当X是N时，该环系是5元; n为1或2; 或其药学上可接受的盐; 涉及包含其的药物组合物，以及这些1-（4-脲基苯甲酰基）哌嗪衍生物在制备用于治疗或预防动脉粥样硬化和与胆汁酸和胆汁酸运输和代谢相关的相关疾病的药物中的用途。