Patents Examined by Jane T. Fan
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Patent number: 5352796Abstract: Unnatural amino acids are provided which can be incorporated into peptides which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. These unnatural amino acids are useful in the synthesis of peptides and have the formula (a): ##STR1## where W is (CH.sub.2).sub.n or ##STR2## n is an integer from 1 to 6; j=1,2 or 3, and preferably, Y is N--CN, X is NH and R.sub.2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pyridyl; or the formula (b): ##STR3## where R.sub.11 is H or acyl and W is as defined in (a), and preferably R.sub.11 is H and W is ##STR4## Disclosed are peptides that are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.Type: GrantFiled: June 17, 1993Date of Patent: October 4, 1994Assignee: The Salk Institute For Biological StudiesInventors: Carl A. Hoeger, Jean E. F. Rivier, John S. Porter
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Patent number: 5342847Abstract: The invention relates to the new dimethyl 2,6-dimethyl-1-n-propyl-4-(trifluoro-methylphenyl)-1,4-dihydropyridine-3-d icarboxylate, a process for its preparation and its use as a medicament in ischaemic diseases which are associated with disorders of the microcirculation. This action can occur both in the peripheral and in the cerebral vascular system.Type: GrantFiled: January 16, 1993Date of Patent: August 30, 1994Assignee: Bayer AktiengesellschaftInventors: Otto Behner, Hartmund Wollweber, Siegfried Goldmann, Bruno Rosen, Siegfried Zaiss
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Patent number: 5340825Abstract: Novel pro-drugs ##STR1## the variables are as defined in the specification. New and unnatural dipeptoids of .alpha.-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the dipeptoids are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to the withdrawal from chronic treatment or with use of nicotine, diazepam, alcohol, cocaine, caffeine, or opioids. The pro-drugs are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the pro-drugs as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject pro-drug compounds in diagnostic compositions.Type: GrantFiled: July 12, 1991Date of Patent: August 23, 1994Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Martyn C. Pritchard, Reginald S. Richardson
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Patent number: 5332750Abstract: New 1,2-dihydro-2-oxopyridines of formula I ##STR1## in which R is the radical ##STR2## and R.sup.1 to R.sup.6 and X are as defined herein,and their salts, have antagonistic properties towards angiotensin II and can be used for the treatment of hypertension, aldosteronism and cardiac insufficiency.Type: GrantFiled: April 22, 1993Date of Patent: July 26, 1994Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Werner Mederski, Norbert Beier, Pierre Schelling, Ingeborg Lues, Klaus-Otto Minck
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Patent number: 5330994Abstract: A novel compound of the following formulas useful in treating immune-related diseases, inflammation, stoke, epilepsy, dystonias, psychoses, anxiety, and depression: ##STR1##Type: GrantFiled: March 24, 1992Date of Patent: July 19, 1994Assignee: Warner-Lambert CompanyInventors: Yazhong Pei, Haile Tecle
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Patent number: 5330997Abstract: Certain 1H-indazole-3-acetic acid derivatives, and their pharmaceutically-acceptable esters and salts, are inhibitors of the aldose reductase enzyme, and so are useful in the treatment of diabetic complications.Type: GrantFiled: February 24, 1993Date of Patent: July 19, 1994Assignee: Pfizer Inc.Inventors: Banavara L. Mylari, William J. Zembrowski
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Patent number: 5328925Abstract: The present invention relates to therapeutically active piperidine compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: August 15, 1991Date of Patent: July 12, 1994Assignee: Novo Nordisk A/SInventors: Per Sauerberg, Preben H. Olesen
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Patent number: 5328918Abstract: This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzheimer's disease and other memory disorders.Type: GrantFiled: March 25, 1993Date of Patent: July 12, 1994Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
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Patent number: 5328920Abstract: There are disclosed various compounds of the formula below, ##STR1## where R, R.sub.1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of neurotransmitter functions such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antiemetics, and for the treatment of personality disorders such as obsessive compulsive disorder.Type: GrantFiled: October 21, 1992Date of Patent: July 12, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin, Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 5328924Abstract: The present invention relates to therapeutically active azacyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: August 14, 1991Date of Patent: July 12, 1994Assignee: Novo Nordisk A/SInventors: Per Sauerberg, Preben H. Olesen
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Patent number: 5328923Abstract: The present invention relates to therapeutically active azacyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: August 13, 1991Date of Patent: July 12, 1994Assignee: Novo Nordisk A/SInventors: Per Sauerberg, Preben H. Olesen
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Patent number: 5326772Abstract: Optically pure diaryl compounds of formula I ##STR1## wherein the substituents and symbols have the meanings given int eh specification are proposed as active ingredients in medicaments for the treatment of tumors.Type: GrantFiled: May 7, 1992Date of Patent: July 5, 1994Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventors: Kurt Klemm, Wolf-Rudiger Ulrich, Dieter Flockerzi
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Patent number: 5321002Abstract: Herbicidal compounds, compositions containing them, and a method for controlling weeds by application of the compositions are disclosed. The herbicidal compounds are 2-(1-aryl-4-cyano-5-pyrazolylmethyleneiminooxy)alkanoic acid derivatives of the structure: ##STR1## in which R is lower alkyl, lower alkenyl, or lower alkynyl, each optionally substituted with halogen, or CH(R.sup.1)--C(O)--Y--R.sup.2 ; R.sup.1 is hydrogen or lower alkyl; R.sup.2 is one of a variety of substituents; Y is O or NH; Z is lower alkyl or lower alkoxy; and Ar is 3-chloro-5-trifluoromethyl-2-pyridyl, 2,6-dichloro-4-trifluoromethylphenyl, or 2,4,6-trichlorophenyl.Type: GrantFiled: August 11, 1993Date of Patent: June 14, 1994Assignee: FMC CorporationInventor: Lester L. Maravetz
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Patent number: 5314898Abstract: Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, psoriasis, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: June 29, 1992Date of Patent: May 24, 1994Assignees: Merck & Co., Inc., Merck Frosst Canada Inc.Inventors: John Y. L. Chung, Robert A. Reamer, Yves Girard, Pierre Hamel
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Patent number: 5314899Abstract: The present invention is directed to compounds, compositions and methods of treating pain, and derivatives that have potent analgetic activity. The compounds have the formula: ##STR1## wherein R.sup.1 is selected from H, lower alkyl, C.sub.3 -C.sub.9 cycloalkyl, acyl, and C.sub.3 -C.sub.9 cycloalkylalkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, or C.sub.3 -C.sub.8 cycloalkenyl or C.sub.3 -C.sub.8 cycloalkynyl; and wherein R is selected from cycloalkyl, aryl, heteroaryls (selected from the group consisting of pyridyl, thienyl, furanyl, imidazolyl, pyrazinyl, and pyrimidyl) or phenoxy and wherein said R groups can be substituted with hydroxyl, C.sub.1 -C.sub.6 lower alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 lower alkoxyl, halo, C.sub.1 -C.sub.6 haloalkyl, amino, C.sub.1 -C.sub.6 alkylamino and C.sub.2 -C.sub.10 dialkylamino, and sulfonamido or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 3, 1992Date of Patent: May 24, 1994Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: John W. Daly, Thomas F. Spande, Hugo M. Garraffo
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Patent number: 5310920Abstract: The present invention relates to novel N-vinylimidazolidine derivatives of the following formula (1), a process for producing them, an insecticide containing the derivatives as an effective ingredient, and novelintermediates. The derivatives (1) are useful as agricultural chemicals (particularly, as insecticides) in the fields of agriculture, and the intermediates are useful in various industrial fields, especially as intermediates for agricultural chemicals. ##STR1## where R.sup.1, R.sup.2, Z are as defined in the specification.Type: GrantFiled: December 15, 1992Date of Patent: May 10, 1994Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Kenji Kodaka, Michihiko Nakaya, Katsutoshi Kinoshita, Koichi Ebihara, Hirozumi Matsuno, Shirou Shiraishi, Kazutomi Ohnuma, Ei-ich Yamada
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Patent number: 5308855Abstract: Insecticidal guanidine derivatives of the formula ##STR1## wherein Z represents an optionally substituted five- or six-membered ring containing at least one ring hetero atom selected from the group consisting of oxygen, sulfur and nitrogen,R.sup.1 represents hydrogen atoms or a C.sub.1-4 alkyl group, R.sup.2 and R.sup.3 each independently represents hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl or optionally substituted phenyl,R.sup.4 and R.sup.5 each independently represents hydrogen, C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 alkynyl, optionally substituted benzyl or a group of the formula Z-C(R.sup.1)H-,n represents the integer 2 or 3, andY represents nitro or cyano.Type: GrantFiled: December 7, 1992Date of Patent: May 3, 1994Assignee: Nihon Bayer AgrochemInventors: Shin-ichi Tsuboi, Koichi Moriya, Yumi Hattori, Shinzaburo Sone, Katsuhiko Shibuya
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Patent number: 5308854Abstract: Novel aminopyridones inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: November 4, 1992Date of Patent: May 3, 1994Assignee: Merck & Co., Inc.Inventors: Jacob M. Hoffman, Jr., Walfred S. Saari, Clarence S. Rooney, John S. Wai
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Patent number: 5302605Abstract: Novel 3-picoline-N-oxides of formula I ##STR1## wherein R.sub.1 and R.sub.2 independently of each other are hydrogen or halogen, R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, n is the number two or three, and Y is nitrogen or the methine group, can be used as pesticides. Especially insects are controlled.Type: GrantFiled: September 11, 1991Date of Patent: April 12, 1994Assignee: Ciba-Geigy CorporationInventors: Odd Kristiansen, Laurenz Gsell, Peter Maienfisch
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Patent number: 5298520Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: January 28, 1993Date of Patent: March 29, 1994Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, Victor G. Matassa, Leslie J. Street