摘要:
New perhydroinsoindole having the general formula (I) wherein R.sub.1 is optionally substituted phenyl or is cyclohexadienyl, naphtyl, indenyl or mono or polycyclic heterocyclyl, saturated or unsaturated 5 to 9C and optionally substituted, R.sub.2 is H or halogen, OH, alkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, alkyloxycarbonyl, dialkylaminoalcyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R.sub.3 is phenyl optionally substituted in position -2 by a radical alkyl or alkyloxy 1 or 2C or by OH or F, or disubstituted by CF.sub.3, and R.sub.4 is an alkyl radical containing 1 or 2C substituted by halogen or CN, N.sub.3 or --NHCN, and the radicals R which are similar or different represent H, alkyl or phenyl, in their isomer forms having the structure (Ia) or mixtures thereof, optionally their salts when they exist and preparation thereof. The new derivatives of the invention are particularly useful as antagonists of substance P.
摘要:
Perhydroisoindole derivatives of formula I, wherein the substituents are as defined in the specification, are particularly suitable as substance P antagonists. Several processes for preparing the compounds are also taught. ##STR1##
摘要:
This invention relates to derivatives of perhydroisoindol of formula: ##STR1## in which the radicals R are hydrogen atoms or together form a bond, the symbols R.sub.2 are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, R.sub.3 is a halogen atom or a hydroxy radical, R.sub.4 is H or halogen if R.sub.3 is halogen, in their isomer forms, or mixture thereof, and possibly also their salts when they exist, and preparation thereof. The derivatives of the invention are particularly interesting as P substance antagonist.
摘要:
This ivention relates to novel perhydroisoindole derivatives having formula (I), ##STR1## wherein the symbols R, which are the same or different, are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical, R' is a phenyl radical optionally 2-substituted by a C.sub.1-2 alkylk or alkyloxy radical, R" is a fluorine atom or a hydroxy radical, and R'" is a hydrogen atom, or else R' and R'" are hydroxy radicals, or R" and R'" together form a bond, and R.sup.o is a hydrogen atom or a protective radical; salts thereof whereever applicable; and preparation thereof. These products are synthetic intermediates for the preparation of derivatives having P substance antagonist activity.
摘要:
This invention relates to novel derivatives of thiopyranopyrrole of general formula (I): ##STR1## in which R is hydrogen, allyl, or a radical having the structure: --CR.sub.a R.sub.b R.sub.c where R.sub.a and R.sub.b are hydrogen atoms or phenyl radicals optionally substituted (by halogen, alkyl, alkyloxy or nitro), and R.sub.c is defined as R.sub.a and R.sub.b or stands for an alkyl or alkyloxyalkyl radical, at least one of R.sub.a, R.sub.b and R.sub.c being a substituted or unsubstituted phenyl radical, and n is 0 to 2, in their stereoisomer forms, and mixtures thereof, and possibly the salts if they exist, and preparation thereof. The novel derivatives of the invention are particularly interesting as synthesis intermediates.
摘要:
This invention relates to novel perhydroisoindole derivatives of general formula (I), ##STR1## wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; R.sub.3 is optionally 2-substituted phenyl; R.sub.4 is OH or fluorine when R.sub.5 is H, or R.sub.4 and R.sub.5 are OH or R.sub.4 and R.sub.5 together form a bond; isomeric forms and mixtures thereof; optionally salts thereof where applicable; and preparation thereof. The novel derivatives are particularly useful as P substance antagonists.
摘要:
This invention relates to derivatives of perhydroisoindol of formula: ##STR1## in which the radicals R are hydrogen atoms or together form a bond, the symbols R' are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, X is an oxygen atom or an NH radical, R.sub.1 is optionally substituted phenyl, or cyclohexadienyl, naphthyl, or heterocyclyl, R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R.sub.3 is halogen or OH and R.sub.4 is H or halogen if R.sub.3 is halogen, in their isomer forms, or mixture thereof, and possibly also their salts when they exist, and preparation thereof. The derivatives of the invention are particularly interesting as P substance antagonist.
摘要:
The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.
摘要:
The invention relates to compounds of formula (I): wherein Ra, R1, Ar, L, A, W, Y, and Z are as defined in the disclosure; to compositions containing them; and to the preparation and use thereof, in particular as anticancer agents.
摘要:
The invention relates to 4-substituted quinoline derivatives of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 represent >C—R′1 to >C—R′5 respectively, or alternatively at most one represents nitrogen, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 0, 1 or 2 and n is 0 or 1, R2 represents a radical R, —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CONH2, —CH2—CONH2, —CH2—CH2—CONH2, —CH2OH, —CH2—CH2OH, —CH2—NH2—CH2—CH2—NH2 or —CH2—CH2—CH2—NH2, R being as defined above, R3 represents phenyl, heteroaryl or alk-Ro3, where alk is alkyl and Ro3 represents various groups, where appropriate containing oxygen, sulfur or amine, in their enantiomeric or diastereoisomeric forms or their mixtures, and/or where appropriate in the syn or anti form or their mixtures, and their salts.
摘要翻译:本发明涉及以下通式的4-取代喹啉衍生物:其作为抗微生物剂是有活性的,其中:X 1,X 2,X 3 SUB >,X 4和X 5分别表示C-R 1至C-R'5 或者至多一个表示氮,Y表示CHR,CO,CROH,CRNH 2,CRF或CF 2,R为氢或烷基,m为0, 1或2,n为0或1,R 2表示基团R,-CO 2 R,-CH 2 CO 2, 2 R 2,-CH 2 -CH 2 CO 2 R 2,-CONH 2, - CH 2,-CO 2 H 2,-CH 2 CH 2,-CONH 2, ,-CH 2 OH,-CH 2 -CH 2 OH,-CH 2 -NH 2, 2个-CH 2 -CH 2 CH 2 -NH 2或-CH 2 -CH R 2如上所定义,R 3表示苯基,杂芳基或烷基-R(R 2) 其中烷基是烷基 和R 3表示各种基团,其中适当地含有它们的对映异构体或非对映异构形式或其混合物中的氧,硫或胺,和/或在合适的情况下在顺式或顺式 抗体形式或它们的混合物及其盐。