.

Deeper Knowledge, Faster

  • Analyze global market entry opportunities
  • Identify first generic entrants
  • Obtain formulation and manufacturing information

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

Serving leading biopharmaceutical companies globally:

Teva
Medtronic
Argus Health
Cerilliant
Johnson and Johnson
Baxter
Healthtrust
UBS
QuintilesIMS
Deloitte

Generated: December 17, 2017

DrugPatentWatch Database Preview

Details for Patent: ► Subscribe

« Back to Dashboard

Details for Patent: ► Subscribe

Title:Epothilone derivatives
Abstract: The present invention relates to compounds of the formula ##STR00001## in which the variables G, W, Q, X, Y, B.sub.1, B.sub.2, Z.sub.1, Z.sub.2, and R.sub.1-R.sub.7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
Inventor(s): Kim; Soong-Hoon (Titusville, NJ), Borzilleri; Robert M. (New Hope, PA), Vite; Gregory D. (Titusville, NJ), Johnson; James A. (Pennington, NJ)
Assignee: Bristol-Myers Squibb Company (Princeton, NJ)
Filing Date:Aug 14, 2013
Application Number:13/966,613
Claims:1. A compound of formula V, ##STR00050## wherein Q is selected from the group consisting of ##STR00051## G is selected from the group consisting of alkyl, substituted alkyl, substituted or unsubstituted aryl, heterocyclo, ##STR00052## W is NR.sub.15; X is O; Y is O; Z.sub.1 and Z.sub.2 are independently CH.sub.2; B.sub.1 and B.sub.2 are OH; D is selected from the group consisting of NR.sub.28R.sub.29, NR.sub.30COR.sub.31 or saturated heterocycle; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.13, R.sub.14, and are selected from the group H, alkyl, substituted alkyl, or aryl and when R.sub.1 and R.sub.2 are alkyl can be joined to form a cycloalkyl; R.sub.3 and R.sub.4 are alkyl can be joined to form a cycloalkyl; R.sub.31 is selected from the group H, alkyl, or substituted alkyl; R.sub.8, R.sub.11, R.sub.12, R.sub.28, R.sub.30, R.sub.32, and R.sub.33 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo; R.sub.15, and R.sub.29 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R.sub.32C.dbd.O, R.sub.33SO.sub.2, hydroxy, O-alkyl or O-substituted alkyl, the pharmaceutically acceptable salts thereof and any hydrates, solvates or geometric, optical and stereoisomers thereof wherein, "alkyl" means a straight or branched chain unsubstituted hydrocarbon group of 1 to 7 carbon atoms; "substituted alkyl" means an alkyl group substituted with one to four substituents selected from trifluoromethyl, trifluoromethoxy, hydroxy, alkoxy, cycloalkoxy, heterocyclooxy, oxo, alkanoyl, aryloxy, alkanoyloxy, amino, alkylamino, arylamino, aralkylamino, cycloalkylamino, heterocycloamino, disubstituted amines in which the 2 amino substituents are selected from alkyl, aryl or aralkyl, alkanoylamino, aroylamino, aralkanoylamino, substituted alkanoylamino, substituted arylamino, substituted aralkanoylamino, thiol, alkylthio, arylthio, aralkylthio, cycloalkylthio, heterocyclothio, alkylthiono, arylthiono, aralkylthiono, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, --SO.sub.2NH.sub.2, substituted sulfonamido, nitro, cyano, carboxy, --CONH.sub.2, --CONH alkyl, CONHaryl, CONHaralkyl, alkoxycarbonyl, aryl, substituted aryl, guanidine, indolyl, imidazolyl, furyl, thienyl, thiazolyl, pyrrolidyl, pyridyl, and pyrimidyl; wherein when the alkyl substituent is further substituted it will be with halogen, alkyl, alkoxy, aryl or aralkyl; "cycloalkyl" means an optionally-substituted, saturated cyclic hydrocarbon ring systems containing 1 to 3 rings and 3 to 7 carbons per ring which may be further fused with an unsaturated C.sub.3-C.sub.7 carbocyclic ring, wherein when substituted, the substituents will include one or more substituents as recited above as alkyl substituents; "aryl" means a monocyclic or bicyclic aromatic hydrocarbon groups having 6 to 12 carbon atoms in the ring portion; "substituted aryl" means an aryl group substituted by one to four substituents selected from alkyl, substituted alkyl, halo, trifluoromethoxy, trifluoromethyl, hydroxy, alkoxy, cycloalkyloxy, heterocyclooxy, alkanoyl, alkanoyloxy, amino, alkylamino, aralkylamino, cycloalkylamino, heterocycloamino, dialkylamino, alkanoylamino, thiol, alkylthio, cycloalkylthio, heterocyclothio, ureido, nitro, cyano, carboxy, carboxyalkyl, carbamyl, alkoxycarbonyl, alkylthiono, arylthiono, alkysulfonyl, sulfonamido, and aryloxy, wherein when the aryl substitute is further substituted, it will be with halo, hydroxy, alkyl, alkoxy, aryl, substituted alkyl or aralkyl; "heterocyclo" means an optionally substituted, fully saturated or unsaturated, aromatic or nonaromatic cyclic group which is a 4 to 7 membered monocyclic, 7 to 11 membered bicyclic, or 10 to 15 membered tricyclic ring system, which has at least one heteroatom in at least one carbon atom-containing ring, each ring of the heterocyclic group containing a heteroatom may have 1, 2 or 3 heteroatoms, wherein the term "heteroatoms" shall include oxygen, sulfur and nitrogen; and wherein when substituted, the substituted heterocyclo group will include one or more substituents as recited above as alkyl substituents.

2. A compound according to claim 1, wherein, Q is selected from the group consisting of ##STR00053## G is selected from the group consisting of alkyl; substituted alkyl; substituted aryl; a 4 to 7 membered monocyclic, 7 to 11 membered bicyclic, or 10 to 15 membered tricyclic saturated or unsaturated ring system having between 1 and 3 heteroatoms selected from nitrogen, oxygen, and sulfur; ##STR00054## W is NR.sub.15; X is O; Y is O; Z.sub.1 and Z.sub.2 are independently CH.sub.2; B.sub.1 and B.sub.2 are independently OH R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.7, are selected from the group consisting of H, alkyl, substituted alkyl, and aryl, and when R.sub.1 and R.sub.2 are alkyl they can be joined to form a cycloalkyl, and when R.sub.3 and R.sub.4 are alkyl they can be joined to form a cycloalkyl; R.sub.6 is methyl; R.sub.8 is hydrogen or methyl; and R.sub.15 is selected from the group consisting of H, alkyl, and substituted alkyl.

3. A pharmaceutical composition comprising one or more compounds of claim 1 and a pharmaceutically acceptable carrier or diluent.
« Back to Dashboard

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

Serving leading biopharmaceutical companies globally:

UBS
AstraZeneca
Farmers Insurance
Queensland Health
Chinese Patent Office
Moodys
Fish and Richardson
Fuji
US Department of Justice
Baxter

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.

Copyright 2002-2017 thinkBiotech LLC
ISSN: 2162-2639

Secure SSL Encrypted
Privacy and Cookies
Terms & Conditions

Follow DrugPatentWatch:

botpot