Abstract:
The present invention relates to compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R is hydrogen or methyl; R is hydrogen or methyl; R is (A) or (B) wherein X, W, Z, R , R , R , R and R are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.
Abstract translation:本发明涉及式(I)化合物,其中碳1和2通过单键或双键连接; R 1是氢或甲基; R 2是氢或甲基; R 3为(A)或(B)其中X,W,Z,R 4,R 5,R 6,R 7和R 8为各种基团, 溶剂化物及其用于治疗雄激素反应性和介导性疾病的用途。
Abstract:
The present invention relates to water soluble, camptothecin derivatives of formula (I), wherein: n represents the integer 1 or 2; and i) R represents: hydrogen, lower alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, amino lower alkyl, lower alkylamino lower alkyl, amino lower alkyl, lower alkoxy lower alkyl or (CH2)tAr wherein: t is 0 to 5 and Ar represents phenyl, furyl, pyridyl, N-methylpyrrolyl, imidazolyl; or phenyl, furyl, pyridyl, N-methylpyrrolyl, imidazolyl, with one or more substituents independently selected from hydroxy, methoxy, halogen, and amino; and R represents: diphenylmethyl or (CH2)tAr; or ii) R1 and R2 taken together with the linking nitrogen represent: N-tetrahydroquinolyl or N-tetrahydroisoquinolyl; and the pharmaceutically acceptable salts and solvates thereof, their use in the treatment of tumors and methods of their preparation.
Abstract:
Compounds of general formula (I) and physiologically acceptable salts thereof wherein the group NR1R2 represents a 5-7 membered saturated heterocyclic ring which may be substituted by one or two methyl groups; R3 is C1-6alkyl, C3-6cycloalkyl or phenyl optionally substituted by 1 or 2 halogen atoms; R4 is phenyl or phenyl substituted by one or two groups selected from halogen, C1-4alkyl, trifluoromethyl, trifluoromethoxy or (CH2)nR5 wherein n is zero or 1 and R5 represents C1-4alkoxy, hydroxy, nitro, cyano, CO2R6, S(O)pCH3, NR7R8, CONR7R8, SO2NR7CO(C1-4alkyl), tetrazolyl, carboxamidotetrazolyl, or a 3-trifluoromethyl 1,2,4-triazolyl; R6 is hydrogen, C1-4alkyl or benzyl; R7 is hydrogen or C1-4alkyl, R8 is hydrogen, C1-4alkyl, SO2CH3 or SO2CF3, X represents hydrogen, C1-4alkyl or halogen; m is zero, 1 or 2, and p is zero, 1 or 2; processes for their preparation and their use in medicine as antagonists of gastrin and CCK.
Abstract translation:通式(I)的化合物及其生理上可接受的盐,其中NR1R2基团可以被一个或两个甲基取代的5-7元饱和杂环; R3是C1-6烷基,C3-6环烷基或任选被1或2个卤素原子取代的苯基; R4是苯基或被一个或两个选自卤素,C 1-4烷基,三氟甲基,三氟甲氧基或(CH 2)n R 5基团取代的苯基,其中n是0或1,R 5代表C 1-4烷氧基,羟基,硝基,氰基,CO 2 R 6,S( O)pCH 3,NR 7 R 8,CONR 7 R 8,SO 2 NR 7 CO(C 1-4烷基),四唑基,羧酰胺基四唑基或3-三氟甲基-1,2,4-三唑基; R6是氢,C1-4烷基或苄基; R7是氢或C1-4烷基,R8是氢,C1-4烷基,SO2CH3或SO2CF3,X代表氢,C1-4烷基或卤素; m为零,1或2,p为零,1或2; 其制备方法及其在医学中的用途,作为胃泌素和CCK的拮抗剂。
Abstract:
The present invention relates to certain substituted 17 beta -substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) wherein R and R are: i) independently hydrogen or lower alkyl and the bond between the carbons bearing R and R is a single or a double bond, or ii) taken together are a -CH2- group to form a cyclopropane ring, and the bond between the carbons bearing R and R is a single bond; R is hydrogen; R is hydrogen, lower alkyl, lower cycloalkyl, lower alkenyl, alkanoyl of 2-6 carbons, -(CH2)mCO2R , -(CH2)mAr , -(CH2)n'CONR R , -(CH2)n'NR R or -(CH2)n'OR , wherein R is hydrogen, lower alkyl or lower alkenyl; R and R are independly hydrogen, lower alkyl lower cycloalkyl or lower alkenyl; Ar is an aromatic group of 6 to 12 carbons; n' is 0 or an integer from 1 to 5; m is an integer from 1 to 5; R and R are independently hydrogen or lower alkyl, or taken together R and R form a carbonyl group(=O); R is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, or NR R , wherein R and R are independently hydrogen, lower alkyl or lower alkenyl; and pharmaceutically acceptable salts thereof, their preparation, medical use and pharmaceutical formulations.
Abstract translation:本发明涉及式(I)的某些取代的17β-取代的羰基-6-氮杂雄甾-4-烯-3-酮,特别是其中R 1和R 1的式(I 1)的那些:i )独立地是氢或低级烷基,并且具有R 1和R 2的碳之间的键是单键或双键,或者ii)一起是-CH 2 - 基团以形成环丙烷环,并且键 在具有R 1和R 2的碳之间是单键; R 3c是氢; R 2是氢,低级烷基,低级环烷基,低级链烯基,2-6个碳原子的烷酰基, - (CH 2)m CO 2 R 16, - (CH 2)mAr a, - (CH 2)n CONR 17 R 18, - (CH 2)n R NR 17或 - (CH 2)n'OR 16,其中R 16是氢,低级烷基或低级烯基; R 17和R 18独立地是氢,低级烷基低级环烷基或低级烯基; Ar a是6〜12个碳的芳香族基团; n'为0或1〜5的整数; m为1〜5的整数; R 19和R 20独立地为氢或低级烷基,或一起R 19和R 20形成羰基(= O); R 5c是低级烷基,低级烯基,低级环烷基,低级烷氧基或NR 21 R 22,其中R 21和R 22独立地是氢,低级烷基或低级烯基; 及其药学上可接受的盐,它们的制备,医疗用途和药物制剂。
Abstract:
A sequential dosing medicament for topical treatment of fungal infections comprising a first pharmaceutical composition having an antifungal agent and an antiinflammatory agent, e.g. a steroid, a second separate pharmaceutical composition having only an antifungal agent as the active ingredient. Also, a method for such sequential dosing, particularly using oxiconazole as the antifungal agent and fluticasone as the steroid.
Abstract:
The present invention relates to the compound of formula (I), also known as 17 beta -N-(2,5-bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5 alpha -androst-1-en-3-one, solvates thereof, its preparation, intermediates used in its preparation, pharmaceutical formulations thereof and its use in the treatment of androgen responsive and mediated diseases.
Abstract:
The present invention relates to water soluble, camptothecin derivatives of formula (I), wherein A represents a moiety of formula (IIA), (IIB) or (IIC), X is selected from the group consisting of alkyl, aryl, (CH2)mOR1, (CH2)mSR1 and (CH¿2?)mNR?1R2¿ wherein m is an integer of 0 to 6, and R?1 and R2¿ are hydrogen, lower alkyl, aryl or together with the nitrogen form a 5-7 membered ring; q is an integer of 0 to 2; n represents the integer 1 or 2; p is an integer of 1 to 6; Y and W are selected from the group consisting of alkyl, aryl, alkoxy, aryloxy and amino, Q is oxygen or sulfur; P is phosphorus; J represents the atoms necessary to complete a 5 or 6 membered aromatic ring; and the pharmaceutically acceptable salts thereof; their use as topoisomerase inhibitors, their preparation; and their use in the treatment of cancer.
Abstract:
The present invention relates to certain substituted 17 beta -substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), wherein R and R i) are independently hydrogen or lower alkyl and the bond between the carbons bearing R and R is a single or a double bond, or ii) taken together are a -CH2- group forming a cyclopropane ring, and the bond between the carbons bearing R and R is a single bond; R is preferably hydrogen, halogen or lower alkyl, R is preferably hydrogen or lower alkyl, X is preferably CH2, Y is preferably hydrogen and Z is preferably CONR R and R and R are a variety of organic groups, and pharmaceutically acceptable salts thereof, preparation, medical use and pharmaceutical formulations.
Abstract translation:本发明涉及式(I)的某些取代的17β-取代的羰基-6-氮杂雄甾-4-烯-3-酮,其中R 1和R 2独立地是氢或低级烷基, 带有R 1和R 2的碳之间的键是单键或双键,或ii)一起形成环丙烷环的-CH 2 - 基团,并且具有R 1和 R 2是单键; R 3优选为氢,卤素或低级烷基,R 4优选为氢或低级烷基,X优选为CH 2,Y优选为氢,Z优选为CONR 14 R 15和R 14, 和R 15是各种有机基团及其药学上可接受的盐,制剂,医疗用途和药物制剂。
Abstract:
A medical capsule device (10) for releasing and/or collecting a substance at a defined location in the gastrointestinal tract. The device has a capsule body (12) defining one or more apertures in the circumferential wall thereof and a sleeve valve rotatably positioned therein having one or more corresponding apertures in the circumferential wall thereof. The sleeve valve comprises a coil and electrically connected heatable resistor which are operatively associated with an actuator member (16J, 16I) formed of a shape memory alloy responsive to heat and which will move from a non-heated first shape to a heated second shape. Actuator stop means (20) are provided in the capsule body for being engaged by the actuator member during movement from the non-heated first shape to the heated second shape so that the actuator member movement will serve to rotate the sleeve valve to either an open or closed position.
Abstract:
Aerosol formulations comprising an inhalation drug, 1,1,1,2-tetrafluoroethane (P134a) and a surface active agent soluble in 1,1,1,2-tetrafluoroethane.