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41. 发明授权

US06908935B2 Calcium receptor modulating agents 有权
标题翻译：钙受体调节剂
公开(公告)号：US06908935B2
公开(公告)日：2005-06-21
申请号：US10444946
申请日：2003-05-22
申请人： Michael G. Kelly , Shimin Xu , Ning Xi , Philip Miller , John F. Kincaid , Chiara Ghiron , Thomas Coulter
发明人： Michael G. Kelly , Shimin Xu , Ning Xi , Philip Miller , John F. Kincaid , Chiara Ghiron , Thomas Coulter
IPC分类号： A61K31/137 , A61K31/145 , A61K31/167 , A61K31/275 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/4045 , A61K31/417 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/426 , A61K31/4418 , A61K31/443 , A61K31/4439 , A61K31/4465 , A61K31/47 , A61K31/4965 , A61K31/50 , A61K31/505 , A61K31/52 , A61K31/5377 , A61P3/14 , A61P5/18 , A61P5/20 , A61P19/10 , C07B53/00 , C07C209/28 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/55 , C07C215/46 , C07C217/54 , C07C217/58 , C07C229/38 , C07C233/43 , C07C235/20 , C07C237/30 , C07C255/58 , C07C255/59 , C07C275/40 , C07C311/08 , C07C317/32 , C07D207/26 , C07D207/32 , C07D207/325 , C07D209/08 , C07D209/10 , C07D209/44 , C07D211/22 , C07D211/26 , C07D211/70 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/62 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/82 , C07D215/12 , C07D231/56 , C07D233/22 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D237/14 , C07D239/26 , C07D239/34 , C07D239/42 , C07D239/47 , C07D241/12 , C07D241/42 , C07D249/18 , C07D261/08 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D271/12 , C07D277/24 , C07D277/28 , C07D277/40 , C07D277/42 , C07D277/66 , C07D277/78 , C07D285/00 , C07D285/01 , C07D295/096 , C07D295/135 , C07D295/185 , C07D295/26 , C07D307/42 , C07D307/52 , C07D307/68 , C07D317/46 , C07D317/54 , C07D317/58 , C07D319/18 , C07D321/10 , C07D333/16 , C07D333/20 , C07D333/56 , C07D401/12 , C07D405/12 , C07D471/04 , C07D473/00 , C07D487/04
CPC分类号： C07C233/36 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/55 , C07C215/46 , C07C217/54 , C07C217/58 , C07C229/38 , C07C233/43 , C07C233/46 , C07C235/20 , C07C237/30 , C07C255/58 , C07C255/59 , C07C275/40 , C07C311/08 , C07C317/32 , C07C2601/02 , C07D207/26 , C07D207/27 , C07D207/325 , C07D209/08 , C07D209/10 , C07D209/44 , C07D211/22 , C07D211/70 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/75 , C07D213/82 , C07D215/12 , C07D215/14 , C07D231/56 , C07D233/22 , C07D235/06 , C07D235/10 , C07D235/12 , C07D237/08 , C07D237/14 , C07D239/26 , C07D239/34 , C07D239/42 , C07D241/12 , C07D241/42 , C07D249/18 , C07D261/08 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/08 , C07D271/10 , C07D271/12 , C07D277/24 , C07D277/28 , C07D277/40 , C07D277/42 , C07D277/66 , C07D285/01 , C07D295/096 , C07D295/135 , C07D295/185 , C07D295/26 , C07D307/42 , C07D307/52 , C07D307/68 , C07D317/46 , C07D317/54 , C07D319/18 , C07D321/10 , C07D333/16 , C07D333/20 , C07D333/56 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04
摘要： The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：本发明的化合物由以下一般结构或其药学上可接受的盐以及含有它们的组合物表示，其中变量在本文中定义，及其用于减少或抑制PTH分泌的用途，包括减少或抑制PTH分泌的方法，以及用于治疗或预防与骨疾病相关的疾病如骨质疏松症或与过度分泌的PTH相关的疾病如甲状旁腺功能亢进的方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

42. 发明授权

US06903216B2 Anthranilamides with heteroarylsulfonyl side chain, process of preparation, and use 有权
标题翻译：具有杂芳基磺酰侧链的邻氨基苯甲酰胺，制备方法和用途
公开(公告)号：US06903216B2
公开(公告)日：2005-06-07
申请号：US10166595
申请日：2002-06-12
申请人： Joachim Brendel , Thomas Böhme , Stefan Peukert , Heinz-Werner Kleemann
发明人： Joachim Brendel , Thomas Böhme , Stefan Peukert , Heinz-Werner Kleemann
IPC分类号： A61K31/42 , A61K31/4245 , A61K31/4402 , A61K31/47 , A61K31/472 , A61K31/497 , A61K45/06 , A61P9/06 , C07D213/70 , C07D215/36 , C07D217/02 , C07D261/10 , C07D271/12 , C07D333/34 , C07D401/12 , C07D405/12
CPC分类号： C07D261/10 , A61K31/47 , A61K45/06 , C07D215/36 , C07D217/02 , C07D271/12 , C07D333/34 , C07D401/12 , C07D405/12 , A61K2300/00
摘要： This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them. Compounds of formula I, in which R1 to R7 have the meanings stated in the claims, act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. They are therefore suitable as novel antiarrhythmic ingredients, such as for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutter.
摘要翻译：本发明包括具有杂芳基磺酰侧链的邻氨基苯甲酰胺，其制备方法，它们作为药物或诊断助剂的用途，以及含有它们的药物制剂。其中R 1至R 7具有权利要求中所述含义的式I化合物作用于Kv1.5钾通道并抑制在人心脏中心被称为超快速活化延迟整流剂的钾电流。因此，它们适合作为新的抗心律失常成分，例如用于治疗和预防心房心律失常，例如，心房颤动（AF）或心房扑动。

43. 发明申请

US20050043536A1 Sulfonamides 审中-公开
公开(公告)号：US20050043536A1
公开(公告)日：2005-02-24
申请号：US10477070
申请日：2002-05-07
申请人： Dashyant Dhanak , Timothy Gallagher , Steven Knight
发明人： Dashyant Dhanak , Timothy Gallagher , Steven Knight
IPC分类号： A61K31/18 , A61K31/381 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/12 , A61P15/10 , A61P19/02 , A61P19/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P31/04 , A61P43/00 , C07C311/21 , C07C311/29 , C07D333/34 , C07D333/72 , C07D207/48 , C07D213/62 , C07D215/20 , C07D271/12
CPC分类号： C07C311/21 , C07C311/29 , C07D333/34
摘要： The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

44. 发明申请

US20050020584A1 Benzamide derivatives as antagonists of orexin receptors 失效
标题翻译：苯甲酰胺衍生物作为食欲素受体的拮抗剂
公开(公告)号：US20050020584A1
公开(公告)日：2005-01-27
申请号：US10494011
申请日：2002-10-30
申请人： Wai Chan , Amanda Johns , Roderick Porter , Rachel Stead , Mythily Vimal
发明人： Wai Chan , Amanda Johns , Roderick Porter , Rachel Stead , Mythily Vimal
IPC分类号： A61K31/166 , A61K31/277 , A61K31/343 , A61K31/36 , A61K31/415 , A61K31/4192 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/47 , A61K31/472 , A61P3/00 , A61P3/04 , A61P3/10 , A61P5/02 , A61P5/06 , A61P5/10 , A61P7/00 , A61P7/04 , A61P9/00 , A61P9/10 , A61P11/00 , A61P15/10 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/28 , A61P43/00 , C07C233/73 , C07C233/76 , C07C233/77 , C07C233/78 , C07C233/87 , C07C235/46 , C07C235/48 , C07C235/84 , C07C255/50 , C07C255/57 , C07C317/14 , C07D215/48 , C07D215/50 , C07D217/26 , C07D231/14 , C07D249/06 , C07D271/06 , C07D271/12 , C07D277/20 , C07D277/56 , C07D277/62 , C07D285/14 , C07D307/79 , C07D317/50 , C07D317/68 , C07D279/12 , A61K31/165 , A61K31/401 , A61K31/421 , A61K31/495 , A61K31/537 , A61K31/54
CPC分类号： C07D271/06 , C07C233/73 , C07C233/77 , C07C233/87 , C07C235/46 , C07C235/84 , C07C255/57 , C07C2603/18 , C07D215/48 , C07D215/50 , C07D217/26 , C07D231/14 , C07D249/06 , C07D277/56 , C07D307/79 , C07D317/68
摘要： This invention relates to certain benzamide derivatives and their use as pharmaceuticals.
摘要翻译：本发明涉及某些苯甲酰胺衍生物及其作为药物的用途。

45. 发明申请

US20050004186A1 MEK inhibiting compounds 审中-公开
标题翻译： MEK抑制化合物
公开(公告)号：US20050004186A1
公开(公告)日：2005-01-06
申请号：US10725206
申请日：2003-12-01
申请人： Stephen Barrett , Cathlin Flamme , Michael Kaufman , Mark Plummer , Jessica Reed , Joseph Warmus , Lu-Yan Zhang
发明人： Stephen Barrett , Cathlin Flamme , Michael Kaufman , Mark Plummer , Jessica Reed , Joseph Warmus , Lu-Yan Zhang
IPC分类号： A61P29/00 , A61P35/00 , C07D249/08 , C07D249/14 , C07D271/10 , C07D271/113 , C07D285/12 , C07D285/135 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D285/14 , A61K31/4196 , A61K31/4245 , A61K31/433 , C07D271/12
CPC分类号： C07D249/08 , C07D271/10 , C07D271/113 , C07D285/135 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14
摘要： This invention provides substituted Phenyl-(2-[1,3,4]thiadiazol-2-yl-phenyl)-amine and (2-[1,3,4]Oxadiazol-2-yl-phenyl)phenyl-amine compounds which act as inhibitors of MAPK/ERK Kinase (“MEK”) enzymes and pharmaceutical compositions and methods for their use in immunomodulation and in the treatment and alleviation of inflammation, and proliferative diseases such as cancer and restenosis.
摘要翻译：本发明提供了取代的苯基 - （2- [1,3,4]噻二唑-2-基 - 苯基） - 胺和（2- [1,3,4]恶二唑-2-基 - 苯基）苯基 - 胺化合物，其中作为MAPK / ERK激酶（“MEK”）酶的抑制剂及其用于免疫调节和治疗和减轻炎症以及增殖性疾病如癌症和再狭窄的药物组合物和方法。

46. 发明授权

US06838484B2 Formulations comprising selective androgen receptor modulators 有权
标题翻译：包含选择性雄激素受体调节剂的制剂
公开(公告)号：US06838484B2
公开(公告)日：2005-01-04
申请号：US10270232
申请日：2002-10-15
申请人： Mitchell S. Steiner , Karen A. Veverka , James T. Dalton , Duane D. Miller , Yali He , Donghua Yin
发明人： Mitchell S. Steiner , Karen A. Veverka , James T. Dalton , Duane D. Miller , Yali He , Donghua Yin
IPC分类号： A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12 , G01N30/72 , G01N30/88 , G01N33/543 , G01N33/74 , A61K31/16
CPC分类号： A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D215/227 , C07D271/12 , G01N30/7233 , G01N33/5438 , G01N33/74 , G01N2030/8813
摘要： The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia,osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.
摘要翻译：本发明涉及包含新型雄激素受体靶向剂（ARTA）的药物组合物和制剂，其表现出雄激素受体的非甾体配体的雄激素和合成代谢活性。这些药剂定义了一种新的选择性雄激素受体调节剂（SARM）的化合物亚类，它们可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌癌症，子宫癌和卵巢癌; d）治疗和/或预防慢性肌肉消瘦; 和/或e）降低前列腺癌的发生率，停止或导致消退。本发明提供了包含选择性雄激素受体调节剂化合物以及药学上可接受的赋形剂的药物组合物。

47. 发明申请

US20040267015A1 Peptide deformylase inhibitors 审中-公开
标题翻译：肽变性酶抑制剂
公开(公告)号：US20040267015A1
公开(公告)日：2004-12-30
申请号：US10473104
申请日：2003-09-29
发明人： Ajita Bhat , Siegfried B. Christensen , James S. Frazee , Martha S. Head , Jack D. Leber , Mei Li
IPC分类号： C07D271/12 , C07D285/10 , C07D277/04 , C07C259/04 , C07D207/46
CPC分类号： C07C259/06 , C07C2601/02
摘要： PDF inhibitors and novel methods for their use are provided.

48. 发明申请

US20040235912A1 Peroxisome proliferator activated receptor alpha agonists 失效
标题翻译：过氧化物酶体增殖物激活受体α激动剂
公开(公告)号：US20040235912A1
公开(公告)日：2004-11-25
申请号：US10495204
申请日：2004-05-10
发明人： Richard Duane Johnston , Nathan Bryan Mantlo , Richard Craig Thompson
IPC分类号： C07D271/12 , A61K031/4245
CPC分类号： C07D271/113
摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, and C3-C6 cycloalkylaryl-C0-2-alkyl; W is O or S; X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom the linker may be replaced with O, NH or S; Y is C, O, S, NH or a single bond; E is C(R3)(R4)A or A. 1
摘要翻译：本发明涉及由以下结构式表示的化合物及其药学上可接受的盐，溶剂合物和水合物，R 1选自氢，取代或未取代的基团，所述基团选自C 1 -C 8烷基，芳基-C 0-4 - 烷基，杂芳基-C 0-4 - 烷基和C 3 -C 6环烷基芳基-C 0-2 - 烷基; W为O或S; X是任选取代的C1-C5亚烷基连接体，其中一个碳原子连接体可被O，NH或S取代; Y是C，O，S，NH或单键; E为C（R3）（R4）A或A.

49. 发明申请

US20040204461A1 1,2,4-oxadiazole benzoic acid compounds and their use for nonsense suppression and the treatment of disease 有权
标题翻译： 1,2,4-恶二唑苯甲酸化合物及其用于无味抑制和治疗疾病的用途
公开(公告)号：US20040204461A1
公开(公告)日：2004-10-14
申请号：US10822259
申请日：2004-04-09
发明人： Gary Mitchell Karp , Seongwoo Hwang , Guangming Chen , Neil Gregory Almstead
IPC分类号： C07D271/12 , A61K031/4245
CPC分类号： A61K31/4245 , A61K9/0053 , A61K9/12 , A61K9/48 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61K31/655 , A61K45/06 , A61P27/02 , C07D271/06 , C07D271/12 , C07D285/14 , C07D413/02 , C07D413/04 , C07D413/10
摘要： Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.
摘要翻译：公开了1,2,4-恶二唑苯甲酸衍生物，1,2,4-恶二唑苯甲酸衍生物的使用方法和药物组合物。所述方法包括治疗或预防通过调节过早翻译终止或无义介导的mRNA衰变而改善的疾病或改善与其相关的一种或多种症状的方法。

50. 发明申请

US20040106795A1 Peptide deformylase inhibitors 失效
公开(公告)号：US20040106795A1
公开(公告)日：2004-06-03
申请号：US10473060
申请日：2003-09-29
发明人： Ajita Bhat , Siegfried B. Christensen IV , James S. Frazee , Martha S. Head , Jack D. Leber , Mei Li
IPC分类号： C07D285/08 , C07D271/12 , C07D271/06 , C07D207/34 , C07D257/10
CPC分类号： C07D207/26 , C07C259/06 , C07D207/38 , C07D207/416 , C07D213/30 , C07D333/16
摘要： PDF inhibitors and novel methods for their use are provided.

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