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81. 发明授权

US07241765B2 Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues 失效
标题翻译：黑色素浓缩激素受体配体：取代的1-苄基-4-芳基哌嗪类似物
公开(公告)号：US07241765B2
公开(公告)日：2007-07-10
申请号：US11436099
申请日：2006-05-17
申请人： Alan J. Hutchison , Linda M. Gustavson , John M. Peterson , Dario Doller , Timothy M. Caldwell , Taeyoung Yoon , Wallace C. Pringle , Rajagopal Bakthavatchalam , Yiping Shen , Cheryl K. Steenstra , Helen Yin , Robert W. DeSimone , Xiao-shu He
发明人： Alan J. Hutchison , Linda M. Gustavson , John M. Peterson , Dario Doller , Timothy M. Caldwell , Taeyoung Yoon , Wallace C. Pringle , Rajagopal Bakthavatchalam , Yiping Shen , Cheryl K. Steenstra , Helen Yin , Robert W. DeSimone , Xiao-shu He
IPC分类号： A61K31/495 , C07D295/096 , A61K31/451
CPC分类号： C07D513/04 , C07D209/86 , C07D211/52 , C07D213/64 , C07D213/74 , C07D215/12 , C07D215/20 , C07D243/08 , C07D295/096 , C07D295/108 , C07D311/18 , C07D317/58 , C07D401/12 , C07D471/04 , C07D487/04 , C07D487/08
摘要： Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要翻译：提供能够调节MCH受体活性的黑色素浓缩激素受体配体（特别是1-苄基-4-芳基哌嗪，1-苄基-4-芳基哌啶和相关化合物）。这样的配体可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗人，驯养的伴侣动物和家畜中的各种代谢，喂养和性障碍。还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。

82. 发明授权

US07211685B2 Calcium receptor antagonists 失效
标题翻译：钙受体拮抗剂
公开(公告)号：US07211685B2
公开(公告)日：2007-05-01
申请号：US10986296
申请日：2004-11-12
申请人： Yuko Shinagawa , Takeo Katsushima , Takashi Nakagawa
发明人： Yuko Shinagawa , Takeo Katsushima , Takashi Nakagawa
IPC分类号： C07C63/36 , C07C205/04 , C07C271/10
CPC分类号： C07D213/30 , C07B2200/07 , C07C217/28 , C07C217/60 , C07C217/76 , C07C229/38 , C07C233/25 , C07C235/42 , C07C235/60 , C07C237/30 , C07C255/54 , C07C311/21 , C07C311/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D277/24 , C07D307/42 , C07D317/58 , C07D333/16 , C07D333/56
摘要： A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided. The compound of the present invention is useful as a therapeutic drug of diseases accompanied by abnormal calcium homeostasis, or osteoporosis, hypoparathyreosis, osteosarcoma, periodontal disease, bone fracture, steoarthrosis, chronic rheumatoid arthritis, Paget's disease, humoral hypercalcemia, autosomal dominant hypocalcemia and the like. In addition, an intermediate for the compound is provided.
摘要翻译：其中R 1为式（I）的化合物为任选取代的芳基或任选取代的杂芳基; R 2是任选取代的C 1-6烷基，C 3-7环烷基等; R 3是氢原子，C 1-6烷基，羟基等; R 4是氢原子，C 1-6烷基等; R 5和R 6各自为C 1-6烷基等; R 7是任选取代的芳基或任选取代的杂芳基; X 1，X 2和X 3各自为C 1-6亚烷基等; 和X 4和X 5各自为单键，亚甲基等，其盐，其溶剂合物或其前药，以及含有化合物，特别是钙受体拮抗剂和骨质疏松症的治疗剂。本发明的化合物可用作伴有异常钙稳态或骨质疏松症，hypoparathyreosis，骨肉瘤，牙周病，骨折，骨关节炎，慢性类风湿性关节炎，佩吉特氏病，体液性高钙血症，常染色体显性低钙血症的疾病的治疗药物喜欢。此外，还提供了化合物的中间体。

83. 发明申请

US20070078139A1 Phosphodiesterase 4 inhibitors 审中-公开
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US20070078139A1
公开(公告)日：2007-04-05
申请号：US11602283
申请日：2006-11-21
申请人： Richard Schumacher , William Brubaker , Michael De Vivo , Hans-Jurgen Hess , Allen Hopper , Ashok Tehim , Ruiping Liu , Axel Unterbeck
发明人： Richard Schumacher , William Brubaker , Michael De Vivo , Hans-Jurgen Hess , Allen Hopper , Ashok Tehim , Ruiping Liu , Axel Unterbeck
IPC分类号： A61K31/505 , A61K31/4965 , A61K31/44 , A61K31/426 , A61K31/47 , A61K31/381 , A61K31/34 , A61K31/137
CPC分类号： C07D213/74 , A61K31/137 , A61K31/16 , A61K31/34 , A61K31/381 , A61K31/426 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/4965 , A61K31/505 , C07C217/92 , C07C229/60 , C07D211/26 , C07D213/38 , C07D213/61 , C07D213/80 , C07D215/12 , C07D217/22 , C07D241/12 , C07D277/28 , C07D307/20 , C07D307/52 , C07D317/58 , C07D333/20 , C07D401/12 , C07D405/12 , C07D405/14 , C07F7/1804
摘要： PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3and R4 are as defined herein.
摘要翻译：通过新化合物，例如N-取代的苯胺和二苯胺类似物来实现PDE4的抑制。本发明的化合物是式I的化合物：其中R 1，R 2，R 3和R 4， >如本文所定义。

84. 发明申请

US20070037795A1 Benzylamine analogues 失效
公开(公告)号：US20070037795A1
公开(公告)日：2007-02-15
申请号：US11583499
申请日：2006-10-19
申请人： Kazuo Koyama , Shinji Marumoto , Narihiro Toda , Hiroshi Kogen , Keiko Suzuki
发明人： Kazuo Koyama , Shinji Marumoto , Narihiro Toda , Hiroshi Kogen , Keiko Suzuki
IPC分类号： C07D333/22 , C07D215/38 , C07D277/00 , C07D275/02 , A61K31/55 , C07D263/34 , C07D261/02 , A61K31/50 , A61K31/4965
CPC分类号： C07C219/30 , C07C271/44 , C07C323/20 , C07C323/25 , C07C333/04 , C07D213/64 , C07D213/68 , C07D215/20 , C07D317/58 , C07D333/38
摘要： A compound of the formula (1): wherein R1 is a C1-C6 alkyl, an amino, a (C1-C6 alkyl)amino, a di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and are a hydrogen or a C1-C6 alkyl; Arom is an unsubstituted or substituted aryl or an unsubstituted or substituted heteroaryl; wherein the substituted aryl is substituted at 1 to 5 positions and the substituted heteroaryl is substituted at 1 to 3 positions; wherein the heteroaryl is furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; and wherein the substituents of the substituted aryl and of the substituted heteroaryl are independently halogen, C1-C6 alkyl, halogeno C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C3 alkylenedioxy, C1-C7 alkanoyl, C2-C7 alkyloxycarbonyl, amino, C1-C7 alkanoylamino, hydroxyl, mercapto, cyano, nitro or carboxyl; A is an ethylene or propylene; Ra is a hydrogen, a C1-C6 alkyl or a C2-C6 alkenyl; E is a single bond, an oxygen, a sulfur or —NR4—, wherein R4 is a hydrogen or a C1-C7 alkanoyl; X1 and X2 are the same or different and are an oxygen or a sulfur, or a pharmacologically acceptable salt or ester thereof.

85. 发明申请

US20070037793A1 Benzylamine analogues 失效
公开(公告)号：US20070037793A1
公开(公告)日：2007-02-15
申请号：US11583404
申请日：2006-10-19
申请人： Kazuo Koyama , Shinji Marumoto , Narihiro Toda , Hiroshi Kogen , Keiko Suzuki
发明人： Kazuo Koyama , Shinji Marumoto , Narihiro Toda , Hiroshi Kogen , Keiko Suzuki
IPC分类号： A61K31/55 , C07D223/16
CPC分类号： C07C219/30 , C07C271/44 , C07C323/20 , C07C323/25 , C07C333/04 , C07D213/64 , C07D213/68 , C07D215/20 , C07D317/58 , C07D333/38
摘要： A compound of the formula (I): wherein R1 is a C1-C6 alkyl group, an amino group, a (C1-C6 alkyl)amino group, a di(C1-C6 alkyl)amino group or a nitrogen-containing saturated heterocyclic group; R3 is a hydrogen atom or a C1-C6 alkyl group; Arom is an unsubstituted or substituted aryl group or an unsubstituted or substituted heteroaryl group; wherein the substituted aryl group is substituted at 1 to 5 positions and the substituted heteroaryl group is substituted at 1 to 3 positions; and wherein the substituents of the aryl group and of the heteroaryl group are independently selected from the group consisting of halogen atom, C1-C6 alkyl, halogeno C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C3 alkylenedioxy, C1-C7 alkanoyl, C2-C7 alkyloxycarbonyl, amino, C1-C7 alkanoylamino, hydroxyl, mercapto, cyano, nitro and carboxyl; A is a C1-C6 alkylene group; Ra together with R2 is a C2-C3 alkylene group containing a double bond; E is a single bond, an oxygen atom, a sulfur atom or a group of the formula: —NR4—, wherein R4 is a hydrogen atom or a C1-C7 alkanoyl group; X1 and X2 are the same or different and are an oxygen atom or a sulfur atom, or a pharmacologically acceptable salt or ester thereof.

86. 发明授权

US07169817B2 Bis-aromatic alkanols 有权
标题翻译：双芳族链烷醇
公开(公告)号：US07169817B2
公开(公告)日：2007-01-30
申请号：US10445967
申请日：2003-05-27
申请人： Shifeng Pan , Nathanael S. Gray , Wenqui Gao , Klaus Hinterding , Sophie Lefebvre , Yuan Mi , Peter Nussbaumer , Wei Wang , Federic Zecri , Fan Yi , Lawrence Blas Perez , Kenneth Richad la Montagne , Peter Ettmayer
发明人： Shifeng Pan , Nathanael S. Gray , Wenqui Gao , Klaus Hinterding , Sophie Lefebvre , Yuan Mi , Peter Nussbaumer , Wei Wang , Federic Zecri , Fan Yi , Lawrence Blas Perez , Kenneth Richad la Montagne , Peter Ettmayer
IPC分类号： C07C211/03 , C07C251/32 , A61K31/15 , A61K31/137
CPC分类号： C07D263/57 , C07C215/28 , C07C215/46 , C07C217/54 , C07C237/30 , C07C251/48 , C07C255/13 , C07C255/43 , C07C255/58 , C07C311/08 , C07C2601/02 , C07C2601/08 , C07D261/08 , C07D317/58 , C07D333/20 , C07F9/094
摘要： The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them. Compounds according to the present invention are based upon the chemical formula: wherein the substituents have the values mentioned herein.
摘要翻译：本发明涉及联苯衍生物，其制备方法及其用途和含有它们的药物组合物。根据本发明的化合物基于以下化学式：其中取代基具有本文提及的值。

87. 发明授权

US07148225B2 Substituted biaryl amides as C5A receptor modulators 失效
标题翻译：取代的联芳酰胺作为C5A受体调节剂
公开(公告)号：US07148225B2
公开(公告)日：2006-12-12
申请号：US10994224
申请日：2004-11-19
申请人： Yang Gao , Alan J. Hutchinson , Wallace C. Pringle , Taeyoung Yoon , He Zhao
发明人： Yang Gao , Alan J. Hutchinson , Wallace C. Pringle , Taeyoung Yoon , He Zhao
IPC分类号： A61K31/34 , A61K31/40 , A61K31/495 , C07D207/10 , C07D241/04
CPC分类号： C07D209/08 , C07C233/65 , C07C233/66 , C07C233/73 , C07C235/62 , C07C237/30 , C07C2602/08 , C07D207/325 , C07D231/56 , C07D317/58 , C07D333/24 , C07D405/12
摘要： Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies
摘要翻译：提供式I的取代的联芳酰胺。这些化合物是可用于在体内或体外调节C5a受体活性的配体，并且特别可用于治疗与人类，驯养的伴侣动物和家畜中的病理性C5a受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法

88. 发明申请

US20060229298A1 Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues 失效
公开(公告)号：US20060229298A1
公开(公告)日：2006-10-12
申请号：US11436099
申请日：2006-05-17
申请人： Alan Hutchison , Linda Gustavson , John Peterson , Dario Dollar , Timothy Caldwell , Taeyoung Yoon , Wallace Pringle , Rajagopal Bakthavatchalam , Yiping Shen , Cheryl Steenstra , Helen Yin , Robert DeSimone , Xiao-shu He
发明人： Alan Hutchison , Linda Gustavson , John Peterson , Dario Dollar , Timothy Caldwell , Taeyoung Yoon , Wallace Pringle , Rajagopal Bakthavatchalam , Yiping Shen , Cheryl Steenstra , Helen Yin , Robert DeSimone , Xiao-shu He
IPC分类号： A61K31/496 , A61K31/551 , A61K31/495 , C07D403/02
CPC分类号： C07D513/04 , C07D209/86 , C07D211/52 , C07D213/64 , C07D213/74 , C07D215/12 , C07D215/20 , C07D243/08 , C07D295/096 , C07D295/108 , C07D311/18 , C07D317/58 , C07D401/12 , C07D471/04 , C07D487/04 , C07D487/08
摘要： Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

89. 发明申请

US20060178414A1 Substituted biaryl amides as C5a receptor modulators 失效
标题翻译：取代的联芳酰胺作为C5a受体调节剂
公开(公告)号：US20060178414A1
公开(公告)日：2006-08-10
申请号：US11324729
申请日：2006-01-03
申请人： Yang Gao , Andrew Thurkauf , He Zhao
发明人： Yang Gao , Andrew Thurkauf , He Zhao
IPC分类号： A61K31/4196 , A61K31/4164 , A61K31/41 , A61K31/415
CPC分类号： C07D209/08 , C07C233/65 , C07C233/66 , C07C233/73 , C07C235/62 , C07C237/30 , C07C2602/08 , C07D207/325 , C07D231/56 , C07D317/58 , C07D333/24 , C07D405/12
摘要： Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供式I的取代的联芳酰胺。这些化合物是可用于在体内或体外调节C5a受体活性的配体，并且特别可用于治疗与人类，驯养的伴侣动物和家畜中的病理性C5a受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

90. 发明申请

US20060173044A1 Substituted propargylamines 审中-公开
标题翻译：取代炔丙胺
公开(公告)号：US20060173044A1
公开(公告)日：2006-08-03
申请号：US11391077
申请日：2006-03-29
申请人： Harald Jakobi , Susan Cramp , Joachim Dickhaut , Stephen Lindell , Jorg Tiebes , Maria Canales , Daniela Jans , Waltraud Hempel , Reed Royalty , Susan McComb , Maria-Theresia Thonessen , Jutta Waibel , Vincent Salgado
发明人： Harald Jakobi , Susan Cramp , Joachim Dickhaut , Stephen Lindell , Jorg Tiebes , Maria Canales , Daniela Jans , Waltraud Hempel , Reed Royalty , Susan McComb , Maria-Theresia Thonessen , Jutta Waibel , Vincent Salgado
IPC分类号： A01N43/40
CPC分类号： C07D239/26 , A01N43/40 , A01N43/42 , A01N43/46 , A01N43/54 , A01N43/60 , A01N43/78 , A01N43/84 , A01N43/90 , A01N47/16 , A61K31/445 , C07D209/02 , C07D211/14 , C07D211/18 , C07D211/54 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/70 , C07D211/74 , C07D213/36 , C07D213/61 , C07D213/85 , C07D215/06 , C07D217/04 , C07D239/30 , C07D239/38 , C07D277/28 , C07D295/03 , C07D295/073 , C07D295/096 , C07D295/116 , C07D295/155 , C07D295/185 , C07D317/58 , C07D333/20 , C07D333/22 , C07D333/28 , C07D333/44 , C07D409/04 , C07D451/02 , C07D491/10
摘要： The present invention relates to the use of substituted aryl- and heteroarylpropargylamines of the formula (I) where a) R1 is heteroaryl or aryl, unsubstituted or mono- or polysubstituted by identical or different radicals, b) A is a group CR4R5 or C═O, where R4 is hydrogen, halogen or alkyl; R5 is hydrogen, halogen or a substituted or unsubstituted hydrocarbon radical; c) R2 and R3 together with the nitrogen atom to which they are attached form N-heteroaryl or N-heterocyclyl, unsubstituted or mono- or polysubstituted by identical or different radicals, if appropriate also as N-oxide or salt, as pesticide against arthropods and helminths for protecting plants and animals.
摘要翻译：本发明涉及式（I）的取代的芳基 - 和杂芳基炔丙基胺的用途，其中a）R 1是未取代的或被相同或不同基团单取代或多取代的杂芳基或芳基，b） A是一个基团，其中R 4是氢，卤素或烷基; R 4是氢， R 5是氢，卤素或取代或未取代的烃基; c）R 2和R 3与它们所连接的氮原子一起形成N-杂芳基或N-杂环基，未被取代或被相同或不同的单取代或多取代自由基，如果适用，还可以作为N-氧化物或盐，作为防治节肢动物和蠕虫的农药用于保护植物和动物。

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