Novel 4-phenylpiperidines for the treatment of pruritic dermatoses
申请人:——
公开号:US20030078282A1
公开(公告)日:2003-04-24
Novel compounds having general formula (I), and pharmaceutically and veterinarily acceptable salts thereof wherein R 1, R 2, R 3, W, Y 1, Y 2, X, n and y are as defined above and processes for their preparation and intermediate compounds prepared therein. The novel compounds are useful for having utility in the treatment. of pruritic dermatoses including allergic dermatitis and atopy in animals and humans
Electrophilic Iron Catalyst Paired with a Lithium Cation Enables Selective Functionalization of Non‐Activated Aliphatic C−H Bonds via Metallocarbene Intermediates
Combining an electrophilic iron complex [Fe(F pda)(THF)]2 (3) [F pda=N,N'-bis(pentafluorophenyl)-o-phenylenediamide] with the pre-activation of α-alkyl-substituted α-diazoesters reagents by LiAl(ORF )4 [ORF =(OC(CF3 )3 ] provides unprecedented access to selective iron-catalyzed intramolecular functionalization of strong alkyl C(sp3 )-H bonds. Reactions occur at 25 °C via α-alkyl-metallocarbene intermediates
Process for the preparation of substituted pyrrolidine neuraminidase inhibitors
申请人:——
公开号:US20030055297A1
公开(公告)日:2003-03-20
A process for the preparation of neuraminidase inhibitors having structural formula (28)
1
or therapeutically acceptable salts thereof, in which R
1
is alkyl, cycloalkyl, cycloalkylalkyl, or arylalkyl; R
2
is alkyl, cycloalkyl, cycloalkylalkyl, or arylalkyl; R
4
is alkyl, cycloalkyalkyl, or aryl-(C
2
-C
4
-alkyl); R
10
is methyl, ethyl, iso-propyl, or vinyl; and
R
12
is hydrogen or alkyl and intermediates useful for the process are disclosed.
Substituted sulfonamides as selective .beta..sub.3 agonists for the
申请人:Merck & Co., Inc.
公开号:US05561142A1
公开(公告)日:1996-10-01
Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.