1,2-thiazoles (including Hydrogenated) Patents (Class 514/372)
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Patent number: 5998451Abstract: Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.Type: GrantFiled: May 6, 1991Date of Patent: December 7, 1999Assignee: Pfizer IncInventors: James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr.
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Patent number: 5990135Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: May 31, 1995Date of Patent: November 23, 1999Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing Leung Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5981550Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: May 22, 1998Date of Patent: November 9, 1999Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Thomas F. Walsh, Feroze Ujjainwalla, Matthew J. Wyvratt, Jr., Jonathan R. Young, Lin Chu
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Patent number: 5981528Abstract: The invention concerns a compound of formula (I): ##STR1## wherein R.sup.1 -R.sup.6, A, B, and D have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising such a compound or salt, and methods of treating a bacterial infection by administering such a compound or salt.Type: GrantFiled: October 21, 1997Date of Patent: November 9, 1999Assignee: Zeneca LimitedInventor: Michael Barry Gravestock
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Patent number: 5977149Abstract: Cyclic amides of Formula (I) which are useful as fungicides wherein: A is O; S; N; NR.sup.5 ;or CR.sup.14--, G is C or N; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, and R.sup.5 are independently, in part, C.sub.1 -C.sub.6 alkyl; Y is, in part, --O--; --S(O).sub.n --,--CHR.sup.6 O--; or --CHR.sup.6 O--N.dbd.C(R.sup.7)--; Z is, in part, optionally substituted cycloalkyl, phenyl, pyridinyl, pyrimidinyl, or naphthyl; and R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.14, m, and n are defined in the disclosure, are disclosed.Type: GrantFiled: January 14, 1998Date of Patent: November 2, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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Patent number: 5977147Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.Type: GrantFiled: April 24, 1996Date of Patent: November 2, 1999Assignee: Hoechst Marion RousselInventors: John Joseph Tegeler, Barbara Seavey Rauckman, Russell Richard Lee Hamer, Brian Scott Freed, Gregory Harold Merriman
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Patent number: 5977122Abstract: The present invention relates to novel 4,4-(disubstituted)cyclohexan-1-ols monomers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production to Tumor necrosis Factor (TNF).Type: GrantFiled: December 2, 1997Date of Patent: November 2, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
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Patent number: 5977148Abstract: A termiticidal composition containing a compound represented by the formula [I]; ##STR1## wherein R.sub.1 represents 2-chloro-5-pyridyl, 2-chloro-5-pyrazinyl, 2-methyl-5-pyrazinyl or 2-chloro-5-thiazolyl; R.sub.2 represents hydrogen, methyl, ethyl, methoxymethyl, cyclopropyl, propynyl or methoxy; R.sub.3 represents hydrogen or methyl or chloromethyl; and R.sub.4 represents cyano or nitro, or a salt thereof as an active ingredient.Type: GrantFiled: January 15, 1998Date of Patent: November 2, 1999Assignee: Nipppon Soda Co., Ltd.Inventors: Michihiko Matsuda, Renpei Hatano, Makio Yano
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Patent number: 5972937Abstract: The invention relates to heterocyclic families of compounds having pharmacological activity, in particular possessing 5HT.sub.2C receptor antagonist activity processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.Type: GrantFiled: September 16, 1997Date of Patent: October 26, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies
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Patent number: 5972981Abstract: There is provided a method for the production of improved biocidal compositions which comprise at least one 3-isothiazolinone of the general formula ##STR1## Y is a hydrogen atom or an unsubstituted alkyl radical having 1 to 18 carbon atoms, a cylo alkyl radical having 5 to 8 carbon atoms, an aralkyl radical having 7 to 11 carbon atoms or an aryl radical having 6 to 10 carbon atoms and R and R' are in each case a hydrogen atom or halogen atom or a C.sub.1 to C.sub.4 -alkyl radical, or, when taken together, R and R' contain an alkylene group to form a hydrocarbon ring, the 3-isothiazolinone being produced in known manner and then stabilized by the addition of a nitrate. The method is characterized by the fact that the mixture obtained upon the production of the 3-isothiazolinone is subjected to an additional stabilization after the addition of the nitrate by storing it at a pH of 0.2 to 2.0 and a temperature of at most 40.degree. C.Type: GrantFiled: April 30, 1997Date of Patent: October 26, 1999Assignee: Thor Chemie GmbHInventor: Rudiger Baum
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Patent number: 5972843Abstract: The present invention relates to novel acylated 5-aminoisothiazoles of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Y have the meaning given in the description, processes for their preparation and their use for controlling animal pests.Type: GrantFiled: May 11, 1998Date of Patent: October 26, 1999Assignee: Bayer AktiengesellschaftInventors: Markus Heil, Christoph Erdelen, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
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Patent number: 5972986Abstract: This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and treating epithelial cell neoplasia in a subject, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula I. ##STR1## wherein A, R.sup.2 and R.sup.3 are as described in the specification.Type: GrantFiled: October 14, 1997Date of Patent: October 26, 1999Assignee: G.D. Searle & Co.Inventors: Karen Seibert, Jaime Masferrer, Gary B Gordon
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Patent number: 5968974Abstract: This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.Type: GrantFiled: October 10, 1997Date of Patent: October 19, 1999Assignee: Merck & Co., Inc.Inventors: Stacia Kargman, Jilly Evans, Thomas J. Simon
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Patent number: 5965619Abstract: Substituted indene derivatives are useful for treating patients having precancerous lesions and for inhibiting the growth of neoplastic cells.Type: GrantFiled: December 23, 1997Date of Patent: October 12, 1999Assignee: Cell Pathways Inc.Inventors: Rifat Pamukcu, Gary A. Piazza, Paul Gross, Gerhard Sperl, Klaus Brendel
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Patent number: 5965565Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: December 11, 1997Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
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Patent number: 5961957Abstract: This invention pertains to the field of foam compositions for application to the skin of a user. More specifically, the invention relates to foam compositions that act as a barrier to water, allergens, poisons, toxins and other skin irritants when applied to the skin of a user.Type: GrantFiled: October 19, 1998Date of Patent: October 5, 1999Inventor: Bill H. McAnalley
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Patent number: 5958957Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.Type: GrantFiled: April 16, 1997Date of Patent: September 28, 1999Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
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Patent number: 5955486Abstract: Stable microbicidal compositions containing a 3-isothiazolone compound, chlorate or perchlorate salts, copper salts and water are disclosed. Also disclosed are methods of preventing or reducing precipitate formation in 3-isothiazolone compositions.Type: GrantFiled: February 13, 1998Date of Patent: September 21, 1999Assignee: Rohm and Haas CompanyInventor: John Robert Mattox
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Patent number: 5955491Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Type: GrantFiled: June 27, 1995Date of Patent: September 21, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
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Patent number: 5952359Abstract: A compound of formula (I),R--S(O).sub.n CH.sub.2 CH.sub.2 CH.dbd.CF.sub.2or a salt thereof, wherein n is 0, 1 or 2; and R is a group of formula (V) or (VII) ##STR1## wherein: at least one of R.sup.2, R.sup.3, R.sup.4 or R.sup.5 is a S(O)nCH.sub.2 CH.sub.2 CH.dbd.CF.sub.2 group; and the remainder of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, alkoxy, alkenyloxy, alkynyloxy, hydroxyalkyl, alkoxyalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxy, optionally substituted heteroarylalkoxy, optionally substituted heteroaryloxyalkyl, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, haloalkenyloxy, haloalkynyloxy, halogen, hydroxy, cyano, nitro, --NR.sup.7 R.sup.Type: GrantFiled: July 3, 1997Date of Patent: September 14, 1999Assignee: ZENECA LimitedInventors: Christopher Richard Ayles Godfrey, Matthew Brian Hotson, Nan Catherine Sillars, Alan John Dowling, Michael Drysdale Turnbull, Harjinder Singh Bansal, Allison Mary Smith, Roger Salmon, Steven Fitzjohn
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Patent number: 5952316Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.Type: GrantFiled: August 14, 1997Date of Patent: September 14, 1999Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Taito Co., Ltd.Inventors: Tetsuro Fujita, Shigeo Sasaki, Masahiko Yoneta, Tadashi Mishina, Kunitomo Adachi, Kenji Chiba
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Patent number: 5952354Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.Type: GrantFiled: July 21, 1993Date of Patent: September 14, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
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Patent number: 5944880Abstract: A wood preservative composition comprising a biocide such as a quaternary ammonium compound, e.g., didecyl-dimethyl ammonium chloride (DDAC), an isothiazolone or an isophthalonitrile, in combination with an antioxidant, e.g., a flavone or a phenol, is useful as a cost-effective and environmentally safe wood preservative. The invention also provides a method for the use of such composition and compositions so treated.Type: GrantFiled: January 26, 1998Date of Patent: August 31, 1999Assignee: Mississippi State UniversityInventors: Tor P. Schultz, Darrel D. Nicholas
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Patent number: 5942532Abstract: The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.Type: GrantFiled: September 5, 1997Date of Patent: August 24, 1999Assignee: Ortho Pharmaceutical CorporationInventors: Kwasi Adomako Ohemeng, Van Nhatton Nguyen
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Patent number: 5935985Abstract: We proposed a novel compound having an activity of PGI.sub.2 receptor agonist.A phenoxyacetic acid derivative of the formula ##STR1## A is --C(R.sup.1).dbd.N.about.OR.sup.2, --CH(R)NH--OR.sup.2, --COE, --SO.sub.2 E, --CH.sub.2 --NR.sup.3 --Y, --Z--NR.sup.3 --CONR.sup.4 R.sup.5, --CH.sub.2 --OR.sup.6, --CO.sub.2 R.sup.6, --CH.sub.2 --O.about.N.dbd.CR.sup.7 R.sup.8, --CH.sub.2 --O--NHCHR.sup.7 R.sup.8, substituted by imidazolyl(methyl), pyrazolylmethyl, oxazolyl(methyl), thioxazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolylmethyl;T is alkylene, alkenylene, etc.;D is --CO.sub.2 R.sup.10, --CONR.sup.11 R.sup.12 ;E is (substitution) amino, hydradino;Y is substituted (thio) carbonyl, substituted sulfonyl;Z is --CH.dbd.N--, --CH.sub.2 NR.sup.3 --;R.sup.1, R.sup.3, R.sup.10 --R.sup.13 is each H or alkyl, etc.;R.sup.2, R.sup.4 --R.sup.9 is each H, alkyl or alkyl substituted by phenyl or hetero ring ,etc. and non-toxic salts thereof, non-toxic acid addition salts thereof, possess an agonistic on PGI.sub.Type: GrantFiled: September 8, 1997Date of Patent: August 10, 1999Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5929099Abstract: A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals and can be used to treat viral infections that comprises a fungicide in combination with chemotherapeutic agents is disclosed. The particular fungicide used is a benzimidazole derivative. Potentiators can also be included in the composition.Type: GrantFiled: July 15, 1996Date of Patent: July 27, 1999Assignee: Procter & Gamble Co.Inventor: James Berger Camden
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Patent number: 5922745Abstract: A synergistic composition and method for inhibiting microbiological growth which comprises a combination of stabilized sodium hypobromite with a mixture of 5-chloro-2-methyl 4-isothiazolin-3-one and 2-methyl-4-isothiazolin-3-one.Type: GrantFiled: November 3, 1997Date of Patent: July 13, 1999Assignee: Nalco Chemical CompanyInventors: Robert E. McCarthy, Anthony W. Dallmier, William F. McCoy
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Patent number: 5922755Abstract: A 4H-1-benzopyran-4-one derivative of the general formura ?1!, ##STR1## or a salt thereof exerts excellent effects on immunomodulation and cell adhesion inhibition, and is further expected to have the effect of relieving autoimmune diseases at a level comparable to that of steroids. Thus, the compound of the general formula ?1! is useful in the teatment and prevention of autoimmune diseases fundamentally caused by immunopathy or unusually accelerated cell adhesion, for example, chronic rheumatoid arthritis, systemic lupus erythematosus, scleroderma, mixed connective tissue disease,polyarteritis nodosa, polymyositis/dermatomyositis, Sjogren's syndrome, Behcet's disease, multiple sclerosis, autoimmune diabetes, Hashimoto's disease, psoriasis, primary myxedema, pernicious anemia, serious adynamia, ulcerative colitis, chronic active hepatitis, autoimmune hemolytic anemia idiopathic thrombocytopenic purpura and the like.Type: GrantFiled: May 6, 1996Date of Patent: July 13, 1999Assignee: Toyama Chemical Co., Ltd.Inventors: Keiichi Tanaka, Shinji Makino, Ichiro Oshio, Tomoya Shimotori, Yukihiko Aikawa, Takihiro Inaba, Chosaku Yoshida, Shuntaro Takano, Yoichi Taniguchi
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Patent number: 5922744Abstract: The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.Type: GrantFiled: January 12, 1998Date of Patent: July 13, 1999Assignee: Merck Sharp & Dohme LimitedInventors: Timothy Harrison, Andrew Pate Owens
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Patent number: 5919786Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.Type: GrantFiled: March 25, 1998Date of Patent: July 6, 1999Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5919808Abstract: Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or "linker" defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15.ANG., are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.Type: GrantFiled: February 28, 1997Date of Patent: July 6, 1999Assignees: Zymogenetics, Inc., Osteoscreen, Inc.Inventors: Charles Petrie, Mark W. Orme, Nand Baindur, Kirk G. Robbins, Maria Kontoyianni, Gregory R. Mundy
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Patent number: 5919400Abstract: This invention relates to a stabilized isothiazolone solution and more particularly, to a stabilized isothiazolone solution comprising isothiazolone expressed by the following formula (I), stabilizer expressed by the following formula (II), and organic solvent diffusing these compounds effectively: ##STR1## In these formulae, n, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 have the same definitions as defined in the detailed description of this application, respectively.Type: GrantFiled: October 2, 1997Date of Patent: July 6, 1999Assignee: Sunkyong Industries Co., Ltd.Inventors: Seung Hwan Kim, Jin Soo Lim, Jin Man Kim, Myung Ho Cho
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5910503Abstract: Stable microbicidal compositions containing a 3-isothiazolone compound, metal nitrate, bromic acid, iodic acid, periodic acid, or their salts and water are disclosed. Also disclosed are methods of preventing or reducing precipitate formation in 3-isothiazolone compositions.Type: GrantFiled: February 13, 1998Date of Patent: June 8, 1999Assignee: Rohm and Haas CompanyInventors: John Robert Mattox, Ethan Scott Simon, Ramesh Balubhai Petigara
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Patent number: 5889058Abstract: Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof.Type: GrantFiled: November 3, 1994Date of Patent: March 30, 1999Assignee: Celltech LimitedInventors: John Robert Porter, Thomas Andrew Millican, John Richard Morphy, Nigel Robert Arnold Beeley
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Patent number: 5888721Abstract: The invention features two novel antibiotics, termed 15352A and 15352B, having the structures shown in the figures.Type: GrantFiled: July 3, 1996Date of Patent: March 30, 1999Assignee: Millennium Pharmaceuticals, Inc.Inventors: David Rothstein, Nagraj Mani, Zhi-Dong Jiang
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Patent number: 5888941Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.Type: GrantFiled: March 31, 1997Date of Patent: March 30, 1999Assignee: J. Uriach & Cia. S.A.Inventors: Javier Bartroli, Enric Turmo, Manuel Anguita
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Patent number: 5883252Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.Type: GrantFiled: January 26, 1996Date of Patent: March 16, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker
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Patent number: 5883106Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.Type: GrantFiled: February 6, 1998Date of Patent: March 16, 1999Assignee: Pfizer Inc.Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
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Patent number: 5882731Abstract: A method is disclosed for applying a mildewcide compound laden film to surfaces by applying an aqueous, film-depositing composition onto said surfaces, allowing to stand momentarily, and rinsing with water. After rinsing, a residual, durable, virtually invisible film remains. This film is mildew resistant, paintable and its sheen closely mimics that of the surfaces prior to application of the aqueous composition. The aqueous composition comprises a mildewcide compound, a non-ionic surfactant, water, and at least one film-former.Type: GrantFiled: July 23, 1997Date of Patent: March 16, 1999Inventor: Richard L. Owens
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Patent number: 5874464Abstract: Conformationally constrained diacylglycerol analogues, pharmaceutical compositions comprising such analogues, and methods of using such analogues as agonists and antagonists of protein kinase C.Type: GrantFiled: January 13, 1995Date of Patent: February 23, 1999Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Victor E. Marquez, Jeewoo Lee, Rajiv Sharma, Shaomeng Wang, George W. A. Milne, Marc C. Nicklaus, Peter M. Blumberg, Nancy E. Lewin
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Patent number: 5874476Abstract: Disclosed is a method of inhibiting the growth of microorganisms in, at, or on a locus subject to microbial attack, comprising introducing to said locus an antimicrobially effective amount of at least one dihaloformaldoxime carbamate.Type: GrantFiled: July 14, 1997Date of Patent: February 23, 1999Assignee: Rohm and Haas CompanyInventors: Adam Chi-Tung Hsu, Barry Clifford Lange, Jemin Charles Hsu
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Patent number: 5869510Abstract: A method paring a stable, dilute aqueous solution of at least one 3-isothiazolone compound comprising 5-chloro-2-methyl-3-isothiazolone, the concentration of said compound(s) in said solution being about 0.5 to 5% by weight based on solution, comprising introducing about 0.1 to 5% by weight based on said solution, of a ferric salt as the stabilizer is disclosed. Dilute aqueous solutions of about 0.5 to 5.0 parts by weight of at least one 3-isothiazolone compound comprising 5-chloro-2-methyl-3-isothiazolone, about 0.1 to 2.5 parts by weight of a stabilizing, water soluble, non-chelated ferric salt, and about 92 to 99 parts by weight of aqueous solvent, are also disclosed.Type: GrantFiled: January 15, 1993Date of Patent: February 9, 1999Assignee: Rohm and Haas CompanyInventor: John Robert Mattox
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Patent number: 5855899Abstract: A biocidal material comprises a biocide immobilized in a porous inorganic polymer network such as a sol-gel matrix. The polymer may be coated on an inorganic support. The material can be used for inhibiting microbial growth in an aqueous medium, e.g., the wash solution of a photoprocessing system. The material can be housed in a flow-through container.Type: GrantFiled: June 26, 1997Date of Patent: January 5, 1999Assignee: Eastman Kodak CompanyInventors: Gregory Nigel Batts, Karen Leeming, Christopher Peter Moore, Danielle Wettling
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Patent number: 5856503Abstract: Aminoalkyl-substituted benzo-heterocyclic compounds of the formula ##STR1## wherein M, Q, R and T are as defined in the specification, as well as acid addition salts thereof. These compounds are useful as cholesterol level lowering agents and as antimycotic agents.Type: GrantFiled: December 6, 1996Date of Patent: January 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Hans-Peter Marki, Hans Lengsfeld, Olivier Morand, Gerard Schmid, Yu-Hua Ji
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Patent number: 5855654Abstract: Disclosed is a method of inhibiting the growth of marine organisms on a marine structure, by applying dihydropyridazinone and pyridazinone compounds onto or into the marine structure. These compounds may be directly incorporated into the marine structure during manufacture, directly applied to the structure, or applied to the structure by means of a coating.Type: GrantFiled: December 9, 1997Date of Patent: January 5, 1999Assignee: Rohm and Haas CompanyInventors: Gary Lewis Willingham, Samuel Eugene Sherba, Barry Clifford Lange, Enrique Luis Michelotti
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Patent number: 5846993Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: December 8, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Bruce A. Dressman, James E. Fritz, Stephen W. Kaldor, Vincent J. Kalish, Siegfried Heinz Reich, John H. Tatlock, Michael J. Rodriguez
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Patent number: 5843972Abstract: The present invention relates to certain compounds of the formula (I) the racemic-enantiomeric mixtures and optical isomers of said compounds and the pharmaceutically acceptable salts or prodrugs thereof, depicted below, which are .beta.-adrenergic receptor agonists and accordingly have utility as, inter alia, hypoglycemic and antiobesity agents. More specifically, the compounds of the instant invention are selective agonists of .beta..sub.3 -adrenergic receptor. The invention also relates to methods of use for the compounds and to pharmaceutical compositions containing them. The compounds of the present invention also possess utility for increasing lean meat deposition and/or improving the lean meat to fat ratio in animals, e.g., ungulate animals, companion animals and poultry. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Y and Z are as defined in the specification.Type: GrantFiled: March 28, 1997Date of Patent: December 1, 1998Assignee: Pfizer Inc.Inventors: Robert L. Dow, Stephen W. Wright
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Patent number: RE36375Abstract: The present invention relates to therapeutically active azacyclic 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: February 18, 1998Date of Patent: November 2, 1999Assignee: Novo Nordisk A/SInventors: Per Sauerberg, Preben H. Olesen, Charles H. Mitch