摘要:
A new compound of the formula: ##STR1## wherein ##STR2## is an optionally substituted benzene ring; R.sup.1 is a carbocyclic or heterocyclic group which is linked to the 4-position of the 1,3-benzoxazine ring through a carbon-carbon bond, a hydrocarbon residue, etc.; and R.sup.2 and R.sup.3 are independently a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group, etc., or a salt thereof is useful for treating and preventing heart, circulatory, respiratory and cerebral diseases.
摘要:
A method for producing optically active compounds is disclosed. The method is highly practical for producing optically active compounds useful for various utilities such as intermediates for synthesizing pharmaceutical agents, liquid crystal materials and agents for optical resolution.
摘要:
A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.
摘要翻译:下式的化合物:其中R 1为可被取代的烃基; R 2为可被取代的环状烃基或可被取代的杂环基; R 3为卤素原子 ,可以被取代的氨基甲酰基,可以被取代的氨磺酰基,可以被取代的酰基,可以被取代的C1-4烷基,可被取代的C1-4烷氧基,氨基 其可以被取代,硝基或氰基; R 4是氢原子或羟基; n是0或1; 和p为0或1至4];或其盐具有有效的CCR5拮抗活性,并且可有利地用作抑制人外周血单核细胞的HIV感染的药物,特别是用于治疗或预防AIDS。
摘要:
A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.
摘要:
A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y− (R5 is a hydrocarbon group; Y− is a counter anion); R3 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4 is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1 is a bond, CO or SO2; G2 is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3 aliphatic hydrocarbon which may be substituted; provided that J is methine when G2 is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1 is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).
摘要翻译:式(I)化合物(其中R 1为氢原子,可被取代的烃基,可被取代的非芳香族杂环基,R 2 O 2 >可以被取代的烃基,可以被取代的非芳族杂环基,或者R 1和R 2可以彼此结合形成A至 形成可以被取代的杂环基; A是N或N + - - - - - - - (R 5) SUP>为烃基; Y为 - 抗衡阴离子); R 3为可被取代的环状烃基或可被取代的杂环基; n 为0或1; R 4为氢原子,可被取代的烃基,可被取代的杂环基,可被取代的烷氧基,可被取代的芳氧基 ,或可以被取代的氨基,E是可以是二价脂族烃基 被除氧基以外的基团取代; G 1是一个键,CO或SO 2; G 2是CO,SO 2,NHCO,CONH或OCO; J为次甲基或氮原子; 并且Q和R中的每一个是可被取代的键或二价C 1-3烷基脂族烃; 条件是当G 2 O是OCO时J为次甲基,当另一个为键并且Q和R各自不被氧代基取代时,Q和R中的一个不为键, 当G 1是一个键时)或其盐具有强的CCR5拮抗活性,并且可以有利地用于治疗或预防人类各种HIV感染性疾病(如艾滋病)。
摘要:
The present invention provides a pharmaceutical composition having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism, tumor such as breast cancer and the like, more particularly, a steroid C17,20-lyase inhibitor containing a compound represented by the formula: wherein A1 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, one of A2 and A3 is a hydrogen atom, a halogen atom, a C1-4 aliphatic hydrocarbon group optionally having substituents or an optionally esterified carboxyl group, the other of A2 and A3 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, and at least one of A1, A2 and A3 is a 3-pyridyl group optionally having substituents, or a salt thereof or a prodrug thereof.
摘要:
A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.
摘要:
This document describes a novel and practically excellent process for the preparation of optically active compounds, such as optically active alcohols or amines which are useful for various applications, for example, as synthetic intermediates of pharmaceuticals, liquid crystal materials, and reagents for optical resolution, wherein a hydrogen transfer type asymmetric reduction is carried out in the presence of both a transition metal complex and an optically active nitrogen compound or a transition metal complex having an optically active nitrogen compounds as an asymmetric ligand, and a hydrogen-donating organic or inorganic compound.
摘要:
This invention pertains to a displacement detecting device for an optical head for detecting focal point displacement of irradiation light. The displacement detecting device has optical means for converting reflected rays from an irradiated face into an astigmatic bundle of rays and a photodetector for detecting a change in the the focused shape. The displacement detecting device thus detects focal point displacement of irradiation light. The optical means is obtained by integrally forming a plurality of Fresnel zone plates having rectilinear gratings, focusing reflected rays from the irradiated face, and having different focal lengths.
摘要:
A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.