1,2-thiazoles (including Hydrogenated) Patents (Class 514/372)
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Patent number: 7115624Abstract: The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.Type: GrantFiled: September 11, 2000Date of Patent: October 3, 2006Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Thomas Kruse Hansen, Lars Fogh Iversen, Jesper Lau, Niels Peter Hundahl Møller, Ole Hvilsted Olsen, Frank Urban Axe, Yu Ge, Daniel Dale Holsworth, Todd Kevin Jones, Luke Milburn Judge, Wiliam Charles Ripka, Barry Zvi Shapira, Roy Teruyuki Uyeda
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Patent number: 7115605Abstract: PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: April 5, 2004Date of Patent: October 3, 2006Assignee: SmithKline Beecham CorporationInventors: Kelly M. Aubart, Siegfried B. Christensen, IV, Jacques Briand, Maxwell David Cummings
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Patent number: 7115600Abstract: This invention is directed to a compound of the formula I as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by modulating histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising aType: GrantFiled: January 28, 2005Date of Patent: October 3, 2006Assignee: Pfizer Inc.Inventors: Travis T. Wager, Ramalakshmi Y. Chandrasekaran
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7087599Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: February 14, 2001Date of Patent: August 8, 2006Assignee: Merck & Co., Inc.Inventors: Dann LeRoy Parker, Jr., Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
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Patent number: 7083801Abstract: Antimicrobial compositions based on haloalkynyl active ingredients that are chemically stable in the presence of chelated metal ion are disclosed. Particularly preferred is the use of metal ion chelating agents based on selected amine compounds that provide the metal ion in a form sufficient to provide stability to other antimicrobial components in the aqueous composition, but without concurrently degrading the antimicrobial effectiveness of the haloalkynyl active ingredient.Type: GrantFiled: June 24, 2003Date of Patent: August 1, 2006Inventors: Beverly Jean El A'mma, Susan Lynn Nagahashi
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Patent number: 7074776Abstract: Compounds of the structure I: are useful for treating bacterial growth, wherein E is selected from the group consisting of B, P, and S, T1 and T2 are each independently selected from the group consisting of O, NR, and CH2, where R?H or C1–C8 alkyl, or C1–C8 oxoalkyl, and L is selected from the group consisting of ethylene, propylene, and four to six-membered alicyclic and aromatic rings, provided that structure I does not include AI-2-borate. The compounds may be used to treat bacterial infections in human beings and to regulate biofilm formation. Pharmaceutical compositions comprising one or more such compounds are useful for treating bacterial infections in human beings.Type: GrantFiled: October 1, 2003Date of Patent: July 11, 2006Assignee: Quorex Pharmaceuticals, Inc.Inventors: Stephen R. Cooper, Kraig M. Yager
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Patent number: 7067538Abstract: The present invention relates to sulfones that are useful in the treatment of chemokine-mediated disorders. In certain embodiments, the present invention concerns the compounds that are MCP-1 receptor antagonists.Type: GrantFiled: May 21, 2003Date of Patent: June 27, 2006Assignee: Warner-Lambert Company, LLCInventors: Larry D. Bratton, Alexander J. Bridges, David T. Connor, Steven R. Miller, Yuntao Song, Kuai-Lin Sun, Bharat K. Trivedi, Paul C. Unangst
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Patent number: 7045660Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: GrantFiled: March 3, 2004Date of Patent: May 16, 2006Assignee: Aventis Pharma LimitedInventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
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Patent number: 7041694Abstract: Selective inhibitors of cyclooxygenase-2 are used to treat liver disease and in combination with anti-viral drugs to treat virus-caused liver disorders. Selective inhibitors of cyclooxygenase-2 which also inhibit the synthesis of cyclooxygenase-2 improve over the efficacy of conventional selective inhibitors of cyclooxygenase-2 in the treatment of inflammatory conditions, Alzheimer's disease and cancer.Type: GrantFiled: December 7, 1998Date of Patent: May 9, 2006Assignee: Cornell Research Foundation, Inc.Inventor: Andrew J. Dannenberg
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Patent number: 7030147Abstract: Epothilone derivatives are co-administered with an antidiarrheal agent, e.g., a DPP-IV inhibitor, in the treatment of a proliferative disease.Type: GrantFiled: March 18, 2002Date of Patent: April 18, 2006Assignee: Novartis AGInventors: John David Rothermel, Horst F. Schran, Diane Greeley, TianLing Chen
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Patent number: 7008545Abstract: Synergistic mixtures of biocides and their use to control the growth of microorganisms in aqueous systems are disclosed. The method of using the synergistic mixtures entails adding an effective amount of a nitrogenous compound activated by an oxidant and at least one non-oxidizing biocide to an aqueous system. The amount of activated nitrogenous compound and non-oxidizing biocide is selected to result in a synergistic biocidal effect.Type: GrantFiled: October 8, 2002Date of Patent: March 7, 2006Assignee: Hercules IncorporatedInventors: John M. Cronan, Jr., Michael J. Mayer
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Patent number: 6989451Abstract: Substituted isothiazole compounds and compositions are provided, wherein particularly preferred compositions and methods are directed towards inhibition of various protein kinases (especially MEK and/or ERK). Consequently, particularly preferred methods include treatment of diseases associated with abnormality in MEK and/or ERK function.Type: GrantFiled: June 4, 2003Date of Patent: January 24, 2006Assignee: Valeant Research & DevelopmentInventors: Weijian Zhang, William Ricketts, Haoyun An, Zhi Hong
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Patent number: 6982336Abstract: A 1,2-dioxetane derivative of the formula (I): wherein R1–R3 and Ar are defined in the claims is provided.Type: GrantFiled: March 7, 2002Date of Patent: January 3, 2006Assignee: Tosoh CorporationInventors: Masakatsu Matsumoto, Nobuko Watanabe, Masashi Yamada
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Patent number: 6982264Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.Type: GrantFiled: June 27, 2002Date of Patent: January 3, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Roy Hom, John Tucker
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Patent number: 6967213Abstract: The present invention relates to an isothiazole derivative of the following formula 1 or nontoxic salt thereof: wherein, R1 is hydrogen, alkoxy group or halogen group; R2 is methyl or amino group. According to the present invention, isothiazole derivative or nontoxic salt thereof having antipyretic, analgesic and antiphlogistic activity and an improved side effect; process for the preparation thereof; and pharmaceutical composition including the same can be provided.Type: GrantFiled: October 9, 2003Date of Patent: November 22, 2005Assignee: CJ Corp.Inventors: Il Hwan Cho, Dong Hyun Ko, Myeong Yun Chae, In Ki Min, Young Hoon Kim, Young Mee Chung, Hyun Jung Park, Ji Young Noh, Il Hwan Kim, Hyung Chul Ryu, Sang Wook Park, Sung Hak Jung, Jong Hoon Kim
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Patent number: 6964975Abstract: The present invention relates to novel isoxazole and thiazole compounds having an excellent lysophosphatidic acid (LPA) receptor antagonistic activity represented by general formula [1] or salts thereof: wherein R1 and R2 represents an optionally substituted alkyl group or the like; R3 represents a hydrogen atom or the like; R4 represent a group selected from the group consisting of (I) optionally substituted phenyl, aryl, or heterocycle, (II) substituted or nonsubstituted alkyl, and (III) substituted or nonsubstituted alkenyl, alternatively, R3 and R4 may form a ring structure together with a carbon atom to which they bind; and X represents an oxygen atom or a sulfur atom, provided that, when R3 is a hydrogen atom, R4 represents a group other than methyl, and the use thereof as a medicine.Type: GrantFiled: February 19, 2001Date of Patent: November 15, 2005Assignee: Kirin Beer Kabushiki KaishaInventors: Akihiro Ueno, Rika Nagao, Tomoko Watanabe, Hideo Ohta, Mikio Yagi
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Patent number: 6956049Abstract: In accordance with the present invention, there are provided methods of modulating the activity of excitatory amino acid receptors using a specifically defined class of heterocyclic compounds. In one embodiment, there are provided methods of modulating metabotropic glutamate receptors. The present invention also discloses methods of treating disease using heterocyclic compounds.Type: GrantFiled: August 31, 1999Date of Patent: October 18, 2005Assignee: Merck & Co., Inc.Inventors: Nicholas D. P. Cosford, Ian A. McDonald, Stephen D. Hess, Mark A. Varney
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Patent number: 6951618Abstract: A method for suppressing the growth of mycobacteria associated with hypersensitivity pneumonitis, in particular Mycobacterium immunogenum, in metalworking fluids is described. The method uses antimicrobial or biocidal compositions which include a metal complex comprising disodium monocopper (II) citrate and an isothiazolone mixture preferably comprising 5-chloro-2-methyl-4-isothiazolin-3-one 2-methyl-4-isothiazolin-3-one. Also described are methods for detecting and identifying the mycobacteria.Type: GrantFiled: April 22, 2003Date of Patent: October 4, 2005Inventor: Harold W. Rossmoore
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Patent number: 6951873Abstract: Methods for the treatment of age-related behavioral disorders in companion animals are disclosed. These comprise administering to a companion animal in need of such treatment a therapeutically effective amount of an acetylcholinesterase inhibitor. A preferred acetylcholinesterase inhibitor is a compound of Formula 1: Pharmaceutical compositions and dosage forms comprising a compound of Formula 1 are also disclosed.Type: GrantFiled: March 3, 2000Date of Patent: October 4, 2005Assignee: Pfizer Inc.Inventor: Kristin M. Lundy
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Patent number: 6949536Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl; halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring. R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4.Type: GrantFiled: February 3, 2004Date of Patent: September 27, 2005Assignee: Pfizer, Inc.Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
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Patent number: 6946492Abstract: Embodiments of the invention relate to methods of reducing weight in mammals and for the prophylaxis or treatment of obesity comprising administration of C2-substituted indan-1-one systems and their physiologically acceptable salts and physiologically functional derivatives. Compounds for use in methods of embodiments of the invention may include compounds of the formula in which the radicals are as defined, and their physiologically acceptable salts.Type: GrantFiled: August 30, 2002Date of Patent: September 20, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Patent number: 6936630Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: wherein R is wherein R9, R10, R11, R12, R13, and R14 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms; R6, and R7 are each, independently, hydrogen, lower alkyl of 1-6 carbon atoms, or CH2COOR8, where R8 is a lower alkyl of 1-6 carbon atoms; and X is O or S; R1 is hydrogen or a lower alkyl of 1-6 carbon atoms; R2, R3, and R4 are each, independently, hydrogen or halogen; and R5 is a lower alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 10, 2003Date of Patent: August 30, 2005Assignee: WyethInventors: Robert J. Steffan, Amedeo A. Failli
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Patent number: 6927216Abstract: The present application describes novel cyclic sulfonyl derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.Type: GrantFiled: September 17, 2001Date of Patent: August 9, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Robert J. Cherney, Bryan W. King
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Patent number: 6927217Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.Type: GrantFiled: October 16, 2002Date of Patent: August 9, 2005Assignee: Warner-Lambert CompanyInventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Elizabeth Ann Lunney, Alexander Pavlovsky, Vara Prasad Venkata Nagendra Josyula, Bradley Dean Tait
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Patent number: 6924287Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be replaced; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.Type: GrantFiled: June 20, 2000Date of Patent: August 2, 2005Assignee: Janssen Pharmacatica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 6916819Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: GrantFiled: December 21, 2001Date of Patent: July 12, 2005Assignee: Neurogen CorporationInventors: Guiying Li, John M. Peterson, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, Vinod Singh, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu
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Patent number: 6905698Abstract: A particulate carrier material is impregnated with a biocidal formulation and serves as a vehicle for introduction of the biocide into a liquid-based media, such as a surface coating or surface cleaning compositions, in order to allow controlled release of the biocide to combat bacterial, fungal, algal or like growth for an extend period of time.Type: GrantFiled: August 24, 1999Date of Patent: June 14, 2005Assignee: Ineos Silicas LimitedInventors: Derek Aldcroft, Helen Jones, Dafydd Turner, Michel Edge, Julie Robinson, Kenneth Seal
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Patent number: 6902727Abstract: A synergistic biocidal composition comprising a mixture of 2-propenal polymer (APC) and 5-chloro-2-methyl-4-isothiazoline-3-one (CIT) and 2-methyl-4-isothiazoline-3-one (MIT).Type: GrantFiled: April 10, 2003Date of Patent: June 7, 2005Assignee: ISP Investments Inc.Inventors: Liu Xianbin, Karen Winkowski
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Patent number: 6903104Abstract: The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula. In this formula, each R1 is independently isoxazolyl, thiazolyl, isothiazolyl, 1,3,4-thiadiazolyl, 1,3-benzothiazolyl, quinolyl, isoquinolyl, thionaphthenyl, or benzofuranyl, each being optionally substituted with 1-6 independent R5; or when taken together with R2 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5. Each R2 is independently H, C1-C10 alkyl, or aryl, each being optionally substituted with 1-4 independent R5; or when taken together with R1 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5.Type: GrantFiled: December 5, 2002Date of Patent: June 7, 2005Assignee: National Health Research InstitutesInventors: Chiung-Tong Chen, Shu-Jen Chen, Ming-Chu Hsu, Der-Ren Hwang, Wen-Tai Li, Chu-Chung Lin
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Patent number: 6884811Abstract: An antifungal composition comprising 3-iodo-2-propynyl butylcarbamate, 4,5-dichloro-2-octyl-isothiazolin-3-one and methyl 2-benzimidazolylcarbamate is useful as industrial antifungal composition, particularly for wood protection.Type: GrantFiled: August 30, 2002Date of Patent: April 26, 2005Assignee: Shinto Fine Co., Ltd.Inventor: Kazuhide Fujimoto
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Patent number: 6875783Abstract: Novel isothiazolecarboxamides of the formula in which R is as defined in the description, a plurality of processes for preparing the novel compounds and their us for protecting plants against attack by undesirable microorganisms and animal pests.Type: GrantFiled: August 29, 2003Date of Patent: April 5, 2005Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Dietmar Kuhnt, Hans-Ludwig Elbe, Christoph Erdelen, Stefan Dutzmann, Gerd Hänssler, Klaus Stenzel, Astrid Mauler-Machnik, Yoshinori Kitagawa, Haruko Sawada, Haruhiko Sakuma
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Patent number: 6875784Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formulea I and II, described herein, or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: October 2, 2003Date of Patent: April 5, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail Fedor Gordeev, Adam Renslo, Dinesh Vinoobhai Patel
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Patent number: 6864276Abstract: 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) agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: May 7, 2001Date of Patent: March 8, 2005Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 6858634Abstract: Controlled release formulations for pesticides and herbicides contain an active ingredient, a matrix polymer and a matrix polymer plasticizer which is present in an amount sufficient to provide a release rate for the active ingredient from the formulation that matches a selected release rate. Methods for making and using the formulation, and seeds and plants that have been treated with the formulations are also included.Type: GrantFiled: September 10, 2001Date of Patent: February 22, 2005Assignee: Monsanto Technology LLCInventors: Jawed Asrar, James F. Essinger, Jr.
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Patent number: 6852716Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: February 10, 2003Date of Patent: February 8, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Jason K. Myers, Vincent E. Groppi, Jr.
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Patent number: 6849622Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.Type: GrantFiled: October 5, 2001Date of Patent: February 1, 2005Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Patent number: 6846839Abstract: The present invention relates to methods for treating diseases and disorders related to unregulated angiogenesis and/or vasculogenesis. More specifically, this invention relates to methods for treating diseases and disorders, such as rheumatoid arthritis, endometriosis, ocular neovascularization, solid tumor growth and metastases, and excessive scarring during wound healing, with indolinone compounds.Type: GrantFiled: June 16, 1999Date of Patent: January 25, 2005Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Laura Kay Shawver, Klaus Peter Hirth, Annie Fong
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Patent number: 6846492Abstract: The use of compounds of formula (1) is described, in which compounds R1, R2 and R3 are each independently of the others hydrogen; C1-C20alkyl; C3-C7cycloalkyl; C2-C20alkenyl; C4-C7cycloalkenyl; C2-C20alkynyl, C4-C7cycloalkynyl; or unsubstituted or C1-C5alkyl-, C3-C7cylcoalkyl-, C1-C5alkoxyl-, C3-C7cycloakoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C7cylcloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl-C1-C5alkyl, naphthyl-C1-C5alkyl, phenylcarbonyl-C1-C5alkyl, naphthylcarbonyl-C1-C5alkyl, pyrrolylalkyl, furanylalkyl, thiophenylalkyl, pyrazolylalkyl, imidazolylalkyl, oxazolylalkyl, thiazolylalkyl, isoxazolylalkyl, isothiazolylalkyl, 1,2,3-triazolylalkyl, 1,2,4-triazolylalkyl, 1,2,3-oxadiazolylalkyl, 1,3,4-oxadiazolylalkyl, 1,2,3-thiadiazolylalkyl, 1,3,4-thiadiazolylalkyl, indolylalkyl, pyridylalkyl, pyridazinylalkyl, pyrimidinylalkyl, pyridazinylalkyl, quinolinylalkyl, isoquinolinylalkyl, pyrrolyl, furanyl,Type: GrantFiled: February 13, 2001Date of Patent: January 25, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Wolfgang Haap, Werner Hölzl, Dietmar Ochs, Karin Petzold, Marcel Schnyder
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Patent number: 6846777Abstract: The invention relates to a biocidal composition which can be added to materials which can be attacked by harmful micro-organisms, containing pyrithione as a biocidal active ingredient. The biocidal composition is characterised in that it contains 2-alkyl isothiazoline-3-one as another biocidally active ingredient. The active ingredients of the biocidal composition behave synergistically and are ideally suitable for controlling bacteria, fungus and algae.Type: GrantFiled: August 20, 2001Date of Patent: January 25, 2005Assignee: Thor GmbHInventors: Dagmar Antoni-Zimmermann, Rüdiger Baum, Thomas Wunder, Hans-Jürgen Schmidt
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Patent number: 6833370Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3 I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: April 26, 2000Date of Patent: December 21, 2004Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jerome F. Daanen, Keith Brian Ryther, Jianguo Ji
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Publication number: 20040254175Abstract: Novel compounds of formula (I), wherein D, W, X, Y, T and R1 have the meanings cited in claim 1, are inhibitors of coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and in the treatment of tumors.Type: ApplicationFiled: May 10, 2004Publication date: December 16, 2004Inventors: Dieter Dorsch, Bertram Cezanne, Christos Tsaklakidis, Werner Mederski, Johannes Gleitz, Christopher Barnes
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Patent number: 6831091Abstract: The invention relates to hydrochloride, hydrobromide, hemi-citrate, acetate, p-tosylate, L-tartrate, hemi-succinate, and mesylate salt forms of 3-(4-bromo-2,6-difluoro-benzyloxy)-5-[3-(4-pyrrolidin-1-yl-butyl)-ureido]-isothiazole-4-carboxylic acid amide having the following formula: The invention also relates to pharmaceutical compositions containing the hydrochloride, hydrobromide, hemi-citrate, acetate, p-tosylate, L-tartrate, hemi-succinate, and mesylate salts of formula I. The invention further relates to methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above salts and to methods of preparing the crystal forms of the above salts.Type: GrantFiled: November 27, 2001Date of Patent: December 14, 2004Assignee: Pfizer Inc.Inventors: Thomas George Gant, Glenn R. Williams
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Publication number: 20040248943Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: July 8, 2002Publication date: December 9, 2004Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Publication number: 20040242540Abstract: Fungicidal compositions are provided that comprise a silthiofam-type fungicide and a fungicide that is selected from the group consisting of diazole fungicides, triazole fungicides and strobilurin type fungicides. Combinations of fluqinconazole and simeconazole or azoxystrobin, and simeconazole and azoxystrobin are also provided. Methods for treating plants and plant propagation materials with the fungicidal compositions are also taught, as are plants and their propagation materials which have been so treated, and controlled release formulations that contain the fungicidal compositions.Type: ApplicationFiled: March 19, 2004Publication date: December 2, 2004Inventors: Jawed Asrar, Claudia Heppener, Yiwei Ding
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Publication number: 20040229869Abstract: Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.Type: ApplicationFiled: March 26, 2004Publication date: November 18, 2004Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Sangita, Atul Kumar, Man Mohan Singh, Girish Kumar Jain, Puvvada Sri Ramanchandra Murthy, Suprabhat Ray
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Publication number: 20040204454Abstract: The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I:Type: ApplicationFiled: March 16, 2004Publication date: October 14, 2004Inventors: Jennifer X. Qiao, Tammy C. Wang
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Publication number: 20040198781Abstract: Methods of treating or preventing carbonic anhydrase associated disorders or diseases in a subject in need of such treatment as prevention comprising the administration of cyclooxygenase-2 inhibitors, or structurally related compounds, having carbonic anhydrase inhibitory properties, as well as combinations of the cyclooxygenase-2 inhibitors, or structurally related compounds, with anti-inflammatory agents or drugs, antineoplastic agents or drugs or ophthalmic agents or drugs in methods of treatment and prevention of disorders or diseases.Type: ApplicationFiled: April 19, 2004Publication date: October 7, 2004Applicant: Pharmacia CorporationInventors: Jaime L. Masferrer, Janet M. O'Neal
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Publication number: 20040198785Abstract: A microbicidal composition containing: (a) at least one non-halogenated 2-alkyl-4-isothiazolin-3-one selected from substituted and unsubstituted 2-(C1-C4)alkyl-4-isothiazolin-3-ones; and (b) at least one of 2,2′-dithiobis(N-methylbenzamide) and 2-methylbenzisothiazolone.Type: ApplicationFiled: March 18, 2004Publication date: October 7, 2004Inventors: Beat Heer, Gerhard Tiedtke, Eileen Fleck Warwick
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Publication number: 20040198729Abstract: A microbicidal composition containing: (a) at least one 2-alkyl-4-isothiazolin-3-one; (b) at least one halopropynyl carbamate; and (c) at least one sulfur-containing s-triazine.Type: ApplicationFiled: March 29, 2004Publication date: October 7, 2004Inventors: Beat Heer, Gerhard Tiedtke, Bryan Martin Hegarty