Patents Represented by Attorney, Agent or Law Firm Rena Patel
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Patent number: 6936628Abstract: The invention relates to methods of increasing the bioavailability of orally administered epothilones. Epothilones administered by the methods of the invention are sufficiently bioavailable to have a pharmacological effect. The invention further relates to pharmaceutical compositions, pharmaceutical dosage forms, and kits for use in the methods of the invention.Type: GrantFiled: April 1, 2003Date of Patent: August 30, 2005Assignee: Bristol-Myers Squibb CompanyInventor: Francis Y. F. Lee
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Patent number: 6831090Abstract: The present invention relates to 2,3-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor. The compounds of the invention as 16-membered macrolides having the general structure, which have microtubule-stabilizing effects and cytotoxic activity against rapidly proliferating cells, such as, tumor cells or other hyperproliferative cellular disease.Type: GrantFiled: September 13, 2002Date of Patent: December 14, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Gregory D. Vite, Robert M. Borzilleri, Gerhard Höfle, Thomas Leibold
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Patent number: 6780620Abstract: A microbial method for the preparation of an epothilone containing a terminal hydroxyalkyl group, comprising contacting at least one epothilone having a terminal alkyl group with an enzyme or microorganism capable of catalyzing the selective hydroxylation of said alkyl group to a hydroxyalkyl group, and effecting said hydroxylation.Type: GrantFiled: December 21, 1999Date of Patent: August 24, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Wenying Li, James A. Matson, Xiaohua Huang, Kin Sing Lam, Grace A. McClure
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Patent number: 6727276Abstract: A method of treating tumors in a mammal, especially a human that have demonstrated resistance to oncology with taxane oncology agents is disclosed. The method is effective where the tumor has initially been unresponsive to taxane therapy or has developed resistance during the course of treatment. The method comprising the administration of an epothilone derivative selected from those represented by formula I: The subject epothilone derivatives are advantageous in addition to their enhanced potency and effectiveness against tumors that have demonstrated resistance to therapy with taxane oncology agents in that both are efficacious upon oral administration.Type: GrantFiled: February 8, 2002Date of Patent: April 27, 2004Assignee: Bristol-Myers Squibb CompanyInventor: Francis Y. F. Lee
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Patent number: 6719540Abstract: The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by formula I: wherein: Q is selected from the group consisting of M is O, NR9, or CR10R11; X is O or NH; and the R groups are as defined, and therapeutic compositions containing them alone or in combination with other therapeutic agents useful in the treatment of cancer or other proliferative diseases.Type: GrantFiled: March 11, 2003Date of Patent: April 13, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Soong-Hoon Kim
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Patent number: 6689802Abstract: There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.Type: GrantFiled: August 9, 2001Date of Patent: February 10, 2004Assignee: Bristol-Myers Squibb CompanyInventors: John D. DiMarco, Jack Z. Gougoutas, Imre M. Vitez, Martha Davidovich, Michael A. Galella, Timothy M. Malloy, Zhenrong Guo, Denis Favreau
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Patent number: 6670384Abstract: A process for formulating certain epothilone analogs for parenteral administration is disclosed wherein the analog is dissolved in a mixture of at least 50% by volume tertiary-butanol in water, the mixture is lyophilized, the resulting lyophilized product is packaged in one vial with a sufficient amount of solvent comprising anhydrous ethanol and a suitable nonionic surfactant in a second vial. All steps are carried out with protection from light. In use, the contents of the second or diluent vial are added to the lyophilized product and mixed to constitute the epothilone analog and the resulting solution is diluted with a suitable diluent to produce a solution for intravenous injection containing the epothilone analog in a concentration of from about 0.1 mg/mL to about 0.9 mg/mL. A preferred surfactant is polyethoxylated castor oil and a preferred diluent is Lactated Ringer's Injection.Type: GrantFiled: January 23, 2002Date of Patent: December 30, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Rebanta Bandyopadhyay, Timothy M. Malloy, Andrea Panaggio, Krishnaswamy Srinivas Raghavan, Sailesh Amilal Varia
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Patent number: 6639074Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.Type: GrantFiled: March 18, 2002Date of Patent: October 28, 2003Assignee: Bristol Myers Squibb CompanyInventors: Bang-Chi Chen, Kyoung S. Kim, S. David Kimball, Raj N. Misra, Mark E. Salvati, Joseph E. Sundeen, Hai-Yun Xiao, Rulin Zhao
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Patent number: 6624310Abstract: The invention relates to compounds which are obtained by fermenting DSM 6773, especially epothilones A1, A2, A8, A9, B10, C1, C2, C3, C4, C5, C6, C7, C8, C9, D1, D2, D5, G1, G2, H1, H2, I1, I2, I3, I4, I5, I6 and K and trans-epothilones C1 and C2.Type: GrantFiled: March 21, 2001Date of Patent: September 23, 2003Assignee: Gesellschaft fuer Biotechnologische Forschung, mbH (GBF)Inventors: Gerhard Hoefle, Hans Reichenbach, Klaus Gerth, Ingo Hardt, Florenz Sasse, Heinrich Steinmetz
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Patent number: 6613911Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I: or a pharmnaceutically acceptable salt thereof, wherein: R1, R2, R4, R5, R6, R8, R9, R12 and R13 are each independently hydrogen, alkyl, aryl or heteroaryl; R3, R7, R10 and R11 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; and X is CH or N, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention also concerns a new process for the preparation of formylarylacetates and formylarylacetic acids.Type: GrantFiled: February 5, 2002Date of Patent: September 2, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Bang-Chi Chen, Kyoung S. Kim, S. David Kimball, Raj N. Misra, Joseph E. Sundeen, Rulin Zhao
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Patent number: 6610724Abstract: The present invention describes compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, and cardiovascular disease.Type: GrantFiled: August 15, 2002Date of Patent: August 26, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, S. David Kimball
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Patent number: 6605599Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.Type: GrantFiled: May 26, 1998Date of Patent: August 12, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
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Patent number: 6593115Abstract: The present invention relates to a process for the preparation of intermediates useful in the synthesis of epothilone analogs by initially enzymatically degrading certain epothilone compounds to form ring-open structures containing a carboxyl group which is esterified, the hydroxyl groups on the moiety protected and the resulting compound oxidized by, e.g. ozone, to form a first intermediate. The first intermediate can be reacted with a triphenylphosphine adduct to yield a compound containing an ester group at position 1 which is subsequently hydrolyzed to form a second intermediate.Type: GrantFiled: March 19, 2001Date of Patent: July 15, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Gregory D. Vite, Soong-Hoon Kim, Gerhard Höfle
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Patent number: 6593356Abstract: The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: July 16, 2001Date of Patent: July 15, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: David Nugiel, David Carini, Susan DiMeo, Anup Vidwans, Eddy Yue
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Patent number: 6576651Abstract: The invention relates to methods of increasing the bioavailability of orally administered epothilones. Epothilones administered by the methods of the invention are sufficiently bioavailable to have a pharmacological effect The invention further relates to pharmaceutical compositions, pharmaceutical dosage forms, and kits for use in the methods of the invention.Type: GrantFiled: January 25, 2002Date of Patent: June 10, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Rebanta Bandyopadhyay, Timothy M. Malloy, Andrea Panaggio, Krishnaswamy Srinivas Raghavan, Sailesh Amilal Varia
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6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
Patent number: 6559152Abstract: The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: February 27, 2001Date of Patent: May 6, 2003Assignee: DuPont Pharmaceuticals CompanyInventors: Jay A. Markwalder, Steven P. Seitz, Susan R. Sherk -
Patent number: 6534531Abstract: The invention provides a method for preventing or treating alopecia induced by chemotherapy or radiotherapy by administering to a mammalian specie in need thereof a therapeutically effective amount of a compound of formula I or II or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 26, 2001Date of Patent: March 18, 2003Assignee: Bristol-Myers Squibb CompanyInventors: S. David Kimball, Kevin R. Webster, David K. Bol
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Patent number: 6531477Abstract: The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: October 12, 1999Date of Patent: March 11, 2003Assignee: DuPont Pharmaceuticals CompanyInventors: Jay A. Markwalder, Steven P. Seitz, Susan R. Sherk
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Patent number: 6521759Abstract: The present invention describes compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, m and n are as defined in the specification. The compounds of formula I are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, chemotherapy-induced alopecia, and cardiovascular disease.Type: GrantFiled: April 20, 2001Date of Patent: February 18, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Kyoung S. Kim, S. David Kimball, Zhen-wei Cai, David B. Rawlins, Raj N. Misra, Michael A. Poss, Kevin R. Webster, John T. Hunt, Wen-Ching Han
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Patent number: 6518421Abstract: The present invention relates to a process for the preparation of epothilone analogs by initially forming novel ring-opened epothilones and carrying out a macrolactamization reaction thereon. The subject process is amenable to being carried out in a single reaction vessel without isolation of the intermediate compound and provides at least about a three-fold increase in yield over prior processes for preparing the desired epothilone analogs.Type: GrantFiled: February 1, 2001Date of Patent: February 11, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Wen Sen Li, John E. Thornton, Zhenrong Guo, Shankar Swaminathan