摘要:
Certain thienopyrimidine derivatives are useful for the inhibition of PDE10 enzymes, and thus are useful for treating psychiatric or neurological syndromes, e.g., pyschoses, obsessive-compulsive disorder and/or Parkinson's disease, as well as, for example, treating a disease state modulated by PDE10 activity.
摘要:
Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein.
摘要:
The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.
摘要:
Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.
摘要:
PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs, The compounds of the present invention are of Formulas I and II: wherein R1, R2, R3, R4, R7 and R8 are as defined herein.
摘要翻译:PDE4抑制是通过新的化合物,例如氨基吲唑和氨基苯并呋喃类似物来实现的。本发明化合物具有式I和II:其中R 1,R 2,R 2, R 4,R 4,R 8和R 8如本文所定义。
摘要:
PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3 and R4 are as defined herein.
摘要:
PDE4 inhibition is achieved by novel nitroxide compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formulas I-III: wherein A, B, D, R1, R2, R3, R7, R8, R9, R10 and R6 are as defined herein.
摘要:
PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2 , R3 and R4 are as defined herein.
摘要:
Described herein are compounds having the general formula: ##STR1## Ar.sub.1 and Ar.sub.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sub.1 or Ar.sub.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sub.1 and Ar.sub.2 may be attached to the central atom to which they are connected by a single bond, an alkylene, alkenylene or alkynylene group;R is H, alkyl or the counter ion for a basic addition salt;R.sub.1 and R.sub.2 are independently selected from the group consisting of H, alkyl and benzyl;R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently selected from the group consisting of H and alkyl;and a stereoisomer, salt, solvate and hydrate thereof.Also described is the use of these compounds as pharmaceuticals for the treatment of diseases in which inhibition of glycine transport via the GlyT-2 transporter is indicated.