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61. 发明申请

US20040121964A1 Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) 审中-公开
标题翻译：药物组合物作为二肽基肽酶-IV（DPP-IV）的抑制剂
公开(公告)号：US20040121964A1
公开(公告)日：2004-06-24
申请号：US10659860
申请日：2003-09-11
发明人： David J. Madar , Stevan W. Djuric , Melissa J. Feenstra , Hana A. Kopecka , Xiaofeng Li , Kenton L. Longenecker , ZhongHua Pei , Daisy Pireh , Hing L. Sham , Kent D. Stewart , Bruce G. Szczepankiewicz , Paul E. Wiedeman , Hong Yong
IPC分类号： A61K038/04 , A61K031/69 , C07K005/04
CPC分类号： C07D207/27 , C07D207/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D417/12
摘要： The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
摘要翻译：本发明涉及抑制二肽基肽酶IV（DPP-IV）并可用于预防或治疗糖尿病，特别是II型糖尿病以及高血糖症，X综合征，高胰岛素血症，肥胖症，动脉粥样硬化和各种免疫调节疾病的化合物。

62. 发明申请

US20040116655A1 Novel polypeptides and anti-hiv drugs containing the same 有权
标题翻译：含有相同的新型多肽和抗HIV药物
公开(公告)号：US20040116655A1
公开(公告)日：2004-06-17
申请号：US10363209
申请日：2003-03-05
发明人： Nobutaka Fujii
IPC分类号： A01N037/18 , C07K005/00 , C07K016/00 , A61K038/04 , A61K038/00 , C07K017/00 , A61K035/37 , C07K007/00 , A61K035/24 , A61K035/64
CPC分类号： C07K7/08 , A61K38/00 , C07K14/43509 , Y10S530/857
摘要： Polypeptides of A1-Arg-A2-Cys-Tyr-A3-A4-X-A5-A6-Cit Cys-A7 (I) or their salts (wherein A1 is hydrogen or a residue of arginine, lysine, ornithine, citrulline, alanine, or the like; A2 is an aromatic amino acid residue; A3, A4 and A6 are each a residue of arginine, lysine, ornithine, citrulline, or alanine; A5 is a residue of tyrosine, phenylalanine, alanine, naphthylalanine, or citrulline; A7 is a lysine or arginine residue whose carboxyl group may be converted into amido; and X is a residue of D-ornithyl-proline, prolyl-D-ornithine, D-lysylproline, or the like, with the proviso that any one of A1, A3, A4, A5, A6 and A7 is a residue of alanine or the like or that X is citrulline or the like).
摘要翻译： A1-Arg-A2-Cys-Tyr-A3-A4-X-A5-A6-Cit Cys-A7（I）的多肽或其盐（其中A1是氢或精氨酸，赖氨酸，鸟氨酸，瓜氨酸，丙氨酸的残基氨基酸残基; A3，A4和A6分别是精氨酸，赖氨酸，鸟氨酸，瓜氨酸或丙氨酸的残基; A5是酪氨酸，苯丙氨酸，丙氨酸，萘丙氨酸或瓜氨酸的残基; A7是其羧基可以转化为酰氨基的赖氨酸或精氨酸残基; X是D-鸟氨酰基脯氨酸，脯氨酰-D-鸟氨酸，D-赖氨酰脯氨酸等的残基，条件是任何一个A1 ，A3，A4，A5，A6和A7是丙氨酸等的残基或X是瓜氨酸等）。

63. 发明申请

US20040115615A1 Hiv peptides antigens, vaccine compositions, immunoassay kit and a method of detecting antibodies induced by hiv 失效
标题翻译： Hiv肽抗原，疫苗组合物，免疫测定试剂盒和检测HIV诱导的抗体的方法
公开(公告)号：US20040115615A1
公开(公告)日：2004-06-17
申请号：US10129331
申请日：2002-06-11
发明人： Birger Sorensen
IPC分类号： C12Q001/70 , C07K005/00 , C07K016/00 , A61K038/00 , C07K001/00 , C12P021/08 , A61K039/21 , C07K017/00 , C07K014/00 , C07K007/00 , A61K038/04 , G01N033/53
CPC分类号： C07K14/005 , A61K2039/55522 , A61K2039/57 , C12N2740/16222
摘要： The present invention comprises novel and modified peptides capable of inducing a HIV-1 specific immune response without antagonizing the cytotoxic T-cell activity in order to achieve an effective prophylactic and therapeutic vaccine against HIV. The peptides are based on conserved regions of HIV gag p17 and p24 proteins. Antigens in free- or carrier-bound form comprising at least one of the said peptides, vaccine compositions containing at least one of the antigens, immunoassay kits and a method of detecting antibodies induced by HIV or HIV specific peptides using such antigens, are described.
摘要翻译：本发明包括能够诱导HIV-1特异性免疫应答而不拮抗细胞毒性T细胞活性以获得针对HIV的有效预防和治疗性疫苗的新型和修饰的肽。肽基于HIV gag p17和p24蛋白的保守区域。描述了包含至少一种所述肽的疫苗，含有至少一种抗原的疫苗组合物，免疫测定试剂盒以及使用这种抗原检测由HIV或HIV特异性肽诱导的抗体的方法。

64. 发明申请

US20040106559A1 Hepatitis C virus inhibitors 有权
标题翻译：丙型肝炎病毒抑制剂
公开(公告)号：US20040106559A1
公开(公告)日：2004-06-03
申请号：US10441657
申请日：2003-05-20
发明人： Xiangdong Alan Wang , Li-Qiang Sun , Sing-Yuen Sit , Ny Sin , Paul Michael Scola , Piyasena Hewawasam , Andrew Charles Good , Yan Chen , Jeffrey Allen Campbell
IPC分类号： A61K038/05 , A61K038/04 , A61K031/4015 , C07K005/04 , C07K005/06
CPC分类号： A61K38/06 , A61K31/40 , A61K38/00 , A61K38/005 , A61K45/06 , C07D207/16 , C07D217/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/14 , C07D491/04 , C07K5/06034 , C07K5/06052 , C07K5/0808 , C07K5/0827 , A61K2300/00
摘要： Hepatitis C virus inhibitors are disclosed having the general formula: 1 wherein R1, R2, R3, Rnull, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
摘要翻译：公开了具有以下通式的丙型肝炎病毒抑制剂：其中R1，R2，R3，R'，B，Y和X在说明书中描述。还公开了包含化合物的组合物和使用该化合物抑制HCV的方法。

65. 发明申请

US20040097425A1 Peptide compounds 失效
标题翻译：肽化合物
公开(公告)号：US20040097425A1
公开(公告)日：2004-05-20
申请号：US10250444
申请日：2003-12-23
发明人： Ichiro Shima , Takehiko Ohkawa , Kentaro Sato , Naoki Ishibashi , Kenichiro Imamura
IPC分类号： A61K038/04 , A61K031/4439 , C07D45/14
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/06191
摘要： The present invention relates to a compound of the formula (I)wherein R1 is benzofuranyl substituted by halogen, or styryl substituted by halogen; R2 is substituted hydroxy, substituted mercapto or substituted sulfonyl; and X is or pharmaceutically acceptable salts thereof. The compound (1) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NO-mediated diseases in human being and animals. 1
摘要翻译：本发明涉及式（I）化合物，其中R 1为被卤素取代的苯并呋喃基或被卤素取代的苯乙烯基; R2是取代的羟基，取代的巯基或取代的磺酰基; X是其药学上可接受的盐。本发明化合物（1）及其药学上可接受的盐对一氧化氮（NO）的产生具有很强的抑制活性，可用于预防和/或治疗人和动物中NO介导的疾病。

66. 发明申请

US20040097424A1 Combination product of a 1,4-benzothiepine 1,1-dioxide compound with at least one other active ingredient and the use of the product 有权
标题翻译： 1,4-苯并噻吩1,1-二氧化物化合物与至少一种其它活性成分的组合产物和产物的用途
公开(公告)号：US20040097424A1
公开(公告)日：2004-05-20
申请号：US10699967
申请日：2003-11-03
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH
发明人： Heiner Glombik , Wendelin Frick , Hans-Ludwig Schaefer , Werner Kramer
IPC分类号： A61K038/06 , A61K038/05 , A61K038/04 , A61K031/7048 , C07K005/06 , C07K005/04
CPC分类号： A61K45/06 , A61K31/395 , A61K31/55 , A61K2300/00
摘要： The present invention is directed to a 1,4-benzothiepine 1,1-dioxide compound of formula I 1 in which the radicals have the meanings defined herein, or a pharmaceutically acceptable salt or physiologically functional derivative thereof, with at least one other active ingredient, or a pharmaceutically acceptable salt or physiologically functional derivative thereof. The invention is also directed to the use of the combination product, pharmaceutical composition comprising the combination product and method for preparing the pharmaceutical composition.
摘要翻译：本发明涉及其中基团具有本文定义的含义，或其药学上可接受的盐或生理功能衍生物的式I的1,4-苯并硫代1,1-二氧化物化合物与至少一种其它活性成分，或其药学上可接受的盐或生理功能衍生物。本发明还涉及组合产品，包含组合产品和方法的药物组合物用于制备药物组合物的用途。

67. 发明申请

US20040077552A1 Inflammation-inhibiting compounds 有权
标题翻译：炎症抑制化合物
公开(公告)号：US20040077552A1
公开(公告)日：2004-04-22
申请号：US10467993
申请日：2003-09-26
发明人： Thomas Luger
IPC分类号： A61K038/05 , A61K038/04 , A61K031/198
CPC分类号： A61K38/06 , A23L33/175 , A23L33/18 , A61K9/06 , A61K31/198 , A61K38/04 , A61K38/05 , A61K39/001 , A61K2039/5154 , C07K5/06086 , C07K5/0815 , C12N2501/86 , A61K2300/00
摘要： The present invention relates to the use of a compound of the formula Lys-X where X is a hydroxyl group, an amino group, alkoxy, Pro or Pro-Thor, or of a pharmaceutically acceptable salt thereof, for the treatment of inflammations. The invention also relates to the use of nullMSH for inducing tolerance.
摘要翻译：本发明涉及式X-羟基，氨基，烷氧基，Pro或Pro-Thor或其药学上可接受的盐的式Lys-X化合物用于治疗炎症的用途。本发明还涉及αMSH用于诱导耐受性的用途。

68. 发明申请

US20040067891A1 Therapeutic and/or preventive agents for diseases due to retinal ischemia 审中-公开
标题翻译：由于视网膜缺血引起的疾病的治疗和/或预防剂
公开(公告)号：US20040067891A1
公开(公告)日：2004-04-08
申请号：US10451780
申请日：2003-06-26
发明人： Nobuo Katsube , Hitoshi Maegawa
IPC分类号： A61K031/454 , A61K038/04
CPC分类号： A61K31/454
摘要： An agent for treating and/or preventing for diseases (glaucoma, diabetic retinopathy, macular degeneration, retinal vascular obstruction, and the like) due to retinal ischemia, which comprises, as an effective ingredient, (2R)-N-(1-benzylpiperidin-4-yl)-3-cyclohexylmethylthio-2-((4R)-3-t-butoxycarbonylthiazolidin-4-ylcarbonylamino)propanamide represented by the following formula (I): 1 or a nontoxic salt thereof.
摘要翻译：治疗和/或预防视网膜缺血引起的疾病（青光眼，糖尿病性视网膜病变，黄斑变性，视网膜血管阻塞等）的药剂，其包含作为有效成分的（2R）-N-（1-苄基哌啶 -4-基）-3-环己基甲硫基-2 - （（4R）-3-叔丁氧羰基噻唑烷-4-基羰基氨基）丙酰胺或其无毒盐。

69. 发明申请

US20040063642A1 Novel benzimidazolone peptidomimetics as thrombin receptor antagonists 有权
标题翻译：新型苯并咪唑酮肽模拟物作为凝血酶受体拮抗剂
公开(公告)号：US20040063642A1
公开(公告)日：2004-04-01
申请号：US10390098
申请日：2003-03-17
发明人： Han-Cheng Zhang , Bruce E. Maryanoff , David F. McComsey , Kimberly B. White
IPC分类号： A61K038/04 , C07K005/04 , C07D43/02 , C07D235/24
CPC分类号： C07K5/06191 , A61K38/00 , C07D235/26 , H01L2924/01013 , H01L2924/01023 , H01L2924/01024 , H01L2924/01027 , H01L2924/01029 , H01L2924/0104 , H01L2924/01042 , H01L2924/01044 , H01L2924/01045 , H01L2924/01046 , H01L2924/01047 , H01L2924/01074 , H01L2924/01076 , H01L2924/01077 , H01L2924/01078 , H01L2924/01079 , H05K3/4092
摘要： The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted benzimidazolone peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
摘要翻译：本发明涉及可用作治疗与血栓形成，再狭窄，高血压，心力衰竭，心律失常，炎症，心绞痛，中风，动脉粥样硬化，缺血性疾病，血管发生相关疾病，癌症相关的疾病的凝血酶受体拮抗剂的新型苯并咪唑酮肽模拟化合物，和神经变性疾病。还公开了包含本发明的取代的苯并咪唑酮肽模拟物的药物组合物和治疗由凝血酶受体介导的病症的方法。

70. 发明申请

US20040053896A1 Pharmaceutically active compound 审中-公开
标题翻译：药物活性化合物
公开(公告)号：US20040053896A1
公开(公告)日：2004-03-18
申请号：US10333525
申请日：2003-09-18
发明人： Charles Oswald Mills
IPC分类号： A61K038/04 , C07J009/00
CPC分类号： A61K47/554 , A61K47/54
摘要： A liver-targeting active compound has the general formula (I):- wherein A is null-OH or null-OH, B is null-H or null-H, C is nullH, null-OH or null-OH, or B and C together form a double bond, D is nullH, null-OH or null-OH, E is nullH, null-OH or null-OH, nullG-is a side chain moiety, nullNHnullJ is selected from (i) a residue of an amino group-containing active compound wherein said nullNHnull group is provided by said amino group of the active compound, and (ii) a residue of an active compound to which an amino group has been added wherein said nullNHnull group is provided by said added amino group; each of X and Y independently represents a single bond, null(CH2)znull (where z is 1 to 8), nullOnull or nullSnull; n is 0 or 1; m is 0 or 1; and p is 0 or 1; provided that, when nullNHnullJ is (i), m is 1. A method of producing such as compound is also disclosed. 1
摘要翻译：肝靶向活性化合物具有通式（I）：其中A为α-OH或β-OH，B为α-H或β-H，C为-H，α-OH或β-OH，或 B和C一起形成双键，D是-H，α-OH或β-OH，E是-H，α-OH或β-OH，-G-是侧链部分，选择-NH-J 由（i）含有氨基的活性化合物的残基，其中所述-NH-基团由所述活性化合物的所述氨基提供，和（ii）已加入氨基的活性化合物的残基，其中，所述-NH-基团由所述加成的氨基提供; X和Y各自独立地表示单键， - （CH 2）z - （其中z是1至8），-O-或-S-; n为0或1; m为0或1; p为0或1; 条件是当-NH-J为（i）时，m为1.还公开了化合物的制备方法。

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