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21. 发明授权

US5182301A Diphenylethylene derivatives pharmaceutical compositions containing same and treatment methods 失效
标题翻译：二苯乙烯衍生物含有相同的药物组合物和治疗方法
公开(公告)号：US5182301A
公开(公告)日：1993-01-26
申请号：US659518
申请日：1991-02-21
申请人： Youji Yamagishi , Kozo Akasaka , Takeshi Suzuki , Mitsuaki Miyamoto , Kouji Nakamoto , Kazuo Okano , Shinya Abe , Hironori Ikuta , Kenji Hayashi , Hiroyuki Yoshimura , Tohru Fujimori , Koukichi Harada , Isao Yamatsu
发明人： Youji Yamagishi , Kozo Akasaka , Takeshi Suzuki , Mitsuaki Miyamoto , Kouji Nakamoto , Kazuo Okano , Shinya Abe , Hironori Ikuta , Kenji Hayashi , Hiroyuki Yoshimura , Tohru Fujimori , Koukichi Harada , Isao Yamatsu
IPC分类号： A61K31/275 , C07C59/64 , C07C69/616 , C07C235/14 , C07C235/34 , C07C251/40 , C07C251/60 , C07C255/32 , C07C255/41 , C07C255/62 , C07C257/06 , C07C257/18 , C07C311/13 , C07C311/17 , C07C327/58 , C07D207/46 , C07D213/40 , C07D213/75 , C07D257/04 , C07D339/08 , C07D521/00
CPC分类号： C07D213/40 , C07C235/14 , C07C235/34 , C07C251/40 , C07C251/60 , C07C255/00 , C07C255/41 , C07C255/62 , C07C257/06 , C07C257/18 , C07C311/13 , C07C311/17 , C07C327/58 , C07C59/64 , C07D207/46 , C07D213/75 , C07D231/12 , C07D233/56 , C07D249/08 , C07D257/04 , C07D339/08
摘要： A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.NOR14)--CH2--COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, --CH(CN)--(CH2)q--COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or --(CH2)p--Z, Z being --SH, --SCH or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2.
摘要翻译：新的二苯基甲烷衍生物可用于抑制血液凝聚，并由式定义，包括二苯基乙烯衍生物和二苯甲酮肟醚衍生物。其中R 1和R 2各自为氢，羟基或低级烷氧基，U为= XY =或NOW，X为氢，氰基或-COR 6，R6为羟基或氨基，Y为-R10- COOR 3，R 3为氢或低级烷氧基，R 10为具有1至3个碳原子的直链或支链的亚烷基，-CO-NR4R5，R4和R5各自为氢，低级烷基或低级芳基烷基，-CH2-NHSO2- C6H5或-C（R8）= NR7，R7为低级烷氧基或芳基，R8为-VR9，V为氧，硫或氮，R9为烷基或芳基，W为-CH2-CO-CH2-COOR13 ，R13为氢或低级烷基，-CH2-C（= NOR14）-CH2-COOR15，R15为氢或低级烷基，R14为低级烷基，-CH（CN） - （CH2）q-COOR16，R16 是氢或低级烷基，q为1〜3的整数，或 - （CH 2）p Z，Z为-SH，-SCH或衍生自五元或六元环的一价基团，其可以被环在环中具有一个或多个硫原子，p为1或2。

22. 发明授权

US5171860A Diamino isothiazole-1-oxides and 1,1 dioxides as gastric secretion inhibitors 失效
标题翻译：二氨基异噻唑-1-氧化物和1,1-二氧化物作为胃分泌抑制剂
公开(公告)号：US5171860A
公开(公告)日：1992-12-15
申请号：US794339
申请日：1991-11-12
申请人： Susan F. Britcher , William C. Lumma, Jr.
发明人： Susan F. Britcher , William C. Lumma, Jr.
IPC分类号： C07D275/02 , C07D275/03 , C07D277/48 , C07F7/10 , C07F7/18
CPC分类号： C07D275/03 , C07C255/00 , C07D277/48 , C07F7/10 , C07F7/1896
摘要： This invention is directed to diamino isothiazole -1-oxides and -1,1-dioxides and related compounds as well as pharmaceutical compositions and methods useful in the treatment of gastric secretion in mammals.
摘要翻译：本发明涉及二氨基异噻唑-1-氧化物和-1,1-二氧化物及相关化合物以及可用于治疗哺乳动物胃分泌的药物组合物和方法。

23. 发明授权

US5126371A Diarylacetylenes, their preparation and their use 失效
标题翻译：二芳基乙炔，其制备及其用途
公开(公告)号：US5126371A
公开(公告)日：1992-06-30
申请号：US569869
申请日：1990-08-20
申请人： Hans-Heiner Wuest , Fritz-Frieder Frickel , Axel Nuerrenbach
发明人： Hans-Heiner Wuest , Fritz-Frieder Frickel , Axel Nuerrenbach
IPC分类号： C07D263/10 , A61K31/015 , A61K31/03 , A61K31/075 , A61K31/085 , A61K31/11 , A61K31/115 , A61K31/12 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/22 , A61K31/275 , A61K31/41 , A61P17/00 , A61P29/00 , A61P35/00 , C07C1/00 , C07C13/465 , C07C13/48 , C07C17/00 , C07C25/24 , C07C27/00 , C07C33/38 , C07C39/23 , C07C39/38 , C07C43/168 , C07C43/176 , C07C43/215 , C07C43/23 , C07C45/00 , C07C45/44 , C07C45/68 , C07C47/548 , C07C47/55 , C07C47/57 , C07C47/575 , C07C49/683 , C07C49/747 , C07C49/757 , C07C49/798 , C07C49/813 , C07C49/835 , C07C49/84 , C07C57/50 , C07C57/62 , C07C59/72 , C07C63/66 , C07C63/74 , C07C65/19 , C07C65/28 , C07C65/38 , C07C67/00 , C07C69/618 , C07C69/65 , C07C69/734 , C07C69/76 , C07C69/78 , C07C209/00 , C07C209/48 , C07C211/44 , C07C211/52 , C07C215/74 , C07C233/05 , C07C233/11 , C07C233/22 , C07C233/29 , C07C233/65 , C07C235/34 , C07C235/38 , C07C235/42 , C07C255/50 , C07C255/51 , C07C255/54 , C07C255/56 , C07D257/04
CPC分类号： C07D257/04 , C07C255/00 , C07C33/38 , C07C43/168 , C07C43/215 , C07C45/44 , C07C45/68 , C07C47/548 , C07C47/57 , C07C47/575 , C07C49/683 , C07C49/747 , C07C49/757 , C07C49/798 , C07C49/835 , C07C49/84 , C07C57/50 , C07C63/66 , C07C63/74 , C07C65/19 , C07C65/28 , C07C65/38
摘要： Novel diarylacetylenes of the formula I ##STR1## where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings stated in the description, are useful for the treatment of disorders.
摘要翻译：式I的新型二芳基乙炔，其中A，R1，R2，R3，R4，R5和R6具有说明书中所述的含义，可用于治疗疾病。

24. 发明授权

US5120467A Anisotropic compounds and liquid crystal mixtures 失效
标题翻译：各向异性化合物和液晶混合物
公开(公告)号：US5120467A
公开(公告)日：1992-06-09
申请号：US333769
申请日：1989-04-06
申请人： Tuong Huynh-Ba , Maged A. Osman
发明人： Tuong Huynh-Ba , Maged A. Osman
IPC分类号： C07C13/28 , C07C17/00 , C07C17/16 , C07C17/26 , C07C19/01 , C07C19/07 , C07C19/08 , C07C22/00 , C07C22/04 , C07C22/08 , C07C25/18 , C07C41/00 , C07C43/192 , C07C43/225 , C07C67/00 , C07C69/74 , C07C69/76 , C07C69/773 , C07C253/00 , C07C255/31 , C07C255/32 , C07C255/33 , C07C255/37 , C07C255/45 , C07C255/51 , C07D237/08 , C07D237/10 , C07D237/14 , C07D237/24 , C07D239/08 , C07D239/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C09K19/00 , C09K19/08 , C09K19/30 , C09K19/32 , C09K19/34 , C09K19/42 , G02F1/13
CPC分类号： C07C255/00 , C07C22/00 , C07C22/04 , C07C43/192 , C07C43/225 , C07D237/08 , C07D237/14 , C09K19/3001 , C09K19/321 , C09K19/3441 , C09K19/3455 , C09K19/3458
摘要： New anisotropic compounds of the formula (1) are useful in liquid crystal mixtures for electrooptical displays; at least one of the end groups of the compounds (1) is an alkyl group which carries cyano or halogen in a terminal or non-terminal position. This offers advantages for longitudinal polarization and/or cross-polarization of the anisotropic compounds with the aid of the comparatively highly polarizing cyano or halogen substituents, in particular high clear points, low ##EQU1## values and/or negative .DELTA..epsilon. values.

25. 发明授权

US5116853A Phenylene derivatives 失效
标题翻译：苯乙烯衍生物
公开(公告)号：US5116853A
公开(公告)日：1992-05-26
申请号：US413458
申请日：1989-09-27
申请人： Toshiyasu Mase , Kiyoshi Murase , Hiromu Hara , Kenichi Tomioka
发明人： Toshiyasu Mase , Kiyoshi Murase , Hiromu Hara , Kenichi Tomioka
IPC分类号： A61K31/195 , C07C45/71 , C07C47/575 , C07C59/70 , C07C59/72 , C07C59/90 , C07C65/21 , C07C65/24 , C07C69/712 , C07C69/734 , C07C233/12 , C07C235/56 , C07C235/64 , C07C255/59 , C07C255/60 , C07C271/28 , C07C275/40 , C07D257/04 , C07D285/12 , C07D285/125 , C07D285/135
CPC分类号： C07D257/04 , C07C235/56 , C07C235/64 , C07C255/00 , C07C255/60 , C07C271/28 , C07C275/40 , C07C45/71 , C07C47/575 , C07C59/70 , C07C59/72 , C07C65/21 , C07C65/24 , C07C69/712 , C07C69/734 , C07D285/125 , C07D285/135
摘要： Novel phenylene derivatives shown by the general formula ##STR1## wherein A represents a hydrogen atom, a phenyl group or a phenoxy group, n represents an integer of 3 to 10, R.sub.1 represents a hydrogen atom or a lower alkoxy group, X.sub.1 represents --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CONH--, B represents ##STR2## (wherein R.sub.2 represents a hydrogen atom, a halogen, atom, a nitro group, etc.), ##STR3## (wherein R.sub.3 represents a hydrogen atom, a hydroxyl group or a lower alkoxy group), X.sub.2 represents --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, etc. and D represents a carboxy group, a lower alkoxycarbonyl group or ##STR4## which are useful as drugs, particularly SRS-A (slow reacting substance of anaphylaxis) antagonist, i.e. they are useful as prophylaxis and treatment for various allergic diseases (e.g. bronchial asthma, allergic rhinitis, urticaria) or, ischemic heart diseases, inflammation, etc. induced by SRS-A.

26. 发明授权

US5110348A Glycine compounds and herbicidal compositions thereof 失效
标题翻译：甘氨酸化合物及其除草剂组合物
公开(公告)号：US5110348A
公开(公告)日：1992-05-05
申请号：US548190
申请日：1990-07-05
申请人： William J. Hopwood
发明人： William J. Hopwood
IPC分类号： A01N37/46 , A01N37/22 , A01N47/12 , A01N47/18 , A01N47/22 , A01N47/34 , A61K38/36 , C07C67/00 , C07C227/00 , C07C229/18 , C07C231/00 , C07C233/12 , C07C233/83 , C07C233/88 , C07C235/52 , C07C235/64 , C07C235/68 , C07C237/30 , C07C255/58 , C07C325/00 , C07C327/20 , C07C327/22 , C07D295/18
CPC分类号： C07C255/00 , A01N37/22 , A01N47/12 , A01N47/18 , A01N47/22 , A01N47/34
摘要： Novel herbicidal compounds of the general formula ##STR1## in which X represents a phenyl group substituted in the 2-position and optionally substituted in one or more of the 3-, 4-, 5- and 6-positions, the 2-substituent being a cyano group, or a group of the general formula CQNR.sup.1 R.sup.2 or COQR.sup.3 where Q represents an oxygen or sulphur atom and each of R.sup.1, R.sup.2 and R.sup.3 represents a hydrogen atom or an optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, phenyl or phenalkyl group, or R.sup.1 and R.sup.2 jointly represent a hydrocarbon chain;Y represents an optionally substituted phenyl group; L represents an oxygen or sulphur atom; andZ represents a hydrogen atom or an optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, phenyl or phenalkyl group;and salts of such compounds.

27. 发明授权

US5091558A Naphthalene anti-psoriatic agents 失效
标题翻译：萘抗牛皮癣药
公开(公告)号：US5091558A
公开(公告)日：1992-02-25
申请号：US23089
申请日：1987-03-06
申请人： Gordon H. Jones , Michael C. Venuti , John M. Young
发明人： Gordon H. Jones , Michael C. Venuti , John M. Young
IPC分类号： C07C46/00 , C07C50/10 , C07C50/14 , C07C50/24 , C07C50/32 , C07C69/00 , C07D213/64 , C07D213/89 , C07D239/38 , C07D333/64
CPC分类号： C07D213/89 , C07C255/00 , C07C317/00 , C07C323/00 , C07C46/00 , C07C50/10 , C07C50/14 , C07C50/24 , C07C50/32 , C07D213/64 , C07D239/38 , C07D333/64
摘要： Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is alkoxy, alkylthio, optionally substituted phenoxy or optionally substituted phenylthio;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2, or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(0).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl.
摘要翻译：哺乳动物中的牛皮癣通过局部施用下式的萘来减轻：其中：R1是烷氧基，烷硫基，任选取代的苯氧基或任选取代的苯硫基; R 2是氢，低级烷基，任选取代的苯基或任选取代的苯基烷基; R3是低级烷基，低级烷氧基或卤素，m是0,1或2，或R3是任选取代的苯基，任选取代的苯基低级烷基，任选取代的苯基低级烷氧基，氨基，低级烷基氨基，低级二烷基氨基，氰基或S （O）n R其中R是低级烷基; 任选取代的苯基; 任选取代的苯基低级烷基; 或含有一个或两个选自氮，氧和硫的杂原子的三至九个环原子的任选取代的杂环芳基及其药学上可接受的酸加成盐; m为1，n为0,1或2; 且W为1至7个碳原子的烷基，任选取代的苯基或任选取代的苄基。

28. 发明授权

US5089516A 1-phenyl-3,5-pyrazolidinedione hydroxystyrene compounds which have tyrosine kinase inhibiting activity 失效
标题翻译：具有酪氨酸激酶抑制活性的1-苯基-3,5-二异氰酸酯化羟基苯乙烯化合物
公开(公告)号：US5089516A
公开(公告)日：1992-02-18
申请号：US584683
申请日：1990-09-19
申请人： Tadayoshi Shiraishi , Keiji Kameyama , Takeshi Domoto , Naohiro Imai , Yoshio Shimada , Yutaka Ariki , Kazunori Hosoe , Masaji Kawatsu , Ikuo Katsumi , Takayoshi Hidaka , Kiyoshi Watanabe
发明人： Tadayoshi Shiraishi , Keiji Kameyama , Takeshi Domoto , Naohiro Imai , Yoshio Shimada , Yutaka Ariki , Kazunori Hosoe , Masaji Kawatsu , Ikuo Katsumi , Takayoshi Hidaka , Kiyoshi Watanabe
IPC分类号： A61K31/425 , C07C255/34 , C07D207/38 , C07D209/34 , C07D231/36 , C07D277/20 , C07D277/36 , C07D277/54 , C07D279/16 , C07D307/58 , C07D417/12 , A61K31/415 , C07D231/04
CPC分类号： C07D277/20 , C07C255/00 , C07C255/34 , C07D207/38 , C07D209/34 , C07D231/36 , C07D277/36 , C07D277/54 , C07D279/16 , C07D307/58 , C07D417/12
摘要： A hydroxystyrene derivative represented by the formula (I): ##STR1## wherein when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O-- (R.sup.5 : H, a C.sub.1 to C.sub.5 alkyl group or benzyl group) and R.sup.2 : benzyl group or PhSCH.sub.2, R.sup.3 and R.sup.4 are taken together to represent --CONH--CS--S--, ##STR2## (X.sup.1 : H, a halogen, methyl group, ethyl group, R.sup.7 O-- (R.sup.7 : methyl or ethyl group), nitro group, aminosulfonyl group or amino group, m.sup.1 : 1 or 2), pyridyl group, furyl group or thienyl group, n.sup.1 : an integer of 0 to 3); when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O-- (R.sup.5 : as defined above) and R.sup.2 : benzyl group, R.sup.3 : cyano group and R.sup.4 : a carbamoyl group, or R.sup.3 and R.sup.4 are taken together to represent --CO--Y--CH.sub.2 CH.sub.2 -- (Y: O or --NH--) or ##STR3## and when R.sup.1 and R.sup.2 : a C.sub.1 to C.sub.3 alkyl group, R.sup.3 and R.sup.4 are taken together to represent ##STR4## (n.sup.1, R.sup.6 : as defined above), or a salt thereof. The hydroxystyrene derivative or a salt thereof is a compound which is useful as an active ingredient of an antiallergic agent, a 5-lipoxygenase inhibiting agent, an antibacterial agent, a tyrosine kinase inhibiting agent, an ultraviolet absorber or a reverse transcriptase inhibiting agent, and also is useful as an intermediate for preparing various organic compounds.

29. 发明授权

US5075032A Smectic liquid-crystalline phases 失效
标题翻译：精密液晶相
公开(公告)号：US5075032A
公开(公告)日：1991-12-24
申请号：US395823
申请日：1989-08-18
申请人： Reinhard Hopf , Bernhard Scheuble , Andreas Wachtler
发明人： Reinhard Hopf , Bernhard Scheuble , Andreas Wachtler
IPC分类号： C07C255/45 , C07C255/46 , C07D213/55 , C07D239/26 , C09K19/00 , C09K19/20 , C09K19/30 , C09K19/32 , C09K19/34 , C09K19/42 , G02F1/13
CPC分类号： C07C255/00 , C09K19/2007 , C09K19/3003 , C09K19/3068 , C09K19/322 , C09K19/3441 , C09K19/3444 , C09K19/3452 , C09K19/3455 , C09K19/3458 , C09K19/42 , C09K2019/325 , C09K2019/326
摘要： The invention relates to the use of compounds of the formula IR.sup.1 -Q.sup.1 -A-(Q.sup.2).sub.q -R.sup.2 IwhereinA denotes ##STR1## and R.sup.1, R.sup.2, Q.sup.1, Q.sup.2 and q have the meaning specified in claim 1, as components of smectic liquid-crystalline phases, and also smectic liquid-crystalline phases, in particular chiral tilted smectic phases containing compounds of formula I.

30. 发明授权

US5072038A 2,3,4,5-tetrahalogenobenzene derivatives 失效
标题翻译： 2,3,4,5-四氢生物碱衍生物
公开(公告)号：US5072038A
公开(公告)日：1991-12-10
申请号：US459876
申请日：1990-01-02
申请人： Erich Klauke , Uwe Petersen , Klaus Grohe
发明人： Erich Klauke , Uwe Petersen , Klaus Grohe
IPC分类号： A61K31/47 , A61K31/495 , A61K31/535 , A61P31/04 , C07B31/00 , C07B39/00 , C07C17/00 , C07C17/14 , C07C17/16 , C07C17/18 , C07C17/20 , C07C25/13 , C07C27/00 , C07C33/46 , C07C45/00 , C07C45/29 , C07C45/43 , C07C47/24 , C07C47/55 , C07C51/00 , C07C53/50 , C07C63/70 , C07C67/00 , C07C233/00 , C07C233/65 , C07C253/00 , C07C255/49 , C07C255/50 , C07D215/56 , C07D401/04 , C07D413/04
CPC分类号： C07D215/56 , C07C17/14 , C07C17/16 , C07C255/00 , C07C33/46 , C07C45/292 , C07C45/43 , C07C47/55 , C07C63/70 , C07D401/04 , C07D413/04
摘要： 2,3,4,5-trihalogenobenzene derivatives of the formula ##STR1## in which R is --COOH, --COCl, --COF, --CN, --CONH.sub.2, --CH.sub.2 OH, --CH.sub.2 Cl, --CHCl.sub.2, --CCl.sub.3 or --CHO,R.sup.1 is H, Cl or F, andR.sup.2 is Cl or F,it only being possible for R.sup.1 or R.sup.2 to be F, and processes for their preparation starting from benzonitriles reacted with potassium fluoride. The novel compounds are intermediates for antibacterials such as quinolone carboxylic acids.
摘要翻译：其中R是-COOH，-COCl，-COF，-CN，-CONH 2，-CH 2 OH，-CH 2 Cl，-CHCl 2，-CCl 3或-CHO的通式为“IMAGE”的2,3,4,5-三卤代苯衍生物， R1是H，Cl或F，R2是Cl或F，R1或R2只能是F，从与氟化钾反应的苯甲腈开始制备它们的制备方法。新型化合物是抗菌剂如喹诺酮羧酸的中间体。

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