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91. 发明申请

WO1996030361A1 PROCESS FOR 2-SUBSTITUTED BENZO[b]THIOPHENE COMPOUNDS AND INTERMEDIATES THEREOF 审中-公开
标题翻译： 2-取代苯并[b]噻吩化合物及其中间体的方法
公开(公告)号：WO1996030361A1
公开(公告)日：1996-10-03
申请号：PCT/US1996004417
申请日：1996-03-28
申请人： ELI LILLY AND COMPANY , HAUSER, Kenneth, L. , PALKOWITZ, Alan, D. , SALL, Daniel, J. , THRASHER, Kenneth, J.
发明人： ELI LILLY AND COMPANY
IPC分类号： C07D333/52
CPC分类号： C07D333/54 , C07D333/56 , C07D333/62 , C07F5/025 , Y02P20/55
摘要： The present invention provides processes for preparing compounds of formula (I), wherein R is -H, -OH, or OR , in which R is a hydroxy protecting group; and R is -H, -OH, or OR , in which R is a hydroxy protecting group, and for preparing compounds of formula (VII), wherein R is -H, -OH, or OR , in which R is a hydroxy protecting group; R is -H, -OH, or OR , in which R is a hydroxy protecting group; R is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; R is bromo, chloro, iodo, or an activating ester group; and n is 2 or 3. Also provided are processes for preparing compounds of formula (VII) in addition to intermediates of formula (IX), wherein R is -OH, or -OR , in which R is a hydroxy protecting group; and Z is bromo, iodo, triflate, or -B(OH)2.
摘要翻译：本发明提供制备式（I）化合物的方法，其中R 1是-H，-OH或OR 3，其中R 3是羟基保护基; 和R 2是-H，-OH或OR 4，其中R 4是羟基保护基，并且用于制备式（VII）的化合物，其中R 1是-H， - OH或OR 3，其中R 3是羟基保护基; R 2是-H，-OH或OR 4，其中R 4是羟基保护基; R 5是1-哌啶基，1-吡咯烷基，甲基-1-吡咯烷基，二甲基-1-吡咯烷基，4-吗啉代，二甲基氨基，二乙基氨基，二异丙基氨基或1-六亚甲基亚氨基; R 6是溴，氯，碘或活化酯基; 还提供了除式（Ⅸ）中间体外还制备式（Ⅶ）化合物的方法，其中R 1'是-OH或-OR 3，其中R 1， 3>是羟基保护基; 和Z是溴，碘，三氟甲磺酸酯或-B（OH）2。

92. 发明申请

WO9604241A3 BENZOYLGUANIDINE DERIVATIVES AS MEDICAMENTS 审中-公开
标题翻译：苯甲酰胺衍生物作为药物
公开(公告)号：WO9604241A3
公开(公告)日：1996-06-20
申请号：PCT/JP9501479
申请日：1995-07-25
申请人： FUJISAWA PHARMACEUTICAL CO , KUNO ATSUSHI , MIZUNO HIROAKI , YAMASAKI KUMI , INOUE YOSHIKAZU
发明人： KUNO ATSUSHI , MIZUNO HIROAKI , YAMASAKI KUMI , INOUE YOSHIKAZU
IPC分类号： C07D295/14 , A61K31/165 , A61K31/185 , A61K31/275 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/495 , A61P9/00 , A61P9/10 , A61P13/02 , A61P15/00 , C07C279/22 , C07D209/08 , C07D215/14 , C07D217/02 , C07D217/16 , C07D241/42 , C07D263/56 , C07D295/13 , C07D295/22 , C07D307/46 , C07D307/56 , C07D307/79 , C07D307/80 , C07D307/82 , C07D311/58 , C07D311/96 , C07D317/54 , C07D317/58 , C07D321/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D333/36 , C07D333/54 , C07D333/56 , C07D333/62 , C07D471/04 , A61K31/155 , A61K31/34 , C07D307/01 , C07D307/81 , C07D333/12 , C07D333/24 , C07D417/04
CPC分类号： C07D263/56 , C07C279/22 , C07C2601/10 , C07C2602/10 , C07C2602/12 , C07C2602/28 , C07D209/08 , C07D215/14 , C07D217/02 , C07D241/42 , C07D295/13 , C07D307/46 , C07D307/56 , C07D307/79 , C07D307/80 , C07D307/82 , C07D311/58 , C07D311/96 , C07D317/54 , C07D333/22 , C07D333/28 , C07D333/36 , C07D333/54 , C07D333/56 , C07D333/62 , C07D471/04
摘要： Guanidine derivatives of formula (I) wherein R1 is hydrogen, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, acyl(lower)alkoxy, acyl(lower)alkenyl, or acyl, and R2 is ar(lower)alkenyl; aryl substituted with two suitable substituents; indenyl, indanyl, dihydrobenzocycloheptenyl, di(or tetra or hexa or octa or deca)hydronaphthyl, cyclopentenyl, dihydrothienyl, dihydrofuryl or heterobicyclic group, each of which may have suitable substituent(s); lower alkylthienyl; mono(or di)halothienyl; mono(or di or tri)halo(lower)alkylthienyl; acylthienyl; halofuryl; or mono(or di or tri)halo(lower)alkylfuryl; and a pharmaceutically acceptable salt thereof, which is useful as a medicament.

93. 发明申请

WO2016131098A8 SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME 审中-公开
标题翻译：磺脲类及相关化合物及其用途
公开(公告)号：WO2016131098A8
公开(公告)日：2017-03-16
申请号：PCT/AU2016050103
申请日：2016-02-16
申请人： UNIV QUEENSLAND , THE PROVOST FELLOWS FOUND SCHOLARS AND THE OTHER MEMBERS OF BOARD OF THE COLLEGE OF THE HOLY AND UND
发明人： O'NEILL LUKE , COLL REBECCA , COOPER MATT , ROBERTSON AVRIL , SCHRODER KATE
IPC分类号： C07D231/18 , A61K31/64 , A61P1/00 , A61P9/00 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/00 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00 , C07C311/54 , C07C311/56 , C07D207/38 , C07D213/71 , C07D217/22 , C07D217/24 , C07D235/02 , C07D241/24 , C07D241/44 , C07D249/04 , C07D249/06 , C07D249/12 , C07D261/18 , C07D271/12 , C07D277/36 , C07D307/18 , C07D307/64 , C07D307/82 , C07D309/08 , C07D311/18 , C07D311/60 , C07D317/62 , C07D333/34 , C07D333/62 , C07D401/06 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D495/06 , C07D498/04
CPC分类号： C07D307/82 , C07C311/56 , C07C311/60 , C07C2601/08 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07C2603/10 , C07D207/38 , C07D213/71 , C07D217/22 , C07D217/24 , C07D231/18 , C07D235/02 , C07D241/24 , C07D241/44 , C07D249/04 , C07D249/06 , C07D249/12 , C07D261/18 , C07D271/12 , C07D277/36 , C07D307/18 , C07D307/64 , C07D309/08 , C07D311/18 , C07D311/60 , C07D317/62 , C07D333/34 , C07D333/62 , C07D401/06 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D495/06 , C07D498/04
摘要： The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.
摘要翻译：本发明提供了某些磺酰脲和相关化合物，其具有有利的性质并且在抑制NLRP3炎性体的活化中显示有用的活性。这些化合物可用于治疗其中炎症过程（或更具体地，NLRP3炎性体）被牵连为关键因素的各种疾病。

94. 发明申请

WO2006105127A8 HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译：羟肟酸脱氢酶抑制剂
公开(公告)号：WO2006105127A8
公开(公告)日：2017-02-09
申请号：PCT/US2006011347
申请日：2006-03-28
申请人： TAKEDA SAN DIEGO INC , AERTGEERTS KATHLEEN , BRENNAN NANCY K , CAO SHELDON X , CHANG EDCON , KIRYANOV ANDRE A , LIU YAN
发明人： AERTGEERTS KATHLEEN , BRENNAN NANCY K , CAO SHELDON X , CHANG EDCON , KIRYANOV ANDRE A , LIU YAN
IPC分类号： C07D295/22 , C07D211/96 , C07D213/71 , C07D215/36 , C07D217/22 , C07D217/24 , C07D231/18 , C07D233/84 , C07D261/10 , C07D261/20 , C07D265/36 , C07D271/12 , C07D277/62 , C07D285/16 , C07D307/87
CPC分类号： C07D241/38 , C07D207/48 , C07D209/08 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/38 , C07D211/54 , C07D211/58 , C07D211/62 , C07D211/76 , C07D211/96 , C07D213/70 , C07D213/74 , C07D215/04 , C07D215/42 , C07D215/58 , C07D217/02 , C07D217/06 , C07D217/08 , C07D217/22 , C07D217/24 , C07D231/18 , C07D231/56 , C07D233/42 , C07D235/26 , C07D239/14 , C07D241/08 , C07D241/50 , C07D261/10 , C07D265/36 , C07D271/12 , C07D277/56 , C07D277/58 , C07D277/62 , C07D279/16 , C07D285/14 , C07D285/16 , C07D295/26 , C07D307/68 , C07D307/79 , C07D333/62 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D413/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/10 , C07D513/04
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with hydroxysteroid dehydrogenases that comprise a compound selected from the group consisting of: formula (I), wherein the variables are as defined herein.
摘要翻译：提供化合物，药物组合物，试剂盒和方法用于含有选自以下的化合物的羟基类固醇脱氢酶：式（I），其中变量如本文所定义。

95. 发明申请

WO2014031784A1 COMPOUNDS FOR THE TREATMENT OF PARAMOXYVIRUS VIRAL INFECTIONS 审中-公开
标题翻译：用于治疗寄生虫病毒感染的化合物
公开(公告)号：WO2014031784A1
公开(公告)日：2014-02-27
申请号：PCT/US2013/056052
申请日：2013-08-21
申请人： ALIOS BIOPHARMA, INC.
发明人： WANG, Guangyi , BEIGELMAN, Leonid , TRUONG, Anh , NAPOLITANO, Carmela , ANDREOTTI, Daniele , HE, Haiying
IPC分类号： C07D333/52 , C07C251/84 , C07C251/86 , C07D207/00 , C07D209/04 , C07D213/00 , C07D215/00 , C07D217/00 , C07D233/60 , C07D235/02 , C07D249/04 , C07D249/18 , C07D261/02 , C07D265/00 , C07D307/02 , C07D307/78 , C07D311/02 , C07D333/02 , C07D335/04 , C07D401/00 , C07D403/00 , C07D407/00 , C07D409/00 , C07D413/00 , C07D417/00 , C07D417/02 , C07D495/02 , C07D495/14 , A61K31/16 , A61K31/33 , A61K31/14
CPC分类号： C07D495/04 , A61K31/165 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/381 , A61K31/382 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/407 , A61K31/4155 , A61K31/4164 , A61K31/4196 , A61K31/423 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/4365 , A61K31/4375 , A61K31/4418 , A61K31/4427 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/4704 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K45/06 , C07C243/18 , C07C243/34 , C07C251/80 , C07C251/84 , C07C255/34 , C07C255/66 , C07C2602/08 , C07D207/335 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/86 , C07D213/42 , C07D213/50 , C07D213/65 , C07D213/68 , C07D215/12 , C07D215/14 , C07D215/38 , C07D215/42 , C07D217/24 , C07D233/38 , C07D233/60 , C07D233/61 , C07D233/64 , C07D233/88 , C07D261/20 , C07D277/56 , C07D277/64 , C07D307/40 , C07D307/52 , C07D307/81 , C07D307/91 , C07D311/68 , C07D333/16 , C07D333/20 , C07D333/50 , C07D333/54 , C07D333/58 , C07D333/62 , C07D333/66 , C07D333/68 , C07D333/76 , C07D335/06 , C07D401/04 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D471/04 , C07D495/14 , A61K2300/00
摘要： Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
摘要翻译：本文公开了新的抗病毒化合物以及包含一种或多种抗病毒化合物的药物组合物及其合成方法。本文还公开了用一种或多种小分子化合物改善和/或治疗副粘病毒病毒感染的方法。副粘病毒感染的实例包括由人呼吸道合胞病毒（RSV）引起的感染。

96. 发明申请

WO2012035171A2 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2012035171A2
公开(公告)日：2012-03-22
申请号：PCT/EP2011/066250
申请日：2011-09-19
申请人： KANCERA AB , BYSTRÖM, Styrbjörn , HEDGECOCK, Charles , HOMAN, Evert , LUNDBÄCK, Thomas , MARTINSSON, Jessica , SARI, Meral , FÄRNEGÅRDH, Katarina , JÖNSSON, Mattias
发明人： BYSTRÖM, Styrbjörn , HEDGECOCK, Charles , HOMAN, Evert , LUNDBÄCK, Thomas , MARTINSSON, Jessica , SARI, Meral , FÄRNEGÅRDH, Katarina , JÖNSSON, Mattias
IPC分类号： C07D257/04 , C07D307/82 , C07D333/34 , C07D333/62 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07C311/21 , C07C311/29 , A61K31/41 , A61K31/422 , A61K31/381 , A61K31/4436 , A61K31/427 , A61K31/343 , A61K31/506 , A61K31/18 , A61P35/00 , A61P29/00
CPC分类号： C07D333/62 , C07C311/21 , C07C311/29 , C07D257/04 , C07D307/82 , C07D333/04 , C07D333/34 , C07D405/12 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.
摘要翻译：式（I）的化合物，其中A是S，O或双键，L是取代的噻唑基，苯基或吡啶基。该化合物可用于治疗炎症和癌症。

97. 发明申请

WO2011161201A1 BISARYLSULFONAMIDES USEFUL AS KINASE INHIBITORS IN THE TREATMENT OF INFLAMMATION AND CANCER 审中-公开
标题翻译：用于治疗炎症和癌症的激酶抑制剂的双相混合物
公开(公告)号：WO2011161201A1
公开(公告)日：2011-12-29
申请号：PCT/EP2011/060526
申请日：2011-06-22
申请人： KANCERA AB , ANGBRANT, Johan , HOMAN, Evert , LUNDBÄCK, Thomas , MARTINSSON, Jessica , SARI, Meral , JÖNSSON, Mattias , FÄRNEGÅRDH, Katarina , HALLBERG, Kenth
发明人： ANGBRANT, Johan , HOMAN, Evert , LUNDBÄCK, Thomas , MARTINSSON, Jessica , SARI, Meral , JÖNSSON, Mattias , FÄRNEGÅRDH, Katarina , HALLBERG, Kenth
IPC分类号： C07D213/34 , C07D215/12 , C07D277/26 , C07D307/79 , C07D333/22 , C07D333/34 , C07D333/62 , C07D409/04 , C07D295/192 , C07D295/096 , C07C311/21 , A61K31/381 , A61P35/00
CPC分类号： C07D333/22 , C07C311/13 , C07C311/21 , C07C311/27 , C07C311/29 , C07C311/39 , C07C311/46 , C07C311/47 , C07C317/14 , C07C323/67 , C07D213/34 , C07D215/12 , C07D277/26 , C07D295/096 , C07D295/192 , C07D307/79 , C07D333/34 , C07D333/62 , C07D409/04
摘要： A compound of formula (I). The compound is useful for treating cancer and inflammatory diseases. A pharmaceutical composition containing the compound.
摘要翻译：式（I）化合物。该化合物可用于治疗癌症和炎性疾病。含有该化合物的药物组合物。

98. 发明申请

WO2008103354A3 MODULATORS OF ACETYL-COENZYME A CARBOXYLASE AND METHODS OF USE THEREOF 审中-公开
标题翻译：乙酰辅酶A羧甲基酶的调节剂及其使用方法
公开(公告)号：WO2008103354A3
公开(公告)日：2009-08-06
申请号：PCT/US2008002186
申请日：2008-02-20
申请人： CROPSOLUTION INC , ANDERSON RICHARD , LEE SHY-FUH , OEY RAFAEL , ELICH TEDD D , HOKAMA TAKEO , BREAZEALE STEVEN
发明人： ANDERSON RICHARD , LEE SHY-FUH , OEY RAFAEL , ELICH TEDD D , HOKAMA TAKEO , BREAZEALE STEVEN
IPC分类号： C07D209/46 , C07D209/48 , C07D211/28 , C07D211/58 , C07D213/81 , C07D217/04 , C07D217/08 , C07D217/10 , C07D239/42 , C07D239/47 , C07D239/88 , C07D251/46 , C07D263/34 , C07D307/85 , C07D307/91
CPC分类号： C07D239/88 , C07D209/46 , C07D209/48 , C07D211/28 , C07D211/58 , C07D213/81 , C07D217/04 , C07D217/08 , C07D217/10 , C07D239/42 , C07D239/47 , C07D251/46 , C07D263/34 , C07D275/03 , C07D295/13 , C07D307/85 , C07D307/91 , C07D317/58 , C07D319/18 , C07D333/34 , C07D333/54 , C07D333/58 , C07D333/62 , C07D333/70 , C07D405/12 , C07D407/12 , C07D417/12 , C07D495/04 , C07D513/04
摘要： The present invention provides compounds of formula (I) along with methods of use thereof for the control of agricultural pests, particularly fungal pests, weedy pests and insect pests, as well as use as pharmaceuticals, particularly the treatment of obesity, metabolic syndrome, atherosclerosis, cardiovascular disease and insulin resistance, e.g., type II or adult-onset diabetes as well as fungal pathogens of humans and animals.
摘要翻译：本发明提供式（I）化合物及其用于控制农业害虫，特别是真菌害虫，杂草害虫和害虫的方法，以及用作药物，特别是用于治疗肥胖症，代谢综合征，动脉粥样硬化，心血管疾病和胰岛素抵抗，例如II型或成人发病的糖尿病以及人和动物的真菌病原体。

99. 发明申请

WO2008084004A1 SULFONAMIDE DERIVATIVES AS CHYMASE INHIBITORS 审中-公开
标题翻译：磺酰胺衍生物作为CHYMAS抑制剂
公开(公告)号：WO2008084004A1
公开(公告)日：2008-07-17
申请号：PCT/EP2008/050027
申请日：2008-01-03
申请人： F. HOFFMANN-LA ROCHE AG , BANNER, David , MAUSER, Harald , MINDER, Rudolf E. , WESSEL, Hans P.
发明人： BANNER, David , MAUSER, Harald , MINDER, Rudolf E. , WESSEL, Hans P.
IPC分类号： C07D213/42 , C07D333/62 , C07D401/12 , C07D403/12 , C07D409/12 , A61K31/4436 , A61P11/00
CPC分类号： C07D333/62 , C07D213/42 , C07D401/12 , C07D403/12 , C07D409/12
摘要： The invention is concerned with novel sulfonamide derivatives of formula (I) wherein A, R 1 to R 2'' , X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型磺酰胺衍生物，其中A，R 1至R 2“，X和Y如说明书和以及其生理上可接受的盐。这些化合物抑制胃促胰酶，可用作药物。

100. 发明申请

WO2008008660B1 CYCLOPENTANE DERIVATIVES AS ANTIGLAUCOMA AGENTS 审中-公开
标题翻译：环戊烷衍生物作为抗玻尿酸药物
公开(公告)号：WO2008008660B1
公开(公告)日：2008-05-15
申请号：PCT/US2007072632
申请日：2007-07-02
申请人： ALLERGAN INC , OLD DAVID W , NGO VINH X
发明人： OLD DAVID W , NGO VINH X
IPC分类号： C07C59/72 , A61K31/192 , A61K31/275 , A61K31/34 , A61K31/381 , A61K31/395 , A61K31/426 , A61P27/06 , C07C255/57 , C07D213/61 , C07D277/56 , C07D307/80 , C07D333/36 , C07D409/12 , C07F9/38
CPC分类号： C07C65/40 , C07C33/50 , C07C59/88 , C07C59/90 , C07C65/36 , C07C69/007 , C07C69/738 , C07C69/78 , C07C255/57 , C07C313/04 , C07C325/02 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07C405/0033 , C07C405/0041 , C07C405/0075 , C07C2601/08 , C07C2602/08 , C07D213/55 , C07D213/57 , C07D213/61 , C07D215/06 , C07D257/04 , C07D277/56 , C07D307/68 , C07D307/79 , C07D333/16 , C07D333/38 , C07D333/62 , C07D405/12 , C07D409/10 , C07D409/12 , C07D417/10 , C07F9/3834 , C07F9/588
摘要： Disclosed and described herein are compounds of the formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed and described.
摘要翻译：本文公开并描述了式（I）的化合物或其药学上可接受的盐，或其前药。还公开和描述了与其相关的治疗方法，组合物和药物。

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