Abstract:
The present invention relates to compounds with the formula (I), or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from the group consisting of (C1-C6)alkyl, -(CR3R4)t(C3-C12)cycloalkyl, -(CR3R4)t(C6-C12)aryl, and -(CR3R4)t(4-10)-membered heterocyclyl; b and k are each independently selected from 1 and 2; j is selected from the group consisting of 0, 1, and 2; t, u, p, q, and v are each independently selected from the group consisting of 0, 1, 2, 3, 4, and 5; T is a (6-10)-membered heterocyclyl containing at least one nitrogen atom; R2 is selected from the group consisting of H, (C1-C6)alkyl, -(CR3R4)t(C3-C12)cycloalkyl, -(CR3R4)t(C6-C12)aryl, and -(CR3R4)t(4-10)-membered heterocyclyl; each R3 and R4 is independently selected from H and (C1-C6)alkyl, the carbon atoms of T, R1, R2, R3 and R4 may each be optionally, substituted by I to 5 R5 groups; R5 is defined in the claims; The compounds of the present invention are 11 ß-hsd-1 inhibitors, and are therefore believed to be useful in the treatment of diabetes, obesity, glaucoma, osteoporosis, cognitive disorders, immune disorders, depression, hypertension, and metabolic diseases.
Abstract:
5-Amidino-2-hydroxybenzenesulfonamide derivatives represented by the following general formula [I] exhibiting a potent and selective inhibitory activity on activated blood coagulation factor X and thus being useful as preventives or remedies for diseases in the onset of which activated blood coagulation factor X participates: [I] wherein R1 represents optionally substituted lower alkyl, optionally substituted lower alkoxy, optionally substituted alkenyl, cycloalkyl, lower acyl, etc.; Q represents hydrogen or optionally substituted lower alkyl; and Z represents hydrogen, hydroxy, etc.; pharmacologically acceptable salts thereof, medicinal compositions containing the same and intermediates in the production thereof. These compounds are useful as preventives or remedies for various diseases such as brain infarction, cerebral thrombosis, cerebral embolism, TIA, cerebral vascular jerk, Alzheimer’s diseases, myocardial infarction, heart attack, heart failure, thrombosis, pulmonary infarction and pulmonary embolism.
Abstract:
The invention provides a compound of formula I: (F) wherein G, R2, R3, and R4 have any of the values defined in specification, or a pharmaceutically acceptable salt thereof, as well as processes and intermediates useful for preparing such compounds or salts, and methods of preventing or treating a herpesvirus infection using such compounds or salts.
Abstract:
Compounds represented by general formula (I) or salts thereof, a process for producing the same, and intermediates therefor, wherein R represents hydrogen or methyl; R1 represents hydrogen, halogeno, hydroxy, benzyloxy, amino, or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2NR4R4, or nitro; R6 represents hydrogen or lower alkyl; and X represents nitrogen, oxygen, sulfur, or methylene, provided that when X represents nitrogen, oxygen, or sulfur, then R9 represents hydrogen, one of R?7 and R8¿ represents hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy, and when X represents methylene, then R?7 and R8¿ each represents hydrogen and R9 represents hydrogen, amino, etc. They have a β-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc.
Abstract:
The invention provides compounds of formula (I), wherein R?1 and R2¿ independently represent H or C¿1-6? alkyl; R?3¿ represents phenyl substituted by at least one group selected form halo, CF¿3?, OCF3, CN, OH, C1-6 alkyl and C1-6 alkoxy; and R?4, R5 and R11¿ independently represent H or -(CH¿2?)n-A, wherein n represents 0, 1 or 2, provided that at least one of R?4, R5 and R11¿ is other than H; A represents CONR6R7 or SO¿2NR?6R7, wherein R?6 and R7¿ independently represent H, C¿3-6? cycloalkyl or C1-6 alkyl, the C?1-6¿ alkyl group being optionally substituted, in addition, R?6 and R7¿ may, together with the N atom to which they are attached, represent a ring which is optionally substituted; CO¿2R?8, wherein R8 represents H or C¿1-6? alkyl; NR?9R10¿, wherein R?9 and R10¿ independently represent H, C¿1-6? alkyl (optionally substituted), (C1-6 alkyl)SO2-, (C1-6 alkyl)CO-, H2NSO2- or H2NCO-; a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, which is optionally substituted; S(O)x(C1-6 alkyl), wherein x represents 0, 1 or 2; OH; CN, NO2; or C1-6 alkoxy which is optionally substituted; provided that when NR?1R2¿ represents N(H) methyl, R4 represents H and R3 represents 4- chlorophenyl, then R5 does not represent methoxy; and pharmaceutically acceptable salts thereof. The compounds of the invention are useful in the treatment or prevention of a variety of disorders, including those in which the regulation of monoamine transporter function is implicated.
Abstract translation:本发明提供式(I)化合物,其中R 1和R 2独立地表示H或C 1-6烷基; R 3表示被至少一个选自卤素,CF 3,OCF 3,CN,OH,C 1-6烷基和C 1-6烷氧基的基团取代的苯基; 和R 4,R 5和R 11独立地表示H或 - (CH 2)n A,其中n表示0,1或2,条件是R 4,R 5和 R 11不是H; A表示CONR 6 R 7或SO 2 NR 6 R 7,其中R 6和R 7独立地表示H,C 3-6环烷基或C 1-6烷基,C 1-6 >烷基任选被取代,此外,R 6和R 7可以与它们所连接的N原子一起代表任选被取代的环; CO 2 R 8,其中R 8表示H或C 1-6烷基; NR 9 R 10,其中R 9和R 10独立地表示H,C 1-6烷基(任选取代的),(C 1-6烷基)SO 2 - ,(C 1-6烷基)CO-, H2NSO2-或H2NCO-; 含有1,2或3个选自N,S和O的杂原子的5-或6-元杂环,其被任选取代; S(O)x(C 1-6烷基),其中x表示0,1或2; 哦; CN,NO2; 或任选取代的C 1-6烷氧基; 条件是当NR 1 R 2表示N(H)甲基时,R 4表示H且R 3表示4-氯苯基,则R 5不表示甲氧基; 及其药学上可接受的盐。 本发明的化合物可用于治疗或预防各种疾病,包括涉及单胺转运蛋白功能调节的疾病。
Abstract:
The invention concerns compounds of formula (I): R-A-R' wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R?1, R2, R3¿, v and R4 are as defined in the description; R' represents a -(CH¿2)t-R?5 group wherein t and R5 are as defined in the description.
Abstract:
The invention relates to compounds of formula (I) in which the symbols have the meanings given in the description. The compounds have excellent antiarrhythmic properties and comprise a cardioprotective component. The inventive compounds can preventively inhibit or strongly reduce the pathophysiological processes when ischaemic induced damages arise, especially during the onset of ischaemic induced cardiac arrhythmias. In addition, the inventive compounds have a strong inhibiting effect on the proliferation of cells.
Abstract:
3-Amidinoaniline derivatives represented by general formula (I) which have potent and selective activity of inhibiting activated blood coagulation factor X and are useful as activated blood coagulation factor X inhibitors, or pharmacologically acceptable salts thereof and intermediates in producing the same, wherein R represents hydrogen, lower alkyl, lower alkenyl, etc; R1 represents hydrogen, hydroxy, lower alkyl, etc.; Y represents a single bond or oxygen; and R2 represents lower alkyl or a group represented by (a) wherein n is 1 or 2; and T is hydrogen or -C(=NH)-W (wherein W is lower alkyl).