Patents Represented by Attorney David M. Morse
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Patent number: 4120857Abstract: Novel ester and ether derivatives of 1,2,3,3-tetramethyl-2-azabicyclo[2.2.2]octan-5-endo-ol have been prepared and found to possess antiarrhythmic or antihypertensive activity. An example of such a derivative possessing excellent antiarrhythmic activity is 5-endo-(3-benzoylaminopropyloxy)-1,2,3,3-tetramethyl-2-azabicyclo[2.2.2]oc tane.Type: GrantFiled: April 26, 1977Date of Patent: October 17, 1978Inventors: Mario Longobardi, Pietro Schenone, Francesco Bondavalli
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Patent number: 4118566Abstract: There is described the stereoselective total synthesis of novel .DELTA..sup.2,3 -1,4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein X is amino, azido or acylamido and Z represents optionally substituted C.sub.1 -C.sub.6 alkyl, aryl, aralkyl or heterocyclic. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.Type: GrantFiled: January 27, 1977Date of Patent: October 3, 1978Assignee: Bristol-Myers CompanyInventors: Donald E. Horning, Leeson R. Morris, James L. Douglas
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Patent number: 4113946Abstract: There is described the stereoselective total synthesis by a variety of routes of novel suitably substituted .DELTA..sup.2,3 -1,4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein Q is hydrogen, alkyl, aralkyl or --CH.sub.2 COOZ where Z is hydrogen or the residue of an ester group and X is amino, azido or acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. Those compounds in which X is acylamino and their physiologically hydrolyzed esters and pharmaceutically acceptable salts are potent antibacterial agents.Type: GrantFiled: January 19, 1977Date of Patent: September 12, 1978Assignee: Bristol-Myers CompanyInventors: Bernard R. Belleau, Terrence W. Doyle, Bing Yu Luh, Terry T. Conway
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Patent number: 4112071Abstract: A novel anthracycline antibiotic complex designated herein as figaroic acid complex is produced by fermentation of Streptosporangium sp. strain C-31,751, A.T.C.C. 31129. Figaroic acid complex inhibits the growth of various microorganisms, e.g., Staphylococcus aureus, exhibits phage inducing properties and inhibits the growth of various tumors in rodents, e.g., Sarcoma 180, L-1210 lymphatic leukemia, B-16 melanoma, Walker 256 carcinosarcoma and P-388 lymphatic leukemia.Type: GrantFiled: September 9, 1977Date of Patent: September 5, 1978Assignee: Bristol-Myers CompanyInventors: William T. Bradner, James A. Bush, Donald E. Nettleton, Jr.
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Patent number: 4112230Abstract: There is described the stereoselective total synthesis of novel .DELTA..sup.2,3 -1,4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein Z is halo, hydroxyl, etherified hydroxyl or hydroxyl esterified with a carboxylic acid residue or a sulfonic acid residue and X is amino, azido or acylamino. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.Type: GrantFiled: January 17, 1977Date of Patent: September 5, 1978Assignee: Bristol-Myers CompanyInventors: Marcel Menard, Gary M. F. Lim, Terry T. Conway
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Patent number: 4108725Abstract: A novel aminoglycoside antibiotic complex designated herein as Bu-2183 is produced by fermentation of Pseudomonas sp. strain D946-B83, A.T.C.C. 31086. Complex Bu-2183 is known to consist of at least five components, said components being herein designated Bu-2183 A, A.sub.2, B, C and D. The complex and the individual aminoglycoside components Bu-2183 A, A.sub.2, and B are found to have a broad spectrum of antibacterial activity and are especially useful in inhibiting aminoglycoside-resistant organisms including Pseudomonas species.Type: GrantFiled: August 13, 1976Date of Patent: August 22, 1978Assignee: Bristol-Myers CompanyInventors: Hiroshi Kawaguchi, Koji Tomita, Kei-ichi Fujisawa, Hiroshi Tsukiura
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Patent number: 4082751Abstract: A series of 2-(substituted)phenyl-5-(5-1H-tetrazolyl)pyrimidin-4(3H)-ones is provided for use as inhibitors of allergic reactions. The compounds show antiallergy activity by both oral and parenteral routes of administration.Type: GrantFiled: December 8, 1976Date of Patent: April 4, 1978Assignee: Bristol-Myers CompanyInventors: Peter Frederick Juby, Richard Anthony Partyka
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Patent number: 4081441Abstract: The penicillanic acids of the formula ##STR1## wherein Z is an oxygen or sulfur atom and their pharmaceutically acceptable salts and physiologically hydrolyzed esters possess antibacterial activity and are particularly valuable in treating Pseudomonas infections.Type: GrantFiled: April 6, 1977Date of Patent: March 28, 1978Assignee: Bristol-Myers CompanyInventors: Stephen Richard Baker, Charles Truman Holdrege
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Patent number: 4079057Abstract: The quinazoline derivative having the formula ##STR1## and pharmaceutically acceptable salts thereof are selective immunosuppressive agents useful in the treatment of immune complex diseases such as rheumatoid arthritis.Type: GrantFiled: May 31, 1977Date of Patent: March 14, 1978Assignee: Bristol-Myers CompanyInventors: Peter Frederick Juby, Thomas William Hudyma
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Patent number: 4068075Abstract: There is described the stereoselective total synthesis of novel .DELTA..sup.2,3 -1,4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein Z is halo, hydroxyl, etherified hydroxyl or hydroxyl esterified with a carboxylic acid residue or a sulfonic acid residue and X is amino, azido or acylamino. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.Type: GrantFiled: August 19, 1976Date of Patent: January 10, 1978Assignee: Bristol-Myers CompanyInventors: Marcel Menard, Gary M. F. Lim, Terry T. Conway
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Patent number: 4068080Abstract: There is described the stereoselective total synthesis of novel .DELTA..sup.2,3 -1,4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1, 6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein Z is halo, hydroxyl, etherified hydroxyl or hydroxyl esterified with a carboxylic acid residue or a sulfonic acid residue and X is amino, azido or acylamino. Also included in the invention are compounds of formula I in which the carbonyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.Type: GrantFiled: August 19, 1976Date of Patent: January 10, 1978Assignee: Bristol-Myers CompanyInventors: Marcel Menard, Gary M. F. Lim, Terry T. Conway
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Patent number: 4068066Abstract: There is described the stereoselective total synthesis of novel .DELTA..sup.2,3 -1,4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein X is amino, azido or acylamido and Z represents optionally substituted C.sub.1 -C.sub.6 alkyl, aryl, aralkyl or heterocyclic. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.Type: GrantFiled: September 23, 1976Date of Patent: January 10, 1978Assignee: Bristol-Myers CompanyInventors: Donald E. Horning, Leeson R. Morris, James L. Douglas
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Patent number: 4068078Abstract: There is described the stereoselective total synthesis of novel .DELTA..sup.2,3 -1,4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein Z is halo, hydroxyl, etherified hydroxyl or hydroxyl esterified with a carboxylic acid residue or a sulfonic acid residue and X is amino, azido or acylamino. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.Type: GrantFiled: August 19, 1976Date of Patent: January 10, 1978Assignee: Bristol-Myers CorporationInventors: Marcel Menard, Gary M. F. Lim, Terry T. Conway
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Patent number: 4066832Abstract: There is described the stereoselective total synthesis of novel .DELTA..sup.2,3 -1,4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1##wherein Z is halo, hydroxyl, etherified hydroxyl or hydroxyl esterified with a carboxylic acid residue or a sulfonic acid residue and X is amino, azido or acylamino. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.Type: GrantFiled: August 19, 1976Date of Patent: January 3, 1978Assignee: Bristol-Myers CompanyInventors: Marcel Menard, Gary M. F. Lim, Terry T. Conway
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Patent number: 4066831Abstract: There is described the stereoselective total synthesis by a variety of routes of novel suitably substituted .DELTA..sup.2,3 -1, 4-morpholine-2-carboxylic acids possessing a fused .alpha.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein Q is hydrogen, alkyl, aralkyl or -CH.sub.2 COOZ where Z is hydrogen or the residue of an ester group and X is amino, azido or acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. Those compounds in which X is acylamino and their physiologically hydrolyzed esters and pharmaceutically acceptable salts are potent antibacterial agents.Type: GrantFiled: August 19, 1976Date of Patent: January 3, 1978Assignee: Bristol-Myers CompanyInventors: Bernard R. Belleau, Terrence W. Doyle, Bing Yu Luh, Terry T. Conway
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Patent number: 4065622Abstract: There is described the stereoselective total synthesis of novel .DELTA..sup.2,3 -1,4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein X is amino, azido or acylamido and Z represents optionally substituted C.sub.1 -C.sub.6 alkyl, aryl, aralkyl or heterocyclic. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.Type: GrantFiled: September 23, 1976Date of Patent: December 27, 1977Assignee: Bristol-Myers CompanyInventors: Donald E. Horning, Leeson R. Morris, James L. Douglas
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Patent number: 4065623Abstract: There is described the stereoselective total synthesis by a variety of routes of novel suitably substituted .DELTA..sup.2,3 -1, 4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein Q is hydrogen, alkyl, aralkyl or --CH.sub.2 COOZ where Z is hydrogen or the residue of an ester group and X is amino, azido or acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. Those compounds in which X is acylamino and their physiologically hydrolyzed esters and pharmaceutically acceptable salts are potent antibacterial agents.Type: GrantFiled: August 19, 1976Date of Patent: December 27, 1977Assignee: Bristol-Myers CompanyInventors: Bernard R. Belleau, Terrence W. Doyle, Bing Yu Luh, Terry T. Conway
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Patent number: 4064014Abstract: A novel anthracycline antibiotic complex designated herein as bohemic acid complex is produced by fermentation of Actinosporangium sp. A.T.C.C. 31127. The complex and two bioactive components designated marcellomycin and musettamycin exhibit antibiotic activity and inhibit the growth of various tumor systems in rodents.Type: GrantFiled: March 23, 1977Date of Patent: December 20, 1977Assignee: Bristol-Myers CompanyInventors: Donald E. Nettleton, Jr., James A. Bush, William T. Bradner, Richard H. Schreiber
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Patent number: 4064234Abstract: A composition for treatment of hypercholesterolemia contains clofibrate or a clofibrate derivative, a magnesium or aluminum ion contributing compound which forms substantially insoluble metal bile acid salts and, optionally, a basic anion exchange resin. The composition components combine to give synergistic effect.Type: GrantFiled: November 26, 1976Date of Patent: December 20, 1977Assignee: Bristol-Myers CompanyInventor: Alan N. Howard
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Patent number: 4051237Abstract: A novel water-soluble basic glycopeptide antibiotic complex designated herein as Bu-2231 is produced by fermentation of a Bu-2231-producing strain of Streptoalloteichus hindustanus. Complex Bu-2231 and two of its major components designated herein as Bu-2231 A and B are found to inhibit the growth of various Gram-positive and Gram-negative and acid-fast bacteria as well as certain plant pathogens. The complex and components Bu-2231 A and B are also useful in inhibiting the growth of various tumors in rodents, for example, Walker 256 carcinosarcoma and Lewis Lung carcinoma.Type: GrantFiled: August 28, 1975Date of Patent: September 27, 1977Assignee: Bristol-Myers CompanyInventors: Hiroshi Kawaguchi, Koji Tomita, Hiroshi Tsukiura, Masataka Konishi