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31. 发明授权

US5633399A Process for the preparation of fluorinated benzoic acids 失效
公开(公告)号：US5633399A
公开(公告)日：1997-05-27
申请号：US463410
申请日：1995-06-05
申请人： Xiu C. Wang , Panos Kalaritis , Michelle L. Chang
发明人： Xiu C. Wang , Panos Kalaritis , Michelle L. Chang
IPC分类号： C07C51/363 , C07C205/12 , C07C205/45 , C07C205/56 , C07C205/58 , C07C255/35 , C07C51/27 , C07C51/305
CPC分类号： C07C255/35 , C07C205/12 , C07C205/45 , C07C205/56 , C07C205/58 , C07C51/363
摘要： A process for the preparation of 2-chloro-4,5-difluorobenzoic acid and 2,4,5-trifluorobenzoic acid as well as synthetic intermediates useful in and prepared according thereto, comprising reacting a nitrobenzene having the formula ##STR1## wherein X is chloro or fluoro, with an appropriate carbanion to form a compound having the formula ##STR2## wherein one of Y and Z is chloro and the other is nitro, and R is a radical selected from the group consisting of --CCl.sub.3, --CH.sub.2 NO.sub.2, --CH(NO.sub.2)R.sup.1, --CH(CO.sub.2 R.sup.1).sub.2, --CH(C(O)R.sup.2).sub.2, --CH(CN)CO.sub.2 R.sup.1, --CH(CO.sub.2 R.sup.1)COR.sup.2 and --COR.sup.2 where R.sup.1 is alkyl or arylalkyl and R.sup.2 is alkyl, aryl or arylalkyl and, where appearing more than once in such a radical, R.sup.1 and R.sup.2 may be the same or different at each occurrence.

32. 发明授权

US5576455A Process for the preparation of fluorinated benzoic acids 失效
标题翻译：氟代苯甲酸的制备方法
公开(公告)号：US5576455A
公开(公告)日：1996-11-19
申请号：US461782
申请日：1995-06-05
申请人： Xiu C. Wang , Panos Kalaritis , Michelle L. Chang
发明人： Xiu C. Wang , Panos Kalaritis , Michelle L. Chang
IPC分类号： C07C51/363 , C07C205/12 , C07C205/45 , C07C205/56 , C07C205/58 , C07C255/35 , C07C255/03 , C07C205/06
CPC分类号： C07C255/35 , C07C205/12 , C07C205/45 , C07C205/56 , C07C205/58 , C07C51/363
摘要： A process for the preparation of 2-chloro-4,5-difluorobenzoic acid and 2,4,5-trifluorobenzoic acid as well as synthetic intermediates useful in and prepared according thereto, comprising reacting a nitrobenzene having the formula ##STR1## wherein X is chloro or fluoro, with an appropriate carbanion to form a compound having the formula ##STR2## wherein one of Y and Z is chloro and the other is nitro, and R is a radical selected from the group consisting of --CCl.sub.3, --CH.sub.2 NO.sub.2, --CH(NO.sub.2)R.sup.1, --CH(CO.sub.2 R.sup.1).sub.2, --CH(C(O)R.sup.2).sub.2, --CH(CN)CO.sub.2 R.sup.1, --CH(CO.sub.2 R.sup.1)COR.sup.2 and --COR.sup.2 where R.sup.1 is alkyl or arylalkyl and R.sup.2 is alkyl, aryl or arylalkyl and, where appearing more than once in such a radical, R.sup.1 and R.sup.2 may be the same or different at each occurrence.
摘要翻译：一种制备2-氯-4,5-二氟苯甲酸和2,4,5-三氟苯甲酸的方法，以及可用于和制备的合成中间体，包括使具有下式的硝基苯：其中X为氯或氟，与适当的碳负离子形成具有下式的化合物：硝基，R是选自-CCl 3，-CH 2 NO 2，-CH（NO 2）R 1，-CH（CO 2 R 1） 2，-CH（C（O）R 2）2，-CH（CN）CO 2 R 1，-CH（CO 2 R 1）COR 2和-COR 2，其中R 1是烷基或芳基烷基，R 2是烷基，芳基或芳烷基，并且其中出现多于一次在这样的基团中，R 1和R 2可以在每次出现时相同或不同。

33. 发明授权

US5458678A Alkaline earth metal salts, transition metal salts and transition metal complexes of ketocarboxylic acids as corrosion inhibitors 失效
标题翻译：碱土金属盐，过渡金属盐和酮羧酸的过渡金属络合物作为腐蚀抑制剂
公开(公告)号：US5458678A
公开(公告)日：1995-10-17
申请号：US222766
申请日：1994-04-04
申请人： William P. Armstrong , Adalbert Braig , Markus Frey , Andreas Kramer
发明人： William P. Armstrong , Adalbert Braig , Markus Frey , Andreas Kramer
IPC分类号： C07C51/41 , C07C59/84 , C07C59/88 , C07C59/90 , C07C205/56 , C09D5/08 , C09K15/06 , C23F11/00 , C09D5/00 , C07C51/00
CPC分类号： C07C59/84 , C07C205/56 , C07C59/88 , C07C59/90 , C09D5/086
摘要： There are described novel alkaline earth metal salts, transition metal salts and transition metal complexes of compounds of the formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are, independently of one another, hydrogen, halogen, nitro, cyano, CF.sub.3, C.sub.1 -C.sub.15 alkyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.2 -C.sub.15 alkenyl, C.sub.1 -C.sub.12 haloalkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, C.sub.6 -C.sub.10 aryl which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl; C.sub.6 -C.sub.10 aryloxy which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl; C.sub.7 -C.sub.12 arylalkyl which is unsubstituted or substituted on the aryl radical by from 1 to 3 C.sub.1 -C.sub.4 alkyl groups; --CO.sub.2 R.sub.6, --COR.sub.6 or ##STR2## where at least one of the radicals R.sub.1 to R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.15 alkyl, in addition the radicals R.sub.1 and R.sub.2, R2 and R.sub.3, R.sub.3 and R.sub.4 or R.sub.4 and R.sub.5 form, together with the carbon atoms to which they are bound, a benzo or cyclohexenyl ring,R.sub.6 is C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkyl interrupted by oxygen, sulfur or >N--R.sub.9 ; C.sub.7 -C.sub.12 arylalkyl which is unsubstituted or substituted on the aryl radical by from 1 to 3 C.sub.1 -C.sub.4 alkyl groups, R.sub.7 and R.sub.8 are, independently of one another, hydrogen, C.sub.1 -C.sub.24 alkyl or C.sub.2 -C.sub.24 alkyl interrupted by oxygen, sulfur or >N--R.sub.9,R.sub.9 is hydrogen or C.sub.1 -C.sub.8 alkyl, andn is an integer in the range from 1 to 10 for use, as corrosion inhibitors in coating compositions for protecting metal surfaces.
摘要翻译：描述了式I（I）化合物的新型碱土金属盐，过渡金属盐和过渡金属络合物，其中R 1，R 2，R 3，R 4和R 5彼此独立地为氢，卤素，硝基，氰基，CF 3，C 1 -C 15烷基，C 5 -C 12环烷基，C 2 -C 15烯基，C 1 -C 12卤代烷基，C 1 -C 12烷氧基，C 1 -C 12烷硫基，未被C 1 -C 4烷基取代的C 6 -C 10芳基; 未取代或被C 1 -C 4烷基取代的C 6 -C 10芳氧基; 未取代或在芳基上被1至3个C 1 -C 4烷基取代的C 7 -C 12芳基烷基; -CO 2 R 6，-COR 6或其中基团R 1至R 5中的至少一个为氢，卤素或C 1 -C 15烷基，此外基团R 1和R 2，R 2和R 3，R 3和R 4或R 4和R 5一起形成与其结合的碳原子，苯并或环己烯基环，R 6是C 1 -C 20烷基，被氧，硫或> N-R 9中断的C 2 -C 20烷基; 未取代或在芳基上被1至3个C 1 -C 4烷基取代的C 7 -C 12芳基烷基，R 7和R 8彼此独立地为氢，C 1 -C 24烷基或C 2 -C 24烷基，其被氧，硫或> N- R9，R9为氢或C1-C8烷基，n为1〜10的整数，用作保护金属表面的涂料组合物中的腐蚀抑制剂。

34. 发明授权

US5237089A Nitro or amino substituted phenylalkyl or phenylalkenyl carboxylic acid derivatives 失效
标题翻译：硝基或氨基取代的苯基烷基或苯基烯基羧酸衍生物
公开(公告)号：US5237089A
公开(公告)日：1993-08-17
申请号：US985534
申请日：1992-12-03
申请人： Peter Plath , Karl Eicken , Norbert Goetz , Jochen Wild , Norbert Meyer , Bruno Wuerzer
发明人： Peter Plath , Karl Eicken , Norbert Goetz , Jochen Wild , Norbert Meyer , Bruno Wuerzer
IPC分类号： A01N37/46 , C07C205/06 , C07C205/34 , C07C205/56 , C07D209/48
CPC分类号： C07D209/48 , A01N37/46 , C07C205/44 , C07C205/56 , C07C255/00
摘要： N-substituted 3,4,5,6-tetrahydrophthalimides and their intermediates of the general formula I ##STR1## where A is --NO.sub.2, --NH.sub.2 or ##STR2## corresponding to the compounds Ia, Ib and Ic, B is --CH.sub.2 --, --CH.sub.2 --CHR.sup.1 --, --CH.sub.2 --CHR.sup.1 --CH.sub.2 --, --CH.dbd., --CH.dbd.CR.sup.1 -- or --CH.dbd.CR.sup.1 --CH.dbd., R.sup.1 being --H, --Cl, --Br or --CH.sub.3, D is ##STR3## or .dbd.C
摘要翻译： B）是N-取代的3,4,5,6-四氢邻苯二甲酰亚胺及其中间体，其中A是与化合物Ia，Ib和Ic相对应的-NO 2，-NH 2或 -CH 2 - ， - CH 2 -CHR 2 - ， - CH =， - CH = CR 1或-CH = CR 1 -CH =，R 1是-H，-Cl，-Br或-CH 3， D为或= C <，取决于末端基团B，X为-H，-Cl或-Br，Y为-H，C 1 -C 7 - 烷基，-Cl，-Br，-CN，-CONH 2 或-CO2R2，其中R2是H，C1-C6-烷基，C5-或C6-环烷基，C1-C4-烷氧基-C2-C4-烷基，C1-C4-烷基巯基-C2-C4-烷基，炔丙基，苄基， α-苯基乙基，α-苯基丙基，被F或Cl单取代或三取代的C 2 -C 4烷基，或CH 3取代或Cl取代的烯丙基，Z是-COOR 2，-CONR 3 R 4，其中R 3和R 4各自为H或C 1 -C 4烷基或一起形成其碳链可被氧原子间隔的5元或6元环脂环。

35. 发明授权

US5236952A Catechol derivatives 失效
标题翻译：儿茶酚衍生物
公开(公告)号：US5236952A
公开(公告)日：1993-08-17
申请号：US686210
申请日：1991-04-16
申请人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose DaPrada , Gerhard Zurcher
发明人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose DaPrada , Gerhard Zurcher
IPC分类号： A61K31/12 , A61K31/195 , A61K31/44 , C07C45/29 , C07C45/30 , C07C45/46 , C07C45/67 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07C205/16 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/49 , C07C255/53 , C07D209/12 , C07D213/02 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04 , C07D498/02 , C07D513/04
CPC分类号： C07D513/04 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/00 , C07C255/53 , C07C45/298 , C07C45/30 , C07C45/305 , C07C45/46 , C07C45/673 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07D209/12 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04
摘要： Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
摘要翻译：式Ia的儿茶酚衍生物其中Ra，Rb和Rc具有本文给出的含义，其在生理条件下可水解的酯和醚衍生物及其药学上可接受的盐被描述并且具有有价值的药理学性质。特别地，它们抑制了儿茶酚-O-甲基转移酶（COMT），一种可溶性的镁依赖性酶，其催化S-邻苯二甲酰甲硫氨酸的甲基转移到儿茶酚底物上，由此形成相应的甲基醚。可以通过COMT进行O-甲基化并因此可以失活的合适的底物是例如外来儿茶酚胺和具有儿茶酚结构的非常给予的治疗活性物质。上述式Ia不仅包括形成本发明一部分的化合物，而且包括已知的化合物; 构成本发明一部分的化合物可以根据已知方法制备。

36. 发明授权

US4873334A 4,7-dihydropyrazolo(3,4-b) pyridine derivatives 失效
标题翻译： 4,7-二氢吡唑并（3,4-b）吡啶衍生物
公开(公告)号：US4873334A
公开(公告)日：1989-10-10
申请号：US99907
申请日：1987-09-22
申请人： Ikuo Adachi , Teruo Yamamori , Motohiko Ueda , Hatsuo Sato
发明人： Ikuo Adachi , Teruo Yamamori , Motohiko Ueda , Hatsuo Sato
IPC分类号： A61K31/44 , C07C205/56 , C07D211/90 , C07D231/38 , C07D401/04 , C07D407/04 , C07D471/04
CPC分类号： C07D231/38 , C07C205/56 , C07C255/00 , C07D211/90 , C07D401/04 , C07D407/04 , C07D471/04
摘要： Novel Ca-blockers, 4,7-dihydropyrazolo[3,4-b]pyridine derivatives having potent antihypertensive and coronary vasodilating actions and useful in treatment for diseases in circulatory system, but without systole inhibitory action.
摘要翻译：新型Ca阻断剂，4,7-二氢吡唑并[3,4-b]吡啶衍生物，具有有效的抗高血压和冠状动脉血管扩张作用，可用于治疗循环系统疾病，但无收缩期抑制作用。

37. 发明授权

US4781750A Herbicidally active enols 失效
标题翻译：除草活性烯醇
公开(公告)号：US4781750A
公开(公告)日：1988-11-01
申请号：US770033
申请日：1985-08-27
申请人： John W. Ashmore
发明人： John W. Ashmore
IPC分类号： C07C253/00 , A01N25/00 , A01N35/02 , A01N37/30 , A01N37/34 , A01N37/36 , A01N37/38 , A01N37/42 , A01N37/44 , A01N37/46 , A01N37/48 , A01N41/02 , A01N41/10 , A01N43/00 , A01N43/02 , A01N43/06 , A01N43/08 , A01N43/10 , A01N43/713 , A01N43/74 , A01N47/30 , C07C49/235 , C07C67/00 , C07C69/732 , C07C205/56 , C07C227/00 , C07C231/00 , C07C233/12 , C07C239/00 , C07C301/00 , C07C313/00 , C07C317/00 , C07D295/185 , C07D307/54 , C07D333/24 , A01N33/12
CPC分类号： C07D295/185 , A01N35/02 , A01N37/30 , A01N37/34 , A01N37/38 , A01N37/42 , A01N41/10 , A01N43/08 , A01N43/10 , C07C205/56 , C07C255/00 , C07C317/00 , C07C49/235 , C07D307/54 , C07D333/24
摘要： Enols, their geometric isomers, tautomers and halogen addition products having the formula ##STR1## as defined herein and compositions containing these compounds exhibit herbicidal activity.
摘要翻译：烯醇，它们的几何异构体，互变异构体和具有如本文所定义的式“IMAGE”的卤素加成产物和含有这些化合物的组合物显示出除草活性。

38. 发明授权

US4727073A Pyrimidine derivatives and composition of the same 失效
标题翻译：嘧啶衍生物及其组成相同
公开(公告)号：US4727073A
公开(公告)日：1988-02-23
申请号：US779043
申请日：1985-09-23
申请人： Takao Takaya , Hisashi Takasugi , Atsushi Kuno , Yoshie Sugiyama
发明人： Takao Takaya , Hisashi Takasugi , Atsushi Kuno , Yoshie Sugiyama
IPC分类号： A61K31/505 , C07C205/56 , C07D239/20 , C07D239/26 , C07D239/30 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D487/04 , C07D491/04
CPC分类号： C07D239/26 , C07C205/45 , C07C205/56 , C07D239/20 , C07D239/30 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/04 , C07D487/04 , C07D491/04
摘要： The invention relates to new pyrimidine derivatives, useful in the treatment of cerebrovascular disease, of the formula: ##STR1## wherein Ar, R.sup.1, R.sup.2 and R.sup.3 are defined in the specification.
摘要翻译：本发明涉及可用于治疗脑血管疾病的新的嘧啶衍生物，具有下式：其中Ar，R 1，R 2和R 3在说明书中定义。

39. 发明授权

US4686217A Calcium antagonist 2-fluoroalkyl-1,4-dihydropyridines 失效
标题翻译：钙拮抗剂2-氟烷基-1,4-二氢吡啶
公开(公告)号：US4686217A
公开(公告)日：1987-08-11
申请号：US601309
申请日：1984-04-17
申请人： Andrew J. G. Baxter , John Dixon , Kenneth J. Gould , Alan C. Tinker
发明人： Andrew J. G. Baxter , John Dixon , Kenneth J. Gould , Alan C. Tinker
IPC分类号： C07C17/093 , C07C45/00 , C07C47/55 , C07C205/56 , C07D205/04 , C07D211/78 , C07D211/90 , C07D305/08 , C07D309/12 , C07D401/04 , C07D405/04 , C07D413/04 , C07D521/00 , A61K31/455
CPC分类号： C07D231/12 , C07C17/093 , C07C205/56 , C07C45/00 , C07C47/55 , C07D205/04 , C07D211/78 , C07D211/90 , C07D233/56 , C07D249/08 , C07D305/08 , C07D309/12 , C07D401/04 , C07D405/04 , C07D413/04
摘要： There are described compounds of formula I, ##STR1## in which R.sub.1 represents benzofurazanyl, pyridyl or phenyl, the pyridyl or phenyl being substituted,--COOR.sub.2 and --COOR.sub.3 are various ester groups,one of R.sub.7 and R.sub.8 represents alkyl Cl to 6 and the other represents --CONR.sub.10 R.sub.11 ; --CSNH.sub.2 ; --C(.dbd.NH)SR.sub.9 ; --S(O).sub.m R.sub.9 ; phenyl optionally substituted by one or more of alkyl Cl to 6, halogen, alkoxy Cl to 6 or nitro; alkyl Cl to 6 substituted by halogen; or furanyl;m is 0 or 1R.sub.9 is alkyl Cl to 6, andR.sub.10 and R.sub.11 each independently represent hydrogen or alkyl Cl to 6, or together with the nitrogen atom to which they are attached form a 5 or 6 membered heterocyclic ring.There are also described processes for making the compounds, and pharmaceutical, e.g. calcium antagonist, formulations containing them.
摘要翻译：描述了式I的化合物，其中R1代表苯并呋喃基，吡啶基或苯基，被取代的吡啶基或苯基，-COOR2和-COOR3是各种酯基，R7和R8之一表示烷基C1至6和另一个代表-CONR10R11; -CSNH2; -C（= NH）SR9; -S（O）m R 9; 任选被一个或多个烷基C1至6，卤素，烷氧基C1至6或硝基取代的苯基; 由卤素取代的C 1-6烷基; 或呋喃基; m为0或1，R 9为C 1-6烷基，R 10和R 11各自独立地表示氢或C 1-6烷基，或与它们所连接的氮原子一起形成5或6元杂环。还描述了制备化合物的方法，以及药物，例如，钙拮抗剂，含有它们的制剂。

40. 发明授权

US4684371A Oxidation hair dyes comprising m-phenylenediamine derivatives as coupling components 失效
标题翻译：包含间苯二胺衍生物作为偶联组分的氧化染发剂
公开(公告)号：US4684371A
公开(公告)日：1987-08-04
申请号：US814062
申请日：1985-12-19
申请人： Gunther Konrad , Norbert Maak , Edgar Lieske
发明人： Gunther Konrad , Norbert Maak , Edgar Lieske
IPC分类号： A61K8/00 , A61K8/41 , A61Q5/10 , C07C67/00 , C07C205/37 , C07C205/56 , C07C213/00 , C07C217/84 , C07C227/00 , C07C227/04 , C07C229/42 , A61K7/13
CPC分类号： A61K8/44 , A61Q5/10 , C07C205/37 , C07C205/56
摘要： This invention is directed to m-phenylenediamine derivatives and salts thereof and to compositions of the developer-coupler type of the dyeing of hair, consisting essentially of m-phenylenediamine derivatives or salts thereof as coupling components and, as developer components, conventional components used in oxidation dyes.
摘要翻译：本发明涉及间苯二胺衍生物及其盐，以及主要由间苯二胺衍生物或其盐作为偶联组分组成的显影剂 - 偶联剂类型的头发染色组合物，作为显影剂组分，用于氧化染料。

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