Pfizer Corporation

Kunio Satake

Hiroaki Wakabayashi

Masami Nakane

Fumitaka Ito

Nakao Kojima

Hiroyuki Nishida

Nobuji Yoshikawa

Hideo Hirai

Katsuomi Ichikawa

Toshihide Kokura

Kazuo Ando

Yuji Shishido

Kaoru Shimada

John Adams Lowe, Iii

Brian Thomas O'Neill

Terry J Rosen

Harry R Howard, Jr

Takashi Mano

Masaya Ikunaka

Noriaki Murase

Nobuko Asai

Process for preparing 1,4-dihydropyridine compounds

Substituted benzylaminopiperidine compounds

5-substituted picolinic acid compounds production by Marasmiellus sp

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,or angiogenesis, especially CNS disorders in a mammalian subject, especially in humans.

The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof:

5-substituted picolinic acid compounds and their method of use

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).

5-Substituted picolinic acid compounds and their production process

Benzyloxyquinuclidines as substance P antagonists

##STR1## Compounds of formula (1), 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.

Substituted 3-aminoquinuclidines

Substituted quinuclidines as substance P antagonists

Heteroatom substituted alkyl benzylaminoquinuclidines

Substituted benzylamino nitrogen containing non-aromatic heterocycles

Substituted benzylaminoquinuclidines as substance P antagonists

Quinuclidine derivatives as substance P antagonists

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.

Aminobenzosultam derivatives as lipoxygenase inhibitors

Growing community of inventors

Handa, Japan

Kunio Satake