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61. 发明申请

US20030203923A1 Method of inhibiting neurotrophin-receptor binding 审中-公开
标题翻译：抑制神经营养因子受体结合的方法
公开(公告)号：US20030203923A1
公开(公告)日：2003-10-30
申请号：US10205601
申请日：2002-07-26
发明人： Gregory M. Ross , Egor L. Shamovsky , Sandra Marone , Donald F. Weaver , Richard J. Riopelle
IPC分类号： A61K031/7052 , A61K031/519
CPC分类号： C07D221/14 , A61K31/00 , A61K31/473 , A61K31/4745
摘要： The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.
摘要翻译：本发明涉及抑制神经生长因子与p75 常见的神经营养因子受体的结合的组合物及其使用方法。在一个实施方案中，抑制神经生长因子与p75 的结合的化合物特别包括当与神经生长因子结合时，包含以下至少两种：（1）位于与Lys相互作用的第一电负性原子或官能团 <34>神经生长因子; （2）定位为与神经生长因子的Lys 95相互作用的第二电负性原子或官能团; （3）定位为与神经生长因子的Lys <88>相互作用的第三电负性原子或官能团; （4）定位为与神经生长因子的Lys 32相互作用的第四电负性原子或官能团; 和（5）疏水部分，其与由神经生长因子的Ile 31，Phe 101和Phe 86形成的疏水区相互作用。

62. 发明申请

US20030199459A1 Macrolides with antibacterial activity 有权
标题翻译：具有抗菌活性的大环内酯类
公开(公告)号：US20030199459A1
公开(公告)日：2003-10-23
申请号：US10362526
申请日：2003-02-21
发明人： Peter Angehrn , Daniel Hunziker , Pierre-Charles Wyss
IPC分类号： A61K031/7052 , A61K031/7048 , C07H017/08
CPC分类号： C07H17/08 , A61K9/0031 , A61K9/02 , A61K9/2018 , A61K9/4866
摘要： The invention provides new macrolides antibiotics of formula (I) with improved biological properties and improved stability formula (I): wherein R1 is hydrogen, cyano, nullS(L)mR2, nullS(O)(L)mR2, or nullS(O)2(L)mR2; L represents null(CH2)nnull or null(CH2)nZ(CH2)nnullnull-; m is 0 or 1; n is 1, 2, 3, or 4; nnull is 0, 1, 2, 3, or 4; Z is O, S or NH; R2 is hydrogen, alkyl, heterocyclyl or aryl; which heterocyclyl and the aryl groups may be further substituted; * indicates a chiral center which is in the (R) or (S) form and pharmaceutically acceptable acid addition salts or in vivo cleavable esters thereof. 1
摘要翻译：本发明提供具有改进的生物学性质和改进的稳定性式（I）的式（I）的新型大环内酯类抗生素：其中R 1是氢，氰基，-S（L）m R 2，-S（O））mR 2或-S（O）2（L）m R 2; L表示 - （CH 2）n - 或 - （CH 2）n Z（CH 2）n' - ; m为0或1; n为1,2,3或4; n'为0,1,2,3或4; Z是O，S或NH; R2是氢，烷基，杂环基或芳基; 哪些杂环基和芳基可以被进一步取代; *表示具有（R）或（S）形式的手性中心及其药学上可接受的酸加成盐或其体内可切割酯。

63. 发明申请

US20030199439A1 Compositions of alpha3beta4 receptor antagonists and opioid agonist analgesics 审中-公开
标题翻译： α3beta4受体拮抗剂和阿片样物质激动剂镇痛药的组合物
公开(公告)号：US20030199439A1
公开(公告)日：2003-10-23
申请号：US10127359
申请日：2002-04-22
发明人： David Lew Simon
IPC分类号： A61K038/33 , A61K031/7052 , A61K031/485 , A61K031/445 , A61K031/192
CPC分类号： A61K45/06 , A61K31/192 , A61K31/445 , A61K31/485 , A61K31/7052 , A61K38/33 , A61K2300/00
摘要： A pharmaceutical composition comprising an opioid agonist analgesic and an null3null4 nicotinic receptor antagonist effective to separate the brain-derived wanting of the opioid from the analgesic or anti-diarrhea effect of the opioid agonist.
摘要翻译：一种药物组合物，其包含阿片样物质激动剂镇痛药和α3β4烟碱受体拮抗剂，其有效地将阿片类药物的脑源性欲望与阿片样物质激动剂的镇痛作用或抗腹泻作用分离。

64. 发明申请

US20030176390A1 Methods of treating insulin resistance syndrome and diabetes 审中-公开
标题翻译：治疗胰岛素抵抗综合征和糖尿病的方法
公开(公告)号：US20030176390A1
公开(公告)日：2003-09-18
申请号：US10145207
申请日：2002-05-14
发明人： Andreas Herling , Gerhard Jaehne , Martin P. Maguire , Alfred P. Spada , Michael R. Myers , Yong Mi Choi-Sledeski , Heinz W. Pauls , William R. Ewing
IPC分类号： A61K031/7076 , A61K031/52 , A61K031/7052 , A61K031/4745
CPC分类号： A61K31/52
摘要： This invention is directed to methods of treating insulin resistance syndrome and diabetes in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a compound derived from adenosine and analogues thereof, or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable prodrug thereof, an N-oxide thereof, a hydrate thereof or a solvate thereof, or a pharmaceutical composition comprising such compound.
摘要翻译：本发明涉及在有需要的患者中治疗胰岛素抵抗综合征和糖尿病的方法，包括向所述患者施用药学有效量的衍生自腺苷及其类似物的化合物或其药学上可接受的盐，药学上可接受的前药其N-氧化物，其水合物或其溶剂化物，或包含该化合物的药物组合物。

65. 发明申请

US20030171307A1 Azalide antibiotic compositions 审中-公开
公开(公告)号：US20030171307A1
公开(公告)日：2003-09-11
申请号：US10205074
申请日：2002-07-25
申请人： Pfizer Inc.
发明人： Wayne A. Boettner
IPC分类号： A61K031/7052
CPC分类号： A61K9/0014 , A61K9/0019 , A61K31/7052 , A61K47/10 , A61K47/12
摘要： Antibiotic compositions comprising an equilibrium mixture of azalide isomers, water, and one or more acids, and methods for preparing such compositions, are disclosed. The antibiotic compositions can be advantageously stabilized by adding one or more water-miscible co-solvents. In a preferred embodiment, the one or more co-solvents is propylene glycol.

66. 发明申请

US20030130206A1 Medical devices incorporating deuterated rapamycin for controlled delivery thereof 失效
标题翻译：结合氘化雷帕霉素的医疗装置用于其控制递送
公开(公告)号：US20030130206A1
公开(公告)日：2003-07-10
申请号：US10301504
申请日：2002-11-20
发明人： Joseph Koziak , Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
IPC分类号： A61K031/7052 , A61K031/4745 , A61M031/00
CPC分类号： C07D498/18 , A61L29/16 , A61L31/16 , A61L2300/416 , A61L2300/602
摘要： Deuterated rapaymcin can be controllably introduced target locations within the patient's body by using an implantable medical device having a structure incorporated with a therapeutic agent comprising a deuterated rapamycin. Representative deuterated rapamycins include epi-7-deuteromthyl rapamycin, 7,43-d6 rapamycin, 7-deuteromethyl rapamycin and 31,42-d2-rapamycin and isomers thereof, and mixtures thereof. The deuterated rapamycin can also be glycosylated.
摘要翻译：通过使用具有结合有包含氘代雷帕霉素的治疗剂的结构的可植入医疗装置，可以可控地将目标位置引入患者体内。代表性的氘代雷帕霉素包括表7-降血磷酸雷帕霉素，7,43-d6雷帕霉素，7-氘代甲基雷帕霉素和31,42-d2-雷帕霉素及其异构体及其混合物。氘代雷帕霉素也可以糖基化。

67. 发明申请

US20030092640A1 Azalide antibiotic compositions 审中-公开
标题翻译：阿片类抗生素组合物
公开(公告)号：US20030092640A1
公开(公告)日：2003-05-15
申请号：US10160235
申请日：2002-05-30
申请人： Pfizer Inc.
发明人： Wayne Alan Boettner
IPC分类号： A61K031/7052
CPC分类号： A61K31/7052 , A61K9/0019 , A61K31/395 , A61K47/10 , A61K47/12
摘要： Aqueous antibiotic compositions comprising a mixture of an azalide compound, propylene glycol, and one or more acids, and methods for preparing such compositions, are disclosed.
摘要翻译：公开了包含氮杂化合物，丙二醇和一种或多种酸的混合物的水性抗生素组合物，以及制备这种组合物的方法。

68. 发明申请

US20030092608A1 Pharmaceutical composition for inhibiting the metastasis or preventing the recurrence of malignant tumor 审中-公开
标题翻译：用于抑制转移或预防恶性肿瘤复发的药物组合物
公开(公告)号：US20030092608A1
公开(公告)日：2003-05-15
申请号：US10224475
申请日：2002-08-21
发明人： Takayuki Kawaguchi , Satoshi Okuno , Toshiro Yano
IPC分类号： A61K038/14 , C07K009/00 , A61K031/7052
CPC分类号： A61K47/61 , A61K47/65
摘要： A pharmaceutical composition for inhibiting the metastasis or preventing the recurrence of a malignant tumor, which comprises as the active ingredient a polysaccharide derivative comprising a polysaccharide having a carboxyl group bound to an active substance having an anti-tumor activity via an amino acid or a peptide consisting of 2 to 8 amino acids which are the same or different, or a salt thereof.
摘要翻译：一种用于抑制转移或预防恶性肿瘤复发的药物组合物，其包含作为活性成分的多糖衍生物，其包含通过氨基酸或肽与具有抗肿瘤活性的活性物质结合的羧基的多糖由相同或不同的2至8个氨基酸组成，或其盐。

69. 发明申请

US20030053981A1 Combinations of bile acid sequestrant(s) and sterol absorption inhibitor(s) and treatments for vascular indications 审中-公开
标题翻译：胆汁酸螯合剂和甾体吸收抑制剂的组合以及血管适应症的治疗
公开(公告)号：US20030053981A1
公开(公告)日：2003-03-20
申请号：US10057534
申请日：2002-01-25
申请人： Schering Corporation
发明人： Harry R. Davis , Teddy Kosoglou
IPC分类号： A61K031/74 , A61K031/7052 , A61K031/655 , A61K031/397
CPC分类号： A61K45/06 , A61K31/337 , A61K31/397 , A61K31/455 , A61K31/655 , A61K31/7052 , A61K31/74 , A61K2300/00
摘要： The present invention provides compositions, therapeutic combinations and methods including: (a) at least one bile acid sequestrant; and (b) at least one substituted azetidinone or substituted null-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.
摘要翻译：本发明提供组合物，治疗组合和方法，包括：（a）至少一种胆汁酸螯合剂; 和（b）至少一种取代的氮杂环丁酮或取代的β-内酰胺甾醇吸收抑制剂，其可用于治疗血管疾病，糖尿病，肥胖症和降低甾醇的血浆水平。

70. 发明申请

US20020197320A1 Composition and method for rectal delivery of a lincosamide antibiotic drug 审中-公开
标题翻译：用于直肠递送林肯素抗生素药物的组合物和方法
公开(公告)号：US20020197320A1
公开(公告)日：2002-12-26
申请号：US10072492
申请日：2002-02-05
发明人： Lorraine E. Pena , Phil B. Bowman , Robert S. Chao , Carolyn V. Pesheck , Clayton W. Jacobsen
IPC分类号： A61K031/7052 , A61K009/14
CPC分类号： A61K9/02 , A61K31/7056
摘要： A suppository composition and method for rectal administration of a lincosamide antibacterial drug, such as clindamycin, lincomycin, or pirlimycin, is disclosed. The composition is a rectal suppository containing an antimicrobially effective amount of the lincosamide in particulate form dispersed in a Hard Fat suppository base, preferably a Hard Fat NF suppository base. The most preferred suppository compositions of the present invention have long term storage stability, while maintaining effectiveness against bacterial infections.
摘要翻译：公开了用于直肠给药林可酰胺抗菌药物的栓剂组合物和方法，例如克林霉素，林可霉素或普瑞霉素。该组合物是含有抗微生物有效量的分散在硬脂肪栓剂基质，优选硬脂肪NF栓剂基质中的颗粒形式的林可酰胺的直肠栓剂。本发明最优选的栓剂组合物具有长期的保存稳定性，同时保持对细菌感染的有效性。

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