Z Radical Contains Nitrogen Patents (Class 514/551)
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Patent number: 6495597Abstract: Compounds of formula (I) wherein R4 is an ester or thioester group and R, R1, R2 and R3 are as defined in the specification, inhibit proliferation of tumor cells.Type: GrantFiled: October 5, 2000Date of Patent: December 17, 2002Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Andrew Paul Ayscough, Lisa Marie Pratt, Alan Hastings Drummond
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Publication number: 20020188022Abstract: Disclosed is a method for inhibiting, stimulating, modulating, or regulating glutamate reuptake. The method makes use of compounds that are ligands of glutamate receptors, including many agonists, or antagonists of glutamate receptors. It has been discovered that such compounds can bind to or modulate glutamate transporters and affect extracellular glutamate levels by affecting transporter activity. The disclosed compounds can have a variety of effects on glutamate transporter activity including activation or inhibition. Such compounds are useful to treat various neurological diseases and conditions involving glutamate transporter and glutamate receptor activation. For example, excess extracellular glutamate is a cause of excessive activation of glutamate receptors. Stimulating glutamate reuptake by glutamate transporters can ameliorate excessive activation of glutamate receptors by reducing the extracellular glutamate concentration. Prodrug forms of transporter compounds can be used as drugs.Type: ApplicationFiled: October 30, 2001Publication date: December 12, 2002Applicant: Annovis. Inc.Inventors: Maria-Luisa Maccecchini, Xue-Feng Pei
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Patent number: 6492420Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.Type: GrantFiled: December 21, 1999Date of Patent: December 10, 2002Assignee: PhotoCure ASInventors: Karl E. Gierskcky, Johan Moan, Qian Peng, Harald Steen, Trond Warloe, Alf Bjorseth
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Publication number: 20020183386Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N-CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.Type: ApplicationFiled: June 7, 2002Publication date: December 5, 2002Inventors: Karl E. Gierskcky, Johan Moan, Qian Peng, Harald Steen, Trond Warloe, Alf Bjorseth
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Patent number: 6476243Abstract: Perfluorinated esters of alkanoyl-L-carnitine of the formula (I): are useful as cationic lipids for the intracellular delivery of pharmacologically active compounds.Type: GrantFiled: September 27, 2000Date of Patent: November 5, 2002Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Mosè Santaniello, Lucia Critelli, Nazareno Scafetta, Maria Grazia Cima, Maria Ornella Tinti, Claudio Pisano, Andrea Pucci
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Publication number: 20020156129Abstract: The object of the present invention is to provide a pharmaceutical composition for treatment of pruritus not associated with dermal inflammation such as pruritus caused by the decrease of cutaneous barrier function. Particularly, the object of the present invention is to provide a pharmaceutical composition, comprising at least one substances having the inhibitory function of NO activity in vivo, such as the inhibitory activity for NO biosynthesis and/or at least one substances having the eliminating activity for NO and a pharmaceutically acceptable carrier.Type: ApplicationFiled: October 17, 2001Publication date: October 24, 2002Inventors: Yasushi Kuraishi, Takayuki Miyamoto
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Publication number: 20020128301Abstract: Non-nucleoside reverse transcriptase inhibitors of formula (P-1) wherein: Ar1 is an unsaturated, optionally substituted, mono or bicyclic ring structure comprising 0 to 3 hetero atoms selected from S, O and N; Ar2 is an aromatic, optionally substituted, monocyclic ring structure comprising at least one nitrogen hetero atom and zero to two further hetero atoms selected from S, O and N; R4 and R5 are independently H or C3-C8 cycloalkyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C5 alkoxy, C1-C4 alkanoyloxy, C1-C4 alkylthio, amino, carboxy, carbamoyl, cyano, halo, hydroxy, aminomethyl, hydroxymethyl, carboxymethyl, or halo substituted C1-C6 alkyl mercapto, nitro; or R4 and RS join to form a 3-6 membered, optionally substituted ring structure; R6 is 0 or S; Rx is the residue of a natural or unnatural amino acid; and L* is a linker moiety which is ether-, carbonate- or ester-bound to the adjacent oxygen and ester linked to Rx; and pharmaceutically acceptable salts thereof are anti-HIV agents with favourable phType: ApplicationFiled: August 10, 2001Publication date: September 12, 2002Inventors: Xiao-Xiong Zhou, Nils-Gunnar Johansson, Horst Wahling, Christian Sund, Lourdes Salvador, Stefan Lindstrom, Hans Wallberg, Christer Sahlberg
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Patent number: 6444657Abstract: The present invention relates to methods of using NAALADase inhibitors to regulate TGF-&bgr; and to treat neurodegenerative disorders, extracellular matrix formation disorders, cell-growth related diseases, infectious diseases, immune related diseases, epithelial tissue scarring, collagen vascular diseases, fibroproliferative disorders, connective tissue disorders, inflammatory diseases, respiratory distress syndrome and infertility.Type: GrantFiled: October 22, 1999Date of Patent: September 3, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Xi-Chun May Lu, Krystyna Wozniak
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Patent number: 6441035Abstract: Heteroatom-interrupted HETE derivatives and methods of their use for treating dry eye are disclosed.Type: GrantFiled: June 25, 2001Date of Patent: August 27, 2002Assignee: Alcon Universal Ltd.Inventors: Raymond E. Conrow, Peter G. Klimko
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Publication number: 20020115721Abstract: Disclosed are prodrug compounds of a class of alkyl carboxy amino acid analogs of glutamic acid that act as specific regulators of the kainate EAA receptor cation channel. These compounds are useful for treating neurological, neuropsychological, neuropsychiatric, neurodegenerative, neuropsychopharmacological and functional disorders associated with excessive or insufficient activation of the kainate subtype of the ionotropic EAA receptors; treating cognitive disorders associated with deactivation, suboptimal activation or over-activation of the kainate receptor; alleviating pain and improving and enhancing memory, learning, and associated mental processes.Type: ApplicationFiled: October 30, 2001Publication date: August 22, 2002Applicant: Annovis, Inc.Inventors: Xue-Feng Pei, Maria-Luisa Maccecchini
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Publication number: 20020099092Abstract: GABA-related pro-drugs of the formula (III) are provided that when administered to humans or other mammals provide an increased duration of active compound in the plasma compared to compounds of corresponding structure in which labile groups are not present.Type: ApplicationFiled: August 1, 2001Publication date: July 25, 2002Inventors: David Clive Blakemore, Justin Stephen Bryans, Sophie Caroline Williams
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Publication number: 20020091092Abstract: The present invention relates to the use of propionyl L-carnitine and the pharmaceutically acceptable salts thereof for the preparation of medicaments useful in the treatment of pathologies whose treatment gains a benefit from inducement of apoptosis, in particular blood vessels, such as restenosis after angioplasty or coronary stenting, or in particular tumors.Type: ApplicationFiled: May 7, 2001Publication date: July 11, 2002Inventors: Menotti Calvani, Claudio Pisano
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Patent number: 6417234Abstract: Nordihydroguaiaretic acid derivatives and methods of use thereof for the treatment of tumors.Type: GrantFiled: October 16, 2000Date of Patent: July 9, 2002Assignee: Johns Hopkins UniversityInventors: Ru Chih C. Huang, Jonathan D. Heller, Jih Ru Hwu, Ke Yung King
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Publication number: 20020065316Abstract: The present invention relates to novel active compounds named Citrullimycines, which are obtainable by cultivation of Streptomyces sp. ST 101396 (DSM 13309), and to their pharmaceutically acceptable salts and derivatives. The present invention further relates to a process for the production of the Citrullimycines, to the microorganism Streptomycetes sp. ST 101396 (DSM 13309), to the use of the Citrullimycines and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, for example as inhibitors of the neurotensin receptor, and to pharmaceutical compositions comprising Citrullimycines or a pharmaceutically acceptable salt or derivative thereof.Type: ApplicationFiled: October 1, 2001Publication date: May 30, 2002Inventors: Cordula Hopmann, Michael Kurz, Mark Bronstrup, Joachim Wink
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Publication number: 20020037898Abstract: The invention involves methods and compositions useful in delivering micronutrients to cells. By formulating the micronutrient in the form of an ester that is convertible to the active form of the micronutrient, one can combine it with a co-ester that inhibits esterases, so that the micronutrient can reach the targeted cells prior to degradation. Both methods and compositions are described.Type: ApplicationFiled: April 11, 2001Publication date: March 28, 2002Inventors: Elaine L. Jacobson, Myron K. Jacobson, Jaber G. Qasem, Hyuntae Kim, Moonsun kim
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Patent number: 6353012Abstract: HETE derivatives and methods of their use for treating dry eye are disclosed.Type: GrantFiled: October 23, 2000Date of Patent: March 5, 2002Assignee: Alcon Universal Ltd.Inventors: Mark R. Hellberg, John M. Yanni, Gustav Graff, Daniel A. Gamache, Peter G. Klimko
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Patent number: 6350782Abstract: The present invention provides methods for treating a cellular disorder in a mammal which is induced by elevated levels of ceramide by administering a basic amino acid, acylated basic amino acid, or a pharmaceutically acceptable salt thereof to effectuate lowering the ceramide levels in the mammal.Type: GrantFiled: April 27, 2000Date of Patent: February 26, 2002Assignees: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Mendes S.r.l.Inventor: Sonia Moretti
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Publication number: 20020019416Abstract: 1 The present invention relates to a novel fatty acid derivative of formula (I), wherein R1 is acyl group; R2 is acyl(lower)alkyl; R3 is hydrogen, aryl(lower)alkyl, etc.; R4 is acyl(lower)alkyl; and X is —O—, —NH— or formula (II) [wherein R5 is lower alkyl, etc.]; and a pharmaceutically acceptable salt thereof, which is useful as a medicament; the processes for the preparation of said fatty acid derivative or a salt thereof; a pharmaceutical composition comprising said fatty acid derivative or a pharmaceutically acceptable salt thereof; etc.Type: ApplicationFiled: April 20, 1998Publication date: February 14, 2002Inventors: NAOKI FUKAMI, SEIJI YOSHIMURA, KEISUKE IMAI, KEIJI HEMMI, MITSUE HEMMI, KEIICHIRO HEMMI, YUSUKE HEMMI
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Patent number: 6346547Abstract: Low-toxicity, highly-bioavailable, pharmaceutical antioxidant compositions for preferred oral administration to mammals are provided which have at least one amino acid-based compound of the general formula (I): A—N(Z)—CH(R1)C(O)—Q (I) wherein A is represented by the formula: XO—[C(R2)2]n— wherein n is an integer of from 1 to about 3, X is selected from the group consisting of a hydrogen atom, an acyl group and a halogenated acyl group and each R2 is independently selected from the group consisting of a hydrogen atom, an alkyl group having from 1 to about 3 carbon atoms, a hydroxyalkyl group having from 1 to about 3 carbon atoms, and CH2OX; Z is selected from the group consisting of a hydrogen atom, an alkyl group of from 1 to about 3 carbon atoms, and A; R1 is an amino acid side chain group or an amino acid side chain group which forms with R2 a single heterocyclic structure having a total of from 5 to 7 atoms in the ring; and wherein Q is a substituent sType: GrantFiled: February 8, 2000Date of Patent: February 12, 2002Assignee: Checkpoint, Genetics, Inc.Inventor: Nathan Tzodikov
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Publication number: 20020016366Abstract: The present invention is directed towards compounds of the general formula (I) 1Type: ApplicationFiled: April 25, 2001Publication date: February 7, 2002Inventor: Gunter Knaup
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Publication number: 20020013344Abstract: This invention relates to the method of using specially formulated neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity to stimulate or promote neuronal growth or regeneration.Type: ApplicationFiled: October 31, 1995Publication date: January 31, 2002Inventors: JOSEPH P. STEINER, GREGORY S. HAMILTON
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Publication number: 20020013364Abstract: Process for treating psychosis such as schizophrenia using glycine-site full agonists or a precursor thereof.Type: ApplicationFiled: May 27, 1999Publication date: January 31, 2002Inventor: DANIEL C. JAVITT
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Publication number: 20020010176Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.Type: ApplicationFiled: July 28, 2001Publication date: January 24, 2002Inventors: Ben C. Askew, Paul J. Coleman, Mark E. Duggan, Wasyl Halczenko, George D. Hartman, Cecilia A. Hunt, John H. Hutchinson, Robert S. Meissner, Michael A. Patane, Garry R. Smith, Jiabing Wang
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Patent number: 6337349Abstract: Solid and non hygroscopic salts consisting of lower alkanoyl L-carnitine magnesium citrates are disclosed which are suitable for preparing solid composition useful as dietary/nutritional supplements for human use and as fodder supplement for veterinary purposes.Type: GrantFiled: September 24, 1999Date of Patent: January 8, 2002Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Nazareno Scafetta, Maria Ornella Tinti
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Publication number: 20010053795Abstract: The present invention relates to a method of treatment of a disease comprising the step of administering to an animal a paradoxical pharmacologic agent, wherein the agent restores compensatory mechanisms or activates redundant mechanisms. More particularly, the invention relates to methods of treatment for hypertension.Type: ApplicationFiled: June 20, 2001Publication date: December 20, 2001Inventor: Richard A. Bond
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Publication number: 20010051743Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.Type: ApplicationFiled: December 21, 1999Publication date: December 13, 2001Inventors: KARL E. GIERSKCKY, JOHAN MOAN, QIAN PENG, HARALD STEEN, TROND WARLOE, ALF BJORSETH
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Patent number: 6306905Abstract: The present invention relates to stable aqueous formulations of the insect repellent ethyl 3-(N-butyl-acetamino)propionate.Type: GrantFiled: July 23, 1999Date of Patent: October 23, 2001Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Thekla Kurz, Sabine Hitzel, Dorothee Wille, Mohammad Jalalian
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Patent number: 6306881Abstract: Compounds of general formula (I) wherein R4 is an ester or thioester group and R, R1, R2, and R3 are as specified in the description, inhibit intracellular Leukotriene A4 hydrolase activity and are therefore of value for the treatment of inflammatory disease.Type: GrantFiled: July 21, 1999Date of Patent: October 23, 2001Assignee: British Biotech PharmaceuticalsInventors: Andrew Paul Ayscough, Mark Whittaker
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Patent number: 6303569Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms.Type: GrantFiled: August 21, 1998Date of Patent: October 16, 2001Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe, Annapurna Pendri
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Patent number: 6217914Abstract: An ascorbic acid-based composition and related method for the treatment of aging or photo-damaged skin is disclosed. The composition includes water and ascorbic acid, at least a portion of which has generally been pretreated by being dissolved under relatively high temperature and concentration conditions. The composition typically includes at least about 5.0% (w/v) ascorbic acid and may advantageously be formulated to have a pH above 3.5. Generally, the composition also includes non-toxic zinc salt, tyrosine compound, and/or pharmaceutically acceptable carrier. In addition, the composition may include an anti-inflammatory compound, such as aminosugar and/or sulfur-containing anti-inflammatory compound. The topical composition may be in the form of a serum, a hydrophilic lotion, an ointment, a cream, or a gel.Type: GrantFiled: July 19, 1999Date of Patent: April 17, 2001Assignee: Bioderm, Inc.Inventor: Lorraine Faxon Meisner
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Patent number: 6214874Abstract: A method for using nordihydroguiaretic acid derivatives, in particular tetramethyl nordihydroguiaretic acid and tetraglycinal nordihydroguiaretic acid, for the localized treatment of tumors induced by human papillomavirus.Type: GrantFiled: October 15, 1999Date of Patent: April 10, 2001Assignee: John Hopkins UniversityInventors: Ru Chih C. Huang, Jonathan D. Heller
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Patent number: 6207710Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis.Type: GrantFiled: September 30, 1998Date of Patent: March 27, 2001Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: James E. Audia, Thomas C. Britton, James J. Droste, Beverly K. Folmer, George W. Huffman, Varghese John, Lee H. Latimer, Thomas E. Mabry, Jeffrey S. Nissen, Warren J. Porter, Jon K. Reel, Eugene D. Thorsett, Jay S. Tung, Jing Wu
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Patent number: 6207173Abstract: Lysine derivatives, salts of the derivatives, their optical isomers of D or L configuration, or their mixtures, the derivatives containing an Ne-alkoxy or Ne-alkenoxycarbonyl group and having the formula: in which: R represents a linear or branched C13-C24 alkyl radical or alkenyl radicals, are used in cosmetic, pharmaceutical, hygiene or food compositions, particularly compact compositions.Type: GrantFiled: April 23, 1999Date of Patent: March 27, 2001Assignee: L'OrealInventors: Michel Philippe, Thierry Bordier
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Patent number: 6201020Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using compounds of the formula: A is O or S; R is C1-C10 straight or branched chain alkyl, C2-C10 straight or branched chain alkenyl, C2-C10 straight or branched chain alkynyl, aryl, heteroaryl, carbocycle, or heterocycle; D is a bond, or a C1-C3 straight or branched chain alkyl, C2-C3 straight or branched chain alkenyl, C2-C3 straight or branched chain alkynyl, wherein any of the carbon atoms of said alkyl, alkenyl, or alkynyl of D are optionally replaced with oxygen, nitrogen, or sulfur; and X is aryl, heteroaryl, carbocycle, or heterocycle.Type: GrantFiled: December 31, 1998Date of Patent: March 13, 2001Assignee: Guilford Pharmaceuticals, Inc.Inventors: Jie Zhang, Larisa E. Serdyuk, Jia-He Li
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Patent number: 6201023Abstract: A method for protecting a crop against plant-parasitic nematode attack by inducing local and systemic resistance of the crop comprising the application of a composition containing an effective amount of &bgr;-amino butyric acid or derivatives thereof to the crop or its locus.Type: GrantFiled: June 10, 1997Date of Patent: March 13, 2001Assignee: Agrogene Ltd.Inventors: Yuji Oka, Yitzhak Spiegel, Yigal Cohen
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Patent number: 6194458Abstract: This invention relates to benzamide potassium channel inhibitors of general structural Formula I. The compounds of this invention are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and related afflictions, diseases and illnesses, and cardiac arrhythmias. Also within the scope of this invention are pharmaceutical formulations comprising a compound of Formula I and a pharmaceutical carrier, as well as pharmaceutical formulations comprising a compound of Formula I, one or more immunosuppressive compounds and a pharmaceutical carrier.Type: GrantFiled: October 21, 1999Date of Patent: February 27, 2001Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Jianming Bao, Frank Kayser, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
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Patent number: 6191117Abstract: Methods are disclosed for the acute and chronic treatment of obesity using drugs whose mechanism includes the interaction and antagonism of the kainate/AMPA receptor. Methods are disclosed for employing the drug topiramate (topomax) as monotherapy or in combination therapy with lamotrigene, valproic acid, valproic acid and carbamezepine combination, or felbamate (felbatol).Type: GrantFiled: July 10, 2000Date of Patent: February 20, 2001Inventor: Walter E. Kozachuk
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Patent number: 6184252Abstract: Topically applicable hair growth-/hair loss-affecting cosmetic/pharmaceutical compositions for treating mammalian subjects with hair or scalp disorders, comprise an effective amount of at least one 2-amino-1,3-alkanediol compound having the structural formula (I): formulated into a physiologically topically acceptable carrier medium therefor.Type: GrantFiled: February 18, 1997Date of Patent: February 6, 2001Assignee: Societe L'Oreal S.A.Inventors: Dominique Fagot, Olivier Gaillard, Michel Philippe, Bruno Bernard
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Patent number: 6174885Abstract: A [6-(substituted-methyl)-3-cyclohexenyl]formamide derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C10-30 expressed by R1 and the other is—(CH2)n-NR2R3; Z is —O—, —OCO—, —OCONR6— or —NR6—; R2 and R3 individually represent a hydrogen, lower alkyl, phenyl or benzyl group, or together represent a heterocycle having 3-7 members; —NR5—(CH2)n-NR2R3 or —NR6—(CH2)n-NR2R3 may be Group W, and —OCONR6—(CH2)n-NR2R3 may be —OCO—W, wherein W is a formula of: wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R2 is a hydrogen, lower alkyl, phenyl or benzyl group; R4 is a halogen, lower alkyl, lower acyl, nitro, cyano, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, lower alkylamino, lower acylamino, lower alkoxy or lower acyloxy group; each of R5 and R6 is a hydrogen, lowType: GrantFiled: February 26, 1999Date of Patent: January 16, 2001Assignee: Shiseido Co., Ltd.Inventors: Hirotada Fukunishi, Tsunao Magara, Koji Kobayashi
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Patent number: 6159988Abstract: Compounds of formula I, ##STR1## and the physiologically tolerable salts thereof, wherein the substituents R.sub.1 -R.sub.4 have the meanings given in the specifications and show an activity against inflammatory conditions.Type: GrantFiled: June 29, 1998Date of Patent: December 12, 2000Assignee: Hoeschst AktiengesellschaftInventors: Ramachandra Ganapati Naik, Vilas Narayan Mumbaikar, Ravishankar Vasumathy, Aftab Dawoodbhai Lakdawala, Mandakini Bipin Alreja, Bansi Lal, Jurgen Blumbach, Klaus Ulrich Weithmann, Robert Ryder Bartlett, Kalpana Sanjay Joshi, Swati Bal-Tembe, Sadagopan Raghavan
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Patent number: 6147068Abstract: A pharmaceutical composition of matter for delivering nitric oxide. The composition is an amine that was reacted with nitric oxide. The composition of matter is lipophilic and insoluble and therefore delivers nitric oxide to the specific area of the body where it is introduced. Also, a method of synthesizing an amine and reacting it with nitric oxide to form the pharmaceutical composition of matter. Finally, a method of using the pharmaceutical composition of matter to deliver nitric oxide to the body.Type: GrantFiled: September 21, 1998Date of Patent: November 14, 2000Assignee: The University of AkronInventors: Daniel J. Smith, Dominick Roselle
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Patent number: 6136804Abstract: The invention provides a method for treating, preventing, or reducing the risk of developing a condition selected from the group consisting of acute coronary ischemic syndrome, thrombosis, thromboembolism, thrombotic occlusion and reocclusion, restenosis, transient ischemic attack, and first or subsequent thrombotic stroke, in a patient, comprising administering to the patient a therapeutically effective amount of an antiplatelet agent in combination with a therapeutically effective amount of a COX-2 inhibitor. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a COX-2 inhibitor, or a pharmaceutically acceptable salt thereof, and an antiplatelet agent, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 12, 1999Date of Patent: October 24, 2000Assignee: Merck & Co., Inc.Inventor: Steven A. Nichtberger
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Patent number: 6130315Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.Type: GrantFiled: August 24, 1998Date of Patent: October 10, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: H. Michael Kolb, Joseph P. Burkhart, Michael J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
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Patent number: 6124345Abstract: The present invention relates to carbomoylcarboxamide oximes of the formula (I): ##STR1## or salts thereof, processes for preparing the carbomoylcarboxamide oximes, compositions containing the carbomoylcarboxamide oximes and processes for controlling harmful fungi with an effective amount of the carbomoylcarboxamide oximes.Type: GrantFiled: November 24, 1998Date of Patent: September 26, 2000Assignee: BASF AktiengesellschaftInventors: Frank Wetterich, Karl Eicken, Reinhard Kirstgen, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6114382Abstract: The present invention provides novel compositions and methods relating to the treatment of Inflammatory Bowel Disease ("IBD"), most notably, Ulcerative Colitis, Crohn's Disease, Colitis and Diverticulitis. The invention relates to the discovery of a parasitic microsporidia infecting the epithelium cells lining the gastrointestinal tract of patients suffering from IBD. The discovery of this correlation between the disease and the microsporidia, described herein, led to the development of methods for the accurate diagnosis of patients suffering from IBD, and also of methods for treating such a patient in accordance with the invention. This discovery also provides for the development of animal models to further elucidate the mechanism of the disease and potential additional cures therefor.Type: GrantFiled: November 11, 1998Date of Patent: September 5, 2000Inventor: Itagiba G. Moretti
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Patent number: 6114385Abstract: The therapeutic use of basic amino acids, acylated basic amino acids and their pharmacologically acceptable salts is disclosed for the treatment of a cellular disorder in a mammal which is induced by elevated levels of ceramide.Type: GrantFiled: February 3, 1998Date of Patent: September 5, 2000Assignees: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Mendes s.r.l.Inventor: Sonia Moretti
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Patent number: 6083986Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: July 15, 1997Date of Patent: July 4, 2000Assignees: ICAgen, Inc., Eli Lilly & CompanyInventors: Neil Alexander Castle, Sean Patrick Hollinshead, Philip Floyd Hughes, Jose Serafin Mendoza, Joseph Wendell Wilson, George Salvatore Amato, Serge Beaudoin, Michael Gross, Grant McNaughton-Smith
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Patent number: 6080786Abstract: Stable and non-hygroscopic salts consisting of L-carnitine or alkanoyl-L-carnitine choline tartrate are disclosed. The salts are suitable for preparing solid compositions useful as dietary/nutritional supplements for human use and as fodder supplement for veterinary purposes.Type: GrantFiled: October 8, 1999Date of Patent: June 27, 2000Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Mose Santaniello, Nazareno Scafetta, Maria Ornella Tinti
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Patent number: 6075051Abstract: A method for protecting a crop against fungal diseases by inducing local and systemic resistance of the crop comprising applying to the crop or its locus a composition containing an effective amount of at least one .beta.-aminobutyric acid or .beta.-amino valeric acid and salts and derivatives thereof.Type: GrantFiled: October 29, 1998Date of Patent: June 13, 2000Assignee: Agrogene Ltd.Inventor: Yigal Cohen
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Patent number: 6063820Abstract: A medical food for diabetics is disclosed which comprises as characterizing active ingredients .gamma.-linolenic acid and at least one alkanoyl-L-carnitine, e.g. acetyl-L-carnitine and/or propionyl-L-carnitine.Type: GrantFiled: March 18, 1998Date of Patent: May 16, 2000Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventor: Claudio Cavazza