Abstract: Novel substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines useful as anti-depressives, in the treatment of Parkinson's disease and in the treatment of diseases related with disturbed enterokinesia.
Type:
Grant
Filed:
February 16, 1988
Date of Patent:
May 2, 1989
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Frans E. Janssens, Theophilus T. J. M. Van Offenwert, Raymond A. Stokbroekx, Bernard R. Boar
Abstract: Novel N-(bicyclic heterocyclyl)-4-piperidinamines having anti-histaminic and serotonin-antagonistic properties which are useful in the treatment of allergic diseases.
Type:
Grant
Filed:
November 2, 1987
Date of Patent:
April 11, 1989
Assignee:
Janssen Pharmaceutica
Inventors:
Frans E. Janssens, Joseph L. G. Torremans, Jozef F. Hens, Theophilus T. J. M. Van Offenwert
Abstract: Compounds useful as antihypertensive agents which are 3-aminoalkyl-1H-indole-5-urea or amide derivatives having the following formula: ##STR1## or a pharmaceutically acceptable acid addition salts thereof, wherein: R is C.sub.1-4 loweralkyl, C.sub.1-4 loweralkoxy, phenyl, ##STR2## pyrrolyl, pyridyl or is a substituted nitrogen represented by: ##STR3## wherein R.sub.1 is H or a C.sub.1-4 loweralkyl or phenyl or cycloalkyl; R.sub.2 is H or a C.sub.1-4 loweralkyl; Y is H or halo; R.sub.3 is H or a C.sub.1-4 loweralkyl; R.sub.4 is H or a C.sub.1-4 loweralkyl; R.sub.5 is H or a C.sub.1-4 loweralkyl or carboxymethyl or carboxytrifluoromethyl; R.sub.6 is H or a C.sub.1-4 loweralkyl, and R.sub.5 and R.sub.6 may also be taken together as an N-loweralkyl-pyrrolidinylidene group.
Abstract: Hexahydropyrrolizines of the formula (I): ##STR1## wherein A is a 3-7 carbon or hetero-containing ring,R.sup.1 is a substituent, andx is 0-3.Also, pharmaceutical compositions for treating pain and methods for synthesis and use as well as novel intermediates in the synthesis.
Abstract: A method for the synthesis of the 2-propanone (I) is described starting from alkoxide (II) through the lactone (IV). ##STR1## Excellent control of the location of the substitution on the phenyl ring is achieved and the reaction proceeds in high yield.
Type:
Grant
Filed:
September 21, 1987
Date of Patent:
January 17, 1989
Assignee:
McNeilab, Inc.
Inventors:
David A. Cherry, Cynthia A. Maryanoff, John E. Mills, Roy A. Olofson, James D. Rodgers
Abstract: Sulfamates of the following formula (I) are anticonvulsants and are useful in the treatment of epilepsy: ##STR1## wherein R is one or more substituents such as alkyl, halo, alkoxy, CH.sub.3 or nitro; andx is 0-3.
Abstract: Alkenes of the formula (I) and epoxides (II) used to make them are useful as anti-inflammatory and antiallergic pharmaceuticals: ##STR1## wherein R.sup.1 =H or CH.sub.3 ; R.sup.2 =phenyl, substituted phenyl, benzyl or a cysteinyl moiety; R.sup.4 and R.sup.5 =alkyl; n=O or 1; and R.sup.3 is as described.
Abstract: An efficient synthesis of quanidines, e.g. of the formula (III), by oxidizing a thiourea, e.g. of the following formula (II): ##STR1## with H.sub.2 O.sub.2 and a molybdenum catalyst to yield an aminoiminomethane sulfonic acid which can then be reacted with an amine followed by optional transamination steps.
Type:
Grant
Filed:
November 24, 1986
Date of Patent:
November 1, 1988
Assignee:
McNeilab, Inc.
Inventors:
Cynthia A. Maryanoff, James N. Plampin, Robin C. Stanzione
Abstract: A method for synthesizing a tri-substituted phenyl compound (I) by using a 1,2-addition followed by a 1,4-addition to 1,4-benzoquinone (II): ##STR1## wherein X is hydroxy, alkoxy or alkanoyloxy, Ar.sup.1 is an organic group and R is an unsubstituted or substituted alkyl group.
Type:
Grant
Filed:
March 19, 1987
Date of Patent:
September 20, 1988
Assignee:
McNeilab, Inc.
Inventors:
Dennis C. Liotta, Cynthia A. Maryanoff, Vasken Paragamian
Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine and B is an aromatic heterocycle, aromatic carbocycle or saturated carbocycle.
Abstract: Novel substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines useful as anti-depressives, in the treatment of Parkinson's disease and in the treatment of diseases related with disturbed enterokinesia.
Type:
Grant
Filed:
June 23, 1987
Date of Patent:
June 7, 1988
Assignee:
Janssen Pharmaceutica N. V.
Inventors:
Frans E. Janssens, Theophilus T. J. M. Van Offenwert, Raymond A. Stokbroekx, Bernard R. Boar
Abstract: Novel D-arabinose-1,5-diphosphate salts of the formula (I): ##STR1## wherein n is from about 3 to 4 and M.sup.+ is a cation as well as racemic and isomeric mixtures of the so-defined and forms of formula (I) are useful as hypoglycemic agents for the treatment of diabetes, e.g., in man.
Abstract: A process to prepare retinoyl chlorides, e.g., of the following formula (I): ##STR1## under very mild chlorinating conditions by the action of a reagent amount of dimethylchloroformamidinium chloride on a corresponding retinoic acid.
Abstract: Acetylenes of the formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, q, Alk, R.sup.3 n and R.sup.4 are as defined herein and Ar.sup.1 and Ar.sup.2 are aromatic, including the salts and ammonium derivatives of formula (I), in treating angina, hypertension and cardiac arrhythmias. Pharmaceutical compositions, methods of use and synthesis and novel intermediates are also part of the invention.
Abstract: Four decapeptides found to be analgesics and have antagonist activity to Neurokinin B which is also known as Neuromedin K. The decapeptide are of the following formula (I):A.sup.1 -D-Pro.sup.2 His.sup.3 -D.sup.4 Phe.sup.5 D-Trp.sup.6 Val.sup.7 -D-Trp.sup.8 -Leu.sup.9 -Nle.sup.10 -NH.sub.2 (I)wherein A.sup.1 and D.sup.4 are Asp or D-Asp amino acids. Also described is an opthalmic solution to treat pain or inflammation and an HPLC separation method using piperidine.
Abstract: Dihydropyridine compounds having 1,4,4-trisubstitution of the following formula (I): ##STR1## wherein R is one of --COR.sup.3, R.sup.3 being a group such as phenyl or benzyl; R.sup.4 where R.sup.4 is a heterocycle; --(CH.sub.2).sub.n NR.sup.5 R.sup.6, with R.sup.5 and R.sup.6 being alkyl or joined to define a ring; or --(CH.sub.2).sub.n COOR.sup.7, with R.sup.7 being alkyl or benzyl.R.sup.1 and R.sup.2 are alkyl, phenyl or substituted phenyl.The compounds are useful for the treatment of hypertension in mammals, e.g., in humans.
Abstract: N-Aminoalkyl 1,5-benzothiazepines of the following formula (I): ##STR1## for the treatment of angina or hypertension or the prevention of heart attacks in mammals, in particular their use as coronary vasodilators.
Abstract: Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y and R.sup.1 are substituents such as hydrogen, alkyl, alkoxy, chloro or fluoro, m is 0-2, R.sup.2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are useful in treating hypertension and/or angina.