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51. 发明申请

US20030008866A1 Bicyclic inhibitors of glycogen synthase kinase 3 审中-公开
标题翻译：糖原合酶激酶3的双环抑制剂
公开(公告)号：US20030008866A1
公开(公告)日：2003-01-09
申请号：US10228621
申请日：2002-08-26
申请人： Chiron Corporation
发明人： John M. Nuss , Xiaohui A. Zhou
IPC分类号： A61K031/542 , A61K031/538 , A61K031/519 , A61K031/517
CPC分类号： C07D471/04
摘要： New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
摘要翻译：提供了新的双环类化合物，体外抑制糖原合成酶激酶（GSK3）活性和体内GSK3介导的病症治疗的组合物和方法。本发明的方法，化合物和组合物可以单独使用或与其它药理活性剂组合用于治疗由GSK3活性介导的病症，例如治疗糖尿病，阿尔茨海默病和其他神经变性疾病，肥胖症，动脉粥样硬化心血管疾病，原发性高血压，多囊卵巢综合征，X综合征，缺血，创伤性脑损伤，双相情感障碍，免疫缺陷或癌症。

52. 发明申请

US20020165229A1 Substituted 3-cyano-[1.7], [1.5], and [1.8] naphthyridine inhibitors of tyrosine kinases 失效
公开(公告)号：US20020165229A1
公开(公告)日：2002-11-07
申请号：US10032587
申请日：2001-12-21
申请人： American Cyanamid Company
发明人： Allan Wissner , Philip R. Hamann , Ayako Yamashita
IPC分类号： C07D471/02 , A61K031/538 , A61K031/498 , A61K031/47 , A61K031/506
CPC分类号： C07D471/04 , A61K31/47 , A61K31/498 , A61K31/506 , A61K31/538
摘要： This invention provides compounds of formula I having the structure 1 wherein: X is cycloalkyl of 3 to 7 carbon atoms, which may be optionally substituted with one or more alkyl of 1 to 6 carbon atom groups; or X is pyridinyl, pyrimidinyl, or Ph; or X is a bicyclic aryl or bicyclic heteroaryl ring system of 8 to 12 atoms, where the bicyclic heteroaryl ring contains 1 to 4 heteroatoms selected from N, O, and S; wherein the bicyclic aryl or bicyclic heteroaryl ring may be optionally mono-, di-, tri-, or tetra-substituted with a substituent selected from the group consisting of halogen, oxo, thio, alkyl of 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, azido, hydroxyalkyl of 1-6 carbon atoms, halomethyl, alkoxymethyl of 2-7 carbon atoms, alkanoyloxymethyl of 2-7 carbon atoms, alkoxy of 1-6 carbon atoms, alkylthio of 1-6 carbon atoms, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, phenoxy, phenyl, thiophenoxy, benzoyl, benzyl, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 2 to 12 carbon atoms, phenylamino, benzylamino, alkanoylamino of 1-6 carbon atoms, alkenoylamino of 3-8 carbon atoms, alkynoylamino of 3-8 carbon atoms, carboxyalkyl of 2-7 carbon atoms, carboalkoxyalkyl of 3-8 carbon atoms, aminoalkyl of 1-5 carbon atoms, N-alkylaminoalkyl of 2-9 carbon atoms, N,N-dialkylaminoalkyl of 3-10 carbon atoms, N-alkylaminoalkoxy of 2-9 carbon atoms, N,N-dialkylaminoalkoxy of 3-10 carbon atoms, mercapto, methylmercapto, and benzoylamino; or X is the radical 2 ; E is pyridinyl, pyrimidinyl, or Ph; T is substituted on E at carbon and is nullNH(CH2)mnull, nullO(CH2)mnull, nullS(CH2)mnull, nullNR(CH2)mnull, null(CH2)mnull(CH2)mNHnull, null(CH2)mOnull, null(CH2)mSnull, or null(CH2)mNRnull; L is a Ph; or L is a 5- or 6-membered heteroaryl ring where the heteroaryl ring contains 1 to 3 heteroatoms selected from N, O, and S; wherein the heteroaryl ring may be optionally mono- or di-substituted with a substituent selected from the group consisting of halogen, oxo, thio, alkyl of 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, azido, hydroxyalkyl of 1-6 carbon atoms, halomethyl, alkoxymethyl of 2-7 carbon atoms, alkanoyloxymethyl of 2-7 carbon atoms, alkoxy of 1-6 carbon atoms, alkylthio of 1-6 carbon atoms, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, phenoxy, phenyl, thiophenoxy, benzoyl, benzyl, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 2 to 12 carbon atoms, phenylamino, benzylamino, alkanoylamino of 1-6 carbon atoms, alkenoylamino of 3-8 carbon atoms, alkynoylamino of 3-8 carbon atoms, carboxyalkyl of 2-7 carbon atoms, carboalkoxyalkyl of 3-8 carbon atoms, aminoalkyl of 1-5 carbon atoms, N-alkylaminoalkyl of 2-9 carbon atoms, N,N-dialkylaminoalkyl of 3-10 carbon atoms, N-alkylaminoalkoxy of 2-9 carbon atoms, N,N-dialkylaminoalkoxy of 3-10 carbon atoms, mercapto, methylmercapto, and benzoylamino; Pyridinyl, pyrimidinyl, or Ph are pyridinyl, pyrimidinyl, or phenyl radicals, respectively, which may be optionally mono- di-, or tri-substituted with a substituent selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, azido, hydroxyalkyl of 1-6 carbon atoms, halomethyl, alkoxymethyl of 2-7 carbon atoms, alkanoyloxymethyl of 2-7 carbon atoms, alkoxy of 1-6 carbon atoms, alkylthio of 1-6 carbon atoms, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, benzoyl, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 2 to 12 carbon atoms, alkanoylamino of 1-6 carbon atoms, alkenoylamino of 3-8 carbon atoms, alkynoylamino of 3-8 carbon atoms, carboxyalkyl of 2-7 carbon atoms, carboalkoxyalkyl of 3-8 carbon atoms, aminoalkyl of 1-5 carbon atoms, N-alkylaminoalkyl of 2-9 carbon atoms, N,N-dialkylaminoalkyl of 3-10 carbon atoms, N-alkylaminoalkoxy of 2-9 carbon atoms, N,N-dialkylaminoalkoxy of 3-10 carbon atoms, mercapto, methylmercapto, and benzoylamino; Z is nullNHnull, nullOnull, nullSnull, or nullNRnull; R is alkyl of 1-6 carbon atoms, or carboalkyl of 2-7 carbon atoms; Anull is a diavalent moiety selected from the group 3 G1, G2, G3, and G4 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, alkenyloxy of 2-6 carbon atoms, alkynyloxy of 2-6 carbon atoms, hydroxymethyl, halomethyl, alkanoyloxy of 2-6 carbon atoms, alkenoyloxy of 3-8 carbon atoms, alkynoyloxy of 3-8 carbon atoms, alkanoyloxymethyl of 2-7 carbon atoms, alkenoyloxymethyl of 49 carbon atoms, alkynoyloxymethyl of 49 carbon atoms, alkoxymethyl of 2-7 carbon atoms, alkoxy of 1-6 carbon atoms, alkylthio of 1-6 carbon atoms, alkylsulphinyl of 1-6 carbon atoms, alkylsulphonyl of 1-6 carbon atoms, alkylsulfonamido of 1-6 carbon atoms, alkenylsulfonamido of 2-6 carbon atoms, alkynylsulfonamido of 2-6 carbon atoms, hydroxy, trifluoromethyl, trifluoromethoxy, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino of 1-4 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 2 to 12 carbon atoms, N-alkylcarbamoyl, N,N-dialkylcarbamoyl, N-alkyl-N-alkenylamino of 4 to 12 carbon atoms, N,N-dialkenylamino of 6-12 carbon atoms, phenylamino, benzylamino, R2NH, 4 nullR7null(C(R6)2)gnullYnull, R7null(C(R6)2)pnullMnull(C(R6)2)knullYnull, Het-(C(R6)2)qnullWnull(C(R6)2)knullYnull, with the proviso that G3 and G4 are not R2NH; Y is a divalent radical selected from the group consisting of 5 R7 is nullNR6R6, nullOR6, nullJ, nullN(R6)3null, or nullNR6(OR6); M is >NR6, nullOnull, >Nnull(C(R6)2)pNR6R6, or >Nnull(C(R6)2)pnullOR6; W is >NR6, nullOnull or is a bond; Het is a heterocyclic radical selected from the group consisting of morpholine, thiomorpholine, thiomorpholine S-oxide, thiomorpholine S,S-dioxide, piperidine, pyrrolidine, aziridine, pyridine, imidazole, 1,2,3-triazole, 1,2,4-triazole, thiazole, thiazolidine, tetrazole, piperazine, furan, thiophene, tetrahydrothiophene, tetrahydrofuran, dioxane, 1,3-dioxolane, tetrahydropyran, and 6 which may be optionally mono- or di-substituted on carbon with R6, hydroxy, nullN(R6)2, nullOR6null(C(R6)2)sOR6 or null(C(R6)2)sN(R6)2; optionally mono-substituted on nitrogen with R6; and optionally mono or di-substituted on a saturated carbon with divalent radicals nullOnull or nullO(C(R6)2)sOnull; R6 is hydrogen, alkyl of 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, cycloalkyl of 1-6 carbon atoms, carboalkyl of 2-7 carbon atoms, carboxyalkyl 2-7 carbon atoms, phenyl, or phenyl optionally substituted with one or more halogen, alkoxy of 1-6 carbon atoms, trifluoromethyl, amino, alkylamino of 1-3 carbon atoms, dialkylamino of 2-6 carbon atoms, nitro, cyano, azido, halomethyl, alkoxymethyl of 2-7 carbon atoms, alkanoyloxymethyl of 2-7 carbon atoms, alkylthio of 1-6 carbon atoms, hydroxy, carboxyl, carboalkoxy of 2-7 carbon atoms, phenoxy, phenyl, thiophenoxy, benzoyl, benzyl, phenylamino, benzylamino, alkanoylamino of 1-6 carbon atoms, or alkyl of 1-6 carbon atoms; with the proviso that the alkenyl or alkynyl moiety is bound to a nitrogen or oxygen atom through a saturated carbon atom; R2, is selected from the group consisting of 7 R3 is hydrogen, alkyl of 1-6 carbon atoms, carboxy, carboalkoxy of 1-6 carbon atoms, phenyl, carboalkyl of 2-7 carbon atoms, 8 , nullR7null(C(R)2)snull, R7null(C(R6)2)pnullMnull(C(R6)2)rnull, R8R9nullCHnullM(C(R6)2)rnull, or Het-(C(R6)2)qnullWnullC(R6)2)rnull; R5 is hydrogen, alkyl of 1-6 carbon atoms, carboxy, carboalkoxy of 1-6 carbon atoms, phenyl, carboalkyl of 2-7 carbon atoms, 9 , nullR7null(C(R6)2)snull, R7null(C(R6)2)pnullMnull(C(R6)2)rnull, R8R9nullCHnullMnull(C(R6)2)rnull, or Het-(C(R6)2)qnullWnull(C(R6)2)rnull; R8, and R9 are each, independently, null(C(R6)2)rNR6R6, or null(C(R6)2)rOR6; J is independently hydrogen, chlorine, fluorine, or bromine; Q is alkyl of 1-6 carbon atoms or hydrogen; anull0-1; gnull1-6; knull0-4; n is 0-1; m is 0-3; pnull2-4; qnull0-4; rnull1-4; snull1-6; unull0-4 and vnull0-4, wherein the sum of unullv is 2-4; or a pharmaceutically acceptable salt thereof, provided that when R6 is alkenyl of 2-7 carbon atoms or alynyl of 2-7 carbon atoms, such alkenyl or alynyl moiety is bound to a nitrogen or oxygen atom through a saturated carbon atom; and provided that when R3 is bound to sulfur, it cannot be hydrogen, carboxy, carboalkoxy, or carboalkyl; and provided that when Y is nullNR6null and R7 is nullNR6R6, nullN(R6)3null, or nullNR6(OR6), then gnull2-6; when M is nullOnull and R7 is nullOR6 then pnull1-4; when Y is nullNR6null then knull2-4; when Y is nullOnull and M or W is nullOnull then knull1-4 when W is not a bond with Het bonded through a nitrogen atom then qnull2-4 and when W is a bond with Het bonded through a nitrogen atom and Y is nullOnull or nullNR6null then knull2-4; and finally provided that when Anull is the moiety 10 nnull0, Z is NH, G1 is hydrogen, halogen, alkyl, alkoxy, hydroxy, alkanoyloxy of 2-6 carbon atoms, or phenoxy, and G2 is hydrogen, halogen, alkyl, hydroxy, carboxyalkyl, carboalkoxyalkyl, hydroxyalkyl, alkoxy,halomethyl, carboxyl, carboalkoxy, alkanoylamino, or alkenoylamino, then X can not be a pyridinyl, pyrimidinyl, or phenyl ring that is substituted with a hydroxy or alkoxy group, which are useful as inhibitors of protein tyrosine kinase.

53. 发明申请

US20020143009A1 Novel bicyclic oxazolidinones as antibacterial agents 审中-公开
标题翻译：新型双环恶唑烷酮作为抗菌剂
公开(公告)号：US20020143009A1
公开(公告)日：2002-10-03
申请号：US10090400
申请日：2002-03-04
申请人： Pharmacia & Upjohn
发明人： Michael J. Genin , Michael Robert Barbachyn , Jackson B. Hester JR. , Paul D. Johnson
IPC分类号： C07D417/02 , C07D413/02 , A61K031/5415 , A61K031/502 , A61K031/538 , A61K031/4709
CPC分类号： C07D413/04
摘要： The present invention provides compounds of formula I useful as antimicrobial agents 1 wherein W, X, Y, R1, R2 and n are as defined in thereof.
摘要翻译：本发明提供可用作抗微生物剂的式I化合物，其中W，X，Y，R 1，R 2和n如其中所定义。

54. 发明申请

US20020061876A1 Compounds, their preparation and use 审中-公开
公开(公告)号：US20020061876A1
公开(公告)日：2002-05-23
申请号：US09995177
申请日：2001-11-27
发明人： Lone Jeppesen , Paul Stanley Bury , Per Sauerberg
IPC分类号： C07D279/18 , C07D265/38 , A61K031/55 , A61K031/5415 , A61K031/538 , A61K031/498 , A61K031/473 , A61K031/403
CPC分类号： C07D471/14 , C07D491/14 , C07D495/14
摘要： The present invention relates to compounds of the general formula (I) 1 The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

55. 发明申请

US20020055502A1 New compounds, their preparation and use 失效
标题翻译：新化合物，其制备和用途
公开(公告)号：US20020055502A1
公开(公告)日：2002-05-09
申请号：US09994986
申请日：2001-11-27
发明人： Lone Jeppesen , Paul Stanley Bury , Per Sauerberg
IPC分类号： A61K031/55 , A61K031/538 , A61K031/5415 , A61K031/473
CPC分类号： C07D471/14 , C07D491/14 , C07D495/14
摘要： The present invention relates to compounds of the general formula (I) 1 The compounds are useful in the treatment and/or prevention of conditions mediated by clear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
摘要翻译：本发明涉及通式（I）的化合物。该化合物可用于治疗和/或预防由透明受体介导的病症，特别是过氧化物酶体增殖物激活受体（PPAR）

56. 发明申请

US20020028803A1 Carbamate caspase inhibitors and uses thereof 失效
标题翻译：氨基甲酸酯半胱天冬酶抑制剂及其用途
公开(公告)号：US20020028803A1
公开(公告)日：2002-03-07
申请号：US09821161
申请日：2001-03-29
发明人： David Bebbington , Ronald Knegtel , Michael Mortimore , David Kay , Julian M.C. Golec
IPC分类号： A61K031/55 , A61K031/5415 , A61K031/538 , A61K031/52 , A61K031/4985 , A61K031/403
CPC分类号： C07D403/12 , C07D209/08 , C07D209/86 , C07D221/12 , C07D223/26 , C07D223/28 , C07D279/30
摘要： This invention provides caspase inhibitors of formula I: 1 wherein Z is oxygen or sulfur; R1 is hydrogen, nullCHN2, R, CH2OR, CH2SR, or nullCH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1null secretion.
摘要翻译：本发明提供了式I的半胱天冬酶抑制剂：其中Z是氧或硫; R1是氢，-CHN2，R，CH2OR，CH2SR或-CH2Y; Y是电负离子团; R2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; R3是能够适应胱天蛋白酶的S2亚位点的基团; R4和R5与间插氮一起形成杂环，R如说明书中所述。这些化合物是凋亡和IL-1β分泌的有效抑制剂。

57. 发明申请

US20020013314A1 3,4-dihydro-2H-benzo[1,4]oxazine inhibitors of factor Xa 审中-公开
标题翻译： 3,4-二氢-2H-苯并[1,4]恶嗪因子Xa抑制剂
公开(公告)号：US20020013314A1
公开(公告)日：2002-01-31
申请号：US09773373
申请日：2001-02-01
发明人： Bing-Yan Zhu , Robert M. Scarborough
IPC分类号： A61K031/538 , C07D265/36
CPC分类号： C07D413/06 , C07D265/36 , C07D413/12 , C07D413/14
摘要： Novel compounds of formula I: 1 including its pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.
摘要翻译：描述了新颖的式I化合物：包括其药学上可接受的异构体，盐，水合物，溶剂合物和具有抗哺乳动物因子Xa活性的前药衍生物。还描述了含有这些化合物的组合物。化合物和组合物可用于体外或体内用于预防或治疗特征在于不希望的血栓形成的哺乳动物的状况。

58. 发明申请

US20040224948A1 Novel substituted benzoxazines as integrin antagonists 失效
标题翻译：新型取代的苯并恶嗪作为整联蛋白拮抗剂
公开(公告)号：US20040224948A1
公开(公告)日：2004-11-11
申请号：US10821104
申请日：2004-04-08
发明人： Paola Vianello , Tiziano Bandiera
IPC分类号： A61K031/538 , C07D413/02
CPC分类号： C07D413/12 , A61K31/538 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a class of compounds represented by the formula (I) 1 or a pharmaceutical acceptable salt, prodrug or ester thereof, pharmaceutical compositions comprising compounds of the formula (I), and methods of selectively inhibiting or antagonizing nullvnull3 integrin.
摘要翻译：本发明涉及一类由式（I）表示的化合物或其药学上可接受的盐，前药或酯，包含式（I）化合物的药物组合物，以及选择性抑制或拮抗α-角蛋白3整联蛋白的方法。

59. 发明申请

US20040198726A1 Tri-and tetraaza-acenaphthylen derivatives as crf receptor antagonists 失效
标题翻译：三 - 和四氮杂苊烯衍生物作为受体拮抗剂
公开(公告)号：US20040198726A1
公开(公告)日：2004-10-07
申请号：US10477886
申请日：2004-05-28
发明人： Romano Di Fabio , Gabriella Gentile , Mustapha Haddach , Yves St Denis , John Patrick Williams
IPC分类号： A61K031/538 , A61K031/519 , C07D491/02 , C07D487/14
CPC分类号： C07D471/16
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure of formula (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, R1, R2, R4, R5, R6, A, X, and Y are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same. 1
摘要翻译：公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。本发明的CRF受体拮抗剂具有以下结构式（I）：其包括立体异构体，其前药和药学上可接受的盐，R 1，R 2，R 4，R 5，R 6，A，X和Y如本文所定义。还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

60. 发明申请

US20040157840A1 Rifalazil compositions and therapeutic regimens 失效
标题翻译：利福拉齐组合物和治疗方案
公开(公告)号：US20040157840A1
公开(公告)日：2004-08-12
申请号：US10668792
申请日：2003-09-23
发明人： Bernard E. Cabana , Arthur F. Michaelis , Gary P. Magnant , Chalom B. Sayada
IPC分类号： A61K031/538
CPC分类号： C07D498/18 , A61K9/0019 , A61K9/08 , A61K31/538 , A61K45/06 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/34 , C07D513/18 , A61K2300/00
摘要： The invention features low-dosage rifalazil compositions and therapeutic regimens which are useful for the treatment of bacterial infections.
摘要翻译：本发明的特征在于低剂量的利福拉齐组合物和治疗方案可用于治疗细菌感染。

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