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1. 发明授权

US06414114B2 Disulfides and thiol compounds 失效
标题翻译：二硫化物和硫醇化合物
公开(公告)号：US06414114B2
公开(公告)日：2002-07-02
申请号：US09256765
申请日：1999-02-24
申请人： Floyd E. Taub , Christopher K. Murray , Randall J. Daughenbaugh , Daniel Lednicer
发明人： Floyd E. Taub , Christopher K. Murray , Randall J. Daughenbaugh , Daniel Lednicer
IPC分类号： C07K500
CPC分类号： C07K5/00 , A23L33/10 , A61K31/00 , A61K31/16 , A61K31/195 , A61K31/215 , A61K31/275 , A61K31/66 , A61K31/675 , A61K38/00 , A61K45/06 , C07C323/41 , Y02A50/411 , Y10S930/26 , A61K2300/00
摘要： The present invention is directed to novel disulfides and thiols that are of up to about eighteen amino acids. One example, is a compound of the formula (1): A—B—C—S—S—D—E—F, wherein: A and F are selected from the group consisting of hydrogen, an amino acid, a dipeptide, a tripeptide, a modified polypeptide up to three amino acids long, and a carbobenzoxy groups, B and E are selected from the group consisting of an amino acid, a dipeptide, a tripeptide, and a modified polypeptide comprising up to and including three amino acids, C and D are selected from the group consisting of a modified polypeptide and a polypeptide comprising up to and including three amino acids, and S is the sulfur atom in the modified polypeptide and the polypeptide in C and D.
摘要翻译：本发明涉及高达约十八个氨基酸的新二硫化物和硫醇。一个实例是式（1）的化合物：ABCSSDEF，其中：A和F选自氢，氨基酸，二肽，三肽，长达三个氨基酸的修饰的多肽，以及苄氧羰基，B和E选自氨基酸，二肽，三肽和包含至多和包括三个氨基酸的修饰的多肽，C和D选自修饰的多肽和包含至多并包括三个氨基酸的多肽，S是修饰多肽中的硫原子，C和D中的多肽。

2. 发明授权

US4212878A Phenylacetamide derivative analgesics 失效
标题翻译：苯乙酰胺衍生物镇痛药
公开(公告)号：US4212878A
公开(公告)日：1980-07-15
申请号：US872632
申请日：1978-01-26
申请人： Daniel Lednicer , Jacob Szmuszkovicz
发明人： Daniel Lednicer , Jacob Szmuszkovicz
IPC分类号： C07D295/135 , C07D317/72 , C07D405/04 , A61K31/40 , C07D207/04
CPC分类号： C07D295/135 , C07D317/72
摘要： N-[(1-Amino-4-(mono or di-oxygen-group-substituted)cyclohex-1-yl)methyl]phenylacetamide derivatives of the formula 1 ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, P, Q, X and Y are defined in the specification, e.g., 2-(3,4-dichlorophenyl)-N-[[8-(1-pyrrolidinyl)-1,4-dioxaspiro[4.5]dec.-8-yl]methyl]acetamide, and their pharmacologically acceptable salts, have analgesic drug properties with lower physical dependence liability characteristics than morphine or methadone, for use as analgesic drugs in mammalian animals including humans.
摘要翻译： N - [（1-氨基-4-（单或二 - 氧基取代的）环己-1-基）甲基]苯基乙酰胺衍生物其中R，R1，R2，R3，P， Q，X和Y在说明书中定义，例如2-（3,4-二氯苯基）-N - [[8-（1-吡咯烷基）-1,4-二氧杂螺[4.5]癸-8-基] 甲基]乙酰胺及其药理学上可接受的盐，具有比吗啡或美沙酮更低的物理依赖性责任特征的止痛药物，用作包括人在内的哺乳动物的止痛药。

3. 发明授权

US3960961A 4'-Fluoro-4-{[4-(phenyl)cyclohexyl]amino}butyrophenones and the salts thereof 失效
标题翻译： 4 {40-氟-4- {55 {8 4-（苯基）环己基{9氨基{56丁基苯及其盐
公开(公告)号：US3960961A
公开(公告)日：1976-06-01
申请号：US329044
申请日：1973-02-02
申请人： Daniel Lednicer
发明人： Daniel Lednicer
IPC分类号： C07C45/29 , C07C45/62 , C07C45/66 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747 , C07D295/073 , C07C97/10
CPC分类号： C07D295/073 , C07C247/00 , C07C45/292 , C07C45/62 , C07C45/66 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747
摘要： This invention relates to novel 4-phenylcyclohexylamines embraced by the formula ##SPC1##Wherein .about. is a generic expression denoting cis and trans stereoconfiguration and mixtures thereof; R is selected from the group consisting of alkyl of from one through four carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, nitro and alkoxy of from one through four carbon atoms; R' and R.sup.1 are selected from the group consisting of hydrogen and alkyl of from one through four carbon atoms; R.sup.2 is selected from the group consisting of hydrogen, alkyl of from one through four carbon atoms, alkanoyl of from one through three carbon atoms, alkylsulfonyl of from one through three carbon atoms, arylsulfonyl of from six through ten carbon atoms, alkylcarbamoyl wherein alkyl is from one through four carbon atoms, alkoxycarbonyl wherein alkyl is from one through four carbon atoms, ring monosubstituted aroylalkyl wherein the substituents have the same meaning as R, above, aryl is from six through ten carbon atoms and alkyl is from one through six carbon atoms and bis (ring monosubstituted) arylalkyl wherein the substituents have the same meaning as R, above, aryl is from six through ten carbon atoms and alkyl is from one through six carbon atoms; R.sup.1 and R.sup.2 when taken together with --N
摘要翻译：本发明涉及以下式所表示的新型4-苯基环己胺：其中差异是一般性表达式，其特征在于其独特的化学反应和其混合物及其混合物; R选自1至4个碳原子的烷基，1至4个碳原子的氟，氯，溴，三氟甲基，硝基和烷氧基; R'和R 1选自氢和一至四个碳原子的烷基; R2选自氢，一至四个碳原子的烷基，一至三个碳原子的烷酰基，一至三个碳原子的烷基磺酰基，六至十个碳原子的芳基磺酰基，其中烷基是一个至四个碳原子，其中烷基是一个至四个碳原子的烷氧基羰基，其中取代基具有与上述R相同的含义的环单取代的芳酰基烷基，芳基是六至十个碳原子，烷基是一至六个碳原子和双（环单取代）芳烷基，其中取代基具有与上述R相同的含义，芳基为6至10个碳原子，烷基为1至6个碳原子; R 1和R 2与-N'一起是选自未取代的和单取代的吡咯烷子基，哌啶子基，六亚甲基亚氨基，吗啉代和哌嗪基的饱和杂环氨基; 及其酸加成盐。它还涉及制备上述新化合物（1）的中间体和方法及其新颖的衍生物。新化合物（1）对人和动物的全身给药抑制其中枢神经系统。

4. 发明授权

US3932425A Benzospiran derivatives 失效
标题翻译： Benzospiran衍生物
公开(公告)号：US3932425A
公开(公告)日：1976-01-13
申请号：US460449
申请日：1974-04-12
申请人： Daniel Lednicer
发明人： Daniel Lednicer
IPC分类号： C07C13/72 , C07C49/675 , C07C49/683 , C07C49/697 , C07C49/747 , C07C49/755 , C07C57/50 , C07C59/54 , C07C59/86 , C07C205/45 , C07D295/02 , C07D295/033 , C07D295/096 , C07D295/135 , C07D317/22 , C07D319/08
CPC分类号： C07D319/08 , C07C205/45 , C07C247/00 , C07C45/44 , C07C49/675 , C07C49/683 , C07C49/697 , C07C49/747 , C07C49/755 , C07C57/50 , C07C59/54 , C07C59/86 , C07D295/033 , C07D295/096 , C07D295/135 , C07D317/22 , C07C2103/94
摘要： This invention relates to novel benzospiran derivatives embraced by the formula ##SPC1##Wherein the sum of A and B is at least the integer 2; A is selected from the group consisting of --(CH.sub.2).sub.n -- wherein n is 1 through 5 and --(C.sub.n H.sub.2n --.sub.2 XY)-- wherein X is selected from the group consisting of hydroxy, acetoxy, amino and acetamido and Y is hydrogen, and X when taken together with Y is selected from the group consisting of =O and =CR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; B is absent or --(CH.sub.2).sub.n -- wherein n is 1 through 3; R.sup.1 is selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; R.sup.2 is selected from the group consisting of hydrogen, lower alkyl of 1 through 3 carbon atoms, ##EQU1## WHEREIN N IS 2 THROUGH 5 AND Ar is phenyl having zero through three substituents selected from the group consisting of lower alkyl of 1 through 3 carbon atoms, lower alkoxy of 1 through 3 carbon atoms, bromine, chlorine and fluorine; R.sup.1 and R.sup.2 taken together with --N
摘要翻译：本发明涉及以下式所示的新型苯并环丙兰衍生物：其中A和B的至少为整数2; A选自 - （CH 2）n - ，其中n为1至5和 - （C n H 2n-2 XY） - 其中X选自羟基，乙酰氧基，氨基和乙酰氨基，Y为氢，以及 X与Y一起选自= O和= CR 3 R 4，其中R 3和R 4选自氢和1至3个碳原子的低级烷基; B不存在或 - （CH 2）n - ，其中n为1至3; R1选自氢和1至3个碳原子的低级烷基; R 2选自氢，1至3个碳原子的低级烷基，O和 - （CH 2）n CAr，其中N为2，并且Ar为具有0至3个选自下列基团的低级烷基的苯基： 1至3个碳原子，1至3个碳原子的低级烷氧基，溴，氯和氟; R 1和R 2与-N'一起是选自未取代的和取代的吡咯烷子基，哌啶子基和六亚甲基亚氨基的饱和杂环氨基; Z选自氢，1至3个碳原子的低级烷基，1至3个碳原子的低级烷氧基，1至3个碳原子的硝基，氨基，一烷基氨基，1至4个碳原子的酰基酰胺基，溴，氯和氟; 及其药理学上可接受的酸加成盐。它还涉及制备上述新化合物（1）的中间体和方法及其新颖的衍生物。新化合物（1）对人和动物的施用抑制其中枢神经系统并降低其血压。

5. 发明授权

US6007819A Methods of inducing immunity using low molecular weight immune stimulants 失效
标题翻译：使用低分子量免疫刺激剂诱导免疫的方法
公开(公告)号：US6007819A
公开(公告)日：1999-12-28
申请号：US733174
申请日：1996-10-17
申请人： Floyd Taub , Thomas J. Perun , Christopher K. Murray , Randall J. Daughenbaugh , Daniel Lednicer
发明人： Floyd Taub , Thomas J. Perun , Christopher K. Murray , Randall J. Daughenbaugh , Daniel Lednicer
IPC分类号： A61K31/66 , A01N37/20 , A01N41/02 , A01N41/04 , A01N57/12 , A01N57/20 , A61K31/00 , A61K31/16 , A61K31/255 , A61K31/661 , A61K31/662 , A61K39/39 , A61P7/00 , A61P7/06 , A61P35/00 , A61P37/00 , A61P37/04 , C07C309/15 , C07C323/41 , C07F9/09 , C07F9/143 , C07F9/38 , C07F9/40 , A61K39/00 , A61K45/00 , A61K31/74 , A01N37/34
CPC分类号： C07F9/091 , A61K39/39 , C07C309/15 , C07C323/41 , C07F9/3808 , A61K2039/55511 , Y10S514/885
摘要： The present invention relates to peptide-like compounds, eg aminocarboxylic acid amide derivatives, and to methods of using same to stimulate cells of the immune system, bone marrow and other organs. The present compounds can be used to enhance vaccination, increase synthesis of and enhance function of blood cell components and enhance anti-neoplastic effects of various agents. The compounds of the invention can be used to produce a variety of further pharmacologic effects.
摘要翻译：本发明涉及肽样化合物，例如氨基羧酸酰胺衍生物，以及其用于刺激免疫系统，骨髓和其他器官的细胞的方法。本发明化合物可用于增强疫苗接种，增加血细胞成分的合成和增强功能，并增强各种药剂的抗肿瘤作用。本发明的化合物可用于产生多种其它药理作用。

6. 发明授权

US4447454A Analgetic compounds, compositions and process of treatment 失效
公开(公告)号：US4447454A
公开(公告)日：1984-05-08
申请号：US263840
申请日：1981-05-15
申请人： Daniel Lednicer
发明人： Daniel Lednicer
IPC分类号： A61K31/135 , C07D295/135 , C07D317/72 , C07C87/34
CPC分类号： C07D295/135 , C07C255/00 , C07D317/72
摘要： Novel compounds of the formula: ##STR1## wherein R.sub.1 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, CH.sub.2 -alkenyl wherein alkenyl is from 2 to 4 carbon atoms, inclusive, cycloalkyl of from 3 to 6 carbon atoms, inclusive, cycloalkylmethyl of from 3 to 6 carbon atoms, inclusive; R.sub.2 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, inclusive, with the proviso that R.sub.1 and R.sub.2 cannot both be hydrogen at the same time; Y is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, halogen, trifluoromethyl, hydroxy, alkanoyloxy from 2 to 5 carbon atoms, inclusive, alkoxy of from 1 to 4 carbon atoms, inclusive, cycloalkyloxy of from 3 to 6 carbon atoms, inclusive, benzyloxy; m is an integer 0, 1, 2; R.sub.5 is a variable consisting of hydrogen and alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.3 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.4 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, CH.sub.2 -alkenyl wherein alkenyl is of from 2 to 4 carbon atoms, inclusive, and arylalkyl wherein alkyl is from 1 to 4 carbon atoms, inclusive, and aryl is ##STR2## wherein Y' is CF.sub.3, halogen, alkyl of 1 to 4 carbon atoms, inclusive, and alkoxy of from 1 to 4 carbon atoms, inclusive; and R.sub.3 and R.sub.4 when taken together with the nitrogen atom to which they are attached can form saturated heterocycles of from 5 to 7 ring members, a second hetero atom of said ring can be oxygen or nitrogen, e.g., morpholine, piperazine, and said heterocycles can be monosubstituted having a total of up to 9 carbon atoms, with the proviso that when ##STR3## is pyrrolidinyl, then m=1, 2, having analgetic activity in humans and animals are prepared in unit dosage forms. The compositions are useful in relieving pain by administering orally, parenterally, and rectally to humans and animals.

7. 发明授权

US4115589A Compounds, compositions and method of use 失效
标题翻译：化合物，组合物和使用方法
公开(公告)号：US4115589A
公开(公告)日：1978-09-19
申请号：US797782
申请日：1977-05-17
申请人： Daniel Lednicer
发明人： Daniel Lednicer
IPC分类号： C07D317/72 , A01N9/20 , C07C91/02
CPC分类号： C07D317/72
摘要： 4-Amino-4-cyclohexan-1-ols are formulated into pharmaceutical compositions for the relief of pain in mammals in need of said treatment.
摘要翻译：将4-氨基-4-环己烷-1-醇配制成用于缓解需要所述治疗的哺乳动物疼痛的药物组合物。

8. 发明授权

US4113866A Analgetic compounds, compositions and process of treatment 失效
标题翻译：化学化合物，组合物和处理方法
公开(公告)号：US4113866A
公开(公告)日：1978-09-12
申请号：US783806
申请日：1977-04-01
申请人： Daniel Lednicer
发明人： Daniel Lednicer
IPC分类号： C07D295/12 , C07D295/135 , C07D317/72 , A61K31/535
CPC分类号： C07D295/135 , C07C255/00 , C07D317/72
摘要： Novel compounds of the formula: ##STR1## wherein R.sub.1 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, CH.sub.2 -alkenyl wherein alkenyl is from 2 to 4 carbon atoms, inclusive, cycloalkyl of from 3 to 6 carbon atoms, inclusive, cycloalkylmethyl of from 3 to 6 carbon atoms, inclusive; R.sub.2 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, inclusive, with the proviso that R.sub.1 and R.sub.2 cannot both be hydrogen at the same time; Y is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, halogen, trifluoromethyl, hydroxy, alkanoyloxy from 2 to 5 carbon atoms, inclusive, alkoxy of from 1 to 4 carbon atoms, inclusive, cycloalkyloxy of from 3 to 6 carbon atoms, inclusive, benzyloxy; m is an integer 0, 1, 2; R.sub.5 is a variable consisting of hydrogen and alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.3 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.4 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, CH.sub.2 -alkenyl wherein alkenyl is of from 2 to 4 carbon atoms, inclusive, and arylalkyl wherein alkyl is from 1 to 4 carbon atoms, inclusive, and aryl is ##STR2## WHEREIN Y' is CF.sub.3, halogen, alkyl of 1 to 4 carbon atoms, inclusive, and alkoxy of from 1 to 4 carbon atoms, inclusive; and R.sub.3 and R.sub.4 when taken together with the nitrogen atom to which they are attached can form saturated heterocycles of from 5 to 7 ring members, a second hetero atom of said ring can be oxygen or nitrogen, e.g., morpholine, piperazine, and said heterocycles can be monosubstituted having a total of up to 9 carbon atoms, with the proviso that when ##STR3## is pyrrolidinyl, then m = 1, 2, having analgetic activity in humans and animals are prepared in unit dosage forms. The compositions are useful in relieving pain by administering orally, parenterally, and rectally to humans and animals.

9. 发明授权

US3975371A Aromatic azo sulfonylnitrene compounds 失效
标题翻译：芳香偶氮磺酰基化合物
公开(公告)号：US3975371A
公开(公告)日：1976-08-17
申请号：US559303
申请日：1975-03-17
申请人： Daniel Lednicer , Edward E. Nishizawa
发明人： Daniel Lednicer , Edward E. Nishizawa
IPC分类号： A61K31/655 , C08F8/30 , C07C107/04 , C07C107/06
CPC分类号： A61K31/655 , C08F8/30
摘要： Compounds of the structure ##SPC1##Wherein R and R.sub.1 are the same or different and are selected from the group consisting of hydrogen, halogen, and alkyl from one to four carbon atoms, inclusive, and R.sub.2 is a substance which inhibits thrombogenic or clotting activity of a material and is that portion of a substituted aromatic which couples with a diazonium salt.
摘要翻译：结构式R和R 1的化合物相同或不同，并且选自氢，卤素和1-4个碳原子的烷基，R2是抑制材料的血栓形成或凝血活性的物质并且是与重氮盐偶联的取代芳族化合物的那部分。

10. 发明授权

US3965180A 4'-Fluoro-4-{[4-(phenyl)-4-alkoxy-cyclo-hexyl]amino}butyrophenones and the salts thereof 失效
标题翻译： 4 {40-氟-4- {55 {8 4-（苯基）-4-烷氧基 - 环己基{9氨基{56丁基苯及其盐
公开(公告)号：US3965180A
公开(公告)日：1976-06-22
申请号：US333896
申请日：1973-02-20
申请人： Daniel Lednicer
发明人： Daniel Lednicer
IPC分类号： C07C35/21 , C07C87/36
CPC分类号： C07C35/21
摘要： This invention relates to novel 4-(substituted alkoxy)-4-(substituted phenyl)cyclohexylamines embraced by the formula ##SPC1##Wherein .about. is a generic expression denoting cis and trans stereoconfiguration and mixtures thereof, with the proviso that when the stereoconfiguration of the linkage connecting the cyclohexane ring and R.sup.3 O is is cis to the amino group, the linkage connecting the cyclohexane and phenyl rings is always trans, and vice versa; R is selected from the group consisting of lower alkyl of 1 through 4 carbon atoms, chlorine, fluorine, bromine, trifluoromethyl, and lower alkoxy of 1 through 4 carbon atoms; R' has the same meaning as R and in addition hydrogen; R.sup.1 is selected from the group consisting of hydrogen and lower alkyl of 1 through 4 carbon atoms; R.sup.2 is selected from the group consisting of hydrogen, lower alkyl of 1 through 4 carbon atoms, ring monosubstituted aroylalkyl wherein the substituents have the same meaning as R and R', above, aryl is from 6 through 10 carbon atoms and alkyl of from 1 through 4 carbon atoms and bis (ring monosubstituted)arylalkyl wherein the substituents have the same meaning as R and R', above, aryl is from 6 through 10 carbon atoms and alkyl of from 1 through 4 carbon atoms; R.sup.1 and R.sup.2 taken together with -N
摘要翻译：本发明涉及新颖的4-（取代的烷氧基）-4-（取代的苯基）环己基胺，其由下式表示：其中不同的是一般性表达式，其特征在于其独特的特征和混合物，以及当链接的连续化连接时环己烷环和R 3 O与氨基是顺式的，连接环己烷和苯环的键总是反式的，反之亦然; R选自1至4个碳原子的低级烷基，氯，氟，溴，三氟甲基和1至4个碳原子的低级烷氧基; R'具有与R和氢相同的含义; R1选自氢和1至4个碳原子的低级烷基; R2选自氢，1至4个碳原子的低级烷基，环单取代的芳酰基烷基，其中取代基具有与R和R'相同的含义，上述芳基为6至10个碳原子，烷基为1 通过4个碳原子和双（环单取代）芳烷基，其中取代基具有与上述R和R'相同的含义，芳基为6至10个碳原子和1至4个碳原子的烷基; R 1和R 2与-N'一起是选自未取代的和单取代的吡咯烷子基，哌啶子基，六亚甲基亚氨基，吗啉代和哌嗪基的饱和杂环氨基; R3是1至4个碳原子的低级烷基; 及其酸加成盐。它还涉及制备上述新化合物（1）的中间体和方法及其新颖的衍生物。新化合物（1）对人和动物的全身给药抑制其中枢神经系统。

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