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    Substituted thiazolo[3,2-a]pyrimidines and process for their preparation
    2.
    发明授权
    Substituted thiazolo[3,2-a]pyrimidines and process for their preparation 失效
    取代的噻唑并[3,2-a]嘧啶及其制备方法

    公开(公告)号：US4551457A

    公开(公告)日：1985-11-05

    申请号：US615346

    申请日：1984-05-30

    申请人： Gianfederico Doria ,  Carlo Passarotti ,  Giuliana Arcari ,  Ada Buttinoni

    发明人： Gianfederico Doria ,  Carlo Passarotti ,  Giuliana Arcari ,  Ada Buttinoni

    IPC分类号： A61K31/519 ,  A61P1/04 ,  A61P29/00 ,  C07D513/04 ,  C07F9/6561 ,  A61K31/505

    CPC分类号： C07D513/04 ,  C07F9/6561 ,  Y10S514/927

    摘要： Pharmacologically active thiazolo[3,2-a]pyrimidines of the formula ##STR1## wherein A is a bond between the .alpha.- and .beta.-carbon atoms or (--CH.sub.2 --) group; R.sub.1 and R.sub.2 represent hydrogen, C.sub.1 -C.sub.4 alkyl, cyano, CF.sub.3, thienyl, pyridyl, biphenyl, naphtyl, phenyl optionally substituted, ##STR2## wherein R' and R" are hydrogen or alkyl; R.sub.3 represents hydrogen, halogen, alkyl, OH, formyloxy, alkanoyloxy, alkenyloxy; R.sub.4 represents substituted pyrrole, substituted phenyl or substituted thiazolyl. The compounds have antiinflammatory, antiulcerorgenic and antigastric secretory activity.

    摘要翻译： 药物活性的噻唑并[3,2-a]嘧啶，其中A是α-和β-碳原子或（-CH 2 - ）基团之间的键; R 1和R 2表示氢，C 1 -C 4烷基，氰基，CF 3，噻吩基，吡啶基，联苯基，萘基，任选取代的苯基，其中R'和R“是氢或烷基; R 3表示氢，卤素，烷基，OH，甲酰氧基，烷酰氧基，烯氧基; R4表示取代的吡咯，取代的苯基或取代的噻唑基。 这些化合物具有抗炎，抗溃疡和抗胃分泌活性。

    Substituted 1,3,4-thiadiazolo[3,2-A]pyrimidines and compositions containing them
    3.
    发明授权
    Substituted 1,3,4-thiadiazolo[3,2-A]pyrimidines and compositions containing them 失效
    取代的1,3,4-噻二唑并[3,2-A]嘧啶和含有它们的组合物

    公开(公告)号：US4537962A

    公开(公告)日：1985-08-27

    申请号：US459188

    申请日：1983-01-19

    申请人： Gianfederico Doria ,  Carlo Passarotti ,  Ada Buttinoni

    发明人： Gianfederico Doria ,  Carlo Passarotti ,  Ada Buttinoni

    IPC分类号： A61K31/505 ,  A61K31/519 ,  A61P1/04 ,  C07D513/04 ,  C07F9/6561 ,  C07D239/00 ,  A61K31/495

    CPC分类号： C07D513/04 ,  C07F9/6561

    摘要： Compounds of the formula (I) ##STR1## wherein R.sub.1 is(a) hydrogen or halogen;(b) a C.sub.1 -C.sub.6 alkyl group, unsubstituted or substituted by C.sub.1 -C.sub.4 alkoxy or by halogen;(c) a phenyl ring unsubstituted or substituted by a group chosen from halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy;(d) a C.sub.1 -C.sub.6 alkylthio group;R.sub.2 is hydrogen or halogen;R.sub.3 is 2-pyridyl, 3-pyridyl or 4-pyridyl, wherein each pyridyl group is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl; and the pharmaceutically acceptable salts thereof. The compounds possess anti-ulcerogenic and gastric anti-secretory activity.

    摘要翻译： 式（I）化合物其中R 1为（a）氢或卤素; （b）未被取代或被C 1 -C 4烷氧基取代或被卤素取代的C 1 -C 6烷基; （c）未被取代或被选自卤素，C 1 -C 4烷基和C 1 -C 4烷氧基的基团取代的苯环; （d）C1-C6烷硫基; R2是氢或卤素; R3是2-吡啶基，3-吡啶基或4-吡啶基，其中每个吡啶基是未取代的或被C 1 -C 4烷基取代; 及其药学上可接受的盐。 该化合物具有抗溃疡和胃的抗分泌活性。

    Condensed cycloaliphatic derivatives of substituted pyrido[1,2-a]pyrimidines and methods of treating allergic conditions, peptic ulcers and inhibiting gastric acid secretion with them
    4.
    发明授权
    Condensed cycloaliphatic derivatives of substituted pyrido[1,2-a]pyrimidines and methods of treating allergic conditions, peptic ulcers and inhibiting gastric acid secretion with them 失效
    取代吡啶并[1,2-a]嘧啶的缩合脂环族衍生物及其治疗过敏性疾病，消化性溃疡和抑制胃酸分泌的方法

    公开(公告)号：US4521419A

    公开(公告)日：1985-06-04

    申请号：US489057

    申请日：1983-04-27

    申请人： Gianfederico Doria ,  Carlo Passarotti ,  Pier P. Lovisolo ,  Ada Buttinoni

    发明人： Gianfederico Doria ,  Carlo Passarotti ,  Pier P. Lovisolo ,  Ada Buttinoni

    IPC分类号： C07D471/04 ,  A61K31/505

    CPC分类号： C07D471/04

    摘要： Compounds of the formula (1) ##STR1## wherein n is 1 or 2;R.sub.1 represents a hydrogen or a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a --CN group, a --CONH.sub.2 group or a --COOR.sub.8 group, wherein R.sub.8 represents hydrogen or a C.sub.1 -C.sub.6 alkyl group, unsubstituted or substituted by di(C.sub.1 -C.sub.4) - alkylamino;each of R.sub.2, R.sub.3 and R.sub.4 independently represents a hydrogen or a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group or a C.sub.3 -C.sub.4 alkenyloxy group;A completes a bond, thereby providing a double bond or, when R.sub.1 is --COOR.sub.8 wherein R.sub.8 is as defined above, A may represent also a --CH.sub.2 -- group, thereby providing a cyclopropane ring fused to the pyrido ring;R is (a) furyl, thienyl or pyridyl; or(b) a group of formula ##STR2## wherein each of R.sub.5, R.sub.6 and R.sub.7 represents, independently, a hydrogen or a halogen atom, hydroxy, formyloxy, C.sub.2 -C.sub.8 alkanoyloxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro or a ##STR3## wherein each of R.sub.9 and R.sub.10 independently represents hydrogen, C.sub.1 -C.sub.4 alkyl, formyl or C.sub.2 -C.sub.8 alkanoyl, or adjacent groups represented by two of R.sub.5, R.sub.6 and R.sub.7, taken together, form a C.sub.1 -C.sub.3 alkylenedioxy group; and the pharmaceutically acceptable salts thereof have pharmaceutical activity in the treatment of allergic conditions and peptic ulcers, and inhibit the secretion of gastric acid.

    摘要翻译： 式（1）的化合物其中n为1或2; R1表示氢或卤素原子，C1-C4烷基，-CN基，-CONH2基或-COOR8基，其中R8表示氢或C1-C6烷基，未取代或被二（C1 -C4） - 烷基氨基; R2，R3和R4各自独立地表示氢或卤素原子，C1-C4烷基，C1-C4烷氧基或C3-C4链烯氧基; A完成键，从而提供双键，或当R 1是-COOR 8，其中R 8如上所定义时，A可以也表示-CH 2 - 基，从而提供与吡啶环稠合的环丙烷环; R是（a）呋喃基，噻吩基或吡啶基; 或（b）一组式（I），其中R 5，R 6和R 7各自独立地表示氢或卤素原子，羟基，甲酰氧基，C 2 -C 8烷酰氧基，C 1 -C 4烷基，C 1 -C 4烷氧基，硝基 或其中R 9和R 10各自独立地表示氢，C 1 -C 4烷基，甲酰基或C 2 -C 8烷酰基或由R 5，R 6和R 7中的两个表示的相邻基团一起形成C 1 -C 3亚烷基二氧基 ; 并且其药学上可接受的盐在治疗过敏性病症和消化性溃疡中具有药物活性，并抑制胃酸的分泌。

    Substituted thiazolo[3,2-a]pyrimidines and process for their preparation
    5.
    发明授权
    Substituted thiazolo[3,2-a]pyrimidines and process for their preparation 失效
    取代的噻唑并[3,2-a]嘧啶及其制备方法

    公开(公告)号：US4444773A

    公开(公告)日：1984-04-24

    申请号：US398302

    申请日：1982-07-14

    申请人： Gianfederico Doria ,  Carlo Passarotti ,  Giuliana Arcari ,  Ada Buttinoni

    发明人： Gianfederico Doria ,  Carlo Passarotti ,  Giuliana Arcari ,  Ada Buttinoni

    IPC分类号： A61K31/519 ,  A61P1/04 ,  A61P29/00 ,  C07D513/04 ,  C07F9/6561

    CPC分类号： C07D513/04 ,  C07F9/6561 ,  Y10S514/927

    摘要： Pharmacologically active thiazolo[3,2-a]pyrimidines of the formula ##STR1## wherein A is a bond between the .alpha. and .beta.-carbon atoms or (--CH.sub.2 --) group; R.sub.1 and R.sub.2 represent hydrogen or halogen, C.sub.1 -C.sub.4 alkyl, cyano, CF.sub.3, thienyl, pyridyl, biphenyl, naphtyl, phenyl optionally substituted, ##STR2## wherein R' and R" are hydrogen or alkyl; R.sub.3 represents hydrogen, halogen, alkyl, OH, formyloxy, alkanoyloxy, alkenyloxy; R.sub.4 represents pyridyl optionally substituted by alkyl. The compounds have antiinflammatory, antiulcerogenic and anti-gastric secretory activity.

    摘要翻译： 药物活性的噻唑并[3,2-a]嘧啶，其结构式为：其中A是α和β-碳原子或（-CH 2 - ）基团之间的键; R 1和R 2表示氢或卤素，C 1 -C 4烷基，氰基，CF 3，噻吩基，吡啶基，联苯基，萘基，任选取代的苯基，其中R'和R“是氢或烷基; R 3表示氢，卤素，烷基，OH，甲酰氧基，烷酰氧基，烯氧基; R 4表示任选被烷基取代的吡啶基。 该化合物具有抗炎，抗溃疡和抗胃分泌活性。

    Carboxamido-derivatives of 5H-1,3,4-thiadiazolo[3,2-a]pyrimidines, compositions and use
    8.
    发明授权
    Carboxamido-derivatives of 5H-1,3,4-thiadiazolo[3,2-a]pyrimidines, compositions and use 失效

    公开(公告)号：US4522944A

    公开(公告)日：1985-06-11

    申请号：US559322

    申请日：1983-12-08

    申请人： Gianfederico Doria ,  Carlo Passarotti ,  Ada Buttinoni

    发明人： Gianfederico Doria ,  Carlo Passarotti ,  Ada Buttinoni

    IPC分类号： A61K31/519 ,  A61P29/00 ,  C07D285/12 ,  C07D285/135 ,  C07D513/04 ,  A61K31/505 ,  A61K31/535

    CPC分类号： C07D285/135 ,  C07D513/04

    摘要： The present invention relates to new carboxamido-derivatives of 5H-1,3,4-thiadiazolo[3,2-a]pyrimidines, to a process for their preparation and to pharmaceutical (i.e. anti-inflammatory and analgesic) compositions containing them.The invention provides compounds having the following general formula (I) ##STR1## wherein R.sub.1 represents:(a) a hydrogen or halogen atom or a C.sub.1 -C.sub.6 alkyl group unsubstituted or substituted by C.sub.1 -C.sub.6 alkoxy;(b) a ##STR2## group, wherein n is zero, 1, 2 or 3 and each of R.sub.4 and R.sub.5 is, independently, hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sub.4 and R.sub.5, taken together with the nitrogen atom to which they are linked, form an unsubstituted N-pyrrolidinyl ring or a piperidino, morpholino, N-piperazinyl or ##STR3## ring, wherein m is zero, 1 or 2, the piperidino and morpholino rings are unsubstituted or substituted by one or two C.sub.1 -C.sub.6 alkyl groups and the N-piperazinyl ring is unsubstituted or substituted by a substituent chosen from C.sub.1 -C.sub.6 alkyl, phenyl and pyridyl;(c) trihalomethyl or a R.sub.6 --S(O).sub.p -- group, wherein p is zero, 1 or 2 and R.sub.6 is C.sub.1 -C.sub.6 alkyl or benzyl, wherein the phenyl ring is unsubstituted or substituted by a substituent chosen from halogen, C.sub.1 -C.sub.6 alkyl and C.sub.1 -C.sub.6 alkoxy; or(d) an unsubstituted pyridyl, pyridyl-N-oxide or thienyl ring or a phenyl ring unsubstituted or substituted by one, two or three substituents independently chosen from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, formyloxy, C.sub.2 -C.sub.8 alkanoyloxy, nitro, amino, formylamino, C.sub.2 -C.sub.8 alkanoylamino and di-(C.sub.1 -C.sub.6) alkyl-amino;R.sub.2 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sub.3 represents:(a') a phenyl ring, unsubstituted or substituted by one or two substituents independently chosen from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy and halogen;(b') an unsaturated heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen and sulphur, unsubstituted or substituted by one or two substituents independently chosen from halogen, C.sub.1 -C.sub.6 alkyl and C.sub.1 -C.sub.6 alkoxy; and the pharmaceutically acceptable salts thereof.

    Substituted 1H-pyrazolo (1,5-a) pyrimidines and process for their preparation
    9.
    发明授权
    Substituted 1H-pyrazolo (1,5-a) pyrimidines and process for their preparation 失效
    取代的1H-吡唑并（1,5-a）嘧啶及其制备方法

    公开(公告)号：US4482555A

    公开(公告)日：1984-11-13

    申请号：US474205

    申请日：1983-03-10

    申请人： Gianfederico Doria ,  Carlo Passarotti ,  Ada Buttinoni

    发明人： Gianfederico Doria ,  Carlo Passarotti ,  Ada Buttinoni

    IPC分类号： C07D231/38 ,  C07D487/04 ,  A61K31/41 ,  A61K31/495

    CPC分类号： C07D231/38 ,  C07D487/04

    摘要： Compounds of general formula (I) ##STR1## wherein R.sub.1 is a 2-pyridyl, 3-pyridyl or 4-pyridyl group; (b) a phenyl ring, unsubstituted or substituted by one or two groups chosen from halogen, trihalo-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkyl, nitro, amino and C.sub.2 -C.sub.6 alkanoylamino; (c) benzyl; or (d) C.sub.1 -C.sub.6 alkyl;each of R.sub.2 and R.sub.3 independently is a hydrogen or a halogen atom or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl;R.sub.5 is (a') ##STR2## wherein each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sub.6 and R.sub.7, taken together with the nitrogen atom to which they are linked, form a morpholino, piperidino, N-pyrrolidinyl or N-piperazinyl ring, wherein the N-piperazinyl ring is unsubstituted or substituted by C.sub.1 -C.sub.6 alkyl;(b') a ##STR3## wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen;(c') --NHR.sub.9, wherein R.sub.9 is a 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidinyl, 2-pyrazinyl, 3-pyrazolyl, 2-thiazolyl or 2-benzothiazolyl group, each of these groups being unsubstituted or substituted by one or two groups chosen from halogen, C.sub.1 -C.sub.6 alkyl, phenyl, hydroxy and C.sub.1 -C.sub.6 alkoxy;(d') ##STR4## wherein m is 1, 2 or 3 and R.sub.6 and R.sub.7 are as defined above; or the pharmaceutically acceptable salts thereof; are disclosed as anti-inflammatory agents.

    摘要翻译： 通式（I）的化合物其中R 1是2-吡啶基，3-吡啶基或4-吡啶基; （b）未被取代或被一个或两个选自卤素，三卤代-C 1 -C 4烷基，C 1 -C 6烷基，硝基，氨基和C 2 -C 6烷酰氨基的基团取代的苯环; （c）苄基; 或（d）C 1 -C 6烷基; R2和R3各自独立地是氢或卤素原子或C1-C6烷基; R4是氢，C1-C6烷基或苯基; R5是（a'），其中R6和R7各自独立地是氢或C1-C6烷基，或R6和R7与它们所连接的氮原子一起形成吗啉代，哌啶子基，N-吡咯烷基 或N-哌嗪基环，其中所述N-哌嗪基环是未取代的或被C 1 -C 6烷基取代; （b'）a其中R 8是氢，C 1 -C 4烷基，C 1 -C 4烷氧基或卤素; （c'）-NHR 9，其中R 9是2-吡啶基，3-吡啶基，4-吡啶基，2-嘧啶基，2-吡嗪基，3-吡唑基，2-噻唑基或2-苯并噻唑基，这些基团各自为未取代的 或被一个或两个选自卤素，C 1 -C 6烷基，苯基，羟基和C 1 -C 6烷氧基的基团取代; （d'）其中m为1,2或3，R6和R7如上定义; 或其药学上可接受的盐; 被公开为抗炎剂。