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61. 发明申请

US20080114002A1 Substituted Acids for the Treatment of Respiratory Diseases 有权
标题翻译：用于治疗呼吸系统疾病的替代酸
公开(公告)号：US20080114002A1
公开(公告)日：2008-05-15
申请号：US11571707
申请日：2005-07-06
申请人： Roger Bonnert , Stephen Thom , Anil Patel , Timothy Luker
发明人： Roger Bonnert , Stephen Thom , Anil Patel , Timothy Luker
IPC分类号： A61K31/196 , A61K31/192 , A61K31/4245 , A61K31/44 , A61K31/505 , A61P11/06 , C07C229/40 , C07C255/57 , C07D213/55 , C07D239/26 , C07D271/06
CPC分类号： C07D213/30 , C07C229/18 , C07C255/54 , C07C311/08 , C07C317/22 , C07C317/36 , C07C323/52 , C07C323/65 , C07D239/26 , C07D271/06
摘要： The invention relates to substituted acids of formula (I), where T, W, X, Y, Z, R1 and R2 as defined in the claims, as useful pharmaceutical compounds for treating asthma and rhinitis, pharmaceutical compositions containing them, and a processes for their preparation.
摘要翻译：本发明涉及如权利要求中所定义的式（I）的取代的酸，其中T，W，X，Y，Z，R 1和R 2如有用用于治疗哮喘和鼻炎的药物化合物，含有它们的药物组合物及其制备方法。

62. 发明申请

US20070105916A1 Amphiphilic pyridinium compounds, method of making and use thereof 有权
标题翻译：两亲性吡啶鎓化合物，其制备方法和用途
公开(公告)号：US20070105916A1
公开(公告)日：2007-05-10
申请号：US10560590
申请日：2004-06-28
申请人： Harvey Pollard , Kenneth Jacobson
发明人： Harvey Pollard , Kenneth Jacobson
IPC分类号： C07D213/55 , A61K31/44
CPC分类号： C07D213/20 , C07D213/30 , C07D213/80 , C07D231/12 , C07D233/60 , C07D295/088 , C07D401/12 , C07D409/12
摘要： The present invention is directed to the amphiphilic pyridinium compounds, such as for suppressing IL-8 secretion and production. The present invention further provides methods of making and using such compounds for the treatment of the IL-8 related diseases, such as cystic fibrosis.
摘要翻译：本发明涉及两性吡啶鎓化合物，例如用于抑制IL-8分泌和产生。本发明还提供制备和使用这些化合物治疗IL-8相关疾病如囊性纤维化的方法。

63. 发明申请

US20060252107A1 Compositions and methods for diagnosing and treating retinal diseases 审中-公开
标题翻译：用于诊断和治疗视网膜疾病的组合物和方法
公开(公告)号：US20060252107A1
公开(公告)日：2006-11-09
申请号：US11361027
申请日：2006-02-22
申请人： Ryo Kubota , Krzysztof Palczewski , Anna Gall
发明人： Ryo Kubota , Krzysztof Palczewski , Anna Gall
IPC分类号： G01N33/53 , C07K16/18 , C07K14/47 , C07D213/55 , C07D213/20 , C12N5/06
CPC分类号： A61K39/0007 , A61K2039/6031 , C07D213/20 , C07D213/38 , C07D213/50 , C07D213/56 , C07K16/44
摘要： The present invention relates generally to the preparation and use of retinoid N-retinylidene-N-retinyl-ethanolamine (A2E) conjugated to a carrier polypeptide and to the preparation and use of antibodies that bind specifically to A2E. The invention relates to the use of A2E conjugates as immunogens or vaccines and to the use of A2E specific antibodies for treatment of ophthalmic diseases. Provided herein are methods for enhancing retinal neuronal cell survival, including photoreceptor cell survival, using antibodies that specifically bind to A2E or by inducing an immune response using an A2E immunoconjugate. Enhancing survival of photoreceptor cells or decreasing accumulation of A2E in the eye using the A2E immunoconjugates or A2E specific antibodies is useful for treatment of ophthalmic diseases such as macular degeneration.
摘要翻译：本发明一般涉及与载体多肽缀合的类视黄醇N-亚视黄基-N-视黄醇 - 乙醇胺（A2E）的制备和用途，以及制备和使用与A2E特异性结合的抗体。本发明涉及使用A2E缀合物作为免疫原或疫苗，以及使用A2E特异性抗体治疗眼科疾病。本文提供了使用特异性结合A2E的抗体或通过使用A2E免疫缀合物诱导免疫应答来增强视网膜神经元细胞存活的方法，包括感光细胞存活。使用A2E免疫缀合物或A2E特异性抗体提高感光细胞的存活或减少A2E在眼中的积累，可用于治疗眼部疾病如黄斑变性。

64. 发明申请

US20060106070A1 Novel pyridine-based metal chelators as antiviral agents 审中-公开
标题翻译：新型吡啶类金属螯合剂作为抗病毒剂
公开(公告)号：US20060106070A1
公开(公告)日：2006-05-18
申请号：US11260816
申请日：2005-10-27
申请人： Raghavan Rajagopalan , John Babu
发明人： Raghavan Rajagopalan , John Babu
IPC分类号： C07D213/84 , C07D213/63 , C07D213/55
CPC分类号： C07D213/69 , C07D213/38
摘要： This invention relates to novel pyridine-based divalent metal ion chelating ligands of Formula I, wherein A or B are independently —R6R7, or —CH(R8)CH(R9). R1 to R9 are various substituents selected to optimize the physicochemical and biological properties such as enzyme binding, tissue penetration, lipophilicity, toxicity, bioavailability, and pharmacokinetics. The compounds of the present invention are useful for inhibiting the activity of viral enzymes responsible for the proliferation of human immunodeficiency virus (HIV).
摘要翻译：本发明涉及式I的新颖的基于吡啶的二价金属离子螯合配体，其中A或B独立地为-R 6，或-CH（R 0 CH（R 9）9。 R 1至R 9是选择用于优化物理化学和生物学特性如酶结合，组织渗透，亲油性，毒性，生物利用度和药代动力学的各种取代基。本发明的化合物可用于抑制负责人免疫缺陷病毒（HIV）增殖的病毒酶的活性。

65. 发明申请

US20060100252A1 Aminoalcohol derivatives 失效
标题翻译：氨基醇衍生物
公开(公告)号：US20060100252A1
公开(公告)日：2006-05-11
申请号：US11304632
申请日：2005-12-16
申请人： Kouji Hattori , Yasuyo Tomishima , Masashi Imanishi
发明人： Kouji Hattori , Yasuyo Tomishima , Masashi Imanishi
IPC分类号： C07D213/55 , A61K31/44 , A61K31/195 , C07C229/34
CPC分类号： C07D295/135 , C07C215/52 , C07C217/60 , C07C217/92 , C07C229/36 , C07C229/38 , C07C255/58 , C07C271/22 , C07C323/32 , C07C323/63 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/38 , C07D295/155 , Y02P20/55
摘要： The present invention relates to a compound formula [I]: wherein ect., X is bond, —CH2—, etc., Y is bond, —O—(CH2)n— (in which n is 1, 2, 3 or 4), etc., Z is cyano, tetrazolyl, etc., R1 is hydrogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, R4 is hydrogen or lower alkyl, R5 and R8 are each independently hydrogen, halogen, hydroxy, lower alkyl, etc., R6 is hydrogen, lower alkyl, etc., R9 is hydrogen or lower alkyl, and i is 1 or 2, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.
摘要翻译：本发明涉及化合物式[I]：其中，X是键，-CH 2 - 等，Y是键，-O-（CH 2 CH 2）（其中n为1,2,3或4）等，Z为氰基，四唑基等，R 1为氢，低级烷基等，R 2是氢或氨基保护基，R 3是氢或低级烷基，R 4是氢或低级烷基，R 5和R 8各自独立地为氢，卤素，羟基，低级烷基等，R 6为氢，低级烷基等，R 9是氢或低级烷基，i是1或2，或其盐。本发明的化合物[I]及其药学上可接受的盐可用于预防和/或治疗呼吸窘迫症或尿失禁。

66. 发明申请

US20050137212A1 Hppars activators 失效
标题翻译： Hppars激活器
公开(公告)号：US20050137212A1
公开(公告)日：2005-06-23
申请号：US10505333
申请日：2003-02-25
申请人： Rodolfo Cadilla , Brad Henke , Millard Lambert III , Guangcheng Liu , Jennifer Smith
发明人： Rodolfo Cadilla , Brad Henke , Millard Lambert III , Guangcheng Liu , Jennifer Smith
IPC分类号： C07D237/22 , A61K31/192 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/454 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/02 , A61P9/10 , A61P17/00 , A61P17/06 , A61P29/00 , A61P43/00 , C07C215/52 , C07C217/60 , C07C279/08 , C07C335/12 , C07D213/38 , C07D213/55 , C07D213/61 , C07D213/74 , C07D237/20 , C07D239/42 , C07D241/20 , C07D261/20 , C07D263/58 , C07D271/06 , C07D271/07 , C07D275/02 , C07D277/20 , C07D277/42 , C07D277/82 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14
CPC分类号： C07D213/74 , C07C217/60 , C07C335/12 , C07D213/53 , C07D213/61 , C07D237/20 , C07D239/42 , C07D241/20 , C07D263/58 , C07D271/06 , C07D271/07 , C07D277/42 , C07D277/82 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14
摘要： Compounds of formula (1) or a pharmaceutically acceptable salt, solvate, acid isostere, or hydrolyzable ester thereof, are disclosed. Methods of making and using the compounds are also disclosed. In particular methods for treating diseases or conditions associated with one or more of human PPAR alpha, gamma, or delta (“hPPARs”) comprising administration of a therapeutically effective amount of a compound of formula (1), are disclosed.
摘要翻译：公开了式（1）的化合物或其药学上可接受的盐，溶剂合物，酸等排体或其可水解的酯。还公开了制备和使用化合物的方法。具体涉及用于治疗与一种或多种人类PPARα，γ或δ（“hPPAR”）相关的疾病或病症的方法，包括施用治疗有效量的式（1）化合物。

67. 发明申请

US20050124668A1 Amino acids with affinity for the alpha2delta-protein 审中-公开
标题翻译：对α2delta蛋白具有亲和力的氨基酸
公开(公告)号：US20050124668A1
公开(公告)日：2005-06-09
申请号：US10949908
申请日：2004-09-24
申请人： Christopher Deur , Kevin Henegar , Christine Kolz , Jonathan Miller , Augastine Osuma , Mark Plummer , Brian Samas , Jacob Schwarz , Andrew Thorpe , David Wustrow
发明人： Christopher Deur , Kevin Henegar , Christine Kolz , Jonathan Miller , Augastine Osuma , Mark Plummer , Brian Samas , Jacob Schwarz , Andrew Thorpe , David Wustrow
IPC分类号： A61P23/00 , C07C227/32 , C07C229/08 , C07C229/28 , C07C229/34 , C07D263/26 , A61K31/44 , A61K31/198 , A61K31/277 , C07D213/55
CPC分类号： C07C229/08 , C07B2200/07 , C07C227/32 , C07C229/28 , C07C229/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D263/26 , Y02P20/582
摘要： Certain β-amino acids that bind to the alpha-2-delta (α2δ) subunit of a calcium channel are disclosed. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders.
摘要翻译：公开了结合钙通道的α-2-δ（α2delta）亚基的某些β-氨基酸。这些化合物及其药学上可接受的盐可用于治疗各种精神病，疼痛和其它疾病。

68. 发明申请

US20050107433A1 Process for production of optically active compounds 失效
标题翻译：光学活性化合物的制造方法
公开(公告)号：US20050107433A1
公开(公告)日：2005-05-19
申请号：US10506309
申请日：2003-03-05
申请人： Toru Yamano , Naohiro Taya
发明人： Toru Yamano , Naohiro Taya
IPC分类号： C07D233/64 , C07B53/00 , C07B61/00 , C07D213/55 , C07D233/54 , C07D43/02 , A61K31/4025 , A61K31/454
CPC分类号： C07D233/64 , C07D213/55
摘要： The present invention provides a method for producing an optically active β-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.
摘要翻译：本发明提供一种制备由以下通式表示的光学活性β-羟基酯化合物的方法：其中R 1表示任选取代的烃基等，R 2 O >表示不同于R 1的含氮杂环基，其由以下通式表示：其中该环可以被取代等，R 3表示任选地取代烃基等，R 4和R 5表示相同或不同的氢原子，卤素原子等，符号“*”表示光学活性中心，其包括在cinchona生物碱等存在下反应，由通式表示的化合物：其中R 1和R 2如上定义与下列通式表示的化合物：其中R 3，R 4和R 5如上所定义，X是卤代基 n原子。

69. 发明申请

US20050090555A1 Compound for the treatment of metabolic disorders 有权
标题翻译：化合物用于治疗代谢紊乱
公开(公告)号：US20050090555A1
公开(公告)日：2005-04-28
申请号：US11005449
申请日：2004-12-06
申请人： Shalini Sharma , Reid von Borstel
发明人： Shalini Sharma , Reid von Borstel
IPC分类号： A61K31/00 , A61K31/16 , A61K31/165 , A61K31/192 , A61K31/198 , A61K31/216 , A61K31/235 , A61K31/27 , A61K31/381 , A61K31/41 , A61K31/4196 , A61K31/4402 , A61K31/445 , A61K31/535 , A61K31/54 , A61P1/16 , A61P3/04 , A61P3/10 , A61P7/00 , A61P9/10 , A61P9/12 , A61P13/12 , A61P17/02 , A61P25/00 , A61P27/12 , C07C59/54 , C07C59/68 , C07C59/90 , C07C69/738 , C07C217/22 , C07C233/47 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C259/06 , C07C323/47 , C07C323/52 , C07C323/59 , C07C323/60 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/22 , A61K31/195 , C07C229/44
CPC分类号： C07B41/12 , A01N37/10 , A61K31/165 , A61K31/192 , A61K31/216 , A61K31/235 , A61K31/41 , A61K31/4196 , A61K31/44 , A61K31/445 , A61K31/535 , A61K31/54 , C07C59/68 , C07C59/90 , C07C67/47 , C07C69/738 , C07C209/68 , C07C217/22 , C07C233/31 , C07C233/47 , C07C235/78 , C07C235/84 , C07C259/06 , C07C323/52 , C07C323/59 , C07C2601/02 , C07C2601/04 , C07C2602/04 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/24 , Y10S514/866
摘要： Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
摘要翻译：公开了可用于治疗各种代谢紊乱（例如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化）的化合物。

70. 发明申请

US20050075367A1 Ester compound and medicinal use thereof 失效
标题翻译：酯化合物及其药用
公开(公告)号：US20050075367A1
公开(公告)日：2005-04-07
申请号：US10492831
申请日：2003-02-28
申请人： Atsushi Hagiwara , Yasuhiro Ohe , Naoya Odani , Shizue Watanabe , Taku Ikenogami , Takashi Kawai , Kenya Madono , Toshio Taniguchi
发明人： Atsushi Hagiwara , Yasuhiro Ohe , Naoya Odani , Shizue Watanabe , Taku Ikenogami , Takashi Kawai , Kenya Madono , Toshio Taniguchi
IPC分类号： A61K31/215 , A61K31/216 , A61K31/235 , A61K31/24 , A61K31/245 , A61K31/277 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/404 , A61K31/4184 , A61K31/423 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/4453 , A61K31/4468 , A61K31/5375 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , C07C69/732 , C07C69/76 , C07C69/773 , C07C69/88 , C07C233/81 , C07C235/06 , C07C235/14 , C07C235/16 , C07C235/26 , C07C235/30 , C07C235/34 , C07C235/40 , C07C235/64 , C07C235/84 , C07C237/42 , C07C311/04 , C07D205/12 , C07D207/09 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/08 , C07D211/58 , C07D213/55 , C07D213/61 , C07D213/82 , C07D235/06 , C07D263/58 , C07D277/30 , C07D277/56 , C07D295/135 , C07D295/192 , C07D333/24 , C07D211/06 , A61K31/445
CPC分类号： C07D207/404 , A61K31/215 , A61K31/216 , A61K31/235 , A61K31/24 , A61K31/245 , A61K31/277 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/404 , A61K31/4184 , A61K31/423 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/4453 , A61K31/4468 , A61K31/5375 , C07C69/732 , C07C69/76 , C07C69/88 , C07C233/81 , C07C235/06 , C07C235/14 , C07C235/16 , C07C235/26 , C07C235/30 , C07C235/34 , C07C235/40 , C07C235/64 , C07C235/84 , C07C237/42 , C07C311/04 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D205/12 , C07D207/09 , C07D207/16 , C07D209/08 , C07D211/58 , C07D213/55 , C07D213/61 , C07D213/82 , C07D235/06 , C07D263/58 , C07D277/30 , C07D277/56 , C07D295/135 , C07D295/192 , C07D333/24
摘要： A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1″) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6alkyl or C1-C6alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R8 and R9 are each independently hydrogen atom, C1-C6alkyl, —CON(R18)(R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.
摘要翻译：作为高脂血症的新型治疗剂，其为由式（1“）表示的酯化合物（其中R 1和R 2各自为氢原子或任选取代的芳基等; X为-COO-或 -CON（R 10） - ; R 3和R 4各自为氢原子，C 1 -C 6烷基或C 1 -C 6烷氧基等; R 5，R 6和R 7为每个氢原子，C 1 -C 6烷基或C 1 -C 6烷氧基等; R 8和R 9各自独立地为氢原子，C 1 -C 6烷基，-CON（R 18）（R 19）或-COO（R 20）等;环A，环B和环C各自独立地为芳基或杂环残基等; Alk 1和Alk 2各自独立地为烷二基等; l 和m为0或1〜3的整数）或其前药，或其药学上可接受的盐。治疗剂选择性地抑制小肠中的MTP，因此不会引起脂肪肝的副作用。

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