Chalcogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/78)
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Patent number: 7504433Abstract: The present invention is directed to compounds represented by the following structural formula, Formula I: and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) X is selected from the group consisting of O, S, S(O)2, N, and a bond; (b) U is an aliphatic linker wherein one carbon atom of the aliphatic linker may be replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with R30; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; and (d) E is C(R3)(R4)A or A.Type: GrantFiled: December 31, 2003Date of Patent: March 17, 2009Assignee: Eli Lilly and CompanyInventors: Nathan Bryan Mantlo, Xiaodong Wang, Guoxin Zhu
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Patent number: 7498126Abstract: A photoacid generator has formula (1). A chemically amplified resist composition comprising the photoacid generator has advantages including a high resolution, focus latitude, long-term PED dimensional stability, and a satisfactory pattern profile shape. When the photoacid generator is combined with a resin having acid labile groups other than those of the acetal type, resolution and top loss are improved. The composition is suited for deep UV lithography.Type: GrantFiled: June 5, 2007Date of Patent: March 3, 2009Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Youichi Ohsawa, Kazunori Maeda, Satoshi Watanabe
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Publication number: 20090054667Abstract: Methods for introducing a 1-halo-1-haloalkene compound onto an aromatic or heteroaromatic ring are provided, including processes for the production of certain 1-halovinyl aryl or heteroaryl derivatives in which the 1-halovinyl group is either 1-fluoro or 1-chlorovinyl and the aromatic species phenyl or thiophene, the processes including coupling an arylmagnesium species with a dihalo olefin in the presence of a nickel or iron catalyst.Type: ApplicationFiled: August 9, 2006Publication date: February 26, 2009Applicant: Replidyne, Inc.Inventors: Joseph W. Guiles, Jian Qiu, Theodore M. Tarasow
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Publication number: 20090023095Abstract: There are provided a novel compound represented by a general formula (b1-1) shown below, which is useful as an acid generator for a resist composition and a manufacturing method thereof, a compound useful as a precursor of the novel compound and a manufacturing method thereof, an acid generator, a resist composition and a method of forming a resist pattern.Type: ApplicationFiled: July 16, 2008Publication date: January 22, 2009Applicant: Tokyo Ohka Kogyo Co., Ltd.Inventors: Hideo Hada, Takeshi Iwai, Takehiro Seshimo, Akiya Kawaue, Keita Ishiduka
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Publication number: 20090018168Abstract: Disclosed herein is a compound having a formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: April 29, 2008Publication date: January 15, 2009Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20080319208Abstract: A process for preparing optically active (1S)-3-chloro-1-(2-thienyl)propan-1-ol of the formula I by, in a medium comprising 3-chloro-1-(2-thienyl)propan-1-one of the formula II reducing this compound to the compound of the formula I by means of an alcohol dehydrogenase from the Thermoanaerobacter genus, and isolating the product formed in substantially enantiomerically pure form.Type: ApplicationFiled: December 13, 2006Publication date: December 25, 2008Applicant: BASF SEInventor: Michael Breuer
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Patent number: 7449580Abstract: Ticlopidine and clopidogrel having high blood platelet aggregation inhibitory and anti-thrombotic activities are simply prepared by reacting a substituted thiophene derivative with a 2-chlorobenzylamine derivative.Type: GrantFiled: March 3, 2005Date of Patent: November 11, 2008Assignee: Hanmi Pharm. Co., LtdInventors: Sangmin Yun, Eun Sook Kim, Hee Seock Kim, Tae Hee Ha, Kwee-Hyun Suh, Gwan Sun Lee
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Patent number: 7449588Abstract: Methods of stabilizing thiophene derivatives of the general formula (I) by treatment with basic compounds: wherein R1 and R2 each independently represents a moiety selected from the group consisting of hydrogen, optionally substituted C1-20 alkyl groups which can contain up to 5 heteroatoms selected from the group consisting of oxygen and sulfur, optionally substituted C1-20 oxyalkyl groups which can contain up to 5 heteroatoms selected from the group consisting of oxygen and sulfur, or wherein R1 and R2 together represent a fused cyclic moiety selected from the group consisting of optionally substituted C1-20 dioxyalkylene groups and C1-20 dioxyarylene groups; and stabilized thiophene derivatives that can be prepared by such methods.Type: GrantFiled: May 4, 2007Date of Patent: November 11, 2008Assignee: H.C. Starck GmbHInventors: Friedrich Jonas, Klaus Wussow, Knud Reuter
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Publication number: 20080275100Abstract: The invention provides para substituted dialkylphenol derivatives of propofol. The invention further provides pharmaceutical compositions comprising such analogs, methods for preparing such analogs, and methods of using such analogs to induce general anesthesia, sedation, and/or hypnotic or sleep effects in a patient.Type: ApplicationFiled: July 9, 2008Publication date: November 6, 2008Applicant: ABRAXIS BIOSCIENCE, INC.Inventors: Chunlin TAO, Cheng Zhi YU, Neil P. DESAI, Vuong TRIEU
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Patent number: 7435835Abstract: The invention relates to a process for preparing enantiomerically pure alcohol of the formula 1, which comprises (i) reducing the ketone of the formula 3to the racemic alcohol of the formula 4, (ii) enantioselectively acylating the racemic alcohol of the formula 4 with succinic anhydride in the presence of a lipase to give the succinic semiester of the formula 7, (iii) separating off the succinic semiester of the formula 7 from the unreacted enantiomer of the formula 4, (iv) reacting the enantiomerically pure alcohol of the formula 4 with methylamine to give the enantiomerically pure alcohol of the formula 1.Type: GrantFiled: January 18, 2005Date of Patent: October 14, 2008Assignee: BASF AGInventor: Rainer Stürmer
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Publication number: 20080194842Abstract: Methods for introducing a 1-halo-1-haloalkene compound onto an aromatic or heteroaromatic ring are provided, including processes for the production of certain 1-halovinyl aryl or heteroaryl derivatives in which the 1-halovinyl group is either 1-fluoro or 1-chlorovinyl and the aromatic species phenyl or thiophene, the processes including coupling an arylmagnesium species with a dihalo olefin in the presence of a nickel or iron catalyst.Type: ApplicationFiled: August 9, 2006Publication date: August 14, 2008Applicant: REPLIDYNE, INC.Inventors: Joseph W. Guiles, Jian Qiu, Theodore M. Tarasow
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Publication number: 20080182203Abstract: A photoresist composition includes about 4% to about 10% by weight of a photoresist resin, about 0.1% to about 0.5% by weight of a photoacid generator having a sulfonium-salt cationic group and a sulfonium-salt anionic group containing a carboxyl group as a hydrophilic site and a remainder of a solvent. The photoresist composition may form a photoresist pattern having a uniform profile.Type: ApplicationFiled: January 24, 2008Publication date: July 31, 2008Applicant: Samsung Electronics Co., Ltd.Inventors: Hyo-Jin Yun, Young-Gil Kwon, Young-Ho Kim, Do-Young Kim, Jae-Hee Choi, Se-Kyung Baek
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Publication number: 20080177020Abstract: A non-metallocene organometallic complex comprising a tridentate ligand and a metal bonded to a tridentate ligand, wherein two substituted aryl groups in the tridentate ligand are connected to a cyclic group at the ortho position via semi-rigid ring-ring linkages, and selected so to provide the resulting non-metallocene organometallic complex with a CS geometry, a C1 geometry, a C2 geometry or a C2v geometry.Type: ApplicationFiled: September 21, 2007Publication date: July 24, 2008Inventors: Theodor Agapie, Suzanne Rose Golisz, Daniel Tofan, John E. Bercaw
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Publication number: 20080167481Abstract: The present invention provides a novel thiophene compound as a synthetic intermediate that is useful for efficient production of kahweofuran or an analogue thereof. The present invention also provides a process for producing kahweofuran or an analogue thereof using the novel thiophene compound as an intermediate material. Of novel thiophene compounds represented by Formula (1): wherein R1 is a hydrogen atom or a C1-C4 lower alkyl group; R2 is a hydrogen atom or an alcohol-protecting group; R3 is a hydrogen atom, —COR4 or —C(OH)R5 (wherein R4 and R5 each represent a C1-C4 lower alkyl group); provided that when R2 and R3 are hydrogen atoms, R1 is not any of a hydrogen atom, methyl group, or n-propyl group; a thiophene compound represented by Formula (2) is reduced and cyclized in the presence of a transition metal catalyst to produce kahweofuran or kahweofuran analogue (3a) shown below: wherein R1 is a hydrogen atom or a C1-C4 lower alkyl group, and R4 is a C1-C4 lower alkyl group.Type: ApplicationFiled: February 22, 2006Publication date: July 10, 2008Applicant: SAN EI GEN F.F.I., INC.Inventors: Shigeo Katsumura, Yanwu Li, Hisakatsu Iwabuchi, Masanobu Onishi, Yusuke Murakami
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Publication number: 20080119539Abstract: Compounds of the formula are disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: September 6, 2007Publication date: May 22, 2008Inventors: David W. Old, Robert M. Burk, Todd S. Gac
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Publication number: 20080119538Abstract: Disclosed herein are compounds of the formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: July 6, 2007Publication date: May 22, 2008Inventors: DAVID W. OLD, Vinh X. Ngo
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Patent number: 7371873Abstract: A sulfoalkylthiophene compound of the following formula [1] and a hydroxyalkylthiophene compound of the following formula [2], from which a useful ?-conjugated conductive polymer monomer capable of oxidation polymerization can be provided: (wherein R is a hydrogen atom, an alkali metal atom or an alkaline earth metal atom, and n is an integer of 1 to 3) (wherein n is as defined above).Type: GrantFiled: November 17, 2004Date of Patent: May 13, 2008Assignee: Nissan Chemical Industries, Ltd.Inventor: Hideo Suzuki
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Patent number: 7351841Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13 SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: GrantFiled: December 6, 2005Date of Patent: April 1, 2008Assignee: Nissan Chemical Industries, Ltd.Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
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Patent number: 7332623Abstract: This invention provides aryl-substituted acyclic enediyne compounds of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1=R2=H; or R1 and R2 together form a moiety represented by the formula R3 represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; and R4 represents a substituted or unsubstituted aryl group having 3-30 carbon atoms; with the proviso that R3 is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R1=R2=H and R4 is o-cyanophenyl,; and with the proviso that R3 is not butyl when R1=R2=H and R4 is phenyl. The compounds of formula (I) are found to have inhibitory activities against topoisomerase I or act as a S phase or G2/M phase blocker.Type: GrantFiled: May 18, 2004Date of Patent: February 19, 2008Assignee: Kaohsiung Medical UniversityInventors: Ming-Jung Wu, Chi-Fong Lin
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Patent number: 7319152Abstract: Compounds of formula I or II are provided, wherein R1-R8 are defined herein, and pharmaceutical compositions and kits containing these compounds.Type: GrantFiled: September 18, 2006Date of Patent: January 15, 2008Assignee: WyethInventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
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Publication number: 20070249647Abstract: The present invention relates to method(s) of treating a subject afflicted with cancer or a precancerous condition, an inflammatory disease or condition, and/or stroke or other ischemic disease or condition, the method comprising administering to the subject or patient in need a composition comprising a therapeutically effective amount of a substituted cis or trans-stilbene.Type: ApplicationFiled: April 25, 2007Publication date: October 25, 2007Inventors: David L. Vander Jagt, Lorraine M. Deck
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Patent number: 7259172Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 2, 2004Date of Patent: August 21, 2007Assignee: MethylGene Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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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: 7202247Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: December 19, 2002Date of Patent: April 10, 2007Assignee: AtheroGenics, Inc.Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten
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Patent number: 7186722Abstract: Novel ?1-pyrrolines of the Formula (I) in which R1, R2, R3 and Het have the meanings given in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.Type: GrantFiled: January 31, 2002Date of Patent: March 6, 2007Assignee: Bayer Cropscience AGInventors: Andrew Plant, Rüdiger Fischer, Thomas Seitz, Christoph Erdelen, Andreas Turberg, Olaf Hansen
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Patent number: 7183310Abstract: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.Type: GrantFiled: August 10, 2004Date of Patent: February 27, 2007Assignee: Allergan, Inc.Inventors: Yariv Donde, Robert M. Burk, Michael E. Garst
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Patent number: 7144893Abstract: The present invention pertains to compounds of the formula (1) which are, inter alia, antiproliferative agents, anticancer agents, antimycobacterial agents, antituberculosis agents, and/or thioredoxin/thioredoxin reductase inhibitor: wherein: Q is ?O or ?N—S(?O)2—RQ;RQ is —II or optionally substituted C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; Ar is optionally substituted C5-20aryl; RO is an oxy substituent; the bond marked ? is a single bond or a double bond; the bond marked ? is a single bond or a double bond; R3 and R5 are each independently ring substituents; R2 and R6 are each independently ring substituents; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for example, in the treatment of proliferative conditions, (e.g., cancer), mycobacterial infections (e.g.Type: GrantFiled: July 5, 2002Date of Patent: December 5, 2006Assignee: Cancer Research Technology LimitedInventors: Malcolm Francis Graham Stevens, Geoffrey Wells, Andrew David Westwell, Tracey Dawn Poole
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Patent number: 7145015Abstract: Benzocycloheptenes of formula (I), in which R1, R2 and Y have the meanings that indicated herein, exhibit selective estrogenic activity on bones and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis:Type: GrantFiled: April 11, 2005Date of Patent: December 5, 2006Assignee: Schering AGInventors: Rolf Bohlmann, Jorg Kroll, Hermann Kuenzer, Christa Hegele-Hartung, Monika Lessl, Rosemarie Lichtner, Yukishige Nishino
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Patent number: 7122294Abstract: Photoacid generators (PAGs) comprising photoactive moieties and perfluorinated, multifunctional anionic moieties (or incipient anionic moieties) are disclosed which provide photoacids with high acid strength, low volatility and low diffusivity. The present invention further relates to photoacid generators as they are used in photoinitiated or acid-catalyzed processes for uses such as photoresists for microlithography and photopolymerization.Type: GrantFiled: May 22, 2003Date of Patent: October 17, 2006Assignee: 3M Innovative Properties CompanyInventor: William M. Lamanna
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Patent number: 7101904Abstract: A compound or a pharmaceutically acceptable salt or a prodrug thereof, wherein A, B, R1, R2, D, and E are defined herein. Use of the diseases for the treatment of diseases, and compositions and medicaments related thereto are also disclosed.Type: GrantFiled: August 10, 2004Date of Patent: September 5, 2006Assignee: Allergan, Inc.Inventors: Yariv Donde, Robert M. Burk, Michael E. Garst
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Patent number: 7087787Abstract: The invention relates to a method for producing derivatives of 4-alkylsulfinyl methylarylene methanols. Derivatives of 4-alkylsulfinyl methylarylene methanols are valuable monomers in the production of conjugated polymers, which are suitable for use as electroluminescent materials.Type: GrantFiled: August 27, 1999Date of Patent: August 8, 2006Assignee: Covion Organic Semiconductors GmbHInventors: Dirk Vanderzande, Joanes Gelan, Albert van Breemen, Michael Van Der Borght, Laurence Lutsen, Raf Kiebooms, Willi Kreuder
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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: 7084136Abstract: A compound of the formula (I): wherein A is alkylene optionally having an unsaturated bond; R is —C(?O)—R1; R1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, having a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor is found.Type: GrantFiled: May 28, 2001Date of Patent: August 1, 2006Assignee: Shionogi & Co., Ltd.Inventors: Norihiko Tanimoto, Akinori Arimura
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Patent number: 7078431Abstract: It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.Type: GrantFiled: May 21, 2003Date of Patent: July 18, 2006Assignee: Atherogenics, Inc.Inventors: Charles Q. Meng, Liming Ni, James A. Sikorski, Lee K. Hoong
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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: 7060846Abstract: Thienothiophene monomers having an SF5 group and conducting oligomers and polymers formed by the polymerization of such monomers and their use as hole injection materials, charge transport materials, or as semiconductors. The compound may be of the formula: where X and X? are independently H, halogen atoms (e.g., F, Cl, Br, and I), MgCl, MgBr, Mgl, Sn(R?)3, where R? comprises C1-6 alkyl or —OC1-6 alkyl, boronic acid, boronic ester, —CH?CHR? (where R? comprises H or C1-6 alkyl), —OC1-6 alkyl, —COOC1-6 alkyl, —S—COR?? and —COR?? (where R?? comprises H or C1-6 alkyl), —C?CH, or polymerizable aromatic rings (such as phenyl, naphthalene, pyrrole, dithiophene, thienothiophene, thiophene and so forth).Type: GrantFiled: September 20, 2005Date of Patent: June 13, 2006Assignee: Air Products and Chemicals, Inc.Inventors: Steffen Zahn, Andrew Francis Nordquist, Kristen Elaine Minnich, Guari Sankar Lal, William Franklin Burgoyne, Jr., Axel Klauck-Jacobs
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Patent number: 7033727Abstract: A photosensitive composition of the present invention has excellent sensitivity and pattern profile, which comprises an acid generator having a specific structure.Type: GrantFiled: September 24, 2003Date of Patent: April 25, 2006Assignee: Fuji Photo Film Co., Ltd.Inventor: Kunihiko Kodama
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Patent number: 7030153Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: December 27, 2002Date of Patent: April 18, 2006Assignee: G.D. Searle & Co.Inventors: John J. Talley, Stephen R. Bertenshaw, Paul W. Collins, Thomas D. Penning, David B. Reitz, Roland S. Rogers
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Patent number: 7026339Abstract: The present invention relates to compounds, process for their synthesis, compositions and methods for the treatment and prevention of hepatitis C virus (HCV) infection. In particular, the present invention provides novel compounds, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment or prevention of HCV infection. The present invention also provides processes and intermediates for the synthesis of these compounds.Type: GrantFiled: November 3, 2004Date of Patent: April 11, 2006Inventors: Fan Yang, Bo Zhang, Nancy Anne Wicnienski, Jeffrey Allen Pfefferkorn, Meredith L. Greene, Ke Chen, Richard A. Nugent, Matthew Todd Reding, Robert Charles Kelly, Mark A. Mitchell, Lee A. Funk, Richard Frederick Heier, III, Rebecca Merry Anderson
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Patent number: 7015217Abstract: The present application describes novel cyclic sulfone derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof. In formula I, A is selected from —COR5, —CO2H, —CO2R6, —C(O)NHOH, —C(O)NHOR5, —C(O)NHOR6, —NHRa, —N(OH)COR5, —N(OH)CHO, —SH, —CH2SH, —S(O)(?NH)Ra, —S(?NH)2Ra, —SC(O)Ra, —PO(OH)2, and —PO(OH)NHRa; B is a thiomorpholine ring; X is absent or is CR3R4; and Ua, Xa, Ya, Za, R1, R2, Rb, and q are defined in the present specification.Type: GrantFiled: October 7, 2002Date of Patent: March 21, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Chu-Biao Xue
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Patent number: 6943182Abstract: The invention relates to cyclopentabenzofuran derivatives, process for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-?B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.Type: GrantFiled: May 30, 2002Date of Patent: September 13, 2005Assignee: Bayer AktiengesellschaftInventors: Walter Guarnieri, Thomas Jaetsch, Andreas Schoop, Jörg Baumgarten, Axel Kretschmer, Horst-Peter Antonicek
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Patent number: 6927290Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p??(1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH??(2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX??(3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.Type: GrantFiled: May 10, 2004Date of Patent: August 9, 2005Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Miki, Hideki Ushio, Isao Kurimoto
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Patent number: 6916956Abstract: A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided.Type: GrantFiled: August 10, 2001Date of Patent: July 12, 2005Assignee: Japan Tobacco, Inc.Inventors: Yuko Shinagawa, Takeo Katsushima, Takashi Nakagawa
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6858602Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: GrantFiled: October 14, 2003Date of Patent: February 22, 2005Assignee: Wellstat Therapeutics CorporationInventors: Shalini Sharma, Reid W. von Borstel
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Patent number: 6831106Abstract: The present invention relates to novel triaromatic compounds having the general formula (I): as well as to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, in carcinology and in the field of autoimmune diseases and that of organ or tissue transplants in particular), or alternatively in cosmetic compositions.Type: GrantFiled: September 5, 2002Date of Patent: December 14, 2004Assignee: Galderma Research & Development, S.N.C.Inventors: Jean-Michel Bernardon, Thibaud Biadatti
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Patent number: 6825359Abstract: Quinomethane compounds having a structure represented by the general formula (1): wherein R1 to R4 and R9 to R12 are the same or different and each represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cyclic alkyl group, an aryl group, or an alkoxy group having 1 to 6 carbon atoms; R5 and R6 are the same or different and each represents an alkyl group having 1 to 12 carbon atoms, an aryl group, or a heterocyclic group; R7 and R8 each represents a hydrogen atom; and optional substituents are each a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, an aryl group, or a heterocyclic group. Since these compounds transport electrons efficiently, they are useful in electrophotographic photoreceptors and/or organic electroluminescence applications.Type: GrantFiled: February 4, 2003Date of Patent: November 30, 2004Assignee: Fuji Electric Imaging Device Co., Ltd.Inventors: Kenichi Ohkura, Yoshihiro Ueno, Masami Kuroda, Nobuyuki Sekine
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Publication number: 20040229935Abstract: Compounds are described that bind to tubulin causing tubulin depolymerization and inhibiting tubulin polymerization. The compounds of the invention are therapeutically effective to inhibit cellular proliferation, for example, as effective anti-cancer agents. The compounds can also induce cytotoxicity in cells such as leukemia cells. The chemical structure of the compounds includes a furan, thiophene, thiazole, oxazole, or imidazole group at one end of the molecule (head) and a hydrophobic, aliphatic chain at the other end of the molecule (tail).Type: ApplicationFiled: May 11, 2004Publication date: November 18, 2004Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Shyi-Tai M. Jan
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Publication number: 20040192908Abstract: The invention concerns novel molecules, their preparation and their uses, in particular in the field of human and veterinary medicine and cosmetics. The inventive compounds are partly fatty acid derivatives and exhibit advantageous pharmacological and cosmetic properties. The invention also concerns various uses of said compounds, the pharmaceutical compositions containing them and methods for preparing them.Type: ApplicationFiled: January 21, 2004Publication date: September 30, 2004Inventors: Jamila Najib-Fruchart, Karine Caumont-Bertrand
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Publication number: 20040067971Abstract: The invention relates to novel stilbene compounds having the general formula (I): 1Type: ApplicationFiled: October 2, 2003Publication date: April 8, 2004Applicant: GALDERMA RESEARCH & DEVELOPMENT, S.N.C.Inventors: Jean-Michel Bernardon, Bruno Charpentier