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31. 发明授权

US5545734A Aryl and heteroaryl macrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的芳基和杂芳基大环内酯
公开(公告)号：US5545734A
公开(公告)日：1996-08-13
申请号：US328225
申请日：1994-10-25
申请人： Robert K. Baker , Gerard R. Kieczykowski , Hyun O. Ok , William H. Parsons , Kathleen M. Rupprecht
发明人： Robert K. Baker , Gerard R. Kieczykowski , Hyun O. Ok , William H. Parsons , Kathleen M. Rupprecht
IPC分类号： C07D498/18 , C07D498/16
CPC分类号： C07D498/18
摘要： Aryl and heteroaryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by olefination at C-27. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases, and illnesses.
摘要翻译：一般结构式I的芳基和杂芳基大环内酯：通过在C-27进行烯化从合适的前体制备。这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病，预防外来器官移植排斥和/或相关疾病，疾病和疾病。

32. 发明授权

US5349061A O-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的O-杂芳基，O-烷基杂芳基，O-烯基杂芳基和O-炔基杂芳基大环内酯
公开(公告)号：US5349061A
公开(公告)日：1994-09-20
申请号：US135200
申请日：1993-10-12
申请人： Peter J. Sinclair , Joung Goulet , Frederick Wong , Mark Goulet , William H. Parsons , Matthew J. Wyvratt
发明人： Peter J. Sinclair , Joung Goulet , Frederick Wong , Mark Goulet , William H. Parsons , Matthew J. Wyvratt
IPC分类号： A61K31/40 , A61K31/445 , A61K31/495 , A61K31/70 , A61P37/06 , C07D498/18 , C07H19/01 , A61K31/345 , C07D491/16
CPC分类号： C07H19/01
摘要： O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroaryl-macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
摘要翻译：通式I的O-杂芳基，O-烷基杂芳基，O-链烯基杂芳基和O-炔基杂芳基 - 大环内酯：通过C-3“和/或C的烷基化和/或芳基化从合适的前体制备 -4“。这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫疾病，感染性疾病，预防外来器官移植排斥和/或相关疾病，疾病和疾病。

33. 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。

34. 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。

35. 发明授权

US4684645A Benzofused lactams as cholecystokinin antagonists 失效
标题翻译：苯佐诺内酯作为胆囊收缩素拮抗剂
公开(公告)号：US4684645A
公开(公告)日：1987-08-04
申请号：US799049
申请日：1985-11-18
申请人： Raymond S. L. Chang , William H. Parsons
发明人： Raymond S. L. Chang , William H. Parsons
IPC分类号： C07D215/38 , A61K31/395 , A61K31/47 , A61K31/55 , A61K38/00 , A61P1/00 , A61P25/00 , A61P43/00 , C07D223/16 , C07D225/06 , C07D333/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07K5/02
CPC分类号： C07D223/16 , C07K5/0222 , A61K38/00
摘要： Benzofused lactams and their use as antagonists of cholecystokinin are disclosed.
摘要翻译：公开了苯并有用的内酰胺及其作为缩胆囊素拮抗剂的用途。

36. 发明授权

US4652641A Benzofused lactams useful as antihypertensive agents and as cholecystokinin antagonists 失效
标题翻译：苯并有用的内酰胺可用作抗高血压药和缩胆囊素拮抗剂
公开(公告)号：US4652641A
公开(公告)日：1987-03-24
申请号：US810118
申请日：1985-12-18
申请人： William H. Parsons
发明人： William H. Parsons
IPC分类号： C07D215/38 , C07D223/16 , C07D225/06 , C07D215/16 , C07D217/04
CPC分类号： C07D215/38 , C07D223/16 , C07D225/06
摘要： Compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of angiotensin I converting enzyme and are useful as antihypertensive agents and are also useful as cholecystokinin antagonists.
摘要翻译：下式的化合物及其药学上可接受的盐是血管紧张素I转化酶的抑制剂，可用作抗高血压药，也可用作缩胆囊素拮抗剂。

37. 发明授权

US4106168A Method and apparatus for assembling a ball cage of the type utilized in a motion transmitting remote control assembly 失效
标题翻译：用于组装运动发射遥控组件中使用的类型的球笼的方法和装置
公开(公告)号：US4106168A
公开(公告)日：1978-08-15
申请号：US670750
申请日：1976-03-26
申请人： William H. Parsons
发明人： William H. Parsons
IPC分类号： B23P15/00 , F16C1/20 , F16C1/28 , B21D53/12 , B21H1/12 , B23P21/00
CPC分类号： F16C1/20 , B23P15/003 , F16C1/28 , Y10T29/49691 , Y10T29/5137 , Y10T29/5191 , Y10T29/5198 , Y10T29/53104 , Y10T74/20444
摘要： A ball cage retainer of the type including a pair of coextensive strips having annular pocket portions defined by truncated angular flanges to define ball retaining pockets for rotatably retaining balls between the strips with the strips spot welded together and a method and apparatus for assembling such a ball cage. The ball cage is utilized in a conduit of a motion transmitting remote control assembly for facilitating the movement of a motion transmitting core element within the conduit. The cage is assembled by indexing a pair of metal ribbon-like strips successively through a plurality of stations by two sets of fixed and movable clamping assemblies. The pocket portions, and alignment notches adjacent the pocket portions, are simultaneously formed in each of the strips at a first station as the strips pass through the first station in parallel relationship to one another. One of the strips passes through a second station and balls are placed in each of the pocket portions of that strip. Thereafter the two strips are guided into coextensive abutting relationship with the coacting pocket portions defining the ball retaining pockets surrounding the balls. With the strips in abutting relationship with one another they pass through a third station where an aligning member engages the alignment notches in the two strips for longitudinally aligning the strips along the length of the strips having the ball retaining pocket therein adjacent which the strips are to be secured together by a welder which engages the strips for spot welding the strips together while the strips are maintained aligned with one another by the aligning member.
摘要翻译：一种球笼保持器，包括一对共同延伸条，其具有由截头角法兰限定的环形袋部分，以限定用于可旋转地保持条之间的球的球保持袋，其中带有点焊接在一起的条带以及用于组装这样的球的方法和装置笼。球笼用于运动传递遥控组件的导管中，以促进运动传递芯元件在导管内的移动。通过两组固定和可移动的夹紧组件，通过多个工位连续地分配一对金属带状条来组装笼。随着条带彼此平行的关系通过第一站时，在第一站处，每个条带中同时形成袋状部分和邻近袋部分的对准槽口。其中一条穿过第二站，球放置在该条的每个口袋部分中。此后，两个条带被引导与限定围绕球的球保持袋的共同作用袋部分的共同邻接关系。当条带彼此邻接关系时，它们穿过第三工位，其中对准构件与两个条带中的对准凹口接合，用于沿着具有球保持袋的条带的长度纵向对准条带，所述条带邻近于条带通过焊接机固定在一起，焊接机将条带接合在一起，同时通过对准部件保持条彼此对准。

38. 发明授权

US4062251A Motion transmitting remote control assembly 失效
标题翻译：运动遥控装置
公开(公告)号：US4062251A
公开(公告)日：1977-12-13
申请号：US670749
申请日：1976-03-26
申请人： William H. Parsons
发明人： William H. Parsons
IPC分类号： F16C1/20 , F16C1/10 , F16C31/00
CPC分类号： F16C1/28 , F16C1/20 , Y10T29/49691 , Y10T74/20444
摘要： A ball cage retainer of the type including a pair of coextensive strips having annular pocket portions defined by truncated angular flanges to define ball retaining pockets for rotatably retaining balls between the strips with the strips spot welded together and a method and apparatus for assembling such a ball cage. The ball cage is utilized in a conduit of a motion transmitting remote control assembly for facilitating the movement of a motion transmitting core element within the conduit. The cage is assembled by indexing a pair of metal ribbon-like strips successively through a plurality of stations by two sets of fixed and movable clamping assemblies. The pocket portions, and alignment notches adjacent the pocket portions, are simultaneously formed in each of the strips at a first station as the strips pass through the first station in parallel relationship to one another. One of the strips passes through a second station and balls are placed in each of the pocket portions of that strip. Thereafter the two strips are guided into coextensive abutting relationship with the coacting pocket portions defining the ball retaining pockets surrounding the balls. With the strips in abutting relationship with one another they pass through a third station where an aligning member engages the alignment notches in the two strips for longitudinally aligning the strips along the length of the strips having the ball retaining pocket therein adjacent which the strips are to be secured together by a welder which engages the strips for spot welding the strips together while the strips are maintained aligned with one another by the aligning member.
摘要翻译：一种球笼保持器，包括一对共同延伸条，其具有由截头角法兰限定的环形袋部分，以限定用于可旋转地保持条之间的球的球保持袋，其中带有点焊接在一起的条带以及用于组装这样的球的方法和装置笼。球笼用于运动传递遥控组件的导管中，以促进运动传递芯元件在导管内的移动。通过两组固定和可移动的夹紧组件，通过多个工位连续地分配一对金属带状条来组装笼。随着条带彼此平行的关系通过第一站时，在第一站处，每个条带中同时形成袋状部分和邻近袋部分的对准槽口。其中一条穿过第二站，球放置在该条的每个口袋部分中。此后，两个条带被引导与限定围绕球的球保持袋的共同作用袋部分的共同邻接关系。当条带彼此邻接关系时，它们穿过第三工位，其中对准构件与两个条带中的对准凹口接合，用于沿着具有球保持袋的条带的长度纵向对准条带，所述条带邻近于条带通过焊接机固定在一起，焊接机将条带接合在一起，同时通过对准部件保持条彼此对准。

39. 发明申请

US20110190364A1 BENZIMIDAZOLE MODULATORS OF VR1 审中-公开
标题翻译： VR1的苯并咪唑调节剂
公开(公告)号：US20110190364A1
公开(公告)日：2011-08-04
申请号：US13084718
申请日：2011-04-12
申请人： Mark R. Player , Scott L. Dax , William H. Parsons , Michael Richard Brandt , Raul R. Calvo , Sharmila Patel , Jian Liu , Wing S. Cheung , Michele C. Jetter , Yu-Kai Lee , Mark A. Youngman , Wenxi Pan , Kenneth M. Wells , Derek A. Beauchamp
发明人： Mark R. Player , Scott L. Dax , William H. Parsons , Michael Richard Brandt , Raul R. Calvo , Sharmila Patel , Jian Liu , Wing S. Cheung , Michele C. Jetter , Yu-Kai Lee , Mark A. Youngman , Wenxi Pan , Kenneth M. Wells , Derek A. Beauchamp
IPC分类号： A61K31/4184 , A61P29/00
CPC分类号： C07D401/06 , C07D235/08 , C07D403/06
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。

40. 发明申请

US20080280873A1 Biaryl Substituted Pyrazinones as Sodium Channel Blockers 审中-公开
标题翻译：二芳基取代的吡嗪酮作为钠通道阻断剂
公开(公告)号：US20080280873A1
公开(公告)日：2008-11-13
申请号：US10594367
申请日：2005-03-25
申请人： Jun Liang , Prasun K. Chakravarty , Deborah E. Pan , William H. Parsons , Pengcheng P. Shao , Feng Yee , Bishan Zhou
发明人： Jun Liang , Prasun K. Chakravarty , Deborah E. Pan , William H. Parsons , Pengcheng P. Shao , Feng Yee , Bishan Zhou
IPC分类号： A61K31/4965 , C07D241/24
CPC分类号： C07D241/24 , B05B1/02 , B05B1/14 , B05B1/34 , B65D83/20 , C07D241/18 , C07D403/06 , C07D405/04 , C07D413/06
摘要： Biaryl substituted pyrazinone 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, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, 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表示的二芳基取代的吡嗪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疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，肠易激综合征，抑郁症，焦虑，多发性硬化和双相性精神障碍，包括单独或与一种或多种其它治疗活性化合物组合施用有效量的本发明化合物。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。

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