Patents Represented by Attorney, Agent or Law Firm Maureen P. O'Brien
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Patent number: 7388098Abstract: Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and thType: GrantFiled: September 24, 2001Date of Patent: June 17, 2008Assignee: Bristol-Myers Squibb CompanyInventors: John J. Venit, Gary D. Madding, Victor W. Rosso, Francis J. Okuniewicz, Robert P. Discordia, Susanne Kiau, Atul S. Kotnis, Michael E. Randazzo, D. David Hennings, Jingyang Zhu, Jason G. Chen
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Patent number: 7300639Abstract: A process is provided for removing one or more metals from liquids. Also provided is a process for the synthesis of aP2 inhibiting compounds having the formula (I) wherein R1, R2, R3, R4, HET, and X-Z are as described herein, which process comprising the step of removing one or more metals from a solution of the compound of formula I or an intermediate or precursor thereof. The processes for removing metal comprise the step of contacting the liquid with a solid extractant comprising a metal-binding functionality.Type: GrantFiled: December 2, 2003Date of Patent: November 27, 2007Assignee: Bristol-Myers Squibb CompanyInventor: Wansheng Liu
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Patent number: 7265145Abstract: Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula wherein m is 0, 1, 2, 3 or 4; each X is independently selected from the group consisting of hydrogen, halo, cyano, nitro, OCF3, hydroxy, amino, carboxyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, haloalkyl, alkoxy, alkoxycarbonylalkyl, hydroxycarbonylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkylalkyl, R1O, R1R2N, R1OCO, R1CO, R1R2NCO, R1R2NCONR2a, R1OCONR2a, R1CONR2a, R1S, R1SO, R1SO2, R1R2NSO2, R1R2NSO2NR2a, and R1SO2NR2a; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; R2 and R2a are the same or different and are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; n is 1, 2, or 3; W is O or H,R3; R3 is hydrogen or hydroxyl; Ar is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl gType: GrantFiled: May 26, 2004Date of Patent: September 4, 2007Assignee: Bristol-Myers Squibb CompanyInventors: John K. Dickson, R. Michael Lawrence, Jacques Y. Roberge, David P. Rotella, Wu Yang
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Patent number: 7253170Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: June 28, 2006Date of Patent: August 7, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Robert V. Moquin, Stephen T. Wrobleski
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Patent number: 7253174Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-? expression utilizing compounds of the present invention are also disclosed.Type: GrantFiled: July 12, 2006Date of Patent: August 7, 2007Assignees: Bristol-Myers Squibb Company, Pharmacopeia, Inc.Inventors: Gulzar Ahmed, Axel Metzger, Ian Henderson, David J. Diller, Jun Wen, Stephen T. Wrobleski, Katerina Leftheris, Chunjian Liu
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Patent number: 7253167Abstract: The present invention relates to compounds having the formula, wherein, Q is optionally substituted aryl or heteroaryl, R1 is hydrogen or C1-4alkyl, and R2, R3, R4 and R5 are hydrogen or optional substituents as defined in the specification.Type: GrantFiled: June 29, 2005Date of Patent: August 7, 2007Assignee: Bristol-Myers Squibb CompanyInventors: James Lin, Stephen T. Wrobleski, Chunjian Liu, Katerina Leftheris
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Patent number: 7098235Abstract: Prodrugs of glycogen phosphorylase inhibiting compounds are provided which are useful in treating diabetes, having the formula I G(—O2CR?)m(—OH)n(—O2C(CH2)pCH3)qI wherein G is a C3 to C5 branched or straight carbon chain and (—O2CR?), (—OH) and (—O2C(CH2)pCH3) are attached to any available carbon atom along G; —O2CR? is a fragment of a compound of formula Ib where W is a bicyclic heteroaryl; m, n, p, q, X, Y, Z, R1 and R2 are as defined herein, as exemplified by Further provided are pharmaceutical compositions and methods for treating diabetes and related diseases employing the above compounds above, either alone or in combination with another therapeutic agent.Type: GrantFiled: November 13, 2003Date of Patent: August 29, 2006Assignee: Bristol-Myers Squibb Co.Inventors: Philip M. Sher, Bruce A. Ellsworth
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Patent number: 6831102Abstract: New thyroid receptor ligands are provided which have the general formula I: wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.Type: GrantFiled: December 6, 2002Date of Patent: December 14, 2004Assignee: Bristol-Myers Squibb CompanyInventor: Jon J. Hangeland
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Patent number: 6794518Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: December 17, 1999Date of Patent: September 21, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
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Patent number: 6780862Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I): Sag-Tag (I) or a pharmaceutically acceptable salt thereof, wherein Sag and Tag are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep and sexual disorders, migraine and other conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: December 19, 2001Date of Patent: August 24, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Ian S. Mitchell
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Patent number: 6777406Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein is R1, R6a, R6b, R7, R8, R9, X, b, m, and n are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: December 19, 2001Date of Patent: August 17, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
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Patent number: 6774112Abstract: Crystalline complexes are obtained from a 1:1 or 2:1 mixtures of either the (D) or (L) enantiomer of natural amino acids and compounds of formula wherein R1, R2 and R2a are independently hydrogen, OH, OR5, alkyl, —OCHF2, —OCF3, —SR5a or halogen; R3 and R4 are independently hydrogen, OH, OR5b, alkyl, cycloalkyl, CF3, —OCHF2, —OCF3, halogen, —CONR6R6a, —CO2R5c, —CO2H, —COR6b, —CH(OH)R6c, —CH(OR5d)R6d, —CN, —NHCOR5e, —NHSO2R5f, —NHSO2Aryl, —SR5g, —SOR5h, —SO2R5i, or a five, six or seven membered heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO2, or R3 and R4 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO2; R5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h and R5i are independently alkyl; R6Type: GrantFiled: April 8, 2002Date of Patent: August 10, 2004Assignee: Bristol-Myers Squibb CompanyInventor: Jack Z. Gougoutas
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Patent number: 6747048Abstract: Novel pyridine-based thyroid receptor ligands are provided which have the general formula I wherein: X is oxygen (—O—), sulfur (—S—), sulfoxide (—S(O)—), sulfonyl (—SO2—), CR8R8 or NR8; Y is —NR8, oxygen (—O—), —CH2— or sulfur (—S—); Z is a bond or substituted or unsubstituted C1-4 alkyl; and wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.Type: GrantFiled: May 7, 2003Date of Patent: June 8, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Minsheng Zhang, Jon Hangeland, Yolanda Caringal, Todd Friends
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Patent number: 6699852Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: December 19, 2001Date of Patent: March 2, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
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Patent number: 6683056Abstract: wherein when Y is or heteroaryl; A is —O(CH2)m, S, —NH(CH2)m, or (CH2)n where n is 0-3 and m is 0-2; and R1 to R6 are as defined herein. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with one, two or more other antidiabetic agents, and/or one, two or more hypolipidemic agents.Type: GrantFiled: February 23, 2001Date of Patent: January 27, 2004Assignee: Bristol-Myers Squibb CompanyInventors: William N. Washburn, Philip M. Sher, Gang Wu
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Patent number: 6638934Abstract: The present invention is directed to novel compounds represented by structural Formulas (I) and (I-a): or a pharmaceutically acceptable salt thereof, wherein R1, R4a, R4b, R5, R6, R7, R8, R9, n, and X are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep and sexual disorders, migraine and other conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: December 19, 2001Date of Patent: October 28, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert Robichaud, Ian S. Mitchell, Taekyu Lee, Wenting Chen
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Patent number: 6624184Abstract: The present invention discloses the identification of the inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.Type: GrantFiled: October 27, 1999Date of Patent: September 23, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Henry H. Gu, T. G. Murali Dhar, Edwin J. Iwanowicz
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Patent number: 6586438Abstract: A low dose antidiabetic pharmaceutical formulation is provided, especially adapted for treating Type II diabetes in drug naive patients, which includes a combination of metformin (employed in a reduced amount (less than 800 mg metformin per day) compared to that employed in generally accepted medical practice) and at least one other antidiabetic agent such as a sulfonyl urea, for example, glyburide, which combination provides at least about substantially equivalent efficacy in treating diabetes in drug naive patients, as do antidiabetic formulations containing metformin employed in dosages prescribed in generally accepted medical practice for first line therapy in treating diabetes, but with substantially reduced side effects, such as hypoglycemia and/or gastrointestinal distress.Type: GrantFiled: November 3, 1999Date of Patent: July 1, 2003Assignee: Bristol-Myers Squibb Co.Inventor: Beth Anne Piper
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Patent number: 6552017Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: June 15, 2000Date of Patent: April 22, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. Mc Clung, Emilie J. B. Calvello, David M. Zawrotny
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Patent number: 6548493Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: June 15, 2000Date of Patent: April 15, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Wenting Chen, Christopher D. McClung, Emilie J. B. Calvello, David M. Zawrotny