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41. 发明授权

US07888345B2 Benzaepinones as sodium channel blockers 失效
标题翻译： Benzaepinones作为钠通道阻滞剂
公开(公告)号：US07888345B2
公开(公告)日：2011-02-15
申请号：US12308209
申请日：2007-06-05
申请人： Scott B. Hoyt , Clare London , Dong Ok , William H. Parsons
发明人： Scott B. Hoyt , Clare London , Dong Ok , William H. Parsons
IPC分类号： C07D223/16 , A61K31/55 , A61P29/02
CPC分类号： C07D223/16 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12
摘要： Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.
摘要翻译：由式（I）表示的苯并氮杂酮化合物或其药学上可接受的盐。药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗与钠通道活性相关或由其引起的症状的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，癫痫，肠易激综合征，尿失禁，瘙痒，瘙痒，过敏性皮炎抑郁，焦虑，多发性硬化和双相性精神障碍，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。

42. 发明授权

US5310903A Imidazolidyl rapamycin derivatives 失效
标题翻译：咪唑烷雷怕霉素衍生物
公开(公告)号：US5310903A
公开(公告)日：1994-05-10
申请号：US26925
申请日：1993-03-05
申请人： Mark Goulet , William H. Parsons , Matthew J. Wyvratt
发明人： Mark Goulet , William H. Parsons , Matthew J. Wyvratt
IPC分类号： C07D498/18 , A61K31/395
CPC分类号： C07D498/18
摘要： Imidazolidyl rapamycin derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-42 and/or C-31. These compounds are useful in a mammalian host for the treatment of autoimmune diseases and diseases of inflammation, infectious diseases, the prevention of rejection of foreign organ transplants and the treatment of solid tumors.
摘要翻译：一般结构式I的咪唑烷基雷帕霉素衍生物：通过C-42和/或C-31的烷基化和/或芳基化从合适的前体制备。这些化合物可用于哺乳动物宿主用于治疗自身免疫性疾病和炎症疾病，感染性疾病，预防外来器官移植排斥和治疗实体瘤。

43. 发明授权

US5039664A Renin inhibitors containing phenylalanyl-histidine replacements 失效
公开(公告)号：US5039664A
公开(公告)日：1991-08-13
申请号：US320666
申请日：1989-03-08
申请人： Arthur A. Patchett , William H. Parsons , William J. Greenlee , Prasun K. Chakravarty
发明人： Arthur A. Patchett , William H. Parsons , William J. Greenlee , Prasun K. Chakravarty
IPC分类号： C07K5/02
CPC分类号： C07K5/0207
摘要： Peptides of the formula: ##STR1## which comprise novel elements replacing the Phe(8)-His(9) sequence in renin-inhibitory peptides based on substrate analogy, which inhibit the substrate-cleaving action of renin and have improved bioavailability; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension or congestive heart failure or of establishing renin as a causative factor in these problems which employ the novel peptides.

44. 发明授权

US4715994A Novel antibacterial agents and potentiators of carbapenem antibiotics 失效
标题翻译：新型抗菌药物和碳青霉烯类抗生素的增效剂
公开(公告)号：US4715994A
公开(公告)日：1987-12-29
申请号：US927028
申请日：1986-11-05
申请人： William H. Parsons , William R. Schoen , Arthur A. Patchett , Masao Taniguchi
发明人： William H. Parsons , William R. Schoen , Arthur A. Patchett , Masao Taniguchi
IPC分类号： C07F9/30 , C07F9/32 , C07F9/58 , A01N31/02 , A01N57/12
CPC分类号： C07F9/582 , C07F9/301 , C07F9/302 , C07F9/3211 , C07F9/3217
摘要： New 3-(1-aminoalkylphosphinyl)-(2-substituted)propionic acids are described which display antibacterial activity and potentiate carbapenem antibiotics.
摘要翻译：描述了新的3-（1-氨基烷基氧膦基） - （2-取代的）丙酸，其表现出抗菌活性并增强碳青霉烯类抗生素。

45. 发明授权

US07612211B2 Benzimidazole TRPV1 inhibitors 有权
标题翻译：苯并咪唑TRPV1抑制剂
公开(公告)号：US07612211B2
公开(公告)日：2009-11-03
申请号：US11954647
申请日：2007-12-12
申请人： Wing S. Cheung , Daniel J. Parks , William H. Parsons , Sharmila Patel , Mark R. Player
发明人： Wing S. Cheung , Daniel J. Parks , William H. Parsons , Sharmila Patel , Mark R. Player
IPC分类号： A61K31/4184 , C07D235/12
CPC分类号： C07D235/12 , C07D235/06 , C07D235/14 , C07D235/26 , C07D235/30 , C07D401/12 , C07D405/12
摘要： The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.
摘要翻译：本发明涉及式（I）的化合物：含有这些化合物的药物组合物和使用它们的治疗方法。

46. 发明授权

US07589116B2 Biaryl substituted pyrazoles as sodium channel blockers 失效
标题翻译：二芳基取代的吡唑作为钠通道阻断剂
公开(公告)号：US07589116B2
公开(公告)日：2009-09-15
申请号：US10552024
申请日：2004-03-30
申请人： Prasun K. Chakravarty , Michael H. Fisher , Jeffrey M. Fisher, legal representative , William H. Parsons , Sriram Tyagarajan , Bishan Zhou
发明人： Prasun K. Chakravarty , Michael H. Fisher , William H. Parsons , Sriram Tyagarajan , Bishan Zhou
IPC分类号： A61K31/415 , C07D231/00
CPC分类号： C07D401/04 , C07D231/14 , C07D401/10 , C07D403/04 , C07D403/10 , C07D403/12 , C07D409/10 , C07D409/14 , C07D413/12 , C07D417/12
摘要： Biaryl substituted pyrazole compounds are sodium channel blockers useful for the treatment of pain and other conditions. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treatment of conditions, including acute pain, chronic pain, visceral pain, inflammatory pain, and neuropathic pain, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more therapeutically active compounds.
摘要翻译：双芳基取代的吡唑化合物是可用于治疗疼痛和其它病症的钠通道阻断剂。药物组合物包含单独的或与一种或多种治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。包括急性疼痛，慢性疼痛，内脏痛，炎性疼痛和神经性疼痛的病症的治疗方法包括单独施用有效量的本发明化合物或与一种或多种治疗活性化合物组合施用。

47. 发明申请

US20080146637A1 BENZIMIDAZOLE TRPV1 INHIBITORS 有权
标题翻译：苯并咪唑TRPV1抑制剂
公开(公告)号：US20080146637A1
公开(公告)日：2008-06-19
申请号：US11954647
申请日：2007-12-12
申请人： Wing S. Cheung , Daniel J. Parks , William H. Parsons , Sharmila Patel , Mark R. Player
发明人： Wing S. Cheung , Daniel J. Parks , William H. Parsons , Sharmila Patel , Mark R. Player
IPC分类号： A61K31/4184 , A61P29/00 , C07D235/12
CPC分类号： C07D235/12 , C07D235/06 , C07D235/14 , C07D235/26 , C07D235/30 , C07D401/12 , C07D405/12
摘要： The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.
摘要翻译：本发明涉及式（I）的化合物：含有这些化合物的药物组合物和使用它们的治疗方法。

48. 发明授权

US06545023B2 Cyclopentyl modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的环戊基调节剂
公开(公告)号：US06545023B2
公开(公告)日：2003-04-08
申请号：US09931454
申请日：2001-08-16
申请人： Lihu Yang , Gabor Butora , William H. Parsons , Alexander Pasternak
发明人： Lihu Yang , Gabor Butora , William H. Parsons , Alexander Pasternak
IPC分类号： A61K31445
CPC分类号： C07D221/20 , A61K31/451 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/52 , C07D211/60 , C07D211/62 , C07D211/64 , C07D217/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/155 , C07D401/08 , C07D401/12 , C07D413/08 , C07D491/10
摘要： The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 and X are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
摘要翻译：本发明涉及可用作趋化因子受体活性调节剂的式I化合物（其中R1，R2，R3，R4，R5，R6和X如本文所定义）。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂。

49. 发明授权

US5145990A Phosphorous containing dhp enzyme inhibitors 失效
标题翻译：含磷的dhp酶抑制剂
公开(公告)号：US5145990A
公开(公告)日：1992-09-08
申请号：US642692
申请日：1991-01-09
申请人： William H. Parsons , William R. Schoen , Arthur A. Patchett
发明人： William H. Parsons , William R. Schoen , Arthur A. Patchett
IPC分类号： A61K31/40 , C07F9/30 , C07F9/58
CPC分类号： C07F9/582 , A61K31/40 , C07F9/301 , C07F9/302 , C07F9/303 , C07F9/306
摘要： Compounds of the formula: ##STR1## wherein R.sub.1 is C.sub.2- C.sub.12 linear or branched unsubstituted alkyl; C.sub.1- C.sub.12 linear or branched substituted alkyl; C.sub.2 -C.sub.12 linear or branched monoalkenyl; C.sub.2 -C.sub.12 linear or branched alkynyl; C.sub.7 -C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein these values for R.sub.1, other than C.sub.2- C.sub.12 linear or branched unsubstituted alkyl, can be substituted by one or more of C.sub.1 -C.sub.4 alkoxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, C.sub.6- C.sub.12 aryloxy, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.10 aralkyloxy, C.sub.7- C.sub.16 aralkyl-thio; and R.sub.5 is H or C.sub.1- C.sub.12 linear or branched alkyl; C.sub.2- C.sub.12 linear or branched monoalkenyl; C.sub.7- C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; heterocyclic alkyl wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the heterocyclic ring is 5-6 membered, optionally fused with a benzene ring, fully aromatic, containing 1 to 2 of oxygen, nitrogen or sulfur as heteroatoms; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein the values for R.sub.5 can be substituted by one or more of halo, hydroxy, carboxy, C.sub.1- C.sub.4 alkoxycarbonyl, C.sub.7- C.sub.16 arylalkoxycarbonyl, C.sub.3- C.sub.7 cycloalkyl, C.sub.1- C.sub.4 alkoxy, C.sub.6- C.sub.12 aryloxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, amino, mono- or di- C.sub.1- C.sub.8 alkylamino, thio, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.16 aralkylthio, or the radical --S--(CH.sub.2).sub.n CH(NH.sub.2)COOH. These compounds have dehydropeptidase (DHP) enzyme inhibitor activity.
摘要翻译：下式的化合物：其中R 1是C 2 -C 12直链或支链未取代的烷基; C1-C12直链或支链取代的烷基; C2-C12直链或支链单烯基; C2-C12直链或支链炔基; C 7 -C 20芳烷基，其中烷基链是直链或支链C 1 -C 8，芳基部分是C 6 -C 12; C4-C10环烷基烷基; C3-C7环烷基; 其中除了C 2 -C 12直链或支链未取代的烷基之外的R 1的这些值可以被一个或多个C 1 -C 4烷氧基，C 3 -C 6环烷氧基，C 3 -C 6环烷硫基，C 6 -C 12芳氧基，C 1 -C 4烷硫基， C6-C12芳硫基，C7-C10芳烷氧基，C7-C16芳烷硫基; R5为H或C1-C12直链或支链烷基; C2-C12直链或支链单烯基; C 7 -C 20芳烷基，其中烷基链是直链或支链C 1 -C 8，芳基部分是C 6 -C 12; 杂环烷基，其中烷基链是直链或支链C1-C8，杂环是5-6元，任选地与完全芳族的苯环稠合，含有1-2个氧，氮或硫作为杂原子; C4-C10环烷基烷基; C3-C7环烷基; 其中R 5的值可被卤素，羟基，羧基，C 1 -C 4烷氧基羰基，C 7 -C 16芳烷氧基羰基，C 3 -C 7环烷基，C 1 -C 4烷氧基，C 6 -C 12芳氧基，C 3 -C 6环烷氧基，C 3 -C 1-6环烷硫基，氨基，单或二-C 1 -C 8烷基氨基，硫代，C 1 -C 4烷硫基，C 6 -C 12芳硫基，C 7 -C 16芳烷硫基或基团-S-（CH 2）n CH（NH 2）COOH。这些化合物具有脱氢肽酶（DHP）酶抑制剂活性。

50. 发明授权

US4873235A Benzofused lactams as antihypertensives 失效
标题翻译：苯佐诺内酰胺作为抗高血压药
公开(公告)号：US4873235A
公开(公告)日：1989-10-10
申请号：US473792
申请日：1983-03-16
申请人： William H. Parsons , Arthur A. Patchett , Eugene D. Thorsett
发明人： William H. Parsons , Arthur A. Patchett , Eugene D. Thorsett
IPC分类号： A61K38/00 , C07K5/02
CPC分类号： C07K5/0222 , A61K38/00
摘要： Benzofused lactams of the formula: ##STR1## and their use as angiotensin converting enzyme inhibitors and antihypertensive agents are disclosed.
摘要翻译：公开了具有下式的苯并有用的内酰胺：其作为血管紧张素转换酶抑制剂和抗高血压药的用途。

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