Unsaturation Between The 1- And 2-positions And The 4- And 5-positions (e.g., Prednisones, Prednisolones, Etc.) Patents (Class 552/576)
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Patent number: 10570269Abstract: A composition which contains microparticles and does not undergo the long-term process of aggregation of the microparticles during storage of the composition. An imidazole compound having a specific structure is added to a composition containing microparticles having a volume average particle diameter of 3000 nm or less. The composition may contain a base material component. The base material component may be a heat-curable or photocurable base material component. The microparticles may be inorganic particles and/or organic particles.Type: GrantFiled: July 15, 2016Date of Patent: February 25, 2020Assignee: TOKYO OHKA KOGYO CO., LTD.Inventors: Kunihiro Noda, Hiroki Chisaka, Koichi Misumi, Dai Shiota
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Publication number: 20150126483Abstract: The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).Type: ApplicationFiled: May 6, 2013Publication date: May 7, 2015Inventors: Thomas Cavanagh, Shikha P. Barman, Tian Hao, Thomas B. Leland, Ritesh V. Thekkedath
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Patent number: 8920838Abstract: Provided are methods for the treatment of a rheumatic disease, such as rheumatoid arthritis, ankylosating spondylitis and/or polymyalgia rheumatic, by administering a delayed-release dosage form of a glucocorticoid to a subject in need thereof wherein the treatment is administered once daily for at least about two weeks. Also provided are methods for the treatment of osteoarthritis by administering a delayed-release dosage form of a glucocorticoid to a subject in need thereof wherein the treatment is administered once daily for at least about two weeks.Type: GrantFiled: April 10, 2013Date of Patent: December 30, 2014Assignee: Horizon Pharma AGInventor: Achim Schaeffler
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Publication number: 20140356417Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.Type: ApplicationFiled: June 12, 2014Publication date: December 4, 2014Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Patent number: 8461139Abstract: The present invention relates to novel oral suspension formulation comprising prednisolone acetate, a pharmaceutically acceptable vehicle and a thickening agent. The present invention further provides a method of treating patients in need of prednisolone with the novel formulation.Type: GrantFiled: May 30, 2012Date of Patent: June 11, 2013Assignee: Taro Pharmaceuticals North America, Inc.Inventors: Satish Asotra, Shen Gao, Avraham Yacobi
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Publication number: 20120238534Abstract: The present invention relates to novel oral suspension formulation comprising prednisolone acetate, a pharmaceutically acceptable vehicle and a thickening agent. The present invention further provides a method of treating patients in need of prednisolone with the novel formulation.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Applicant: Taro Pharmaceutical North America, Inc.Inventors: Satish ASOTRA, Shen Gao, Avraham Yacobi
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Publication number: 20120183468Abstract: Provided herein are water-soluble, functionalized fullerenes, and processes for producing water-soluble, functionalized fullerenes. The process includes sulfonating a fullerene in an acidic solution comprising sulfuric acid to produce a sulfonated fullerene, isolating the sulfonated fullerene from the acidic solution without neutralizing the acidic solution, reacting the sulfonated fullerene with hydrogen peroxide to form a reaction product, and isolating a polyhydroxylated fullerene from the reaction product produced from reacting the sulfonated fullerene with the hydrogen peroxide. The process of producing water-soluble fullerenes further includes functionalizing a polyhydroxylated fullerene with one or more pendant functional groups by reacting the polyhydroxylated fullerene with one or more functional group precursors.Type: ApplicationFiled: January 17, 2012Publication date: July 19, 2012Applicant: MARELLE, LLCInventors: Mark Farrell, Michelle Guaragno
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Publication number: 20120157373Abstract: Antimicrobial compounds, such as silanol or alcohol, include a protecting or leaving group that can protect the compound from degradation during the process of preparing a medical device containing the compound or reduce the volatility of the compound relative to its counterpart without the leaving group. Nearly any hydrolysable leaving group may be employed. The leaving group may be an agent that may serve a therapeutic function in addition to protecting or retaining the antimicrobial agents.Type: ApplicationFiled: February 29, 2012Publication date: June 21, 2012Applicant: MEDTRONIC, INC.Inventors: Paul Hsien-Fu Wu, Catherine E. Taylor, Linnus Cheruiyot, Jianwei Li, Terese A. Bartlett, Matt Bergan
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Publication number: 20120088745Abstract: Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.Type: ApplicationFiled: October 11, 2011Publication date: April 12, 2012Inventors: C. Simone Fishburn, David Lechuga-Ballesteros, Tacey Viegas, Mei-Chang Kuo, Yuan Song, Hema Gursahani, Chester Leach
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Publication number: 20120040945Abstract: Methods, devices and compositions for treatment of severe and uncontrolled asthma are provided by which high amounts of an inhaled corticosteroid are directed to the small airways of the lower lungs. The invention provides for a substantial decrease in the dose of concurrently administered oral corticosteroids. A particular advantage of the invention is the significant reduction in corticosteroid-related adverse effects.Type: ApplicationFiled: February 3, 2010Publication date: February 16, 2012Applicant: ACTIVAERO GMBH RESEARCH & DEVELOPMENTInventors: Bernard Muellinger, Thomas Hofmann, Gerhard Scheuch, Philipp Kroneberg
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Patent number: 7812009Abstract: A pharmaceutical composition for intramammary administration to a nonhuman mammal comprising an antibacterial agent and prednisolone, wherein the composition comprises at least 20 mg of prednisolone, and its use for the treatment of clinical mastitis.Type: GrantFiled: December 10, 2003Date of Patent: October 12, 2010Assignee: Intervet International B.V.Inventors: Peter Gerardus Franciscus Cox, Joseph Antonius Clemens Maria Lohuis, Selma Marianne Hensen
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Patent number: 7632826Abstract: Corticosteroid receptors and/or mineralo-corticoid receptors are administered in combination with an addictive drug or the pharmacodynamic equivalent thereof for the therapy of an addictive disease triggered by said addictive drug or connected thereto.Type: GrantFiled: June 8, 2005Date of Patent: December 15, 2009Assignee: Curamentis Ltd.Inventor: Jochen Wolffgramm
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Patent number: 7390796Abstract: Compounds are disclosed of the formula in which R3 is C8 to C24 hydrocarbon or the residue of misoprostol. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.Type: GrantFiled: November 14, 2006Date of Patent: June 24, 2008Assignee: Sepracor Inc.Inventors: Mark G. Currie, Steven Jones, Charles M. Zepp
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Patent number: 6835724Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds Corticoid 17,21-dicarboxylic esters and corticoid 17-carboxylic ester 21-carbonic esters of the formula I: are described, in which A is CHOH and CHCl, CH2, C═O or 9(11) double bond; Y is H, F or Cl; Z is H, F or methyl; R(1) is aryl or hetaryl; R(2) is alkyl and R(3) is H or methyl. They are obtained, inter alia, by reacting a compound of the formula II: in which R(5) is OH, with an activated carboxylic acid of the formula III: R(6)-CO—(O)n[(C1-C4)-alkyl]m-R(1) III. They have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects. They are used, inter alia, as agents for treating inflammatory dermatoses.Type: GrantFiled: July 22, 1997Date of Patent: December 28, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Ulrich Stache, Hans-Georg Alpermann, Walter Dürckheimer, Manfred Bohn
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Publication number: 20040171597Abstract: There are provided compound of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents C3-8 cycloalkyl or C3-8 cycloalkenyl either of which may optionally be substituted by one or more groups selected from oxo, methyl, methylene and halogen; R3 represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and (AA) represents a single or a double bond; and solvates thereof, processes for preparing them and their use in therapy.Type: ApplicationFiled: November 24, 2003Publication date: September 2, 2004Inventors: Keith Biggadike, Paul Jones, Jeremy John Payne
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Patent number: 6762175Abstract: The properties of biologically active compounds, for example drugs and agrochemicals, which contain in their molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and carboxylic acid ester groups are modified by replacing one or more of these functional groups by a lipophilic group selected from those of the formula: RCOO—, RCONH—, RCOS—, RCH2O—, RCH2NH—, —COOCH2R, —CONHCH2R and —SCH2R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.Type: GrantFiled: April 5, 2002Date of Patent: July 13, 2004Assignee: Norsk Hydro ASAInventors: Finn Myhren, Bernt Børretzen, Are Dalen, Marit Liland Sandvold
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Patent number: 6756366Abstract: Orally Active androgens are derivative of 7&agr;-methyl-19-nortestosterone. The compounds satisfy formula (I) wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl; R2 is selected from the group consisting of (C2-3)alkyl, isopropyl, (C2-3)1-alkenyl, isopropenyl, 1,2-proandienyl, or (C2-3)1-alynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2)alkyl, or halogen; R3 is hydrogen, (C1-2)alkyl, or ethenyl; R4 is (C1-2)alkyl; R5 is hydrogen, or (C1-15)acyl; and the dotted lines indicate optional bonds.Type: GrantFiled: September 24, 2001Date of Patent: June 29, 2004Assignee: Akzo Nobel N.V.Inventors: Jaap van der Louw, Dirk Leysen, Roberta Burma Bursi
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Patent number: 6541465Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.Type: GrantFiled: July 31, 2001Date of Patent: April 1, 2003Assignee: Akzo Nobel N.V.Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
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Patent number: 6288051Abstract: This invention describes the new 7&agr;-(5-methylaminopentyl)-estratrienes of general formula I in which R2 stands for a hydrogen or fluorine atom, R17 stands for a hydrogen atom, a methyl or ethinyl group, n stands for 2, 3 or 4, and x stands for 0, 1 or 2. The new compounds are strong, pure antiestrogens and can be used for the production of pharmaceutical agents for treatment of estrogen-dependent diseases, for example, breast cancer, endometrial carcinoma, prostatic hyperplasia, anovulatory infertility and melanoma.Type: GrantFiled: October 14, 1999Date of Patent: September 11, 2001Assignee: Schering AktiengesellschaftInventors: Dieter Bittler, Rolf Bohlmann, Nikolaus Heinrich, Jorg Kroll, Gerhard Sauer, Yukishige Nishino, Karsten Parczyk, Martin Schneider, Christa Hegelehartung, Rosemarie Lichtner
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Patent number: 6180101Abstract: A remedy for tragomaschalia characterized in that it conntains an effective amount of adrenocorticosteroid and from 1 to 10% by weight of an extraction product from lactic acid fermentation based on one gram of a base. The extraction product from lactic acid fermentation has a metabolism product of lactic acid bacteria and ingredients of bacterial cells of lactic acid bacteria together. By inhibition of the secretion itself of a odoriferous steroid which is the cause of tragomaschalia, remetabolism and generation of such a steroid compound by tragomaschalia bacteria are completely eliminated, and there is little fear of adverse drug reactions by the adrenocorticosteroid used for that purpose.Type: GrantFiled: October 5, 1999Date of Patent: January 30, 2001Inventor: Keiko Yamamoto
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Patent number: 6066292Abstract: The invention is directed to a method for sterilizing a pharmaceutical formulation comprising a suspension of a water-insoluble pharmaceutical, comprising the steps of heat-sterilizing an aqueous solution of a viscosity enhancer, to result in a first sterile pre-mix. Next is sterile-filtering an aqueous solution of a mixture of a pharmaceutically-active compound, which results in a second sterile pre-mix. Next is heat-sterilizing a mixture of water, a water-insoluble pharmaceutical, and at least a partial amount of an electrolyte to provide a sub-saturated solution of the electrolyte, and adding under aseptic conditions an aqueous surfactant, to give a third sterile pre-mix. Finally, combining all three pre-mixes in sterile fashion to achieve a sterile suspended pharmaceutical formulation. Thus, for the third pre-mix, use of either Sodium chloride (in varying proportion) or Sodium acetate (in one proportion, but not limited to) is given as an example.Type: GrantFiled: December 19, 1997Date of Patent: May 23, 2000Assignee: Bayer CorporationInventor: Shivaji Purwar
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Patent number: 6013256Abstract: The invention provides methods of preventing acute rejection following renal or other solid organ transplantation. The methods entail administering, e.g., intravenously, to a transplant patient a monoclonal antibody which binds to the p55 subunit of the human interleukin-2 (IL-2) receptor of human T lymphocytes. The monoclonal antibody is preferably a chimeric or humanized antibody that blocks binding of IL-2 to the IL-2 receptor. In some methods, a single dose of about 1 mg/kg of antibody is administered about every other week, commencing immediately prior to transplantation and continuing until 8 weeks after transplantation.Type: GrantFiled: September 22, 1997Date of Patent: January 11, 2000Assignee: Protein Design Labs, Inc.Inventors: Susan Light, Cary Queen
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Patent number: 5886200Abstract: The invention provides an improved process for the preparation of 17-esters of 9.alpha.,21 -dihalo-pregnane-11.beta.,17.alpha.-diol-20-ones, and in particular for the preparation of 17-esters of anti-inflammatory steroids according to the following scheme: ##STR1## wherein RCO, R.sup.1, X, Y and the dotted line are as defined in the specification. The novel process is especially suitable for the preparation of Mometasone Furoate.Type: GrantFiled: June 25, 1997Date of Patent: March 23, 1999Assignee: Schering CorporationInventors: Daw-Iong Albert Kwok, David J. S. Tsai, Chou-Hong Tann, Xiaoyong Fu
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Patent number: 5702702Abstract: The invention provides a modified human cytotoxic T cell line, which is characterized by dual activity in vitro and in vivo against malignant cells and virus-infected cells. Also provided are effective and safe methods for use of the modified cells in adoptive therapy of cancer and untreatable vital diseases in MHC-mismatched recipients, and in marrow purging to achieve complete eradication of residual tumor cells from marrows of patients with leukemia and other types of cancer. Also provided are effective and safe methods for use of the cytokine stimulated, irradiated TALL-104 cells in the manufacture of a veterinary composition for adoptive therapy of canine and feline malignancies.Type: GrantFiled: June 6, 1995Date of Patent: December 30, 1997Assignee: The Wistar Institute of Anatomy and BiologyInventors: Daniela Santoli, Giovanni Rovera, Alessandra Cesano
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Patent number: 5670676Abstract: Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethylformamide; at a temperature within the range of about -78.degree. to about 0.degree. C.Type: GrantFiled: May 31, 1995Date of Patent: September 23, 1997Assignee: Schering CorporationInventors: Richard W. Draper, Eugene J. Vater
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Patent number: 5616573Abstract: Glucocorticoids of general formula IR--Val--O--GC (II),are described,in whichO-GC is the radical of a 21-hydroxycorticoid that has an antiinflammatory action,Val represents a valine radical in the 21-position of the corticoid andR means a hydrogen atom or a hydrocarbon radical with up to 32 carbon atoms that is optionally substituted by hydroxy groups, amino groups, oxo groups and/or halogen atoms and/or interrupted by oxygen atoms, SO.sub.2 groups and/or NH groups and their salts.Type: GrantFiled: October 6, 1995Date of Patent: April 1, 1997Assignee: Schering AktiengesellschaftInventors: Hans J. Zentel, Michael Topert, Henry Laurent, Thomas Brumby, Peter Esperling
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Patent number: 5510538Abstract: A process for the selective oxidation of a primary or secondary alcohol to an aldehyde or ketone and for the oxidation of a 1,2-diol to an .alpha.-ketol or .alpha.-diketone, which comprises contacting the alcohol or 1,2-diol with o-iodoxybenzoic acid. This process is suited for selective oxidation of alcohols containing easily oxidizable groups, such as amino or thioether groups and easily oxidizable heterocycles.Type: GrantFiled: December 16, 1994Date of Patent: April 23, 1996Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Marco Frigerio, Simona Sputore, Marco Santagostino
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Patent number: 5468729Abstract: A method and composition for treating autoimmune hepatitis in a patient utilizes an immunomodulatory amount of T.alpha..sub.1 and an anti-inflammatory amount of a corticosteroid.Type: GrantFiled: October 26, 1993Date of Patent: November 21, 1995Assignees: Alpha 1 Biomedicals, The Board of Governers of Wayne State UniversityInventors: Paul B. Chretien, Milton G. Mutchnick
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Patent number: 5362721Abstract: The disclosed invention includes corticoid-17-alkylcarbonates substituted in the 17-position, a process for their preparation and pharmaceuticals containing them. These corticoid-17-alkylcarbonates have the following formula I ##STR1## where A is CHOH in any desired steric arrangement, C.dbd.O or CH.sub.2 ; Y is H, F, or Cl; Z is H, F or CH.sub.3 ; R(1) is O-acyl, carbonylalkyl, alkylsulfonate or arylsulfonate;R(2) is branched alkyl or (CH.sub.2).sub.2-4 --OCH.sub.3 andR(3) is H or methyl. They have excellent local and topical antiinflammatory action. They are distinguished by a particularly good ratio of local to systemic antiinflammatory activity and in some cases also show stronger local antiinflammatory activities than their isomeric corticoid-17-alkylcarbonates having a linear alkyl group in the 17-alkylcarbonate moiety.Type: GrantFiled: February 8, 1993Date of Patent: November 8, 1994Assignee: Hoechst AktiengesellschaftInventors: Ulrich Stache, Walter Durckheimer, Hans G. Alpermann, Walter Petri
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Patent number: 5352808Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.sub.Type: GrantFiled: November 5, 1992Date of Patent: October 4, 1994Assignee: Roussel UclafInventors: Jean Buendia, Michel Vivat
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Patent number: 5278156Abstract: 11.beta.,17.alpha.,21-Trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] of the formula ##STR1## an antiinflammatory composition thereof and a method for the production thereof.11.beta.,17.alpha.,21-Trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] of the present invention exhibits remarkably excellent antiinflammatory action and besides, displays reduced side effects and can be produced in high selectivity and good yield and conveniently.Type: GrantFiled: March 24, 1992Date of Patent: January 11, 1994Assignees: Kuraray Co., Ltd., Taiho Pharmaceutical Co., Ltd.Inventors: Yutaka Mizushima, Keiko Hoshi, Rie Igarashi, Hirofusa Ajioka, Noriyuki Yamamoto, Masahito Komuro, Koichi Kanehira, Masayuki Inoue, Takashi Nishida, Michio Terasawa, Kenzo Arizono
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Patent number: 5266712Abstract: A process for crystallizing a pharmaceutically active steroidal product, without mechanical procedure, to obtain a homogeneous granulometric class which may be prepared beforehand, wherein the product which is desired to be crystallized is dissolved in a ternary mixture made of a lipophilic solvent, a hydrophilic solvent and a surface active agent at a temperature close to the boiling point of the mixture of solvents and wherein the mixture of solvents is allowed to revert to a temperature where the crystallization initiates, then, the thus-formed crystals are recovered.Type: GrantFiled: August 14, 1992Date of Patent: November 30, 1993Assignee: Laboratoire Theramex S.A.Inventor: Michel Lanquetin
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Patent number: 4948533Abstract: The present invention relates to 21-(3-carboxy-1-oxopropoxy) -17.alpha.-hydroxy-11.alpha.-(3,3-dimethyl-1-oxobutoxy)pregna-1,4-diene-3, 20 dione and pharmaceutically acceptable salts thereof which are useful steroid prodrugs.Type: GrantFiled: February 16, 1989Date of Patent: August 14, 1990Assignee: The Upjohn CompanyInventors: John M. Braughler, Edward D. Hall, Wendell Wierenga, John M. McCall
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Patent number: 4920216Abstract: This invention concerns a method of substituting a chlorine atom for a predetermined hydrogen atom located within an organic compound which comprises contacting the organic compound containing the predetermined hydrogen atom with an esterifying agent comprising a pyridine ring or a substituted or fused ring derivative of a pyridine ring so as to produce an ester and treating the ester with a chlorinating agent so as to substitute the chlorine atom for the predetermined hydrogen atom. The ester comprises the pyridine ring or the substituted or fused ring derivative of the pyridine ring so positioned within the ester with respect to the predetermined hydrogen atom that a chlorine atom attached to the nitrogen atom of the pyridine ring or substituted or fused ring derivative of the pyridine ring reacts with the predetermined hydrogen atom.Type: GrantFiled: May 28, 1987Date of Patent: April 24, 1990Assignee: The Trustees of Columbia in the City of New YorkInventors: Ronald Breslow, Michael Brandl, Alan D. Adams, Jurgen Hunger