Tricyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/437)
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Patent number: 5880146Abstract: Disclosed are chemical agents for modulating certain cellular immune reactions that can lead to autoimmune disorders. By specific modulation, harmful immune reactions can be lessened in severity or even prevented without resorting to potentially dangerous general immune suppression. The described chemical agents inhibit IL-12 induction of the secretion of key immune modulators. The described chemical agents are specific inhibitors of IL-12 induced Th1 immune response.Type: GrantFiled: June 7, 1995Date of Patent: March 9, 1999Assignee: Fuji ImmunoPharmaceuticals CorporationInventors: Stephen D. Gillies, John Wesolowski
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Patent number: 5827856Abstract: The present invention provides a novel method for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: April 2, 1996Date of Patent: October 27, 1998Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Rolf Hohlweg, Tine Krogh J.o slashed.rgensen, Peter Madsen, Henrik Sune Andersen, Uffe Bang Olsen, Polivka Zdenek, Silhankova Alexandra, Sidelar Karel
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Patent number: 5728846Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist and/or retinoid inverse-agonist-like biological activity.Type: GrantFiled: December 12, 1996Date of Patent: March 17, 1998Assignee: AllerganInventors: Vidyasagar Vuligonda, Alan T. Johnson, Roshantha A. Chandraratna
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Patent number: 5726208Abstract: New compounds of formula: ##STR1## wherein: --A--D--E, X, n, Y and Z are as defined in the description, in racemic form and in the form of optical isomers,and their addition salts with pharmaceutically acceptable acids.Those compounds may be used as medicaments.Type: GrantFiled: October 11, 1996Date of Patent: March 10, 1998Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Jean-Christophe Harmange, Joel Vian, Aimee Dessinges, Mark Millan, Valerie Audinot
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Patent number: 5721260Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts therefor, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: April 4, 1996Date of Patent: February 24, 1998Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Peter Madsen, Henrik Sune Andersen
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Patent number: 5665760Abstract: Disclosed are reconstituted lyophilized formulations for the treatment of mammalian tumors comprising a thioxanthenone antitumor agent in combination with mannitol or sucrose as a stabilizer in a lactate buffer.Type: GrantFiled: September 18, 1995Date of Patent: September 9, 1997Assignee: Sanofi Winthrop, Inc.Inventors: Stephen Brown, Gurdial Singh Sandhu
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Patent number: 5571825Abstract: The present invention provides a method of selectively inhibiting prostaglandin G/H synthase-2 that comprises administering to a patient in need of such inhibition an inhibiting amount of a compound having the Formula I, II or III ##STR1## wherein the R groups and heterocycles are defined in the disclosure.Type: GrantFiled: March 31, 1995Date of Patent: November 5, 1996Assignee: Warner-Lambert CompanyInventors: Diane H. Boschelli, David T. Connor, Richard D. Dyer, Sonya S. Khatana, James B. Kramer, William H. Roark
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Patent number: 5550110Abstract: Novel antagonists of endothelin are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, metabolic, endocrinological, neurological disorders especially cerebral vasospasm, stroke, and head injury, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease, restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, and diabetes.Type: GrantFiled: June 30, 1994Date of Patent: August 27, 1996Assignee: Warner-Lambert CompanyInventors: Wayne L. Cody, Annette M. Doherty, John G. Topliss
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Patent number: 5447960Abstract: A plant fungicide method comprises applying to the locus of a plant pathogen a fungicidally effective amount of a compound of formula (I) ##STR1## or a salt or a complex thereof, wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently H, halo, NO.sub.2, (C.sub.1 -C.sub.4) alkyl, or halo(C.sub.1 -C.sub.4) alkyl;R.sup.3', R.sup.4', R.sup.5', R.sup.3", R.sup.4", and R.sup.5" are independently H, halo, OH, or CH.sub.3, provided that at least one is OH;R.sup.6 ' and R.sup.6 " are independently H or OH.Type: GrantFiled: October 4, 1993Date of Patent: September 5, 1995Assignee: DowElancoInventors: Deirdre M. Sinnott, Hak-Fun Chow, Robert J. Ehr, Steven D. Lubetkin, Stephen E. Bales, Muthiah N. Inbasekaran
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Patent number: 5438056Abstract: The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.Type: GrantFiled: October 5, 1993Date of Patent: August 1, 1995Assignee: American Home Products CorporationInventors: Steven W. Felman, Kevin A. Memoli, Ivo Jirkovsky
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Patent number: 5380749Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.Type: GrantFiled: March 23, 1994Date of Patent: January 10, 1995Assignee: Sterling Winthrop Inc.Inventors: Theodore C. Miller, Joseph C. Collins, Kenneth C. Mattes, Mark P. Wentland, Robert B. Perni, Thomas H. Corbett, Joseph W. Guiles
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Patent number: 5360803Abstract: A pharmaceutical composition for treatment of cancer comprises:(A) a therapeutically effective amount of at least one compound selected from the group consisting of compounds represented by the General Formula (I) ##STR1## wherein X.sub.1 and X.sub.2, which may be the same or different, each represents O, S, Se, --CH.dbd.CH--, ##STR2## Y.sub.1 represents O, S, Se, or ##STR3## R.sub.1 and R.sub.3, which may be the same or different, each represents an alkyl group;R.sub.2 represents an alkyl group, an aryl group or a heterocyclic group;Z.sub.1 and Z.sub.2, which may be the same or different, each represents an atomic group necessary to form a 5- or 6-membered ring;L.sub.1 represents a methine group or L.sub.1 and R.sub.3 may combine and form a 5- or 6-membered ring;R.sub.4 and R.sub.5, which may be the same or different, each represents a alkyl group;R.sub.6 and R.sub.Type: GrantFiled: November 6, 1992Date of Patent: November 1, 1994Assignees: Dan Farber Cancer Institute, Fuji Photo Film Co., Ltd.Inventors: Tadao Shishido, Lan B. Chen
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Patent number: 5346917Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.Type: GrantFiled: April 8, 1993Date of Patent: September 13, 1994Assignee: Sterling Winthrop Inc.Inventors: Theodore C. Miller, Joseph C. Collins, Kenneth C. Mattes, Mark P. Wentland, Robert B. Perni, Thomas H. Corbett, Joseph W. Guiles
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Patent number: 5302595Abstract: Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.Type: GrantFiled: January 6, 1993Date of Patent: April 12, 1994Assignee: Pfizer Inc.Inventors: Peter E. Cross, Alexander R. MacKenzie
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Patent number: 5276053Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: October 6, 1992Date of Patent: January 4, 1994Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5196445Abstract: Heteroaryl-3-oxo-propanenitrile derivatives of formula (I) ##STR1## wherein X represents an oxygen atom or a --CH(R.sub.4)--, --O--CH(R.sub.4)--, --S(O).sub.n --CH(R.sub.4)--, --CH(R.sub.4)--O--, --CH(R.sub.4)--S(O).sub.n -- --CH(R.sub.4)--CH.sub.2 -- group wherein n is 0, 1 or 2; R.sub.1 represents C.sub.1 -C.sub.6 alkyl, pyridyl or unsubstituted or substituted phenyl; R.sub.2, R.sub.3, and R.sub.4 are as herein defined; and Q is hydrogen, carboxy, C.sub.2 -C.sub.7 -alkoxycarbonyl or a --CON(R.sub.a)R.sub.b group, R.sub.a and R.sub.b being as defined herein; and their pharmaceutically acceptable salts are useful in the preparation of pharmaceutical compositions active in the treatment of autoimmune diseases.Type: GrantFiled: October 31, 1990Date of Patent: March 23, 1993Assignee: Farmitalia Carlo Erba SrlInventors: Gianfederico Doria, Anna M. Isetta, Rinaldo Ferreccio, Mario Ferrari, Maria C. Fornasiero, Domenico Trizio
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Patent number: 5192765Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.Type: GrantFiled: June 6, 1991Date of Patent: March 9, 1993Assignee: Pfizer Inc.Inventors: David Alker, Robert J. Bass, Peter E. Cross
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Patent number: 5180736Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: May 17, 1991Date of Patent: January 19, 1993Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5104858Abstract: A method for sensitizing multidrug resistant cells to antitumor agents comprosing contacting multidrug resistant cells, with an effective amount of a compound of the formula ##STR1## wherein n is 1, 2 or 3, X is CF.sub.3, --O--CH.sub.3, Br, I, Cl, H, W and S--CH.sub.3 and R.sup.1 and R.sup.2, independently of each other are --CH.sub.3 --CH.sub.2 --CH.sub.3, CH.sub.2 CH.sub.2 OHCH.sub.2 OH, or NR.sup.1 R.sup.2 form a ring ##STR2## wherein R.sup.3 is --CH.sub.3, CH.sub.2 --CH.sub.3, --H, CH.sub.2 OH and CH.sub.2 CH.sub.2 OH.Type: GrantFiled: September 29, 1988Date of Patent: April 14, 1992Assignee: Yale UniversityInventors: William N. Hait, James M. Ford
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Patent number: 5091410Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.Type: GrantFiled: June 10, 1991Date of Patent: February 25, 1992Assignee: Sterling Winthrop Inc.Inventors: Theodore C. Miller, Michael E. Ross
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Patent number: 5071853Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: February 27, 1990Date of Patent: December 10, 1991Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
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Patent number: 4999373Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA: cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.Type: GrantFiled: February 9, 1990Date of Patent: March 12, 1991Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4921871Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.Type: GrantFiled: November 16, 1987Date of Patent: May 1, 1990Assignee: Warner-Lambert CompanyInventors: Mary E. Carethers, Wiaczeslaw A. Cetenko, David T. Connor, Elizabeth A. Johnson, John S. Kiely, Charles F. Schwender, Jagadish C. Sircar, Roderick J. Sorenson, Paul C. Unangst, Robert F. Bruns
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Patent number: 4920146Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: December 28, 1987Date of Patent: April 24, 1990Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
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Patent number: 4886795Abstract: Retinal edema, in particular cystoid macular edema, is prevented or treated by administering to the patient afflicted with retinal edema or in danger of experiencing retinal edema an amount of a dopaminergic antagonist effective to reduce the edema. The activity of the dopaminergic antagonist may be potentiated by concurrent administration of ascorbic acid.Type: GrantFiled: October 24, 1986Date of Patent: December 12, 1989Inventor: Ronald A. Schachar
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Patent number: 4886815Abstract: Retinal edema, in particular cystoid macular edema, is prevented or treated by administering to the patient afflicted with retinal edema or in danger of experiencing retinal edema an amount of a dopaminergic antagonist effective to reduce the edema. A preferred dopaminergic antagonist is haloperidol. The activity of the dopaminergic antagonist may be potentiated by concurrent administration of ascorbic acid.Type: GrantFiled: October 24, 1986Date of Patent: December 12, 1989Inventor: Ronald A. Schachar
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Patent number: 4853410Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.Type: GrantFiled: October 9, 1987Date of Patent: August 1, 1989Assignee: Pfizer Inc.Inventor: Christopher A. Lipinski
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Patent number: 4851421Abstract: The invention relates to a biocidal fine powder with increased biocidal activity and an agricultural suspension containing the biocidal fine powder and an adjuvant selected from the group consisting of polyoxyalkylene-type nonionic surface active agents and polyoxyalkylene alkyl or alkylaryl ether phosphates or their salts.Type: GrantFiled: December 22, 1986Date of Patent: July 25, 1989Assignee: Kao CorporationInventors: Tetsuji Iwasaki, Yasushi Kamihisa
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Patent number: 4737514Abstract: Compounds of formula (I) ##STR1## wherein n is 0, 1 or 2;one or R.sup.1 and R.sup.2 is hydrogen and the other is selected from carbamoyl, N-C.sub.1-4 alkylcarbamoyl, N,N-di-C.sub.1-4 alkylcarbamoyl, carbamimidoyl, N.sup.1 -C.sub.1-4 alkylcarbamimidoyl, N.sup.2 -C.sub.1-4 alkylcarbamimidoyl, N.sup.1 -C.sub.1-4 alkyl-N.sup.2 -C.sub.1-4 alkylcarbamimidoyl, N.sup.1,N.sup.1 -di-C.sub.1-4 alkylcarbamimidoyl, N.sup.1,N.sup.1 -di-C.sub.1-4 alkyl-N.sup.2 -C.sub.1-4 alkylcarbamimidoyl and imidazolin-2-yl (optionally substituted by one or more C.sub.1-4 alkyl groups); andR.sup.3 is selected from hydrogen, saturated and unsaturated aliphatic hydocarbon moieties containing from 1 to 4 carbon atoms, groups OR.sup.4 (where R.sup.4 is selected from hydrogen and saturated and unsaturated aliphatic hydrocarbon moieties containing from 1 to 4 carbon atoms), halo, groups of formula--NR.sup.5 R.sup.6 (where R.sup.5 and R.sup.6 are independently selected from hydrogen, C.sub.1-4 alkyl and hydroxy C.sub.Type: GrantFiled: January 2, 1986Date of Patent: April 12, 1988Assignee: Burroughs Wellcome Co.Inventors: Morton Harfenist, Charles T. Joyner, Darryl J. Heuser
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Patent number: 4624949Abstract: The invention relates to compounds having the general formula (I) ##STR1## wherein R.sub.1 is carboxy, esterified carboxy or an amide of formula ##STR2## in which R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl, A is C.sub.2 -C.sub.6 alkylene and R.sub.a and R.sub.b are hydrogen or C.sub.1 -C.sub.6 alkyl or R.sub.a and R.sub.b taken together with the nitrogen atom to which they are linked form a saturated, optionally substituted, heteromonocyclic ring;R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;each of R.sub.3 to R.sub.8 is independently hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.4 alkenyloxy or C.sub.1 -C.sub.6 alkoxy; and the pharmaceutically acceptable salts thereof, which are useful as immunomodulating and anti-viral agents.Type: GrantFiled: March 4, 1986Date of Patent: November 25, 1986Assignee: Farmitalia Carlo Erba, S.p.A.Inventors: Piero Melloni, Paolo Salvadori, Pier P. Lovisolo
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Patent number: 4623656Abstract: 3-N-methylcarbamoylthioxanthen-9-one 10,10-dioxide of formula (I) ##STR1## is an inhibitor of monoamine oxidase-A, and is therefore useful in the prophylaxis and treatment of certain mental disorders such as depression.Type: GrantFiled: February 25, 1985Date of Patent: November 18, 1986Inventors: Morton Harfenist, Charles T. Joyner
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Patent number: 4582851Abstract: 1,4-Aminoalkylamino-9H-thioxanthen-9-ones have antimicrobial activity and activity against leukemic cells. Methods for their preparation, use and pharmaceutical compositions are described.Type: GrantFiled: January 10, 1985Date of Patent: April 15, 1986Assignee: Warner-Lambert CompanyInventor: Donald F. Worth
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Patent number: 4571405Abstract: Certain 5-substituted chromones and thiochromones and pharmacologically acceptable salts thereof are disclosed. The compounds possess antiallergic properties and are represented by the formula: ##STR1## wherein: X is selected from the group consisting of --O--, --S--, and --SO.sub.2 --;R.sub.1 and R.sub.2 are each independently H or lower alkyl having from 1 to 4 carbon atoms or together with C.sub.2 and C.sub.3 from a cyclohexane ring having the structure: ##STR2## wherein R.sub.3 and R.sub.4 are each independently H or a lower alkyl having from 1 to 4 carbon atoms.Also taught are valuable intermediates useful in the preparation of said 5-substituted chromones and thiochromones represented by the formula: ##STR3## wherein B is selected from the group consisting of --NHCOC(CH.sub.3).sub.3, 1,3-oxazolinyl and --CONHR, wherein R is methyl, phenyl, or t-butyl; Y is selected from the group consisting of CO.sub.2 H, CHO, CO.sub.Type: GrantFiled: May 29, 1984Date of Patent: February 18, 1986Assignee: Miles Laboratories, Inc.Inventors: Trevor S. Abram, Peter Norman, Warren, Brian T.