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131. 发明授权

US4742060A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US4742060A
公开(公告)日：1988-05-03
申请号：US821621
申请日：1986-01-21
申请人： Kozo Shiokawa , Shinichi Tsuboi , Shinzo Kagabu , Koichi Moriya
发明人： Kozo Shiokawa , Shinichi Tsuboi , Shinzo Kagabu , Koichi Moriya
IPC分类号： A01N43/78 , A01N20060101 , A01N33/18 , A01N43/00 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/647 , A01N43/653 , A01N43/66 , A01N43/72 , A01N43/74 , A01N43/76 , A01N43/80 , A01N43/82 , A01N43/84 , A01N43/86 , A01N43/88 , A01N47/02 , A01N47/16 , A01N47/22 , A01N47/38 , A01N51/00 , A01N57/32 , C07D20060101 , C07D207/20 , C07D207/22 , C07D211/70 , C07D211/72 , C07D213/00 , C07D213/61 , C07D233/20 , C07D233/52 , C07D239/06 , C07D239/18 , C07D263/10 , C07D263/28 , C07D265/08 , C07D277/00 , C07D277/10 , C07D277/18 , C07D279/00 , C07D279/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D419/06 , C07F9/6558 , A01N43/707 , A01N43/713 , C07D407/06 , C07D407/14 , C07D411/06 , C07D411/14
CPC分类号： C07D239/06 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/653 , A01N43/74 , A01N43/80 , A01N43/82 , A01N43/86 , A01N47/02 , A01N47/16 , A01N47/22 , A01N47/38 , A01N51/00 , A01N57/32 , C07D207/20 , C07D207/22 , C07D211/70 , C07D211/72 , C07D233/20 , C07D233/52 , C07D239/18 , C07D263/10 , C07D263/28 , C07D265/08 , C07D277/10 , C07D277/18 , C07D279/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07F9/65583
摘要： Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.
摘要翻译：式中，n为0或1的新型杀虫剂，其中X为S，O，Y为N或Z为5或6元含氮杂环，R为 R9各自表示氢或特定的有机基团。

132. 发明授权

US4695577A Anti-hypertensive agents 失效
公开(公告)号：US4695577A
公开(公告)日：1987-09-22
申请号：US64901
申请日：1979-08-14
申请人： James W. Ryan , Alfred Chung
发明人： James W. Ryan , Alfred Chung
IPC分类号： A61K38/00 , C07D207/16 , C07D207/22 , C07D207/50 , C07K5/068 , C07K5/078 , A61K31/40 , A61K31/41 , C07D207/00 , C07D211/72
CPC分类号： C07K5/06173 , C07D207/16 , C07D207/22 , C07D207/50 , C07K5/06086 , A61K38/00
摘要： Novel compounds are disclosed as potent inhibitors of angiotensin converting enzyme and as orally effective antihypertensive agents. The compounds have the general formula: ##STR1##

133. 发明授权

US4692437A Anti-hypertensive agents 失效
标题翻译：抗高血压药
公开(公告)号：US4692437A
公开(公告)日：1987-09-08
申请号：US156749
申请日：1980-06-05
申请人： James W. Ryan , Alfred Chung
发明人： James W. Ryan , Alfred Chung
IPC分类号： A61K38/55 , A61K20060101 , A61K31/40 , A61K31/401 , A61K31/405 , A61K38/00 , A61P9/12 , A61P43/00 , C07C20060101 , C07C67/00 , C07C325/00 , C07C327/20 , C07D207/16 , C07D207/22 , C07D207/50 , C07D403/12 , C07K1/113 , C07K5/06 , C07K5/068 , C07K5/078 , C07K5/08 , C07K14/81 , A61K31/425 , C07D207/00 , C07D277/04
CPC分类号： C07D207/16 , C07D207/22 , C07D207/50 , C07K5/06086 , C07K5/06173 , A61K38/00 , Y10S930/12
摘要： Inhibitors of angiotensin converting enzyme which are physiologically acceptable salts of compounds which have the formula: ##STR1## wherein R is hydrogen, formyl, acetyl, propanoyl, butanoyl, phenylacetyl, phenylpropanoyl, benzoyl, cyclopentanecarbonyl, tert-butyloxycarbonyl, cyclopentanecarbonyl-L-lysyl, pyro-L-glutamyl-L-lysyl, L-lysyl, L-arginyl or pyro-L-glutamyl;A is phenylalanyl, glycyl, alanyl, tryptophyl, tyrosyl, isoleucyl, leucyl, histidyl, or valyl, the .alpha.-amino group thereof being in amide linkage with R;R.sub.1 is hydrogen or methyl;R.sub.2 is L-proline, L-3,4-dehydroproline, D,L-3,4-dehydroproline, L-3-hydroxyproline, L-4-hydroxyproline, L-thiazolidine-4-carboxylic acid, or L-5-oxo-proline, the imino group thereof being in imide linkage with the adjacent ##STR2## and, n is 0 or 1, such that when n is O, R.sub.1 is methyl are disclosed as useful anti-hypertensive agents.
摘要翻译：其中R为氢，甲酰基，乙酰基，丙酰基，丁酰基，苯乙酰基，苯基丙酰基，苯甲酰基，环戊烷羰基，叔丁氧基羰基，环戊烷羰基-L-赖氨酰基的化合物的生理上可接受的盐的血管紧张素转换酶抑制剂，pyro-L-谷氨酰-L-赖氨酰，L-赖氨酰，L-精氨酰或焦-L-谷氨酰; A是与R的酰胺键合的苯丙氨酰基，甘氨酰基，丙氨酰基，色氨酸，酪氨酰基，异亮氨酰基，亮氨酰基，组氨酰基或缬氨酰基; R1是氢或甲基; R2是L-脯氨酸，L-3,4-脱氢脯氨酸，D，L-3,4-脱氢脯氨酸，L-3-羟脯氨酸，L-4-羟基脯氨酸，L-噻唑烷-4-羧酸或L-5- 氧基 - 脯氨酸，其亚氨基与相邻的“IMAGE”具有酰亚胺键，并且n为0或1，使得当n为O时，R 1为甲基作为有用的抗高血压剂公开。

134. 发明授权

US4680413A Process for the production of 3-phenyl-4-cyanopyrroles 失效
标题翻译： 3-苯基-4-氰基吡咯的制备方法
公开(公告)号：US4680413A
公开(公告)日：1987-07-14
申请号：US814893
申请日：1985-12-30
申请人： Yoshikazu Genda , Hiroyuki Muro , Kiyoharu Nakayama , Yoshiaki Miyazaki , Yoshiji Sugita
发明人： Yoshikazu Genda , Hiroyuki Muro , Kiyoharu Nakayama , Yoshiaki Miyazaki , Yoshiji Sugita
IPC分类号： C07D207/34 , C07D405/04 , C07D207/22
CPC分类号： C07D405/04 , C07D207/34
摘要： A process for the production of a compound having the formula: ##STR1## which comprises a reaction of a compound having the formula: ##STR2## with a compound having the formulaR.sup.2 SO.sub.2 CH.sub.2 NCwhereinX is same or different substituent(s) selected from the group consisting of halogen, C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, C.sub.1-6 alkylamino, C.sub.1-6 alkoxy, nitro, cyano and methylenedioxy;COOR.sup.1 is carboxylic acid or ester;R.sup.2 is C.sub.1-10 cyclic hydrocarbon which may be substituted by substituent(s) not giving negative effects to said reaction;n is 0, 1 or 2.
摘要翻译：制备具有下式的化合物的方法：包括具有下式的化合物与下式的化合物的反应：其中X是相同或不同的选自下列基团的取代基：由卤素，C 1-6烷基，C 1-6卤代烷基，C 1-6烷基氨基，C 1-6烷氧基，硝基，氰基和亚甲二氧基组成。 COOR1是羧酸或酯; R2是可以被不对所述反应产生负面影响的取代基取代的C1-10环烃; n为0,1或2。

135. 发明授权

US4656270A Process for producing guanidines such as linogliride 失效
标题翻译：生产鸟苷类药物的方法
公开(公告)号：US4656270A
公开(公告)日：1987-04-07
申请号：US711948
申请日：1985-03-15
申请人： Cynthia A. Maryanoff , James N. Plampin , Robin C. Stanzione
发明人： Cynthia A. Maryanoff , James N. Plampin , Robin C. Stanzione
IPC分类号： C07D207/22 , B01J23/00 , C07B61/00 , C07C67/00 , C07C301/00 , C07C303/16 , C07C309/16 , C07C313/00 , C07C335/16 , C07C381/14 , C07D207/26 , C07D207/273 , C07D295/14 , C07D295/215 , C07D295/12 , C07D413/12
CPC分类号： C07D207/273 , C07C381/14 , C07D295/215
摘要： Novel synthetic steps and intermediates leading to guanidines such as the anti-diabetic compound linogliride. Included is a hydrogen peroxide oxidation of a thiourea (II) to a sulfonic acid (I) which may then be reacted with morpholine to form the carboximidamide (III): ##STR1##
摘要翻译：新的合成步骤和中间体导致胍如抗糖尿病化合物林格列里。包括硫脲（II）到磺酸（I）的过氧化氢氧化，然后其可以与吗啉反应以形成甲脒（III）：

136. 发明授权

US4650749A Heat-developable light-sensitive material 失效
标题翻译：可热成像的感光材料
公开(公告)号：US4650749A
公开(公告)日：1987-03-17
申请号：US769274
申请日：1985-08-26
申请人： Kozo Sato , Yoshiharu Yabuki , Hiroyuki Hirai , Ken Kawata
发明人： Kozo Sato , Yoshiharu Yabuki , Hiroyuki Hirai , Ken Kawata
IPC分类号： G03C8/40 , B41M5/26 , C07C51/00 , C07C59/58 , C07C59/64 , C07C59/66 , C07C67/00 , C07C239/00 , C07C279/02 , C07C301/00 , C07C311/03 , C07D207/22 , C07D231/12 , C07D231/56 , C07D233/60 , C07D235/06 , C07D235/22 , C07D249/18 , C07D257/04 , C07D317/30 , C07D317/46 , C07D521/00 , G03C1/06 , G03C1/498 , G03C7/00 , G03C1/02
CPC分类号： G03C1/49845 , Y10S430/156
摘要： A heat developable light-sensitive material containing a compound represented by formula (I) or (II) ##STR1## wherein R.sub.1 and R.sub.2 each represents a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aralkyl group, an aryl group, a heterocyclic group, a carboxyl group or a salt thereof, a halogen atom, a cyano group, an alkylsulfonyl or arylsulfonyl group, a sulfamoyl group, a carbamoyl group, an alkoxycarbonyl or aryloxycarbonyl group, a di- or mono-alkylphosphoryl or arylphosphoryl group, a di- or mono-alkylphosphinyl or arylphosphinyl group, an alkylsulfinyl or arylsulfinyl group, an acyl group, an amino group, an acylamino group, an acyloxy group or a group represented by X; X represents a decarboxylation accelerating group; or any two of R.sub.1, R.sub.2, and X may combine to form a ring; and the groups represented by R.sub.1, R.sub.2 and X may further be substituted with a substituent; B represents an organic base; and n represents 1 when B represents a monoacid base or 2 when B represents a diacid base, provided that when ##STR2## is a free dibasic acid, n is 1/2 of the above described numbers, respectively.The heat developable light-sensitive material containing a base precursor represented by formula (I) or (II) has excellent stability during preservation before use, and provides a color image having a high color density and low fog in a short time.
摘要翻译：含有式（I）或（II）表示的化合物的热显影性感光材料其中R 1和R 2各自表示氢原子，烷基，环烷基，烯基，炔基，芳烷基，芳基，杂环基，羧基或其盐，卤素原子，氰基，烷基磺酰基或芳基磺酰基，氨磺酰基，氨基甲酰基，烷氧基羰基或芳氧基羰基，二 - 或单烷基磷酰基或芳基磷酰基，二 - 或单烷基氧膦基或芳基氧膦基，烷基亚磺酰基或芳基亚磺酰基，酰基，氨基，酰氨基，酰氧基或由X代表的组; X表示脱羧加成基团; 或者R1，R2和X中的任何两个可以结合形成环; 并且由R 1，R 2和X表示的基团可以进一步被取代基取代; B表示有机碱; 当B代表一酸基时，n表示1，B表示二酸基时，n表示1，条件是当为游离二元酸时，n分别为上述数字的1/2。含有由式（I）或（II）表示的碱前体的可热显影的感光材料在使用前的保存期间具有优异的稳定性，并且在短时间内提供具有高着色密度和低雾度的彩色图像。

137. 发明授权

US4393218A 2,2,4,5,5-Pentamethyl-3-formyl-.DELTA..sup.3 -pyrroline and the preparation thereof 失效
标题翻译： 2,2,4,5,5-五甲基-3-甲酰基-3β-吡咯啉及其制备方法
公开(公告)号：US4393218A
公开(公告)日：1983-07-12
申请号：US327753
申请日：1981-12-07
申请人： Silvestro Costanzi , Francesco Tessarolo , Maurizio Brunelli
发明人： Silvestro Costanzi , Francesco Tessarolo , Maurizio Brunelli
IPC分类号： C07D207/22 , C07D207/08 , C07D207/20 , C07D207/24
CPC分类号： C07D207/08 , C07D207/20
摘要： A process for preparing 2,2-dialkyl-4-methyl-5,5-dialkyl-3-formyl-.DELTA..sup.3 -pyrrolines by reacting the corresponding dialkyl substituted di-tert-propargylamines with water at a pH equal to or less than 3.0. Preferably, an inorganic mercury compound is used as a catalyst.
摘要翻译：通过使相应的二烷基取代的二 - 叔炔丙胺与等于或小于3.0的pH的水反应来制备2,2-二烷基-4-甲基-5,5-二烷基-3-甲酰基-D-TA-吡咯啉的方法。优选使用无机汞化合物作为催化剂。

138. 发明授权

US4377701A 4-Methylene-1-[[(alranoyl or arylcarbonyl)mercapto]acyl]proline and pipecolic acid 失效
标题翻译： 4-亚甲基-1 - [[（丙烯酰基或芳基羰基）巯基]酰基]脯氨酸和哌啶酸
公开(公告)号：US4377701A
公开(公告)日：1983-03-22
申请号：US304148
申请日：1981-09-21
申请人： Sesha I. Natarajan , Miguel A. Ondetti
发明人： Sesha I. Natarajan , Miguel A. Ondetti
IPC分类号： A61K31/40 , A61K31/401 , A61K31/445 , A61K31/455 , A61P9/12 , A61P43/00 , C07D207/22 , C07D211/78
CPC分类号： C07D211/78 , C07D207/22 , Y02P20/55
摘要： Compounds having the formula ##STR1## and salts thereof, wherein R.sub.1 is a readily hydrolyzable acyl protecting group;R.sub.2 is hydrogen or alkyl;R.sub.3 is hydrogen, alkyl or arylalkyl;n is 1 or 2; andp is 1 or 2inhibit the action of angiotensin converting enzyme.
摘要翻译：具有式“IMAGE”的化合物及其盐，其中R 1是易水解的酰基保护基; R2是氢或烷基; R3是氢，烷基或芳基烷基; n为1或2; p为1或2抑制血管紧张素转换酶的作用。

139. 发明授权

US4259238A N-Phenyl amidines 失效
标题翻译： N-苯基脒
公开(公告)号：US4259238A
公开(公告)日：1981-03-31
申请号：US95891
申请日：1979-11-19
申请人： Yao H. Wu , Walter G. Lobeck, Jr.
发明人： Yao H. Wu , Walter G. Lobeck, Jr.
IPC分类号： C07D207/22 , A61K31/395 , C07D225/00
CPC分类号： C07D207/22
摘要： N-Phenyl amidines which have diuretic, antithrombogenic, smooth muscle relaxant, anti-inflammatory and antiarrhythmic properties have been discovered. They are prepared by reacting a substituted aniline with a carboxamide selected from the group consisting of amides and lactams in the presence of phosphorus oxychloride. Typical examples of substituted N-phenyl amidines thus obtained are 5-methyl-2-(N-phenylbenzylamino)-1-pyrroline, 2-(N-phenylbenzylamino)-1-pyrroline, 3-[(N-1-pyrrolin-1-yl-p-anisidino)methyl]indole and 4,5,6,7,8,9-hexahydro-2-(N-phenylphenethylamino)-3H-azonine. Indole substituted N-phenyl amidines can be arranged to provide iminopyrrolinidinylindoles which are useful as diuretic, antithrombogenic and smooth muscle relaxant agents. In the case of 3-[(N-1-pyrrolin-2-yl-p-anisidino)methyl]indole, the rearranged product is 3-[[2-p-methoxyphenylimino)-1-pyrrolidinyl]methyl]indole.
摘要翻译：已经发现具有利尿，抗血栓形成，平滑肌松弛剂，抗炎和抗心律失常性质的N-苯基脒。它们通过在磷酰氯存在下使取代的苯胺与选自酰胺和内酰胺的羧酰胺反应来制备。由此获得的取代的N-苯基脒的典型实例是5-甲基-2-（N-苯基苄基氨基）-1-吡咯啉，2-（N-苯基苄基氨基）-1-吡咯啉，3 - [（N-1-吡咯啉-1-基 - 对 - 茴香酰基）甲基]吲哚和4,5,6,7,8,9-六氢-2-（N-苯基苯乙基氨基）-3H-吖嗪。吲哚取代的N-苯基脒可以被排列成提供可用作利尿剂，抗血栓形成和平滑肌松弛剂的亚氨基吡咯烷啶二醇。在3 - [（N-1-吡咯啉-2-基 - 对茴香酰基）甲基]吲哚的情况下，重排产物是3 - [[2-对 - 甲氧基苯基亚氨基] -1-吡咯烷基]甲基]吲哚。

140. 发明授权

US4255334A Process for preparing 3-azabicyclo(3.1.0)hexane-2-carboxylic acid 失效
公开(公告)号：US4255334A
公开(公告)日：1981-03-10
申请号：US49374
申请日：1979-06-18
申请人： Janet A. Day , Barry R. J. Devlin , Robert J. G. Searle
发明人： Janet A. Day , Barry R. J. Devlin , Robert J. G. Searle
IPC分类号： C07D209/52 , C07D207/20 , C07D207/22
CPC分类号： C07C255/00 , C07D209/52
摘要： 3-Azabicyclo(3.1.0)hexane-2-carboxylic acid, a plant gametocide, is prepared by effecting reaction between cis 2-aminomethylcyclopropyl-1,1-dimethyl acetal and a cyanide in the presence of a liquid lower-alkanecarboxylic acid; treating the resulting N-alkanoyl-3-azabicyclo(2.1.0)hexane-2-carbonitrile with a strong acid; treating the resulting 3-alkanoyl-3-azabicyclo(3.1.0)hexane-2-carboxylic acid with strong acid to form the desired 3-azabicyclo(3.1.0)hexane-2-carboxylic acid.

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