Q Is Monocyclic Patents (Class 514/604)
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Patent number: 6498157Abstract: The present invention relates to a method of inhibiting or preventing infection and blood coagulation in or near a medical prosthetic device after said device has been inserted in a patient comprising administering to the device a pharmaceutically effective amount of a composition comprising: (A) at least one taurinamide derivative, and (B) at least one compound selected from the group consisting of biologically acceptable acids and biologically acceptable salts thereof, whereby there are no systemic anti-clotting and no systemic biocidal effects.Type: GrantFiled: November 30, 2001Date of Patent: December 24, 2002Assignee: Biolink CorporationInventor: Klaus Sodemann
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Patent number: 6495604Abstract: The present invention provides a compound represented by the formula: wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula: wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents, and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating diseaseType: GrantFiled: August 14, 2000Date of Patent: December 17, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Yuzo Ichimori, Masayuki Ii, Katsumi Itoh, Tomoyuki Kitazaki, Junji Yamada
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Patent number: 6482860Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.Type: GrantFiled: July 18, 1997Date of Patent: November 19, 2002Assignee: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
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Patent number: 6476064Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein a hatched line represents the &agr; configuration, a triangle represents the &bgr; configuration, a straight line, e.g.Type: GrantFiled: June 13, 2001Date of Patent: November 5, 2002Assignee: Allergan, Inc.Inventors: David W. Old, Robert M. Burk
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Patent number: 6472406Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 5, 2000Date of Patent: October 29, 2002Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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Patent number: 6472393Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: March 21, 2000Date of Patent: October 29, 2002Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
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Patent number: 6469040Abstract: 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. wherein A, R2 and R3 are as described in the specification.Type: GrantFiled: May 21, 2001Date of Patent: October 22, 2002Assignee: G.D. Searle & Co.Inventors: Karen Seibert, Jaime Masferrer, Gary B Gordon
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Patent number: 6462088Abstract: Liquid germicidal formulation containing, as the active ingredients, a combination of an alcohol and an organic N-chloroamine, which combination shows a high bactericidal activity and an unexpected stability in time, while maintaining its effectiveness substantially unchanged even after a prolonged storage. The formulation comprises, in water, chloramine-T or chloramine-B and one or more, aliphatic alcohols having up to 12 carbon atoms, preferably isopropanol, said solution having a pH not lower than 8.5.Type: GrantFiled: December 14, 2000Date of Patent: October 8, 2002Assignee: Eurospital S.p.A.Inventors: Antonello Russo, Hana Dannan
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Patent number: 6458845Abstract: Macrophage scavenger receptor antagonists are provided. Methods of treating cardiovascular disease comprising administration of the present compounds are also provided. The present compounds inhibit lipid accumulation within macrophage-derived foam cells.Type: GrantFiled: December 12, 2001Date of Patent: October 1, 2002Assignee: SmithKline Beecham CorporationInventors: Joseph Weinstock, Robert G. Franz, Dimitri E. Gaitanopoulos
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Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Patent number: 6436925Abstract: Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be aromType: GrantFiled: October 3, 2000Date of Patent: August 20, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Patent number: 6436914Abstract: Compounds are provided having the formula including pharmaceutically acceptable salts thereof, wherein R1 is lower alkyl, aryl or arylalkyl; A is hydrogen or B is hydrogen, alkyl, alkenyl, or but when A is hydrogen, B may only be R2, R2′, R2″, R3 R3′ and R3″ are as defined herein; m is 0−3. These compounds possess activity at the beta 3 adrenergic receptor in mammals and are useful in the treatment of diabetes, obesity, depression, achalasia and intestinal hypermotility disorders.Type: GrantFiled: July 25, 2001Date of Patent: August 20, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, William N. Washburn, Jollie D. Godfrey, Jr.
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Patent number: 6433017Abstract: In accordance with the present invention, there are provided amphiphilic polyamine compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: February 28, 2001Date of Patent: August 13, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
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Patent number: 6429317Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.Type: GrantFiled: September 5, 2000Date of Patent: August 6, 2002Assignee: Eli Lilly and CompanyInventors: Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
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Patent number: 6423691Abstract: A pharmaceutical composition for the prophylaxis and therapy of a disease arising from ocular fundus tissue cytopathy such as retinochoroidal disease, glaucoma, and posterior complication arising form photocoagulation, which contains, as an active ingredient, a compound of formula (I) wherein R1 represents an alkyl group having 1 to 4 carbon atoms or an aryl group having 6 to 10 carbon atoms which is optionally substituted; R2 and R3 may be the same or different and each represents hydrogen or an alkyl group having 1 to 4 carbon atoms or R2 and R3 may jointly form a ring having 3 to 7 carbon atoms; and R4 represents a lower alkyl group which substituted by aryl, cycloalkyl, or aromatic heterocyclic residue, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 5, 2000Date of Patent: July 23, 2002Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Mitsuyoshi Azuma, Yukuo Yoshida, Yuji Sakamoto, Jun Inoue
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Patent number: 6423751Abstract: A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell Nitric Oxide Synthase activity. As a result, agents that disrupt actin cytoskeletal organization are useful in treating or preventing conditions that result from the abnormally low expression and/or activity of endothelial cell Nitric Oxide Synthase. Such conditions include pulmonary hypertension, ischemic stroke, impotence, heart failure, hypoxia-induced conditions, insulin deficiency, progressive renal disease, gastric or esophageal motility syndrome, etc. Subjects thought to benefit mostly from such treatments include nonhyperlipidemics and nonhypercholesterolemics, but not necessarily exclude hyperlipidemics and hypercholesterolemics.Type: GrantFiled: July 14, 1998Date of Patent: July 23, 2002Assignee: The Brigham and Women's Hospital, Inc.Inventor: James K. Liao
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Patent number: 6414020Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: May 9, 2001Date of Patent: July 2, 2002Assignee: 3- Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6403630Abstract: Cancers associated with overexpression of HER-2/neu are treated with a selective inhibitor of cyclooxygenase-2 as the sole treating agent or said inhibitor in combination regimen with HERCEPTIN® and/or standard therapy. Uses include adjuvant therapy for HER-2/neu positive breast cancer and treatment of HER-2/neu positive breast cancer that has metastasized.Type: GrantFiled: June 22, 2001Date of Patent: June 11, 2002Assignee: Cornell Research Foundation, Inc.Inventors: Andrew J. Dannenberg, Kotha Subbaramaiah
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Patent number: 6395781Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),14(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.Type: GrantFiled: February 23, 1999Date of Patent: May 28, 2002Assignee: MCW Research FoundationInventors: Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
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Patent number: 6395737Abstract: New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.Type: GrantFiled: December 28, 1999Date of Patent: May 28, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Elisabeth Defossa, Uwe Heinelt, Otmar Klingler, Gerhard Zoller, Hans Matter, Fahad A. Al-Obeidi, Armin Walser, Peter Wildgoose
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Patent number: 6391918Abstract: Novel &agr;-amino acid amides of formula (I) as well as possible isomers and mixtures of isomers thereof, wherein the substituents are defined as follows: n is the number zero or one; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; or a group NRaRb wherein Ra and Rb are each independently of the other hydrogen, alkyl or form together an alkylene bridge; R2 is hydrogen or alkyl; R3 is optionally substituted aryl or heteroaryl; A is alkylene; and B is optionally substituted aryl; with the exception of the following compounds 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methylphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-chlorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-nitrolphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methoxyphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-fluorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-phenyl-sulfonylamino-acetamide and 2-phenyl-N-(1-pType: GrantFiled: August 25, 2000Date of Patent: May 21, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: André Jeanguenat, Martin Zeller
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Patent number: 6391877Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.Type: GrantFiled: November 8, 2000Date of Patent: May 21, 2002Assignee: Synaptic Pharmaceutical CorporationInventors: Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
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Patent number: 6388131Abstract: The invention provides compounds, compositions and methods relating to novel electrophilic aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: May 31, 2001Date of Patent: May 14, 2002Assignee: Tularik, Inc.Inventors: Julio Cesar Medina, David Louis Clark, John A. Flygare, Terry J. Rosen, Bei Shan
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Patent number: 6387954Abstract: The present invention provides certain alkenyl sulphonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: May 14, 2002Assignee: Eli Lilly and CompanyInventors: Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6388132Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: October 24, 2000Date of Patent: May 14, 2002Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6384080Abstract: Compounds of formula (I) where R1 is hydrogen; R2 is nitro, cyano or halo(lower)alkyl; R3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene group; R4 is a group CR6R7R8 wherein R6 and R7 form, together with the carbon atom to which they are attached a cycloalkyl group optionally substituted with hydroxy, lower alkoxy or a lower alkanoylamino; and R8 is hydrogen; its prodrug and a salt thereof.Type: GrantFiled: April 23, 2001Date of Patent: May 7, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Kozo Sawada, Akio Kuroda, Takayuki Inoue, Natsuko Kayakiri, Yuki Sawada, Tsuyoshi Mizutani
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Patent number: 6380199Abstract: A method of treating ADHD comprising administering a 5-HT6 receptor antagonist according to formula (A) hereinbelow: wherein: P is phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur; A is a single bond, a C1-6alkylene or a C1-6alkenylene group; R1 is halogen, C1-6alkyl optionally substituted by one or more halogen atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, nitro, amino, C1-6alkylamino or diC1-6alkylamino, cyano or R1 is phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur; n is 0, 1, 2, 3, 4, 5 or 6, R2 is hydrogen, C1-6 alkyl or aryl C1-6 alkyl; R3 is a group R5 or together with R5 forms a group (CH2)2O or (CH2)3O or R3 is linked to R2 to form a group (CH2)2 or (CH2)3; R4 is &mdashType: GrantFiled: April 17, 2001Date of Patent: April 30, 2002Assignee: SmithKline Beechan p.l.c.Inventors: Charles Alan Reavill, Carol Routledge
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Publication number: 20020045666Abstract: Liquid germicidal formulation containing, as the active ingredients, a combination of an alcohol and an organic N-chloroamine, which combination shows a high bactericidal activity and an unexpected stability in time, while maintaining its effectiveness substantially unchanged even after a prolonged storage. The formulation comprises, in water, chloramine-T or chloramine-B and one or more, aliphatic alcohols having up to 12 carbon atoms, preferably isopropanol, said solution having a pH not lower than 8.5.Type: ApplicationFiled: December 14, 2000Publication date: April 18, 2002Inventors: Antonello Russo, Hana Dannan
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Patent number: 6362230Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: November 21, 2000Date of Patent: March 26, 2002Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Dennis Michael Zimmerman, Ana Maria Escribano
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Patent number: 6350778Abstract: The present invention relates to cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives of formula I in which A(1), A(2), A(3), R(1), R(2), R(3), R(4), X, Y, and Z have the meanings indicated in the claims. Compounds of formula I are valuable pharmaceutical active compounds which exhibit, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency or cardiomyopathies, or for the prevention of sudden cardiac death, or for improving decreased contractility of the heart. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, and pharmaceutical preparations comprising them.Type: GrantFiled: May 19, 2000Date of Patent: February 26, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Heinrich Christian Englert, Klaus Wirth, Heinz Gögelein
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Patent number: 6348476Abstract: Pharmaceutical combination preparation of an inhibitor of the sodium/hydrogen exchanger and a medicament for the treatment of cardiovascular diseases. These combinations of an NHE inhibitor can comprise one or more therapeutically active compounds having cardiovascular activity. The combination of the cardioprotective properties with known therapies of cardiovascular diseases leads on the one hand to an improvement of the quality of the treatment and on the other hand in a large number of combinations to an additive or potentiated increase of the cardiovascular effects of the individual active compounds alone.Type: GrantFiled: July 5, 2000Date of Patent: February 19, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Wolfgang Scholz, Udo Albus
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Patent number: 6348499Abstract: Amphiphilic polyamide compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: November 24, 1999Date of Patent: February 19, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
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Patent number: 6342512Abstract: Sulfonylcarboxamide derivatives of formula I, their physiologically acceptable salts and/or physiologically functional derivatives, methods of making these compounds, their use for preparing medicines for the prevention and treatment of hyperlipidemia and arteriosclerotic disorders. The compounds of formula I have the following structure: in which the radicals are as defined and their physiologically acceptable salts and physiologically functional derivatives are described.Type: GrantFiled: September 1, 2000Date of Patent: January 29, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Reinhard Kirsch, Hans-Ludwig Schaefer, Eugen Falk, Horst Hemmerle
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Patent number: 6333349Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.Type: GrantFiled: June 29, 1999Date of Patent: December 25, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
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Patent number: 6319956Abstract: Nobel polyamine compounds and polyamine compounds having carcinostatic action are provided. There are also provided anticancer agents containing as active ingredient at least one of polyamine compounds represented by the following Formula (I) or (III) and/or pharmaceutically acceptable salts thereof. Specifically, there are provided anticancer agents containing as active ingredient at least one of 1,18-bis(ethylamino)-5,14-diazaoctadecane, 1,16-bis(cyclopropylmethylamino)-5,12-diazahexadecane, 1,17-bis(cyclopropylmethylamino)-5,13-diazaheptadecane and/or pharmaceutically acceptable salts thereof.Type: GrantFiled: December 20, 1999Date of Patent: November 20, 2001Assignee: RikenInventor: Masaaki Iwata
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Patent number: 6316496Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: February 1, 2000Date of Patent: November 13, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6316484Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: August 7, 2000Date of Patent: November 13, 2001Assignee: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
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Patent number: 6316503Abstract: The invention provides compounds, compositions and methods for modulating the effects of LXR in a cell. The compounds and compositions are useful both as diagnostic indicators of LXR function and as pharmacologically active agents. The compounds and compositions find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.Type: GrantFiled: March 14, 2000Date of Patent: November 13, 2001Assignee: Tularik Inc.Inventors: Leping Li, Julio C. Medina, Kevin Lustig, Bei Shan, Hirohiko Hasegawa, Serena T. Cutler, Jiwen Liu, Liusheng Zhu
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Patent number: 6288121Abstract: Nimesulide topical formulations are provided in the form of liquid crystals. The emulsifier cetylstearyl glycoside is used, and constituents of the lipid phase such as caprylic/capric triglycerides and jojoba oil, consistence factors such as cetylstearyl alcohol. Also disclosed is a process for the preparation thereof. The formulations have advantages such as higher stability, better release and absorption of nimesulide, and a higher bioavailability of the active ingredient.Type: GrantFiled: August 4, 1999Date of Patent: September 11, 2001Assignee: Helsinn Healthcare S.A.Inventors: Stefano Bader, Enrique Hausermann, Tiziana Monti
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Patent number: 6284795Abstract: The present invention provides compounds having the Formula I The present invention also provides methods of treating or preventing atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.Type: GrantFiled: August 18, 1999Date of Patent: September 4, 2001Assignee: Warner-Lambert CompanyInventors: Helen Tsenwhei Lee, Randy Ranjee Ramharack, Bruce David Roth, Karen Elaine Sexton
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Patent number: 6284923Abstract: The invention provides compounds, compositions and methods relating to novel electrophilic aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: August 22, 1997Date of Patent: September 4, 2001Assignee: Tularik INCInventors: Julio Cesar Medina, David Louis Clark, John A. Flygare, Terry J. Rosen, Bei Shan
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Patent number: 6271262Abstract: A compound of formula (I) useful as metalloproteinase inhibitors.Type: GrantFiled: January 11, 2000Date of Patent: August 7, 2001Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Fionna Mitchell Martin, Andrew Miller, Richard Simon Todd, Mark Whittaker
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Patent number: 6265446Abstract: Hydrazine derivatives of the formula wherein R1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R2 represents heterocyclyl or NR5R6, R3 represents hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl or aryl-lower alkyl, R4 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a grouping of the formula -Z-aryl, -Z-heterocyclyl or —(CH2)n—, CH═CR7R8, R5 and R6 each independently represent hydrogen or lower alkyl, R7 and R8 each independently represent hydrogen or lower alkyl or R7 and R8 together represent lower alkylene in which one CH2 group is optionally replaced by a hetero atom, X and Z each represType: GrantFiled: November 22, 1999Date of Patent: July 24, 2001Assignee: Hoffmann-La Roche Inc..Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
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Publication number: 20010004643Abstract: The invention discloses a safer Antiarrhythmic drug with controlled Beta Adrenergic activity which comprises a combination of dextro- and laevo-rotatory isomers of sotalol as active ingredients, pharmaceutical compositions with said combination as active ingredients and its preparation and use of the said combination in the treatment of cardiac ailments in mammals including human beings.Type: ApplicationFiled: December 19, 2000Publication date: June 21, 2001Inventor: Alangudi Sankaranarayanan
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Patent number: 6242493Abstract: Compounds of formula I: as well as pharmaceutically acceptable salts, hydrates and esters thereof, are disclosed. The compounds are useful for treating or preventing prostaglandin mediated diseases. Pharmaceutical compositions containing such compounds and methods of treatment are also included.Type: GrantFiled: March 10, 1999Date of Patent: June 5, 2001Assignee: Merck Frosst Canada & Co.Inventors: Yves Gareau, Marc LaBelle, Helene Juteau, Michel Gallant, Nicolas LaChance, Michel Belley
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Patent number: 6221914Abstract: The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.Type: GrantFiled: October 27, 1998Date of Patent: April 24, 2001Assignee: Array Biopharma Inc.Inventors: Laurence E. Burgess, James P. Rizzi
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Patent number: 6221898Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: August 29, 1997Date of Patent: April 24, 2001Assignee: Astra AktiebolagInventor: Thomas Antonsson
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Patent number: 6221888Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.Type: GrantFiled: November 29, 1999Date of Patent: April 24, 2001Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, William K. Hagmann, Malcolm Maccoss, Sander G. Mills, Richard A. Mumford
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Patent number: 6221907Abstract: The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.Type: GrantFiled: February 2, 1999Date of Patent: April 24, 2001Assignee: Hoechst Marion RousselInventors: Serge Bernard, Denis Carniato, Jean-Francois Gourvest, Jean-Georges Teutsch, Jochen Knolle, Hans-Ulrich Stilz, Volkmar Wehner, Sarah C. Bodary, Thomas R. Gadek, Robert S. McDowell, Robert M. Pitti
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Patent number: 6218435Abstract: A method of reducing hair growth in a mammal includes applying, to an area of skin from which reduced hair growth is desired, a dermatologically acceptable composition containing a suppressor of the metabolic pathway for the conversion of glucose to acetyl-CoA.Type: GrantFiled: July 17, 1998Date of Patent: April 17, 2001Inventors: James Henry, Gurpreet Ahluwalia, Douglas Shander