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公开(公告)号：WO2006046593A1
公开(公告)日：2006-05-04
申请号：PCT/JP2005/019676
申请日：2005-10-26
IPC分类号： C07C65/24 , C07C65/26 , C07C65/28 , C07C65/30 , C07C65/34 , C07C65/40 , C07C217/80 , C07C205/35 , C07C235/34 , C07C235/46 , C07C255/57 , C07C311/04 , C07C311/08 , C07C311/25 , C07C317/06 , C07C317/22 , C07C317/46 , A61K31/192 , A61K31/216 , C07D239/26 , A61K31/506 , A61K31/24 , C07D213/79 , A61K31/4418 , C07D213/55 , C07D213/65 , C07D213/80 , A61K31/455 , C07D213/71 , C07D307/84 , A61K31/343 , C07D257/04 , A61K31/41 , C07D333/24 , A61K31/381 , C07D277/30 , A61K31/425
CPC分类号： C07C217/80 , C07C45/00 , C07C45/673 , C07C45/68 , C07C47/565 , C07C65/24 , C07C65/30 , C07C65/34 , C07C65/40 , C07C69/78 , C07C69/88 , C07C69/92 , C07C69/94 , C07C205/35 , C07C235/34 , C07C235/46 , C07C255/57 , C07C311/04 , C07C311/08 , C07C317/22 , C07C317/46 , C07C323/62 , C07D213/55 , C07D213/65 , C07D213/71 , C07D213/79 , C07D213/80 , C07D239/26 , C07D257/04 , C07D277/30 , C07D307/84 , C07D333/24
摘要： Disclosed is an excellent LXR modulator. Specifically disclosed is a compound represented by the general formula (I) below or the like. (I) [In the formula, R 1 represents a -COR 9 (wherein R 9 represents an alkyl, optionally substituted alkoxy or optionally substituted amino); R 2 represents an H, OH, alkoxy, optionally substituted amino or the like; R 3 represents an H, optionally substituted alkyl, cycloalkyl, optionally substituted alkoxy, optionally substituted amino, halogeno or the like; R 4 and R 5 respectively represent an H, optionally substituted alkyl, halogeno or the like; R 6 and R 7 respectively represent an H or alkyl; R 8 represents a -X 2 R 10 [wherein R 10 represents a -COR 11 (wherein R 11 represents an OH, optionally substituted alkoxy, optionally substituted amino or the like), -SO 2 R 12 (wherein R 12 represents an optionally substituted alkyl, optionally substituted amino or the like), tetrazole-5-yl or the like; and X 2 represents a single bond, optionally substituted alkylene or the like]; X 1 represents an -NH-, -O-, -S- or the like; Y 1 represents an optionally substituted phenyl or optionally substituted 5-membered or 6-membered aromatic heterocyclyl; and Y 2 represents an optionally substituted aryl, substituted heterocyclyl or the like.]
摘要翻译： 公开了优良的LXR调节剂。 具体公开了下述通式（I）表示的化合物等。 （I）[式中，R 1表示-COR 9（其中R 9表示烷基，任意取代的烷氧基或任意取代的 氨基）; R 2表示H，OH，烷氧基，任选取代的氨基等; R 3表示H，任选取代的烷基，环烷基，任选取代的烷氧基，任选取代的氨基，卤代等; R 4和R 5分别表示H，任选取代的烷基，卤代等; R 6和R 7分别表示H或烷基; R 8表示一个-X 2 O 2 R 10，其中R 10表示-COR 11， （其中R 11表示OH，任选取代的烷氧基，任选取代的氨基等），-SO 2 R 12（其中R 11表示OH，任选取代的烷氧基，任选取代的氨基等） 其中R 12表示任选取代的烷基，任选取代的氨基等），四唑-5-基等; 和X 2表示单键，任选取代的亚烷基等]; X 1表示-NH-，-O-，-S-等; Y 1表示任选取代的苯基或任选取代的5元或6元芳族杂环基; 和Y 2表示任选取代的芳基，取代的杂环基等。]
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2.发明申请PROCESS FOR PREPARING OPTICALLY ACTIVE alpha -HYDROXY ACIDS AND DERIVATIVES THEREOF 审中-公开制备光活性α-羟基酸及其衍生物的方法
公开(公告)号：WO01040153A1
公开(公告)日：2001-06-07
申请号：PCT/US1999/028440
申请日：1999-12-02
IPC分类号： C07D317/72 , C07B53/00 , C07C51/00 , C07C51/09 , C07C59/105 , C07C59/11 , C07C67/00 , C07C69/732 , C07C303/40 , C07C311/10 , C07C311/25 , C07D307/94 , C07C35/22 , C07C35/24 , C07C43/30 , C07C43/32 , C07C45/00 , C07C59/01 , C07C69/66 , C07C69/76 , C07C309/65
CPC分类号： C07D307/94 , C07B2200/07 , C07C51/09 , C07C67/00 , C07C303/40 , C07C59/08 , C07C59/105 , C07C59/50 , C07C59/42 , C07C69/732 , C07C311/10
摘要： The present invention provides a process for preparing optically active alpha -hydroxy acids and derivatives thereof by subjecting the alkylated 1,3-dioxolanones of formula (IV) wherein R1 and R2 are the same or different and are each independently H or C1-6 alkyl; R5 is H, C1-16 alkyl, or unsubstituted or substituted phenyl; and R6 is C1-8 alkyl, C2-7 alkenyl or unsubstituted or substituted benzyl, to either alcoholysis or hydrolysis, in which the alkylated 1,3-dioxolanones are obtained by using 10-camphorsulfonamide as a chiral auxiliary.
摘要翻译： 本发明提供了通过使式（Ⅳ）的烷基化1,3-二氧戊环酮（其中R 1和R 2相同或不同且各自独立地为H或C 1-6烷基）而制备光学活性α-羟基酸及其衍生物的方法 ; R5是H，C1-16烷基，或未取代或取代的苯基; 并且R6是C1-8烷基，C2-7链烯基或未取代或取代的苄基，用于醇解或水解，其中通过使用10-樟脑磺酰胺作为手性助剂获得烷基化1,3-二氧戊环。
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3.发明申请CARBOCYCLIC SIDE CHAIN CONTAINING, N-SUBSTITUTED METALLOPROTEASE INHIBITORS 审中-公开含有碳链的侧链，N-取代的金属蛋白酶抑制剂
公开(公告)号：WO0170720A3
公开(公告)日：2002-02-28
申请号：PCT/US0108782
申请日：2001-03-20
申请人： PROCTER & GAMBLE , NATCHUS MICHAEL GEORGE , PIKUL STANISLAW , ALMSTEAD NEIL GREGORY , LAUFERSWEILER MATTHEW J , BISWANATH DE
发明人： NATCHUS MICHAEL GEORGE , PIKUL STANISLAW , ALMSTEAD NEIL GREGORY , LAUFERSWEILER MATTHEW J , DE BISWANATH
IPC分类号： C07D295/14 , A61K31/198 , A61K31/357 , A61K31/36 , A61K31/4015 , A61K31/4172 , A61K31/421 , A61K31/425 , A61K31/535 , A61P19/02 , A61P29/00 , A61P35/00 , C07C311/29 , C07D207/26 , C07D207/27 , C07D233/72 , C07D233/74 , C07D235/02 , C07D263/20 , C07D263/22 , C07D265/10 , C07D265/32 , C07D275/02 , C07D295/155 , C07D317/72 , C07D319/08 , C07C311/19 , C07C311/25
CPC分类号： C07D207/27 , C07C311/29 , C07C2601/14 , C07D233/72 , C07D235/02 , C07D263/20 , C07D265/10 , C07D265/32 , C07D275/02 , C07D295/155 , C07D317/72 , C07D319/08
摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R , R , R , n, A, E, E', L, L', G and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
摘要翻译： 公开了作为金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，化合物具有下式（I）的结构：其中R 1，R 2，R 3，n，A，E，E'，L，L'，G和Z 具有说明书和权利要求书中描述的含义，以及式I的光学异构体，非对映异构体和对映异构体及其药学上可接受的盐，可生物水解的酰胺，酯和酰亚胺。 还描述了包含这些化合物的药物组合物，以及使用该化合物或药物组合物治疗金属蛋白酶相关疾病的方法。
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公开(公告)号：WO0170682A3
公开(公告)日：2002-01-31
申请号：PCT/US0108784
申请日：2001-03-20
申请人： PROCTER & GAMBLE , NATCHUS MICHAEL GEORGE , PIKUL STANISLAW , ALMSTEAD NEIL GREGORY , LAUFERSWEILER MATTHEW J , BOOKLAND ROGER GUNNARD , TULLIS JOSHUA S , BISWANATH DE
发明人： NATCHUS MICHAEL GEORGE , PIKUL STANISLAW , ALMSTEAD NEIL GREGORY , LAUFERSWEILER MATTHEW J , BOOKLAND ROGER GUNNARD , TULLIS JOSHUA S , DE BISWANATH
IPC分类号： C07D233/78 , A61K31/198 , A61K31/357 , A61K31/36 , A61K31/4015 , A61K31/4164 , A61K31/4166 , A61K31/421 , A61K31/426 , A61K31/535 , A61K31/5375 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C311/29 , C07D207/26 , C07D207/27 , C07D233/72 , C07D235/02 , C07D263/20 , C07D263/24 , C07D265/10 , C07D265/32 , C07D275/02 , C07D295/096 , C07D317/72 , C07D319/08 , C07C311/19 , C07C311/25
CPC分类号： C07D207/27 , C07C311/29 , C07C2601/14 , C07D233/72 , C07D235/02 , C07D263/20 , C07D265/10 , C07D265/32 , C07D275/02 , C07D295/096 , C07D317/72 , C07D319/08
摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to Formula (I) where R , R , n, A, E, E', L, L', G and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
摘要翻译： 公开了作为金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，化合物具有式（I）的结构，其中R 1，R 2，n，A，E，E'，L，L'，G和Z具有说明书和 权利要求书，以及式（I）的光学异构体，非对映异构体和对映体及其药学上可接受的盐，生物可水解的酰胺，酯和酰亚胺。 还描述了包含这些化合物的药物组合物，以及使用该化合物或药物组合物治疗金属蛋白酶相关疾病的方法。
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5.发明申请N-SUBSTITUTED AMINOTETRALINS AS LIGANDS FOR THE NEUROPEPTIDE Y Y5 RECEPTOR USEFUL IN THE TREATMENT OF OBESITY AND OTHER DISORDERS 审中-公开作为治疗肥胖和其他疾病的神经病毒Y Y5受体的配体的N-取代的氨基葡萄糖
公开(公告)号：WO99055667A1
公开(公告)日：1999-11-04
申请号：PCT/US1999/007971
申请日：1999-04-12
IPC分类号： A61K31/18 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/415 , A61K31/4164 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/12 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07C311/05 , C07C311/15 , C07C311/18 , C07C311/20 , C07C311/21 , C07C311/22 , C07C311/25 , C07C311/29 , C07C311/37 , C07C311/41 , C07C317/14 , C07D213/16 , C07D213/38 , C07D233/54 , C07D233/64 , C07D307/52 , C07D333/20 , C07D333/34
CPC分类号： C07D233/64 , C07C311/18 , C07C311/29 , C07C311/37 , C07C317/14 , C07D213/38 , C07D307/52 , C07D333/20 , C07D333/34
摘要： beta -Aminotetralin derivatives of formula (1): which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a beta -aminotetralins derivative as the active ingredient are described. The beta -aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.
摘要翻译： 描述了作为神经肽Y Y5（NPY5）受体的配体的制备方法和含有β-氨基托萘林衍生物作为活性成分的药物组合物的式（1）的β-氨基-1,2,3,4-四氢喹啉衍生物。 β-aminotetralins可用于治疗与NPY受体亚型Y5相关的疾病和疾病。
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