-
公开(公告)号：US06288046B1
公开(公告)日：2001-09-11
申请号：US09298866
申请日：1999-04-26
IPC分类号： A61K31683
CPC分类号： A61K31/661 , A61K31/194 , A61K38/05 , A61K38/06 , C07F9/301
摘要： The present invention relates to phosphonic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.
摘要翻译： 本发明涉及抑制N-乙酰化α连接酸性二肽酶（NAALADase）酶活性的膦酸衍生物，包含这些衍生物的药物组合物，以及使用这些衍生物抑制NAALADase活性的方法，治疗谷氨酸异常和治疗 动物前列腺疾病。
-
42.发明授权Asymmetric syntheses and intermediates for preparing enantiomer-enriched hydroxyphosphinyl derivatives 失效制备富含对映体的羟基氧膦基衍生物的不对称合成和中间体
公开(公告)号：US6028216A
公开(公告)日：2000-02-22
申请号：US2146
申请日：1997-12-31
申请人： Guillermo Morales , Weixing Li , Paul F. Jackson
发明人： Guillermo Morales , Weixing Li , Paul F. Jackson
CPC分类号： C07F9/3217 , C07F9/301 , C07F9/302 , C07F9/3826
摘要： The present invention relates to asymmetric syntheses and intermediates for preparing enantiomer-enriched hydroxyphosphinyl derivatives.
摘要翻译： 本发明涉及用于制备富含对映体的羟基氧膦基衍生物的不对称合成和中间体。
-
43.发明授权Pharmaceutical compositions and methods of treating a glutamate abnormality and effecting a neuronal activity in an animal using NAALADase inhibitors 失效使用NAALADase抑制剂治疗谷氨酸异常和影响动物神经元活性的药物组合物和方法
公开(公告)号：US6017903A
公开(公告)日：2000-01-25
申请号：US884479
申请日：1997-06-27
IPC分类号： A61K31/194 , A61K31/665 , A61K31/675 , A61K38/05 , A61K38/06 , C07F9/30 , C07F9/38 , C07F9/40 , C07F9/44 , C07F9/58 , C07F9/655 , C07F9/6553 , A61K31/66
CPC分类号： A61K31/661 , A61K31/194 , A61K31/665 , A61K31/675 , A61K38/05 , A61K38/06 , C07F9/301 , C07F9/3808 , C07F9/3826 , C07F9/4075 , C07F9/4465 , C07F9/582 , C07F9/65515 , C07F9/6552 , C07F9/655345
摘要： The present invention relates to a method of treating a glutamate abnormality and a method of effecting a neuronal activity in an animal using a NAALADase inhibitor, and a pharmaceutical composition comprising an effective amount of a NAALADase inhibitor for treating a glutamate abnormality and effecting a neuronal activity in an animal.
摘要翻译： 本发明涉及一种治疗谷氨酸异常的方法和使用NAALADase抑制剂在动物中进行神经元活性的方法，以及包含有效量的用于治疗谷氨酸异常和影响神经元活性的NAALADase抑制剂的药物组合物 在一个动物
-
公开(公告)号：US5962521A
公开(公告)日：1999-10-05
申请号：US825997
申请日：1997-04-04
IPC分类号： A61P25/04 , A61K31/194 , A61K31/197 , A61K31/4409 , A61K38/05 , A61K38/06 , A61K45/00 , A61P9/10 , A61P13/08 , A61P21/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P35/00 , A61P43/00 , C07C259/06 , C07D213/76 , C07D213/81 , C07F9/30 , A61K31/215 , C07C229/48 , C07C255/02
CPC分类号： A61K31/661 , A61K31/194 , A61K38/05 , A61K38/06 , C07F9/301
摘要： The present invention relates to hydroxamic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.
摘要翻译： 本发明涉及抑制N-乙酰化α-脱氢酸二肽酶（NAALADase）酶活性的异羟肟酸衍生物，包含这些衍生物的药物组合物，以及使用这些衍生物抑制NAALADase活性的方法，治疗谷氨酸异常和治疗 动物前列腺疾病。
-
公开(公告)号：US5747523A
公开(公告)日：1998-05-05
申请号：US590641
申请日：1996-01-24
申请人： Paul F. Jackson
发明人： Paul F. Jackson
IPC分类号： C07D205/04 , C07D207/32 , C07D207/325 , C07D213/30 , C07D231/12 , C07D239/26 , C07D295/088 , C07D521/00 , A01N43/36 , C07D207/04 , C07D207/18 , C07D207/30
CPC分类号： C07D207/325 , C07D205/04 , C07D213/30 , C07D231/12 , C07D233/56 , C07D239/26 , C07D249/08 , C07D295/088
摘要： The invention relates to substituted ethyl .alpha.,.alpha.-diarylmethyl ether derivatives and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, and methods of treating cocaine addiction and overdose, and diseases and conditions characterized by abnormal dopaminergic neurotransmission, using the same.
摘要翻译： 本发明涉及取代的α，α-二芳基甲基醚衍生物及其药学上可接受的盐，包含它们的药物组合物，治疗可卡因成瘾和过量的方法，以及特征为异常多巴胺能神经传递的疾病和病症。
-
公开(公告)号：US5502048A
公开(公告)日：1996-03-26
申请号：US255613
申请日：1994-06-09
申请人： Marc J. Chapdelaine , Timothy W. Davenport , Laura E. Garcia-Davenport , Paul F. Jackson , Jeffrey A. McKinney , Charles D. McLaren
发明人： Marc J. Chapdelaine , Timothy W. Davenport , Laura E. Garcia-Davenport , Paul F. Jackson , Jeffrey A. McKinney , Charles D. McLaren
IPC分类号： A61K31/55 , A61P25/00 , A61P25/28 , C07D223/16 , C07D401/04 , C07D405/04 , C07D409/04 , C07F7/08
CPC分类号： C07D223/16 , C07D401/04 , C07D405/04 , C07D409/04 , C07F7/0812
摘要： Antagonists at the NMDA receptor complex which are benz b!azepines having a hydroxy, alkoxy or amino substituent at the 3-position and a 4-position alkenyl, alkynyl, aryl or heteroaryl substituent for treatment of stroke and/or other neurodegenerative disorders.
摘要翻译： NMDA受体复合物的拮抗剂是苯并[b]吖庚因，其在3-位上具有羟基，烷氧基或氨基取代基，以及4-位烯基，炔基，芳基或杂芳基取代基，用于治疗中风和/或其它神经变性疾病。
-
47.发明授权Methods of treatment using allosteric processing inhibitors for matrix metalloproteinases 有权使用变构加工抑制剂治疗基质金属蛋白酶的方法公开(公告)号：US08883473B2
公开(公告)日：2014-11-11
申请号：US13533131
申请日：2012-06-26
申请人： Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Carl Crysler , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Carl Manthey , Cynthia M. Milligan , Beverley Moore , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett A. Tounge , Aihua Wang
发明人： Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Carl Crysler , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Carl Manthey , Cynthia M. Milligan , Beverley Moore , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett A. Tounge , Aihua Wang
IPC分类号： A61K31/4439 , A61K31/427 , A61P19/02 , A61K31/425
CPC分类号： A61K31/425 , A61K31/4439 , C07K2299/00 , G01N2333/96486
摘要： The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.
摘要翻译： 本发明包括晶体，其包含基质金属蛋白酶（proMMP）的形式的复合物和抑制该proMMP活化的小分子变构加工抑制剂，用于鉴定抑制激活的小分子变构加工抑制剂的方法 proMMP和使用抑制proMMP激活的小分子变构加工抑制剂的治疗方法。 本发明涉及与抑制proMMP9激活的小分子变构加工抑制剂结合的proMMP9的复合物的晶体结构。 本发明还涉及用于设计，选择和/或优化抑制proMMP9和proMMP9同源物激活的小分子变构加工抑制剂的方法和结晶及相关结构信息的使用。 本发明还涉及小分子变构加工抑制剂用于治疗由不适当的基质金属蛋白酶（MMP）活性介导的疾病的用途。
-
48.发明授权Arylindenopyrimidines compound and use as an adenosine A2a receptor antagonists 失效亚苄基嘧啶化合物，用作腺苷A2a受体拮抗剂公开(公告)号：US08017614B2
公开(公告)日：2011-09-13
申请号：US12253358
申请日：2008-10-17
申请人： Brian C. Shook , Paul F. Jackson
发明人： Brian C. Shook , Paul F. Jackson
IPC分类号： A61K31/497 , A61K31/505 , A01N43/54 , C07D239/70 , C07D403/00
CPC分类号： C07D239/70
摘要： This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease.
摘要翻译： 本发明涉及一种新型的吲哚基嘧啶A及其治疗和预防用途。 治疗和/或预防的疾病包括帕金森病。
-
公开(公告)号：US06452044B2
公开(公告)日：2002-09-17
申请号：US09866758
申请日：2001-05-30
IPC分类号： C07C32110
CPC分类号： C07D231/06 , C07C63/307 , C07C63/68 , C07C65/05 , C07C65/40 , C07C229/38 , C07C229/60 , C07C235/80 , C07C259/06 , C07C259/10 , C07C317/44 , C07C323/12 , C07C323/56 , C07C323/62 , C07D307/52 , C07F9/3834 , C07F9/3882
摘要： New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnstic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neutopathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.
-
50.发明授权Compounds, methods and pharmaceutical compositions for treating neural or cardiovascular tissue damage 失效用于治疗神经或心血管组织损伤的化合物，方法和药物组合物公开(公告)号：US06306889B1
公开(公告)日：2001-10-23
申请号：US09047502
申请日：1998-03-25
申请人： Jia-He Li , Jie Zhang , Paul F. Jackson , Keith M. Maclin
发明人： Jia-He Li , Jie Zhang , Paul F. Jackson , Keith M. Maclin
IPC分类号： A61K31407
CPC分类号： C07D249/08 , A61K31/4741 , A61K31/502 , A61K31/5025 , C07D231/12 , C07D233/56 , C07D237/32 , C07D491/06 , C07D495/06
摘要： This invention relates to compounds, pharmaceutical compositions, and methods for the treatment or prevention of neural or cardiovascular tissue damage related to cerebral ischemia and reperfusion injury in an animal by administering Poly(ADP-ribose) polymerase (“PARP”) inhibitors.
摘要翻译： 本发明涉及通过施用Poly（ADP-核糖）聚合酶（“PARP”）抑制剂来治疗或预防与脑缺血和再灌注损伤相关的神经或心血管组织损伤的化合物，药物组合物和方法。
-
-
-
-
-
-
-
-
-
搜索结果
58 条记录 (耗时 0.051 秒)
