Nitrogen Bonded Directly To The Bicyclo Ring System Patents (Class 549/439)
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Patent number: 10035760Abstract: Compounds of Formula I with activity against HIV, including pharmaceutical compositions and methods for using these compounds in treating human immunodeficiency virus (HIV) infection, are set forth:Type: GrantFiled: October 23, 2014Date of Patent: July 31, 2018Assignee: ViiV HEALTHCARE UK (NO. 5) LIMITEDInventors: Annapurna Pendri, Guo Li, John A. Bender, Zhong Yang, Alan Xiangdong Wang, Brett R. Beno, Robert A. Fridell, Makonen Belema, Nicholas A. Meanwell, Robert G. Gentles
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Publication number: 20140121242Abstract: The present invention relates to substituted cinnamamide derivatives, the method for preparing thereof and the use thereof. Each of said derivatives has a structure of formula (I). The method for preparing the substituted cinnamamides and their derivatives of the present invention is also disclosed. Substituted piperonal derivatives are selected as starting materials to prepare the substituted cinnamamide derivatives of the present invention by Wittig reaction and acid-amine condensation reaction. Further, a use of the present compounds in preventing and treating depressive-type mental diseases is disclosed.Type: ApplicationFiled: June 26, 2012Publication date: May 1, 2014Applicant: TASLY PHARMACEUTICAL GROUP CO., LTD.Inventors: Xiaohui Ma, Yuanpeng Jin, Min Han, Shuiping Zhou, Wangyi Zhou, Xuejun Luo, Guocheng Wang, Lulu Yan, Lanlan Zhang, Yonghong Zhu
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Patent number: 8653286Abstract: Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.Type: GrantFiled: August 7, 2012Date of Patent: February 18, 2014Assignee: Nektar TherapeuticsInventors: Samuel P. McManus, Antoni Kozlowski, Tracy L. Hutchison, Brian Bray, Xiaoming Shen
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Patent number: 8648071Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.Type: GrantFiled: June 26, 2009Date of Patent: February 11, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Joseph Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
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Publication number: 20130338210Abstract: A method for delivering a nucleic acid to a cell can include exposing sample cells to a composition which includes charged lipids.Type: ApplicationFiled: December 7, 2010Publication date: December 19, 2013Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Khallanthottathil G. Rajeev, Muthusamy Jayaraman, David Butler, Mamta Kapoor, Rajesh Kumar Kainthan
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Publication number: 20130331328Abstract: Small molecule inhibitors of AGBL2 are provided, as well as methods of using the inhibitors to treat or prevent cancer and neurologic disorders.Type: ApplicationFiled: February 14, 2012Publication date: December 12, 2013Applicant: GEORGETOWN UNIVERSITYInventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Ziad Sahab
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Patent number: 8450506Abstract: The present invention relates to compounds of formula (I), where R1 and R2, which may be identical or different, are selected from the group comprising H, CnH2n-1, a linear or branched alkyl group having 1 to 6 carbons, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is —CO—CH3, —NHOH, —OH, or —OR6 where R6 is a linear or branched alkyl group having 1 to 6 carbon atoms; R4 is H, linear or branched alkyl group having from 1 to 6 atoms, phenyl, benzyl, —CF3 or CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.Type: GrantFiled: February 15, 2012Date of Patent: May 28, 2013Assignee: Nogra Pharma LimitedInventors: Giancarlo Naccari, Sergio Baroni
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Patent number: 8362024Abstract: This invention relates to novel purinyl derivatives of formula Ia or Ib Wherein the symbols are as defined in the Specification and of pharmaceutically acceptable salts thereof useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, for the preparation of a medicament for such treatment and to pharmaceutical compositions containing such compounds.Type: GrantFiled: March 27, 2008Date of Patent: January 29, 2013Assignee: NeuroSearch A/SInventors: Birgitte L. Eriksen, Ulrik Svane Sørensen, Charlotte Hougaard, Dan Peters, Tina Holm Johansen, Palle Christophersen
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Publication number: 20130005019Abstract: The invention relates to a caged lysine, wherein the caged lysine is according to Formula (I): or salts thereof. The invention further relates to polypeptides comprising a caged lysine, and to methods of making same. The invention further relates to tRNA synthetases capable of charging tRNA with caged lysine.Type: ApplicationFiled: March 4, 2011Publication date: January 3, 2013Applicants: North Carolina State University, Medical Research CouncilInventors: Jason Chin, Duy P. Nguyen, Arnaud Gautier, Alexander Dieters
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Publication number: 20120283101Abstract: The present invention pertains to plant additives containing a molecule selected in a family of compounds, wherein said molecule can modulate some molecular markers and physiological modifications observed in cases of phosphate deficiency. The family of compounds comprises the molecule MC2 of formula (I) as well as analogues thereof.Type: ApplicationFiled: September 17, 2010Publication date: November 8, 2012Inventors: Mathilde Clement, Thierry Desnos, Laurent Nussaume
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Patent number: 8258324Abstract: Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.Type: GrantFiled: September 15, 2011Date of Patent: September 4, 2012Assignee: Nektar TherapeuticsInventors: Samuel P. McManus, Antoni Kozlowski, Tracy L. Hutchison, Brian Bray, Xiaoming Shen
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Patent number: 8163943Abstract: The present invention is to provide manufacturing intermediates which can be led to useful ?-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: wherein R1 and R2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R6—O— or R7—N(R8)—; where R6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R7 and R8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R4 and R5 represent the same groups as R7 and R8, respectively, and R4 and R5 optionally form a ring together; and X represents —O— or —N(R9)—, where R9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R4 or R5, andType: GrantFiled: October 31, 2007Date of Patent: April 24, 2012Assignee: Seikagaku Kogyo Kabushiki KaishaInventors: Nobuo Kobayashi, Tsuneo Koji, Takashi Fujita, Tomofumi Nishimura, Akihiko Hosoda
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Patent number: 8138357Abstract: Therefore the present invention relates specifically to the compounds of general formula (I), in which R1 and R2, which may be identical or different, are selected from the group comprising H, —CnH2n-1, a linear or branched alkyl group having from 1 to 6 carbon atoms, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is selected from —CO—CH3, —NHOH, —OH, —OR6 in which R6 is a linear or branched alkyl group having from 1 to 6 carbon atoms; R4 is selected from H, a linear or branched alkyl group having from 1 to 6 carbon atoms, phenyl, benzyl, —CF3 or —CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O. and use thereof in the medical field.Type: GrantFiled: July 24, 2006Date of Patent: March 20, 2012Assignee: Giuliani International LimitedInventors: Giancarlo Naccari, Sergio Baroni
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Publication number: 20120046288Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: June 26, 2009Publication date: February 23, 2012Inventors: Joseph A. Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
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Publication number: 20120027796Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).Type: ApplicationFiled: November 10, 2009Publication date: February 2, 2012Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, David Butler, Jayaprakash K. Narayanannair, Muthusamy Jayaraman, Laxmab Eltepu
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Publication number: 20110224260Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.Type: ApplicationFiled: May 24, 2011Publication date: September 15, 2011Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Yueh-Hsiung Kuo, Ming-Jai Su
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Publication number: 20110201577Abstract: The present application relates to processes for the preparation of oseltamivir and the H3PO4 salt of oseltamivir, Tamiflu®. The application further relates to novel intermediate compounds and to pharmaceutical compositions containing said compounds. The application further relates to a method of using the novel intermediates to treat or prevent influenza.Type: ApplicationFiled: May 12, 2009Publication date: August 18, 2011Applicant: BROCK UNIVERSITYInventors: Tomas Hudlicky, Bradford Sullivan
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Publication number: 20110071142Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g.Type: ApplicationFiled: March 19, 2010Publication date: March 24, 2011Applicant: BETH ISRAEL DEACONESS MEDICAL CENTERInventors: Peter Oettgen, Alan C. Rigby, Towia Libermann
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Publication number: 20100324266Abstract: Novel compounds are provided, which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Y, wherein Y is a chemical structure as shown in FIG. 1. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.Type: ApplicationFiled: June 9, 2010Publication date: December 23, 2010Applicant: Affymetrix, INC.Inventors: Anthony D. Barone, Glenn H. McGall
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Publication number: 20100286204Abstract: There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0Type: ApplicationFiled: November 19, 2008Publication date: November 11, 2010Applicant: Sterix LimitedInventors: Nigel Vicker, Helen Victoria Bailey, Wesley Heaton, Joanna Mary Day, Atul Purohit, Barry Victor Lloyd Potter
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Patent number: 7825278Abstract: The invention relates to substituted enaminones of Formula I and their derivatives and the discovery that these compounds modulate the effect of ?-aminobutyric acid (GABA) on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.Type: GrantFiled: May 5, 2005Date of Patent: November 2, 2010Assignee: The Regents of the University of CaliforniaInventors: Derk J. Hogenkamp, Timothy B. C. Johnstone, Kelvin W. Gee
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Patent number: 7790689Abstract: The present invention relates to monosaccharide derivatives as anti-inflammatory agents. The compounds disclosed herein can be useful for inhibition and prevention of inflammation and associated pathologies including inflammatory and autoimmune diseases such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection, psoriasis, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis and allergic rhinitis. Pharmacological compositions containing compounds disclosed herein and the methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, type I diabetes, psoriasis, allograft rejection, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis, allergic rhinitis and other inflammatory and/or autoimmune disorders, using the compounds are also provided.Type: GrantFiled: May 30, 2007Date of Patent: September 7, 2010Assignee: Ranbaxy Laboratories LimitedInventors: Ashwani Kumar Verma, Sanjay Malhotra, Sankaranarayanan Dharmarajan, Abhijit Ray, Rajkumar Shirumalla
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Publication number: 20100137600Abstract: This invention describes reagent precursors and methods for chemical and biochemical reactions. These reagent precursors that can be activated in solution upon irradiation to generate reagents required for the subsequent chemical reactions. Specifically, photogenerated reagents (PGR) are useful for controlling parallel combinatorial synthesis and various chemical and biochemical reactions.Type: ApplicationFiled: May 18, 2009Publication date: June 3, 2010Inventors: Xiaolian Gao, Zhuo Xiaochruan, Wu Yao, Jean-Phillipe Pollols
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Publication number: 20100113400Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and minocycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: ApplicationFiled: May 28, 2009Publication date: May 6, 2010Applicant: Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Roger Frechette, Mohamed Y. Ismail, Laura Honeyman, Todd Bowser, Beena Bhatia
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Publication number: 20100035849Abstract: The present invention provides novel methylenedioxy phenolic compounds and their derivatives, methods of making them and methods of using them to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease.Type: ApplicationFiled: August 5, 2009Publication date: February 11, 2010Applicants: OHIO STATE UNIVERSITY RESEARCH FOUNDATION, INVASC THERAPEUTICS, INC.Inventors: Sampath Parthasarathy, Sanjay Rajagopalan, Desikan Rajagopal
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Patent number: 7652006Abstract: The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.Type: GrantFiled: February 6, 2004Date of Patent: January 26, 2010Assignee: Euro-Celtique S.A.Inventors: Ravi Upasani, Sui X Cai, Nancy C Lan, Yan Wang, George Field, David B Fick
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Patent number: 7544682Abstract: The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.Type: GrantFiled: January 8, 2007Date of Patent: June 9, 2009Assignee: Sanofi-AventisInventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Pierre Perreaut
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Publication number: 20090124686Abstract: The invention relates to urea derivatives of formula (I) as inhibitors of glycogen synthase kinase 3?, GSK-3, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which GSK-3 is involved, such as Alzheimer's disease or non-insulin dependent diabetes mellitus.Type: ApplicationFiled: July 28, 2006Publication date: May 14, 2009Applicant: NEUROPHARMA, S.A.Inventors: Ana Martinez Gil, Miguel Medina Padilla, Mercedes Alonso Cascon, Ana Fuertes Huerta, Maria Luisa Navarro Rico, Maria Jose Perez Puerto, Ana Castro Morera, Ester Martin Aparicio
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Publication number: 20090082395Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.Type: ApplicationFiled: September 9, 2008Publication date: March 26, 2009Inventor: Richard D. Gless, JR.
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Patent number: 7452999Abstract: Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features: (1) make use of a particular ?-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxy-propionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.Type: GrantFiled: February 20, 2004Date of Patent: November 18, 2008Assignee: Novartis AGInventors: Mahavir Prashad, Hong-Yong Kim, Bin Hu, Joel Slade, Prasad Koteswara Kapa, Michael John Girgis
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Patent number: 7442793Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: December 11, 2003Date of Patent: October 28, 2008Assignee: SmithKline Beecham CorporationInventors: Jinhwa Lee, Siegfried B. Christensen, IV
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Publication number: 20080221206Abstract: The present invention relates to lidocaine derived compounds, which present less anesthetic activity than lidocaine itself, but with more anti-inflammatory and spasmolytic activity than said lidocaine as well as pharmaceutical compositions with at least one of these compounds or a salt of those as active principle and to the use of such compositions to treat, prevent or inhibit atopic diseases including asthma, rhinitis, allergic urticaria, chronic lung inflammation associated with eosinophilia, following the example of atopic asthma and chronic intestinal inflammation, as colitis for instance. The pharmaceutical composition may be available in spray form, solution, suspension, emulsion destinated to be applied by nebulization, or in any of the pharmaceutical available forms for oral or injectable use.Type: ApplicationFiled: June 7, 2005Publication date: September 11, 2008Applicant: FUNDÇÃO OSWALDO CRUZ-FIOCRUZInventors: Marco Aurelio Martins, Jorge Carlos Santos Da Costa, Nubia Boechat, Rodrigo de Azeredo Siqueira
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Patent number: 7417153Abstract: A method for the production of acetals and ketals of 3-amino-5-(hydroxymethyl) cyclopenlane-1,2-diols of formula (I): (and/or the enantiomer), where R1 is H, C1-6-alkyl, C3-8-cycloalkyl or benzyl and (i) R2 is methyl and R3 is ethyl, (ii) R2 is H and R3 is C1-6-alkyl or phenyl or (iii) R2 and R3 together form a group of formula —(CH2)n— with n=4 to 6, present as free amines or as salts of di- or tri-basic organic acids, starting from 2-acetyl-2-aza-bicyclo[2.2.1]hept-5-en-3-one of formula (II): (and/or the enantiomer). The method is equally useful, depending on the starting material, for the production of enantiomerically-pure compounds, or mixtures with arbitrary enantiomeric content.Type: GrantFiled: January 24, 2005Date of Patent: August 26, 2008Assignee: Lonza AGInventors: Gareth-John Griffiths, Silvia Lange, Walter Brieden
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Patent number: 7326799Abstract: The present invention is to provide manufacturing intermediates which can be led to useful ?-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: wherein R1 and R2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R6—O— or R7—N(R8)—; where R6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R7 and R8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R4 and R5 represent the same groups as R7 and R8, respectively, and R4 and R5 optionally form a ring together; and X represents —O— or —N(R9)—, where R9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R4 or R5, andType: GrantFiled: December 30, 2002Date of Patent: February 5, 2008Assignee: Seikagaku Kogyo Kabushiki KaishaInventors: Nobuo Kobayashi, Tsuneo Koji, Takashi Fujita, Tomofumi Nishimura, Akihiko Hosoda
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Patent number: 7291744Abstract: The present application describes modulators of chemokine receptors of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: November 12, 2004Date of Patent: November 6, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Soo S. Ko, Douglas G. Batt, George V. Delucca, John V. Duncia, Daniel S. Gardner, Joseph B. Santella
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Patent number: 7259267Abstract: The invention relates to difluorobenzo-1,3-dioxoles, to a process for their preparation, and to their use for preparing medicaments and crop protection agents.Type: GrantFiled: May 11, 2005Date of Patent: August 21, 2007Assignee: LANXESS Deutschland GmbHInventors: Axel Pleschke, Albrecht Marhold
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Patent number: 7208169Abstract: The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: GrantFiled: April 16, 2003Date of Patent: April 24, 2007Assignee: Bayer CropScience LPInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Robert Markert, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Martin Kugler, Thomas Jaetsch
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Patent number: 7166600Abstract: The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1–R4, m, n, o and p are as defined herein. Also provided are compositions comprising compounds of formula I and a carrier, diluent or excipient as well as methods of treating a disease or condition mediated by the binding interaction of alpha-4 integrins to its ligands such as inflammatory diseases.Type: GrantFiled: January 11, 2006Date of Patent: January 23, 2007Assignee: Genentech, Inc.Inventor: David Y. Jackson
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Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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Patent number: 7148242Abstract: N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl]-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes or imidazacyclo4-7alkanes have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections.Type: GrantFiled: June 14, 2002Date of Patent: December 12, 2006Assignee: Novartis AGInventors: Jeffrey Jacobs, Rakesh K. Jain, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 7105567Abstract: The present invention relates to a urea derivative of the formula (1) wherein each symbol is as described in the specification, a pharmaceutically acceptable salt thereof and pharmaceutical use thereof. The compound of the present invention has a C5a receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of diseases or syndromes due to inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis, pancreatitis and the like) due to activation of leukocytes caused by ischemia, trauma, burn, surgical invasion and the like].Type: GrantFiled: August 10, 2001Date of Patent: September 12, 2006Assignee: Mitsubishi Pharma CorporationInventors: Seigo Ishibuchi, Hiroshi Sumichika, Katsuhiko Itoh, Yoichi Naka
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 7015323Abstract: The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1–R4, m, n, o and p are as defined herein. Also provided are compositions comprising compounds of formula I and a carrier, diluent or excipient as well as methods of treating a disease or condition mediated by the binding interaction of alpha-4 integrins to its ligands such as inflammatory diseases.Type: GrantFiled: May 19, 2004Date of Patent: March 21, 2006Assignee: Genentech, Inc.Inventor: David Y. Jackson
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Patent number: 6984661Abstract: The present invention is directed to compounds of the structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof: Formula I (a) R1, R2 and R6 are each independently selected from the group consisting of hydrogen, C1-C8 alkyl substituted C1-C8 alkyl, aryl-C0-4-alkyl, substituted aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, substituted heteroaryl-C0-4-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl, and substituted C3-C6 cycloalkylaryl-C0-2-alkyl; (b) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S; (c) Y is C, O, S, NH or a single bond; and (d) E is selected from the group consisting of hydrogen, C(R3)(R4)A, A, (CH2)n COOR19 and substituted (CH2)n COOR19.Type: GrantFiled: January 21, 2003Date of Patent: January 10, 2006Assignee: Eli Lilly and CompanyInventors: James Robert Henry, YiHong Li
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Patent number: 6965040Abstract: This invention describes reagent precursors and methods for chemical and biochemical reactions. These reagent precursors that can be activated in solution upon irradiation to generate reagents required for the subsequent chemical reactions. Specifically, photogenerated reagents (PGR) are useful for controlling parallel combinatorial synthesis and various chemical and biochemical reactions.Type: GrantFiled: November 4, 2003Date of Patent: November 15, 2005Inventors: Xiaolian Gao, Jean Philippe Pellois, Wu Yao
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Patent number: 6780998Abstract: The oxidation hair dye precursor composition contains from 0.005 to 20.0 percent by weight of one or more coupler compounds and from 0.005 to 20.0 percent by weight of one or more developer compounds. The one or more developer compounds include at least one substituted 2-aminoalkyl-1,4-diaminobenzene compound of the formula (I): New substituted 2-aminoalkyl-1,4-diaminobenzene compounds of formula (I) are described.Type: GrantFiled: April 17, 2002Date of Patent: August 24, 2004Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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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: 6710089Abstract: 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-fused-phenyl-N-benzyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: March 23, 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: 6699990Abstract: The present patent application relates to 3-(2,5-diaminophenyl)acrylamide derivatives of general formula (I) or to physiologically tolerated, water-soluble-salts thereof and to agents containing said compounds and used for oxidative dyeing of fibers.Type: GrantFiled: October 21, 2002Date of Patent: March 2, 2004Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6608061Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.Type: GrantFiled: February 14, 2000Date of Patent: August 19, 2003Assignees: Kyoma Hakko Kogyo Co., Ltd., Fuji Photo Film Co., Ltd.Inventors: Yoshiyuki Yonetani, Takeshi Takahashi, Yuko Kanda, Tamio Mizukami, Tatsuya Tamaoki, Shun-ichi Ikeda, Masanobu Takashima, Naoki Asanuma, Tadashi Inaba, Hiroshi Takeuchi, Hiroshi Kawamoto, Yoshihisa Tsukada, Masato Satomura, Hiroshi Kitaguchi