IP Library Granted Patent US 7,071,222
Granted Patent B2
US 7,071,222 · App. 09/101,672 · Granted Jul 4, 2006

Preparation containing a combination of 5-methylisoxazole-4-carboxylic acid-(4-trifluoromethyl)-anilide and N-(4-trifluoromethylphenyl)2-cyano-3-hydroxycrotonic acid amide

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Quick Facts
Patent No.
US 7,071,222
App. No.
09/101,672
Granted
Jul 4, 2006
Kind
B2
Abstract

A solid composition comprising 5-methyl-4′-trifluoromethyl-4-isoxazole carboxanilide and N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonic acid amide, suitable for treatment of immunological and cancerous diseases.

Claims (28)

1. A solid composition comprising:

a first component comprising 5-methyl-4′-trifluoromethyl-4-isoxazolecarboxanilide;

a second component comprising a compound of formula I

or a stereoisomeric form of the compound of formula I, or a physiologically tolerated salt of the compound of formula I; and

a third component comprising a pharmaceutically tolerated excipient;

wherein the first component has a concentration from about 2 to about 20 mg and the second component has a concentration from about 0.3% to about 15% of the first component.

2. The composition as claimed in claim 1 , wherein the concentration of the second component is from about 1% to about 10% of the first component.

3. The composition as claimed in claim 1 , wherein the concentration of the second component is from about 1% to about 5% of the first component.

4. The composition as claimed in claim 1 , which comprises a first component and a second component in a form for rectal or oral administration.

5. The composition as claimed in claim 1 , wherein the concentration of the second component is from about 0.5 % to about 15 % of the first component.

6. The composition as claimed in claim 1 , wherein the concentration of the second component is from about 0.8 % to about 15 % of the first component.

7. A process for the preparation of a pharmaceutical composition of claim 1 , which comprises processing components 1, 2, and 3 into a pharmaceutically acceptable form for administration.

8. A method of treating an immunological disease comprising administering to a patient in need of such treatment, a therapeutically effective amount of a solid composition comprising

a first component comprising 5-methyl-4′-trifluoromethyl-4-isoxazolecarboxanilide;

a second component comprising a compound of formula I

or a sterioisomeric form of the compound of formula I, or a physiologically tolerated salt of the compound of formula I; and

a third component comprising a pharmaceutically tolerated excipient;

wherein the first component has a concentration from about 2 to about 20 mg and the second component has a concentration from about 0.3% to about 15% of the first component.

9. The method of claim 6 , wherein the composition produces a hyperadditive increase in the immunosuppressive effect.

10. A method according to claim 6 , wherein the immunological disease is an acute immunological disease.

11. A method according to claim 8 , wherein the acute immunological disease is sepsis, allergy, graft-versus-host reaction, or host-versus-graft reactions.

12. A method according to claim 6 , wherein the immunological disease is an autoimmune disease.

13. A method according to claim 10 , wherein the autoimmune disease is rheumatoid arthritis, systemic lupus erythrematosus, multiple sclerosis, psoriasis.

14. A method of treating a disease comprising administering to a patient in need of such treatment, a therapeutically effective amount of a solid composition comprising a first component comprising 5-methyl-4′-trifluoromethyl-4-isoxazolecarboxanilide;

a second component comprising a compound of formula I

or a stereoisomeric form of the compound of formula I, or a physiologically tolerated salt of the compound of formula I; and

a third component comprising a pharmaceutically tolerated excipient;

wherein the first component has a concentration from about 2 to about 20 mg and the second component has a concentration from about 0.3% to about 15% of the first component, and wherein the disease is atopic dermatitis, asthma, urticaria, rhinitis, uveitis, type II diabetes, cystic fibrosis, colitis, or hepatic fibrosis.

Assignments (4)
CHANGE OF NAME Recorded Dec 14, 2005
From: AVENTIS PHARMA DEUTSCHLAND GMBH
To: SANOFI-AVENTIS DEUTSCHLAND GMBH
Reel/Frame 016891/0619 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2002
From: HOECHST AKTIENGESELLSCHAFT (HOECHST AG)
To: AVENTIS PHARMA DEUTSCHLAND GMBH (AVENTIS PHARMA)
Reel/Frame 012722/0545 →
CHANGE OF NAME Recorded Aug 18, 2000
From: HOECHST MARION ROUSSEL DEUTSCHLAND GMBH
To: AVENTIS PHARMA DEUTSCHLAND GMBH
Reel/Frame 011019/0234 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 23, 1998
From: BARTLETT, KRISTA; BARTLETT, ROBERT (DECEASED); THEN, JOHANN
To: HOECHST AKTIENGESELLSCHAFT
Reel/Frame 009533/0395 →