公开(公告)号：US20060040956A1

公开(公告)日：2006-02-23

申请号：US11234713

申请日：2005-09-23

申请人： 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 Kim ,  Tae-Seong Kim ,  Alexander Kiselyov ,  Xiaohu Ouyang ,  Vinod Patel ,  Leon Smith ,  Markian Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Yuan ,  Michael Croghan

发明人： 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 Kim ,  Tae-Seong Kim ,  Alexander Kiselyov ,  Xiaohu Ouyang ,  Vinod Patel ,  Leon Smith ,  Markian Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Yuan ,  Michael Croghan

IPC分类号： A61K31/506 ,  C07D403/02

CPC分类号： 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

摘要： 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. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

公开(公告)号：US06958356B2

公开(公告)日：2005-10-25

申请号：US10098994

申请日：2002-03-13

申请人： Patrick Y. Lam ,  Charles G. Clark ,  Celia Dominguez ,  John M. Fevig ,  Amy Qi Han ,  Renhua Li ,  Donald J. Pinto ,  James R. Pruitt ,  Mimi L. Quan

发明人： Patrick Y. Lam ,  Charles G. Clark ,  Celia Dominguez ,  John M. Fevig ,  Amy Qi Han ,  Renhua Li ,  Donald J. Pinto ,  James R. Pruitt ,  Mimi L. Quan

IPC分类号： C07D231/14 ,  C07D231/56 ,  C07D233/54 ,  C07D233/61 ,  C07D261/20 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D413/04 ,  C07D413/14 ,  A61K31/42 ,  A61K31/415 ,  C07D231/00 ,  C07D235/04

CPC分类号： C07D413/14 ,  C07D231/14 ,  C07D231/56 ,  C07D261/20 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D413/04

摘要： The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.

摘要翻译： 本申请描述了含氮杂芳族化合物及其式I的衍生物或其药学上可接受的盐形式，其中环D-E表示胍模拟物，其可用作因子Xa的抑制剂。

公开(公告)号：US5731439A

公开(公告)日：1998-03-24

申请号：US409303

申请日：1995-03-24

申请人： David John Carini ,  Joseph Cacciola ,  Celia Dominguez ,  John Matthew Fevig

发明人： David John Carini ,  Joseph Cacciola ,  Celia Dominguez ,  John Matthew Fevig

IPC分类号： A61K38/00 ,  C07F5/02 ,  C07K5/06 ,  C07F5/04 ,  C07F5/05

CPC分类号： C07F5/025 ,  C07F5/02 ,  C07K5/06191 ,  A61K38/00

摘要： The present invention relates generally to .alpha.-aminoboronic acids and corresponding peptide analogs in which the .alpha.-carbon is substituted with an optionally functionalized piperidine containing alkyl group. These compounds are useful as inhibitors of trypsin-like serine protease enzymes.

摘要翻译： 本发明一般涉及α-氨基硼酸和相应的肽类似物，其中α-碳被任选官能化的含哌啶烷基取代。 这些化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂。

公开(公告)号：US08946197B2

公开(公告)日：2015-02-03

申请号：US13509783

申请日：2010-11-12

申请人： Celia Dominguez ,  John Wityak ,  Michael Prime ,  Stephen Martin Courtney ,  Christopher Yarnold ,  Frederick Brookfield ,  Richard Marston ,  Douglas Macdonald

发明人： Celia Dominguez ,  John Wityak ,  Michael Prime ,  Stephen Martin Courtney ,  Christopher Yarnold ,  Frederick Brookfield ,  Richard Marston ,  Douglas Macdonald

IPC分类号： A61K31/635 ,  C07C311/46 ,  C07D211/34 ,  C07D211/54 ,  C07D211/58 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D215/38 ,  C07D217/14 ,  C07D217/22 ,  C07D239/42 ,  C07D263/58 ,  C07D277/42 ,  C07D295/205 ,  C07D295/26 ,  C07D307/52 ,  C07D401/04 ,  C07D487/04 ,  C07D495/04

CPC分类号： C07C311/46 ,  C07C2601/14 ,  C07D211/34 ,  C07D211/54 ,  C07D211/58 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D215/38 ,  C07D217/14 ,  C07D217/22 ,  C07D239/42 ,  C07D263/58 ,  C07D277/42 ,  C07D295/205 ,  C07D295/26 ,  C07D307/52 ,  C07D401/04 ,  C07D487/04 ,  C07D495/04

摘要： 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.

摘要翻译： 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：US20140163009A1

公开(公告)日：2014-06-12

申请号：US13981107

申请日：2012-01-23

申请人： Christopher A Luckhurst ,  Alen F Haughan ,  Perla Breccia ,  Andrew J Stott ,  Roland W Burli ,  Samantha J Hughes ,  Ignacio Munoz-Sanjuan ,  Celia Dominguez

发明人： Christopher A Luckhurst ,  Alen F Haughan ,  Perla Breccia ,  Andrew J Stott ,  Roland W Burli ,  Samantha J Hughes ,  Ignacio Munoz-Sanjuan ,  Celia Dominguez

IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D231/12 ,  C07D409/08 ,  C07D233/64 ,  C07D267/14 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07C259/08 ,  C07C311/14 ,  C07C2601/02 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/10 ,  C07D209/44 ,  C07D209/46 ,  C07D209/82 ,  C07D211/58 ,  C07D211/70 ,  C07D213/56 ,  C07D213/74 ,  C07D215/18 ,  C07D231/12 ,  C07D233/61 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D263/32 ,  C07D265/36 ,  C07D267/14 ,  C07D277/30 ,  C07D295/155 ,  C07D317/46 ,  C07D319/18 ,  C07D401/04 ,  C07D409/08 ,  C07D413/04 ,  C07D417/08 ,  C07D471/04 ,  C07D487/04 ,  C07D491/10

摘要： Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.

摘要翻译： 提供式I的组蛋白脱乙酰酶（HDAC）抑制剂，其组合物及其使用方法。

公开(公告)号：US08642624B2

公开(公告)日：2014-02-04

申请号：US13297213

申请日：2011-11-15

申请人： Guoqing Chen ,  Jeffrey A. Adams ,  Jean E. Bemis ,  Shon Booker ,  Guolin Cai ,  Lucian V. DiPietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Stephanie Geuns-Meyer ,  Michael K. Handley ,  Qi Huang ,  Joseph L. Kim ,  Tae-Seong Kim ,  Alexander S. Kiselyov ,  Xiaohu Ouyang ,  Vinod F. Patel ,  Leon M. Smith ,  Markian M. Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Chenguang Yuan ,  Michael D. Croghan

发明人： Guoqing Chen ,  Jeffrey A. Adams ,  Jean E. Bemis ,  Shon Booker ,  Guolin Cai ,  Lucian V. DiPietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Stephanie Geuns-Meyer ,  Michael K. Handley ,  Qi Huang ,  Joseph L. Kim ,  Tae-Seong Kim ,  Alexander S. Kiselyov ,  Xiaohu Ouyang ,  Vinod F. Patel ,  Leon M. Smith ,  Markian M. Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Chenguang Yuan ,  Michael D. Croghan

IPC分类号： A01N43/40 ,  A61K31/44 ,  A01N43/38 ,  A61K31/40 ,  A61K31/405

CPC分类号： 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

摘要： 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.

摘要翻译： 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：US20130029988A1

公开(公告)日：2013-01-31

申请号：US13575019

申请日：2011-01-20

申请人： Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Dirk Winkler ,  Frederick Brookfield ,  Paula C. De Aguiar Pena

发明人： Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Dirk Winkler ,  Frederick Brookfield ,  Paula C. De Aguiar Pena

IPC分类号： C07D403/04 ,  A61K31/505 ,  A61K31/506 ,  C07D413/04 ,  C07D413/14 ,  A61P25/08 ,  C07D401/04 ,  A61K31/513 ,  C07D417/04 ,  A61P25/28 ,  A61P25/16 ,  A61P25/00 ,  C07D239/28 ,  A61K31/5377

CPC分类号： C07D403/04 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4245 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

摘要： 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.

摘要翻译： 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：US20090143575A1

公开(公告)日：2009-06-04

申请号：US12367352

申请日：2009-02-06

申请人： 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

发明人： 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分类号： C07D413/14 ,  C07D471/04 ,  C07D401/14

CPC分类号： C07D401/04 ,  C07D235/30 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： 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.

摘要翻译： 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。

公开(公告)号：US07332511B2

公开(公告)日：2008-02-19

申请号：US11195159

申请日：2005-08-01

申请人： Elizabeth M. Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark H. Norman ,  Hui-Ling Wang ,  Christopher H. Fotsch ,  Ning Chen ,  Partha P. Chakrabarti ,  Celia Dominguez ,  James Richard Falsey ,  Christopher Hulme ,  Jodie Katon ,  Thomas Nixey ,  Vassil I. Ognyanov ,  Liping H. Pettus ,  Robert Michael Rzasa

发明人： Elizabeth M. Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark H. Norman ,  Hui-Ling Wang ,  Christopher H. Fotsch ,  Ning Chen ,  Partha P. Chakrabarti ,  Celia Dominguez ,  James Richard Falsey ,  Christopher Hulme ,  Jodie Katon ,  Thomas Nixey ,  Vassil I. Ognyanov ,  Liping H. Pettus ,  Robert Michael Rzasa

IPC分类号： C07D213/30 ,  C07D213/32 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  A61K31/4427 ,  A61P19/02 ,  A61P35/00

CPC分类号： 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

摘要： 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：US07105682B2

公开(公告)日：2006-09-12

申请号：US10046622

申请日：2002-01-10

申请人： Guoqing Chen ,  Jeffrey Adams ,  Jean Bemis ,  Lucian Di Pietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Qi Huang ,  Joseph L. Kim ,  Xiaohu Ouyang ,  Vinod F. Patel ,  Leon M. Smith ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Chenguang Yuan ,  Michael Croghan ,  Tae-Seong Kim

发明人： Guoqing Chen ,  Jeffrey Adams ,  Jean Bemis ,  Lucian Di Pietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Qi Huang ,  Joseph L. Kim ,  Xiaohu Ouyang ,  Vinod F. Patel ,  Leon M. Smith ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Chenguang Yuan ,  Michael Croghan ,  Tae-Seong Kim

IPC分类号： C07D401/02 ,  A61K31/44

CPC分类号： C07D401/14 ,  A61K31/00 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  Y02A50/401

摘要： Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis 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.