US 7,067,553 B2 · Thiourea compounds and the pharmaceutical compositions containing the same

Abstract

The present invention relates to thiourea compounds and the pharmaceutical compositions containing the same, and particularly, to novel thiourea compounds as an antagonist against vanilloid receptor (VR) and the pharmaceutical compositions thereof. As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.

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Claims6

Dependent claims

A compound of formula I:

or a pharmaceutically acceptable salt thereof,
wherein,
X represents a sulfur atom or an oxygen atom;
R1 represents a lower alkyl sulfonyl group having 1 to 5 carbon atoms, an aryl sulfonyl group or a lower alkyl carbonyl group having 1 to 5 carbon atoms, which may be unsubstituted or substituted with a halogen atom;
R2 represents a hydrogen atom, a methoxy group or a halogen atom;
when A is —NHCH2—, B represents
wherein, n is 0 or 1, or when A is —CH2—, B represents 4-t-butylbenzyl,
3,4-dimethylphenylethyl,
or an oleyl group;
Y represents —CH2— or —CH2CH2—;
R3 represents a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms;
and
R4 represents a lower alkyl group having 1 to 5 carbon atoms or a phenyl group.

10 more elements

Dependencies are inferred from the claim text.

Description6,900 words

Summary1,916 words

#The present invention relates to thiourea compounds and the pharmaceutical compositions containing the same, and particularly, to thiourea compounds with superior efficacy as an antagonist against vanilloid receptor (VR) and the pharmaceutical compositions thereof.

#As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides pharmaceutical compositions for prevention or treatment of these diseases.

#Yet, the diseases described above are only for enumeration, not to limit the scope of clinical application of vanilloid receptor antagonist.

Detailed description4,984 words

#The present invention is more specifically explained by the following examples. However, it should be understood that the present invention is not limited to these examples in any manner.

#The Examples 1˜8 are divided into three steps (step 1, 2 and 3), and the general methods for synthesizing the respective compounds are as follows.

#Step 1: General Method for Synthesizing Compound (1-2)

Facts

Application

10/362,079Filed 20 Aug 2001

Priority

KR 2000-4838521 Aug 2000

Published

US 2003/0212140 A113 Nov 2003

Granted

27 Jun 2006

Term ended

3 Sep 2021

Estimated · how

20 years from earliest known nonprovisional domestic filing plus recorded patent term adjustment, including 14 days of adjustment. Maintenance-fee lapses, terminal disclaimers and statutory extensions have not been checked. The continuity chain may be incomplete; this is not an enforceability determination.

Classification49 codes

C07D 333/42
With hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals,…:…
A61P 1/04
Drugs for disorders of the alimentary tract or the digestive system: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of…
A61P 3/10
For glucose homeostasis: for hyperglycaemia, e.g. antidiabetics
A61P 9/00
Drugs for disorders of the cardiovascular system

Timeline

21 Aug 2000Priority claimedKR 2000-48385
20 Aug 2001Application filedUS 10/362,079
20 Feb 2003Assigned to Pacific Corporationassignment of assignor's interest
13 Nov 2003PublishedUS 2003/0212140 A1
27 Jun 2006GrantedUS 7,067,553 B2
3 Sep 2021Term endedEstimated, includes 14 days of adjustment

Thiourea compounds and the pharmaceutical compositions containing the same

Life of this patent

Thiourea compounds and the pharmaceutical compositions containing the same

Life of this patent

Life of this patent

Abstract

Drawings

Drawings

Claims6

Description6,900 words

Drawings

Classification49 codes

Life of this patent

Description6,900 words