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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

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。

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

US4551459A Method of treating heart failure using (2-oxo-1,2,3,5-tetrahydroimidazo-[2,1-b]quinazolinyl)oxyalkylamides 失效
标题翻译：（2-氧代-1,2,3,5-四氢咪唑并[2,1-b]喹唑啉基）氧烷基酰胺治疗心力衰竭的方法
公开(公告)号：US4551459A
公开(公告)日：1985-11-05
申请号：US599858
申请日：1984-04-13
申请人： Gordon H. Jones , Michael C. Venuti , Robert Alvarez , John J. Bruno
发明人： Gordon H. Jones , Michael C. Venuti , Robert Alvarez , John J. Bruno
IPC分类号： C07C205/37 , C07C205/44 , C07C205/56 , C07D209/08 , C07D215/08 , C07D217/06 , C07D295/185 , C07D487/04 , A61K31/505
CPC分类号： C07D295/185 , C07C205/37 , C07C205/44 , C07C205/56 , C07D209/08 , C07D215/08 , C07D217/06 , C07D487/04
摘要： Compounds according to the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbon;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 combined are oxo;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl and its acylates, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl or amino acid side chains;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;A is an amide forming group wherein the nitrogen substituents are: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms; cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR.sub.5, halo, --NH.sub.2, --N(R.sub.5).sub.2, --NHCOR.sub.5, --COOH, or --COO(R.sub.5) group wherein R.sub.5 is lower alkyl; phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with 1 or more lower alkyl, halo or lower alkoxy groups or an --NH.sub.2, --N(R.sub.5).sub.2, --NHCOR.sub.5, --COOH, or --COOR.sub.5 group wherein R.sub.5 is lower alkyl; morpholinyl; piperidinyl; perhexylenyl; N-loweralkylpiperazinyl; pyrrolidinyl; tetrahydroquinolinyl; tetrahydroisoquinolinyl; (.+-.)-decahydroquinolinyl or indolinyl. These compounds have inotropic activity.
摘要翻译：根据式（I）的化合物及其药学上可接受的酸加成盐，其中：n为1至6的整数; R1是氢或1-4个碳的烷基; R 2为氢或R 1和R 2为氧基; R3为氢，1-6个碳原子的烷基，苯基，苄基，羟基低级烷基及其酰化物，氨基甲酰基烷基，羧基烷基，烷氧基羰基烷基或氨基酸侧链; R4是氢，1-6个碳原子的烷基，苄基或羟基低级烷基; Y是氢，1-4个碳原子的烷基，卤代或低级烷氧基; A是酰胺形成基团，其中氮取代基是：氢; 1至6个碳原子的烷基; 1至6个碳原子的羟烷基和1至6个碳原子的脂族酰化物或7至12个碳原子的芳基酰化物; 3至8个碳原子的环烷基或4至12个碳原子的环烷基低级烷基，其中环烷基环未被取代或被低级烷基，低级烷氧基，-OH，-OCOR5，卤素，-NH2，-N（R5）2 ，-NHCOR 5，-COOH或-COO（R 5）基，其中R 5是低级烷基; 苯基或苯基低级烷基，其中苯基未被取代或被1个或多个低级烷基，卤代或低级烷氧基或-NH 2，-N（R 5）2，-NHCOR 5，-COOH或-COOR 5基团取代，其中R 5为低级烷基 ; 吗啉基哌啶基; 全己烯基; N-低级烷基哌嗪基; 吡咯烷基四氢喹啉基; 四氢异喹啉基; （+/-） - 十氢喹啉基或二氢吲哚基。这些化合物具有变力活性。

5. 发明授权

US4490371A N,N-Di substituted-(2-oxo-1,2,3,5-tetrahydroimidazo-[2,1-B]quinazolinyl)oxyalkyl amides 失效
标题翻译： N，N-二取代 - （2-氧代-1,2,3,5-四氢咪唑并[2,1-B]喹唑啉基）氧烷基酰胺
公开(公告)号：US4490371A
公开(公告)日：1984-12-25
申请号：US467125
申请日：1983-02-16
申请人： Gordon H. Jones , Michael C. Venuti , Robert Alvarez , John J. Bruno
发明人： Gordon H. Jones , Michael C. Venuti , Robert Alvarez , John J. Bruno
IPC分类号： A61K31/505 , A61K31/517 , A61K31/519 , A61K31/535 , A61P7/02 , A61P9/04 , A61P35/00 , A61P35/04 , A61P43/00 , C07C205/37 , C07C205/44 , C07C205/56 , C07D209/08 , C07D215/08 , C07D217/06 , C07D295/185 , C07D487/04
CPC分类号： C07D295/185 , C07C205/37 , C07C205/44 , C07C205/56 , C07D209/08 , C07D215/08 , C07D217/06 , C07D487/04 , Y10S514/822
摘要： Compounds according to the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl or hydroxy lower alkyl;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;A is an amide forming group wherein the nitrogen substituents are: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms; cycloalkyl of 3 to 7 carbon atoms or cycloalkyl lower alkyl of 4 to 11 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, OH, --OCOR.sub.5, halo, --NH.sub.2, --N(R.sub.5).sub.2, --NHCOR.sub.5, --COOH, or --COO(R.sub.5) group wherein R.sub.5 is lower alkyl; phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with 1 or more lower alkyl, halo or lower alkoxy groups or an NH.sub.2, --N(R.sub.5).sub.2, --NHCOR.sub.5, --COOH, or --COOR.sub.5 group wherein R.sub.5 is lower alkyl; morpholinyl; piperidinyl; perhexylenyl; N-loweralkylpiperazinyl; tetrahydroquinolinyl; tetrahydroisoquinolinyl; (.+-.)-decahydroquinolinyl or indolinyl. These compounds are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic agents and the like in mammals.
摘要翻译：根据式（I）的化合物及其药学上可接受的酸加成盐，其中：n为1至6的整数; R1是氢或1至4个碳的烷基; R2是氢或R1和R2组合形成氧代基团; R3是氢，1-6个碳的烷基，苯基，苄基或羟基低级烷基; R4是氢，1-6个碳原子的烷基，苄基或羟基低级烷基; Y是氢，1-4个碳原子的烷基，卤代或低级烷氧基; A是酰胺形成基团，其中氮取代基是：氢; 1至6个碳原子的烷基; 1至6个碳原子的羟烷基和1至6个碳原子的脂族酰化物或7至12个碳原子的芳基酰化物; 3至7个碳原子的环烷基或4至11个碳原子的环烷基低级烷基，其中环烷基环未被取代或被低级烷基，低级烷氧基，OH，-OCOR 5，卤素，-NH 2，-N（R 5） -NHCOR 5，-COOH或-COO（R 5）基，其中R 5是低级烷基; 苯基或苯基低级烷基，其中苯基未被取代或被1个或多个低级烷基，卤代或低级烷氧基或NH 2，-N（R 5）2，-NHCOR 5，-COOH或-COOR 5基团取代，其中R 5为低级烷基; 吗啉基哌啶基; 全己烯基; N-低级烷基哌嗪基; 四氢喹啉基; 四氢异喹啉基; （+/-） - 十氢喹啉基或二氢吲哚基。这些化合物是哺乳动物中用作抗血栓形成剂等的环AMP磷酸二酯酶抑制剂。

6. 发明授权

US4663320A (2-oxo-1,2,3,5-tetrahydroimidazo[2,1-b]quinoazolinyl)oxyalkylamides, compositions and the use thereof 失效
公开(公告)号：US4663320A
公开(公告)日：1987-05-05
申请号：US744100
申请日：1985-06-11
申请人： Gordon H. Jones , Michael C. Venuti , Robert Alvarez , John J. Bruno , Jurg R. Pfister
发明人： Gordon H. Jones , Michael C. Venuti , Robert Alvarez , John J. Bruno , Jurg R. Pfister
IPC分类号： C07C205/37 , C07C205/44 , C07C205/56 , C07D209/08 , C07D215/08 , C07D217/06 , C07D295/185 , C07D487/04 , A61K31/55 , A61K31/505 , C07D213/08 , C07D213/14
CPC分类号： C07D295/185 , C07C205/37 , C07C205/44 , C07C205/56 , C07D209/08 , C07D215/08 , C07D217/06 , C07D487/04
摘要： Compounds according to the formula ##STR1## an optical isomer thereof, or a pharmaceutically acceptable acid addition salt thereof wherein:n is an integer of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl or an aliphatic acylate thereof of 1 to 6 carbon atoms or an aryl acylate thereof of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl of an .alpha.-amino acid side chain;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;A is NR.sub.5 R.sub.6 wherein R.sub.5 and R.sub.6 are independently selected from the group consisting of: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms or an aliphatic acylate thereof of 1 to 6 carbon atoms or an aryl acrylate thereof of 7 to 12 carbon atoms; cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR.sub.7, halo, --NH.sub.2, --N(R.sub.7).sub.2, --NHCOR.sub.7, --COOH, or --COO(R.sub.7) group wherein R.sub.5 is lower alkyl; and phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with at least one lower alkyl, halo or lower alkoxy group or an --NH.sub.2, --N(R.sub.7).sub.2, --NHCOR.sub.7, --COOH, or --COOR.sub.7 group wherein R.sub.7 is lower alkyl; or wherein R.sub.5 and R.sub.6 are combined to form a compound selected from the group consisting of: morpholinyl; piperidinyl; perhexylenyl; N-loweralkylpiperazinyl; pyrrolidinyl; tetrahydroquinolinyl; tetrahydroisoquinolinyl; (.+-.)-decahydroquinolinyl and indolinyl. These compounds are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic agents and the like in mammals. The compounds also have inotropic and anti-metastatic activities.

7. 发明授权

US4466981A Naphthalene anti-psoriatic agents 失效
标题翻译：萘抗牛皮癣药
公开(公告)号：US4466981A
公开(公告)日：1984-08-21
申请号：US437063
申请日：1982-10-27
申请人： Gordon H. Jones , Michael C. Venuti , Young, John M.
发明人： Gordon H. Jones , Michael C. Venuti , Young, John M.
IPC分类号： C07C69/035 , A61K31/10 , A61K31/22 , A61K31/275 , A61P17/00 , A61P33/00 , C07C45/63 , C07C46/00 , C07C46/02 , C07C50/24 , C07C50/32 , C07C67/00 , C07C67/08 , C07C69/16 , C07C69/28 , C07C205/48 , C07C213/00 , C07C219/34 , C07C253/00 , C07C255/41 , C07C255/53 , C07C255/55 , C07C313/00 , C07C317/00 , C07C317/22 , C07C319/14 , C07C319/24 , C07C321/30 , C07C323/21 , C07C323/22 , C07C323/41 , C07C323/62 , C07D213/30 , C07D213/70 , C07D213/71 , C07D213/89 , C07D233/84 , A61K31/415 , A61K31/44 , A61K31/505 , C07C121/75 , C07D213/55
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 lower alkoxy or lower alkylthio;R.sup.3 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, 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 n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms.
摘要翻译：哺乳动物的牛皮癣通过局部施用下式的萘来缓解：其中：R1和R2是低级烷氧基或低级烷硫基; R 3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; 且n为0,1或2; W是1至7个碳原子的烷基。

8. 发明授权

US5134161A Method for treating disease states in mammals with naphthalene lipoxygenase-inhibiting agents 失效
标题翻译：用萘脂氧合酶抑制剂治疗哺乳动物疾病状态的方法
公开(公告)号：US5134161A
公开(公告)日：1992-07-28
申请号：US181869
申请日：1988-04-15
申请人： Michael C. Venuti , John M. Young
发明人： Michael C. Venuti , John M. Young
IPC分类号： C07C46/00 , C07C50/10 , C07C50/24 , C07C50/32
CPC分类号： C07C46/00 , C07C50/10 , C07C50/24 , C07C50/32 , Y10S514/886 , Y10S514/887
摘要： Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy,R.sup.2 is the same as R.sup.1, or R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl,R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;both X groups are the same and X is either --C(O)OR.sup.4 or --C(O)NR.sup.5 R.sup.6, whereinR.sup.4 is alkyl, phenyl or benzyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl, cycloalkyl or phenyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo.The compounds of this invention are also useful for the treatment of disease-states caused by lipoxygenase activity in mammals, particularly 5-lipoxygenase activity, when administered systemically.
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：R 1是低级烷氧基或任选取代的苯氧基，R 2与R 1相同，或R 2是氢，低级烷基，任选取代的苯基或任选地取代的苯基烷基，R 3是氢，低级烷基，低级烷氧基，卤素，任选取代的苯基，任选取代的苯基 - 低级烷基或任选取代的苯基 - 低级烷氧基，m是1或2; 两个X基团相同，X是-C（O）OR 4或-C（O）NR 5 R 6，其中R 4是烷基，任选被一个或两个低级烷基，低级烷氧基或卤素取代的苯基或苄基; 且R 5和R 6独立地为氢，低级烷基，环烷基或任选被一个或两个低级烷基，低级烷氧基或卤素取代的苯基。当系统给药时，本发明的化合物也可用于治疗由哺乳动物的脂氧合酶活性引起的疾病状态，特别是5-脂氧合酶活性。

9. 发明授权

US4946845A Naphthalene anti-psoriatic agents 失效
标题翻译：萘抗牛皮癣药
公开(公告)号：US4946845A
公开(公告)日：1990-08-07
申请号：US248525
申请日：1988-11-25
申请人： D. V. Krishna Murthy , Michael C. Venuti , John M. Young
发明人： D. V. Krishna Murthy , Michael C. Venuti , John M. Young
IPC分类号： C12N9/99 , A61K20060101 , A61K31/215 , A61K31/22 , A61K31/235 , A61K31/265 , A61K31/33 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4418 , A61P17/00 , A61P29/00 , A61P43/00 , C07C20060101 , C07C50/32 , C07C69/013 , C07C69/16 , C07C69/28 , C07C69/635 , C07D209/30 , C07D213/70 , C07D213/71 , C07D215/36 , C07D233/84 , C07D239/38 , C07D521/00
CPC分类号： A61K31/22 , C07C50/32 , C07C69/017 , C07C69/16 , C07C69/28 , C07C69/63 , C07C69/635
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 or optionally substituted phenoxy,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;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.4 whereinW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl; andR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl.
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，为低级烷氧基或任选取代的苯氧基，R3为低级烷基，低级烷氧基或卤素，m为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; X或Y中的至少一个为C（O）W，另一个X或Y为不同的且为氢，C（O）W或R 4，其中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 ; 并且R 4是低级烷基或任选取代的苯基 - 低级 - 烷基。

10. 发明授权

US5155132A Naphthalene lipoxygenase-inhibiting agents 失效
标题翻译：萘类脂氧合酶抑制剂
公开(公告)号：US5155132A
公开(公告)日：1992-10-13
申请号：US170490
申请日：1988-03-21
申请人： Michael C. Venuti , John M. Young
发明人： Michael C. Venuti , John M. Young
IPC分类号： C07C46/00 , C07C50/10 , C07C50/24 , C07C50/32
CPC分类号： C07C50/32 , C07C46/00 , C07C50/10 , C07C50/24
摘要： Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X and Y are different and are either R.sup.4 or --C(O)W whereinR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl;W is --OR.sup.5 or --NR.sup.6 R.sup.7,whereinR.sup.5 is alkyl, optionally substituted phenyl or optionally substituted benzyl; and R.sup.6 and R.sup.7 are independently hydrogen, lower alkyl, cycloalkyl or optionally substituted phenyl.The compounds of this invention are also useful for the treatment of disease-states caused by lipoxygenase activity in mammals, particularly 5-lipoxygenase activity, when administered systemically.
摘要翻译：哺乳动物的银屑病通过局部施用下式的萘来缓解：其中：R1是低级烷氧基或任意取代的苯氧基; 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; R 3是氢，低级烷基，低级烷氧基，卤素，任选取代的苯基，任选取代的苯基 - 低级烷基或任选取代的苯基 - 低级烷氧基，m是1或2; X和Y不同，为R 4或-C（O）W，其中R 4为低级烷基或任选取代的苯基 - 低级 - 烷基; W是-OR 5或-NR 6 R 7，其中R 5是烷基，任选取代的苯基或任选取代的苄基; 且R 6和R 7独立地为氢，低级烷基，环烷基或任选取代的苯基。当系统给药时，本发明的化合物也可用于治疗由哺乳动物的脂氧合酶活性引起的疾病状态，特别是5-脂氧合酶活性。

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