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11. 发明授权

US5668180A Alkoxyaryl compounds 失效
标题翻译：烷氧基芳基化合物
公开(公告)号：US5668180A
公开(公告)日：1997-09-16
申请号：US655439
申请日：1996-05-30
申请人： Daniel Lesieur , Patrick Depreux , Veronique Leclerc , Philippe Delagrange , Pierre Renard
发明人： Daniel Lesieur , Patrick Depreux , Veronique Leclerc , Philippe Delagrange , Pierre Renard
IPC分类号： A61K31/165 , A61K31/17 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61P3/08 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/28 , A61P35/00 , A61P43/00 , C07C233/18 , C07C233/19 , C07C233/60 , C07C275/10 , C07C275/24 , C07C327/42 , C07C335/12 , C07D209/08 , C07D209/16 , C07D307/78 , C07D307/81 , C07D333/58 , A61K31/16 , C07C233/05
CPC分类号： C07C233/18 , C07C233/60 , C07D209/16 , C07D307/81 , C07D333/58 , C07C2101/02 , C07C2101/04 , C07C2101/14 , C07C2101/16 , C07C2102/10 , Y10S514/929
摘要： A compound selected from those of formula (I): ##STR1## in which A, R, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the description,and a medicinal product containing the same useful for treating a disorder of the melatoninergic system.
摘要翻译：选自式（I）的化合物：其中A，R，Y，R 1，R 2和R 3如说明书中所定义的其中含有相同用途的药物产品褪黑激素系统。

12. 发明授权

US5578595A Cyclopropylacetic acid derivatives 失效
标题翻译：环丙基乙酸衍生物
公开(公告)号：US5578595A
公开(公告)日：1996-11-26
申请号：US407741
申请日：1995-03-21
申请人： Manfred B oger
发明人： Manfred B oger
IPC分类号： A01N33/04 , A01N37/12 , A01N37/18 , A01N43/10 , A01N43/28 , A01N43/34 , A01N43/36 , A01N43/48 , A01N43/824 , A01N43/828 , A01P7/02 , A01P7/04 , C07C67/08 , C07C67/307 , C07C69/56 , C07C69/635 , C07C69/743 , C07C233/19 , C07C233/60 , C07C321/28 , C07C321/30 , C07C323/20 , C07D213/63 , C07D213/64 , C07D213/647 , C07D233/68 , C07D237/14 , C07D239/34 , C07D241/20 , C07D249/08 , C07D249/14 , C07D285/08 , C07D285/12 , C07D307/40 , C07D307/58 , C07D307/64 , C07D333/16 , C07D333/18 , C07D333/32 , C07D333/34 , A01N43/58 , C07C69/74 , C07C233/00 , C07D211/72 , C07D233/40 , C07D237/02 , C07D333/24
CPC分类号： C07D213/647 , C07C233/19 , C07C323/20 , C07C69/56 , C07C69/635 , C07D285/08 , C07C2101/02
摘要： Novel 2-(2,2-difluorocyclopropyl)-acetic acid derivatives of formula I ##STR1## wherein A is oxygen or --NR.sub.1 --,B is C.sub.2 -C.sub.6 alkylene,D is oxygen, sulfur or --O--CH.sub.2 --,E is phenyl; phenyl substituted by from one to three substituents selected from the group halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 haloalkyl and C.sub.1 -C.sub.4 alkoxy; a five-membered aromatic heterocycle having from one to three hetero atoms selected from the group nitrogen, oxygen and sulfur; a five-membered aromatic heterocycle having from one to three hetero atoms selected from the group nitrogen, oxygen and sulfur that is substituted by one or two substituents selected from the group halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.3 haloalkyl; a six-membered aromatic heterocycle having from one to three nitrogen atoms; or a six-membered aromatic heterocycle having from one to three nitrogen atoms that is substituted by one or two substituents selected from the group halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.3 haloalkyl,L is halogen or methyl,n is 0, 1 or 2, andR.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, phenylthio or tolylthio,can be used as pesticides. Especially insects and arachnids can be controlled.
摘要翻译：式I的新型2-（2,2-二氟环丙基） - 乙酸衍生物其中A是氧或-NR1-，B是C 2 -C 6亚烷基，D是氧，硫或-O-CH 2 - ， E是苯基; 被1至3个选自卤素，C 1 -C 4烷基，C 1 -C 3卤代烷基和C 1 -C 4烷氧基的取代基取代的苯基; 具有1至3个选自氮，氧和硫的杂原子的五元芳族杂环; 具有1至3个选自氮，氧和硫的杂原子的五元芳族杂环，其被一个或两个选自卤素，C 1 -C 4烷基和C 1 -C 3卤代烷基的取代基取代; 具有1至3个氮原子的6元芳族杂环; 或具有1至3个氮原子的6元芳族杂环，其被一个或两个选自卤素，C 1 -C 4烷基和C 1 -C 3卤代烷基的取代基取代，L是卤素或甲基，n是0,1或2， R1为氢，C1-C4烷基，苯硫基或甲苯硫基，可用作农药。特别是可以控制昆虫和蜘蛛。

13. 发明授权

US5565476A N-(hydroxyethyl)butanediamide derivatives 失效
标题翻译： N-（羟乙基）丁二酰胺衍生物
公开(公告)号：US5565476A
公开(公告)日：1996-10-15
申请号：US432409
申请日：1995-05-01
申请人： Paul C. Anderson , Teddy Halmos , Grace L. Jung , Marc-Andr e Poupart , Bruno Simoneau
发明人： Paul C. Anderson , Teddy Halmos , Grace L. Jung , Marc-Andr e Poupart , Bruno Simoneau
IPC分类号： A61K31/16 , A61K31/165 , A61K31/40 , A61K31/4015 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61P9/12 , A61P43/00 , C07C233/18 , C07C233/19 , C07C237/22 , C07D207/26 , C07D207/27 , C07D213/40 , C07D233/54 , C07D233/64 , C07D277/28 , C07D277/30 , C07D277/40 , C07D317/58 , C07D417/12
CPC分类号： C07D207/27 , C07C233/18 , C07C233/19 , C07D213/40 , C07D233/64 , C07D277/30 , C07D277/40 , C07D317/58 , C07C2101/02 , C07C2101/14
摘要： Disclosed herein are compounds of the formula:A'--N(R.sup.1')C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A' is, for example, HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1' is R.sup.7 R.sup.8 NC(O)CH.sub.2 wherein R.sup.7 is lower alkyl and R.sup.8 is pyridinyl-(CH.sub.2).sub.n wherein n is the integer one or two; R.sup.2 is, for example, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R), 3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
摘要翻译：本文公开的是下式的化合物：A'-N（R 1'）C（O）CH 2 CHR 2 C（O）-B，其中A'是例如HO-CR 5（R 6）CH 2，其中R 5和R 6与碳原子它们连接形成1,1-（低级环烷二基）; R 1'是R 7 R 8 NC（O）CH 2，其中R 7是低级烷基，R 8是吡啶基 - （CH 2）n，其中n是整数1或2; R2是例如4-噻唑基甲基或（2-氨基-4-噻唑基）甲基; B是肾素底物过渡态模拟物，例如[1（S） - （环己基甲基）-2（R），3（S） - 二羟基-5-甲基己基]氨基。该化合物抑制肾素活性，并被指示用于治疗高血压和充血性心力衰竭。

14. 发明授权

US5025017A Seco-mevinic acid derivatives useful as antihypercholesterolemic agents and new intermediates 失效
标题翻译：山梨酸衍生物可用作抗高胆固醇血症药物和新中间体
公开(公告)号：US5025017A
公开(公告)日：1991-06-18
申请号：US413656
申请日：1989-09-28
申请人： Donald S. Karanewsky
发明人： Donald S. Karanewsky
IPC分类号： C12N9/99 , A61K31/19 , A61K31/365 , A61K31/366 , A61K31/785 , A61K45/06 , A61P3/06 , A61P43/00 , C07C69/675 , C07C69/732 , C07C69/734 , C07C69/75 , C07C233/18 , C07C233/19 , C07D309/30 , C07D319/06 , C07D405/08 , C07D407/08 , C07D409/08 , C07F7/18
CPC分类号： C07D405/08 , C07C69/675 , C07D309/30 , C07D319/06 , C07D407/08 , C07D409/08 , C07F7/1856
摘要： Seco-mevinic acid derivatives are provided which has the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis. New intermediates for preparing the above seco-mevinic acid derivatives are also provided.

15. 发明授权

US4246198A Hindered phenolic amides 失效
标题翻译：受阻酚酰胺
公开(公告)号：US4246198A
公开(公告)日：1981-01-20
申请号：US37854
申请日：1979-05-10
申请人： Siegfried Rosenberger , Andreas Schmidt
发明人： Siegfried Rosenberger , Andreas Schmidt
IPC分类号： C08K5/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07C233/18 , C07C233/19 , C07C233/25 , C07C233/26 , C07C233/60 , C07C235/34 , C08K5/20 , C08L7/00 , C08L21/00 , C08L23/00 , C08L51/00 , C08L51/02 , C08L77/00 , C08L101/00 , C09K15/24 , C07C103/38 , C07C103/78
CPC分类号： C08K5/20 , C09K15/24
摘要： A phenol of the formulae I, II or III ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 are independent of one another and one of these is C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.6 -cycloalkyl or C.sub.7 -C.sub.9 -aralkyl and the others are hydrogen, C.sub.1 -C.sub.12 -alkyl or C.sub.5 -C.sub.6 -cycloalkyl, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independent of one another and one of these is C.sub.1 -C.sub.12 -alkyl or C.sub.5 -C.sub.6 -cycloalkyl and the others are hydrogen, C.sub.1 -C.sub.12 -alkyl or C.sub.5 -C.sub.6 cycloalkyl, or R.sub.4 and R.sub.5, or R.sub.6 and R.sub.7, together with the C atom which links them, form a 5-12-membered ring, R.sub.8, R.sub.9 and R.sub.10 are independent of one another and one of these is C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.6 -cycloalkyl or C.sub.7 -C.sub.9 -aralkyl and the others are hydrogen, C.sub.1 -C.sub.12 -alkyl or C.sub.5 -C.sub.6 -cycloalkyl, x and y independently of one another are 0, 1, 2 or 3, one of m and n is 1 and the other is 0 or 1, A is a monovalent, divalent or trivalent hydrocarbon radical which, in formula II, can also be interrupted by S, and Z is 1, 2 or 3, corresponding to the valency of A, and, in compounds of the formula II and III, m is 1 and R.sub.4 and R.sub.5 independently of one another are C.sub.1 -C.sub.12 -alkyl or C.sub.5 -C.sub.6 -cycloalkyl and, in compounds of the formula I, R.sub.6 can be bridged with A to form a carbocyclic structure as stabilizers for organic material.
摘要翻译：式Ⅰ，Ⅱ或Ⅲ的苯酚，其中R 1，R 2和R 3彼此独立，其中之一是C 1 -C 12 - （C 1 -C 12）烷基，C 5 -C 6 - 环烷基或C 7 -C 9 - 芳烷基，其余为氢，C 1 -C 12 - 烷基或C 5 -C 6 - 环烷基，R 4，R 5，R 6和R 7彼此独立，并且其中之一为C1- C 12 - 烷基或C 5 -C 6 - 环烷基，其余为氢，C 1 -C 12 - 烷基或C 5 -C 6环烷基，或者R 4和R 5或R 6和R 7与连接它们的C原子一起形成5-12- R 8，R 9和R 10彼此独立，其中之一为C 1 -C 12 - 烷基，C 5 -C 6 - 环烷基或C 7 -C 9 - 芳烷基，其余为氢，C 1 -C 12 - 烷基或C 5 -C 6 环烷基，x和y彼此独立地是0,1,2或3，m和n中的一个是1，另一个是0或1，A是一价，二价或三价烃基，其在式II中，也可以被S中断，Z是1,2或3，对应于A的化合价，并且在化合物中 Ia和III，m是1，R 4和R 5彼此独立地是C 1 -C 12 - 烷基或C 5 -C 6 - 环烷基，并且在式I的化合物中，R 6可以与A桥接以形成碳环结构作为稳定剂用于有机材料。

16. 发明授权

US09096619B2 Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy 有权
标题翻译：氨基四氢萘衍生物，含有它们的药物组合物及其在治疗中的应用
公开(公告)号：US09096619B2
公开(公告)日：2015-08-04
申请号：US13789967
申请日：2013-03-08
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Wilhelm Amberg , Michael Ochse , Udo Lange , Andreas Kling , Berthold Behl , Wilfried Hornberger , Mario Mezler , Charles W. Hutchins
IPC分类号： A61K31/135 , C07C211/27 , A61K31/16 , C07C215/70 , C07F7/08 , C07D295/135 , C07D265/30 , C07D403/12 , C07D207/09 , C07D205/04 , C07D305/08 , C07C271/24 , C07C311/13 , C07C317/28 , C07D213/71 , C07C255/58 , C07D231/18 , C07C307/06 , C07D333/34 , C07C309/65 , C07D233/84 , C07C311/05 , C07C311/07 , C07C311/09 , C07C311/10 , C07C311/14 , C07C311/17 , C07C311/18 , C07C311/20 , C07C311/24 , C07C317/18 , C07C215/64 , C07C217/74 , C07D249/12 , C07C233/18 , C07C233/19 , C07D261/08 , C07C233/69 , C07D207/10 , C07D207/12 , C07D207/27 , C07D275/02 , C07D207/36 , C07D207/48 , C07D295/096
CPC分类号： C07C311/05 , C07C215/64 , C07C217/74 , C07C233/18 , C07C233/19 , C07C233/69 , C07C255/58 , C07C271/24 , C07C307/06 , C07C309/65 , C07C311/07 , C07C311/09 , C07C311/10 , C07C311/13 , C07C311/14 , C07C311/17 , C07C311/18 , C07C311/20 , C07C311/24 , C07C317/18 , C07C317/28 , C07C2601/02 , C07C2601/04 , C07C2602/10 , C07D205/04 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/27 , C07D207/36 , C07D207/48 , C07D213/71 , C07D231/18 , C07D233/84 , C07D249/12 , C07D261/08 , C07D265/30 , C07D275/02 , C07D295/096 , C07D295/135 , C07D305/08 , C07D333/34 , C07D401/12 , C07D403/12 , C07D409/12 , C07F7/081
摘要： The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
摘要翻译：本发明涉及式（I）的氨基四氢化萘衍生物或其生理上耐受的盐。本发明涉及包含这种氨基四氢化萘衍生物的药物组合物，以及这种氨基四氢化萘衍生物用于治疗目的的用途。氨基四氢叶酸衍生物是GlyT1抑制剂。

17. 发明申请

US20120129894A1 Alkoxy Compounds for Disease Treatment 有权
公开(公告)号：US20120129894A1
公开(公告)日：2012-05-24
申请号：US13111679
申请日：2011-05-19
申请人： Ian L. Scott , Vladimir A. Kuksa , Mark W. Orme , Thomas Little , Anna Gall , Feng Hong
发明人： Ian L. Scott , Vladimir A. Kuksa , Mark W. Orme , Thomas Little , Anna Gall , Feng Hong
IPC分类号： A61K31/426 , A61K31/24 , A61K31/22 , A61K31/16 , A61K31/155 , A61K31/15 , A61K31/135 , C07D277/28 , C07D309/06 , C07C229/38 , C07C69/017 , C07C233/19 , C07C233/22 , C07C279/08 , C07C257/14 , C07C243/42 , C07C225/18 , C07C215/46 , A61K31/351
CPC分类号： A61K31/137 , A61K31/165 , A61K31/222 , C07C215/20 , C07C217/20 , C07C217/60 , C07C217/62 , C07C217/64 , C07C217/72 , C07C217/84 , C07C225/16 , C07C229/38 , C07C233/18 , C07C235/08 , C07C251/86 , C07C279/08 , C07C309/06 , C07C317/28 , C07C323/25 , C07C323/33 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D277/24 , C07D309/06
摘要： The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

18. 发明申请

US20100234454A1 TREATMENT OF CNIDARIA INTOXICATION 审中-公开
标题翻译：治疗CNIDARIA INTOXICATION
公开(公告)号：US20100234454A1
公开(公告)日：2010-09-16
申请号：US12304047
申请日：2007-06-11
申请人： Eva Cuypers , Evert Karlsson , Jan Tytgat , Angel Yanagihara
发明人： Eva Cuypers , Evert Karlsson , Jan Tytgat , Angel Yanagihara
IPC分类号： A61K31/165 , C07D223/16 , C07D317/70 , C07C233/19 , C07K2/00 , C07J17/00 , C07C233/16 , A61K31/357 , A61P43/00
CPC分类号： A61K31/55 , A61K31/11 , A61K31/16 , A61K31/167 , A61K31/17 , A61K31/335 , A61K31/337 , A61K31/4045 , A61K31/444 , A61K31/4725 , A61K31/501 , A61K31/575
摘要： The present invention relates to the use of vanilloid receptor (VR) antagonists, and more particularly vanilloid receptor 1 (VR1) antagonist, as analgesics in the treatment and/or prohylaxis of cnidaria envenomations.
摘要翻译：本发明涉及香草素受体（VR）拮抗剂，尤其是香草酸受体1（VR1）拮抗剂在止痛药治疗和/或预防中的应用。

19. 发明申请

US20100150847A1 THERAPEUTIC DENTAL COMPOSITION AND RELATED METHODS 有权
标题翻译：治疗性牙齿组合物及相关方法
公开(公告)号：US20100150847A1
公开(公告)日：2010-06-17
申请号：US12594994
申请日：2008-07-10
申请人： Jie Yang , Bhaskar V. Velamakanni , Sumita B. Mitra , Alphonsus V. Pocius , John J. Stofko, JR. , Jeremy M. Yarwood
发明人： Jie Yang , Bhaskar V. Velamakanni , Sumita B. Mitra , Alphonsus V. Pocius , John J. Stofko, JR. , Jeremy M. Yarwood
IPC分类号： A61K8/41 , C07C233/19 , C07C215/10 , A61K8/42
CPC分类号： A61K8/41 , A61Q11/00
摘要： Dental compositions are provided comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof: wherein n is an integer from about 2 to about 5.
摘要翻译：提供牙科组合物，其包含式（I）的化合物或其药学上可接受的盐：其中n为约2至约5的整数。

20. 发明授权

US5071875A Substituted 2-amidotetralins as melatonin agonists and antagonists 失效
标题翻译：取代的2-AMIDOTETRALINS作为MELATONIN AGONISTS和ANTAGONISTS
公开(公告)号：US5071875A
公开(公告)日：1991-12-10
申请号：US411675
申请日：1989-09-25
申请人： Alan S. Horn , Margarita L. Dubocovich
发明人： Alan S. Horn , Margarita L. Dubocovich
IPC分类号： A61K31/16 , A61K31/165 , A61K51/00 , A61P25/00 , A61P25/18 , A61P25/28 , A61P27/02 , A61P27/06 , A61P43/00 , C07C233/06 , C07C233/19 , C07C233/23 , C07C233/60 , C07C233/65 , C07C233/67 , C07C233/74
CPC分类号： C07C233/60 , C07C233/06 , C07C233/23 , C07C233/65 , C07C233/74 , C07C2101/02 , C07C2102/10
摘要： The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.

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