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61. 发明授权

US4666901A Substituted lactams useful as angiotensin converting enzyme inhibitors 失效
标题翻译：用作血管紧张素转换酶抑制剂的取代的内酰胺
公开(公告)号：US4666901A
公开(公告)日：1987-05-19
申请号：US810125
申请日：1985-12-18
申请人： William H. Parsons
发明人： William H. Parsons
IPC分类号： C07D223/12 , C07D225/02 , A61K31/55 , C07D223/10
CPC分类号： C07D223/12 , C07D225/02
摘要： Substituted lactams and related compounds and methods for their preparation are disclosed. These compounds are useful as angiotensin converting enzyme inhibitors and as antihypertensives.
摘要翻译：公开了取代的内酰胺及其相关化合物及其制备方法。这些化合物可用作血管紧张素转换酶抑制剂和抗高血压药。

62. 发明授权

US4550169A Platinum chelates of 2-hydrazino-azoles 失效
标题翻译： 2-肼基 - 吡唑的铂螯合物
公开(公告)号：US4550169A
公开(公告)日：1985-10-29
申请号：US553675
申请日：1983-11-21
申请人： Joseph J. Hlavka , Panayota Bitha , Yang-I Lin
发明人： Joseph J. Hlavka , Panayota Bitha , Yang-I Lin
IPC分类号： A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/445 , A61K31/454 , A61K31/496 , A61K31/505 , A61K31/55 , A61P35/00 , A61P35/02 , C07D207/22 , C07D211/72 , C07D223/12 , C07D223/16 , C07D225/02 , C07D233/42 , C07D233/52 , C07D233/88 , C07D235/28 , C07D235/30 , C07D239/10 , C07D239/18 , C07D243/04 , C07D243/08 , C07D243/10 , C07F15/00
CPC分类号： C07D239/10 , C07D207/22 , C07D211/72 , C07D223/12 , C07D233/42 , C07D233/52 , C07D235/28 , C07D235/30 , C07D239/18 , C07D243/04 , C07D243/08 , C07F15/0093
摘要： This disclosure describes platinum chelates of 2-hydrazino-1-aza (or 1,3-diaza,1-oxa-3-aza or 1-thia-3-aza)-1-cyclo-alkenes which possess activity as antitumor agents.
摘要翻译：本公开内容描述了具有活性作为抗肿瘤剂的2-肼基-1-氮杂（或1,3-二氮杂，1-氧杂-3-氮杂或1-硫杂-3-氮杂）-1-环烯烃的铂螯合物。

63. 发明授权

US4259239A Resolution of enantiomeric complexes of nickelous chloride and alpha-aminocaprolactam 失效
标题翻译：拆分氯化镍和α-氨基己内酰胺的对映体络合物
公开(公告)号：US4259239A
公开(公告)日：1981-03-31
申请号：US142530
申请日：1980-04-21
申请人： Stylianos Sifniades , Meir Lahav , William J. Boyle, Jr.
发明人： Stylianos Sifniades , Meir Lahav , William J. Boyle, Jr.
IPC分类号： C07D223/12 , C07D223/10
CPC分类号： C07D223/12
摘要： A racemic mixture of D- and L- forms of alpha-aminocaprolactam ("ACL") dissolved in e.g. ethanol is resolved, and preferably the undesired form remaining is solution is simultaneously racemized, by forming a supersaturated solution of the D,L-(ACL).sub.3 NiCl.sub.2. EtOH complex; providing an optically active form of lysine (e.g. L-lysine) as crystallization inhibitor of the undesired enantiomer of said complex (e.g. the D-form), and crystallizing a portion of the desired form of the complex from the solution. The undesired form remaining in solution can be simultaneously racemized by providing a strong base and an excess of ACL over the stoichiometric proportion required to form the complex. The recovered crystals of the desired form of the complex can be processed to afford the desired form of ACL, and to recover the nickel reagent. The ACL can be converted to the desired form of lysine, a nutritionally valuable amino acid.
摘要翻译： D-和L-形式的α-氨基己内酰胺（“ACL”）的外消旋混合物溶于例如乙醇被分解，并且优选地，通过形成D，L-（ACL）3 NCl 2的过饱和溶液，将残留的不需要的形式溶液同时外消旋化。乙醇络合物提供赖氨酸（例如L-赖氨酸）的光学活性形式作为所述复合物（例如D型）的不需要的对映异构体的结晶抑制剂，并从溶液中结晶一部分所需形式的络合物。残留在溶液中的不需要的形式可以通过提供形成复合物所需的化学计量比例的强碱和过量的ACL来同时外消旋化。可以将所需形式的复合物的回收晶体加工以提供所需形式的ACL，并回收镍试剂。 ACL可以转化为所需形式的赖氨酸，这是一种营养有价值的氨基酸。

64. 发明授权

US4140686A Method for purifying .alpha.-amino-.epsilon.-caprolactam 失效
标题翻译：纯化{60-氨基 - {68-己内酰胺
公开(公告)号：US4140686A
公开(公告)日：1979-02-20
申请号：US845392
申请日：1977-10-25
申请人： Ichiro Kawamoto , Takeshi Sekoguchi , Yoshihiro Shibai
发明人： Ichiro Kawamoto , Takeshi Sekoguchi , Yoshihiro Shibai
IPC分类号： C07D223/12 , C07D223/10
CPC分类号： C07D223/12
摘要： Purified .alpha.-amino-.epsilon.-caprolactam free from not only visible ray-absorbing substances but ultra-violet ray-absorbing substances, such as, tetrahydrophenazine and octahydrophenazine, and volatile basic substances such as, ammonium salts, is obtained by dissolving a crude .alpha.-amino-.epsilon.-caprolactam in a solvent consisting of at least one alkyl ester of saturated aliphatic acid of the formula:C.sub.m H.sub.2m+1 COOC.sub.n H.sub.2n+1wherein m is 1 or 2 and n is 1, 2, 3 or 4, at an elevated temperature at which the crude material can be completely dissolved in the solvent, cooling the solution to a lowered temperature at which the .alpha.-amino-.epsilon.caprolactam is allowed to recrystallize from the solution, and separating the crystals of the purified .alpha.-amino-undecanoic acid from the solution.
摘要翻译：通过溶解粗α（α-甲基苯乙烯）衍生物，得到纯化的α-氨基 - ε-己内酰胺，不仅含有可见光吸收物质，而且不含有四氢吩嗪和八氢吩嗪等紫外线吸收物质，以及挥发性碱性物质如铵盐， - 氨基 - ε-己内酰胺在由至少一种下式的饱和脂族酸的烷基酯组成的溶剂中：

65. 发明授权

US4126621A Substituted cycloalkyl lactamimides 失效
公开(公告)号：US4126621A
公开(公告)日：1978-11-21
申请号：US877652
申请日：1978-02-14
申请人： Johann M. Grisar , Thomas R. Blohm , Edward M. Roberts
发明人： Johann M. Grisar , Thomas R. Blohm , Edward M. Roberts
IPC分类号： C07D207/22 , C07D211/72 , C07D223/10 , C07D223/12 , C07D225/02 , A61K31/40 , A61K31/445 , A61K31/55 , C07D409/08
CPC分类号： C07D207/22 , C07D211/72 , C07D223/10 , C07D223/12 , C07D225/02 , Y10S514/822 , Y10S514/866 , Y10S514/869 , Y10S514/884
摘要： Compounds possessing hypoglycemic, hypotensive, antiinflammatory, anticoagulant and diuretic activity are represented by compounds of the following formula ##STR1## wherein Y is thienyl, cycloalkyl of from 5 to 7 carbon atoms, phenyl or substituted phenyl in which case the substituents on the substituted phenyl are selected from halogen, such as fluorine, chlorine, bromine or iodine, lower alkyl of from 1 to 4 carbon atoms and lower alkoxy of from 1 to 4 carbon atoms; Z is hydrogen or hydroxy; R is hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl of from 1 to 4 carbon atoms or halogen, such as chlorine, fluorine, bromine or iodine; m is from 3 to 6; and n is from 3 to 11. Pharmaceutical compositions of these compounds and their use are also disclosed.

66. 发明授权

US3988320A Single stage resolution/racemization of .alpha.-amino-.epsilon.-caprolactam 失效
标题翻译： {60-氨基 - {68-己内酰胺的单级拆分/外消旋化
公开(公告)号：US3988320A
公开(公告)日：1976-10-26
申请号：US565911
申请日：1975-04-07
申请人： Stylianos Sifniades , William J. Boyle, Jr. , Jan F. Van Peppen
发明人： Stylianos Sifniades , William J. Boyle, Jr. , Jan F. Van Peppen
IPC分类号： C07D223/12 , C07D223/08
CPC分类号： C07D223/12
摘要： Resolution of .alpha.-amino-.epsilon.-caprolactam with simultaneous racemization of the undesired D-.alpha.-amino-.epsilon.-caprolactam enantiomer is effected by forming a coordinately saturated .alpha.-amino-.epsilon.-caprolactam complex with NiCl.sub.2, preferably crystallizing the L-.alpha.-amino-.epsilon.-caprolactam complex in the presence of fine seed crystals of L-.alpha.-amino-.epsilon.-caprolactam complex of NiCl.sub.2 and catalytic amounts of a strong base selected from the alkoxides or hydroxides of Ni(II) and recovering L-.alpha.-amino-.epsilon.-caprolactam hydrochloride from the crystalline product.
摘要翻译：通过与NiCl 2形成配位饱和的α-氨基 - ε-己内酰胺络合物，优选结晶L-阿尔法 - ε-己内酰胺对映异构体，同时消除不需要的D- 存在NiCl 2的L-氨基 - ε-己内酰胺络合物和催化量的选自Ni（II）的醇盐或氢氧化物的强碱的精细晶种存在下的氨基ε-己内酰胺络合物，并回收L- 氨基 - ε-己内酰胺盐酸盐。

67. 发明授权

US3963748A 1-Phenyl-3-azacarbocyclic-ureas 失效
标题翻译： 1-苯基-3-氮杂环脲
公开(公告)号：US3963748A
公开(公告)日：1976-06-15
申请号：US536755
申请日：1974-12-27
申请人： Guy D. Diana
发明人： Guy D. Diana
IPC分类号： C07C51/373 , C07D207/22 , C07D211/72 , C07D211/76 , C07D223/10 , C07D223/12 , C07D207/14
CPC分类号： C07D223/12 , C07C51/373 , C07D207/22 , C07D211/72 , C07D211/76 , C07D223/10
摘要： The compounds of this invention are novel 1-phenyl-3-azacarbocyclic-ureas having anthelmintic activity which are prepared by the reaction of azacarbocyclicamines or azacarbocyclicimines with appropriate phenyl isocyanates.
摘要翻译：本发明的化合物是具有驱虫活性的新颖的1-苯基-3-氮丙
环脲，它是通过氮杂环丙胺或氮杂环丙烷与适当的苯基异氰酸酯反应而制备的。

68. 发明授权

US3904610A Method of preparing an ' -amino-'7 -lactam 失效
标题翻译：制备'-AMINO-7 -LACTAM的方法
公开(公告)号：US3904610A
公开(公告)日：1975-09-09
申请号：US52628174
申请日：1974-11-22
申请人： ALLIED CHEM
发明人： FUHRMANN ROBERT , PISANCHYN JOHN
IPC分类号： C07D223/12 , C07D207/26 , C07D211/76
CPC分类号： C07D223/12
摘要： There is provided an improved method of producing an Alpha amino- omega -lactam of the formula

BY THE Beckmann rearrangement of an Alpha -aminocycloalkanone oxime of the formula

WHEREIN N IS AN INTEGER BETWEEN 0 AND 12, THE IMPROVEMENT COMPRISING THE STEPS OF: 1. DISSOLVING, IN A FIRST REACTION STEP, THE OXIME OR A MIXTURE CONTAINING THE OXIME AND AN ACID SALT THEREOF, AND NH4Cl in sulfuric acid having a concentration of about 100 to 110% (i.e., water-free sulfuric acid containing up to 45% by weight of free SO3) while maintaining a temperature in the first reaction step in the range of about -5* to 35*C; 2. removing the evolved HCl gas formed in the first reaction step; 3. ADDING, IN A SECOND REACTION STEP THE SOLUTION FROM THE FIRST REACTION STEP TO SULFURIC ACID OF A CONCENTRATION OF ABOUT 100 TO 110% OR TO A Beckmann rearrangement mixture derived from said oxime containing sulfuric acid of such concentration while maintaining a temperature in said second reaction step below about 100*C by cooling, the rate of addition of the solution and the amount of cooling being adjusted to maintain the temperature in said range, whereby a rearrangement mixture is formed; 4. REMOVING THE EVOLVED HCl gas formed in the second reaction step; and 5. STRIPPING RESIDUAL HCl from the rearrangement mixture, whereby a lactam solution substantially free of HCl is formed.

69. 发明授权

US3865809A O-(n-methylthiocarbamoyl)-hexamethylenimine-2-oxime 失效
标题翻译： O-（N-甲基氨基甲酰基） - 十六酰基嘧啶-2-氧化物
公开(公告)号：US3865809A
公开(公告)日：1975-02-11
申请号：US38386473
申请日：1973-07-30
申请人： ALLIED CHEM
发明人： TETENBAUM MARVIN THEODORE
IPC分类号： A01N47/24 , C07D223/12 , C07D27/04 , C07D29/34 , C07D41/04
CPC分类号： C07D223/12 , A01N47/24
摘要： Novel derivatives of alkylenimine-2-oximes having the general formula:

WHEREIN N IS 2 TO 10 AND R and R'' are selected from the group consisting of hydrogen, alkenyl, alkyl, cycloalkyl, aryl, and substituted aryl, are effective in controlling soil nematodes and plant diseases caused by microorganisms such as plant pathogenic fungi.
摘要翻译：具有以下通式的亚烷基亚胺-2-肟的新衍生物：

70. 发明授权

US3687940A Process for the production of 3-amino-azacycloheptan-2-one 失效
标题翻译：制备3-氨基亚氨基二酚-2-酮的方法
公开(公告)号：US3687940A
公开(公告)日：1972-08-29
申请号：US3687940D
申请日：1970-06-24
申请人： CIBA GEIGY CORP
发明人： FOITL VERENA R , TRABER WALTER
IPC分类号： C07D223/12 , C07D41/06
CPC分类号： C07D223/12
摘要： A process is given for the production of 3-amino-azacycloheptan2-one which comprises reducing 1-formyl-3-nitroazacycloheptan-2on with hydrogen under pressure in the presence of ammonia. It is thus possible to obtain 3-amino-azacycloheptan-2-one ( Alpha amino- Epsilon -caprolactam) by a technically simple process.
摘要翻译：给出了制备3-氨基 - 氮杂环庚烷-2-酮的方法，其包括在氢气存在下，在压力下用氢气还原1-甲酰基-3-硝基氮杂环庚烷-2-酮。因此，可以通过技术上简单的方法获得3-氨基 - 氮杂环庚烷-2-酮（α-氨基 - ε-己内酰胺）。

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