摘要:
This invention relates to novel heterocyclic carboxamide derivatives and salts thereof. More particularly, it relates to novel heterocyclic carboxamide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
摘要:
A compound of the formula: wherein R1 is amino or protected amino; R2 is hydrogen, lower alkyl or hydroxy protective group; R3 is carboxy or protected carboxy; R4 is an unsubstituted 5, 6 or 7-membered heteromonocyclic group containing two nitrogen atoms as heteroatoms, and which optionally further contains one oxygen or sulfur atom; or R4 is said 5, 6 or 7-membered heteromonocyclic group substituted by 1 to 4 groups selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino, cyclo(lower)alkyl, cyclo(lower)alkenyl, halogen, amino, protected amino, protected hydroxy, cyano, nitro, carboxy, hydroxy(lower)alkyl, amino(lower)alkyl, and carbamoyloxy; and n is 1 or 2.
摘要翻译:下式的化合物:其中R 1是氨基或被保护的氨基; R 2是氢,低级烷基或羟基保护基; R 3是羧基或被保护的羧基; R 4是未取代的5,6或7元杂单环基, 杂原子,并且任选地还含有一个氧或硫原子; 或R4是由1-4个选自低级烷基,低级烷氧基,低级烷硫基,低级烷基氨基,环(低级)烷基,环(低级)烯基,卤素 ,氨基,保护的氨基,保护的羟基,氰基,硝基,羧基,羟基(低级)烷基,氨基(低级)烷基和氨基甲酰氧基; andn是1或2。
摘要:
A steel composition particularly suitable for the manufacture of electric resistance welded pipes for use in most hostile environments and able to display excellent sour resistance and high toughness. The aluminum content of the steel composition is reduced to not more than 0.005%, while from 0.006 to 0.2% in total of one or both of titanium and zirconium is used instead for steel containing 0.0005 to 0.008% Ca. The steel, apart from iron and unavoidable impurities further contains:0.01 to 0.35% C0.02 to 0.5% Si0.1 to 1.8% Mnnot more than 0.015% P, andnot more than 0.003% SCu, Ni, Cr, Mo, Nb and V may be added in appropriate amounts to enhance the steel performance.
摘要:
This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
摘要:
This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
摘要:
A compound represented by the following general formula: ##STR1## which is useful as an intermediate for production of a clinically excellent synthetic antibacterial, a salt thereof, and a process for producing the same.In said formula,R.sup.1 is a hydrogen atom or a carboxyl-protecting group;R.sup.2 is a hydrogen atom or a lower alkyl group;X.sup.1 is a hydrogen atom or a halogen atom;X.sup.2 is a halogen atom;X.sub.a.sup.5 is a hydrogen atom or a halogen atom;A is a methylene group; a group of >CH--COOR.sup.4, etc.,in which R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom or a carboxyl-protecting group;B is a methylene group or a carbonyl group;provided that both A and B must not be methylene groups at the same time.
摘要:
Cephem compounds having the following formula are disclosed: ##STR1## R.sup.1 =amino or protected amino R.sup.2 =an organic group ##STR2## R.sup.6 =lower alkyl R.sup.7, R.sup.8 .dbd.OH or protected OHY.dbd.N or CHThe compounds are useful as antimicrobial agents.
摘要翻译:公开了具有下式的头孢烯化合物:R1 =氨基或被保护的氨基R2 =有机基团R6 =低级烷基R7,R8 = OH或受保护的OH Y = N或CH该化合物可用作抗微生物剂 。
摘要:
Cephem compounds of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,Z is N or CH,R.sup.2 is lower alkyl, mono(or di or tri)halo(lower)alkyl, lower alkenyl, lower alkynyl, phenyl, naphthyl, phenyl(lower)alkyl, carboxy(lower)alkyl or protected carboxy(lower)alkyl, andR is a group of the formula: ##STR2## in which R.sup.3 and R.sup.4 are each lower alkyl,A is lower alkylene, andR.sup.5 is hydroxy or a protected hydroxy group; or pharmaceutically acceptable salts thereof show antimicrobial activities and are useful in the treatment of microbial infections.
摘要:
The present invention relates to a compound of the formula (I) wherein R1 is optionally substituted aryl; R2 is optionally substituted aryl, optionally substituted heteroaryl, optionally substituted lower cycloalkyl, optionally substituted aryloxy, optionally substituted arylsulfonyl, vinyl, carbamoyl, protected carboxy or protected amino; ring A is bivalent residue derived from optionally substituted aryl or optionally substituted heteroaryl; X is bivalent residue derived from the group consisting of cycloalkene, naphthalene, unsaturated 5 or 6-membered heteromonocyclic group, each of which is optionally substituted, and substituted benzene; Y is -(A1)m1-(A2)m2-; and Z is direct bond or piperazine, or a salt thereof. The compound of the present invention and a salt thereof inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.
摘要:
Compounds of the formula: ##STR1## wherein R is a group of the formula: ##STR2## in which R.sup.3 and R.sup.4 are each lower alkyl or R.sup.3 and R.sup.4 are linked together to form C.sub.3 -C.sub.6 alkylene, A is lower alkylene, and R.sup.5 is hydroxy or a protected hydroxy group;or a group of the formula: ##STR3## in which R.sup.6 is lower alkyl, R.sup.7 and R.sup.8 are each hydroxy or a protected hydroxy group, and Y is N or CH, and salts thereof are intermediates for cephem compounds which show antimicrobial activities and which are useful in the treatment of microbial infections.