The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jul. 04, 2000

Filed:

Mar. 19, 1999
Applicant:
Inventors:

Masaya Ikunaka, Chita-gun, JP;

Yuji Shishido, Chita-gun, JP;

Masami Nakane, Nagoya, JP;

Assignee:

Pfizer Inc, New York, NY (US);

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K / ; A61K / ; C07D / ; C07D / ;
U.S. Cl.
CPC ...
5142305 ; 514311 ; 514326 ; 514314 ; 514317 ; 514318 ; 514319 ; 514320 ; 514321 ; 514323 ; 514324 ; 514329 ; 544105 ; 544106 ; 546153 ; 546155 ; 546157 ; 546174 ; 546194 ; 546196 ; 546197 ; 546202 ; 546205 ; 546207 ; 546209 ; 546210 ; 546213 ; 546214 ; 546223 ; 546224 ;
Abstract

A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C.sub.2 -C.sub.4 alkylene; Z is a valence bond or C.sub.1 -C.sub.6 alkylene; R.sup.1 is substituted or unsubstituted aryl (e.g., phenyl and naphthyl) or heteroaryl (e.g., thienyl and furyl); R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.3 is hydrogen, hydroxy or the like; R.sup.4 is substituted or unsubstituted benzyl or the like. Typical examples are (2S*,3S*,4R*,5R*)-4-Carboxy-3-[N-(5-Isopropyl-2-methoxy-benzyl)amino]-5-me thyl-2-phenylpyrrolidine and (2S*,3S*,5S*)-5-Carboxy-3-[N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-2- phenylpiperidine. The novel substituted azaheterocyclecarboxylic acids in this invention have excellent substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis or migraine in mammals, especially humans.


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