Two Double Bonds Between Ring Members Of The Five-membered Hetero Ring Patents (Class 548/560)
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Patent number: 7741357Abstract: Reaction of nordihydroguaiaretic acid with various alkyl chlorides, 1-piperidinecarbonyl chloride, methyl chloroformate, or 1,1?-carbonyldiimidazole under alkaline conditions produced the corresponding phenol ethers, carbamates and carbonates, respectively, in 67-83% yields (Scheme 1 and Scheme 2). Among these derivatives, the nitrogen-containing compounds were converted to the corresponding hydrochloride salts. Having good solubility, these NDGA derivatives were found to be stable in aqueous solution. These new compounds exerted potent activities against HIV Tat-regulated transactivation in cos-7 cells. The most active transcription inhibitor compound of this series 5b (P4N, Tetrapiperidino NDGA, meso-2,3-dimethyl-1,4-bis(3,4-[2-(piperidino)ethoxyphenyl])butane tetrakishydrochloride salt) has an IC50 of 0.88 ?M.Type: GrantFiled: April 13, 2007Date of Patent: June 22, 2010Assignee: Johns Hopkins UniversityInventors: Ru Chih C. Huang, Apostolos Gittis, Evangelos Moudrianakis, Julie A. Dohm, Jih Ru Hwu, Ming-Hua Hsu
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Patent number: 7737241Abstract: The invention is a system for initiating free radical polymerization comprising: a) in one part, one or more amido-borate compounds containing one or more anionic amido-borate moieties comprising an organoborate wherein the boron atom is bonded to a nitrogen atom of ammonia or an organic compound containing one or more nitrogen atoms, such as a hydrocarbyl amine, a hydrocarbyl polyamine, or an aromatic heterocycle containing one or more nitrogen atoms and optionally containing one or more heteroatoms or heteroatom containing functional moieties, and one or more cationic counter ions and b) in a second part, a liberating compound which reacts with the nitrogen atom(s) bound to the boron atom(s) upon contact with the amido-borate to form an organoborane radical.Type: GrantFiled: October 6, 2006Date of Patent: June 15, 2010Assignee: Dow Global Technologies Inc.Inventors: Shaoguang Feng, Gary L. Jialanella, Peter Nickias, Toni Ristoski
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Patent number: 7718702Abstract: There are disclosed compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.Type: GrantFiled: August 15, 2005Date of Patent: May 18, 2010Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Neng-Yang Shih, Brian J. Lavey, Razia K. Rizvi, Bandarpalle B. Shankar, James M. Spitler, Ling Tong, Ronald L. Wolin, Michael K. Wong
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Publication number: 20100028535Abstract: This invention relates to organometallic compounds represented by the formula LML? wherein M is a metal or metalloid, L is a substituted or unsubstituted cyclopentadienyl group or cyclopentadienyl-like group, a substituted or unsubstituted pentadienyl group or pentadienyl-like group, or a substituted or unsubstituted pyrrolyl group or pyrrolyl-like group, and L? is a substituted or unsubstituted pyrrolyl group or pyrrolyl-like group, a process for producing the organometallic compounds, and a method for producing a film or coating from the organometallic compounds. The organometallic compounds are useful in semiconductor applications as chemical vapor or atomic layer deposition precursors for film depositions.Type: ApplicationFiled: September 23, 2009Publication date: February 4, 2010Inventor: Scott Houston Meiere
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Publication number: 20100015076Abstract: Novel (co)polymeric structures having functional groups making possible, under conditions that are safe for human use, the formation of chemical bonds with human keratin, and in particular with the keratin present in hair, eyelashes and eyebrows, skin, nails, lips, the oral mucosa and tissues of the external genital organs are disclosed; the invention also relates to the synthesis of such (co)polymeric structures and the use thereof in the fields of cosmetics and medicine.Type: ApplicationFiled: December 23, 2005Publication date: January 21, 2010Applicant: EUDERMIC S.R.L.Inventors: Matteo Zanotti Russo, Nicola Barbini
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Publication number: 20090298905Abstract: This invention is related to new nitrogenated trans-stilbene analog compounds, more specifically, imine, pyrrol and Indole derivatives, with procedures for the preparation and use thereof as pharmaceutical compositions for the treatment and/or chemoprevention of those mammalian diseases such as cancer, fibrosclerosis and acute/chronic inflammation, graft-versus-host reaction, ischemic-reperfusion tissue injury in stroke and heart attack, neurodegeneration, and during organ transplantation, whose pathogenic and pathophysiological mechanisms depend on or are significantly contributed by undesirable oxidative stress, angiogenic and proliferative responses.Type: ApplicationFiled: April 12, 2006Publication date: December 3, 2009Inventors: Fernando Pedro Cossio, Eneko Aldaba Arevalo, Yosu Ion Vara Salazar, Aizpea Zubia Olascoaga, Silvia Vivanco Amato, Miren Lorea Mendoza Arteche, Clarisa Salado Pogonza, Natalia Gallot Escobal, Fernando Vidal Vanaclocha
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Patent number: 7615647Abstract: A process is provided for preparing pharmaceutical grade atorvastatin hemicalcium salt comprising: (a) deesterifying, wherein R is an ester protecting group to (b) extracting R(R*,R*)-3 into an organic solvent or mixture of solvents, (c) adding a base of formula NR1R2R3 wherein R1, R2 and R3 are independently selected from H, substituted or non-substituted C1 to C7 alkyl, C6 to C9 aryl, C8 to C10 aralkyl or aminoalkyl to form atorvastatin base salt, (d) isolating by precipitation of the above atorvastatin base salt and purifying when necessary, (e) converting atorvastatin base salt to atorvastatin hemicalcium salt by treatment with a calcium salt solution, and (f) isolating the atorvastatin hemicalcium salt.Type: GrantFiled: August 5, 2005Date of Patent: November 10, 2009Assignee: Apotex Pharmachem Inc.Inventors: K.S. Keshava Murthy, Yajun Zhao, Daqing Che, Bhaskar Reddy Guntoori, Sammy Chris Duncan, Stephen E. Horne
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Patent number: 7569704Abstract: The present invention relates to a novel dye compound, represented by the following formula (I): wherein R1, D1, D2, X, and Y are defined the same as the specification. The dye compound of the present invention is suitable for Dye-Sensitized Solar Cell (DSSC). In addition, the dye compound of the present invention has high molar absorption coefficient, so that the DSSC manufactured by the dye compound of the present invention can have good photoelectric characteristics.Type: GrantFiled: May 29, 2008Date of Patent: August 4, 2009Assignees: Everlight USA, Inc., Academia SinicaInventors: Jiann-T'suen Lin, Yung-Sheng Yen, Ying-Chan Hsu, Ta-Chung Yin
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Publication number: 20090123514Abstract: Conductive surfaces of e.g., implantable devices, coated with electropolymerized polymers having active substances attached thereto are disclosed. Electropolymerizable monomers designed and used for obtaining such conductive surfaces and processes, devices and methods for attaching the electropolymerized polymers to conductive surfaces are also disclosed. The polymers, processes and devices presented herein can be beneficially used in the preparation of implantable medical devices.Type: ApplicationFiled: July 19, 2006Publication date: May 14, 2009Applicant: Elutex Ltd.Inventor: Abraham J. Domb
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Patent number: 7507767Abstract: There are disclosed compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.Type: GrantFiled: February 6, 2002Date of Patent: March 24, 2009Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Neng-Yang Shih, Brian J. Lavey, Razia K. Rizvi, Bandarpalle B. Shankar, James M. Spitler, Ling Tong, Ronald L. Wolin, Michael K. Wong
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Patent number: 7488832Abstract: The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: GrantFiled: February 13, 2006Date of Patent: February 10, 2009Assignee: WyethInventors: Derek Cecil Cole, Eric Steven Manas, Lee Dalton Jennings, Frank Eldridge Lovering, Joseph Raymond Stock, William Jay Moore, John Watson Ellingboe, Jeffrey Scott Condon, Mohani Nirmala Sukhdeo, Ping Zhou, Junjun Wu, Koi Michele Morris
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Publication number: 20080275253Abstract: A practical and efficient method for halogenation of activated carbon atoms using readily available N-haloimides and a Lewis acid catalyst has been disclosed. This methodology is applicable to a range of compounds and any halogen atom can be directly introduced to the substrate. The mild reaction conditions, easy workup procedure and simple operation make this method valuable from both an environmental and preparative point of view.Type: ApplicationFiled: February 29, 2008Publication date: November 6, 2008Inventors: Yanhua Zhang, Hisashi Yamamoto, Kazutaka Shibatomi
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Publication number: 20080255169Abstract: The invention relates to sulphonamide derivatives of formula (I), where RC is optionally substituted 4-6-membered heterocyclic ring containing one or more N atoms, or RC forms together with the phenyl ring to which it is attached a benzodioxolyl group, or RC is —NR1R2, RA is a group having the formula RB is hydrogen or alkyl. The invention also relates to the use of derivatives of formula (I) as inhibitors for collagen receptor integrins and a process for preparing sulphonamides of formula (I).Type: ApplicationFiled: July 12, 2004Publication date: October 16, 2008Inventors: David Smith, Anne Marjamaki, Marika Ojala, Marjo Pihlavisto, Jyrki Heino, Jarmo Kapyla, Olli Pentikainen, Tommi Nyronen, Mark Johnson, Mikko Huhtala
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Patent number: 7414142Abstract: Compounds of formula I, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R3-R5, R10, and R11 are defined herein.Type: GrantFiled: September 18, 2006Date of Patent: August 19, 2008Assignee: WyethInventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
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Patent number: 7410999Abstract: The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)-(VI) as recited throughout the application.Type: GrantFiled: November 20, 2006Date of Patent: August 12, 2008Assignees: University of North Carolinia at Chapel Hill, Georgia State University Research Foundation, Inc., Auburn UniversityInventors: Christine C. Dykstra, Maurice Daniel Givens, David A. Stringfellow, Kenny Brock, David Boykin, Arvid Kumar, W. David Wilson, Richard R. Tidwell, Chad F. Stephens
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Patent number: 7326696Abstract: Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.Type: GrantFiled: December 15, 2003Date of Patent: February 5, 2008Assignee: Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Kwasi Ohemeng, Roger Frechette, Paul Abato, Victor Amoo, Haregewein Assefa, Joel Berniac, Beena Bhatia, Todd Bowser, Jackson Chen, Laura Honeyman, Mohamed Y. Ismail, Oak Kim, Rachid Mechiche, N. Laxma Reddy, Atul K. Verma, Peter Viski, Tadeusz Warchol, Ivan Yanachkov
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Patent number: 7314885Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for making the compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: March 22, 2006Date of Patent: January 1, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, Upul K. Bandarage, David J. Lauffer, Pan Li, Ronald C. Tomlinson
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Patent number: 7276612Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: April 6, 2004Date of Patent: October 2, 2007Assignee: Pharmacyclics, Inc.Inventors: Eric J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20070197620Abstract: The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification d or not; and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms.Type: ApplicationFiled: January 19, 2007Publication date: August 23, 2007Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 7250444Abstract: HMGCo-A reductase inhibitor compounds useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Methods of making and methods of using the compounds are also provided.Type: GrantFiled: June 7, 2004Date of Patent: July 31, 2007Assignee: Pfizer Inc.Inventors: Robert Michael Kennedy, William Keun-Chan Park, Bruce David Roth, Yuntao Song, Bharat K. Trivedi
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Patent number: 7241803Abstract: A group of compounds that inhibit HIV replication by blocking HIV entry was identified. Two representative compounds, designated NB-2 and NB-64, inhibited HIV replication (p24 production) with IC50 values <0.5 ?g/ml.Type: GrantFiled: November 12, 2003Date of Patent: July 10, 2007Assignee: New York Blood CenterInventors: Shibo Jiang, Asim Kumar Debnath
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Patent number: 7202368Abstract: A process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)benzamidine, the process comprising: (a) condensing an optionally suitably substituted diaminobenzene with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)phenylamino]acetic acid; (b) hydrogenating the product obtained from step (a); and (c) optionally carboxylating the amidino group of the product obtained from step (b).Type: GrantFiled: June 9, 2005Date of Patent: April 10, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Georg Zerban, Arndt Hausherr, Kerstin Schlarb, Heinz-Peter Schmitt, Bjoern Weyell, Gunter Koch, Rainer Hamm
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Patent number: 7186749Abstract: The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.Type: GrantFiled: August 22, 2005Date of Patent: March 6, 2007Assignee: WyethInventors: Thomas J. Commons, Douglas John Jenkins
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Patent number: 7179581Abstract: Resist compositions comprising nitrogen heterocyclic compounds having a pyrrole or nitrogen-bearing 5-membered ring structure and a polar functional group have an excellent resolution and an excellent focus margin and are useful in microfabrication using electron beams or deep-UV light.Type: GrantFiled: May 20, 2004Date of Patent: February 20, 2007Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Takeru Watanabe, Jun Hatakeyama
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Patent number: 7138423Abstract: The present disclosure relates to chemical compounds and their use in treatment of human diseases. A particular embodiment relates to compounds of Formula (I) or an isomer, a pharmaceutically acceptable salts or solvates thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.Type: GrantFiled: July 18, 2005Date of Patent: November 21, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Huan He, Joanne J. Bronson
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Patent number: 7109243Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: March 23, 2004Date of Patent: September 19, 2006Assignee: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Patent number: 6969744Abstract: Disclosed is a method of preparing terminally functionalized telechelic polymers using a cationic living polymer product or a terminal tert-chloride chain end of a carbocationic quasiliving polymer product, which comprises quenching the polymer product with an N-substituted pyrrole to thereby functionalize the N-substituted pyrrole at the terminal reactive polymer chain end(s). Also disclosed are the terminal functionalized polyisobuyl N-substituted pyrrole compounds where the polyisobutyl group is substituted at the 2 and 3 position of the N-substituted pyrrole.Type: GrantFiled: June 19, 2003Date of Patent: November 29, 2005Assignees: University of Southern Mississippi, Chevron Oronite Company LLCInventors: Casey D. Stokes, Robson F. Storey, James J. Harrison
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Patent number: 6933390Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.Type: GrantFiled: July 15, 2004Date of Patent: August 23, 2005Assignee: Warner-Lambert CompanyInventors: Hubert Barth, Klaus Steiner, Simon Schneider, Ulrich Bayer, Manfred Westermayer, Ulrike Wolfsperger, Hans-Jürgen Betche
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Patent number: 6911468Abstract: A compound of the formula (I): wherein X1 and X2 are the same or different and each is a bond or a spacer having 1 to 20 atom(s) in the main chain; one of R1 and R2 is a cycle group having substituent(s) selected from 1) an optionally substituted carboxy-C1-6 alkoxy group and 2) an optionally substituted carboxy-C1-6 aliphatic hydrocarbon group, wherein the cycle group optionally has additional substituent(s), and the other is an optionally substituted cycle group or a hydrogen atom; and R3, R4 and R5 are the same or different and each is a hydrogen atom or a substituent, or R4 may link together with R3 or R5 to form an optionally substituted ring; provided that when R3 is a hydrogen atom, R4 is a hydrogen atom and R5 is methyl, X2—R2 is not 4-cyclohexylphenyl; when R3 is 4-methoxyphenyl, R4 is a hydrogen atom and R5 is methyl, X2—R2 is not 4-methoxyphenyl; and when R1 or R2 is a hydrogen atom, the adjacent X1 or X2 is not a C1-7 alkylene; or a salt thereof exhibits a protein tyrosine phosphatase inhibiType: GrantFiled: May 21, 2001Date of Patent: June 28, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Takahiro Matsumoto, Nozomi Katayama, Hiroshi Mabuchi
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Patent number: 6864270Abstract: Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.Type: GrantFiled: August 8, 2002Date of Patent: March 8, 2005Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 6723753Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.Type: GrantFiled: February 7, 2002Date of Patent: April 20, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6677368Abstract: The present invention relates to 4-arylindolinones, as well as pharmaceutical compositions thereof, capable of modulating protein kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. The present invention also relates to methods for treating protein kinase related disorders.Type: GrantFiled: December 20, 2001Date of Patent: January 13, 2004Assignee: Sugen, Inc.Inventors: Jingrong Cui, Ruofei Zhang, Hong Shen, Ji Yu Chu, Fang-Jie Zhang, Marcel Koenig, Steven Huy Do, Xiaoyuan Li, Chung Chen Wei, Peng Cho Tang
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Patent number: 6649658Abstract: A description is given here of novel solid and stable derivatives of (−)-verbenone having formula (I) wherein, when X=O Z=H, ═CHAr, ═C(OH)COOEt, ═NOR; Y=H, NH2, NH3+X1−, NHCOAr, NHCOR, NHCONHR, NHCONHAr, X1-=pharmaceutically acceptable anion; Ar-aryl or heteroaryl, preferably phenyl, 4-chlorophenyl, 2-furyl, 2-thienyl, 2-hydroxyphenyl, 2-acetoxyphenyl; R=H, C1-C4 alkyl, C4-C6 cycloalkyl, CH2COOH, CH2COOEt, CH2COCH3, CH2CN, CH2COCH2COOEt, CH2C6H5; and, when X=dimethylamino, diethylamino, pyrrolidino, piperidino or morpholino: Y=H; Z=H, CONHAr, COHNR; Ar=aryl, preferably phenyl; R=H, C1-C4 alkyl, C4-C6 cycloakyl. A description is also given of the processes for the preparation of these derivatives and of the novel intermediates used in those processes. The novel derivatives are characterized by their solubility in water; some of them also have a high anti-inflammatory activity.Type: GrantFiled: October 15, 2001Date of Patent: November 18, 2003Assignee: Euphar Group SRLInventors: Paolo Corvi Mora, Angelo Ranise
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Patent number: 6632963Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): in which Ar1 is a radical having one of the structural formulae (a)-(c): Ar2 is a radical having one of the following formulae (d)-(h): and X is a radical having one of the following formulae (i)-(l): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: March 29, 1999Date of Patent: October 14, 2003Assignee: Galderma Research & Development S.N.C.Inventor: Jean-Michel Bernardon
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Patent number: 6603013Abstract: The present invention relates to a process wherein heterogeneous finely-dispersed palladium catalysts are used in a cross-coupling reaction of alkenyl halides and aryl or heteroaryl boronic acids in the presence of base in an aprotic solvent to produce aryl- or heteroaryl-olefin compounds of Formula I:Type: GrantFiled: July 16, 2001Date of Patent: August 5, 2003Assignee: Merck & Co., Inc.Inventors: Yongkui Sun, Carl LeBlond, John R. Sowa, Jr.
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Patent number: 6579987Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioaryl-alkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is seleType: GrantFiled: December 20, 2002Date of Patent: June 17, 2003Assignee: NPS Allelix CorporationInventors: Ian Egle, Jennifer Frey, Methvin Isaac
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Patent number: 6576780Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: October 13, 2000Date of Patent: June 10, 2003Assignee: GD Searle & CompanyInventors: Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth
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Patent number: 6531472Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, X and Y have the meanings defined in the specification. The compounds have histone deacetylase (HDAC) inhibitory activity which is useful in cancer treatment. Also provided is a process for making a compound of formula I by reacting a compound of formula III with a compound of formula IV wherein A is a displaceable group and PG is a protecting group.Type: GrantFiled: December 4, 2001Date of Patent: March 11, 2003Assignee: Hoffman-La Roche Inc.Inventors: Guy Georges, Adelbert Grossmann, Tim Sattelkau, Wolfgang Schaefer, Ulrich Tibes
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Patent number: 6525085Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioaryl-alkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is selecType: GrantFiled: June 17, 2002Date of Patent: February 25, 2003Assignee: NPS Allelix Corp.Inventors: Ian Egle, Jennifer Frey, Methvin Isaac
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Patent number: 6492413Abstract: 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: March 20, 2000Date of Patent: December 10, 2002Assignee: 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: 6489515Abstract: Here is provided a process capable of efficiently carrying out a gas-phase dehydration reaction comprising contacting a raw material gas with a solid oxide catalyst containing an alkali metal element to allow reaction to progress by inhibiting decomposition of the raw material and the objective product. This process comprises using a sintered oxide comprising an alkali metal element and silica and/or alumina as a loading material for preheating of the raw material gas and/or as a supporting material for fixation of the position of the catalyst.Type: GrantFiled: January 26, 2001Date of Patent: December 3, 2002Assignee: Nippon Shokubai Co., Ltd.Inventors: Hideyuki Kambe, Shukichi Ugamura, Yuuji Shimasaki, Shinji Takasaki
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Patent number: 6465471Abstract: Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: July 1, 1999Date of Patent: October 15, 2002Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, John Clifford Head, John Robert Porter, Sarah Catherine Archibald
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Patent number: 6441177Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.Type: GrantFiled: December 16, 1999Date of Patent: August 27, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synèse Jolidon, Hans Lengsfeld, Olivier Morand, Gérard Schmid, Yu-Hua Ji
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Patent number: 6417372Abstract: The present invention relates to arylpyrrole particles which are prepared by a process in which the particles are aged and milled, and pesticidal suspension concentrate compositions comprising them. The size of the particles of this invention remains surprisingly stable during storage.Type: GrantFiled: April 2, 2001Date of Patent: July 9, 2002Assignee: BASF AktiengesellschaftInventors: Mimi Yih-Pei Chou Schaaf, Steven Brunt, Jian James Xu, Andrew Evelyn Goldsmith, Anthony Francis Walker, Patrick C. Mowery, Edward S. Donoghue, Srinivasan Rajan
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Publication number: 20020058691Abstract: 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.Type: ApplicationFiled: March 20, 2000Publication date: May 16, 2002Inventors: JOHN J. TALLEY, Stephen R. Bertenshaw, Paul W. Collins, Thomas D. Penning, David B. Reitz, Ronald S. Rogers
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Patent number: 6331636Abstract: This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.Type: GrantFiled: March 12, 1992Date of Patent: December 18, 2001Assignee: The Upjohn CompanyInventors: Arthur G. Romero, William H. Darlington
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Patent number: 6294568Abstract: The present invention provides compounds represented by the general formula (I): and a salt thereof, and anti-inflammatory agents and antitumor agents containing the compounds as the active ingredients.Type: GrantFiled: June 26, 2000Date of Patent: September 25, 2001Assignee: Nissin Food Products Co., Ltd.Inventors: Toshihiro Yamada, Yoichi Nobuhara, Kazuhiro Kobayashi, Satoshi Hirano, Takanobu Sakurai, Hiroshi Mikami, Ayako Miyake
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Patent number: 6248765Abstract: Novel imidazole derivatives as histamine receptor H3 antagonists and/or agonists, preparation thereof and therapeutical uses thereof. Chemical compounds for use as histamine receptor H3 agonists, partial agonists or antagonists, having general formula (Ia) or (Ib), the use thereof for making drugs, and methods for revealing the agonist, partial agonist or antagonist activity of such compounds in vivo, are disclosed.Type: GrantFiled: January 9, 1997Date of Patent: June 19, 2001Assignees: Institut National de la Sante et de la Recherche Medical, Societe Civile BioprojetInventors: Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Agnes Quemener, Jeanne-Marie Lecomte, Xavier Ligneau, Walter G. Schunack, Holger Stark, Katja Purand, Annette Huls, Reidemeister Sybille, Athmani Salah, Charon Robbin Ganellin, Nadia Pelloux-Leon, Wasyl Tertiux, Michael C. O. Krause, Sadek Bassem
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Patent number: 6242613Abstract: The present invention relates to arylpyrrole particles which are prepared by a process in which the particles are aged and milled, and pesticidal suspension concentrate compositions comprising them. The size of the particles of this invention remains surprisingly stable during storage.Type: GrantFiled: April 6, 1999Date of Patent: June 5, 2001Assignee: American Cyanamid Co.Inventors: Mimi Yih-Pei Chou Schaaf, Steven Brunt, Jian James Xu, Andrew Evelyn Goldsmith, Anthony Francis Walker, Patrick C. Mowery, Edward S. Donoghue, Srinivasan Rajan
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Patent number: 6194599Abstract: The present invention provides a process for preparing biaryl compounds comprising reacting an arylzinc reagent with an arylchloride in the presence of a nickel catalyst or a palladium catalyst. The present invention specifically provides a process for the preparation of 2-(4′-methylphenyl)benzonitrile comprising reacting a 4-methylphenylzinc reagent with 2-chlorobenzonitrile in the presence of a nickel catalyst or a palladium catalyst.Type: GrantFiled: April 8, 1997Date of Patent: February 27, 2001Assignee: Catalytica, Inc.Inventors: Joseph A. Miller, Robert P. Farrell