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61. 发明授权

US5079361A Thiol-reactive cross-linking reagents 失效
标题翻译： THIOL反应性交联试剂
公开(公告)号：US5079361A
公开(公告)日：1992-01-07
申请号：US246548
申请日：1988-09-09
申请人： Rikki P. Alexander , Michael A. W. Eaton , Thomas A. Millican , Richard C. D. Titmas
发明人： Rikki P. Alexander , Michael A. W. Eaton , Thomas A. Millican , Richard C. D. Titmas
IPC分类号： C07D251/22 , C07D213/00 , C07D213/30 , C07D239/28 , C07K1/107 , C07K14/00 , C07K16/00 , C07K19/00 , C08F26/06 , C08F226/06 , C08G75/02 , C08G75/04
CPC分类号： C07D213/30
摘要： Cross-linking reagents which are highly specific for sulphydryl groups and react with thiols at an excellent rate. The essential feature of the reagents is at least one vinyl group conjugated with an armoatic nitrogen heterocycle. Particular examples include vinyl pyridines, vinyl pyrimidines and vinyl triazines.
摘要翻译： PCT No.PCT / GB88 / 00028 Sec。 371日期：1988年9月9日 102（e）日期1988年9月9日PCT提交1988年1月15日PCT公布。出版物WO88 / 05433 日期：1988年7月28日。交联试剂，其对巯基具有高度特异性，并以极好的速率与硫醇反应。试剂的基本特征是至少一个与铠装的氮杂环共轭的乙烯基。具体实例包括乙烯基吡啶，乙烯基嘧啶和乙烯基三嗪。

62. 发明授权

US4945098A Novel propane-1,3-diol derivatives and use 失效
标题翻译：新型丙-1,3-二醇衍生物和用途
公开(公告)号：US4945098A
公开(公告)日：1990-07-31
申请号：US78525
申请日：1987-07-10
申请人： Gunnar Grue-Sorensen , Christian K. Nielsen
发明人： Gunnar Grue-Sorensen , Christian K. Nielsen
IPC分类号： C07C271/08 , C07C67/00 , C07C213/00 , C07C227/00 , C07C227/08 , C07C229/12 , C07C239/00 , C07C271/06 , C07C325/00 , C07C333/02 , C07D213/00 , C07D217/10 , C07D277/10 , C07D277/22 , C07D277/24 , C07D453/00
CPC分类号： C07D277/24 , C07C271/06 , C07C333/02
摘要： A derivative of 2-methylenepropane-1,3-diol of the general formula I ##STR1## where O--A.sup.1 and O--A.sup.2, which can be the same or different, each represents O, O--C(O), O--C(O)NH, O--C(S)NH or O--C(O)O, R.sup.1 represents an alkyl or alkenyl group of 10-22 carbon atoms, n is an integer from 1 to 11, B.sup.+ represents a quaternary ammonium group, either N.sup.+ R.sup.4 R.sup.5 R.sup.6, or N.sup.+ (Het), where R.sup.4, R.sup.5 and R.sup.6 are similar or different alkyl groups of 1-4 carbon atoms, or two or all of R.sup.4, R.sup.5 and R.sup.6 may be incorporated into a cyclic or bicyclic structure, which may contain additional hetero atoms; X.sup.- means the anion of a pharmceutically acceptable inorganic or organic acid; and R.sup.2 and R.sup.3 are the same or different, and represent hydrogen or alkl groups of 1-4 carbon atoms.The present compounds have been shown to possess a PAF antagonistic effect and an inhibitory effect on the growth of tumor cells, and are thus valuable in the human and veterinary practice as platelet aggregation inhibitors, anti-thrombotic agents, anti-asthmatic agents, anti-allergic agents, anti-inflammatory agents, anti-hypotensive agents, anti-ulcer agents, anti-psoriatic agents, anti-graft rejection agents, anti-conception agents and anti-tumor agents.
摘要翻译： PCT No.PCT / DK86 / 00128 Sec。 371日期1987年7月10日第 102（e）日期1987年7月10日PCT提交1986年11月20日PCT公布。公开号WO87 / 03281 日本6月4日，1987.通式I的2-亚甲基丙烷-1,3-二醇的衍生物，其中O-A1和O-A2可以相同或不同，各自表示O，OC （O），OC（O）NH，OC（S）NH或OC（O）O，R 1表示10-22个碳原子的烷基或链烯基，n为1至11的整数，B +表示季铵基团，N + R4R5R6或N +（Het），其中R4，R5和R6是1-4个碳原子的相似或不同的烷基，或者R4，R5和R6中的两个或全部可以并入环状或双环结构，其可以含有额外的杂原子; X-表示药物可接受的无机或有机酸的阴离子; R2和R3相同或不同，表示1-4个碳原子的氢或烷基。本发明化合物已显示具有PAF拮抗作用和对肿瘤细胞生长的抑制作用，因此在人和兽医学实践中作为血小板聚集抑制剂，抗血栓形成剂，抗哮喘药，抗 - 过敏剂，抗炎剂，抗低血压剂，抗溃疡剂，抗牛皮癣剂，抗移植物排斥剂，抗受孕剂和抗肿瘤剂。

63. 发明授权

US4942169A Piperidine derivative and pharmaceutical composition 失效
标题翻译：哌啶衍生物和药物组合物
公开(公告)号：US4942169A
公开(公告)日：1990-07-17
申请号：US321624
申请日：1989-03-10
申请人： Hachiro Sugimoto , Takaharu Nakamura , Yutaka Tsuchiya , Hiroyuki Sugumi , Kunizou Higurashi , Norio Karibe , Yoshiharu Yamanishi , Hiroo Ogura , Shin Araki , Atsuhiko Kubota , Michiko Ohtake , Kiyomi Tamatsu
发明人： Hachiro Sugimoto , Takaharu Nakamura , Yutaka Tsuchiya , Hiroyuki Sugumi , Kunizou Higurashi , Norio Karibe , Yoshiharu Yamanishi , Hiroo Ogura , Shin Araki , Atsuhiko Kubota , Michiko Ohtake , Kiyomi Tamatsu
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/495 , A61K31/505 , A61P21/00 , A61P25/02 , A61P25/18 , A61P25/28 , A61P43/00 , C07D211/00 , C07D211/14 , C07D211/22 , C07D211/26 , C07D211/32 , C07D211/70 , C07D211/94 , C07D213/00 , C07D239/00 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D471/04 , C07D487/04 , C12N9/99
CPC分类号： C07D401/06 , C07D211/22 , C07D211/26 , C07D401/12 , C07D401/14 , C07D471/04 , C07D487/04
摘要： A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2.] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR5## (in all the above formulas, n is an integer of 1 through 7 and R.sup.3 represents a lower alkyl group or a benzyl group), a group of the formula ##STR6## a group of the formula ##STR7## a group of the formula --O--CH.sub.2 CH.sub.2 CH.dbd. or a group of the formula ##STR8## the ring A denotes a group of the formula ##STR9## a group of the formula ##STR10## a group of the formula ##STR11## or a group of the formula ##STR12## and R.sup.2 denotes a hydrogen atom, a lower alkyl group, a substituted or unsubstituted benzyl group, a substituted or unsubstituted benzoly group, a pyridyl group, a 2-hydroxyethyl group, a pyridylmethyl group or a group of the formula ##STR13## (wherein Z represents a halogen atom).

64. 发明授权

US4937245A Bisphenylalkylpiperazine derivatives, a method of their preparation and a pharmaceutical preparation 失效
标题翻译：二苯基烷基哌嗪衍生物，其制备方法和药物制剂
公开(公告)号：US4937245A
公开(公告)日：1990-06-26
申请号：US282130
申请日：1988-11-30
申请人： Tomas Fex , Knut G. Olsson , Aina L. Abramo , Erik G. Christensson , Torbjorn E. Lundstedt
发明人： Tomas Fex , Knut G. Olsson , Aina L. Abramo , Erik G. Christensson , Torbjorn E. Lundstedt
IPC分类号： A61K31/495 , A61K31/505 , A61K31/535 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D20060101 , C07D213/00 , C07D213/72 , C07D213/74 , C07D213/76 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D239/42 , C07D401/00 , C07D401/04 , C07D401/06 , C07D403/00 , C07D403/04
CPC分类号： C07D213/80 , C07D213/72 , C07D213/82 , C07D213/85 , C07D239/42 , C07D401/06
摘要： A compound having the formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein all the symbols are defined in the specification; having valuable pharmaceutical properties, useful for the treatment of mental disorders, such as psychoses, depression and anxiety.
摘要翻译： PCT No.PCT / SE88 / 00144 Sec。 371日期：1988年11月30日 102（e）1988年11月30日日期PCT提交1988年3月25日PCT公布。出版物WO88 / 07528 日本特开昭通报，1988年10月6日。具有式（I）的化合物或其药学上可接受的盐：其中所有符号在说明书中定义; 具有宝贵的药物性质，可用于治疗精神障碍，如精神病，抑郁症和焦虑症。

65. 发明授权

US4925863A Antifugal azole compounds 失效
标题翻译：防腐唑化合物
公开(公告)号：US4925863A
公开(公告)日：1990-05-15
申请号：US156017
申请日：1988-02-16
申请人： Richard W. Bayles , Francis T. Boyle , Michael B. Gravestock , James M. Wapdleworth
发明人： Richard W. Bayles , Francis T. Boyle , Michael B. Gravestock , James M. Wapdleworth
IPC分类号： A01N43/653 , A01N20060101 , A01N47/02 , A61K20060101 , A61K31/41 , A61K31/44 , A61K31/4427 , A61P31/04 , C07D20060101 , C07D213/00 , C07D233/22 , C07D233/24 , C07D233/26 , C07D249/00 , C07D249/08 , C07D249/14 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D521/00
CPC分类号： C07D231/12 , A01N43/653 , A01N47/02 , C07D233/56 , C07D249/08
摘要： 1,3-Diazolyl-2-propanol derivatives of the formula ##STR1## wherein X and Y are N or CH, R.sup.1 is phenyl, heterocyclyl, heterocyclyl-alkyl, -alkenyl or -alkynyl, optionally substituted, R.sup.2 and R.sup.3 are hydrogen or alkyl, and R.sup.4 and R.sup.5 are hydrogen, amino, alkoxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, or alkenyl, or phenyl, phenylalkyl or phenylalkenyl, heterocycyl, heterocyclyalkyl or heterocyclylalkenyl, each optionally substituted, provided that when R.sup.1 is optionally substituted phenyl at least one of R.sup.1, R.sup.4 and R5 is, or contains, a phenyl ring bearing at least one substitutent selected from cyano, cyanoalkyl, nitro, aminocarbonylalkyl, halogeneoalkoxy and radicals of the formulae --CONR.sup.6 R.sup.7, --NHCOR.sup.8 or OR.sup.9 as defined herein, and the acid addition salts of compounds which contain a basic substituent; together with processes for their manufacture, pharmaceutical, veterinary and plant antifungal compositions, a method of treating fungal diseases in plants, and the use of the compounds for the manufacture of pharmacuetical or veterinary antifungal compositions.
摘要翻译：其中X和Y是N或CH，R 1是苯基，杂环基，杂环基 - 烷基， - 烯基或 - 炔基，任选地被取代，R 2和R 3是氢或烷基，和R 4和R 5是氢，氨基，烷氧基烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基或链烯基，或苯基，苯基烷基或苯基烯基，杂环基，杂环烷基或杂环烯基，各自任选取代，条件是当R 1是任选取代的苯基时，的R 1，R 4和R 5是或含有带有至少一个选自氰基，氰基烷基，硝基，氨基羰基烷基，卤代烷氧基的取代基的苯环，以及如本文所定义的式-CONR 6 R 7，-NHCOR 8或OR 9的基团，含有碱性取代基的化合物的盐; 以及其制造方法，药物，兽医和植物抗真菌组合物，在植物中治疗真菌疾病的方法，以及该化合物用于制备药物或兽医抗真菌组合物的用途。

66. 发明授权

US4913837A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US4913837A
公开(公告)日：1990-04-03
申请号：US116079
申请日：1987-09-01
申请人： George W. Gray , Kenneth J. Toyne , David Lacey , Michael P. Burrow , Rudolf Eidenschink , Andreas Wachtler , Georg Weber
发明人： George W. Gray , Kenneth J. Toyne , David Lacey , Michael P. Burrow , Rudolf Eidenschink , Andreas Wachtler , Georg Weber
IPC分类号： C07D213/00 , C07D213/16 , C07D213/26 , C07D213/30 , C07D213/55 , C07D213/57 , C07D241/12 , C07D241/14 , C07D241/18 , C07D241/24 , C09K19/34
CPC分类号： C07D213/16 , C07D213/26 , C07D213/30 , C07D213/55 , C07D213/57 , C07D241/12 , C07D241/18 , C07D241/24 , C09K19/3444 , C09K19/3452
摘要： Heterocyclic compounds of the formula IR.sup.1 -A.sup.1 -Z.sup.1 -A.sup.2 -[Z.sup.2 -A.sup.3 ].sub.n -R.sup.2Iwherein R.sup.1, R.sup.2, A.sup.1, A.sup.2, A.sup.3, Z.sup.1, Z.sup.2 and n are defined in claim 1, can be used as components of liquid-crystalline phases.
摘要翻译： PCT No.PCT / EP86 / 00760 Sec。 371日期1987年9月1日 102（e）1987年9月1日PCT PCT 1986年12月18日PCT公布。出版物WO87 / 04158 日本1987年7月16日。式I R1-A1-Z1-A2- [Z2-A3] n-R2I的杂环化合物，其中R1，R2，A1，A2，A3，Z1，Z2和n如权利要求1中所定义，可用作液晶相的成分。

67. 发明授权

US4849450A New arthropodicides 失效
标题翻译：新的节肢动物杀虫剂
公开(公告)号：US4849450A
公开(公告)日：1989-07-18
申请号：US044765
申请日：1987-05-01
申请人： George Holan , Reimund A. Walser , Bryan C. Elmes
发明人： George Holan , Reimund A. Walser , Bryan C. Elmes
IPC分类号： C07C69/753 , A01N37/08 , A01N37/10 , A01N37/38 , A01N43/12 , A01N43/30 , A01N43/40 , C07C67/00 , C07C67/08 , C07C69/757 , C07C253/00 , C07C313/00 , C07C323/62 , C07D213/00 , C07D213/64 , C07D213/643
CPC分类号： C07D213/643 , A01N37/08 , A01N37/38 , A01N43/30 , A01N43/40
摘要： Compounds with arthropodicidal activity having the general formula (I); ##STR1## wherein R.sup.1 is a halo group; or a lower alkyl, lower alkoxy or lower alkylthio group, in each of which the alkyl group may be substituted with one or more halo groups; R.sup.2 is hydrogen or a halo or methyl group; or R.sup.1 and R.sup.2 together form a methylenedioxy, or a difluoro-methylenedioxy group or, R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached, form an aromatic ring; R.sup.3 is hydrogen, CN, or C.ident.CH; Y is --CH-- or --N--; Z is H or F; and X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are the same or different and each is hydrogen or a fluoro, bromo or chloro group; with the proviso that Y is --N-- when Z is H.
摘要翻译：具有通式（I）的具有节肢动物杀伤活性的化合物; （I）其中R1是卤素基团; 或低级烷基，低级烷氧基或低级烷硫基，其中烷基可被一个或多个卤素取代; R2是氢或卤素或甲基; 或R 1和R 2一起形成亚甲二氧基或二氟亚甲二氧基，或者R 1和R 2与它们所连接的碳原子一起形成芳香环; R3是氢，CN或C = CH; Y是-CH-或-N-; Z为H或F; 且X 1，X 2，X 3和X 4相同或不同，各自为氢或氟，溴或氯基团; 条件是当Z为H时Y为-N-

68. 发明授权

US4814525A Vapor phase bromination of aromatic compounds 失效
标题翻译：芳香族化合物的气相溴化
公开(公告)号：US4814525A
公开(公告)日：1989-03-21
申请号：US29951
申请日：1987-03-25
申请人： Mark Rule , Donald W. Lane , Gerald C. Tustin
发明人： Mark Rule , Donald W. Lane , Gerald C. Tustin
IPC分类号： C07D213/00 , B01J29/14 , B01J29/16 , C07B31/00 , C07B39/00 , C07B61/00 , C07C17/00 , C07C17/156 , C07C25/02 , C07C25/13 , C07C25/18 , C07C25/22 , C07C41/00 , C07C41/22 , C07C43/29 , C07C45/00 , C07C49/813 , C07C67/00 , C07C313/00 , C07C315/04 , C07C317/14 , C07D213/61 , C07C17/15 , C07C17/152
CPC分类号： C07C17/156
摘要： The process relates to a process for the vapor phase bromination of aromatic compounds in the presence of oxygen and a catalyst comprising an oxidizing metal and an inert support.
摘要翻译：该方法涉及在氧存在下芳族化合物的气相溴化和包含氧化性金属和惰性载体的催化剂的方法。

69. 发明授权

US4792641A Process for preparing iodinated aromatic compounds 失效
标题翻译：制备碘化芳香族化合物的方法
公开(公告)号：US4792641A
公开(公告)日：1988-12-20
申请号：US29899
申请日：1987-03-25
申请人： Mark Rule , Donald W. Lane , Thomas H. Larkins , Gerald C. Tustin
发明人： Mark Rule , Donald W. Lane , Thomas H. Larkins , Gerald C. Tustin
IPC分类号： C07D215/18 , B01J29/10 , C07B31/00 , C07B39/00 , C07B61/00 , C07C17/00 , C07C17/12 , C07C17/156 , C07C17/358 , C07C25/02 , C07C25/18 , C07C25/22 , C07C41/22 , C07C67/00 , C07C313/00 , C07C315/04 , C07C317/14 , C07C319/20 , C07C323/09 , C07D213/00 , C07D307/00 , C07D333/00 , C07C17/24
CPC分类号： C07C17/358 , C07C17/00 , C07C17/156
摘要： The invention relates to a process for isomerizing and transiodinating iodoaromatic compounds over a non-acid catalyst.
摘要翻译：本发明涉及一种在非酸催化剂上异构化和转移碘代芳族化合物的方法。

70. 发明授权

US4788206A Pentadieneamides 失效
标题翻译：戊二酰胺
公开(公告)号：US4788206A
公开(公告)日：1988-11-29
申请号：US72389
申请日：1987-07-10
申请人： Robert W. Guthrie , Richard W. Kierstead , Jefferson W. Tilley
发明人： Robert W. Guthrie , Richard W. Kierstead , Jefferson W. Tilley
IPC分类号： C07D213/38 , A61K31/16 , A61K31/34 , A61K31/35 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/535 , A61K31/54 , A61P7/02 , C07C233/38 , C07D207/335 , C07D213/40 , C07D213/56 , C07D217/02 , C07D217/14 , C07D217/16 , C07D227/00 , C07D247/00 , C07D269/00 , C07D283/00 , C07D409/12 , C07D521/00 , C07D213/00
CPC分类号： C07D409/12 , C07D213/56 , C07D217/02 , C07D217/16
摘要： Compounds of the formula ##STR1## Y is O ir S, *A is paraphenylene or *----(CH.sub.2)n----(X).sub.m --(CH.sub.2).sub.r ----, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, aryl, R.sub.3, R.sub.4 and R.sub.8, independently, are hydrogen, lower alkyl, aryl, R.sub.5 and R.sub.6, independently, are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof, are described.The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characerized by excess platelet activating factor or for the prevention and treatment of cardiovascular disease, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.
摘要翻译：式（I）的化合物是O，S是对亚苯基或* - （CH 2）n - （X）m - （CH 2）r - ，X是O，S或-CH = CH- ，n或r独立地为0至3的整数，s为0至1的整数，m为0至1的整数，条件是当m为1时，n + s必须至少为2，R1和 R2独立地是氢，低级烷基，环烷基，低级烯基，Het，芳基，R3，R4和R8独立地是氢，低级烷基，芳基，R5和R6独立地是氢或低级烷基，R7是氢，低级烷基，环烷基，Het-低级烷基或芳基，Het是含有一个或两个选自氮，氧和硫的杂原子的单环五元或六元杂芳族或双环杂芳族基团，该基团可以被低级烷基，卤素或芳基，星号表示连接点，当R 6和R 7不同时，当R 1和R 2不同时，它们的对映异构体和外消旋混合物，它们的几何异构体和药学上可接受的描述了它们的酸加成盐。式I的化合物表现出作为血小板活化因子（PAF）拮抗剂的活性，因此可用于由过量血小板活化因子引起的疾病状态或用于预防和治疗心血管疾病，肺部疾病，免疫学疾病，炎性疾病，皮肤病学疾病，休克或移植排斥。

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