公开(公告)号：US4792556A

公开(公告)日：1988-12-20

申请号：US856929

申请日：1986-04-28

申请人： D. V. K. Murthy ,  Michael C. Venuti ,  John M. Young

发明人： D. V. K. Murthy ,  Michael C. Venuti ,  John M. Young

IPC分类号： A61K31/22 ,  C07C50/32 ,  C07C67/08 ,  C07C67/297 ,  C07C69/157 ,  C07C69/16 ,  C07C69/63 ,  C07C69/635 ,  C07C205/45 ,  A61K31/275 ,  A61K31/415 ,  A61K31/44

CPC分类号： A61K31/22 ,  C07C50/32 ,  C07C67/08 ,  C07C67/11 ,  C07C67/29 ,  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.4whereinW 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.

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。

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。

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

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。

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。

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。

公开(公告)号：US4761416A

公开(公告)日：1988-08-02

申请号：US889641

申请日：1986-07-25

申请人： John H. Fried ,  Michael C. Venuti

发明人： John H. Fried ,  Michael C. Venuti

IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P7/02 ,  A61P9/04 ,  A61P43/00 ,  C07D239/84

CPC分类号： C07D239/84

摘要： Pharmaceutical compositions comprising, or compositions consisting essentially of, compounds according to the formula ##STR1## or an optical isomer thereof are disclosed, wherein the substituents A, Z and R.sup.1 are defined herein. The invention is also directed to certain compounds of the above class. The compounds of Formula I are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents and the like in mammals.

摘要翻译： 公开了包含或基本上由式（I）化合物或其旋光异构体组成的药物组合物，其中取代基A，Z和R 1在本文中定义。 本发明还涉及上述类型的某些化合物。 式I的化合物是用作哺乳动物中的抗血栓形成和变力剂等的环AMP磷酸二酯酶抑制剂。

公开(公告)号：US4970297A

公开(公告)日：1990-11-13

申请号：US25426

申请日：1987-03-13

申请人： Arlindo L. Castelhano ,  Diana H. Pliura ,  Michael C. Venuti

发明人： Arlindo L. Castelhano ,  Diana H. Pliura ,  Michael C. Venuti

IPC分类号： A61K38/00 ,  C07D261/04 ,  C07K5/06

CPC分类号： C07D261/04 ,  C07K5/06191 ,  A61K38/00 ,  Y02P20/55

摘要： This invention is directed to compounds of the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:n is 0, 1 or 2;p and q are independently 0, 1 or 2 and the sum of (p+q) is less than or equal to 3;X is selected from the group consisting of: halo; --OR.sup.2, --SR.sup.2, --S(O)R.sup.2, --S(O).sub.2 R.sup.2, and --S(O).sub.2 NHR.sup.2, wherein R.sup.2 is lower alkyl, mono-, di- or tri-fluoro alkyl of 2 or 3 carbon atoms, optionally substituted aryl;R is H or an N-protecting group;R.sup.1 is alkylthio, arylthio, amino, alkylamino, optionally substituted arylamino, or optionally substituted aralkylamino; and when the sum of n+p+q is greater than or equal to one, R.sup.1 is also hydroxy, alkoxy, or aralkoxy; andeach (aa) is independently an .alpha.-amino acid residue with an optionally protected amino acid side chain.

摘要翻译： 本发明涉及下式的化合物：其中n为0,1或2;其中：n为0,1或2; p和q独立地为0,1或2，（p + q）的和小于或等于3; X选自：卤素; -OR 2，-SR 2，-S（O）R 2，-S（O）2 R 2和-S（O）2 NHR 2，其中R 2是低级烷基，2或3个碳原子的一，二或三氟烷基 ，任选取代的芳基; R为H或N-保护基; R 1是烷硫基，芳硫基，氨基，烷基氨基，任选取代的芳基氨基或任选取代的芳烷基氨基; 并且当n + p + q的总和大于或等于1时，R 1也是羟基，烷氧基或芳烷氧基; 并且每个（aa）独立地是具有任选保护的氨基酸侧链的α-氨基酸残基。

公开(公告)号：US4739056A

公开(公告)日：1988-04-19

申请号：US935659

申请日：1986-11-26

申请人： Michael C. Venuti

发明人： Michael C. Venuti

IPC分类号： C07D239/84 ,  A61K31/495

CPC分类号： C07D239/84

摘要： Compounds are disclosed according to the formula ##STR1## or an optical isomer thereof. The compounds of Formula I are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents and the like in mammals.

摘要翻译： 根据式（I）或其旋光异构体公开化合物。 式I的化合物是用作哺乳动物中的抗血栓形成和变力剂等的环AMP磷酸二酯酶抑制剂。