The Hetero Ring Is Six-membered Patents (Class 514/432)
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Publication number: 20090048261Abstract: The present invention is related to the pharmaceutical industry in general and in particular with the pharmaceutical industry of production of ophthalmic compositions. More specifically, the present invention relates to the pharmaceutical industry of production of ophthalmologic compositions for the treating of ocular hypertension. The advantage of the present invention against the present state of the technique is the fulfilling of a synergic effect of its components for the decreasing of ocular hypertension with no antagonistic effect between its components. The present invention consists of a pharmaceutical composition for the treatment of ocular hypertension characterized by comprising a pharmacologically effective amount of dorzolamide, with a pharmacologically effective amount of timolol and a pharmacologically effective amount of brimonidine.Type: ApplicationFiled: January 11, 2008Publication date: February 19, 2009Inventors: Jose Ruben Tornero Montano, Leopoldo Martin Baiza Duran, Juan De Dios Quintana Hau
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Publication number: 20090042907Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.Type: ApplicationFiled: June 20, 2008Publication date: February 12, 2009Applicants: Cephalon, Inc., Cephalon FranceInventors: Edward R. Bacon, Sankar Chatterjee, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet
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Patent number: 7485752Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: May 5, 2006Date of Patent: February 3, 2009Assignee: Hoffman-La Roche Inc.Inventor: Christophe Michoud
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Patent number: 7476673Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.Type: GrantFiled: December 17, 2004Date of Patent: January 13, 2009Assignee: Allergan, Inc.Inventors: Kwok Yin Tsang, Santosh Sinha, Xiaoxia Liu, Smita Bhat, Roshantha A. Chandraratna
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Patent number: 7470671Abstract: The invention relates to novel 5-thioxylose compounds, preferably derivatives of the 5-thioxylopyranose type, to the method for their preparation and to their use as active principles of drugs intended especially for the treatment or prevention of thromboses or cardiac insufficiency.Type: GrantFiled: September 24, 2004Date of Patent: December 30, 2008Assignee: Laboratoire FournierInventors: Véronique Barberousse, Soth Samreth, Benaïssa Boubia, François Bellamy, Vincent Peyrou
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Patent number: 7468360Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.Type: GrantFiled: August 8, 2007Date of Patent: December 23, 2008Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20080312310Abstract: Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders, for example, by modulating the activity of KSP, are disclosed.Type: ApplicationFiled: September 27, 2007Publication date: December 18, 2008Inventors: Han-Jie Zhou, Andrew McDonald
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Publication number: 20080306136Abstract: The invention provides compounds of formula I: useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: April 1, 2008Publication date: December 11, 2008Inventors: Shon R. Pulley, John A. Tucker
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Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
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Publication number: 20080234320Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.Type: ApplicationFiled: March 25, 2008Publication date: September 25, 2008Inventors: James P. Snyder, Matthew C. Davis, Brian Adams, Mamoru Shoji, Dennis C. Liotta, Eva M. Ferstl, Ustun B. Sunay
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Publication number: 20080226716Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.Type: ApplicationFiled: May 28, 2008Publication date: September 18, 2008Applicant: XenoPortInventors: Mark Gallop, Kenneth C. Cundy, Randall A. Scheuerman, Ronald W. Barrett, Noa Zerangue
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Publication number: 20080214652Abstract: The current invention relates to methods for treating hyperlipidemia in mammals, including humans. More specifically, the current invention relates to the use of retinoid or retinoid derivative that is able to act as an antagonist or inverse agonist of a retinoid receptor to treat hyperlipidemia.Type: ApplicationFiled: February 27, 2008Publication date: September 4, 2008Inventors: Yang-Dar Yuan, Scott M. Thacher, Elliott S. Klein, Roshantha A. Chandraratna
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Patent number: 7420002Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.Type: GrantFiled: June 11, 2002Date of Patent: September 2, 2008Assignee: XenoportInventors: Mark Gallop, Kenneth C. Cundy, Randall A. Scheuerman, Ronald W. Barrett, Noa Zerangue
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Publication number: 20080207696Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: November 21, 2007Publication date: August 28, 2008Inventors: Jose Aquino, Varghese John, John Tucker, Roy Hom, Shon Pulley, Ruth Tenbrink
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Patent number: 7417057Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)?C(R7)N(R8)—, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)?C(R12)C(R13)?C(R14) 1 12, —, where R,R,R 6, R 7, R8, R I1, R R 13, R 14, and X are described.Type: GrantFiled: April 28, 2003Date of Patent: August 26, 2008Assignee: Bayer Cropscience AGInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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Patent number: 7417059Abstract: The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases such as, cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, and septic shock.Type: GrantFiled: March 31, 2005Date of Patent: August 26, 2008Assignee: Takeda Pharmacetical Company LimitedInventors: Norikazu Tamura, Takashi Ichikawa, Masayuki Ii
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Patent number: 7414072Abstract: There is provided a 5-thio-?-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.Type: GrantFiled: August 8, 2003Date of Patent: August 19, 2008Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Hiroyuki Kakinuma, Hajime Asanuma
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Substituted Benzo-Condensed Cycloheptanone Derivatives and the Use Thereof for Medicament Production
Publication number: 20080161352Abstract: The invention relates to substituted benzo-condensed cyclohexanone derivatives, to a method for the production thereof, to medicaments containing said derivatives and to the use of the inventive compounds for producing medicaments.Type: ApplicationFiled: May 17, 2006Publication date: July 3, 2008Applicant: Gruenenthal GmbHInventors: Robert Frank, Michael Przewosny, Ruth Jostock -
Publication number: 20080159955Abstract: Therapeutic methods for inhibiting the growth of preneoplastic/neoplastic vertebrate cells that abnormally express MN protein are disclosed. Screening assays are provided for identifying compounds, preferably organic compounds, preferably aromatic and heterocylic sulfonamides, which inhibit the enzymatic activity of MN/CA IX and that are useful for treating patients with preneoplastic/neoplastic disease. Further, the CA IX-specific inhibitors when labeled or linked to an appropriate visualizing means can also be used diagnostically/prognostically for preneoplastic/neoplastic disease, and for imaging use, for example, to detect hypoxic precancerous cells, tumors and/or metastases, by selectively binding to activated CA IX, preferably CA IX activated under hypoxic conditions, and not to inactive CA IX. Such detection of hypoxic conditions can be helpful in determining effective treatment options, and in predicting treatment outcome and the prognosis of disease development.Type: ApplicationFiled: October 30, 2007Publication date: July 3, 2008Inventors: Claudiu Supuran, Andrea Scozzafava, Silvia Pastorekova, Jaromir Pastorek
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Publication number: 20080161354Abstract: The present invention relates to stable S-nitrosothiols derivatives of formula (I) having vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparation of medicaments for treatment of NO related diseases. The invention also relates to a process for the synthesis of the compounds of formula (I).Type: ApplicationFiled: March 1, 2007Publication date: July 3, 2008Applicant: LACER, S.A.Inventors: Jose Repolles Moliner, Francisco Pubill Coy, Marisabel Mourelle Mancini, Juan Carlos del Castillo Nieto, Lydia Cabeza Llorente, Juan Martinez Bonin, Ana Modolell Saladrigas
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Publication number: 20080132563Abstract: The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.Type: ApplicationFiled: January 10, 2006Publication date: June 5, 2008Inventors: Hiroyuki Kakinuma, Yuko Hashimoto, Takahiro Oi, Hitomi Takahashi
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Patent number: 7351742Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: January 19, 2005Date of Patent: April 1, 2008Assignee: Pfizer Inc.Inventors: Alan Daniel Brown, Kim James, Charlotte Alice Louise Lane, Ian Brian Moses, Nicholas Murray Thomson
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Publication number: 20080058389Abstract: The invention relates to novel carboxamides of formula (I), in which M represents a phenyl ring, pyridine ring or pyrimidine, pyridazine or pyrazine ring, respectively monosubstituted by R8, or represents a thiazole ring substituted by R8-A; R8 represents hydrogen, fluorine, chlorine, methyl, isopropyl, methylthio or trifluoromethyl; R8 can also represent methoxy; R8-A represents hydrogen, methyl, methylthio or trifluoromethyl; L1 represents C1-C10 alkene (alkanediyl); Q represents O, S, SO, SO2 or NR9; L2 represents a direct bond, SiR10R11 or CO; R represents hydrogen, C1-C8 alkyl, C1-C8 alkoxy, C1-C4 alkoxy-C1-C4-alkyl, C1-C4 alkylthio-C1-C4-alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C1-C6 haloalkyl, C2-C6-haloalkenyl, C2-C6 haloalkynyl or C3-C6 cycloalkyl; A represents the group of formula (AI); the remaining substituents are defined in claim 1.Type: ApplicationFiled: January 22, 2005Publication date: March 6, 2008Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Benoit Hartmann, Jorg Nico Greul, Stefan Herrmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Patent number: 7338971Abstract: This invention provides for the treatment of inflammatory, cancer and thrombotic disorders through the administration, in combination, of a COX2 inhibitor, low dose aspirin, and antioxidant flavanoids, flavonoids or isoflavones and at least one of these combinations will be given in a subtherapeutic amount for improved anti-inflammatory, anti-cancer, and anti-thrombotic efficacy and safety.Type: GrantFiled: August 30, 2001Date of Patent: March 4, 2008Inventors: Mawaheb M. El-Naggar, Ahmed S. Mousa
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Patent number: 7329654Abstract: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.Type: GrantFiled: December 2, 2002Date of Patent: February 12, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Ramesh M. Kanojia, Nareshkumar F. Jain, Raymond Ng, Zhihua Sui, Jiayi Xu
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Patent number: 7317125Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: January 31, 2006Date of Patent: January 8, 2008Assignee: Hoffman-La Roche Inc.Inventors: David Robert Bolin, Christophe Michoud
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Patent number: 7294650Abstract: Compounds of formula (I): and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective ?2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).Type: GrantFiled: December 15, 2004Date of Patent: November 13, 2007Assignee: Glaxo Group LimitedInventor: Keith Biggadike
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Patent number: 7282502Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: March 28, 2006Date of Patent: October 16, 2007Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C. B. Harriman, Zhan Shi, Chen Shaowu
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Publication number: 20070232653Abstract: The present invention relates to a process for the preparation of cis substituted cyclic ?-aryl or heteroaryl carboxylic acid derivatives in high diastereo- and enantioselectivity by enantioselective hydrogenation in accordance with the following scheme wherein X, Ar, n, and m are defined herein and corresponding salts thereof.Type: ApplicationFiled: March 30, 2007Publication date: October 4, 2007Inventors: Stephan Bachmann, Michelangelo Scalone, Patrick Schnider
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Publication number: 20070185055Abstract: The present invention relates to a method of treatment of cachexia in a subject in need of treatment. More specifically, the present invention relates to the use of retinoid compounds that act on retinoid X receptors (RXRs) for the treatment of cachexia in a subject in need of treatment. The cachexia is associated with, in other words a complication of, a primary disease, condition or disorder. Primary diseases, conditions and disorders include, but are not limited to, cancer, AIDS, liver cirrhosis, diabetes mellitus, chronic renal failure, chronic obstructive pulmonary disease, chronic cardiac failure, immune system diseases (e.g., rheumatoid arthritis and systemic lupus erythematosus), tuberculosis, cystic fibrosis, gastrointestinal disorders (e.g., irritable bowel syndrome and inflammatory bowel disease), Parkinson's disease, anorexia nervosa, dementia, major depression, an aged condition and sarcopenia.Type: ApplicationFiled: February 6, 2006Publication date: August 9, 2007Inventors: Guang Liang Jiang, Yang-Dar Yuan, Roshantha A. Chandraratna
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Publication number: 20070172522Abstract: Disclosed is a method for stabilizing a pharmaceutically active bi-cyclic compound of formula (i): comprising the step of: admixing the same with a polyol and/or a fatty acid ester other than glyceride and a composition obtained by the method. In addition a soft gelatin capsule formulation of the compound of formula (I) obtained by incorporating the compound in a soft gelatin capsule shell comprising gelatin and a polyol plasticizer.Type: ApplicationFiled: January 23, 2007Publication date: July 26, 2007Applicant: R-TECH UENO, LTD.Inventors: Ryu Hirata, Yasuhiro Harada
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Patent number: 7244725Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and RC are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.Type: GrantFiled: September 10, 2003Date of Patent: July 17, 2007Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn CompanyInventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth TenBrink
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Patent number: 7241810Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: March 21, 2005Date of Patent: July 10, 2007Assignee: Pfizer IncInventors: Alan Daniel Brown, Mark Edward Bunnage, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Paul Alan Glossop, Kim James, David Anthony Price
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Patent number: 7229988Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: GrantFiled: June 5, 2003Date of Patent: June 12, 2007Assignee: Samsung Electronics Co., Ltd.Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
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Patent number: 7214701Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: June 25, 2004Date of Patent: May 8, 2007Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7138411Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I? wherein X, A1, A2, A3, A4, R, R?, R1 and R2 are as described in the specification.Type: GrantFiled: November 22, 2002Date of Patent: November 21, 2006Assignee: G.D. Searle & Co.Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan Raj Nagarajan, Cathleen E Hanau, Susan J Hartmann, Cindy L Ludwig, Suzanne Metz, Donald E Korte
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Patent number: 7125907Abstract: This invention provides new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, inhibiting angiogenesis, effecting a TGF-? activity or a neuronal activity, and treating a glutamate abnormality, a compulsive disorder, neuropathy, pain, a prostate disease, cancer, Huntington's disease, diabetes, a retinal disorder or glaucoma.Type: GrantFiled: March 3, 2004Date of Patent: October 24, 2006Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Takashi Tsukamoto
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Patent number: 7115277Abstract: A method for enabling deliver of an active agent is provided which includes the preparation of doses of the active agent distributing educational materials and guidelines for counseling patients with regard to what the patients need to know and what the patients must do in order to both avoid adverse side effects while taking the dose and to receive prescriptions for the doses.Type: GrantFiled: December 2, 2002Date of Patent: October 3, 2006Assignee: Allergan, Inc.Inventors: Bruce A. Firestone, Thao Tran, Teresa G. Joshi
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Patent number: 7115632Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.Type: GrantFiled: May 11, 2000Date of Patent: October 3, 2006Assignee: G. D. Searle & Co.Inventors: Louis J Bedell, Joseph J McDonald, Thomas E Barta, Daniel P Becker, Rao N Shashidhar, John N Freskos, Brent V Mischke, Daniel P Getman, Gary A DeCrescenzo, Clara I Villamil
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Patent number: 7105566Abstract: The invention provides in one embodiment a method for treating vascular trauma. The method can include administering to an individual undergoing vascular trauma an effective amount of a retinoic acid receptor (RAR) antagonist or an RAR inhibitor. The methods can be used to lower serum triglycerides in a patient undergoing an invasive vascular procedure such as vascular surgery.Type: GrantFiled: October 22, 2002Date of Patent: September 12, 2006Assignee: Allergan, Inc.Inventors: Roshantha A. Chandraratna, Yang-Dar Yuan, Tuong P. Dang, Sheng Z. Loh
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Patent number: 7105518Abstract: The present invention provides compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein R1 and R2 are independently hydrogen, an option ally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and R3 is an optionally substituted C3-20 heterocyclyl or C5-20 aryl group, and their use as pharmaceuticals, particularly in treating diseases which are retroviral mediated or ameliorated by the inhibition of DNA-PK,Type: GrantFiled: August 14, 2002Date of Patent: September 12, 2006Assignee: Cancer Research Technology LimitedInventors: Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Roger John Griffin, Bernard Thomas Golding, Ian Robert Hardcastle, Laurent Jean Martin Rigoreau, David Richard Newell, Hilary Alan Calvert, Nicola Jane Curtin, Paul Workman, Florence Irene Raynaud, Bernard Paul Nutley
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Patent number: 7074819Abstract: The present invention relates to a novel benzopyran or thiobenzopyran derivative represented by formula (1): pharmaceutically acceptable salt or stereoisomer thereof, in which X, R1, R2, R3, R4 and A are defined as described in the specification, and to a process for preparation thereof and a pharmaceutical composition having anti-estrogenic activity which contains the compound (1) as an active component.Type: GrantFiled: August 12, 2003Date of Patent: July 11, 2006Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Jae Chon Jo, Hyun Suk Lim, Jong Min Kim, Ju Su Kim, Kazumi Morikawa, Yoshitake Kanbe, Myung Hwa Kim, Masahiro Nishimoto
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Patent number: 7053115Abstract: The present invention relates to a novel crystalline form of dorzolamide hydrochloride, to processes for its preparation and a pharmaceutical composition containing it.Type: GrantFiled: April 7, 2003Date of Patent: May 30, 2006Assignee: Hetero Drugs LimitedInventors: Reddy Bandi Parthasaradhi, Reddy Kura Rathnakar, Reddy Rapolu Raji, Reddy Dasari Muralidhara, Reddy Itiyata Srinivas
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Patent number: 7053109Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: July 10, 2002Date of Patent: May 30, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
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Patent number: 6992101Abstract: The present invention provides compounds of formula (I) the prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs, wherein R?, R?, R??, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof in treating diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, and tissue ischemia.Type: GrantFiled: November 6, 2003Date of Patent: January 31, 2006Assignee: Pfizer, Inc.Inventors: Donald L. Bussolotti, Ronald B. Gammill, Jana Polivkova
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Patent number: 6916831Abstract: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(?O)R6, —O(C?O)OR6; and —O(C?O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.Type: GrantFiled: February 24, 2003Date of Patent: July 12, 2005Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
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Patent number: 6908934Abstract: Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia ?and (b) Formula Ib are novel LXR agonists and are useful in the treatment of dyslipidemic conditions particularly depressed levels of HDL cholesterol.Type: GrantFiled: May 30, 2002Date of Patent: June 21, 2005Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Aileen Bouffard, James F. Dropinski, Clare E. Gutteridge, A. Brian Jones, Weiguo Lui, John George Ondeyka, Ali Shiafee, Sheo Bux Singh
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Patent number: 6890937Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical.Type: GrantFiled: January 7, 2003Date of Patent: May 10, 2005Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrezcenzo, Theresa R. Fletcher, John N. Freskos, Daniel P. Getman, Gunnar J. Hanson, Susan L. Hockerman, Carol P. Howard, Stephen A. Kolodziej, Madeleine H. Li, Joseph J. McDonald, Deborah A. Mischke, Patrick B. Mullins, Joseph G. Rico, Nathan W. Stehle, Clara I. Villamil
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Patent number: 6884813Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein A is a structure i, ii, iii, or iv X is CR7; Y is —S(?O)n—, —S(?NR8)—, or —S(?NR8)(?O)—; Z is —NHC(?O)R1, —NHC(?S)R1, —NR-het1, —O-het1, —S-het1, or -het2; and n is independently 0, 1, or 2. The compounds of formula I are useful as antimicrobials against a number of human and veterinary pathogens.Type: GrantFiled: January 21, 2003Date of Patent: April 26, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Adam Renslo, Gary W. Luehr, Stuart Lam, Neil E. Westlund, Dinesh V. Patel
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Patent number: 6881742Abstract: Novel benzamidoxime derivatives, processes and intermediates for their preparation and their use as fungicides are described. In the context of the present invention, benzamidoxime derivatives are compounds of the formula I where: A is an aryl or hetaryl radical; Y is a straight-chain or branched C1-C4-alkylene group, where one carbon can be replaced by oxygen, nitrogen or sulfur or by a cyclopropyl group; Rn1 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy; R2 is unsubstituted or substituted phenyl-C1-C6-alkyl, thienyl-C1-C4-alkyl, or pyrazolyl-C1-C4-alkyl, Rp3 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy, C1-C6-alkylcarbonyl; n is 0-5; p is, depending on the number of free valencies, 0-4.Type: GrantFiled: October 5, 2000Date of Patent: April 19, 2005Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Karl Eicken, Ingo Rose, Thomas Grote, Eberhard Ammermann, John-Bryan Speakman, Siegfried Strathmann, Gisela Lorenz