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1. 发明授权

US4840965A Naphthalene anti-psoriatic agents 失效
标题翻译：萘抗牛皮癣药
公开(公告)号：US4840965A
公开(公告)日：1989-06-20
申请号：US70456
申请日：1987-07-07
申请人： Gordon H. Jones , Michael C. Venuti , John M. Young
发明人： Gordon H. Jones , Michael C. Venuti , John M. Young
IPC分类号： C07D317/70 , C07D319/22 , C07D321/10
CPC分类号： C07D319/22 , C07D317/70 , C07D321/10
摘要： Naphthalenes of the formula: ##STR1## wherein: m is 1 or 2;n is 1, 2, or 3;R.sup.1 is alkyl of one to seven carbon atoms or an optionally substituted phenyl;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl, optionally substituted phenyl-lower-alkoxy, amino, lower alkylamino, lower dialkylamino, halo, cyano, hydroxy, or lower alkylthio are useful in relieving psoriasis.
摘要翻译：下式的萘：其中：m为1或2; n为1,2或3; R 1是1至7个碳原子的烷基或任选取代的苯基; R 2是氢，低级烷基，低级烷氧基，任选取代的苯基，任选取代的苯基 - 低级烷基，任选取代的苯基 - 低级烷氧基，氨基，低级烷基氨基，低级二烷基氨基，卤素，氰基，羟基或低级烷硫基可用于缓解牛皮癣

2. 发明授权

US4442127A Naphthoquinone anti-psoriatic agents 失效
标题翻译：萘醌类抗牛皮癣药
公开(公告)号：US4442127A
公开(公告)日：1984-04-10
申请号：US459165
申请日：1983-01-19
申请人： Gordon H. Jones , John M. Young
发明人： Gordon H. Jones , John M. Young
IPC分类号： C07C17/14 , C07C45/54 , C07C46/00 , C07C50/32 , A61K31/12 , A61K31/275 , C07C50/00 , C07C97/18
CPC分类号： C07C50/32 , C07C17/14 , C07C45/54 , C07C46/00 , Y10S514/863
摘要： Psoriasis in mammals is relieved by topically administering naphthoquinones of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are lower alkoxy; andR.sup.3 is halo or cyano.
摘要翻译：哺乳动物中的银屑病通过局部施用下式的萘醌缓解：其中：R1和R2是低级烷氧基; 并且R 3是卤素或氰基。

3. 发明授权

US5091558A Naphthalene anti-psoriatic agents 失效
标题翻译：萘抗牛皮癣药
公开(公告)号：US5091558A
公开(公告)日：1992-02-25
申请号：US23089
申请日：1987-03-06
申请人： Gordon H. Jones , Michael C. Venuti , John M. Young
发明人： Gordon H. Jones , Michael C. Venuti , John M. Young
IPC分类号： C07C46/00 , C07C50/10 , C07C50/14 , C07C50/24 , C07C50/32 , C07C69/00 , C07D213/64 , C07D213/89 , C07D239/38 , C07D333/64
CPC分类号： C07D213/89 , C07C255/00 , C07C317/00 , C07C323/00 , C07C46/00 , C07C50/10 , C07C50/14 , C07C50/24 , C07C50/32 , C07D213/64 , C07D239/38 , C07D333/64
摘要： Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is alkoxy, alkylthio, optionally substituted phenoxy or optionally substituted phenylthio;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2, or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(0).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl.
摘要翻译：哺乳动物中的牛皮癣通过局部施用下式的萘来减轻：其中：R1是烷氧基，烷硫基，任选取代的苯氧基或任选取代的苯硫基; R 2是氢，低级烷基，任选取代的苯基或任选取代的苯基烷基; R3是低级烷基，低级烷氧基或卤素，m是0,1或2，或R3是任选取代的苯基，任选取代的苯基低级烷基，任选取代的苯基低级烷氧基，氨基，低级烷基氨基，低级二烷基氨基，氰基或S （O）n R其中R是低级烷基; 任选取代的苯基; 任选取代的苯基低级烷基; 或含有一个或两个选自氮，氧和硫的杂原子的三至九个环原子的任选取代的杂环芳基及其药学上可接受的酸加成盐; m为1，n为0,1或2; 且W为1至7个碳原子的烷基，任选取代的苯基或任选取代的苄基。

4. 发明授权

US4593120A Naphthalene anti-psoriatic agents 失效
标题翻译：萘抗牛皮癣药
公开(公告)号：US4593120A
公开(公告)日：1986-06-03
申请号：US564155
申请日：1983-12-22
申请人： Gordon H. Jones , Michael C. Venuti , John M. Young
发明人： Gordon H. Jones , Michael C. Venuti , John M. Young
IPC分类号： A61K31/215 , A61K31/22 , A61K31/235 , A61K31/265 , A61K31/275 , A61P17/00 , A61P29/00 , C07C45/63 , C07C46/00 , C07C46/02 , C07C50/24 , C07C50/32 , C07C67/00 , C07C69/017 , C07C69/76 , C07C69/78 , C07C205/48 , C07C213/00 , C07C219/34 , C07C253/00 , C07C255/55 , C07C313/00 , C07C317/22 , C07C323/20 , C07C323/38 , C07D213/70 , C07D213/71 , C07D213/89 , C07D521/00
CPC分类号： C07D213/70 , C07C205/48 , C07C255/00 , C07C317/00 , C07C323/00 , C07C45/63 , C07C46/00 , C07C46/02 , C07C50/24 , C07C50/32 , C07D213/89
摘要： Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy, lower alkylthio, optionally substituted phenoxy or optionally substituted phenylthio,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl.
摘要翻译：哺乳动物的银屑病通过局部施用下式的萘来减轻：其中：R1和R2相同，为低级烷氧基，低级烷硫基，任选取代的苯氧基或任选取代的苯硫基，R 3为低级烷基，低级烷氧基或卤素，m为0,1或2或R3为任选取代的苯基，任选取代的苯基低级烷基，任选取代的苯基低级烷氧基，氨基，低级烷基氨基，低级二烷基氨基，氰基或S（O）n R其中R为低级烷基任选取代的苯基; 任选取代的苯基低级烷基; 或含有一个或两个选自氮，氧和硫的杂原子的三至九个环原子的任选取代的杂环芳基及其药学上可接受的酸加成盐; m为1，n为0,1或2; 且W为1至7个碳原子的烷基，任选取代的苯基或任选取代的苄基。

5. 发明授权

US06387395B1 N-[1, (1-1) -dialkyloxy] - and N- [1, (1-1) -dialkenyloxy]- alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor 失效
标题翻译： N- [1，（1-1） - 二烷氧基] - 和N- [1,1-（1,1-） - 二烯氧基] - 烷-1-基-N，N，N-四取代的铵脂质及其用途
公开(公告)号：US06387395B1
公开(公告)日：2002-05-14
申请号：US08348635
申请日：1994-12-02
申请人： Deborah A. Eppstein , Philip L. Felgner , Thomas R. Gadek , Gordon H. Jones , Richard B. Roman
发明人： Deborah A. Eppstein , Philip L. Felgner , Thomas R. Gadek , Gordon H. Jones , Richard B. Roman
IPC分类号： A61K9127
CPC分类号： C07D453/02 , A61K9/0014 , A61K9/0019 , A61K9/1272 , A61K47/186 , C12N15/88 , Y10S435/829
摘要： This invention relates to compounds of the formula or an optical isomer thereof wherein R1 and R2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R3, R4 and R5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R3, R4, and R5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
摘要翻译：本发明涉及式的化合物或其光学异构体，其中R 1和R 2相同或不同，为6至24个碳原子的烷基或烯基; R3，R4和R5相同或不同，为碳原子数为1〜8的烷基，芳基，碳原子数为7〜11的芳烷基，或者当R3，R4，R5中的2个或3个相同时，可以形成奎宁二基，哌啶子基，吡咯烷子基或吗啉代; n为1至8; X是药学上可接受的阴离子。

6. 发明授权

US4946787A N-(.omega.,(.omega.-1)-dialkyloxy)- and N-(.omega.,(.omega.-1)-dialkenyloxy)-alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor 失效
标题翻译： N-（ω，（ω-1） - 二烷氧基） - 和N-（ω，（ω-1） - 二烯氧基） - 烷基-1-基-N，N，N-四取代的铵脂质及其用途
公开(公告)号：US4946787A
公开(公告)日：1990-08-07
申请号：US428815
申请日：1989-10-27
申请人： Deborah A. Eppstein , Philip L. Felgner , Thomas R. Gadek , Gordon H. Jones , Richard B. Roman
发明人： Deborah A. Eppstein , Philip L. Felgner , Thomas R. Gadek , Gordon H. Jones , Richard B. Roman
IPC分类号： A61K9/127 , A61K47/18 , C07D453/02 , C12N15/88
CPC分类号： C12N15/88 , A61K47/186 , A61K9/0014 , A61K9/0019 , A61K9/1272 , C07D453/02
摘要： This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
摘要翻译：本发明涉及式I的化合物或其旋光异构体，其中R 1和R 2相同或不同，为6至24个碳原子的烷基或烯基; R 3，R 4和R 5相同或不同，为碳原子数为1〜8的烷基，芳基，碳原子数为7〜11的芳烷基，或者当R3，R4，R5中的2个或3个为一起形成亚硝酰基，哌啶子基，吡咯烷子基或吗啉代; n为1至8; X是药学上可接受的阴离子。

7. 发明授权

US4234571A Nonapeptide and decapeptide derivatives of luteinizing hormone releasing hormone 失效
标题翻译：促黄体激素释放激素的非肽和十肽衍生物
公开(公告)号：US4234571A
公开(公告)日：1980-11-18
申请号：US47661
申请日：1979-06-11
申请人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
发明人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
IPC分类号： A61K38/04 , A61K38/00 , A61K38/08 , A61K38/22 , A61P5/00 , C07K1/04 , C07K1/06 , C07K7/06 , C07K7/23 , C07K14/00 , C07K14/575 , A61K37/00 , C07C103/52
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/12 , Y10S930/13
摘要： Nonapeptide and decapeptide analogs of LH-RH of the formula(pyro)Glu-His-V-Ser-W-X-Y-Arg-Pro-Z (I)and the pharmaceutically acceptable salts thereof wherein:V is tryptophyl, phenylalanyl or 3-(1-naphthyl)-L-alanyl;W is tyrosyl, phenylalanyl or 3-(1-pentafluorophenyl)-L-alanyl;X is a D-amino acid residue ##STR1## wherein R is (a) a carbocyclic aryl-containing radical selected from the group consisting of naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl, benzhydryl and phenyl substituted with three or more straight chain lower alkyl groups; or(b) a saturated carbocyclic radical selected from the group consisting of cyclohexyl substituted with three or more straight chain lower alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl and adamantyl;Y is leucyl, isoleucyl, nor-leucyl or N-methyl-leucyl;Z is glycinamide or --NH--R.sup.1, whereinR.sup.1 is lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR2## wherein R.sup.2 is hydrogen or lower alkyl,are disclosed. These compounds exhibit potent LH-RH agonist properties.
摘要翻译：式（pyro）Glu-His-V-Ser-WXY-Arg-Pro-Z（I）的LH-RH的非肽和十肽类似物及其药学上可接受的盐，其中：V是色氨酸，苯丙氨酰或3-（1 - 萘基）-L-丙氨酰; W是酪氨酰基，苯丙氨酰基或3-（1-五氟苯基）-L-丙氨酰; X是D-氨基酸残基，其中R是（a）选自萘基，蒽基，芴基，菲基，联苯基，二苯甲基和被三个或更多个直链低级取代的苯基的含碳环芳基的基团烷基; 或（b）选自由三个或更多个直链低级烷基取代的环己基，全氢萘基，全氢联苯基，全氢-2,2-二苯基甲基和金刚烷基的饱和碳环基团; Y是亮氨酰基，异亮氨酰基，正亮氨酰基或N-甲基 - 亮氨酰基; Z是甘氨酰胺或-NH-R 1，其中R 1是低级烷基，环烷基，氟低级烷基或其中R 2是氢或低级烷基。这些化合物显示出有效的LH-RH激动剂性质。

8. 发明授权

US4082736A Novel immunological adjuvant compounds and methods of preparation thereof 失效
标题翻译：新型免疫调节剂及其制备方法
公开(公告)号：US4082736A
公开(公告)日：1978-04-04
申请号：US680618
申请日：1976-04-26
申请人： Gordon H. Jones , John G. Moffatt , John J. Nestor, Jr.
发明人： Gordon H. Jones , John G. Moffatt , John J. Nestor, Jr.
IPC分类号： C07K9/00 , C07C103/52 , A61K37/00
CPC分类号： C07K9/005
摘要： This application relates to novel immunological adjuvant compounds of the formula: ##STR1## wherein each of R and R.sup.1 are the same or different and are hydrogen or an acyl radical; R.sup.2 is an unsubstituted or substituted alkyl radical, or an unsubstituted or substituted aryl radical; R.sup.6 is an alkyl radical X is an aminoacyl moiety; and Y is D-isoasparagine or D-isoglutamine.

9. 发明授权

US4318905A Nonapeptide and decapeptide agonists of luteinizing hormone releasing hormone containing heterocyclic amino acid residues 失效
标题翻译：含有杂环氨基酸残基的促黄体激素释放激素的非肽和十肽激动剂
公开(公告)号：US4318905A
公开(公告)日：1982-03-09
申请号：US162455
申请日：1980-06-23
申请人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
发明人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
IPC分类号： C07D235/16 , C07D277/64 , C07K7/23 , A61K37/00 , C07C103/52
CPC分类号： C07D277/64 , C07D235/16 , C07K7/23 , Y10S514/80 , Y10S930/13
摘要： Nonapeptide and decapeptide analogs of LH-RH of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein: V is tryptophyl, phenylalanyl or 3-(1-naphthyl)-L-alanyl;W is tyrosyl, phenylalanyl or 3-(1-pentafluorophenyl)-L-alanyl;X is a D-amino acid residue of the formula: ##STR2## wherein R is a heterocyclic aryl containing radical selected from the group consisting of radicals represented by the following structural formulas: ##STR3## wherein A and A' are independently selected from the group consisting of hydrogen, lower alkyl, chlorine, and bromine, and G is selected from the group consisting of oxygen, nitrogen, and sulfur;Y is leucyl, isoleucyl, nor-leucyl or N-methyl-leucyl;Z is glycinamide or --NH--R.sup.1, wherein:R.sup.1 is lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR4## wherein R.sup.2 is hydrogen or lower alkyl,are disclosed. These compounds exhibit potent LH-RH agonist properties.
摘要翻译：式（I）的LH-RH的非肽和十肽类似物及其药学上可接受的盐，其中：V是色氨酸，苯丙氨酰基或3-（1-萘基）-L-丙氨酰; W是酪氨酰基，苯丙氨酰基或3-（1-五氟苯基）-L-丙氨酰; X是下式的D-氨基酸残基：其中R是含有基团的杂环芳基，其选自由以下结构式表示的基团：其中A 和A'独立地选自氢，低级烷基，氯和溴，并且G选自氧，氮和硫; Y是亮氨酰基，异亮氨酰基，正亮氨酰基或N-甲基 - 亮氨酰基; Z是甘氨酰胺或-NH-R 1，其中：R 1是低级烷基，环烷基，氟低级烷基或其中R 2是氢或低级烷基。这些化合物显示出有效的LH-RH激动剂性质。

10. 发明授权

US4082735A Novel immunological adjuvant compounds and methods of preparation thereof 失效
公开(公告)号：US4082735A
公开(公告)日：1978-04-04
申请号：US680260
申请日：1976-04-26
申请人： Gordon H. Jones , John G. Moffatt , John J. Nestor, Jr.
发明人： Gordon H. Jones , John G. Moffatt , John J. Nestor, Jr.
IPC分类号： A61K38/00 , A61K31/70 , A61K31/7028 , A61K39/39 , A61P31/04 , A61P37/04 , C07H15/04 , C07K1/06 , C07K9/00 , C07C103/52 , A61K37/00
CPC分类号： C07K9/005
摘要： This application relates to novel immunological adjuvant compounds of the formula: ##STR1## wherein each of R and R.sup.1 are the same or different and are hydrogen or an acyl radical; R.sup.2 is an unsubstituted or substituted alkyl radical, or an unsubstituted or substituted aryl radical; X is an aminoacyl moiety; and Y is D-isoasparagine or D-isoglutamine.

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