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1. 发明授权

US4921862A Carbostyril derivatives as combined thromboxane synthetase and cyclic-amp phosphodiesterase inhibitors 失效
标题翻译：卡波他特尔衍生物作为联合血栓素合成酶和环磷酸二酯酶抑制剂
公开(公告)号：US4921862A
公开(公告)日：1990-05-01
申请号：US247134
申请日：1988-09-21
申请人： Keith A. M. Walker , John J. Bruno , Gregory R. Martinez
发明人： Keith A. M. Walker , John J. Bruno , Gregory R. Martinez
IPC分类号： C07D401/04 , C07D401/06 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06
摘要： The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein:X is chosen from the group consisting of: ##STR2## and a covalent bond in which R.sup.1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R.sup.2 is H or OH, or R.sup.1 and R.sup.2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene;R.sup.3 is H or alkyl having 1-6 carbon atoms, R.sup.4 is H and R.sup.3 and R.sup.4 are either cis or trans to each other, or R.sup.3 and R.sup.4 taken together represent a covalent bond;n is an integer from 0-3;Het is 1-imidazolyl or 3-pyridyl; and the dotted line represents an optional covalent bond.
摘要翻译：本发明涉及一种抑制具有特征在于血栓素水平升高或前列环素/血栓素水平不平衡的疾病的哺乳动物中的血栓素合成酶和环-AMP磷酸二酯酶的方法，其用下式化合物或其药学上可接受的盐其中：X选自：其中R 1为H，具有1-6个碳原子的烷基，任选取代的苯基或任选取代的苯基低级烷基的共价键，当R 2为H或OH时，或R 1和R 2一起代表氧代，具有1-6个碳原子的亚烷基或任选取代的亚苄基; R3是H或具有1-6个碳原子的烷基，R4是H，R3和R4彼此是顺式或反式，或者R3和R4一起代表共价键; n是0-3的整数; Het是1-咪唑基或3-吡啶基; 而虚线表示任选的共价键。

2. 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.

3. 发明授权

US4593029A Novel .omega.-(N-imidazolyl)alkyl ethers of 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones 失效
标题翻译： 1,2,3,5-四氢咪唑并[2,1-b]喹唑啉-2-酮的新型ω-（N-咪唑基）烷基醚
公开(公告)号：US4593029A
公开(公告)日：1986-06-03
申请号：US580411
申请日：1984-02-15
申请人： Michael C. Venuti , John J. Bruno
发明人： Michael C. Venuti , John J. Bruno
IPC分类号： C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： Novel compound of the formula ##STR1## wherein n is an integer of 1 to 8;R.sub.1 is hydrogen or alkyl of 1-6 carbons;R.sub.2 is hydrogen;R.sub.3 is hydrogen, alkyl of 1-6 carbons, phenyl, benzyl, hydroxy lower alkyl, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl;R.sub.4 is hydrogen, alkyl of 1-6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;any of its optical isomers, the mixture thereof, or the pharmaceutically acceptable acid addition salt.These compounds are inhibitors of thromboxane synthetase and cyclic AMP phosphodiesterase and are therefore potential cardiovascular agents particularly useful as platelet aggregation inhibitors and anti-thrombotic agents. Accordingly, these compounds will preferably be useful in treating cardiovascular disorders with thrombotic complications. However, they also possess vasodilatory, antisecretory, antihypertensive, inotropic and antimetastatic activities.
摘要翻译：式（I）的新化合物，其中n为1至8的整数; R1是氢或1-6个碳的烷基; R2是氢; R3是氢，1-6个碳的烷基，苯基，苄基，羟基低级烷基，氨基甲酰基烷基，羧基烷基，烷氧基羰基烷基; R4是氢，1-6个碳的烷基，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; 其任何光学异构体，其混合物或药学上可接受的酸加成盐。这些化合物是血栓素合成酶和环AMP磷酸二酯酶的抑制剂，因此是特别可用作血小板聚集抑制剂和抗血栓形成剂的潜在心血管药。因此，这些化合物优选可用于治疗具有血栓并发症的心血管疾病。然而，它们也具有血管扩张，抗分泌，抗高血压，变力和抗转移活性。

4. 发明授权

US4766127A 2-(3-pyridylmethyl)naphthalene-6-carboxylic acid as a thromboxane synthetase inhibitor 失效
标题翻译： 2-（3-吡啶基甲基）萘-6-羧酸作为血栓素合成酶抑制剂
公开(公告)号：US4766127A
公开(公告)日：1988-08-23
申请号：US12979
申请日：1987-02-10
申请人： Gregory R. Martinez , John J. Bruno
发明人： Gregory R. Martinez , John J. Bruno
IPC分类号： A61K31/44 , A61K31/435 , C07D213/06
CPC分类号： A61K31/44
摘要： The invention concerns a method of inhibiting thromboxane synthetase with a compound of the formula: ##STR1## or a pharmaceutically acceptable salt or ester thereof, in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclinthromboxane levels.
摘要翻译：本发明涉及一种具有以下结构式的化合物或其药学上可接受的盐或酯在具有以血栓素水平升高或前列环素血栓烷甲烷水平不平衡为特征的哺乳动物中抑制血栓素合成酶的方法。

5. 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。

6. 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。

7. 发明授权

US4792561A Carbostyril derivatives as combined thromboxane synthetase and cyclic-AMP phosphodiesterase inhibitors 失效
标题翻译：卡波他汀衍生物作为联合血栓素合成酶和环AMP磷酸二酯酶抑制剂
公开(公告)号：US4792561A
公开(公告)日：1988-12-20
申请号：US868845
申请日：1986-05-29
申请人： Keith A. M. Walker , John J. Bruno , Gregory R. Martinez
发明人： Keith A. M. Walker , John J. Bruno , Gregory R. Martinez
IPC分类号： C07D401/04 , C07D401/06 , C07D521/00 , A61K31/47 , C07D401/10 , C07D401/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06
摘要： The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein:X is chosen from the group consisting of: ##STR2## and a covalent bond in which R.sup.1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R.sup.2 is H or OH, or R.sup.1 and R.sup.2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene;R.sup.3 is H or alkyl having 1-6 carbon atoms, R.sup.4 is H and R.sup.3 and R.sup.4 are either cis or trans to each other, or R.sup.3 and R.sup.4 taken together represent a covalent bond;n is an integer from 0-3;Het is 1-imidazolyl or 3-pyridyl; and the dotted line represents an optional covalent bond.
摘要翻译：本发明涉及一种抑制具有特征在于血栓素水平升高或前列环素/血栓素水平不平衡的疾病的哺乳动物中的血栓素合成酶和环-AMP磷酸二酯酶的方法，其用下式化合物或其药学上可接受的盐其中：X选自：其中R 1为H，具有1-6个碳原子的烷基，任选取代的苯基或任选取代的苯基低级烷基的共价键，当R 2为H或OH时，或R 1和R 2一起代表氧代，具有1-6个碳原子的亚烷基或任选取代的亚苄基; R3是H或具有1-6个碳原子的烷基，R4是H，R3和R4彼此是顺式或反式，或者R3和R4一起代表共价键; n是0-3的整数; Het是1-咪唑基或3-吡啶基; 而虚线表示任选的共价键。

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