Abstract:
Imidazoquinazoline derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, which have potent and selective inhibitory effects on cyclic guanosine-3',5'-monophosphate (cGMP)-specific phosphodiesterase and are useful in, for example, treating or relieving cardiovascular diseases such as thrombosis, angina pectoris, hypertension, cardiac insufficiency and arteriosclerosis, asthma, etc. and treating sexual impotence. In said formula, R represents hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted bicycloalkyl, optionally substituted tricycloalkyl, etc.; R represents hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted bicyclaolkyl, optionally substituted tricycloalkyl, optionally substituted lower alkenyl, optionally substituted aralkyl, etc.; R represents hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted bicycloalkyl, optionally substituted tricycloalkyl, optionally substituted lower alkenyl, optionally substituted aralkyl, etc., or R and R may form together with N an optionally substituted heterocyclic group; and X represents O or S.
Abstract translation:对通式(I)表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐,对环鸟嘌呤-3',5'-单磷酸(cGMP)特异性磷酸二酯酶具有有效和选择性的抑制作用,可用于例如治疗或缓解 心血管疾病如血栓形成,心绞痛,高血压,心功能不全和动脉硬化,哮喘等,并治疗性阳。。 在所述式中,R 1表示氢,任选取代的低级烷基,任选取代的环烷基,任选取代的双环烷基,任选取代的三环烷基等; R 2表示氢,任选取代的低级烷基,任选取代的环烷基,任选取代的双环烷基,任选取代的三环烷基,任选取代的低级烯基,任选取代的芳烷基等; R 3表示氢,任选取代的低级烷基,任选取代的环烷基,任选取代的双环烷基,任选取代的三环烷基,任选取代的低级链烯基,任选取代的芳烷基等,或R 2和R 3可与 N为任选取代的杂环基; X表示O或S.
Abstract:
Imidazoquinazoline derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R represents hydrogen, optionally substituted lower alkyl, etc.; R and R are the same or different and each represents hydrogen, optionally substituted lower alkyl, optionally substituted aralkyl, optionally substituted aryl, etc., or R and R together form an optionally substituted nitrogenous heterocycle; R represents hydrogen or optionally substituted lower alkyl; X represents O or S; Y represents a single bond or O; and n is 0, 1, 2 or 3.
Abstract translation:由通式(I)表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐,其中R 1表示氢,任选取代的低级烷基等; R 2和R 3相同或不同,各自表示氢,任选取代的低级烷基,任选取代的芳烷基,任选取代的芳基等,或R 2和R 3一起形成任选取代的 含氮杂环 R 4表示氢或任选取代的低级烷基; X表示O或S; Y表示单键或O; n为0,1,2或3。
Abstract:
An imidazoquinazoline derivative represented by formula (I) or a pharmacologically acceptable salt thereof, wherein R andR may be the same or different from each other and each represents hydrogen, lower alkyl, lower alkenyl, aryl, etc.; R represents hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aryl, etc.; and X represents O or S. This compound has a potent and selective cCMP-specific PDE inhibitor activity and is useful for treating or mitigating cardiovascular diseases such as thrombosis, angina pectoris, hypertension and arteriosclerosis, asthma, and so forth.
Abstract translation:由式(I)表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐,其中R 1和R 2可以相同或不同,各自代表氢,低级烷基,低级烯基,芳基等; R 3表示氢,低级烷基,环烷基,低级烯基,芳基等; X表示O或S.该化合物具有有效和选择性的cCMP特异性PDE抑制剂活性,可用于治疗或缓解心血管疾病如血栓形成,心绞痛,高血压和动脉硬化,哮喘等。
Abstract:
An endothelin-antagonizing peptide compound represented by general formula (I) and a pharmacologically acceptable salt thereof: R -R -R -R -R -R -R -R -R -R -R -R -Phe-R -R -R -R -R -Ile-R -Z wherein R is X -Gly, X (a), X -SCH2CO or hydrogen; R is Asn, Asp, Phe, Tyr, Ser or a single bond; R is Trp, Ile, Pro, Ala or a single bond; R is His, Lys, Gly, Trp, Ala or a single bond; R is Gly, Thr, Trp, Val or a single bond; R is Gly, Thr, Asn, Tyr, Asp or a single bond; R is Ala, Ser, Asn, Asp, Tyr, Phe or a single bond; R is Pro, Ala, Arg or a single bond; R is (b), (c) or a single bond; R is Trp or Ala; R is Val, Pro or a single bond; R is Tyr or a single bond; R is Ala, MeAla, Ser or Cys; R is His or Trp; R is Leu or Nva; R is Asp, Thr, Asn, Ser, Gly or Glu; R is Ile, Leu, Cha, Abu, Thi, Met, Tyr, MeLeu, MeIle, Phg or Nle; R is Trp, Phe or Tyr; and Z is hydroxy, lower alkoxy or amino.
Abstract translation:由通式(I)表示的内皮素拮抗肽化合物及其药理学上可接受的盐:R 1 -R 2 -R 3 -R 4 -R 5 -R 6 - [R <7> -R <8> -R <9> -R <10> -R <11> -R <12> -Phe-R <14> -R <15> -R <16> -R <17 其中R 1为X 1 -Gly,X 3(a),X 2 -SCH 2 CO或氢; R 2是Asn,Asp,Phe,Tyr,Ser或单键; R 3是Trp,Ile,Pro,Ala或单键; R 4是His,Lys,Gly,Trp,Ala或单键; R 5是Gly,Thr,Trp,Val或单键; R 6是Gly,Thr,Asn,Tyr,Asp或单键; R 7是Ala,Ser,Asn,Asp,Tyr,Phe或单键; Pro,Ala,Arg或单键; R 9为(b),(c)或单键; R 10是Trp或Ala; R 11是Val,Pro或单键; R 12是Tyr或单键; R 14是Ala,MeAla,Ser或Cys; R 15是His或Trp; R 16是Leu或Nva; R 17是Asp,Thr,Asn,Ser,Gly或Glu; R 18是Ile,Leu,Cha,Abu,Thi,Met,Tyr,MeLeu,MeIle,Phg或Nle; R 20是Trp,Phe或Tyr; Z为羟基,低级烷氧基或氨基。
Abstract:
Stable crystalline hydrate of (6R, 7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)-a cetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)-methyl-3-cephem-4 -carboxylate which is useful as an agent for treating diseases caused by bacterial infection is disclosed.
Abstract:
Commands such as installation operation and launch program commands need to be executed after appropriately switching between an administrator account and another account, for each command, when an installer constituting a program for readily performing installation operations collectively for a plurality of pieces of software or the like is launched. When an installer is launched in the present invention, process-to-process communication is secured between the processes of an administrator account and a user account, and an account to execute a command included in the installer is determined in the process of the administrator account. If the determination result indicates that the account to execute the command is the user account, the command is executed in the process of the user account rather than in the process of the administrator account.
Abstract:
Novel acridone compounds represented by general formula (I) or pharmacologically acceptable salts thereof efficacious in the prevention and treatment of diseases in which chemical transmitters (histamine, leukotriene, etc.) participate, typified by asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, digestive tract allergy, food allergy, etc., wherein R , R , R , R , R and R are the same or different and each represents hydrogen, hydroxy, halogeno, lower alkyl, cycloalkyl, lower alkoxy, etc.; Y represents -(CH2)t-(B)m-(CH2)-Z [wherein m is 0 or 1; t and n represent each an integer of from 0 to 6; B represents lower alkylene, optionally substituted arylene, etc.; and Z represents cyano, optionally protected carboxy, acyl or -NR R (wherein R and R are the same or different and each represents hydrogen, lower alkyl, lower alkoxy, hydroxyalkyl, etc.)]; and D represents oxygen or sulfur.
Abstract:
An acridone derivative represented by general formula (I) and a pharmacologically acceptable salt thereof, efficacious in preventing or treating deseases wherein histamine, leucotriene and the like participate and allergic diseases such as asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy, and food allergy, wherein R to R represent each hydrogen, lower alkyl, etc.; and n represents an integer of 1 to 6.
Abstract:
Commands such as installation operation and launch program commands need to be executed after appropriately switching between an administrator account and another account, for each command, when an installer constituting a program for readily performing installation operations collectively for a plurality of pieces of software or the like is launched. When an installer is launched in the present invention, process-to-process communication is secured between the processes of an administrator account and a user account, and an account to execute a command included in the installer is determined in the process of the administrator account. If the determination result indicates that the account to execute the command is the user account, the command is executed in the process of the user account rather than in the process of the administrator account.
Abstract:
The invention relates to a compound of a formula (I): , or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.