Abstract: This invention provides a compound of the formula: and its pharmaceutically acceptable salts, wherein R1 is C1-C6 alkyl; R2 is hydrogen, C1-C6 alkyl, halo C1-C6 alkyl or phenyl; R3 is hydrogen or halo; R4 and R5 are independently hydrogen, C1-C6 alkyl or halo C1-C6 alkyl; and n is one, two or three. These compounds are useful as analgesics or anti-inflammatory agents, or in the treatment of cardiovascular diseases, allergic disorders, angiogenesis, CNS disorders, emesis, gastrointestinal disorders, sunburn, urinary incontinence, or diseases, disorders or adverse conditions caused by Helicobacter pylori, or the like, in a mammalian subject, especially humans. Intermediates for preparation of the compounds of Formula (I) are also disclosed.

Abstract: A process for preparing a 1,4-dihydropyridine compound comprising contacting an enamine compound and a compound having a structure of in the presence of a base; and treating the reaction mixture thus obtained in the presence of an acid or a combination of acids under mild reaction conditions. A resulting 1,4-dihydropyridine compound is useful as an anti-inflammatory agent or the like.

Abstract: This invention provides a compound of the formula: 1

Abstract: A process for preparing a 1,4-dihydropyridine compound comprising contacting an enamine compound 1

Abstract: The invention provides a compound of formula (I): and its pharmaceutically acceptable salts, wherein R is halo C2-C8 alkenyl or halo C2-C8 alkynyl; R1 is hydrogen, halo or C1-C6 alkoxy; or R and R1, together with the two carbon atoms to which they are attached, form a C4-C6 cycloalkyl or a C4-C6 oxacycloalkyl ring wherein said ring may be optionally substituted by one or more substituents selected from the group consisting of halo, C1-C6 alkyl and halo C1-C6 alkyl; X is C1-C6 alkoxy, halo C1-C6 alkoxy, phenoxy or halo; and Ar is phenyl optionally substituted by halo. These compounds are useful in the treatment of a gastrointestinal disorder; a central nervous system (CNS) disorder; an inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by Heliobacter pylori; or angiogenesis especially CNS disorders in a mammalian subject, especially humans.

Abstract: The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is —C(O)O—C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).

Abstract: The invention provides a substituted benzylaminopiperidine compounds that are useful in the treatment of gastrointestinal disorders; central nervous system (CNS) disorders; inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by Heliobacter pylori; or angiogenesis, especially CNS disorders in a mammalian subject, especially in humans.

Abstract: The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is —C(O)O—C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).

Abstract: The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 are independently H, C.sub.2 -C.sub.6 acyl or halo-substituted benzoyl; and R.sup.3 is --C(O)O--C.sub.1 -C.sub.6 alkyl, C(O)OH, CN, CONH.sub.2, CONHCH.sub.3, CON(CH.sub.3).sub.2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R.sub.2 is acetyl and R.sup.3 is methoxycarbonyl, R.sup.1 is not H; and that when R.sup.3 is CN, CONH.sub.2, CONHCH.sub.3, CON(CH.sub.3).sub.2, 1-methyltetrazole or 2-methyltetrazole, R.sup.1 and R.sup.2 are H.The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like.The present invention further relates to a process for producing the compounds of the formula (I).

Abstract: This invention provides a compound of the formula: ##STR1## and its pharmaceutically acceptable salts, wherein R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or halo C.sub.1 -C.sub.6 alkoxy; R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyl-S-, C.sub.1 -C.sub.6 alkyl-SO--, C.sub.1 -C.sub.6 alkyl-SO.sub.2 --, cyclopropyl, phenyl, --NH.sub.2, --NH(CH.sub.3), --NHC(.dbd.O)CH.sub.3, --N(CH.sub.3).sub.2, --N(C.sub.2 H.sub.5).sub.2 or --CH.sub.2 C(.dbd.O)CF.sub.3 ; Ar.sup.1 and Ar.sup.2 are independently phenyl, halophenyl or thienyl; X is NH, O or S; and Y is hydrogen, --COOR.sup.3 or --CONR.sup.4 R.sup.5, wherein R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.6 alkyl.

Abstract: A compound of chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein X and Y are each hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, halosubstituted C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, or tri(C.sub.1 -C.sub.6 alkyl)silyl; Ar.sup.1 and Ar.sup.2 are each independently aryl or heteroaryl, optionally substituted by halogen; A is --CO-- or -(CH.sub.2)-; Z-A- is at the 2 or 3 position on the quinuclidine ring; and Z is --OH, C.sub.1 -C.sub.6 alkoxy, NR.sup.1 R.sup.2 or the like. Representative compounds are (3S,4R,5S,6S)-5-?3,5-bis(trifluoromethyl)-benzyloxy!-N,N-dimethyl-6-diphen ylmethyl-1-azabicyclo?2.2.2!octan-3-carboxamide, and -3-carboxylic acid.

Abstract: Certain novel substituted quinuclidine compounds having the ability to antagonize substance P and having the following formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl;X is --CONR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CH.sub.2 OR.sup.3, --CH.sub.2 NR.sup.3 R.sup.4 or --CONR.sup.3 OR.sup.4 ;R.sup.1, R.sup.3 and R.sup.4 are each, independently, hydrogen or alkyl having 1 to 4 carbon atoms;R.sup.

Abstract: Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I and the pharmaceutically-acceptable salts thereof; ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl; X is C.sub.1 -C.sub.6 alkyl having one or more substituents which include at least one heteroatom; Ar.sup.1 and Ar.sup.2 are each, independently, aryl optionally substituted by one C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, halogen, cyano, nitro, phenoxy, mono C.sub.1 -C.sub.6 alkylamino, di C.sub.1 -C.sub.6 alkylamino, halosubstituted C.sub.1 -C.sub.6 alkyl, or halosubstituted C.sub.1 -C.sub.6 alkoxy; Y is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, Z--(CH.sub.2).sub.p --, or W--(CH.sub.2).sub.m --CHR.sup.2 --(CH.sub.2).sub.n --NR.sup.1 CO-- wherein Y is at the 4-, 5- or 6-position on the quinuclidine ring; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl or --(CH.sub.2).sub.r --W; R.sup.

Abstract: The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula ##STR1## wherein W, R.sup.1, R.sup.2, R.sup.3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: Compounds of the formula ##STR1## wherein W, Ar.sup.1, Ar.sup.2 and Ar.sup.3 are defined as below; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

Abstract: Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I ##STR1## and the pharmaceutically-acceptable salts thereof, wherein Ar.sup.1 and Ar.sup.2 are each independently aryl or substituted aryl; R.sup.1 is alkyl having from 1 to 6 carbon atoms;R.sup.

Abstract: Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of formula (I) and the pharmaceutically-acceptable salts thereof, wherein X.sup.1 is alkoxy or halosubstituted alkoxy; X.sup.2 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halosubstitued alkyl, halosubstituted alkoxy, alkylamino, dialkylamino, alkylsulfonylamino (which may be substituted), N-alkyl-N-alkylsulfonylamino (which may be substituted), alkanoylamino (which may be substituted) or N-alkyl-N-alkanoylamino (which may be substituted); Ar.sup.1 and Ar.sup.2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; A is Y--(CH.sub.2).sub.m --CH(R.sup.2)--(CH.sub.2).sub.n --NR.sup.1 --; R.sup.1 is hydrogen, alkyl, benzyl or --(CH.sub.2).sub.p --Y; R.sup.2 is hydrogen, alkyl (which may be substituted), benzyl, 4-hydroxybenzyl, 3-indolylmethyl or --(CH.sub.2).sub.p --Y; Y is --CN, --CH.sub.

Abstract: Aminobenzosultam derivatives, which are inhibitors of lipoxygenase, having the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Ar is cycloalkyl having five to seven carbon atoms, tetrahydropyranyl, pyridyl, oxazolyl, phenyl or substituted phenyl wherein said substituent is methyl, methoxy, fluoro, chloro or trifluoromethyl; n is an integer of 1 to 3; X is hydrogen, methyl, methoxy, fluoro, chloro or trifluoromethyl; Z is --NH--, --O--, or --CH.sub.2 --; and R.sup.1 is hydrogen or alkyl having one to three carbon atoms.

Abstract: This invention relates to certain benzoxazolinones which inhibit lipoxygenase and/or cyclooxygenase enzymes. Such compounds are useful in inhibiting such enzymes, per se, and are useful in treating allergic and inflammatory conditions in a mammal. This invention also relates to methods of inhibiting lipoxygenase and/or cyclooxygenase in a mammal with such benzoxazolinones; methods of treating an allergic condition in a mammal with such compounds; methods of treating an inflammatory condition in a mammal with such compounds; and pharmaceutical compositions comprising the benzoxazolinones hereof.