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  C7 ester and c10 hydroxy substituted taxanesUSPTO Application #: 20070249708Title: C7 ester and c10 hydroxy substituted taxanes Abstract: Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents. (end of abstract) Agent: Senniger Powers - St Louis, MO, US Inventor: Robert A. Holton USPTO Applicaton #: 20070249708 - Class: 514449000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Oxygen Containing Hetero Ring The Patent Description & Claims data below is from USPTO Patent Application 20070249708. Brief Patent Description - Full Patent Description - Patent Application Claims
REFERENCE TO RELATED APPLICATION [0001] This application is a continuation based on U.S. Ser. No. 10/606,027, filed Jun. 25, 2003, which is a continuation based on U.S. Ser. No. 09/775,851, now U.S. Pat. No. 6,610,860, filed Feb. 2, 2001, which claims benefit of U.S. provisional application Ser. No. 60/179,794, filed on Feb. 2, 2000. BACKGROUND OF THE INVENTION [0002] The present invention is directed to novel taxanes which have exceptional utility as antitumor agents. [0003] The taxane family of terpenes, of which baccatin III and taxol are members, has been the subject of considerable interest in both the biological and chemical arts. Taxol itself is employed as a cancer chemotherapeutic agent and possesses a broad range of tumor-inhibiting activity. Taxol has a 2'R, 3'S configuration and the following structural formula: wherein Ac is acetyl. [0004] Colin et al. reported in U.S. Pat. No. 4,814,470 that certain taxol analogs have an activity significantly greater than that of taxol. One of these analogs, commonly referred to as docetaxel, has the following structural formula: [0005] Although taxol and docetaxel are useful chemotherapeutic agents, there are limitations on their effectiveness, including limited efficacy against certain types of cancers and toxicity to subjects when administered at various doses. Accordingly, a need remains for additional chemotherapeutic agents with improved efficacy and less toxicity. SUMMARY OF THE INVENTION [0006] Among the objects of the present invention, therefore, is the provision of taxanes which compare favorably to taxol and docetaxel with respect to efficacy as anti-tumor agents and with respect to toxicity. In general, these taxanes possess an ester substituent other than formate, acetate and heterosubstituted acetate at C-7, a hydroxy substituent at C-10 and a range of C-3' substituents. [0007] Briefly, therefore, the present invention is directed to the taxane composition, per se, to pharmaceutical compositions comprising the taxane and a pharmaceutically acceptable carrier, and to methods of administration. [0008] Other objects and features of this invention will be in part apparent and in part pointed out hereinafter. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS [0009] In one embodiment of the present invention, the taxanes of the present invention correspond to structure (1): wherein [0010] R.sub.2 is acyloxy; [0011] R.sub.7 is R.sub.7aCOO--; [0012] R.sub.7a is hydrocarbyl, substituted hydrocarbyl, or heterocyclo wherein said hydrocarbyl or substituted hydrocarbyl contains carbon atoms in the alpha and beta positions relative to the carbon of which R.sub.7a is a substituent; [0013] R.sub.9 is keto, hydroxy, or acyloxy; [0014] R.sub.10 is hydroxy; [0015] R.sub.14 is hydrido or hydroxy; [0016] X.sub.3 is substituted or unsubstituted alkyl, alkenyl, alkynyl, phenyl or heterocyclo; [0017] X.sub.5 is --COX.sub.10, --COOX.sub.10, or --CONHX.sub.10; [0018] X.sub.10 is hydrocarbyl, substituted hydrocarbyl, or heterocyclo; [0019] Ac is acetyl; and [0020] R.sub.7, R.sub.9, and R.sub.10 independently have the alpha or beta stereochemical configuration. Continue reading... Full patent description for C7 ester and c10 hydroxy substituted taxanes Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this C7 ester and c10 hydroxy substituted taxanes patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. Start now! - Receive info on patent apps like C7 ester and c10 hydroxy substituted taxanes or other areas of interest. ### Previous Patent Application: Use of certain biphenyl compounds for protection of neurons and oligodendrocytes in the treatment of multiple sclerosis (ms) Next Patent Application: Taxanes having c7 hydroxy and c10 heterosubstituted acetate substituents Industry Class: Drug, bio-affecting and body treating compositions ### FreshPatents.com Support Thank you for viewing the C7 ester and c10 hydroxy substituted taxanes patent info. IP-related news and info Results in 3.39148 seconds Other interesting Feshpatents.com categories: Medical: Surgery , Surgery(2) , Surgery(3) , Drug , Drug(2) , Prosthesis , Dentistry |
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