摘要:
The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.
摘要:
An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. (The symbols in the formula have the following meanings. (wherein
A: heteroarylene; X: bond, O, S, -NR 5 -, -NR 5 CO-, -NR 5 CONH-, -NR 5 SO 2 - or -NR 5 C(=NH)NH-; R 1 : -H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl; R 2a , R 2b : -H or -lower alkyl, which may be the same or different; R 3 : -H or -lower alkyl; R 4a , R 4b : -H or -OH, which may be the same different, or R 4a and R 4b are taken together to form =O or =N∼O-lower alkyl; and R 5 : -H or -lower alkyl.)
摘要翻译:由以下通式(I)表示的酰胺衍生物或其盐和含有酰胺衍生物和药学上可接受的载体的药物组合物。 (其中A:亚杂芳基; X:键,O,S,-NR 5 - ,-NR 5 CO - , - NR 5 CONH- ,-NR 5 SO 2 - 或-NR 5 C(= NH)NH-; R 1:-H, - 取代的低级烷基, - 取代的芳基, - 取代的杂芳基或 - 取代的环烷基 R 2a,R 2b:-H或 - 低级烷基,其可以相同或不同; R 3:-H或 - 低级烷基; R 4a,R 4b:-H 或-OH,其可以是相同的,或者R 4a和R 4b一起形成= O或= N型O-低级烷基;以及R 5:-H或 - 低级烷基。 )
摘要:
A quinuclidine derivative represented by general formula (I), a salt, N-oxide or quaternary ammonium salt thereof, and a medicinal composition containing the same, wherein the ring A represents optionally substituted aryl, cycloalkyl, cycloalkenyl, heteroaryl containing 1 to 4 heteroatoms selected from among oxygen, nitrogen and sulfur, or 5- to 7-membered saturated heterocycle; X represents a single bond or methylene; R represents halogeno, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, lower acyl, mercapto, lower alkylthio, sulfonyl, lower alkylsulfonyl, sulfinyl, lower alkylsulfinyl, sulfonamido, lower alkanesulfonamido, carbamoyl, thio-carbamoyl, mono- or di(lower alkyl)carbamoyl, nitro, cyano, amino, mono- or di(lower alkyl)amino, methylenedioxy, ethylenedioxy or lower alkyl optionally substituted by halogeno, hydroxy, lower alkoxy, amino or mono- or di(lower alkyl)amino; 1 is 0 or 1; m is an integer of 1 to 3; and n is an integer of 1 or 2. The compound has an antagonistic effect on muscarine M3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.
摘要:
Amide derivatives represented by general formula (I), or their salts and medicinal compositions containing these derivatives and pharmaceutically acceptable carriers, wherein each symbol has the following meaning: A: heteroarylene; X: a bond, O, S, -NR?5-, -NR5¿CO-, -NR5CONH-, -NR5SO2- or -NR5C(=NH)NH-; R1: H, optionally substituted lower aryl, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted cycloalkyl; R?2a and R2b¿: being the same or different from each other and each representing H or lower alkyl; R3: H or lower alkyl; R?4a and R4b¿: being the same or different from each other and each representing H or OH, or R?4a and R4b¿ forming together =O or =N~O-lower alkyl; and R5: H or lower alkyl. These compounds are useful as remedies for diabetes having an insulin secretion accelerating effect together with an insulin sensitivity increasing effect.
摘要:
Quinuclidine derivatives represented by general following general formula (I), salts, N-oxides or quaternary ammonium salts thereof, and medicinal compositions containing the same. The compound has an antagonistic effect on muscarinic M 3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.
摘要:
Carbamate derivatives represented by the general formula (I), salts thereof, hydrates thereof or solvates thereof wherein each symbol has the following meaning:
A ring: a benzene ring or a pyridine ring, B ring: a nitrogen-containing saturated hetero-ring which may have a substituent on the nitrogen atom and which may have a cross-linking, R 1 : a phenyl group which may have a substituent, a cycloalkyl or cycloalkenyl group having 3 to 8 carbon atoms or a five- or six-membered nitrogen-containing heterocyclic group, X: a single bond or a methylene group, Y: a single bond, a carbonyl group, a methylene group which may be substituted with a hydroxyl group or a group represented by the formula -S(O) ℓ -, and ℓ: an integer of 0, 1 or 2.
They have muscarinic M 3 receptor antagonism and are useful as an agent for the prevention and treatment of gastrointestinal diseases, respiratory diseases or urinary diseases.