Ring Carbon Is Shared By Three Of The Cyclos Patents (Class 546/75)
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Patent number: 7015327Abstract: New anthrapyridone compounds represented by the general formula (14): {wherein R represents a hydrogen atom, an alkyl group (optionally substituted with mono- or di-alkylamino group), a lower alkyl group (optionally substituted with a hydroxyl group or a cyano group), or a cyclohexyl group; Y represents a chlorine atom, a hydroxyl group, an amino group, mono- or di-alkylamino group (optionally substituted with a sulfonic acid group, a carboxy group, or a hydroxyl group), an aralkyl- or cycloalkyl-amino group, an alkoxy group, a phenoxy group (optionally substituted with a sulfonic acid group, a carboxy group, an acetylamino group, an amino group, or a hydroxyl group), an anilino group (optionally substituted with a sulfonic acid group or a carboxy group), or a naphthylamino group (optionally substituted with a sulfonic acid group); and X represents a bridging group}; or salts thereof and magenta inks containing the same, which have hues and vividness suitable for ink-jet recording and give records excelleType: GrantFiled: April 1, 2005Date of Patent: March 21, 2006Assignee: Nippon Kayaku Kabushiki KaishaInventors: Hiroyuki Matsumoto, Katsunori Fujii, Takafumi Fujii, Yasuo Shirasaki
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Patent number: 7011701Abstract: A dye is disclosed, which is represented by the following formula: wherein Z is an atomic group necessary to form a 6-membered nitrogen containing aromatic ring; R11 is a hydrogen bonding group; R12, R13 and R14 are independently a hydrogen atom or a substituent; n11 and n13 are each an integer of 1 to 4; n12 is an integer of 1 to 3. There is also disclosed an ink for ink jet printing which contains the foregoing dye.Type: GrantFiled: November 19, 2003Date of Patent: March 14, 2006Assignee: Konica Minolta Holdings, Inc.Inventors: Kyoko Iwamoto, Hidetaka Ninomiya, Satoru Ikesu, Takatugu Suzuki, Mari Takahashi
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Patent number: 6858733Abstract: Novel compounds comprising a C—C double bond substituted at one carbon with two sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence rapidly by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes or peroxide-producing enzymes and in assays employing enzyme-labeled specific binding pairs.Type: GrantFiled: July 25, 2002Date of Patent: February 22, 2005Assignee: Lumigen, Inc.Inventors: Hashem Akhavan-Tafti, Renuka de Silva, Wenhua Xie
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Publication number: 20040259900Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: ApplicationFiled: August 16, 2004Publication date: December 23, 2004Inventors: Jia-He Li, Jie Zhang, Vincent Kalish
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Publication number: 20040198759Abstract: The invention provides aporphine and oxoaporphine compounds that have endothelial nitric oxide synthase (eNOS) maintaining or enhancing activities and may be used to manufacture a medicaments for preventing or treating ischemic diseases in human and mammal, and the ischemic diseases may include ischemic cerebral apoplexy, ischemic cerebral thrombosis, ischemic cerebral embolism, hypoxic ischemic encephlopathy, ischemic cardiac disease or ischemic enteropathy etc.Type: ApplicationFiled: April 2, 2004Publication date: October 7, 2004Inventors: MingJai Su, ShoeiSheng Lee
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Patent number: 6645975Abstract: The present invention relates to a novel process for the preparation of compounds of the formula wherein R1, R2, R4, R5, R6 and A are as defined herein, and to certain derivations of Formula IX which are useful for the treatment of movement disorders.Type: GrantFiled: January 27, 2003Date of Patent: November 11, 2003Assignee: Purdue Research FoundationInventors: Sing-Yuen Sit, Swanee E. Jacutin-Porte
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Publication number: 20030170771Abstract: Novel compounds comprising a C—C double bond substituted at one carbon with two sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence rapidly by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes or peroxide-producing enzymes and in assays employing enzyme-labeled specific binding pairs.Type: ApplicationFiled: July 25, 2002Publication date: September 11, 2003Inventors: Hashem Akhavan-Tafti, Renuka de Silva, Wenhua Xie
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Publication number: 20020132824Abstract: Compounds of the formula 1Type: ApplicationFiled: April 23, 2002Publication date: September 19, 2002Inventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
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Patent number: 6433172Abstract: This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.Type: GrantFiled: October 25, 1999Date of Patent: August 13, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Luc Grondard, Jean-Paul Casimir, Patrick Leon, Michael K. O'Brien, Matthew R. Powers, Daniel Robin
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Patent number: 6372756Abstract: A novel compound N-demethyl-sinomenine, a metabolite of the anti-arthritic alkaloid sinomenine, has been identified and characterized. The compound may be incorporated in a pharmaceutical composition and may be administered to patients for treatment of various disorders, such as rheumatoid arthritis. The novel compound has superior biological activity and water solubility as compared to sinomenine.Type: GrantFiled: February 19, 1999Date of Patent: April 16, 2002Assignee: AvMax, Inc.Inventors: Uwe Christians, Volkhard W. Kaever
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Patent number: 6348596Abstract: The invention provides asymmetric cyanine dye compounds having the general formula: including substituted forms thereof, which are non-fluorescent quencher molecules. The invention further provides reporter-quencher dye pairs, wherein the asymmetric cyanine dyes are the quenchers, polynucleotides incorporating the asymmetric cyanine dyes, and nucleic acid hybridization detection methods utilizing the dye-labeled polynucleotides.Type: GrantFiled: July 20, 1999Date of Patent: February 19, 2002Assignee: PE Corporation (NY)Inventors: Linda G. Lee, Ronald J. Graham, Khairuzzaman B. Mullah, Francis T. Haxo
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Publication number: 20020002176Abstract: Apomorphine derivative compounds; pharmaceutically active compositions of apomorphine derivative compounds; and the use of apomorphine derivative compounds in methods for treating sexual dysfunction or for enhancing apomorphine effectiveness for patients treated with apomorphine are disclosed. The apomorphine derivatives may be esters, ethers, amides, mixed anhydrides, hemiacetals, glucuronates, sulfates or phosphonates. A preferred apomorphine derivative is norapomorphine.Type: ApplicationFiled: March 29, 2001Publication date: January 3, 2002Inventors: Pramod K. Gupta, Deborah Milkowski, Debra Sutkowski-Markmann
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Patent number: 6313134Abstract: The present invention discloses thaliporphine and its derivatives for the treatment and/or prophylaxis of cardiac diseases, including cardiac arrhythmia, myocardial ischemia or myocardial infarction, and sudden death caused by cardiac arrhythmia or acute myocardial infarction.Type: GrantFiled: August 23, 2000Date of Patent: November 6, 2001Assignee: National Science CouncilInventors: Ming-Jai Su, Shoei-Sheng Lee
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Patent number: 6248884Abstract: Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure In addition, methods of making and using the dyes as fluorescent labels are disclosed.Type: GrantFiled: June 3, 1999Date of Patent: June 19, 2001Assignee: The Perkin-Elmer CorporationInventors: Joe Y. L. Lam, Scott C. Benson, Steven M. Menchen
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Patent number: 6174891Abstract: This invention provides an antipruritic comprising an opiate &kgr; receptor agonist as an effective component, a new morphinan quaternary ammonium salt derivative and a new morphinan-N-oxide derivative which are useful in treating pruritus complicated with some diseases.Type: GrantFiled: August 24, 1998Date of Patent: January 16, 2001Assignee: Toray Industries, Inc.Inventors: Hiroshi Nagase, Jun Utsumi, Takashi Endoh, Toshiaki Tanaka, Junzo Kamei, Kuniaki Kawamura
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Patent number: 6136818Abstract: A method of treating sexual dysfunction comprising administering a therapeutically effective amount of a combination of phentolamine and apomorphine, as well as pharmaceutical compositions and kits useful in those methods, are disclosed.Type: GrantFiled: October 8, 1999Date of Patent: October 24, 2000Assignee: Schering CorporationInventor: Thomas Mark Estok
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Patent number: 6121275Abstract: The present invention provides protoberberine alkaloid derivatives useful as anticancer agents, and methods of use thereof. The invention also provides protoberberine derivatives useful as topoisomerase inhibitors. The invention further provides coralyne and nitidine derivatives which are topoisomerase I-targeted therapeutics effective against camptothecin resistant cancer cells, and are especially effective against CNS tumors.Type: GrantFiled: July 31, 1998Date of Patent: September 19, 2000Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Leroy Fong Liu, Darshan B. Makhey
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Patent number: 5959110Abstract: The present invention is directed to a novel dopamine receptor ligands of the formula: ##STR1## pharmaceutical formulations of such compounds, and a method using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system.Type: GrantFiled: October 18, 1996Date of Patent: September 28, 1999Assignees: Purdue Research Foundation, University of North CarolinaInventors: David E. Nichols, Richard Mailman, Debasis Ghosh
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Patent number: 5717098Abstract: A process for the preparation of a .gamma.-lactone of the formula ##STR1## which can be used to produce a single enantiomer of aminoazanoradamantane which is coupled to aromatic acid moieties to produce compounds useful as 5-HT agonists or antagonists.Type: GrantFiled: July 22, 1996Date of Patent: February 10, 1998Assignee: G. D. Searle & Co.Inventors: Daniel Paul Becker, Daniel Lee Flynn, Alan Edward Moormann, Clara Ines Villamil
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Patent number: 5622958Abstract: A quinone imine enediyne possessing cytotoxic activity towards cancer cells having the general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently the same or different and are H, Br, Cl, F, NH.sub.2, CO.sub.2 H, or OH or a linear or branched alkyl, etc.; wherein R.sub.4 is H, OH or a linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R.sub.5 is H, Br, Cl, F, O.dbd., OH or S--SR, or a linear or branched alkyl, etc.; wherein R.sub.6 is H, Br, Cl, F, CO.sub.2 H, OH or S--SR', or a linear or branched alkyl, etc; wherein R.sub.7 is H, OH or S--SR", or a linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl group; and wherein R, R' and R" are independently the same or different and are a linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl group.Type: GrantFiled: December 1, 1994Date of Patent: April 22, 1997Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Matthew D. Shair, Taeyoung Yoon, T.-C. Chou
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Patent number: 5534521Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof; pharmaceutical compositions containing the compounds and a method for treating serotonin mediated condition with the compositionswhich act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.Type: GrantFiled: November 8, 1994Date of Patent: July 9, 1996Assignee: G. D. Searle & Co.Inventors: Daniel L. Flynn, Alan E. Moormann, Daniel P. Becker, Michael S. Dappen, Roger Nosal, Robert L. Shone, Clara I. Villamil
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Patent number: 5258384Abstract: S-11-hydroxy-10-methylaporphine and its biologically active salt forms are used as 5-HT.sub.1A inhibitors. Since these compounds function as 5-HT.sub.1A they can be used as an antidote for effects of cocaine and as appetite suppressants.Type: GrantFiled: January 22, 1993Date of Patent: November 2, 1993Assignee: British Technology Group LimitedInventors: Joseph G. Cannon, Scott T. Moe, John P. Long, Ranbir K. Bhatnagar
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Patent number: 5245028Abstract: Processes for the preparation of a series of tetracyclic amines useful in the treatment and/or prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: September 3, 1991Date of Patent: September 14, 1993Assignee: Warner-Lambert CompanyInventor: Thomas C. Malone
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Patent number: 5154887Abstract: Certain phenalenimine fluorescent compounds represented by the structure ##STR1## wherein R' and R" are independently hydrogen, alkyl, cycloalkyl, aryl or a heterocycle, or R' comprises the carbon and heteroatoms which form a fused ring with the compound nucleus, are useful in biomedical and analytical determinations. These compounds can be used for staining cells, as well as for the determination of various analytes found in human or animal biological fluids. Such determinations can be carried out in solution or by using dry analytical elements. The fluorescent compounds can be reacted with quinone nuclei to form reducible compounds which are also useful in analytical methods. In addition, the compounds can be incorporated into what are known as "loadable" latex particles to form detectable labels and biological reagents.Type: GrantFiled: May 28, 1991Date of Patent: October 13, 1992Assignee: Eastman Kodak CompanyInventors: Bruce E. Babb, Fred T. Oakes
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Patent number: 5109136Abstract: A novel series of tetracyclic amines, methods of preparation, compositions containing the amines, and methods for using them in the treatment and/or prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: August 9, 1990Date of Patent: April 28, 1992Assignee: Warner-Lambert CompanyInventor: Thomas C. Malone
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Patent number: 5070093Abstract: A novel series of tetracyclic amines, methods of preparation, compositions containing the amines, and methods for using them in the treatment and/or prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: March 28, 1991Date of Patent: December 3, 1991Assignee: Warner-Lambert CompanyInventor: Thomas C. Malone
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Patent number: 5001115Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.Type: GrantFiled: May 17, 1989Date of Patent: March 19, 1991Assignee: University of FloridaInventor: Kenneth B. Sloan
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Patent number: 4933324Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug.In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be digested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: February 24, 1989Date of Patent: June 12, 1990Inventor: Victor E. Shashoua
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Patent number: 4873349Abstract: A method for forming bridged biaryl compounds via the intramolecular oxidative biarylic coupling of precursor compounds containing two aromatic rings linked via a hydrocarbon chain is disclosed along with the ruthenium catalyst for its implementation and new compounds resulting therefrom. The biarylic coupling method is characterized in that the biarylic precursors are cyclized in the presence of the catalyst tetrakis(trifluoroacetate) of ruthenium (IV).Type: GrantFiled: November 5, 1987Date of Patent: October 10, 1989Assignee: Universite Du Maine (Le Mans)Inventors: Jean-Pierre Robin, Yannick Landais
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Patent number: 4687773Abstract: Antidopaminergic agents having selective limbic activity, comprising (S)-enantiomers of aporphine compounds of either the following structures: ##STR1## wherein R.sub.1 is lower alkyl, alkyl substituted lower alkyl, alkyl substituted cycloalkyl, lower alkenyl, alkyl substituted lower alkenyl, lower alkynyl, alkyl substituted lower alkynyl, phenyl lower alkyl, phenyl lower alkenyl, and phenyl lower alkynyl, and the following structure where R.sub.1 is above and R.sub.2 and R.sub.3 are hydrogen, methyl, or R.sub.1 ##STR2## R.sub.1 is as above R.sub.4 is H, CH.sub.3 lower alkyl, or R.sup.1 C0--where R.sup.1 =CH.sub.3 or lower alkyl.Type: GrantFiled: May 31, 1985Date of Patent: August 18, 1987Assignees: McLean Hospital, Northeastern UniversityInventors: John L. Neumeyer, Ross J. Baldessarini
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Patent number: 4591587Abstract: Novel cyclopropyl pyridine compounds useful as calcium channel blockers, pharmaceutical compositions thereof, and methods of treatment are disclosed.Type: GrantFiled: October 1, 1984Date of Patent: May 27, 1986Assignee: Merck & Co., Inc.Inventor: David C. Remy
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Patent number: 4590276Abstract: A novel process for the preparation of cyclopropyl pyridine compounds, which are useful as calcium channel blockers, is disclosed.Type: GrantFiled: October 1, 1984Date of Patent: May 20, 1986Assignee: Merck & Co., Inc.Inventor: Stella W. King
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Patent number: 4543256Abstract: A method for providing orally effective aporphine compounds, and new compounds which are orally effective in the prevention and treatment of duodenal ulcers and in the treatment of neurological and psychiatric disorders having the following formula ##STR1## wherein R.sub.1 is lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, phenyl lower alkyl, phenyl lower alkenyl and phenyl lower alkynyl, R.sub.2 and R.sub.3 are hydrogen, methyl, lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, phenyl lowerThe invention described herein was made in the course of work under a grant or award from the Department of Health and Human Services.Type: GrantFiled: May 18, 1982Date of Patent: September 24, 1985Assignee: Northeastern UniversityInventor: John L. Neumeyer
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Patent number: 4522946Abstract: 1,2,3,7,8,12b-Hexahydrobenzo[6,7]cyclohepta[1,2,3-de]isoquinoline derivatives, characterized by having two adjacent oxy substituents at positions 4 and 5 or at positions 5 and 6, are disclosed. Thus, the substituent at position 5 is lower alkoxy or hydroxy and the substituents at positions 4 and 6 are different and are hydrogen or hydroxy. The derivatives are neuroleptic agents, free of extrapyramidal side effects. Methods for the preparation and for the use of the derivatives also are disclosed.Type: GrantFiled: June 13, 1983Date of Patent: June 11, 1985Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Andre A. Asselin, Leslie G. Humber
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Patent number: 4461895Abstract: The present invention provides dibenzo(de,g)quinoline derivatives of the general formula: ##STR1## wherein R is an unsaturated aliphatic hydrocarbon radical containing up to 6 carbon atoms or a cycloalkylalkyl radical containing 4 to 6 carbon atoms; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for combating colds and allergies.Type: GrantFiled: May 7, 1982Date of Patent: July 24, 1984Assignee: Warner-Lambert CompanyInventors: Edgar Fritschi, Johannes Hartenstein, Wolfgang Heidt, Gerhard Satzinger
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Patent number: 4425350Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and are hydroxy, straight or branched-chain alkoxy of from 1 to 5 carbon atoms, phenoxy, benzyloxy, two adjacent groups may be methylenedioxy, or hydrogen provided R.sub.4 and R.sub.5 are not simultaneously hydrogen; R.sub.6 is hydrogen, straight or branched-chain alkyl of from 1 to 5 carbon atoms, straight or branched-chain alkenyl of from 2 to 5 carbon atoms, cycloalkylalkyl of from 4 to 7 carbon atoms, alkoxy carbonyl of from 2 to 6 carbon atoms, trifluoroacetyl, aralkyl of from 5 to 11 carbon atoms, or acyl which is derived from an aliphatic, araliphatic or aromatic carboxylic acid of from 1 to 11 carbon atoms; and the pharmaceutically acceptable salts thereof; excluding 5,6,6a,7-tetrahydro-1-hydroxy-2,9,10trimethoxy-5-methyl-4H-dibenz(de,g)-is oquinoline and 5,6,6a,7-tetrahydro-1,2,9,10-tetramethoxy-5-methyl-4H-dibenz(de,g)isoquino line.Type: GrantFiled: April 3, 1981Date of Patent: January 10, 1984Assignee: Warner-Lambert CompanyInventors: Johannes Hartenstein, Edgar Fritschi
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Patent number: 4358592Abstract: A crystalline form of d,l-glaucine phosphate is prepared by digesting d,l-glaucine phosphate with an alkanol. Glaucine phosphate has potent analgesic and antitussive properties, excellent flavor characteristics and stability properties and the new crystalline form has improved handling properties.Type: GrantFiled: February 2, 1981Date of Patent: November 9, 1982Assignee: The Dow Chemical Company & Merrell Dow Pharmaceuticals IncorporatedInventor: Christian T. Goralski
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Patent number: 4353912Abstract: N-substituted haloalkyl apomorphines of the formula ##STR1## wherein R.sub.1 is hydrogen or R.sub.2 O; R.sub.2 is hydrogen, acyl, lower alkyl or ##STR2## R.sub.3 and R.sub.4 are lower alkyl; and X is halogen; and their acid addition salts. Representative compounds have neuroleptic properties.Type: GrantFiled: May 8, 1980Date of Patent: October 12, 1982Assignee: Northeastern UniversityInventor: John L. Neumeyer
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Patent number: 4315010Abstract: Novel phosphate salts of 1 and d,l-glaucine are prepared by reacting 1 or d,l-glaucine base with phosphoric acid. The glaucine salts have potent analgesic and antitussive properties, excellent flavor characteristics and stability properties. Pharmaceutical compositions, and methods of using the same are also described.Type: GrantFiled: July 13, 1979Date of Patent: February 9, 1982Assignee: The Dow Chemical CompanyInventor: Samuel S. M. Wang
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Patent number: 4309542Abstract: A process for the O-methylation of hydroxyaporphines is disclosed. This process utilizes a trimethylphenylammonium base as the alkylating agent.Type: GrantFiled: December 19, 1978Date of Patent: January 5, 1982Assignee: Warner-Lambert CompanyInventors: Johannes Hartenstein, Gerhard Satzinger
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Patent number: 4302399Abstract: Acetylation of residual primary and secondary alkyl amine groups in polymeric colorants, when said colorants are in the form of a crude preparation reaction mixture, is disclosed. The acetylation improves the colorants' water solubility.Type: GrantFiled: March 10, 1980Date of Patent: November 24, 1981Assignee: DynapolInventors: Daniel J. Dawson, Robert E. Wingard, Guy A. Crosby
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Patent number: 4294834Abstract: Novel azocine derivatives and a method for their preparation are disclosed. The compounds display analgesic effects in mammals.Type: GrantFiled: November 13, 1979Date of Patent: October 13, 1981Assignee: Godecke AktiengesellschaftInventors: Johannes Hartenstein, Gerhard Satzinger, Heinrich Bahrmann, Volker Ganser
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Patent number: 4259329Abstract: Disclosed are 6-methylene-morphinan compounds corresponding to the formula: ##STR1## wherein R.sub.1 and R.sub.3 are H or methyl and R.sub.2 is cyclopropylmethyl or cyclobutylmethyl. These compounds are useful as mixed analgesics/narcotic antagonists.Type: GrantFiled: April 21, 1980Date of Patent: March 31, 1981Assignee: Miles Laboratories, Inc.Inventors: Michael P. Kotick, Joseph O. Polazzi
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Patent number: 4202980Abstract: A process for the preparation of 1-hydroxyaporphine derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.3 and R.sub.4, which are the same or different, are lower alkyl, aryl or aralkyl radicals or R.sub.3 and R.sub.4 can together form a lower alkylene bridge member and R.sub.2 is a hydrogen atom or a lower alkyl, aralkyl or alkoxycarbonyl radical or an acyl radical derived from an aliphatic, aromatic or araliphatic carboxylic acid.Type: GrantFiled: December 19, 1978Date of Patent: May 13, 1980Assignee: Warner-Lambert CompanyInventors: Johannes Hartenstein, Gerhard Satzinger
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Patent number: 4128650Abstract: Compounds of the formula: ##STR1## wherein the symbols X each represent hydrogen or methoxy, R represents hydrogen or carboxymethyl, the symbols R.sub.1 each represent hydrogen or together represent a valency bond and the symbols R.sub.2 each represent hydrogen or together represent a valency bond, the pair of symbols R.sub.2 having the same significance as the pair of symbols R.sub.1, and when the symbols R.sub.1 and R.sub.2 represent hydrogen the symbol X also represents hydrogen, are new compounds possessing antiviral activity.Type: GrantFiled: May 18, 1977Date of Patent: December 5, 1978Assignee: Rhone-Poulenc IndustriesInventors: Jean-Louis Fabre, Daniel Farge, Claude James
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Patent number: 4126616Abstract: N-Propylnorapomorphine dialkanoate, dibenzoate and dicyclopropanecarboxylate esters and acid-addition salts thereof, having anti-parkinson activity, are prepared by reaction of N-propylnorapomorphine with a respective alkanoyl, benzoyl or cyclopropanecarbonyl halide or corresponding acid anhydride in the presence of an acid acceptor.Type: GrantFiled: December 13, 1976Date of Patent: November 21, 1978Assignee: William B. HinshawInventors: William Banks Hinshaw, Jack Pearl