# US 5,352,676 A · Morphalinomethyl-substituted 1-phenyl-indero-[1,2-c]pyrazol-3-yl derivatives of 2-cyano-3-oxo-propanamides useful in the treatment of rheumatoid arthritis

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- Number: US 5,352,676 A
- Document ID: US5352676A
- Status: Granted
- Kind: A
- Application number: 08/084,470
- Filed: 1993-07-01
- Granted: 1994-10-04
- Earliest claimed: 1989-04-06
- Assignees: Farmitalia Carlo Erba S.p.A.
- Inventors: Gianfederico Doria; Anna M. Isetta; Rinaldo Ferreccio; Mario Ferrari; Maria C. Fornasiero; Domenico Trizio
- Web page: https://patentgrep.com/patent/US5352676A

## CPC

- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/415: 1,2-Diazoles
- A61P 37/00: Drugs for immunological or allergic disorders
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

This invention relates to a method of treating rheumatoid arthritis, which method comprises administering to a mammal a therapeutically effective amount of a compound of formula (I): ##STR1## wherein R1 is unsubstituted or substituted phenyl; R.sub.2 is a morpholinomethyl group; R.sub.3 is hydrogen; R.sub.4 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.a is hydrogen; and R.sub.b is a group --(A).sub.m --R.sub.5 wherein m is zero or 1, A is a C.sub.1 -C.sub.6 alkylene chain and R.sub.5 is unsubstituted or substituted phenyl; or a pharmaceutically acceptable salt thereof.

## Claims

### Claim 1

A method of treating a mammal suffering from rheumatoid arthritis, which method comprises administering to said mammal a therapeutically effective amount of a heteroaryl-3-oxo-propanenitrile derivative of formula (I) ##STR43## wherein X represents a --CH(R.sub.4)--group, wherein R.sub.4 represents hydrogen or C.sub.1 -C.sub.6 alkyl;
R.sub.1 represents phenyl, the phenyl being unsubstituted or substituted by a substituent chosen from halogen, trifluoromethyl and C.sub.1 -C.sub.6 alkyl;
R.sub.2 represents a ##STR44## group wherein each of R' and R", taken together with the nitrogen atom to which they are linked, form a morpholino ring which is unsubstituted or substituted by C.sub.1 -C.sub.6 alkyl;
R.sub.3 is hydrogen;
Q represents a ##STR45## group wherein R.sub.a represents hydrogen and R.sub.b represents a --(A).sub.m --R.sub.5 group wherein m is zero or 1, A is a C.sub.1 -C.sub.6 alkylene chain and R.sub.5 is phenyl, unsubstituted or substituted by one substituent chosen from halogen, CF.sub.3 and C.sub.1 -C.sub.6 alkyl; or a pharmaceutically or veterinarily acceptable salt thereof.

### Claim 2 (depends on 1)

A method according to claim 1, wherein said derivative is chosen from the group consisting of 2-cyano-3-(1,4-dihydro-5-morpholinomethyl-1-phenyl-indeno-[1,2-c]pyrazol-3 -yl]-3-oxo-N-phenyl propanamide;
2-cyano-3-(1,4-dihydro-7-morpholinomethyl-1-phenyl-indeno-[1,2-c]pyrazol-3- yl)-3-oxo-N-phenyl propanamide;
and the pharmaceutically and veterinarily acceptable salts thereof.