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35 条记录 (耗时 0.022 秒)

    Analgesic and antiinflammatory 1,3-diacyl-2-oxindole compounds
    1.
    发明授权
    Analgesic and antiinflammatory 1,3-diacyl-2-oxindole compounds 失效
    镇痛和抗炎性1,3-二酰基-2-羟吲哚化合物

    公开(公告)号：US4808601A

    公开(公告)日：1989-02-28

    申请号：US196187

    申请日：1988-05-19

    申请人： Saul B. Kadin

    发明人： Saul B. Kadin

    IPC分类号： C07D209/34 ,  C07D209/42 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  A61K31/42 ,  C07D413/06

    CPC分类号： C07D401/06 ,  C07D209/34 ,  C07D209/42 ,  C07D405/06 ,  C07D409/06

    摘要： Certain novel 2-oxindole compounds, having an acyl substituent at both the 1-position and the 3-position, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic agents and antiinflammatory agents in mammalian subjects. These 1,3-diacyl-2-oxindole compounds are of particular value for acute administration for ameliorating pain in human patients recovering from surgery or trauma, and also for chronic administration to human subjects for alleviating the symptoms of chronic diseases such as rheumatoid arthritis and osteoarthritis.

    摘要翻译： 在1-位和3-位具有酰基取代基的某些新的2-羟基吲哚化合物是环加氧酶（CO）和脂氧合酶（LO））的抑制剂，并且可用作哺乳动物受试者中的止痛剂和抗炎药 。 这些1,3-二酰基-2-羟吲哚化合物对于从手术或创伤中恢复的人类患者的急性给药具有特别的价值，并且还用于慢性给予受试者以缓解慢性疾病如类风湿性关节炎和 骨关节炎。

    [1,2,4]Triazolo[4,3-a]quinoxaline-4-amine derivatives
    2.
    发明授权
    [1,2,4]Triazolo[4,3-a]quinoxaline-4-amine derivatives 失效
    [1,2,4]三唑并[4,3-a]喹喔啉-4-胺衍生物

    公开(公告)号：US4623725A

    公开(公告)日：1986-11-18

    申请号：US796134

    申请日：1985-11-08

    申请人： Saul B. Kadin ,  Reinhard Sarges

    发明人： Saul B. Kadin ,  Reinhard Sarges

    IPC分类号： C07D241/44 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D241/44

    摘要： A series of novel [1,2,4]triazolo[4,3-a]quinoxaline-4-amine derivatives wherein the amine group is optionally substituted with lower alkyl, phenylalkyl having up to three carbon atoms in the alkyl moiety or alkanoyl having from two to five carbon atoms, or the amine group alternatively completes a piperazino ring, the quinoxaline ring is optionally substituted with fluorine, chlorine, bromine or methoxy, and the triazolo ring is optionally substituted with lower alkyl, lower perfluoroalkyl or phenyl are disclosed. These novel compounds are useful for treatment of symptoms associated with depression. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention.

    摘要翻译： 一系列新的[1,2,4]三唑并[4,3-a]喹喔啉-4-胺衍生物，其中胺基任选被低级烷基取代，在烷基部分具有至多三个碳原子的苯基烷基或具有 2-5个碳原子或胺基交替地完成哌嗪环，喹喔啉环任选被氟，氯，溴或甲氧基取代，三唑并任选被低级烷基，低级全氟烷基或苯基取代。 这些新型化合物可用于治疗与抑郁症有关的症状。 还公开了含有本发明新化合物的药物组合物。

    1-Oxo-1H-6-piperidinopyrimido[1,2-a]quinoline-2-carboxylic acids and esters
    5.
    发明授权
    1-Oxo-1H-6-piperidinopyrimido[1,2-a]quinoline-2-carboxylic acids and esters 失效
    1-氧代-1H-6-哌啶子基嘧啶并[{1,2-a {9喹啉-2-羧酸和酯

    公开(公告)号：US4014881A

    公开(公告)日：1977-03-29

    申请号：US594766

    申请日：1975-07-10

    申请人： Saul B. Kadin ,  Peter F. Moore

    发明人： Saul B. Kadin ,  Peter F. Moore

    IPC分类号： A61K31/505 ,  A61P1/04 ,  C07D215/38 ,  C07D471/04 ,  C07D401/04

    CPC分类号： C07D215/38 ,  C07D471/04 ,  Y10S514/927

    摘要： As antiulcer agents, a series of 1-oxo-1H-6-substituted pyrimido[1,2-a]quinoline-2-carboxylic acids and esters of the formula ##STR1## wherein R.sub.1 is alkoxy having from one to two carbon atoms or piperidino; and R.sub.2 is hydrogen or alkyl having from one to four carbon atoms; the pharmaceutically acceptable acid addition salts of those compounds wherein R.sub.1 is piperidino, and the pharmaceutically acceptable cationic salts of those compounds wherein R.sub.2 is hydrogen.

    摘要翻译： 作为抗溃疡剂，可以使用一系列1-氧代-1H-6-取代的嘧啶并[1,2-a]喹啉-2-羧酸和式的化合物，其中R1是具有1至2个碳原子的烷氧基或 哌啶子 并且R 2是氢或具有1-4个碳原子的烷基; 其中R 1为哌啶子基的那些化合物的药学上可接受的酸加成盐及其中R2为氢的化合物的药学上可接受的阳离子盐。

    N,3-Disubstituted 2-oxindole-1-carboxamides as analgesic and antiinflammatory agents
    7.
    发明授权
    N,3-Disubstituted 2-oxindole-1-carboxamides as analgesic and antiinflammatory agents 失效
    N，3-二取代的2-羟基吲哚-1-甲酰胺作为止痛剂和抗炎剂

    公开(公告)号：US4569942A

    公开(公告)日：1986-02-11

    申请号：US714012

    申请日：1985-03-22

    申请人： Saul B. Kadin

    发明人： Saul B. Kadin

    IPC分类号： C07D209/34 ,  C07D209/60 ,  C07D209/70 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D491/04 ,  C07D495/04 ,  A61K31/40

    CPC分类号： C07D401/06 ,  C07D209/34 ,  C07D209/60 ,  C07D209/70 ,  C07D405/06 ,  C07D409/06 ,  C07D491/04 ,  C07D495/04

    摘要： Certain 2-oxindole-1-carboxamide compounds having an acyl substituent at the 3-position, and also further substituted on the carboxamide nitrogen by an alkyl, cycloalkyl, phenyl or substituted phenyl group, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and antiinflammatory agents in mammalian subjects. These 2-oxindole-1-carboxamide compounds are of particular value for ameliorating pain in human patients recovering from surgery or trauma, and alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.Certain 2-oxindole-1-carboxamide compounds unsubstituted at C-3, but having a substituent on the carboxamide nitrogen, are useful as intermediates to the analgesic and antiinflammatory agents of the invention.

    摘要翻译： 某些2-位羟基吲哚-1-甲酰胺化合物，其在3-位上具有酰基取代基，并且还在羧酰胺氮上被烷基，环烷基，苯基或取代的苯基取代，是环加氧酶（CO）和脂氧合酶 LO）酶，并且在哺乳动物受试者中可用作镇痛和抗炎剂。 这些2-羟基吲哚-1-甲酰胺化合物对于改善人类受试者恢复的人类患者的疼痛和减轻慢性疾病如类风湿性关节炎和骨关节炎的症状具有特别的价值。 在C-3未被取代但在羧酰胺氮上具有取代基的某些2-羟基吲哚-1-甲酰胺化合物可用作本发明的止痛和抗炎剂的中间体。

    1-Oxo-1H-thiazolo[3,2-a]pyrimidine-2-carboxamides
    8.
    发明授权
    1-Oxo-1H-thiazolo[3,2-a]pyrimidine-2-carboxamides 失效
    1-氧代-1H-噻唑并[3,2-a]嘧啶-2-甲酰胺

    公开(公告)号：US4414388A

    公开(公告)日：1983-11-08

    申请号：US330578

    申请日：1981-12-14

    申请人： Saul B. Kadin

    发明人： Saul B. Kadin

    IPC分类号： C07D277/40 ,  C07D277/42 ,  C07D277/60 ,  C07D277/82 ,  C07D513/04 ,  C07D513/02 ,  A61K31/505

    CPC分类号： C07D277/60 ,  C07D277/40 ,  C07D277/42 ,  C07D277/82 ,  C07D513/04

    摘要： Antiallergy and antiulcer agents having the formula (I), ##STR1## and their pharmaceutically acceptable salts, wherein R.sub.1 and R.sub.2 taken separately are each hydrogen or lower alkyl; and R.sub.1 and R.sub.2 taken together are alkylene of 3-9 carbon atoms or phenylalkylene of 9-11 carbon atoms, with the proviso that the ring so formed is between 5- and 8-membered; acids of the formula (II), ##STR2## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.3 is hydrogen, which are useful as intermediates for compounds of the formula (I), but in many instances also possess the same useful biological activity as do formula I compounds; and intermediates of the formula II wherein R.sub.1 and R.sub.2 are defined as above, and R.sub.3 is alkyl of 1 to 4 carbon atoms, carbalkoxy of 2 to 5 carbon atoms, carbophenoxy or carbobenzoxy, are also described.

    摘要翻译： 具有式（I），其中R1和R2分别为氢或低级烷基的式（I）及其药学上可接受的盐的抗过敏剂和抗溃疡剂; 并且R 1和R 2一起是3-9个碳原子的亚烷基或9-11个碳原子的苯基亚烷基，条件是如此形成的环为5-和8-元; 式（II）的酸，其中R 1和R 2如上所定义，R 3是氢，其可用作式（I）化合物的中间体，但在许多情况下也具有相同的有用的 生物活性如式I化合物; 和式II的中间体，其中R 1和R 2如上定义，并且R 3是1至4个碳原子的烷基，2至5个碳原子的烷氧基，碳苯氧基或苄氧羰基。

    Diphenylpropenamides as SRS-A antagonists
    9.
    发明授权
    Diphenylpropenamides as SRS-A antagonists 失效
    二苯基丙烯酰胺作为SRS-A拮抗剂

    公开(公告)号：US4342781A

    公开(公告)日：1982-08-03

    申请号：US268439

    申请日：1981-05-29

    申请人： Saul B. Kadin

    发明人： Saul B. Kadin

    IPC分类号： C07C205/56 ,  A61K31/24 ,  C07C101/453

    CPC分类号： C07C205/56 ,  Y10S514/826

    摘要： Certain new diphenylpropenamides having a carboxyalkanamido or a carboxyalkenamido group on one of the phenyl rings and their use for antagonizing the spasmogenic activity of the slow-reacting substance of anaphylaxis (SRS-A) in a human subject. In particular, the compounds of the invention are useful for preventing and treating certain obstructive airways diseases, notably allergic bronchial asthma, allergic rhinitis and certain skin disorders, in human subjects.

    摘要翻译： 在苯环之一上具有羧基烷酰氨基或羧烯酰胺基的某些新的二苯基丙烯酰胺及其用于拮抗人受试者中过敏性缓慢反应物质（SRS-A）的痉挛性活性的用途。 特别地，本发明的化合物可用于预防和治疗人受试者中某些阻塞性气道疾病，特别是过敏性支气管哮喘，过敏性鼻炎和某些皮肤病。

    1-Oxo-6-substituted pyrimido [1,2-a]quinoline-2-carboxylic acids and derivatives thereof and their use as antiallergy agents
    10.
    发明授权
    1-Oxo-6-substituted pyrimido [1,2-a]quinoline-2-carboxylic acids and derivatives thereof and their use as antiallergy agents 失效
    1-氧代-6-取代的嘧啶并[8 1,2-a {9喹啉-2-羧酸及其衍生物及其作为抗过敏剂的用途

    公开(公告)号：US4066766A

    公开(公告)日：1978-01-03

    申请号：US650713

    申请日：1976-01-20

    申请人： Saul B. Kadin

    发明人： Saul B. Kadin

    IPC分类号： C07D215/38 ,  C07D215/48 ,  A61K31/505 ,  C07D471/04

    CPC分类号： C07D215/38 ,  C07D215/48 ,  Y10S514/826

    摘要： A novel series of 1-oxo-1H-6-substitutedpyrimido[1,2-a]quinoline-2-carboxylic acids of the formula ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3 is hydrogen, alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 5 carbon atoms, carboalkoxy having from 1 to 5 carbon atoms in the alkoxy group, fluoro, chloro, bromo, methylthio or methylsulfinyl; with the proviso that no more than two of R.sub.1, R.sub.2 and R.sub.3 are bulky groups; i.e., branched-chain alkyl or branched-chain alkoxy, and when two of said R.sub.1, R.sub.2 and R.sub.3 are bulky groups they are located on non-adjacent positions; R.sub.4 is selected from the group consisting of chloro and bromo and --OR.sub.4 ' wherein OR.sub.4 ' is selected from the group consisting of alkoxy having from 1 to 5 carbon atoms, alkenyloxy of 3 to 4 carbon atoms and alkynyloxy of 3 to 4 carbon atoms; R.sub.5 is hydroxy, alkoxy having from 1 to 5 carbon atoms and hydroxy substituted alkoxy having from 2 to 5 carbon atoms; R.sub.2 and R.sub.3 when taken together are 1,3-butadienyl or alkylenedioxy of one to two carbon atoms; and the pharmaceutically-acceptable cationic salts of those compounds wherein R.sub.5 is hydroxy; compositions thereof; and their use as antiallergy agents.

    摘要翻译： 式Ⅰ的1-氧代-1H-6-取代的嘧啶-2-甲酸的新型系列，其中R 1，R 2和R 3各自为氢，具有1至5个 碳原子，具有1至5个碳原子的烷氧基，在烷氧基中具有1至5个碳原子的烷氧基，氟，氯，溴，甲硫基或甲基亚磺酰基; 条件是不超过两个R1，R2和R3是大体积基团; 即支链烷基或支链烷氧基，当所述R1，R2和R3中的两个为大体积时，它们位于非相邻位置上; R 4选自氯和溴，-OR 4'，其中OR 4'选自具有1至5个碳原子的烷氧基，3至4个碳原子的链烯氧基和3至4个碳原子的炔氧基; R5是羟基，具有1至5个碳原子的烷氧基和具有2至5个碳原子的羟基取代的烷氧基; 当R 2和R 3一起是1至2个碳原子的1,3-丁二烯基或亚烷基二氧基时; 和其中R5是羟基的那些化合物的药学上可接受的阳离子盐; 组合物; 并将其用作抗过敏剂。