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1. 发明专利

CA1192190A HETEROCYCLIC DERIVATIVES AS HISTAMINE H IN2- ANTAGONISTS 未知
公开(公告)号：CA1192190A
公开(公告)日：1985-08-20
申请号：CA407940
申请日：1982-07-23
申请人： GLAXO GROUP LTD
发明人： HAYES ROGER , BAYS DAVID E , MACKINNON JOHN W M
IPC分类号： C07C279/28 , C07D239/46 , C07D249/14 , C07D257/06 , C07D295/096 , C07D401/06 , C07D471/04 , C07D401/12 , C07D413/12 , C07D401/14
摘要： The invention relates to compounds of the general formula (I) (I) and physiclogically acceptable salts, hydrates and bioprecursors thereof, in which R1 represents hydrogen, C1-14 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, heteroaralkyl or alkyl substituted by cycloalkyl, hydroxy, alkoxy, amino, alkylamino or dialkylamino; and R2 represents hydrogen or C1-4 alkyl group; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom selected from oxygen or sulphur; Alk represents a straight or branched alkylene chain of 1 to 3 carbon atoms; Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1- and 3- or 1- and 4- positions: R5 represents hydrogen or acyl; n and m, which may be the same or different, are each 1 or 2; Z represents one of the groups or ?NHR8 continued where X represents NCN, NSO2Methyl, NSO2Phenyl or CHNO2; R8 represents alkyl; R3 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxy C2-6 alkyl, alkoxy C2-6 alkyl or C1-4 alkanoyloxy C2-6 alkyl; R7 represents hydrogen, alkyl, alkenyl, aralkyl, acyloxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aralkyloxyalkyl, or the group (CH2)qR5 where q is zero, 1, 2, 3, 4, 5 or 6 and the alkylene chain (CH2)q may be straight or branched, and R6 is hydroxy, alkoxy, nitro, heteroaryl, tetrahydropyranyloxy or CH2NHC(=X)NHR9 where X is as defined above, and R9 is alkyl; or R6 is the group NR10R11, where R10 is hydrogen or alkyl; and R11 is hydrogen, alkyl, alkenyl, aryl, aralkyl, or heteroaralkyl, or R11 is the group SO2R12 where R12 is alkyl or aryl; or R11 is the group COR13 where R13 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halomethyl, heteroaryl, heteroaralkyl or the group NHR14 where R14 is hydrogen, alkyl, cycloalkyl, aryl or aralkyl; or R10 and R11 together represent the group =CR15R16 where R15 represents aryl or heteroaryl and R16 represents hydrogen or alkyl; or R6 is the group SO2R17 in which R17 is hydroxy, alkyl, aryl or the group NR18R19 where R18 and R19, which may be the same or different, each represent hydrogen or alkyl; or R6 is the group COR20 where R20 is hydrogen, hydroxy, alkoxy, aryloxy, aralkyloxy, alkyl, aryl, aralkyl or the group NR21R22 where R21 is hydrogen or alkyl optionally substituted by a hydroxy or alkoxy group; and R22 is hydrogen, alkyl (optionally substituted continued by a hydroxy or alkoxy group), alkenyl, aryl, aralkyl or cycloalkyl, or NR21R22 forms a 5 to 8 membered ring which may contain another heteroatom, e.g. oxygen, or a double bond and/or may be substituted by hydroxy or one or two C1-3 alkyl groups; or R6 is the group CR23=NR24 where R23 is hydrogen, alkyl, aryl or aralkyl and R24 is hydroxy, alkoxy, aralkyloxy or -NHC(=Y)NH2 where Y is oxygen or sulphur; with the proviso that when the group R6 contains a carbon atom through which it is linked to the alkylene group (CH2)q then the total number of carbon atoms in the resulting chain is not greater than 6 (i.e. g is not greater than 5); R4 represents phenyl, phenoxy or pyridinyl which may optionally be substituted by one or more halogen, alkyl, alkoxyalkyl or alkoxy groups or by a methylenedioxy group; p represents an integer which is 1, 2 or 3; the compounds show pharmacological activity as selective histamine H2-antagonists.

2. 发明专利

CA1189508A HETEROCYCLIC DERIVATIVES AS HISTAMINE H.SUB.2- ANTAGONISTS 未知
公开(公告)号：CA1189508A
公开(公告)日：1985-06-25
申请号：CA407949
申请日：1982-07-23
申请人： GLAXO GROUP LTD
发明人： HAYES ROGER , BAYS DAVID E , MACKINNON JOHN W M , CAREY LINDA , BLATCHER PHILIP
IPC分类号： C07C279/28 , C07D239/46 , C07D249/14 , C07D257/06 , C07D295/096 , C07D471/04
摘要： The invention relates to compounds of the general formula (I) (I) and physiologically acceptable salts, hydrates and bioprecursors thereof, in which R1 represents hydrogens, C1-14 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, heteroaralkyl or alkyl substituted by cycloalkyl, hydroxy, alkoxy, amino, alkylamino or dialkylamino; and R2 represents hydrogen or C1-4 alkyl group; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom selected from oxygen or sulphur: Alk represents a straight or branched alkylene chain of l to 3 carbon atoms; Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1and 3- or 1- and 4- positions: R5 represents hydrogen or acyl; n and m, which may be the same or different, are each 1 or 2; R3 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxy C2-6 alkyl, alkoxy C2-6 alkyl or C1-4 alkanoyloxy C2-6 alkyl; and R7 represents hydrogen, alkyl, alkenyl, aralkyl, acyloxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aralkyloxyalkyl, or the group (CH2)qR6 where q is zero, 1, 2, 3, 4, 5 or 6 and the alkylene chain (CH2)q may be straight or branched, and R6 is hydroxy, alkoxy, nitro, heteroaryl, tetrahydropyranyloxy or CH2NHC(=X)NHR9 where X represents NCN, continued... NSO2 Methyl, NSO2 Phenyl or CHNO2 and R9 is alkyl; or R6 is the group NR10R11, where R10 is hydrogen or alkyl; and R11 is hydrogen, alkyl, alkenyl, aryl, aralkyl, or heteroaralkyl, or R11 is the group SO2R12 where R12 is alkyl or aryl; or R11 is the group COR13 where R13 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halomethyl, heteroaryl, heteroaralkyl or the group NHR14 where R14 is hydrogen, alkyl, cycloalkylr aryl or aralkyl; or R10 and R11 together represent the group =CR15R16 where R15 represents aryl or heteroaryl and R16 represents hydrogen or alkyl; or R6 is the group SO2R17 in which R17 is hydroxy, alkyl, aryl or the group NR18R19 where R18 and R19, which may be the same or different, each represent hydrogen or alkyl; or R6 is the group COR20 where R20 is hydrogen, hydroxy, alkoxy, aryloxy, aralkyloxy, alkyl, aryl, aralkyl or the group NR21R22 where R21 is hydrogen or alkyl optionally substituted by a hydroxy or alkoxy group; and R22 is hydrogen, alkyl (optionally substituted by a hydroxy or alkoxy group), alkenyl, aryl, aralkyl or cycloalkyl, or NR21R22 forms a 5 to 8 membered ring which may contain another heteroatom, e.g. oxygen, or a double bond and/or may be substituted by hydroxy or one or two C1-3 alkyl groups or R6 is the group CR23=NR24 where R23 is hydrogen, alkyl, aryl or aralkyl and R24 is hydroxy, alkoxy, aralkyloxy or -NHC(=Y)NH2 where Y is oxygen or sulphur; or when A represents CR7 and B represents N, the groups R3 and R7 taken together represent or -(CH2)4-; with the proviso that when the group R6 contains a carbon atom through which it is linked to the alkylene group (CH2)q then the total number of carbon atoms in the resulting chain is not greater than 6 (i.e. q is not greater than 5). The compounds show pharmacological activity as selective histamine H2-antagonists.

3. 发明专利

CA1169428A INDOLE DERIVATIVES 未知
公开(公告)号：CA1169428A
公开(公告)日：1984-06-19
申请号：CA383670
申请日：1981-08-12
申请人： GLAXO GROUP LTD
发明人： BAYS DAVID E , WEBB COLIN F , DOWLE MICHAEL D
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , A61P25/04 , C07D209/16 , C07D209/18 , C07D209/48 , C07D401/06 , C07D403/06
摘要： Compounds are disclosed of general formula (I) wherein R1, R3, R4, R6 and R7, which may be the same or different, each represents a hydrogen atom or an alkyl group; R2 represents a hydrogen atom or an alkyl, aryl, aralkyl, cycloalkyl or alkenyl qroup; or R1 and R2, together with the nitrogen atom to which they are attached, form a saturated monocyclic 5 to 7-membered ring which may optionally contain a further hetero function; R5 represents a hydrogen atom or an alkyl or alkenyl group; or R4 and R5 together form an aralkylidene group; Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C1-3 alkyl groups; and X represents an oxygen or sulphur atom; and physiologically acceptable salts, solvates and bioprecursors thereof. The compounds are described as potentially useful for the treatment of migraine and may be formulated as pharmaceutical compositions in conventional manner using one or more pharmaceutically acceptable carriers or excipients. Various processes for the preparation of the compounds are disclosed including, for example, a process involving reacting an indole having an appropriate nitrile group at the 5-position, with a suitable oxygenor sulphur-containing compound in order to introduce the required amide or thioamide group at the 5position on the indole nucleus.

4. 发明专利

CA2041175A1 CARBOXYLIC ACID DERIVATIVES 未知
公开(公告)号：CA2041175A1
公开(公告)日：1991-10-27
申请号：CA2041175
申请日：1991-04-25
申请人： GLAXO GROUP LTD
发明人： COLLINGTON ERIC W , CLITHEROW JOHN W , BAYS DAVID E
IPC分类号： A61K31/34 , A61K31/341 , A61K31/555 , A61P1/00 , A61P1/04 , A61P31/04 , C07C59/255 , C07C59/265 , C07D307/52 , C07D405/06 , C07D405/12 , C07F9/94 , C07D307/38 , A61K31/41
摘要： CARBOXYLIC ACID DERIVATIVES The invention relates to a salt of a basic histamine H2-receptor antagonist of formula (I) (I) and a complex of bismuth with a carboxylic acid selected from tartaric acid, citric acid and alkyl citric acids, or a solvate of such a salt, wherein R1 represents a group of formula or where R3 represents methyl or the group (CH2)2CONR4R5 in which R4 and R5 both represent ethyl groups; R2 represents a hydrogen atom or, when R1 is the group -C(=CHNO2)NHCH3, R2 may also represent a methyl group; and n is 3 and X is oxygen, or n is 2 and X is CH2 or sulphur; with the provisos that (i) when R1 represents 6877/ABS or then X is sulphur and n is 2; (ii) when R1 represents -C(=CHNO2)NHCH3 and R2 is hydrogen, then X is oxygen and n is 3 or X is CH2 and n is 2; and (iii) when R1 represents -C(=CHNO2)NHCH3 and R2 is methyl, then X is oxygen and n is 3 or X is sulphur and n is 2. The salts and solvates thereof are useful in the treatment of gastro-intestinal disorders, such as peptic ulcer disease, gastritis and non-ulcer dyspepsia. 6877/ABS

5. 发明专利

CA1169077A INDOLE DERIVATIVES 未知
公开(公告)号：CA1169077A
公开(公告)日：1984-06-12
申请号：CA383717
申请日：1981-08-12
申请人： GLAXO GROUP LTD
发明人： COATES IAN H , MILLS KEITH , WEBB COLIN F , DOWLE MICHAEL D , BAYS DAVID E
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61P9/00 , A61P25/04 , C07D209/16 , C07D209/48 , C07D471/04 , C07D403/06
摘要： Compounds are disclosed of general formula (I) (I) wherein R1 represents a group CHO, COR8, CO2R8, CONR9R10, CSNR9R10 or SO2NR9R10, where R8 represents an alkyl, cycloalkyl, aryl or aralkyl group, R9 represents a hydrogen atom or an alkyl group, and R10 represents a hydrogen atom or an alkyl, cycloalkyl, aryl or aralkyl group; R2, R3, R4, R6 and R7, which may be the same or different, each represents a hydrogen atom or a C1-3 alkyl group; R5 represents a hydrogen atom or an alkyl, cycloalkyl, alkenyl or an aralkyl group or R4 and R5 together form an aralkylidene group or R4 and R5 together with the nitrogen atom to which they are attached form a saturated monocyclic 5- to 7-membered ring; and Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C1-3 alkyl groups; continued... and physiologically acceptable salts, solvates and bioprecursors thereof. The compounds are described as potentially useful for the treatment of migraine and may be formulated as pharmaceutical compositions in conventional manner using one or more pharmaceutically acceptable carriers or excipients. Various processes for the preparation of the compounds are disclosed including, for example, reaction of an aminoalkyl indole with an acid of formula R1OH or an acylating agent corresponding thereto or with an inorganic cyanate or an organic isocyanate or isothiocyanate in order to introduce the desired R1 group at the 5-position on the indole nucleus.

6. 发明专利

CA1158649A SUBSTITUTED AMINO TRIAZOLES 未知
公开(公告)号：CA1158649A
公开(公告)日：1983-12-13
申请号：CA371889
申请日：1981-02-27
申请人： GLAXO GROUP LTD
发明人： CLITHEROW JOHN W , BRADSHAW JOHN , MACKINNON JOHN W M , JUDD DUNCAN B , BAYS DAVID E , HAYES ROGER , PEARCE ANDREW
IPC分类号： C07D249/00 , A61K31/41 , A61K31/4402 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P1/04 , A61P29/00 , A61P43/00 , C07D209/48 , C07D213/86 , C07D249/08 , C07D249/10 , C07D249/14 , C07D333/20 , C07D333/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D403/12
摘要： - A1 The invention provides compounds of the general formula (I) (I) and physiologically acceptable salts, hydrates and bioprecursors thereof, in which R1 represents hydrogen, C1-14 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, heteroaralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl; and R2 represents hydrogen or C1-4 alkyl; or R1 and R2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C1-3 alkyl groups or a hydroxy group and/ or may contain another heteroatom selected from oxygen or sulphur; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms, Q represents a furan or thiophon ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5- positions, the furan or thiophen ring optionally bearing a further substituent R5 adjacent to the group R1R2N-Alk-; or Q represents a thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2- and 4- positions, the thiophen ring optionally bearing a further substituent R5 adjacent to the group R1R2NAlk with the proviso that where the group R1R2NAlk is in the 4- position then the group R5 is in the 5- position; or Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1- and 3- or 1- and 4- positions; R5 represents halogen or C1-4 alkyl which may be - A2 substituted by hydroxy or C1-4 alkoxy; X represents oxygen, sulphur, -NH-, methylene or a bond; Y represents oxygen, sulphur, methylene or a bond n represents zero, 1, 2 or 3, and m is an integer from 2 to 5, with the provisos that (a) the total number of atoms in the chain X(CH2)nY(CH2)m is an integer from 3 to 8, (b) when X and Y represent oxygen or sulphur then n is 2 or 3, and (c) when X represents -NH- then Q is a benzene ring and Y represents methylene or a bond; R3 represents hydrogen, alkyl, alkenyl, aralkyl, or C2-6 alkyl substituted by hydroxy or alkoxy; R4 represents the group (CH2)pCH=CHR6 or (CH2)qR7 where p is zero, 1, or 2 and q is zero, 1,2, 3, 4, 5 or 6 and the alkylene chain (CH2)q may be straight or branched, and R6 is hydroxymethyl, 1H-tetrazol-5-yl, cyano, or the group CH2NHCOR17 or CH2NHSO2R17 where R17 is alkyl; or the group COR19 where R19 is hydrogen, hydroxyl, alkyl, alkoxy, amino, alkylamino or dialkylamino; or the group CRa19 = NR20 where Ra19 is hydrogen or alkyl and R20 is hydroxy, alkoxy, aralkyloxy or -NHC(=A)NH2 where A is oxygen or sulphur; R7 is nitro, cyano, halomethyl, heteroaryl, arylaminomethyl, aralkylaminomethyl, alkylthioalkyl, arylthioalkyl, 1H-tetrazol-5-yl, aryl CH = NCH2- or CH2NHC(=B)NHR17 where B is NCN, NSO2methyl,NSO2Phenyl or CHNO2; or R7 is the group SO2R8 in which R8 is hydroxy, alkyl, aryl or the group NR9R10 wherc R9 and R10 are the same or different and represent hydrogen, alkyl, aryl or aralkyl; or R7 is the group COR11 where R11 is hydrogen, hydroxy, alkoxy, aryloxy, aralkyloxy, alkyl, aryl, aralkyl or the group NR12R13 where R12 is hydrogen or alkyl optionally substituted by a hydroxy or alkoxy group, and R13 is hydrogen. alkyl (optionally substituted by a hydroxy or alkoxy group), alkenyl, aryl, aralkyl or -A3 cycloalkyl, or NR12R13 forms a 5 to 8 membered ring which may contain another heteroatom e.g. oxygen, or a double bond and/or may be substituted by hydroxy or one or two C1-3 alkyl (e.g. methyl) groups; or R7 is the group CRa11 = NR20 where Ra11 is hydrogen, alkyl, aryl or arlkyl and R20 is as defined above; or R7 is the group CH2NR18SO2R14 where R14 is alkyl or aryl and R18 is hydrogen or alkyl; or R7 is the group CH2NR18COR15 where R15 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halomethyl, or the group NHR16 where R16 is hydrogen, alkyl, cycloalkyl, aryl or aralkyl; with the proviso that when the group R7 contains a carbon atom through which it is linked to the alkylene group (CH2)q then the total number of carbon atoms in the resulting chain is not greater than 6 (i.e. q is not greater than 5). The compounds show pharmaceutical activity as selective histamine H2-antagonists.

7. 发明专利

CA2011107A1 LACTAM DERIVATIVES 未知
公开(公告)号：CA2011107A1
公开(公告)日：1991-08-31
申请号：CA2011107
申请日：1990-02-28
申请人： GLAXO GROUP LTD
发明人： BAYS DAVID E , COATES IAN H , OXFORD ALEXANDER W , NORTH PETER C
IPC分类号： A61K31/475 , A61K31/535 , C07D471/16 , C07D498/16 , C07D513/16
摘要： LACTAM DERIVATIVES The invention provides lactam derivatives of the general formula (I) (I) wherein n represents 2 or 3; Im represents an imidazolyl group of the formula : or wherein one of the groups represented by R1, R2 and R3 is a hydrogen atom or a C1-6alkyl, C3-7cycloalkyl, C3-6alkenyl, phenyl or phenylC1-3alkyl- group, and each of the other two groups, which may be the same of different, represents a hydrogen atom or a C1-6alkyl group: Y represents a group -(CH2)m-, wherein m represents 2, 3 or 4; or Y represents a group -X(CH2)p-, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR4, where R4 is a C1-6alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof. The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT3 receptors and are useful, for example in the treatment of psychotic disorders, anxiety and nausea and vomiting.

8. 发明专利

CA1281334C INDOLE DERIVATIVES 未知
公开(公告)号：CA1281334C
公开(公告)日：1991-03-12
申请号：CA525059
申请日：1986-12-11
申请人： GLAXO GROUP LTD
发明人： OXFORD ALEXANDER W , BAYS DAVID E , COATES IAN H , WEBB COLIN F
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , A61P25/04 , C07D209/16 , C07D209/20
摘要： Indoles are disclosed of formula (I): (I) wherein R1 represents R5R6NCOCH2-, R5CONH(CH2)p-, R5R6NSO2(CH2)p- or R7SO2NH(CH2)p-, (where R5 and R6 each represents a hydrogen atom or a C1-3 alkyl group, R7 represents C1-3 alkyl and p is zero or one), R2 is hydrogen or C1-3 alkyl; R3 and R4 each represents hydrogen atom, C1-3 alkyl, or 2-propenyl; m is zero or an integer from 1 to 4; and n is an integer from 2 to 5; and physiologically acceptable salts and solvates (e.g. hydrates) thereof. The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. They may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers or excipients for administration by any convenient route. Various methods for the preparation of the compounds (I) are disclosed.

9. 发明专利

CA1192545A HETEROCYCLIC DERIVATIVES AS HISTAMINE H.SUB.2- ANTAGONISTS 未知
公开(公告)号：CA1192545A
公开(公告)日：1985-08-27
申请号：CA407958
申请日：1982-07-23
申请人： GLAXO GROUP LTD
发明人： HAYES ROGER , BAYS DAVID E , MACKINNON JOHN W M , CAREY LINDA
IPC分类号： C07C279/28 , C07D239/46 , C07D249/14 , C07D257/06 , C07D295/096 , C07D471/04 , C07D401/12 , C07D413/12
摘要： The invention relates to compounds of the general formula (I) and physiologically acceptable salts, hydrates and bioprecursors thereof, in which R1 represents hydrogen, C1-14 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, heteroaralkyl or alkyl substituted by cycloalkyl, hydroxy, alkoxy, amino, alkylamino or dialkylamino; and R2 represents hydrogen or C1-4 alkyl group; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom selected from oxygen or sulphur; Alk represents a straight or branched alkylene chain of 1 to 3 carbon atoms; Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1and 3- or 1- and 4- positions; R5 represents hydrogen or acyl; n and m, which may be the same or different; are each 1 or 2; and R3 represents hydrogen, alkyl, alkenyl, aralky ? hydroxy C2-6 alkyl, alkoxy C2-6 alkyl or C1-4 alkanoyloxy C2-6 alkyl The compounds show pharmacological activity as selective histamine H2-antagonists.

10. 发明专利

CA1169429A INDOLE DERIVATIVES 未知
公开(公告)号：CA1169429A
公开(公告)日：1984-06-19
申请号：CA383718
申请日：1981-08-12
申请人： GLAXO GROUP LTD
发明人： COATES IAN H , MILLS KEITH , WEBB COLIN F , DOWLE MICHAEL D , BAYS DAVID E
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61P9/00 , A61P25/04 , C07D209/16 , C07D209/48 , C07D471/04 , C07D403/06
摘要： Title: HETEROCYCLIC COMPOUNDS Compounds are disclosed of general formula (I) (I) wherein R1 repr nts an alkyl, cycloalkyl, aryl or ar group; R2, R3, R4, R6 and R7, which may be the same or different, each represents a hydrogen atom or a C1-3 alkyl group; R5 represents a hydrogen atom or an alkyl, cycloalkyl, alkenyl or an aralkyl group; or R4 and R5 together form an aralkylidene group or R4 and R5 together with the nitrogen atom to which they are attached form a saturated monocyclic 5- to 7-membered ring; Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C1-3 alkyl groups; and physiologically acceptable salts, solvates and bioprecurosors thereof. The compounds are described as potentially useful for the treatment of migraine and may be formulated as pharmacetuical compositions in conventional manner using one or more pharmaceutically acceptable carriers or excipients, Various processes for the preparation of the compounds are disclosed including, for example, a process involving reaction of an aminoalkyl indole with a sulphonylating agent in order to introduce the -SO2- group at the 5-position on the indole nucleus.

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