USRE47475EExpiredUtilityPatentIndex 71
Selective agents for pain suppression
Est. expiryMar 28, 2022(expired)· nominal 20-yr term from priority
Inventors:COOK JAMES MHUANG SHENGMINGEDWANKAR RAHULNAMJOSHI OJAS AWang zhi jianHUANG QIHE XIAOHUILI XIAOYANYU JIANMINGHAN DONGMEI
C07D 487/06C07D 243/24C07D 519/00C07D 471/04C07D 495/04C07D 243/20C07D 243/12C07D 487/04C07D 498/04A61K 31/5517C07F 7/0812
71
PatentIndex Score
4
Cited by
21
References
15
Claims
Abstract
In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of the often chronic, severe and debilitating pain that can accompany inflammatory diseases and neuropathic insults, pain that is often unresponsive to conventional analgesic treatment. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of neuropathic pain, migraine-related pain and inflammatory pain with reduced sedative and ataxic side effects.
Claims
exact text as granted — not AI-modifiedThe invention claimed is:
1. A method for the treatment and suppression of neuropathic pain, inflammatory pain and migraine-associated pain comprising administering to a patient in need of such treatment an effective amount of a compound of the formula wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 , R′ is CO 2 CH 2 CH 3 , CO 2 CH(CH 3 ) 2 , CO 2 CH 2 CH(CH 3 ) 2 , CON(CH 3 ) 2 , CONHCH 3 , or COSCH 3 and where R′ 2 R 2 ′ is CH(CH 3 ) 2 , CH 2 CH 3 , or CH 3 .
2. The method of claim 1 wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 .
3. The method of claim 1 wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 .
4. A method for the treatment and suppression of neuropathic pain, inflammatory pain and migraine-associated pain comprising administering to a patient in need of such treatment an effective amount of a compound of the formula, wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 .
5. A method for the treatment and suppression of neuropathic pain, inflammatory pain and migraine-associated pain comprising administering to a patient in need of such treatment an effective amount of a compound of the formula wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 .
6. A method for the treatment and suppression of neuropathic pain, inflammatory pain and migraine-associated pain comprising administering to a patient in need of such treatment an effective amount of a compound of the formula wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 and R′ is CO 2 CH(CH 3 ) 2 , CO 2 CH 2 CH(CH 3 ) 2 , CON(CH 3 ) 2 , CONHCH 3 , or COSCH 3 .
7. A method for the treatment and suppression of neuropathic pain, inflammatory pain and migraine-associated pain comprising administering a patient in need of such treatment an effective amount of a compound of the formula wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 and R′ is CO 2 CH(CH 3 ) 2 , CO 2 CH 2 CH(CH 3 ) 2 , CON(CH 3 ) 2 , CONHCH 3 , or COSCH 3 .
8. A method for the treatment and suppression of neuropathic pain, inflammatory pain and migraine-associated pain comprising administering to a patient in need of such treatment an effective amount of a compound of the formula wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 and R′ is CO 2 CH(CH 3 ) 2 , CO 2 CH 2 CH 2 (CH 3 ) 2 , CON(CH 3 ) 2 , CONHCH 3 , or COSCH 3 .
9. A method for the treatment and suppression of neuropathic pain, inflammatory pain and migraine-associated pain comprising administering to a patient in need of such treatment an effective amount of a compound of the formula wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 , and where R′ 2 R 2 ′ is CH(CH 3 ) 2 , CH 2 CH 3 , or CH 3 .
10. A method for the treatment and suppression of neuropathic pain, inflammatory pain and migraine-associated pain comprising administering to a patient in need of such treatment an effective amount of a compound of the formula wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 , and where R′ 2 R 2 ′ is CH(CH 3 ) 2 , CH 2 CH 3 , or CH 3 .
11. A method for the treatment and suppression of neuropathic pain, inflammatory pain and migraine-associated pain comprising administering to a patient in need of such treatment an effective amount of a compound of the formula wherein the compound is
and salts thereof where R is H or Si(CH 3 ) 3 , and where R′ 2 R 2 ′ is CH(CH 3 ) 2 , CH 2 CH 3 , or CH 3 .
12. A compound according to formula
or a salt thereof,
where R is —Si(CH 3 ) 3 ;
R 1 is —H or —CH 3 ;
R 3 is —CH 3 and R 4 is —H or R 3 is —H and R 4 is —CH 3 ;
R 10 is —CO 2 CH(CH 3 ) 2 , —CO 2 CH 2 CH(CH 3 ) 2 , —CON(CH 3 ) 2 , —CONHCH 3 or —COSCH 3 ; and
X is H, F, Cl, or Br.
13. The compound of claim 12, wherein R 1 is —H.
14. The compound of claim 12, wherein R 3 is —CH 3 and R 4 is —H.
15. The compound of claim 12, wherein X is F.Cited by (0)
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