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1. 发明申请

US20080234370A1 Calcilytic Compounds 审中-公开
标题翻译：钙化合物
公开(公告)号：US20080234370A1
公开(公告)日：2008-09-25
申请号：US10587771
申请日：2005-02-04
申请人： Robert W. Marquis , Joshi M. Ramanjulu
发明人： Robert W. Marquis , Joshi M. Ramanjulu
IPC分类号： A61K31/235 , C07C69/76 , A61K31/135 , C07C211/01 , A61P19/02 , A61P1/02 , A61P19/10
CPC分类号： C07C255/57 , C07C217/36
摘要： Novel calcilytic compounds and methods of using them are provided.
摘要翻译：提供新的钙质化合物及其使用方法。

2. 发明授权

US07132422B2 Sodium channel modulators 有权
公开(公告)号：US07132422B2
公开(公告)日：2006-11-07
申请号：US11052504
申请日：2005-02-04
申请人： Seok-Ki Choi , Paul R. Fatheree , David C. Green , Daniel Marquess
发明人： Seok-Ki Choi , Paul R. Fatheree , David C. Green , Daniel Marquess
IPC分类号： A61K31/5375 , A61K31/40 , C07D265/30 , C07D207/04
CPC分类号： C07D213/30 , A61K31/135 , A61K31/401 , A61K31/4152 , A61K31/417 , A61K31/4184 , A61K31/4402 , A61K31/4465 , A61K31/5375 , C07C217/08 , C07C217/30 , C07C217/36 , C07C217/76 , C07C217/84 , C07C255/54 , C07C2601/18 , C07C2602/10 , C07D207/09 , C07D211/26 , C07D213/38 , C07D213/65 , C07D215/20 , C07D233/56 , C07D233/64 , C07D235/06 , C07D295/13 , C07D317/54 , C07D333/16
摘要： The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).

3. 发明申请

US20040063760A1 Sodium channel modulatiors 有权
标题翻译：钠通道调节剂
公开(公告)号：US20040063760A1
公开(公告)日：2004-04-01
申请号：US10659931
申请日：2003-09-11
发明人： Seok-Ki Choi , Paul R. Fatheree , David C. Green , Daniel Marquess
IPC分类号： A61K031/445 , A61K031/40
CPC分类号： C07D213/30 , A61K31/135 , A61K31/401 , A61K31/4152 , A61K31/417 , A61K31/4184 , A61K31/4402 , A61K31/4465 , A61K31/5375 , C07C217/08 , C07C217/30 , C07C217/36 , C07C217/76 , C07C217/84 , C07C255/54 , C07C2601/18 , C07C2602/10 , C07D207/09 , C07D211/26 , C07D213/38 , C07D213/65 , C07D215/20 , C07D233/56 , C07D233/64 , C07D235/06 , C07D295/13 , C07D317/54 , C07D333/16
摘要： The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).
摘要翻译：本发明提供了钠通道调节化合物，其可用于治疗与钠通道活性相关的疾病或病症，例如神经性疼痛。本发明还提供包含本发明化合物的药物组合物，以及包括向哺乳动物（例如人）施用此类化合物或盐的治疗方法。

4. 发明授权

US06518450B2 Guaiacoxypropanolamines with alpha/beta adrenergic blocking activity 失效
标题翻译： Guaiacoxypropanolamines具有α/β肾上腺素能阻滞活性
公开(公告)号：US06518450B2
公开(公告)日：2003-02-11
申请号：US09740754
申请日：2000-12-20
申请人： Ing-Jun Chen
发明人： Ing-Jun Chen
IPC分类号： C07C22900
CPC分类号： C07C217/34 , C07C217/36 , C07C233/18
摘要： The present invention reveals a novel structure of guaiacoxypropanolamines shown in formula I: The composition comprising formula I acts as active intergant and pharmaceutical acceptable vehicle. The composition by perfect administration routes in the mammal when given potential &agr;/&bgr;-adrenergic blocking, is selective for emergency hypertension.
摘要翻译：本发明揭示了式I所示的愈创木酚胺的新结构：包含式I的组合物作为活性中间体和药物可接受的载体。当给予潜在的α/β-肾上腺素能阻断时，哺乳动物完美给药途径的组合物对于紧急高血压是有选择性的。

5. 发明授权

US4829086A Soft .beta.-adrenergic blocking agents 失效
标题翻译：软β-肾上腺素能阻滞剂
公开(公告)号：US4829086A
公开(公告)日：1989-05-09
申请号：US922462
申请日：1986-10-23
申请人： Nicholas S. Bodor
发明人： Nicholas S. Bodor
IPC分类号： C07C217/36
CPC分类号： C07C217/36 , C07C2101/14 , C07C2101/18 , C07C2102/42 , C07C2103/74
摘要： New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.
摘要翻译：可用于治疗或预防心血管疾病和治疗青光眼的新型软β-肾上腺素能阻断剂具有式（I）其中n为0至10的整数; R是C6-C12环烷基-C1H2p-，C6-C18多环烷基-C1H2p + 13，C6-C18多环烯基-C1H2p-或C6C12环烯基-C1H2p-（其中p是0,1,2或3），或与相邻的 “IMAGE”组代表各种其他复杂的酯基; R1是C1-C7烷基; 并且Ar是含有至少一个芳香核的二价基团。还描述了相应的药学上可接受的酸加成盐。

6. 发明授权

US07560586B2 Acid and ester compounds and methods of using the same 有权
标题翻译：酸和酯化合物及其使用方法
公开(公告)号：US07560586B2
公开(公告)日：2009-07-14
申请号：US10508893
申请日：2003-03-26
申请人： Scott K. Thompson , Lara S. Kallander , Chun Ma , Joseph Marino , Dennis Lee
发明人： Scott K. Thompson , Lara S. Kallander , Chun Ma , Joseph Marino , Dennis Lee
IPC分类号： C07C229/00
CPC分类号： C07D213/38 , C07B2200/07 , C07C45/515 , C07C47/24 , C07C217/18 , C07C217/22 , C07C217/36 , C07C217/58 , C07C2601/08
摘要： Disclosed is a compound of having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.
摘要翻译：公开了具有下式的化合物：其药学上可接受的盐或溶剂合物和含有该化合物的药物组合物，其中结构变量如本文所定义。本发明的化合物，盐和溶剂化物可用作LXR激动剂。

7. 发明授权

US07226950B2 Sodium channel modulators 有权
标题翻译：钠通道调节剂
公开(公告)号：US07226950B2
公开(公告)日：2007-06-05
申请号：US11500078
申请日：2006-08-07
申请人： Seok-Ki Choi , Paul R. Fatheree , David C. Green , Daniel Marquess
发明人： Seok-Ki Choi , Paul R. Fatheree , David C. Green , Daniel Marquess
IPC分类号： A61K31/135 , C07C211/03
CPC分类号： C07D213/30 , A61K31/135 , A61K31/401 , A61K31/4152 , A61K31/417 , A61K31/4184 , A61K31/4402 , A61K31/4465 , A61K31/5375 , C07C217/08 , C07C217/30 , C07C217/36 , C07C217/76 , C07C217/84 , C07C255/54 , C07C2601/18 , C07C2602/10 , C07D207/09 , C07D211/26 , C07D213/38 , C07D213/65 , C07D215/20 , C07D233/56 , C07D233/64 , C07D235/06 , C07D295/13 , C07D317/54 , C07D333/16
摘要： The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).
摘要翻译：本发明提供了钠通道调节化合物，其可用于治疗与钠通道活性相关的疾病或病症，例如神经性疼痛。本发明还提供包含本发明化合物的药物组合物，以及包括向哺乳动物（例如人）施用此类化合物或盐的治疗方法。

8. 发明申请

US20060276467A1 Sodium channel modulators 有权
公开(公告)号：US20060276467A1
公开(公告)日：2006-12-07
申请号：US11500078
申请日：2006-08-07
申请人： Seok-Ki Choi , Paul Fatheree , David Green , Daniel Marquess
发明人： Seok-Ki Choi , Paul Fatheree , David Green , Daniel Marquess
IPC分类号： A61K31/5377 , A61K31/445 , A61K31/40 , C07D207/04 , C07D211/20 , A61K31/138
CPC分类号： C07D213/30 , A61K31/135 , A61K31/401 , A61K31/4152 , A61K31/417 , A61K31/4184 , A61K31/4402 , A61K31/4465 , A61K31/5375 , C07C217/08 , C07C217/30 , C07C217/36 , C07C217/76 , C07C217/84 , C07C255/54 , C07C2601/18 , C07C2602/10 , C07D207/09 , C07D211/26 , C07D213/38 , C07D213/65 , C07D215/20 , C07D233/56 , C07D233/64 , C07D235/06 , C07D295/13 , C07D317/54 , C07D333/16
摘要： The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).

9. 发明申请

US20030065039A1 Biologically active 1,3-bis-aromatic-prop-2-en-1-ones, 1,3-bis-aromatic-propan-1-ones, and 1,3-bis-aromatic-prop-2-yn-1-ones 审中-公开
标题翻译：生物活性的1,3-双 - 芳族 - 丙-2-烯-1-酮，1,3-双 - 芳族 - 丙-1-酮和1,3-双 - 芳基 - 丙-2-炔-1-酮 -那些
公开(公告)号：US20030065039A1
公开(公告)日：2003-04-03
申请号：US10062208
申请日：2002-01-31
申请人： Statens Serum Institute
发明人： Arsalan Kharazmi , Soren Brogger Christensen , Simon Feldbaek Nielsen
IPC分类号： A61K031/12
CPC分类号： C07C255/40 , A61K31/12 , A61K31/136 , A61K31/277 , C07C45/00 , C07C45/41 , C07C45/455 , C07C45/67 , C07C45/673 , C07C45/74 , C07C49/813 , C07C49/84 , C07C205/45 , C07C217/22 , C07C217/36 , C07C225/16 , C07C225/22 , C07C233/33 , Y02A50/409 , C07C47/565 , C07C47/575
摘要： The invention relates to the use of 1,3-bis-aromatic-prop-2-en-1-ones (chalcones), 1,3-bis-aromatic-propan-1-ones (dihydrochalcones), and 1,3-bis-aromatic-prop-2-yn-1-ones for the preparation of pharmaceutical compositions for the treatment or prophylaxis of a number of serious diseases including i) conditions relating to harmful effects of inflammatory cytokines, ii) conditions involving infection by Helicobacter species, iii) conditions involving infection by viruses, iv) neoplastic disorders, and v) conditions caused by microorganisms or parasites. The invention also relates to novel chalcones and dihydrochalcones (especially alkoxy substituted variants) having advantageous substitution patterns with respect to their effect as drug substances, and to methods of preparing them, as well as to pharmaceutical compositions comprising the novel chalcones. Moreover, the present invention relates to a method for the isolation of Leishmania fumarate reductase, QSAR methodologies for selecting potent compounds for the above-mentioned purposes.
摘要翻译：本发明涉及1,3-双芳族 - 丙-2-烯-1-酮（查耳酮），1,3-双芳族 - 丙-1-酮（二氢查耳酮）和1,3-二 - 用于制备用于治疗或预防许多严重疾病的药物组合物的双芳族 - 丙-2-炔-1-酮，包括i）与炎性细胞因子的有害作用有关的病症，ii）涉及幽门螺杆菌感染的病症，iii）涉及病毒感染的病症，iv）肿瘤性疾病，以及v）由微生物或寄生虫引起的病症。本发明还涉及具有相对于其作为药物物质的效果的有利取代模式的新型查耳酮和二氢查耳酮（特别是烷氧基取代的变体）及其制备方法，以及包含新颖的查尔酮的药物组合物。此外，本发明涉及用于分离富马酸利什曼原虫还原酶的方法，用于选择上述目的的有效化合物的QSAR方法。

10. 发明授权

US5254595A Aryloxypropanolaminotetralins, a process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：丙烯酰氧基丙醇氨基四氢化萘，其制备方法和含有它们的药物组合物
公开(公告)号：US5254595A
公开(公告)日：1993-10-19
申请号：US818513
申请日：1992-01-09
申请人： Umberto Guzzi , Marco Baroni , Sergio Boveri , Luciano Manara , Alberto Bianchetti
发明人： Umberto Guzzi , Marco Baroni , Sergio Boveri , Luciano Manara , Alberto Bianchetti
IPC分类号： C07C217/30 , C07C217/32 , C07C217/34 , C07C217/36 , C07C233/25 , C07C255/54 , C07D209/08 , C07D209/12 , C07D209/34 , C07D209/42 , C07D209/86 , C07D215/04 , C07D215/20 , C07D215/22 , C07D215/227 , C07D215/26 , C07D217/04 , C07D231/22 , C07D231/32 , C07D235/26 , C07D241/42 , C07D257/04 , C07D261/20 , C07D263/56 , C07D263/57 , C07D275/04 , C07D277/22 , C07D277/34 , C07D277/66 , C07D285/06 , C07D285/10 , C07D285/14 , C07D307/79 , C07D307/85 , C07D307/88 , C07D309/40 , C07D311/16 , C07D311/64 , C07D311/72 , C07D311/76 , C07D311/82 , C07D311/86 , C07D319/18 , C07D321/10 , C07D321/12 , C07D333/08 , C07D333/38 , C07D333/54 , C07D335/06 , C07D471/04 , C07D493/04 , C07D495/04 , C07C237/02 , A61K31/135 , A61K31/165 , C07C215/56
CPC分类号： C07C255/54 , C07C217/30 , C07C217/32 , C07C217/34 , C07C217/36 , C07C233/25 , C07D209/08 , C07D209/12 , C07D209/34 , C07D209/42 , C07D209/86 , C07D215/04 , C07D215/20 , C07D215/22 , C07D215/227 , C07D215/26 , C07D217/04 , C07D231/22 , C07D231/32 , C07D235/26 , C07D241/42 , C07D257/04 , C07D261/20 , C07D263/57 , C07D275/04 , C07D277/22 , C07D277/34 , C07D277/66 , C07D285/06 , C07D285/10 , C07D285/14 , C07D307/79 , C07D307/85 , C07D307/88 , C07D309/40 , C07D311/16 , C07D311/64 , C07D311/72 , C07D311/76 , C07D311/82 , C07D311/86 , C07D319/18 , C07D321/10 , C07D321/12 , C07D333/08 , C07D333/38 , C07D333/54 , C07D335/06 , C07D471/04 , C07D493/04 , C07D495/04 , C07C2102/08 , C07C2102/10 , C07C2103/18 , C07C2103/88
摘要： Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.
摘要翻译：描述了具有式（ⅰ）其中R为氢，羟基或甲氧基且具有光学活性或无活性形式的任选取代的芳族或杂芳族基团的式（ⅰ）的β-拮抗剂活性的丙烯酰氧基丙醇氨基十氢化萘及其酸加成盐。还描述了其制备方法和含有式（i）化合物或其药学上可接受的酸加成盐的药物组合物。

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