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21. 发明申请

US20060052627A1 Novel modulators of the PPAR-type receptors and cosmetic/pharmaceutical compositions comprised thereof 审中-公开
标题翻译： PPAR型受体的新型调节剂及其组合的美容/药物组合物
公开(公告)号：US20060052627A1
公开(公告)日：2006-03-09
申请号：US11202019
申请日：2005-08-12
申请人： Philippe Diaz , Etienne Thoreau , Isabelle Carlavan , Pascale Mauvais , Johannes Voegel
发明人： Philippe Diaz , Etienne Thoreau , Isabelle Carlavan , Pascale Mauvais , Johannes Voegel
IPC分类号： C07D241/02 , C07D239/02 , C07D237/02 , C07C229/40
CPC分类号： C07C323/62
摘要： Novel compounds which modulate PPAR-type receptors have the following general formula (I): and are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology and in the fields of cardiovascular diseases, immune diseases and/or diseases linked to lipid metabolism), or are formulated into cosmetic compositions.
摘要翻译：调节PPAR-型受体的新型化合物具有以下通式（I）：

22. 发明申请

US20040209957A1 Tetrafluorobenzyl derivatives and pharmaceutical composition for preventing and treating acute and chronic neurodegenerative diseases in central nervous system containing the same 有权
标题翻译：四氟苄基衍生物和用于预防和治疗含有其的中枢神经系统中的急性和慢性神经变性疾病的药物组合物
公开(公告)号：US20040209957A1
公开(公告)日：2004-10-21
申请号：US10481648
申请日：2003-12-22
发明人： Byoung-Joo Gwag , Sung-Hwa Yoon , Ho-Sang Moon , Eun-Chan Park , Seok-Joon Won , Young-Ae Lee , Hae-Un Lee
IPC分类号： A61K031/195 , C07C229/40
CPC分类号： C07C215/76 , A61K31/136 , C07C229/60 , C07C229/64 , C07C235/60 , C07C309/49 , C07C2601/14
摘要： The present invention relates to a tetrafluorobenzyl derivative and a pharmaceutical composition for prevention and treatment of acute and chronic neurodegenerative disease in central nervous system and ophthalmic diseases containing the same. The tetrafluorobenzyl derivative of the present invention can effectively be used to prevent and treat chronic neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease, degenerative brain disease such as epilepsy and ischemic brain disease such as stroke.
摘要翻译：本发明涉及四氟苄基衍生物和用于预防和治疗中枢神经系统中的急性和慢性神经变性疾病的药物组合物和含有它们的眼科疾病。本发明的四氟苄基衍生物可有效地用于预防和治疗慢性神经变性疾病如阿尔茨海默病，帕金森病和亨廷顿病，退行性脑病如癫痫和脑缺血性脑疾病如中风。

23. 发明申请

US20040082793A1 Methods of ortho alkylation 失效
标题翻译：邻位烷基化方法
公开(公告)号：US20040082793A1
公开(公告)日：2004-04-29
申请号：US10468637
申请日：2003-08-20
发明人： Gary David Annis , Richard James Brown , Albert Loren Casalnuovo , Stephen Ernest Jacobson , Philip Osborne Moss
IPC分类号： C07D213/63 , C07C069/88 , C07C229/40
CPC分类号： C07D213/73 , C07C67/297 , C07C68/06 , C07C209/68 , C07C211/52 , C07C213/08 , C07C227/16 , C07C231/12 , C07C231/14 , C07C233/25 , C07C317/28 , C07C319/14 , C07C323/29 , C07C381/10 , C07D213/64 , C07D213/68 , C07D213/75 , C07D213/76 , C07C69/017 , C07C69/24 , C07C69/96 , C07C233/15 , C07C69/63 , C07C69/157 , C07C69/16
摘要： The present invention pertains to methods for preparing a compound of Formula (I), wherein A is O or NnullL; each L is independently H or an acyl group; K is, together with the two contiguous linking carbon atoms, a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system wherein each ring or ring system is optionally substituted; R1is H, C1 to C4 alkyl or CO2R3; R2 is H or C1 to C4 alkyl; and R3 is C1 to C4 alkyl; comprising hydrogenating a compound of Formula (II), wherein n is 0, 1 or 2 in the presence of a catalyst comprising palladium to form the compound of Formula (I). This invention further pertains to methods for preparing compounds of Formula (II) useful for preparing compounds of Formula (I). This invention also pertains to compounds used in these methods. 1
摘要翻译：本发明涉及制备式（I）化合物的方法，其中A为O或N-L; 每个L独立地是H或酰基; K与两个相邻的连接碳原子连同苯环，5或6元杂芳环或芳族8,9-或10元稠合的碳双环或杂双环系统，其中每个环或环系是任选取代; R 1是H，C 1至C 4烷基或CO 2 R 3; R 2是H或C 1至C 4烷基; 且R 3为C 1至C 4烷基; 包括在包含钯的催化剂存在下氢化式（II）化合物，其中n为0,1或2，以形成式（I）化合物。本发明还涉及制备可用于制备式（I）化合物的式（II）化合物的方法。本发明还涉及用于这些方法的化合物。

24. 发明申请

US20040044238A1 Optically active diamines and their use in catalytic processes 失效
标题翻译：光活性二胺及其在催化过程中的应用
公开(公告)号：US20040044238A1
公开(公告)日：2004-03-04
申请号：US10643855
申请日：2003-08-19
发明人： Jurgen Kocher
IPC分类号： C07F009/02 , C07C255/31 , C07C229/40
CPC分类号： C07C255/24 , B01J31/1805 , B01J2231/643 , B01J2531/26 , B01J2531/845 , C07B2200/07 , C07C29/143 , C07C229/16 , C07C229/76 , C07C237/06 , C07C2601/14 , C07F9/4006 , C07C33/20 , C07C33/46
摘要： The invention relates to stereoisomerically enriched diamines, to metal complexes comprising these diamines and also to their use in a process for asymmetrically reducing ketones using silanes, in particular polymethylhydrosiloxane, as reducing agents.
摘要翻译：本发明涉及立体异构体富集的二胺，包括这些二胺的金属络合物，也涉及它们在使用硅烷，特别是聚甲基氢硅氧烷作为还原剂的不对称还原酮的方法中的用途。

25. 发明授权

US6111115A Preparation of 2-(10,11-dihydro-10-oxodibenzo-[b,f]thiepin-2-yl) propionic acid 失效
标题翻译：制备2-（10,11-二氢-10-氧代二苯并[b，f]硫杂-2-基）丙酸
公开(公告)号：US6111115A
公开(公告)日：2000-08-29
申请号：US242483
申请日：1999-02-17
申请人： Masao Yamamoto , Kunio Kobayashi , Katsumasa Harada , Shigeyoshi Nishino , Hiroshi Sasaki
发明人： Masao Yamamoto , Kunio Kobayashi , Katsumasa Harada , Shigeyoshi Nishino , Hiroshi Sasaki
IPC分类号： C07D337/14 , C07C205/56 , C07C229/40 , C07C323/62 , C07C205/00 , C07C229/00
CPC分类号： C07D337/14
摘要： A process for preparation of 2-(10,11-dihydro-10-oxodibenzo[b,f]thiepin-2-yl)propionic acid (i.e., Zaltoprofen) is performed by subjecting 2-(4-amino-3-carboxy-methylphenyl)propionic acid or its salt to diazotization and subsequent reaction with thiophenol to produce 2-(3-carboxymethyl-4-phenylthiophenyl)propionic acid or its salt, and subjecting the product to cyclization reaction. Other related processes and related compounds are also disclosed.
摘要翻译： PCT No.PCT / JP97 / 02922 Sec。 371日期1999年2月17日 102（e）日期1999年2月17日PCT提交1997年8月22日PCT公布。第WO98 / 07717号公报日期：1998年2月26日制备2-（4-甲氧基二苯并[b，f]硫杂-2-基）丙酸（即扎洛芬）的方法， -3-羧基 - 甲基苯基）丙酸或其盐进行重氮化，随后与苯硫酚反应，生成2-（3-羧甲基-4-苯硫基苯基）丙酸或其盐，并使产物环化反应。还公开了其它相关方法和相关化合物。

26. 发明授权

US5874473A Substituted cycloalkanecarboxylic acid derivatives as matrix metalloprotease inhibitors 失效
标题翻译：取代的环烷烃羧酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5874473A
公开(公告)日：1999-02-23
申请号：US864666
申请日：1997-05-28
申请人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , Kerry Jeanne Combs , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , Jill Elizabeth Wood , Stephan Schneider
发明人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , Kerry Jeanne Combs , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , Jill Elizabeth Wood , Stephan Schneider
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , C07C321/00
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the subscript "e" is 2 or 3; the group R.sup.14 represents a variety of possible substituent groups on the cycloalkyl ring between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
摘要翻译：基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。本发明的化合物具有通用化合物“IMAGE”，其中每个T是取代基; x为0,1或2; 组D表示，下标“e”为2或3; 基团R14表示D和G之间的环烷基环上各种可能的取代基，基团G表示M，其中M表示-CO 2 H，-CON（R 11）2或-CO 2 R 12; R13表示19个非环状天然氨基酸的任一侧链。

27. 发明授权

US5854277A Thiophenebutanoic acid derivatives as matrix metalloprotease inhibitors 失效
标题翻译：噻吩丁酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5854277A
公开(公告)日：1998-12-29
申请号：US865639
申请日：1997-05-30
申请人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , William Harrison Bullock , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , Jill Elizabeth Wood , David Ross Brittelli
发明人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , William Harrison Bullock , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , Jill Elizabeth Wood , David Ross Brittelli
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , A61K31/38 , A61K31/41 , A61K31/415 , A61K31/435
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
摘要翻译：基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。本发明的化合物具有通用化合物“IMAGE”，其中每个T是取代基; x为0,1或2; 基团D表示基团R6表示D和G之间的碳链上的各种可能的取代基，基团G表示M，其中M表示-CO 2 H，-CON（R 11）2，或-CO 2 R 12; R13表示19个非环状天然氨基酸的任一侧链。

28. 发明授权

US5654452A Lipophilic contrast agents for use in hepatocyte-selective oil-in-water emulsions 失效
标题翻译：用于肝细胞选择性水包油乳剂的亲脂性造影剂
公开(公告)号：US5654452A
公开(公告)日：1997-08-05
申请号：US477388
申请日：1995-06-07
申请人： Rolf Lohrmann , Dung K. Hong
发明人： Rolf Lohrmann , Dung K. Hong
IPC分类号： A61K9/127 , A61K9/107 , A61K49/04 , C07C69/65 , C07C69/76 , C07C229/40 , C07C229/42 , C07C233/18 , C07C237/20 , C07C237/46 , G07C233/00
CPC分类号： C07C229/42 , A61K49/0409 , A61K49/0461 , A61K9/1075 , C07C237/20 , C07C69/65 , C07C69/76
摘要： Aromatic acid-derived lipophilic polyhalogenated compounds are provided for use as contrast agents in diagnostic imaging or as therapeutic agents. These compounds are particularly useful when incorporated into an oil-in-water emulsion for tissue-specific delivery to the liver. For hepatocyte-selective delivery, the emulsion is chylomicron remnant-like by being in a size range of 50 to 200 nm and having a composition simulating naturally-occuring chylomicron remnants.
摘要翻译：提供芳族酸衍生的亲脂性多卤代化合物用作诊断成像中的造影剂或作为治疗剂。当掺入到水包油乳剂中用于组织特异性递送至肝脏时，这些化合物特别有用。对于肝细胞选择性递送，通过在50至200nm的尺寸范围内，该乳剂是乳糜微粒残留物，并具有模拟天然存在的乳糜微粒残留物的组成。

29. 发明授权

US5538940A .beta.-substituted cinnamic acid derivative 失效
标题翻译： β-取代肉桂酸衍生物
公开(公告)号：US5538940A
公开(公告)日：1996-07-23
申请号：US440126
申请日：1995-05-12
申请人： Hubert Sauter , Herbert Bayer , Klaus Oberdorf , Horst Wingert , Wolfgang Von Deyn , Wassilios Grammenos , Hartmann Koenig , Harald Rang , Franz Roehl , Gisela Lorenz , Eberhard Ammermann
发明人： Hubert Sauter , Herbert Bayer , Klaus Oberdorf , Horst Wingert , Wolfgang Von Deyn , Wassilios Grammenos , Hartmann Koenig , Harald Rang , Franz Roehl , Gisela Lorenz , Eberhard Ammermann
IPC分类号： C07C69/618 , A01N37/36 , A01N37/38 , A01N37/44 , A01N37/48 , A01N43/08 , A01N43/10 , A01N43/36 , A01N43/56 , A01N43/74 , A01N43/78 , A01N43/80 , A01N43/82 , A61K31/21 , A61K31/40 , A61K31/505 , C07C67/343 , C07C69/65 , C07C69/734 , C07C69/736 , C07C69/738 , C07C69/75 , C07C69/76 , C07C69/84 , C07C69/86 , C07C69/92 , C07C69/94 , C07C205/34 , C07C205/38 , C07C205/56 , C07C229/40 , C07C229/44 , C07C233/11 , C07C235/32 , C07C235/34 , C07C251/38 , C07C251/48 , C07C251/52 , C07C251/60 , C07C251/66 , C07C255/57 , C07C255/64 , C07C275/64 , C07C309/66 , C07C309/73 , C07C311/09 , C07C311/21 , C07C311/29 , C07C313/04 , C07C313/06 , C07C317/44 , C07C317/46 , C07C323/56 , C07C323/62 , C07C327/22 , C07C327/48 , C07D207/32 , C07D207/335 , C07D207/337 , C07D213/53 , C07D213/64 , C07D213/643 , C07D213/66 , C07D213/68 , C07D213/70 , C07D215/22 , C07D215/227 , C07D215/233 , C07D215/36 , C07D231/12 , C07D233/84 , C07D235/28 , C07D239/52 , C07D249/12 , C07D257/04 , C07D261/08 , C07D263/32 , C07D263/34 , C07D263/58 , C07D271/06 , C07D271/10 , C07D271/113 , C07D277/28 , C07D277/30 , C07D277/36 , C07D277/68 , C07D277/74 , C07D285/12 , C07D285/125 , C07D307/46 , C07D307/52 , C07D307/54 , C07D309/06 , C07D333/24 , C07D409/04 , C07D413/04 , C07D513/04 , C07D521/00 , C07F7/08 , A01N37/18
CPC分类号： C07D207/335 , A01N37/36 , A01N37/38 , A01N37/48 , A01N43/08 , A01N43/10 , A01N43/36 , A01N43/56 , A01N43/74 , A01N43/80 , A01N43/82 , C07C205/34 , C07C205/38 , C07C205/56 , C07C229/44 , C07C251/48 , C07C251/52 , C07C251/60 , C07C255/64 , C07C275/64 , C07C309/66 , C07C309/73 , C07C311/09 , C07C311/21 , C07C311/29 , C07C313/04 , C07C313/06 , C07C317/46 , C07C323/56 , C07C323/62 , C07C327/22 , C07C327/48 , C07C69/734 , C07C69/736 , C07D207/337 , C07D213/53 , C07D213/643 , C07D213/66 , C07D213/68 , C07D213/70 , C07D215/227 , C07D215/233 , C07D215/36 , C07D231/12 , C07D233/56 , C07D233/84 , C07D235/28 , C07D239/52 , C07D249/08 , C07D249/12 , C07D257/04 , C07D261/08 , C07D263/32 , C07D263/34 , C07D263/58 , C07D271/06 , C07D271/113 , C07D277/28 , C07D277/30 , C07D277/36 , C07D277/74 , C07D285/12 , C07D285/125 , C07D307/46 , C07D307/52 , C07D307/54 , C07D309/06 , C07D333/24 , C07D409/04 , C07D413/04 , C07D513/04 , C07F7/0818 , C07C2101/14 , C07C2102/08
摘要： .beta.-Substituted cinnamic acid derivatives of the formula 1, ##STR1## where R.sup.1 is substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, and R.sup.1 can also be chlorine or bromine,--X-- is --O--, --S--, ##STR2## m is 0 or 1, --Y is --OR.sup.4, --O--N.dbd.CR.sup.5 R.sup.6, --NR.sup.7 R.sup.8, --NR.sup.7 R.sup.8, --N(OR.sup.9)R.sup.10 or SR.sup.11, where the abovementioned substitutes R.sup.2 to R.sup.11 are substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, and R.sup.2, R.sup.3 and R.sup.5 to R.sup.11 can be hydrogen and Z, U, V, W are defined in the specification.
摘要翻译：式1的β取代肉桂酸衍生物，其中R 1是取代或未取代的烷基，烯基，炔基，环烷基或环烯基，R 1也可以是氯或溴，-X-是-O-，-S - ， - Y是-OR 4，-ON = CR 5 R 6，-NR 7 R 8，-NR 7 R 8，-N（OR 9）R 10或SR 11，其中上述取代基R 2至R 11是取代或未取代的烷基，烯基，炔基，环烷基或环烯基，R2，R3和R5至R11可以是氢，Z，U，V，W在说明书中定义。

30. 发明授权

US5482942A (3,4-dioxocyclobuten-1-yl)chromene, indene, and dihydronaphthalenone derivatives as smooth muscle relaxants 失效
标题翻译：（3,4-二氧杂环丁烯-1-基）色烯，茚和二氢萘酮衍生物作为平滑肌松弛剂
公开(公告)号：US5482942A
公开(公告)日：1996-01-09
申请号：US267691
申请日：1994-06-28
申请人： Richard M. Soll , Paul J. Dollings
发明人： Richard M. Soll , Paul J. Dollings
IPC分类号： A61K31/35 , A61K31/352 , A61P9/00 , A61P9/02 , A61P11/00 , A61P13/02 , A61P15/00 , C07C225/20 , C07D311/58 , A61K31/495 , A61K31/415 , C07C229/40 , C07D211/82 , C07D241/02 , C07D311/74 , C07D407/02
CPC分类号： C07D311/58
摘要： This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.1-6 perfluoroacylamino, mono or di-C.sub.1-12 alkylamino, C.sub.1-6 alkylsulfonyl, C.sub.6-10 arylsulfonyl, carboxyl, C.sub.1-12 mono or di-alkylaminocarbonyl, or hydrogen;a and b together form an --O-- linkage, C.dbd.O, or a direct bond:R.sub.3 and R.sub.4, independent from each other, are H or C.sub.1-6 alkyl, optionally substituted by fluorine;R.sub.5 is amino or C.sub.1-12 mono alkylamine;R.sub.6 is H, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.6-10 aryl, or mono or bicyclic heteroaryl containing 1-3 heteroatoms selected from N, O, or S.
摘要翻译：本发明涉及具有平滑肌松弛活性的新型4-（3,4-二氧杂环丁烯-1-基）色烯和二氢萘酮及其3-（3,4-二氧杂环丁烯-1-基）茚及其盐，用于治疗高血压以及治疗周围血管疾病，充血性心力衰竭，涉及尿路过度平滑肌收缩的疾病，例如失禁或胃肠道，例如肠易激综合征，哮喘和脱发，以及药物组合物含有发明化合物。本发明公开了由式（I）表示的化合物：其中：R 1和R 2彼此独立地选自如下：C 1-6全氟烷氧基，C 1-6全氟烷基，C 1-6烷基，C 1 1-6烷氧基，羟基，C 1-6烷氧基羰基，硝基，氰基，卤素，C 1-6烷基磺酰氨基，C 1-6全氟烷基磺酰氨基，氨基，C 1-6酰氨基，C 1-6全氟酰基氨基，单或二-C 1-12烷基氨基， 6烷基磺酰基，C 6-10芳基磺酰基，羧基，C 1-12单或二烷基氨基羰基或氢; a和b一起形成O-键，C = O或直接键：R 3和R 4彼此独立地是H或任选被氟取代的C 1-6烷基; R5是氨基或C1-12单烷基胺; R 6是H，C 1-6全氟烷基，C 1-6烷基，C 6-10芳基或含有1-3个选自N，O或S的杂原子的单或双环杂芳基。

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