公开(公告)号：US20050277631A1

公开(公告)日：2005-12-15

申请号：US11195134

申请日：2005-08-01

Applicant: Elizabeth Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark Norman ,  Hui-Ling Wang ,  Christopher Fotsch ,  Ning Chen ,  Partha Chakrabarti ,  Celia Dominguez ,  James Falsey ,  Christopher Hulme ,  Jodie Katon ,  Thomas Nixey ,  Vassil Ognyanov ,  Liping Pettus ,  Robert Rzasa

Inventor： Elizabeth Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark Norman ,  Hui-Ling Wang ,  Christopher Fotsch ,  Ning Chen ,  Partha Chakrabarti ,  Celia Dominguez ,  James Falsey ,  Christopher Hulme ,  Jodie Katon ,  Thomas Nixey ,  Vassil Ognyanov ,  Liping Pettus ,  Robert Rzasa

IPC: A61P29/00 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/64 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/22 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/40 ,  C07D231/56 ,  C07D233/38 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  A61K31/549 ,  A61K31/501 ,  C07D417/02 ,  C07D43/02

CPC classification number: C07D231/40 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/56 ,  C07D233/38 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

公开(公告)号：US06552042B2

公开(公告)日：2003-04-22

申请号：US09772303

申请日：2001-01-29

Applicant: Qi Han ,  Celia Dominguez ,  Eugene C. Amparo ,  Jeongsook M. Park ,  Mimi L. Quan ,  Karen A. Rossi

Inventor： Qi Han ,  Celia Dominguez ,  Eugene C. Amparo ,  Jeongsook M. Park ,  Mimi L. Quan ,  Karen A. Rossi

IPC: C07D23526

CPC classification number: C07D263/58 ,  C07D209/34 ,  C07D235/26 ,  C07D241/44

Abstract: The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3 may be N or C and J, Ja, and Jb combine to form a substituted carbocycle or heterocycle.

Abstract translation: 本申请描述了式I的因子Xa或其药学上可接受的盐形式的抑制剂，其中W，W 1，W 2和W 3可以是N或C并且J，J a和J b结合形成取代的碳环或杂环。

公开(公告)号：US20170292150A1

公开(公告)日：2017-10-12

申请号：US15507217

申请日：2015-08-28

Applicant: Celia DOMINGUEZ ,  John WITYAK ,  Jonathan BARD ,  Christopher John BROWN ,  Michael Edward PRIME ,  Derek Alexander WEDDELL ,  Daryl Simon WALTER ,  Paul Richard GILES ,  Ian James WIGGINTON ,  George Malcolm TAYLOR ,  Sébastien René Gabriel GALAN ,  Peter David JOHNSON ,  Thomas Martin KRÜLLE ,  Inaki MORAO ,  Daniel CLARK-FREW ,  Sabine SCHAERTL ,  Frank HERRMANN ,  Steffen Kaspar GRIMM ,  Jan Dirk KAHMANN ,  Christoph SCHEICH ,  HDI Management, Inc.

Inventor： Celia Dominguez ,  John Wityak ,  Jonathan Bard ,  Christopher John Brown ,  Michael Edward Prime ,  Derek Alexander Weddell ,  Daryl Simon Walter ,  Paul Richard Giles ,  Ian James Wigginton ,  Malcolm George Taylor ,  Sébastien René Gabriel Galan ,  Peter David Johnson ,  Thomas Martin Krülle ,  Inaki Morao ,  Daniel Clark-Frew

IPC: C12Q1/68 ,  C07D401/04 ,  C07D253/08 ,  C07D473/00

Abstract: Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use.

公开(公告)号：US09428464B2

公开(公告)日：2016-08-30

申请号：US14241699

申请日：2012-08-28

Applicant: Stephen Martin Courtney ,  Michael Prime ,  William Mitchell ,  Christopher John Brown ,  Paula C. De Aguiar Pena ,  Peter Johnson ,  Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Ignacio Muñoz-Sanjuan

Inventor： Stephen Martin Courtney ,  Michael Prime ,  William Mitchell ,  Christopher John Brown ,  Paula C. De Aguiar Pena ,  Peter Johnson ,  Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Ignacio Muñoz-Sanjuan

IPC: C07D239/52 ,  A61K31/506 ,  C07D239/28 ,  C07D403/12 ,  C07D403/06 ,  C07D405/12 ,  C07D413/12 ,  C07D491/048 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D239/28 ,  A61K31/506 ,  C07D239/42 ,  C07D239/52 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  Y02A50/401 ,  Y02A50/411 ,  Y02A50/465

Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Abstract translation: 本文提供了某些化学实体。 还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。 描述了治疗患有对KMO活性的抑制作用的某些疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症的体征或症状的化学实​​体。 这些疾病包括神经变性疾病如亨廷顿氏病。 还描述了治疗方法，包括给予至少一种作为单一活性剂的化学实体或与一种或多种其它治疗剂组合施用至少一种化学实体。 还提供了用于筛选能够抑制KMO活性的化合物的方法。

公开(公告)号：US09096565B2

公开(公告)日：2015-08-04

申请号：US12100200

申请日：2008-04-09

Applicant: Pierre Tessier ,  Silvana Leit ,  David Smil ,  Robert Deziel ,  Alain Ajamian ,  Yves Andre Chantigny ,  Celia Dominguez

Inventor： Pierre Tessier ,  Silvana Leit ,  David Smil ,  Robert Deziel ,  Alain Ajamian ,  Yves Andre Chantigny ,  Celia Dominguez

IPC: C07D295/088 ,  A61K31/5375 ,  C07D307/79 ,  C07C259/06 ,  C07C275/42 ,  C07C311/08 ,  C07C311/21 ,  C07C323/52 ,  C07D205/04 ,  C07D207/263 ,  C07D207/337 ,  C07D209/08 ,  C07D209/44 ,  C07D211/34 ,  C07D211/46 ,  C07D211/52 ,  C07D211/64 ,  C07D211/76 ,  C07D213/56 ,  C07D213/64 ,  C07D213/70 ,  C07D213/74 ,  C07D215/26 ,  C07D219/04 ,  C07D231/14 ,  C07D233/84 ,  C07D235/16 ,  C07D235/28 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D249/06 ,  C07D267/20 ,  C07D277/36 ,  C07D277/74 ,  C07D285/12 ,  C07D295/155 ,  C07D295/192 ,  C07D295/205 ,  C07D295/26 ,  C07D311/84 ,  C07D317/50 ,  C07D333/24 ,  C07D401/04 ,  C07D401/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D471/04 ,  C07D491/08 ,  C07D491/10 ,  C07D513/04

CPC classification number: C07D307/79 ,  C07C259/06 ,  C07C275/42 ,  C07C311/08 ,  C07C311/21 ,  C07C323/52 ,  C07D205/04 ,  C07D207/263 ,  C07D207/337 ,  C07D209/08 ,  C07D209/44 ,  C07D211/34 ,  C07D211/46 ,  C07D211/52 ,  C07D211/64 ,  C07D211/76 ,  C07D213/56 ,  C07D213/64 ,  C07D213/70 ,  C07D213/74 ,  C07D215/26 ,  C07D219/04 ,  C07D231/14 ,  C07D233/84 ,  C07D235/16 ,  C07D235/28 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D249/06 ,  C07D267/20 ,  C07D277/36 ,  C07D277/74 ,  C07D285/12 ,  C07D295/088 ,  C07D295/155 ,  C07D295/192 ,  C07D295/205 ,  C07D295/26 ,  C07D311/84 ,  C07D317/50 ,  C07D333/24 ,  C07D401/04 ,  C07D401/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D471/04 ,  C07D491/08 ,  C07D491/10 ,  C07D513/04

Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.

Abstract translation: 本发明涉及抑制组蛋白脱乙酰酶的化合物。 更具体地说，本发明提供式（I）的化合物及其N-氧化物，水合物，溶剂化物，其药学上可接受的盐，前体药物和复合物，以及其外消旋和可比混合物，非对映异构体和对映异构体，其中基团L，M，X 和Y如本文所定义。

公开(公告)号：US08889716B2

公开(公告)日：2014-11-18

申请号：US13466018

申请日：2012-05-07

Applicant: Michael Prime ,  Stephen Martin Courtney ,  Richard Marston ,  Celia Dominguez ,  Douglas MacDonald ,  John Wityak

Inventor： Michael Prime ,  Stephen Martin Courtney ,  Richard Marston ,  Celia Dominguez ,  Douglas MacDonald ,  John Wityak

IPC: A61K31/445 ,  C07D211/96 ,  C07D409/12 ,  C07D205/04 ,  C07D405/12 ,  C07D405/14 ,  C07D207/48 ,  C07D401/14 ,  C07D401/12

CPC classification number: C07D205/04 ,  C07D207/48 ,  C07D211/96 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12

Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.

Abstract translation: 本文提供了某些化合物和药学上可接受的盐。 还提供了包含至少一种化合物或其药学上可接受的盐的药物组合物和一种或多种药学上可接受的载体。 描述了治疗患有某种疾病状态的患者对抑制转谷氨酰胺酶TG2活性有反应的方法。 这些疾病状态包括神经变性疾病如亨廷顿病。 还描述了治疗方法，包括给予至少一种化合物或其药学上可接受的盐作为单一活性剂，或者与一种或多种其它治疗剂组合施用至少一种化合物或其药学上可接受的盐。

公开(公告)号：US20140329816A1

公开(公告)日：2014-11-06

申请号：US14235253

申请日：2012-07-26

Applicant: Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Stephen Martin Courtney ,  Michael Prime ,  William Mitchell ,  Christopher John Brown ,  Paula C. De Aguiar Pena ,  Peter Johnson

Inventor： Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Stephen Martin Courtney ,  Michael Prime ,  William Mitchell ,  Christopher John Brown ,  Paula C. De Aguiar Pena ,  Peter Johnson

IPC: C07D417/04 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D239/28 ,  C07D403/04

CPC classification number: A61K31/506 ,  A61K31/505 ,  A61K31/513 ,  A61K31/5377 ,  C07D239/26 ,  C07D239/28 ,  C07D239/42 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D491/044 ,  C07D491/048 ,  C07D491/052

Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Abstract translation: 本文提供了某些化学实体。 还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。 描述了治疗患有对KMO活性的抑制作用的某些疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症的体征或症状的化学实​​体。 这些疾病包括神经变性疾病如亨廷顿氏病。 还描述了治疗方法，包括给予至少一种作为单一活性剂的化学实体或与一种或多种其它治疗剂组合施用至少一种化学实体。 还提供了用于筛选能够抑制KMO活性的化合物的方法。

公开(公告)号：US08685983B2

公开(公告)日：2014-04-01

申请号：US13308310

申请日：2011-11-30

Applicant: Tae-Seong Kim ,  David Bauer ,  Steven Bellon ,  Alessadro Boezio ,  Shon Booker ,  Deborah Choquette ,  Derin C. D'Amico ,  Noel D'Angelo ,  Celia Dominguez ,  Ingrid M. Fellows ,  Julie Germain ,  Russell Graceffa ,  Jean-Christophe Harmange ,  Satoko Hirai ,  Daniel La ,  Matthew Lee ,  Longbin Liu ,  Mark H. Norman ,  Michele Potashman ,  Philip Roveto ,  Aaron C. Siegmund ,  Ning Xi ,  Kevin Yang

Inventor： Tae-Seong Kim ,  David Bauer ,  Steven Bellon ,  Alessadro Boezio ,  Shon Booker ,  Deborah Choquette ,  Derin C. D'Amico ,  Noel D'Angelo ,  Celia Dominguez ,  Ingrid M. Fellows ,  Julie Germain ,  Russell Graceffa ,  Jean-Christophe Harmange ,  Satoko Hirai ,  Daniel La ,  Matthew Lee ,  Longbin Liu ,  Mark H. Norman ,  Michele Potashman ,  Philip Roveto ,  Aaron C. Siegmund ,  Ning Xi ,  Kevin Yang

IPC: A61K31/497 ,  A61K31/5377 ,  A61K31/437 ,  A61K31/519 ,  A61K31/4184 ,  A61K31/501 ,  A61K31/4709 ,  A61K31/4365

CPC classification number: C07D413/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US20120070413A1

公开(公告)日：2012-03-22

申请号：US13308310

申请日：2011-11-30

Applicant: Tae-Seong KIM ,  David Bauer ,  Steven Bellon ,  Alessadro Boezio ,  Shon Booker ,  Deborah Choquette ,  Derin C. D'Amico ,  Noel D'Angelo ,  Celia Dominguez ,  Ingrid M. Fellows ,  Julie Germain ,  Russell Graceffa ,  Jean-Christophe Harmange ,  Satoko Hirai ,  Daniel La ,  Matthew Lee ,  Longbin Liu ,  Mark H. Norman ,  Michele Potashman ,  Philip Roveto ,  Aaron C. Siegmund ,  Ning Xi ,  Kevin Yang

Inventor： Tae-Seong KIM ,  David Bauer ,  Steven Bellon ,  Alessadro Boezio ,  Shon Booker ,  Deborah Choquette ,  Derin C. D'Amico ,  Noel D'Angelo ,  Celia Dominguez ,  Ingrid M. Fellows ,  Julie Germain ,  Russell Graceffa ,  Jean-Christophe Harmange ,  Satoko Hirai ,  Daniel La ,  Matthew Lee ,  Longbin Liu ,  Mark H. Norman ,  Michele Potashman ,  Philip Roveto ,  Aaron C. Siegmund ,  Ning Xi ,  Kevin Yang

IPC: A61K38/21 ,  A61K31/497 ,  A61K31/5377 ,  A61P35/00 ,  A61K31/437 ,  A61K31/519 ,  A61K31/4184 ,  A61K31/501 ,  A61K31/4709 ,  A61K31/4365

CPC classification number: C07D413/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US07919504B2

公开(公告)日：2011-04-05

申请号：US12218523

申请日：2008-07-15

Applicant: Qingping Zeng ,  Chester Chenguang Yuan ,  Guomin Yao ,  Xianghong Wang ,  Seifu Tadesse ,  Andreas Reichelt ,  Qingyian Liu ,  Matthew R. Lee ,  Xin Huang ,  Fang-Tsao Hong ,  Nianhe Han ,  Christopher H. Fotsch ,  Celia Dominguez ,  Matthew P. Bourbeau ,  John G. Allen

Inventor： Qingping Zeng ,  Chester Chenguang Yuan ,  Guomin Yao ,  Xianghong Wang ,  Seifu Tadesse ,  Andreas Reichelt ,  Qingyian Liu ,  Matthew R. Lee ,  Xin Huang ,  Fang-Tsao Hong ,  Nianhe Han ,  Christopher H. Fotsch ,  Celia Dominguez ,  Matthew P. Bourbeau ,  John G. Allen

IPC: A61K31/47 ,  C07D401/04

CPC classification number: C07D285/135 ,  C07D417/04 ,  C07D417/14 ,  C07D495/04

Abstract: The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

Abstract translation: 本发明涉及式I和式II的噻唑化合物及其用于治疗由蛋白激酶B（PKB）介导的疾病的组合物，其中变量具有本文提供的定义。 本发明还涉及这种噻唑化合物及其组合物治疗与异常细胞生长，癌症，炎症和代谢紊乱相关的疾病的治疗用途。