Patents Represented by Attorney Burton Rodney

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  • Non-cryogenic process for forming glycosides
    Patent number: 7164015
    Abstract: The present invention provides a method for making glycoside compounds including the steps of: (a) lithiating an aromatic reactant having a leaving group using a lithium reagent in a first microreactor under non-cryogenic conditions to form a lithiated anion species, and (b) coupling the lithiated anion species with a carbonyl substituted reactant to form a glycoside.
    Type: Grant
    Filed: February 27, 2004
    Date of Patent: January 16, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lifen Shen, San Kiang, Zhenrong Guo
  • Enzymatic resolution of aryl and thio-substituted acids
    Patent number: 7141694
    Abstract: Provided is a method of resolving a racemic mixture of a compound of formula I to obtain a desired enantiomer: wherein Ar is C6 or C10 aromatic group that can be substituted with H, C1 to C6 alkyl, trifluoromethyl or halo, R5 is halo or —S—R1, wherein R1 is H or acetyl, and R2 is H or C1 to C6 alkyl, the method comprising: reacting a compound of formula I wherein the compound is an ester whereby R2 is C1 to C6 alkyl with a lipase derived from Mucor meihei to stereoselectively hydrolyze the ester bond to produce an acid; and isolating the acid, wherein the reaction is conducted in a solvent comprising 80% to 98% v/v % organic phase and a residue of water phase (which can be buffered).
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: November 28, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingyang Zhu, Shannon X. Zhao
  • High drug load acid labile pharmaceutical composition
    Patent number: 7122207
    Abstract: A high drug load spheronized beadlet is provided wherein said beadlet comprises about 80% to 100% by weight of an acid labile medicament, preferably didanosine, about 0% to about 10% by weight of a disintegrant, and about 0% to about 10% by weight of a binder selected from the group consisting of sodium carboxymethylcellulose, hydroxypropylmethylcellulose, potassium alginate, and partially pregelatinized corn starch. A high drug load pharmaceutical composition, comprising the beadlet, with an enteric coating disposed thereon, is also provided.
    Type: Grant
    Filed: May 3, 2001
    Date of Patent: October 17, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ismat Ullah, Gary J Wiley
  • Aripiprazole complex formulation and method
    Patent number: 7115587
    Abstract: An aripiprazole formulation is provided which includes the antipsychotic agent aripiprazole in the form of an inclusion complex in a ?-cyclodextrin, preferably, sulfobutyl ether ?-cyclodextrin (SBECD), which in the form of an injectable produces reversible generally minimal to mild irritation at the intramuscular injection site. A method for minimizing or reducing irritation caused by aripiprazole at an intramuscular injection site and a method for treating schizophrenia employing the above formulation are also provided.
    Type: Grant
    Filed: August 14, 2003
    Date of Patent: October 3, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Manoj Nerurkar, Vijay Naringrekar
  • 2-substituted cyclic amines as calcium sensing receptor modulators
    Patent number: 7105537
    Abstract: The present invention relates to modulators of the calcium sensing receptor having the formula I wherein Ar1, X, n, R1, R2, R3 and Q are as defined herein.
    Type: Grant
    Filed: January 27, 2004
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashvinikumar V. Gavai, Roy J. Vaz, John K. Dickson, Jr., Jacques Y. Roberge, Wu Yang, Timur Gungor, James R. Corte, David P. Rotella, Yufeng Wang
  • Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
    Patent number: 7084162
    Abstract: Compounds are provided which have the structure wherein Q is C or N, A is O or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: September 5, 2003
    Date of Patent: August 1, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Pratik Devasthale, Yoon Jeon, Sean Chen, Hao Zhang
  • Lactam glycogen phosphorylase inhibitors and method of use
    Patent number: 7057046
    Abstract: A compound of formula I wherein W is a bicyclic hetroaryl of the structure X is —O—, —S—, —SO2—, —CHR5—, —CHR5O—, —CHR5S—, —CHR5SO2—, —CHR5CO— or —CH2CHR5—; Y is a bond or —CHR6—; Z is an aryl or heteroaryl group of the following structure: A is —CH— or —N—; B is —O— or —S—; and R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. Further provided is a method for treating diabetes and related diseases employing a glycogen phosphorylase inhibiting amount of the above compound, either alone or in combination with another therapeutic agent.
    Type: Grant
    Filed: May 19, 2003
    Date of Patent: June 6, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Philip Sher, Gang Wu, Terry Stouch, Bruce Ellsworth
  • Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
    Patent number: 7053106
    Abstract: Compounds are provided which have the structure wherein Q is C or N, A is O or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: December 16, 2003
    Date of Patent: May 30, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Pratik Devasthale, Yoon Jeon, Sean Chen, Hao Zhang
  • Process for preparing 4-alkyl- or 4-aryl-oxycarbonyl paclitaxel analogs and novel intermediates
    Patent number: 7030253
    Abstract: A process is provided for preparing 4-alkyl- or 4-aryl-oxycarbonyl paclitaxel analogs which includes the steps of converting paclitaxel into a C-7 acylprotected paclitaxel employing an electrophilic protecting group, such as benzoyloxycarbonyl, and converting the C-7 protected analog into the 4-alkyloxycarbonyl or 4-aryloxycarbonyl paclitaxel analog. Novel intermediates produced in the process are also provided.
    Type: Grant
    Filed: August 2, 2004
    Date of Patent: April 18, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Frank S. Gibson, Joydeep Kant, Rajendra P. Deshpande, Karen L. TenHuisen, Jing Liang, Jun Li, Susan D. Boettger, Edward J. Gublo, Ulhas P. Dhokte
  • Enzymatic resolution of aryl and thio-substituted acids
    Patent number: 7026143
    Abstract: Provided is a method of resolving a racemic mixture of a compound of formula I to obtain a desired enantiomer: wherein Ar is C6 or C10 aromatic group that can be substituted with H, C1 to C6 alkyl, trifluoromethyl or halo, R5 is halo or —S—R1, wherein R1 is H or acetyl, and R2 is H or C1 to C6 alkyl, the method comprising: reacting a compound of formula I wherein the compound is an ester whereby R2 is C1 to C6 alkyl with a lipase derived from Mucor meihei to stereoselectively hydrolyze the ester bond to produce an acid; and isolating the acid, wherein the reaction is conducted in a solvent comprising 80% to 98% v/v % organic phase and a residue of water phase (which can be buffered).
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: April 11, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingyang Zhu, Li You, Brenda J. White, Shannon X. Zha, Paul M. Skonezny
  • 3-aryl-hydroxybenzoxazines and 3, 4-dihydro-3-aryl-hydroxybenzoxazines as selective estrogen receptor beta modulators
    Patent number: 7015219
    Abstract: Substituted benzoxazine and 3,4-dihydrobenzoxazine derivatives possessing activity as estrogen receptor beta (ER?) modulators are provided which have the structure of formula I wherein the substitutents are as described herein. In addition, a method is provided for preventing, inhibiting or treating the progression or onset of pathological conditions associated with the estrogen receptor and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: December 18, 2002
    Date of Patent: March 21, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: John K. Dickson, Timur Gungor, Wu Yang
  • Modulators of the glucocorticoid receptor and method
    Patent number: 6995181
    Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where Z is CONR1R2 or CH2NR1R2 and where R, Ra, Rb, Rc, Rd, Z, A and B are defined herein.
    Type: Grant
    Filed: July 17, 2003
    Date of Patent: February 7, 2006
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Wayne Vaccaro, Bingwei Vera Yang, Soong-Hoon Kim, Tram Huynh, David R. Tortolani, Kenneth J. Leavitt, Wenying Li, Arthur M. Doweyko, Xiao-Tao Chen, Lidia Doweyko
  • Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same
    Patent number: 6979691
    Abstract: Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, in which E is X is N or CH, W is —NR16R17, —NR16C(?O)R22, —NR16CO2R22, —OR23, or a heteroaryl or heterocyclo group as defined in the specification, and R1 through R12, R16, R17, R22, R23, x, y, and z are as defined in the specification, are useful as modulaters of melanocortin receptors, particularly MC-1R and MC-4R.
    Type: Grant
    Filed: March 4, 2002
    Date of Patent: December 27, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guixue Yu, John Macor, Timothy Herpin, R. Michael Lawrence, George C. Morton, Rejean Ruel, Graham S. Poindexter, Edward H. Ruediger, Carl Thibault
  • Substituted azole acid derivatives useful as antidiabetic and antiobesity agents and method
    Patent number: 6967212
    Abstract: Compounds are provided which have the structure wherein Q is C or N; R2a, R2b, R2c, X1 to X7, R1, R2, R3, R3a, R4, A, Y, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents. The present invention further provides a method for treating obesity and dyslipidemia in mammals including humans through simultaneous inhibition of peroxisome proliferator activated receptor-? (PPAR?) and stimulation of peroxisome proliferator activated receptor-? (PPAR?).
    Type: Grant
    Filed: November 14, 2002
    Date of Patent: November 22, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Hao Zhang
  • Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
    Patent number: 6919358
    Abstract: Compounds are provided which have the structure wherein Q is C or N, A is O or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: February 22, 2002
    Date of Patent: July 19, 2005
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Peter T. Cheng, Pratik Devasthale, Yoon Jeon, Sean Chen, Hao Zhang
  • Heterocyclic sodium/proton exchange inhibitors and method
    Patent number: 6887870
    Abstract: Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl gorup, R1, R2, R3 and R4 are as defined herein, and where X is N. R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.
    Type: Grant
    Filed: September 25, 2000
    Date of Patent: May 3, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Shung C. Wu, Steven V. O'Neil, Khehyong Ngu, Karnail S. Atwal, David S. Weinstein
  • Process for preparing chiral diol sulfones and dihydroxy acid HMG CoA reductase inhibitors
    Patent number: 6875867
    Abstract: A process is provided for preparing chiral diol sulfones of the structure where R3 is preferably where R4a is preferably aryl such as phenyl, and R1a is preferably alkyl such as t-butyl, which are intermediates used in preparing HMG CoA reductase inhibitors.
    Type: Grant
    Filed: May 30, 2002
    Date of Patent: April 5, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Paul R. Brodfuehrer, Thomas R. Sattelberg, Joydeep Kant, Xinhua Qian
  • Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method
    Patent number: 6875782
    Abstract: Compounds are provided which are useful as antidiabetic agents and antiobesity agents and have the structure wherein m is 0, 1 or 2; n is 0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x1 where x1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is —(CH2)x2—O—(CH2)x3— where x2 is 0 to 5 and x3 is 0 to 5, provided that at least one of x2 and x3 is other than 0; B is a bond or is (CH2)x4 where x4 is 1 to 5; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; and A, R1, R2, R2a, R2b, R2c, R3 and Y are as defined herein.
    Type: Grant
    Filed: July 8, 2003
    Date of Patent: April 5, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. W. Cheng, Sean Chen, Charles Z. Ding, Timothy F. Herpin
  • Glyburide composition
    Patent number: 6830760
    Abstract: The present invention relates to a physical form of the known drug substance glyburide, also known as glibenclamide, and chemically defined as 5-chloro-N-[2-[4-[[[(cyclohexylamino)-carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxybenzamide (Merck Index, Tenth Edition, p. 642), as well as to dosage forms, e.g., tablets and capsules, incorporating said physical form of glyburide.
    Type: Grant
    Filed: April 30, 2003
    Date of Patent: December 14, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gillian Cave, Sarah J. Nicholson
  • HMG-CoA reductase inhibitors and method
    Patent number: 6812345
    Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.
    Type: Grant
    Filed: June 24, 2003
    Date of Patent: November 2, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jeffrey A. Robl, Bang-Chi Chen, Chong-Qing Sun