公开(公告)号：US5656625A

公开(公告)日：1997-08-12

申请号：US442867

申请日：1995-05-17

Applicant: Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

Inventor： Wayne Bowen ,  Brian R. de Costa ,  Celia Dominguez ,  Xiao-Shu He ,  Kenner C. Rice

IPC: C07D207/14 ,  C07D211/56 ,  C07D223/12 ,  C07D409/06 ,  C07D403/04 ,  A61K31/55 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D409/06 ,  C07D207/14 ,  C07D211/56 ,  C07D223/12

Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

Abstract translation: 描述某些含氮环杂环烷基氨基芳基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。 特别感兴趣的化合物具有下式：其中R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R8至R11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中n为4-6的整数; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。 或其药学上可接受的盐。

公开(公告)号：US09981918B2

公开(公告)日：2018-05-29

申请号：US14241374

申请日：2012-08-28

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

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

IPC: C07D237/28 ,  A61K31/70 ,  C07D239/28 ,  C07D405/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10 ,  C07D239/42 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/048 ,  C07D491/052 ,  C07H13/10 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

CPC classification number: C07D239/28 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/048 ,  C07D491/052 ,  C07H13/10

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.

公开(公告)号：US20150232420A1

公开(公告)日：2015-08-20

申请号：US14429288

申请日：2013-09-19

Applicant: Celia DOMINGUEZ ,  Michael PRIME ,  Richard MARSTON ,  Frederick A. BROOKFIELD ,  Stephen M. COURTNEY ,  Douglas MACDONALD ,  John WITYAK ,  Christopher John YARNOLD ,  Darshan VAIDYA

Inventor： Celia Dominguez ,  Michael Prime ,  Richard Marston ,  Frederick A. Brookfield ,  Stephen M. Courtney ,  Douglas Macdonald ,  John Wityak ,  Christopher John Yarnold ,  Darshan Vaidya

IPC: C07C271/22 ,  C07D207/06 ,  C07D213/74 ,  C07D205/04 ,  C07D211/08 ,  C07D295/185 ,  C07D223/04

CPC classification number: C07C271/22 ,  C07D205/04 ,  C07D207/06 ,  C07D207/16 ,  C07D211/08 ,  C07D211/16 ,  C07D213/72 ,  C07D213/74 ,  C07D223/04 ,  C07D277/42 ,  C07D295/18 ,  C07D295/185 ,  C07D309/08 ,  C07D401/12

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：US08691824B2

公开(公告)日：2014-04-08

申请号：US13056919

申请日：2009-08-03

Applicant: John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

Inventor： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

IPC: A61K31/497

CPC classification number: A61K31/42 ,  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：US20130331370A1

公开(公告)日：2013-12-12

申请号：US13963822

申请日：2013-08-09

Applicant: John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

Inventor： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

IPC: C07D239/52 ,  C07D403/12 ,  C07D401/12 ,  C07D239/38 ,  C07D239/69

CPC classification number: C07D239/52 ,  A61K31/505 ,  A61K31/506 ,  C07D213/79 ,  C07D213/81 ,  C07D239/28 ,  C07D239/38 ,  C07D239/42 ,  C07D239/69 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  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.

公开(公告)号：US20120329812A1

公开(公告)日：2012-12-27

申请号：US13056919

申请日：2009-08-03

Applicant: John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

Inventor： John Wityak ,  Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Paula C. De Aguiar Pena ,  Andreas Scheel ,  Dirk Winkler

IPC: A61K31/42 ,  C07D413/12 ,  A61K31/4439 ,  A61K31/506 ,  A61P25/08 ,  A61K31/437 ,  A61K31/422 ,  C07D413/06 ,  A61P25/28 ,  A61P25/16 ,  C07D261/04 ,  C07D471/04

CPC classification number: A61K31/42 ,  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：US20120065185A1

公开(公告)日：2012-03-15

申请号：US13297213

申请日：2011-11-15

Applicant: Guoqing CHEN ,  Jeffrey Adams ,  Jean Bemis ,  Shon Booker ,  Guolin Cai ,  Lucian Di Pietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Stephanie Geuns-Meyer ,  Michael Handley ,  Qi Huang ,  Joseph L. Kim ,  Tae-Seong Kim ,  Alexander Kiselyov ,  Xiaohu Ouyang ,  Vinod F. Patel ,  Leon M. Smith ,  Markian Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Chenguang Yuan ,  Michael Croghan

Inventor： Guoqing CHEN ,  Jeffrey Adams ,  Jean Bemis ,  Shon Booker ,  Guolin Cai ,  Lucian Di Pietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Stephanie Geuns-Meyer ,  Michael Handley ,  Qi Huang ,  Joseph L. Kim ,  Tae-Seong Kim ,  Alexander Kiselyov ,  Xiaohu Ouyang ,  Vinod F. Patel ,  Leon M. Smith ,  Markian Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Chenguang Yuan ,  Michael Croghan

IPC: A61K31/4436 ,  A61K31/4709 ,  A61K31/4725 ,  A61P3/00 ,  A61P7/00 ,  A61P35/00 ,  A61P31/00 ,  A61K31/444 ,  A61K31/5377

CPC classification number: C07D213/82 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/00 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like.

Abstract translation: 所选择的杂环化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新型化合物，类似物，前药及其药学上可接受的衍生物，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。

公开(公告)号：US08088794B2

公开(公告)日：2012-01-03

申请号：US12945575

申请日：2010-11-12

Applicant: Tae-Seong Kim ,  David Bauer ,  Steven Bellon ,  Alessandro 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 ,  Alessandro 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: A61K31/47 ,  C07D453/02

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：US08084479B2

公开(公告)日：2011-12-27

申请号：US12378195

申请日：2009-02-11

Applicant: Qingping Zeng ,  John G. Allen ,  Matthew P. Bourbeau ,  Celia Dominguez ,  Christopher H. Fotsch ,  Nianhe Han ,  Fang-Tsao Hong ,  Xin Huang ,  Matthew R. Lee ,  Aiwen Li ,  Qingyian Liu ,  James T. Rider ,  Seifu Tadesse ,  Andrew S. Tasker ,  Vellarkad N. Viswanadhan ,  Xianghong Wang ,  Kurt E. Weiler ,  George E. Wohlhieter ,  Guomin Yao ,  Chester Chenguang Yuan

Inventor： Qingping Zeng ,  John G. Allen ,  Matthew P. Bourbeau ,  Celia Dominguez ,  Christopher H. Fotsch ,  Nianhe Han ,  Fang-Tsao Hong ,  Xin Huang ,  Matthew R. Lee ,  Aiwen Li ,  Qingyian Liu ,  James T. Rider ,  Seifu Tadesse ,  Andrew S. Tasker ,  Vellarkad N. Viswanadhan ,  Xianghong Wang ,  Kurt E. Weiler ,  George E. Wohlhieter ,  Guomin Yao ,  Chester Chenguang Yuan

IPC: A01N43/38 ,  A01N43/78 ,  A61K31/405 ,  A61K31/425 ,  C07D277/00

CPC classification number: C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

Abstract: The invention relates to methods of using thiazole compounds of Formula I and Formula II and compositions thereof for treating diseases mediated by protein kinase B (PKB) such as cancer and other proliferative disorders where the variables have the definitions provided herein.

Abstract translation: 本发明涉及使用式I和式II的噻唑化合物及其组合物用于治疗由蛋白激酶B（PKB）介导的疾病，例如癌症和其它增殖性疾病，其中变量具有本文提供的定义。

公开(公告)号：US08026241B2

公开(公告)日：2011-09-27

申请号：US12367352

申请日：2009-02-06

Applicant: Chenera Balan ,  Yunxin Bo ,  Celia Dominguez ,  Christopher H. Fotsch ,  Vijay K. Gore ,  Vu Van Ma ,  Mark H. Norman ,  Vassil I. Ognyanov ,  Yi-xin Qian ,  Xianghong Wang ,  Ning Xi ,  Shimin Xu

Inventor： Chenera Balan ,  Yunxin Bo ,  Celia Dominguez ,  Christopher H. Fotsch ,  Vijay K. Gore ,  Vu Van Ma ,  Mark H. Norman ,  Vassil I. Ognyanov ,  Yi-xin Qian ,  Xianghong Wang ,  Ning Xi ,  Shimin Xu

IPC: A61K31/497 ,  C07D403/04 ,  C07D401/04

CPC classification number: C07D401/04 ,  C07D235/30 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: Therapeutic benzimidazoles 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 necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

Abstract translation: 治疗性苯并咪唑和含有它们的组合物，用于治疗急性，炎性和神经性疼痛，牙痛，一般头痛，偏头痛，丛集性头痛，混合血管和非血管综合征，紧张性头痛，一般炎症，关节炎，风湿性疾病，骨关节炎 ，炎症性肠病，炎症性眼病，炎症性或不稳定性膀胱病，银屑病，皮肤炎症成分炎症，慢性炎性病症，炎性疼痛及相关的痛觉过敏和异常性疼痛，神经性疼痛及相关的痛觉过敏和异常性疼痛，糖尿病性神经病疼痛，灼痛，交感神经痛 维持疼痛，输血综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道，泌尿生殖道，胃肠道或血管区内脏运动紊乱，伤口，烧伤，过敏性皮肤反应，瘙痒，白癜风，一般胃肠道疾病，胃溃疡 十二指肠溃疡，腹泻，坏死因子诱发的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。