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71. 发明申请

US20040198741A1 Compounds, compositions and methods for treating or preventing viral infections and associated diseases 审中-公开
标题翻译：用于治疗或预防病毒感染和相关疾病的化合物，组合物和方法
公开(公告)号：US20040198741A1
公开(公告)日：2004-10-07
申请号：US10829864
申请日：2004-04-22
发明人： Thomas R. Bailey , Dorothy C. Young
IPC分类号： A61K031/501 , A61K031/505 , A61K031/515 , A61K031/4439 , A61K031/427 , A61K031/422
CPC分类号： C07D277/20 , A61K31/4178 , A61K31/426 , A61K31/427 , A61K31/429 , C07D405/06 , C07D417/06 , C07D417/14 , C07D513/04
摘要： Compounds, compositions and methods are provided for the treatment and prophylaxis of infections and associated diseases caused by viruses of the Flaviviridae family by administering certain rhodanine derivatives, and analogs thereof, tri- and tetracyclic rhodanine alkanoic acids and rhodanine benzoic acids being particularly effective.
摘要翻译：提供化合物，组合物和方法用于治疗和预防由黄病毒科家族病毒引起的感染和相关疾病，通过施用某些罗丹宁衍生物及其类似物，三环四环类罗丹宁链烷酸和罗丹宁苯甲酸是特别有效的。

72. 发明申请

US20040176431A1 Antiproliferative 2-(sulfo-phenyl)-aminothiazole derivatives and pharmaceutical compositions, and methods for their use 审中-公开
标题翻译：抗增殖性2-（磺基 - 苯基） - 氨基噻唑衍生物和药物组合物及其使用方法
公开(公告)号：US20040176431A1
公开(公告)日：2004-09-09
申请号：US10776450
申请日：2004-02-11
申请人： Pfizer, Inc.
发明人： Wesley K.M. Chong , Shao Song Chu , Rohit K. Duvadie , James Na , Lana Schaffer , Yi Yang , Lin Li
IPC分类号： A61K031/427 , A61K031/426 , C07D417/02
CPC分类号： C07D277/42 , C07D277/52 , C07D417/12
摘要： Aminothiazole compounds substituted with sulfur-containing groups are represented by the Formula (I), and their pharmaceutically acceptable salts, prodrugs, active metabolites, and pharmaceutically acceptable salts of said metabolites are described. 1 These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.
摘要翻译：用含硫基团取代的氨基噻唑化合物由式（I）表示，其所述代谢物的药学上可接受的盐，前体药物，活性代谢物和药学上可接受的盐被描述。这些药物调节和/或抑制蛋白激酶的细胞增殖和活性，并且可用作治疗恶性肿瘤和其它疾病的药物。

73. 发明申请

US20040171643A1 Acylaminothiazole derivatives, their preparation and therapeutic use 有权
标题翻译：酰氨基噻唑衍生物，其制备和治疗用途
公开(公告)号：US20040171643A1
公开(公告)日：2004-09-02
申请号：US10485837
申请日：2004-02-04
发明人： Paul De Cointet , Pierre Despeyroux , Daniel Frehel , Chantal Guenet , Corinne Heckel , Jean-Pierre Maffrand , Rebecca Pruss
IPC分类号： A61K031/454 , A61K031/427 , C07D417/02
CPC分类号： C07D417/12 , C07D277/40 , C07D277/42 , C07D277/46
摘要： The invention concerns a compound of general formula (I), wherein: X represents an oxygen or sulphur atom; R1 represents, independently of each other when nnull2 or 3, a halogen atom, a hydroxy, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, a trifluoromethyloxy or a methylenedioxy; R2 represents a C1-C6 alkyl group optionally substituted, a C3-C7 cycloalkyl, piperidinyl or phenyl group, the C3-C7 cycloalkyl, piperidinyl or phenyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-C6 alkyl group optionally substituted; R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 and R5null represent, independently of each other, a hydrogen atom, a hydroxy, a halogen atom, a C1-C3 alkyl group, or R5 and R5null form together an oxo group; R6 represents a hydrogen atom, a halogen atom, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, or a trifluoromethoxy; in the form of a base, addition to an acid, hydrate or solvate. The invention is applicable in therapy. 1
摘要翻译：本发明涉及通式（I）的化合物，其中：X表示氧或硫原子; 当n = 2或3时，R 1彼此独立地表示卤素原子，羟基，C 1 -C 3烷基，C 1 -C 3烷氧基，三氟甲基，三氟甲氧基或亚甲二氧基; R 2表示任选取代的C 1 -C 6烷基，C 3 -C 7环烷基，哌啶基或苯基，C 3 -C 7环烷基，哌啶基或苯基任选被取代; R 3表示氢原子或任选取代的C 1 -C 6烷基; R4代表氢原子或C1-C4烷基; 并且R5和R5'彼此独立地表示氢原子，羟基，卤素原子，C1-C3烷基或R5和R5'一起形成氧代基团; R6表示氢原子，卤素原子，C1-C3烷基，C1-C3烷氧基，三氟甲基或三氟甲氧基; 以碱的形式加入酸，水合物或溶剂化物。本发明适用于治疗。

74. 发明申请

US20040157827A1 2-Ureido-thiazole derivatives, process for their preparation, and their use as antitumor agents 审中-公开
标题翻译： 2-脲基 - 噻唑衍生物，其制备方法及其作为抗肿瘤剂的用途
公开(公告)号：US20040157827A1
公开(公告)日：2004-08-12
申请号：US10770019
申请日：2004-02-02
发明人： Paolo Pevarello , Raffaella Amici , Gabriella Traquandi , Manuela Villa , Anna Vulpetti , Antonella Isacchi
IPC分类号： A61K031/55 , A61K031/454 , A61K031/427
CPC分类号： C07D277/62 , C07D277/48 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D491/10
摘要： Compounds which are 2-ureido-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from: i) straight or branched C1-C6 alkyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R1 is an optionally substituted group selected from: i) straight or branched C1-C6 alkyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring, iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain: R2 is hydrogen, a straight or branched C1-C4 alkyl or C2-C4 alkenyl or alkynyl group; or, taken together with the nitrogen atom to which they are bonded, R1 and R2 form a substituted or unsubstituted group selected from: i) an optionally benzocondensed or bridged 5 to 7 membered heterocycle; or ii) a 9 to 11 membered spiro-heterocyclic compound; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.
摘要翻译：作为式（I）的2-脲基-1,3-噻唑衍生物的化合物，其中R是卤素原子，硝基，任选取代的氨基，或者它是任选进一步取代的选自以下的基团：i）直链或支链C 1 -C 6烷基; ii）C 3 -C 6环烷基; iii）在直链或支链烷基链中具有1至6个碳原子的芳基或芳基烷基; R1是任选取代的基团，其选自：i）直链或支链C 1 -C 6烷基; ii）3至6元碳环或5至7元杂环，iii）芳基或芳基羰基; iv）在直链或支链烷基链中具有1至6个碳原子的芳基烷基：R 2是氢，直链或支链C 1 -C 4烷基或C 2 -C 4烯基或炔基; 或者与其键合的氮原子一起，R1和R2形成取代或未取代的基团，其选自：i）任选苯并稠合或桥连的5至7元杂环; 或ii）9至11元螺 - 杂环化合物; 或其药学上可接受的盐; 可用于治疗与改变的细胞依赖性激酶活性相关的细胞增殖性疾病。

75. 发明申请

US20040127528A1 Metalloproteinase inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US20040127528A1
公开(公告)日：2004-07-01
申请号：US10471900
申请日：2004-01-14
发明人： Anders Eriksson , Matti Lepisto , Michael Lundkvist , Magnus Munck Af Rosenschold , Pavol Zlatoidsky
IPC分类号： A61K031/427 , A61K031/426 , A61K031/421 , A61K031/4178 , A61K031/4164
CPC分类号： C07D403/04 , C07D233/76 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04
摘要： Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
摘要翻译：式（I）的化合物，其中z是SO 2或SO，可用作金属蛋白酶抑制剂，特别是作为MMP12的抑制剂。

76. 发明申请

US20040122067A1 Treatment of chronic heart failure 审中-公开
公开(公告)号：US20040122067A1
公开(公告)日：2004-06-24
申请号：US10325420
申请日：2002-12-20
发明人： Lin Zhao
IPC分类号： A61K031/426 , A61K031/427
CPC分类号： A61K31/427 , A61K31/426
摘要： Methods of treating chronic heart failure (CHF) by increasing the high energy phosphate concentrations available to heart muscle by administering a xanthine oxidase inhibitor to a patient having CHF are provided. As a result of such therapy, contractility of the heart is improved.

77. 发明申请

US20040110807A1 Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：US20040110807A1
公开(公告)日：2004-06-10
申请号：US10650434
申请日：2003-08-28
发明人： Alfred Binggeli , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr
IPC分类号： A61K031/427 , C07D417/02
CPC分类号： C07D417/06 , C07D277/24 , C07D417/12
摘要： The present invention provides compounds of formula (I) 1 wherein R1 to R10, X, Y and n are indicated in the specification, and pharmaceutically acceptable salts and esters thereof. The compounds are useful for the treatment of non-insulin dependent diabetes mellitus.
摘要翻译：本发明提供其中R 1至R 10，X，Y和n在说明书中表示的式（I）化合物及其药学上可接受的盐和酯。该化合物可用于治疗非胰岛素依赖性糖尿病。

78. 发明申请

US20040106613A1 Sulfonamides as potassium channel blockers 失效
标题翻译：磺酰胺作为钾通道阻滞剂
公开(公告)号：US20040106613A1
公开(公告)日：2004-06-03
申请号：US10641686
申请日：2003-08-14
申请人： Icagen, Inc.
发明人： Grant A. McNaughton-Smith , Aimee D. Reed , Robert N. Atkinson
IPC分类号： A61K031/53 , A61K031/506 , A61K031/501 , A61K031/497 , A61K031/427
CPC分类号： C07D271/06 , A61K9/0048 , A61K31/165 , A61K45/06 , C07C311/20 , C07C317/44 , C07C323/56 , C07C2601/16 , C07D263/32 , C07D307/52 , C07D333/70
摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides sulfonamides, and compositions and methods utilizing sulfonamides that are useful in the treatment of diseases by blocking potassium channels associated with the onset or recurrence of the indicated conditions. Exemplary diseases treatable with the compounds, compositions and methods of the invention include sickle cell disease and glaucoma.
摘要翻译：提供了通过电压依赖钾通道调节钾离子通量可用于治疗疾病的化合物，组合物和方法。更具体地，本发明提供磺酰胺，以及利用磺酰胺的组合物和方法，其可用于通过阻断与指定条件的发作或复发相关的钾通道来治疗疾病。用本发明化合物，组合物和方法治疗的示例性疾病包括镰状细胞病和青光眼。

79. 发明申请

US20040102494A1 Novel heterocyclic compounds having antibacterial activity: process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：具有抗菌活性的新型杂环化合物：其制备方法和含有它们的药物组合物
公开(公告)号：US20040102494A1
公开(公告)日：2004-05-27
申请号：US10613414
申请日：2003-07-03
申请人： Dr. Reddy's Laboratories Limited , Dr. Reddy's Laboratories Inc.
发明人： Natesan Selvakumar , Jagattaran Das , Sanjay Trehan , Javed Iqbal , Magadi Sitaram Kumar , Ramanujam Rajagopalan , Mamidi Naga Venkata Srinivasa Rao
IPC分类号： A61K031/541 , A61K031/427 , A61K031/422 , C07D417/02 , C07D413/02
CPC分类号： C07D263/20 , C07D263/22 , C07D263/24 , C07D413/10 , C07D413/14 , C07D417/10
摘要： The present invention relates to novel oxazolidinone compounds of formula (I), their stereoisomers, their salts and pharmaceutical compositions containing them. 1 The present invention also relates to a process for the preparation of the above said novel compounds, their stereoisomers, their salts and pharmaceutical compositions.
摘要翻译：本发明涉及式（I）的新型恶唑烷酮化合物，其立体异构体，其盐和含有它们的药物组合物。本发明还涉及制备上述新化合物，其立体异构体，其盐和药物组合物的方法。

80. 发明申请

US20040102480A1 Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia 失效
标题翻译：苯氧基 - 乙酸可用于治疗胰岛素抵抗和高血糖症
公开(公告)号：US20040102480A1
公开(公告)日：2004-05-27
申请号：US10300997
申请日：2002-11-21
申请人： Wyeth
发明人： Michael S. Malamas , Jay E. Wrobel , Arlene J. Dietrich , Zenan Li , Iwan Gunawan
IPC分类号： A61K031/4439 , A61K031/427 , A61K031/422 , A61K031/4178 , C07D417/02 , C07D413/02 , C07D43/02
CPC分类号： C07D333/60 , C07D307/80 , C07D333/56
摘要： This invention provides compounds of Formula I having the structure 1 wherein: A is O, S, or N; B is null(CH2)mnull, nullCH(OH)null, or carbonyl; R1 is hydrogen, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, or trifluoromethyl; R2 is alkyl of 1-18 carbon atoms, aryl of 6-10 carbon atoms, arylalkyl of 7-15 carbon atoms, Het-alkyl wherein the alkyl moiety is 1-6 carbon atoms; Het is 2 R2a is alkylene of 1-3 carbon atoms; G is oxygen, sulfur, or nitrogen; R3, R4 are each, independently, hydrogen, halogen, alkyl of 1-3 carbon atoms, aryl of 6-10 carbon atoms or a heterocyclic ring of 5 to 7 ring atom containing 1 to 3 heteroatoms selected from oxygen, nitrogen, sulfur; R5 is hydrogen, alkyl of 1-6 carbon atoms, nullCH(R7)R8, nullC(CH2)nCO2R9, nullC(CH3)2CO2R9, nullCH(R7)(CH2)nCO2R9, or CH(R7)C6H4CO2R9; R6 is hydrogen, halogen, alkyl of 1-6 carbon atoms, or nullOR5; mnull1-6; nnull1-6; R7 is hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, or arylalkyl of 7-15 carbon atoms; R8 is nullCO2R10, nullCONHR10, tetrazole, or nullPO3; R9 and R10 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, or arylalkyl of 7-15 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
摘要翻译：本发明提供具有以下结构的式I化合物：其中：A是O，S或N; B是 - （CH 2）m - ， - CH（OH） - 或羰基; R 1是氢，卤素，1-6个碳原子的烷基，1-6个碳原子的烷氧基或三氟甲基; R 2是1-18个碳原子的烷基，6-10个碳原子的芳基，7-15个碳原子的芳基烷基，其中烷基部分是1-6个碳原子的Het-烷基; Het是R 2a是1-3个碳原子的亚烷基; G是氧，硫或氮; R 3，R 4各自独立地为氢，卤素，1-3个碳原子的烷基，6-10个碳原子的芳基或含有1至3个选自以下的杂原子的5至7个环原子的杂环：氧，氮，硫; R 5是氢，1-6个碳原子的烷基，-CH（R 7）R 8，-C（CH 2）n CO 2 R 9，-C（CH 3）2 CO 2 R 9，-CH （R 7）（CH 2）n CO 2 R 9或CH（R 7）C 6 H 4 CO 2 R 9; R 6是氢，卤素，1-6个碳原子的烷基或-OR 5; m = 1-6; n = 1-6; R 7是氢，1-6个碳原子的烷基，6-10个碳原子的芳基或7-15个碳原子的芳基烷基; R 8是-CO 2 R 10，-CONHR 10，四唑或-PO 3; R 9和R 10各自独立地为氢，1-6个碳原子的烷基，6-10个碳原子的芳基或7-15个碳原子的芳基烷基; 或其药学上可接受的盐，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。

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