Flexible Flat-Rate Plans

Flat-rate pricing for predictable budgeting

Short-term plans for project- or client-based billing

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 8,273,895

« Back to Dashboard

Details for Patent: 8,273,895

Title:NK.sub.1 antagonists
Abstract: A NK.sub.1 antagonist having the formula (I), ##STR00001## wherein Ar.sup.1 and Ar.sup.2 are optionally substituted phenyl or heteroaryl, X.sup.1 is an ether, thio or imino linkage, R.sup.4 and R.sup.5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
Inventor(s): Paliwal; Sunil (Monroe Township, NJ), Reichard; Gregory A. (Ann Arbor, MI), Wang; Cheng (Summit, NJ), Xiao; Dong (Warren, NJ), Tsui; Hon-Chung (East Brunswick, NJ), Shih; Neng-Yang (Warren, NJ), Arredondo; Juan D. (Montclair, NJ), Wrobleski; Michelle Laci (Whitehouse Station, NJ), Palani; Anandan (Bridgewater, NJ)
Assignee: Opko Health, Inc. (Miami, FL)
Filing Date:Dec 14, 2010
Application Number:12/967,132
Claims:1. A compound having the formula (I): ##STR00256## or a pharmaceutically acceptable salt thereof, wherein Ar.sup.1 is phenyl, wherein said phenyl can be unsubstituted or substituted with 1 to 3 fluoro; Ar.sup.2 is bis(trifluoromethyl)phenyl; X.sup.1 is --O--; R.sup.1 and R.sup.2 are independently selected from the group consisting of H, C.sub.1-C.sub.6 alkyl or hydroxyl(C.sub.1-C.sub.3 alkyl), C.sub.3-C.sub.8 cycloalkyl, --CH.sub.2F, --CHF.sup.2, --CF.sub.3; R.sup.3 is H, C.sub.1-C.sub.6 alkyl, hydroxyl(C.sub.1-C.sub.3 alkyl), C.sub.3-C.sub.8 cycloalkyl, --CH.sub.2F, --CF.sub.2H, or --CF.sub.3; R.sup.6 and R.sup.7 are independently selected from H or C.sub.1-C.sub.6 alkyl; n.sub.2 is 1 or 2; R.sup.4 and R.sup.5 together are .dbd.O; R.sup.18 is C.sub.1-C.sub.6 alkyl, Cbz or H; R.sup.32 and R.sup.33 are each H; or a diaseteromer, enantiomer, stereoisomer, regioisomer, rotamer, or tautomer thereof.

2. The compound according to claim 1, wherein: at least one of R.sup.1 or R.sup.2 is C.sub.1-C.sub.6alkyl and the other of R.sup.1 or R.sup.2 is H; R.sup.3 is H; R.sup.6 and R.sup.7 are H; R.sup.18 is Cbz or H; R.sup.32 and R.sup.33 are H; and n.sub.2 is 2, or a pharmaceutically acceptable salt thereof.

3. The compound according to claim 1 having the formula: ##STR00257##
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.