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1. 发明授权

US4584297A Pyrrolo[1,2-c]-1,3-thiazines 失效
标题翻译：吡咯并[1,2-c] -1,3-噻嗪
公开(公告)号：US4584297A
公开(公告)日：1986-04-22
申请号：US721773
申请日：1985-04-10
申请人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
发明人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
IPC分类号： A61K31/429 , A61K31/435 , A61K31/54 , A61P7/02 , C07D213/02 , C07D213/55 , C07D279/06 , C07D401/06 , C07D417/04 , C07D417/06 , C07D471/04 , C07D487/04 , C07D487/06 , C07D495/04 , C07D513/04 , C07D417/14
CPC分类号： C07D401/06 , C07D213/55 , C07D279/06 , C07D417/06 , C07D471/04 , C07D487/04 , C07D487/06 , C07D513/04
摘要： Antithrombotics of the formula ##STR1## in which A=S, SO or SO.sub.2, R.sub.3 =H, alkyl or substituted or unsubstituted phenyl, X=O, S, NH or variously substituted nitrogen, p is 0 or 1 and y=H, NH.sub.2, or various substituted amines.
摘要翻译：其中A = S，SO或SO 2，R 3 = H，烷基或取代或未取代的苯基，X = O，S，NH或各种取代的氮，p为0或1，y = H， NH 2或各种取代的胺。

2. 发明授权

US4547504A Substituted phenyl piperazinyl pyrrolidin-2-ones and related compounds useful as anti-depressants and their use 失效
标题翻译：取代的苯基哌嗪基吡咯烷-2-酮和可用作抗抑郁剂的相关化合物及其用途
公开(公告)号：US4547504A
公开(公告)日：1985-10-15
申请号：US558775
申请日：1983-12-06
申请人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
发明人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
IPC分类号： C07D401/04 , A61K31/40 , A61P25/00 , C07D207/24 , C07D207/26 , C07D207/273 , C07D295/135 , C07D403/04 , A61K31/445 , A61K31/495
CPC分类号： C07D207/273 , C07D207/24 , C07D295/135
摘要： Pyrrolidine derivatives of the formula: ##STR1## wherein X represents an oxygen or sulphur atom, R represents a hydrogen atom or an alkyl radical, R.sub.o represents a hydrogen atom, an alkyl radical or a phenyl radical optionally substituted by a halogen atom or by an alkyl, alkoxy, alkylthio or nitro radical, A represents a nitrogen atom or a radical .dbd.CH--, the symbol Y represents a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, alkylcarbonyl, nitro, amino, alkylcarbonylamino, alkylamino, dialkylamino, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, cyano, trifluoromethyl, hydroxy, mercapto, alkylcarbonyloxy or alkylcarbonylthio radical, n represents zero or 1, and p represents 1, 2 or 3, it being understood that the alkyl and alkoxy radicals, and alkyl and alkoxy moieties of any of the aforementioned groups, contain from 1 to 4 carbon atoms are new therapeutically useful compounds, more particularly useful as antidepressants.
摘要翻译：下式的吡咯烷衍生物：其中X表示氧或硫原子，R表示氢原子或烷基，Ro表示氢原子，烷基或任选被卤素原子取代的苯基，或由烷基，烷氧基，烷硫基或硝基，A表示氮原子或基团= CH-，符号Y表示氢或卤素原子或烷基，烷氧基，烷硫基，烷基羰基，硝基，氨基，烷基羰基氨基，烷基氨基，二烷基氨基，烷基亚磺酰基，烷基磺酰基，烷氧基羰基，氰基，三氟甲基，羟基，巯基，烷基羰基氧基或烷基羰基硫基，n表示0或1，p表示1,2或3，应理解烷基和烷氧基，烷基和烷氧基部分含有1至4个碳原子的任何上述基团是新的治疗上有用的化合物，更特别可用作抗抑郁药。

3. 发明授权

US4539400A Pyridin-3-yl substituted ortho-fused pyrrole derivatives 失效
标题翻译：吡啶-3-基取代的邻 - 稠合吡咯衍生物
公开(公告)号：US4539400A
公开(公告)日：1985-09-03
申请号：US569909
申请日：1984-01-11
申请人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
发明人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
IPC分类号： A61K31/428 , C07D213/54 , C07D213/55 , C07D279/06 , C07D401/04 , C07D401/06 , C07D417/04 , C07D417/06 , C07D471/04 , C07D487/04 , C07D487/06 , C07D513/04 , C07D521/00 , C07D498/04
CPC分类号： C07D213/54 , C07D213/55 , C07D231/12 , C07D233/56 , C07D249/08 , C07D279/06 , C07D401/04 , C07D401/06 , C07D417/04 , C07D417/06 , C07D471/04 , C07D487/04 , C07D487/06 , C07D513/04
摘要： The invention provides new derivatives of the formula: ##STR1## in which either (a) Y=COOH or a radical of the formula (II), in which R.sub.2 =alkyl or benzyl, A=a sulphur atom, m=1, n=0, R=pyridin-3-yl and R.sub.1 =H, or (b) Y=CN, COOH or a radical of the formula ##STR2## defined as above, A=S, O or CH.sub.2, m=1 or 2 and n=0, 1 or 2, (m+n) being 1, 2 or 3, R=H, alkyl or phenyl (optionally substituted by halogen, alkyl, alkoxy or CF.sub.3) and R.sub.1 =a radical of the formula ##STR3## in which p=0 or 1, the alkyl radicals and alkyl portions being straight-chain or branched-chain and containing 1 to 4 carbon atoms each. Processes for the production of these compounds are described. They are useful as intermediates for the preparation of new medicaments.
摘要翻译：本发明提供下式的新衍生物：其中（a）Y = COOH或式（II）的基团，其中R 2 =烷基或苄基，A =硫原子，m = 1，n = 0，R =吡啶-3-基和R 1 = H，或（b）Y = CN，COOH或如上定义的式（II）的基团，A = S，O或CH2 ，m = 1或2，n = 0,1或2，（m + n）为1,2或3，R = H，烷基或苯基（任选被卤素，烷基，烷氧基或CF 3取代），R 1 = 其中p = 0或1的式（III）的基团，烷基和烷基部分是直链或支链的并且各自含有1至4个碳原子。描述了这些化合物的制备方法。它们作为制备新药物的中间体是有用的。

4. 发明授权

US4684658A Anti-thrombotic ortho-condensed pyrrole derivatives, compositions, and method of use therefor 失效
公开(公告)号：US4684658A
公开(公告)日：1987-08-04
申请号：US684061
申请日：1984-12-20
申请人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
发明人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
IPC分类号： A61K31/435 , A61K31/505 , A61P7/02 , C07D401/06 , C07D401/14 , C07D417/06 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , A61K31/38 , C07D417/14
CPC分类号： C07D401/06 , C07D401/14 , C07D417/06 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The invention provides novel pyrrole derivatives of formula: ##STR1## in which R'=H, alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, Z=0 or S, p=0 or 1, andeither A is a heterocyclic ring such that it forms, with pyrrole, a 1H,3H-pyrrolo[1,2-c]thiazole, 2,3-dihydro-1H-pyrrolizine optionally substituted by OH, 5,6,7,8-tetrahydroindolizine, 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-thiazine, 2,3-dihydropyrrolo[2,1-b]thiazole, 1H,3H-pyrrolo[1,2-c]oxazole, 1,2-dihydro-4H-pyrrolo]1,2-c]-1,3-oxazine or 2,3-dihydropyrrolo[2,1-b]oxazole ring system, n=0 or 1, Het=3-pyridyl or 5-thiazolyl, and(1) either R=H, halogen, alkyl or phenyl optionally substituted by halogen, alkyloxy or alkylthio and Y=alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, or Y=--NR.sub.1 R.sub.2 with:either R.sub.1 =H and R.sub.2 =unsubstituted alkyl, cycloalkyl (C.sub.3 -C.sub.6), alkenyl (C.sub.2 -C.sub.4), alkynyl (C.sub.3 -C.sub.4), benzyl or phenyl radicals optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3 or NO.sub.2, or R.sub.2 =adamantyl, pyridyl or pyridylmethyl,or R.sub.1 and R.sub.2 =both unsubstituted alkylor R.sub.1 and R.sub.2 from a 4-phenylpiperazin-1-yl radical the phenyl part of which may be substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3 or NO.sub.2(2) or R=halogen, alkyl or phenyl optionally substituted by halogen, alkyloxy or alkylthio, and Y=NH.sub.2or A is a heterocyclic ring such that it forms, with pyrrole, a 2,3-dihydro-1H-pyrrolizine substituted by OH, 2,3-dihydropyrrolo[2,1-b]thiazole or 2,3-dihydropyrrolo[2,1-b]oxazole ring system, R=H, Y=NH.sub.2, n=0 or 1 or Het=5-thiazolyl or 3-pyridyl,or A is a heterocyclic ring such that it forms, with pyrrole, a 1H,3H-pyrrolo[1,2-c]thiazole, 2,3-dihydro-1H-pyrrolizine, 5,6,7,8-tetrahydroindolizine, 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-thiazine, 1H,3H-pyrrolo[1,2-c]oxazole or 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-oxazine ring system, R=H, Y=NH.sub.2 andeither Het=5-thiazolyl and n=0 or 1or Het=3-pyridyl and n=1, the alkyl containing 1 to 4 C as a straight or branched chain, and their acid addition salts, pharmaceutical compositions containing the said pyrrole derivatives and process for their preparation. These pyrrole derivatives are useful in prophylactic and therapeutic treatment of thrombotic complaints.

5. 发明授权

US4546100A Pyrrolo[1,2-c]thiazoles useful as antithrombotic agents 失效
标题翻译：吡咯并[1,2-c]噻唑可用作抗血栓形成剂
公开(公告)号：US4546100A
公开(公告)日：1985-10-08
申请号：US569907
申请日：1984-01-11
申请人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
发明人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
IPC分类号： A61K31/429 , A61K31/435 , A61K31/54 , A61P7/02 , C07D213/02 , C07D213/55 , C07D279/06 , C07D401/06 , C07D417/04 , C07D417/06 , C07D471/04 , C07D487/04 , C07D487/06 , C07D495/04 , C07D513/04 , C07D401/08 , A61K31/44
CPC分类号： C07D401/06 , C07D213/55 , C07D279/06 , C07D417/06 , C07D471/04 , C07D487/04 , C07D487/06 , C07D513/04
摘要： Antithrombotics of the formula: ##STR1## wherein A is S, SO or SO.sub.2 ; R.sub.3 is H, alkyl or substituted or unsubstituted phenyl; p is zero or 1; X is O, S, N or variously substituted nitrogen; Y is H or various substituted amines.
摘要翻译：下式的抗血栓药物：其中A是S，SO或SO 2; R3是H，烷基或取代或未取代的苯基; p为零或1; X是O，S，N或各种取代的氮; Y是H或各种取代的胺。

6. 发明授权

US4529728A 1H,3H-pyrrolo[1,2-c]thiazole derivatives having anti-allergic and anti-inflammatory activity 失效
标题翻译： 1H，具有抗过敏和抗炎活性的3H-吡咯并[1,2-c]噻唑衍生物
公开(公告)号：US4529728A
公开(公告)日：1985-07-16
申请号：US569908
申请日：1984-01-11
申请人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
发明人： Jean-Louis Fabre , Daniel Farge , Claude James , Daniel Lave
IPC分类号： C07D471/04 , A61K31/425 , A61K31/429 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/54 , A61P7/02 , A61P29/00 , A61P37/08 , C07D213/02 , C07D233/60 , C07D513/04 , C07D521/00 , A61K31/445
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D513/04
摘要： New compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 =H or alkyl and(a) R=CN or alkylcarbonyl, or(b) R=CON(R.sub.3)R.sub.4, in which R.sub.3 =H and R.sub.4 =NH.sub.2, alkylamino, dialkylamino, phenylamino or diphenylamino; or R.sub.3 and R.sub.4 =H, alkyl (1 to 5 C) or substituted phenyl; or R.sub.3 =H and R.sub.4 =pyridyl or alkyl (1 to 5 C) substituted by COOH, NH.sub.2, alkylamino, dialkylamino, morpholino, piperidino, pyrrolidin-1-yl, piperazin-1-yl (optionally substituted by alkyl, pyridyl or optionally substituted phenyl or benzyl), optionally substituted phenyl, pyridyl or imidazolyl; or R.sub.3 and R.sub.4 form an imidazolyl radical or a 5-membered or 6-membered heterocycle which can contain an oxygen, sulphur or nitrogen atom and which is optionally substituted by alkyl, alkoxycarbonyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, pyridyl, pyrimidinyl, pyrazinyl, optionally substituted phenyl or optionally substituted benzyl; or(c) R=--C(.dbd.NOH)NH.sub.2 or --C[.dbd.NN(R'R")NH.sub.2 ], in which R' and R"=alkyl,the said alkyl radicals and alkyl portions being straight-chain or branched-chain and, unless mentioned otherwise, containing 1 to 4 carbon atoms, and the substituted phenyl and benzyl radicals carrying a halogen atom or an alkyl, alkoxy, alkylthio, trifluoromethyl or dialkylamino radical, and their tautomeric forms, addition salts with acids and the metals salts and the addition salts with nitrogen bases, are useful anti-allergic and anti-inflammatory agents. A variety of methods of making them are described.
摘要翻译：式（I）的新化合物，其中R 1和R 2 = H或烷基和（a）R = CN或烷基羰基，或（b）R = CON（R3）R4，其中R3 = H和R4 = NH 2，烷基氨基，二烷基氨基，苯基氨基或二苯基氨基; 或R 3和R 4 = H，烷基（1至5 C）或取代的苯基; 或R 3 = H和R 4 =被COOH，NH 2，烷基氨基，二烷基氨基，吗啉代，哌啶子基，吡咯烷-1-基，哌嗪-1-基取代的吡啶基或烷基（1至5 C）（任选地被烷基，吡啶基或任选地取代的苯基或苄基），任选取代的苯基，吡啶基或咪唑基; 或R3和R4形成咪唑基或可含有氧，硫或氮原子的5元或6元杂环，并且其任选被烷基，烷氧基羰基，羟基烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，吡啶基，嘧啶基，吡嗪基，任选取代的苯基或任选取代的苄基; 或（c）R = -C（= NOH）NH 2或-C [= NN（R'R“）NH 2]，其中R'和R”=烷基，所述烷基和烷基部分为直链，链或支链，除非另有说明，含有1至4个碳原子，并且取代的苯基和苄基带有卤素原子或烷基，烷氧基，烷硫基，三氟甲基或二烷基氨基，以及它们的互变异构形式，与酸和金属盐和与氮碱的加成盐是有用的抗过敏和抗炎剂。描述了制作它们的各种方法。

7. 发明授权

US4786645A 1H, 3H-pyrrolo (1,2-C) thiazole derivatives and pharmaceutical compositions 失效
标题翻译： 1H，3H-吡咯（1,2-C）噻唑衍生物和药物组合物
公开(公告)号：US4786645A
公开(公告)日：1988-11-22
申请号：US69211
申请日：1987-07-02
申请人： Jean-Louis Fabre , Claude James , Daniel Lave
发明人： Jean-Louis Fabre , Claude James , Daniel Lave
IPC分类号： A61K31/50 , A61K31/44 , A61K31/47 , A61P7/02 , A61P29/00 , C07D513/04 , C07D417/14
CPC分类号： C07D513/04
摘要： A compound of the general formula I: ##STR1## in which Ar is a pyridyl, quinolinyl, isoquinolinyl, naphthyridinyl, pyrimidyl, quinazolinyl, thiazolyl, benzothiazolyl, imidazolyl, benzimidazolyl, oxazolyl, benzoxazolyl, thienyl, benzothienyl or naphthyl group; optionally substituted with one or more halogen or alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, alkylcarbonyl, benzoyl, alkyloxycarbonyl, carboxy, phenoxycarbonyl, alkylcabonyloxy, benzoyloxy, alkylcarbonylamino, benzamido, phenyl, benzyl, phenoxy or phenylthio group, provided that (i) when Ar is a pyridyl group, the pyridyl group must be substituted, (ii) an alkyl moiety contains 1 to 4 straight- or branched chain carbon atoms; (iii) a phenyl moiety may be unsubstituted or substituted with one or more halogen or alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, phenyl or benzyl groupin separate enantiomeric form or mixtures thereof, or a pharmaceutically acceptable salt thereof is useful in the treatment of all pathological conditions in which PAF-acether may be implicated directly or indirectly.
摘要翻译：其中Ar是吡啶基，喹啉基，异喹啉基，萘啶基，嘧啶基，喹唑啉基，噻唑基，苯并噻唑基，咪唑基，苯并咪唑基，恶唑基，苯并恶唑基，噻吩基，苯并噻吩基或萘基的通式I的化合物：其中Ar是吡啶基，烷基氨基，烷基磺酰基，磺酰氨基，烷基亚磺酰氨基，二烷基磺酰氨基，烷基羰基，苯甲酰基，烷氧基羰基，羧基，苯氧基羰基，烷基羰基氧基，苯甲酰氧基，烷基羰基氨基，苯甲酰氨基，苯基，苄基，苯氧基或苯硫基，条件是（ⅰ）当Ar是吡啶基时，吡啶基必须被取代，（ii）烷基部分含有1-4个直链或支链碳原子; （iii）苯基部分可以是未取代的或被一个或多个分开的对映体形式或其混合物中的一个或多个卤素或烷基，烷氧基，烷硫基，三氟甲基，氨基，烷基氨基，二烷基氨基，羟基，氰基，苯基或苄基其可接受的盐可用于治疗PAF-乙酰胆碱可直接或间接牵连的所有病理状况。

8. 发明授权

US4783472A 1H,3H-pyrrol[1,2-c]thiazole derivatives and pharmaceutical compositions containing them 失效
公开(公告)号：US4783472A
公开(公告)日：1988-11-08
申请号：US69520
申请日：1987-07-02
申请人： Jean-Louis Fabre , Claude James , Daniel Lave
发明人： Jean-Louis Fabre , Claude James , Daniel Lave
IPC分类号： A61K31/44 , A61P7/02 , A61P29/00 , C07D513/04 , C07D409/00 , C07D215/04 , C07D217/00 , C07D401/00
CPC分类号： C07D513/04
摘要： A compound of the general formula I; ##STR1## in which R is hydrogen or a halogen or an alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridylcarbamoyl, dipyridylcarbamoyl, benzyl, alkylcarbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, benzoyloxy, alkylcarbonylamino, benzamido, phenyl, phenoxy or phenylthio group, X is oxygen or sulphur or an imino, alkylimino, phenylimino, benzylimino, sulphinyl, sulphonyl, carbonyl, carbonylmethylene, methylenecarbonyl, carbonylvinylene or vinylenecarbonyl group, or X represents a valency bond or a straight-chain alkylene group containing 1 to 4 carbon atoms and Ar is a phenyl, naphthyl, pyridyl, quinolinyl, isoquinolinyl, thienyl, benzothienyl, thieno[3,2-b]thien-2-yl or thieno[2,3-b]thien-2-yl group, it being possible for the group Ar to be unsubstituted or substituted with one or more halogen or alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridylcarbamoyl, dipyridylcarbamoyl, benzyl, alkylcarbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, benzoyloxy, alkylcarbonylamino or benzamido group;each alkyl moiety containing 1 to 4 straight- or branched-chain carbon atoms; the compound being in separate enantiomeric form or mixtures thereof or a pharmaceutically acceptable salt thereof is useful in the treatment of all the pathological conditions in which PAF-acether may be directly or indirectly implicated.

9. 发明授权

US4128650A Dibenzo[de, h]quinoline derivatives 失效
标题翻译： Dibenzo {8 de，h {9 quinoline derivatives
公开(公告)号：US4128650A
公开(公告)日：1978-12-05
申请号：US798139
申请日：1977-05-18
申请人： Jean-Louis Fabre , Daniel Farge , Claude James
发明人： Jean-Louis Fabre , Daniel Farge , Claude James
IPC分类号： A61K31/47 , A61K31/473 , A61P31/12 , C07D209/48 , C07D217/16 , C07D221/18 , C07D471/04 , C07D215/20
CPC分类号： C07D209/48 , C07D209/49 , C07D217/16 , C07D221/18 , C07D471/04
摘要： Compounds of the formula: ##STR1## wherein the symbols X each represent hydrogen or methoxy, R represents hydrogen or carboxymethyl, the symbols R.sub.1 each represent hydrogen or together represent a valency bond and the symbols R.sub.2 each represent hydrogen or together represent a valency bond, the pair of symbols R.sub.2 having the same significance as the pair of symbols R.sub.1, and when the symbols R.sub.1 and R.sub.2 represent hydrogen the symbol X also represents hydrogen, are new compounds possessing antiviral activity.
摘要翻译：其中符号X各自表示氢或甲氧基，R表示氢或羧甲基，符号R1各自表示氢或一起代表价键，符号R2各自表示氢或一起代表价键，该对符号R2具有与该对符号R1相同的含义，并且当符号R1和R2表示氢时，符号X也表示氢，是具有抗病毒活性的新化合物。

10. 发明授权

US4419356A 2,3,6,7-Tetrahydrothiazolo[3,2-a]pyrimidine derivatives having anti-rheumatic properties and pharmaceutical compositions containing them 失效
标题翻译：具有抗风湿性质的2,3,6,7-四氢噻唑并[3,2-a]嘧啶衍生物和含有它们的药物组合物
公开(公告)号：US4419356A
公开(公告)日：1983-12-06
申请号：US285845
申请日：1981-07-22
申请人： Francois Debarre , Jean-Louis Fabre , Daniel Farge , Claude James
发明人： Francois Debarre , Jean-Louis Fabre , Daniel Farge , Claude James
IPC分类号： C07D513/02 , A61K31/505 , A61K31/519 , A61P25/04 , A61P29/00 , A61P37/08 , C07D513/04
CPC分类号： C07D513/04 , Y10S514/825
摘要： Thiazolo[3,2-a]pyrimidine derivative of the formula: ##STR1## wherein R represents phenyl, alkyl of 1 through 4 carbon atoms, alkyl of 1 through 4 carbon atoms substituted by 1 through 3 halogen atom, alkenyl of 2 through 4 carbon atoms, or cycloalkyl of 3 through 6 carbon atoms and R.sub.1 represents hydrogen, or R and R.sub.1 each represent phenyl or unsubstituted alkyl of 1 through 4 carbon atoms, or R and R.sub.1 together represent an alkylene radical of 4 or 5 carbon atoms, and R.sub.2 and R.sub.3 each represent hydrogen or unsubstituted alkyl of 1 through 4 carbon atoms, or R and R.sub.1 each represent hydrogen, and one of R.sub.2 and R.sub.3 represents hydrogen and the other represents unsubstituted alkyl of 1 through 4 carbon atoms, or R.sub.2 and R.sub.3 both represent unsubstituted alkyl of 1 through 4 carbon atoms, are new compounds possessing pharmacological properties. They are especially useful in the treatment of rheumatic disease or allergic states, or as analgesics. Processes for the preparation of the compounds are described.
摘要翻译：具有下式的噻唑并[3,2-a]嘧啶衍生物，其中R表示苯基，1至4个碳原子的烷基，1至4个碳原子被1至3个卤素原子取代的烷基，2至4的烯基碳原子或3至6个碳原子的环烷基，R 1表示氢，或R和R 1各自表示1至4个碳原子的苯基或未取代的烷基，或R和R 1一起表示4或5个碳原子的亚烷基， R2和R3各自表示氢或1至4个碳原子的未取代的烷基，或R和R1各自表示氢，R2和R3之一表示氢，另一个表示1至4个碳原子的未取代烷基，或R2和R3均为表示1至4个碳原子的未取代烷基，是具有药理学性质的新化合物。它们特别适用于治疗风湿性疾病或过敏状态，或作为镇痛药。描述了制备化合物的方法。

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