Polycyclo Ring System Patents (Class 562/466)
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Publication number: 20110053974Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.Type: ApplicationFiled: September 29, 2010Publication date: March 3, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Narihiro TODA, Masao YOSHIDA, Rieko TAKANO, Masahiro INOUE, Takeshi HONDA, Koji MATSUMOTO, Ryutaro NAKASHIMA
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Publication number: 20110034528Abstract: The present invention describes Elansolids, a new class of novel anti-bacterial compounds of formula (I).Type: ApplicationFiled: February 19, 2009Publication date: February 10, 2011Inventors: Klaus Gerth, Heinrich Steinmetz, Gerhard Höfle
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Patent number: 7872026Abstract: Novel ligand compounds having the structural formula (I): in which: Ar is a radical selected from among the radical of formulae (a) to (c) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, or, alternatively, into cosmetic compositions.Type: GrantFiled: June 8, 2006Date of Patent: January 18, 2011Assignee: Galderma Research & DevelopmentInventors: Thibaud Biadatti, Olivier Roye
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Publication number: 20110009623Abstract: Methods and an apparatus for producing stable crystal polymorphs are provided. Inner surfaces of glass vials with a concave bottom topography are coated with nonstick compounds to select for nucleation of stable polymorphs.Type: ApplicationFiled: March 20, 2007Publication date: January 13, 2011Applicant: Worcester Polytechnic InstituteInventors: Jason R. Cox, Marta Dabros, Venkat R. Thalladi
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Publication number: 20100298367Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: ApplicationFiled: March 4, 2009Publication date: November 25, 2010Inventors: Sean P. Brown, Paul J. Dransfield, Jonathan Houze, Todd J. Kohn, Jiwen Liu, Julio Medina, Vatee Pattaropong, Wang Shen, Marc Vimolratana, Yingcai Wang, Ming Yu, Liusheng Zhu
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Publication number: 20100282622Abstract: Moderate moisture levels, such as greater than 3% but no greater than 7%, may be beneficial for solid formulations of certain prostacyclin analogs. Accordingly, a solid formulation containing a prostacyclin analog may be packaged inside a pharmaceutical packaging with such amount of a desiccant or a drying agent that after the storage the solid formulation may have a moderate level of moisture in it.Type: ApplicationFiled: May 6, 2010Publication date: November 11, 2010Inventor: Kenneth R. Phares
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Publication number: 20100278896Abstract: A solid, implantable dosage form comprising a therapeutically active agent in solid form, optionally with one or more pharmaceutically acceptable excipients, wherein the one or more excipients, when present, do not lead to a significant delay or prolongation of the release of active agent, as compared to an equivalent dosage form containing no excipients when tested in vitro.Type: ApplicationFiled: November 17, 2008Publication date: November 4, 2010Applicant: UCL BUSINESS PLCInventors: Peng T. Khaw, Stephen Brocchini
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Publication number: 20100273883Abstract: Novel ligand compounds having the structural formula (I): in which: Ar is a radical selected from among the radicals of formulae (a)-(c) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, or, alternatively into cosmetic compositions.Type: ApplicationFiled: July 6, 2010Publication date: October 28, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Thibaud Biadatti, Jean-Marie Arlabosse
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Publication number: 20100227927Abstract: The present invention concerns salts of Tramadol and Naproxen and their crystalline forms, and compositions thereof, for the treatment of pain, as well as their process for preparation.Type: ApplicationFiled: July 31, 2008Publication date: September 9, 2010Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Helmut Heinrich Buschmann, Antoni Torrens-Jover, Josep Mas-Prio, Jordi Benet-Buchholz, Lluis Sola-Carandell, Jordi Carles Ceron-Bertran
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Publication number: 20100216694Abstract: Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.Type: ApplicationFiled: October 27, 2008Publication date: August 26, 2010Inventors: Gui-Bai Liang, Xibin Liao, Weiguo Liu, Paul E. Finke, Dooseop Kim, Lihu Yang, Songnian Lin
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Publication number: 20100204199Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.Type: ApplicationFiled: April 14, 2010Publication date: August 12, 2010Inventors: Xiang-Yang Ye, Jeffrey A. Robl, Ronald L. Hanson, Zhiwei Guo, Ramesh N. Patel
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Publication number: 20100204234Abstract: The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.Type: ApplicationFiled: March 27, 2008Publication date: August 12, 2010Inventors: Rolf Hartmann, Martin Frotscher, Sandrine Oberwinkler, Erika Ziegler, Josef Messinger, Heinrich-Hubert Thole
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Publication number: 20100152272Abstract: Compounds selected from: where DRUG-OH, DRUG-COOH and DRUG-NH2 are biologically active compounds; each X is independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone moiety), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO—, where y is 2-4 or 6-24 and —(CH2CH2O)zCH2COO—, where z is 2-24; each Y is independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester moiety), —COCH2CH2CH2CH2CH2O— (caprolactone ester moiety), —CO(CH2)mO—, where m is 2-4 or 6-24 and —COCH2O(CH2CH2O)n— where n is between 2-24; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; and p is 1-6. Multi-functional compounds and drug dimers, oligomers and polymers are also disclosed.Type: ApplicationFiled: February 17, 2010Publication date: June 17, 2010Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
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Publication number: 20100152409Abstract: Triptycene derivatives and method for preparing the same are provided. The triptycene derivatives may be triptycene di-ester of the formula (I) or triptycene di-acid of the formula (II): where n=1-5.Type: ApplicationFiled: December 29, 2008Publication date: June 17, 2010Applicant: TAIWAN TEXTILE RESEARCH INSTITUTEInventors: Chin-Wen Chen, I-Pin Fu, Yu-Chi Tseng, Jye-Shane Yang, Jyu-Lun Yan
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Patent number: 7737176Abstract: The invention relates to compounds of the formula I: and to the pharmaceutically acceptable salts thereof, to processes for the preparation of them and to pharmaceutical compositions comprising them, which are useful especially for the treatment and prevention of dyslipidaemia, atherosclerosis and diabetes.Type: GrantFiled: August 11, 2003Date of Patent: June 15, 2010Assignee: Merck Patent GmbHInventors: Michel Brunet, Jean-Jacques Zeiller, Gérard Ferrand, Yves Bonhomme
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Publication number: 20100105725Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: October 26, 2007Publication date: April 29, 2010Inventors: Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
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Publication number: 20090281189Abstract: There is provided a stable monohydrate form of treprostinil and pharmaceutical formulation comprising the same, method of making and using the same.Type: ApplicationFiled: May 7, 2009Publication date: November 12, 2009Inventor: David A. Walsh
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Publication number: 20090275598Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, L2, M, X, L3, and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: ApplicationFiled: July 10, 2009Publication date: November 5, 2009Applicant: Amgen Inc.Inventors: Michelle Akerman, Sean Brown, Jonathan B. Houze, Jinqian Liu, Jiwen Liu, Zhihua Ma, Julio C. Medina, Wei Qiu, Michael J. Schmitt, Rajiv Sharma, Yingcai Wang, Liusheng Zhu
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Publication number: 20090170908Abstract: The Spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereofType: ApplicationFiled: October 24, 2008Publication date: July 2, 2009Applicant: Japan Tobacco Inc.Inventors: Takashi Shimada, Hiroshi Ueno, Kazuhiro Tsutsumi, Kouichi Aoyagi, Tomoyuki Manabe, Shin-Ya Sasaki, Susumu Katoh
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Publication number: 20090163738Abstract: This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.Type: ApplicationFiled: December 15, 2008Publication date: June 25, 2009Inventors: Hitesh BATRA, Sudersan M. TULADHAR, Raju PENMASTA, David A. WALSH
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Patent number: 7495127Abstract: A potassium channel opener including a compound (e.g., pimaric acid) represented by the formula [I]: wherein R1, R2, R3, R4, R5, R6 and R7 are each independently hydrogen, alkyl, alkenyl, halogen, hydroxy, halogenated alkyl, hydroxyalkyl, aminoalkyl, alkoxy, aryl, heteroaryl, acyl, carboxyl, alkoxycarbonyl, hydroxamate, sulfo, carbamoyl, sulfonamide, aldehyde, or nitrile; or R4 and R5 may be bonded to each other to form a ring; or R6 and R7 may be bonded to each other to form a ring; and all of three bonds represented by are single bonds, or one of the three bonds is double bond and the other bonds are single bonds, or a physiologically acceptable salt thereof as an effective ingredient.Type: GrantFiled: February 14, 2006Date of Patent: February 24, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yuji Imaizumi, Tomohiko Ohwada
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Publication number: 20090042980Abstract: Neurite outgrowth-promoting prostaglandins (NEPPs) and other electrophilic compounds bind to Keap1, a negative regulator of the transcription factor Nrf2, and prevent Keap1-mediated inactivation of Nrf2 and, thus, enhance Nrf2 translocation into the nucleus of neuronal cells. Therefore, neuroprotective compositions and related methods are provided that employ such neuroprotective compounds, and prodrugs of such compounds, to cause dissociation of Nrf2 from a Keap1/Nrf2 complex.Type: ApplicationFiled: October 10, 2007Publication date: February 12, 2009Applicant: Burnham Institute for Medical ResearchInventors: Stuart A. Lipton, Takumi Satoh
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Patent number: 7482484Abstract: Disclosed are Compounds of formula I And methods of use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes.Type: GrantFiled: December 16, 2003Date of Patent: January 27, 2009Assignee: Merck Patent GmbHInventors: Nathalie Adje, Michel Brunet, Didier Roche, Jean-Jacques Zeiller, Stéphane Yvon, Valérie Guyard-Dangremont, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
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Publication number: 20090023811Abstract: Biphenyl compounds having the formula (I): are useful for preventing/treating pathologies linked to a deficiency of the activation of the RAR gamma receptor, e.g., for treating a pathology linked to a cell differentiation and/or proliferation disorder, for treating acne, for treating psoriasis.Type: ApplicationFiled: June 16, 2008Publication date: January 22, 2009Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Thibaud Biadatti, Etienne Thoreau
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Publication number: 20090012093Abstract: The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.Type: ApplicationFiled: November 6, 2003Publication date: January 8, 2009Inventors: Kohji Fukatsu, Shinobu Sasaki, Shuji Hinuma, Yasuaki Ito, Nobuhiro Suzuki, Masataka Harada, Tsuneo Yasuma
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Patent number: 7470807Abstract: A compound represented by the formula (I): [In the formula, Link represents a saturated or unsaturated straight hydrocarbon chain having 1 to 3 carbon atoms, C2 to C6 in the aromatic ring (E) independently represent a ring-constituting carbon atom, one of the ring-constituting carbon atoms may be replaced with V, V represents nitrogen atom, or carbon atom substituted with Zx, Zx represents a saturated alkyl group having 1 to 4 carbon atoms and the like, Rs represents -D-Rx etc., D represents a single bond, oxygen atom and the like, Rx represents a saturated alkyl group having 3 to 8 carbon atoms and the like, AR represents a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or a heterocyclic ring, and Y represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms and the like] or a salt thereof. A compound having prostaglandin production-suppressing action and leukotriene production-suppressing action is provided.Type: GrantFiled: August 13, 2004Date of Patent: December 30, 2008Assignee: Asahi Kasei Pharma CorporationInventors: Motoshi Shoda, Hiroshi Kuriyama
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Publication number: 20080312286Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: July 26, 2005Publication date: December 18, 2008Inventors: Anthony B. Pinkerton, Jean-Michel Vernier, Rowena Cube, John Hutchinson, Celine Bonnefous, Theodore Kamenecka
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Publication number: 20080293728Abstract: A complex comprises at least an ?2-adrenergic receptor agonist and a compound that provides an opposite charge to a charge on the ?2-adrenergic receptor agonist, wherein the complex is charge neutral as a whole and has a solubility in a range from about 0.3 ?g/ml to about 2.5 mg/ml in water at pH of about 7 and temperature of about 25° C. The complex is included in a composition, device, or implant for use in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.Type: ApplicationFiled: May 15, 2008Publication date: November 27, 2008Inventors: Gregory L. McIntire, Stephen R. Davio, Arthur E. Harms, Hongna Wang
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Patent number: 7446222Abstract: Compounds of formula (I) or derivatives thereof: wherein A, B, Z, R1, R2a, R2b, Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: GrantFiled: October 30, 2003Date of Patent: November 4, 2008Assignee: Glaxo Group LimitedInventors: Rino Antonio Bit, Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Neil Derek Miller, Tiziana Scoccitti
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Patent number: 7442808Abstract: Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.Type: GrantFiled: May 11, 2007Date of Patent: October 28, 2008Assignee: Merck & Co., Inc.Inventors: Min Ge, Jiafang He, Fiona Wai Yu Lau, Gui-Bai Liang, Songnian Lin, Weiguo Liu, Shawn P. Walsh, Lihu Yang
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Patent number: 7425644Abstract: The present invention provides pure pravastatin compositions and pure compactin compositions, and methods for the preparation thereof.Type: GrantFiled: November 23, 2004Date of Patent: September 16, 2008Assignee: TEVA Gyógyszergyár Zártkörűen Működő RészvénytársaságInventors: Vilmos Keri, Istvan Melczer
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Publication number: 20080194868Abstract: A device and process for crystallizing a compound using hydrodynamic cavitation comprising the steps of mixing at least one stream of a solution of such compound to be crystallized with at least one stream of an anti-solvent and passing the mixed streams at an elevated pressure through a local constriction of flow to create hydrodynamic cavitation thereby causing nucleation and the direct production of crystals. The compound to be crystallized can be, for example, an active pharmaceutical ingredient.Type: ApplicationFiled: July 24, 2007Publication date: August 14, 2008Inventor: Oleg V. Kozyuk
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Publication number: 20080176956Abstract: Modified green tea polyphenols and methods of their use are provided. One aspect provides compounds and compositions containing green tea polyphenols with one on more ester-linked fatty acids.Type: ApplicationFiled: August 10, 2006Publication date: July 24, 2008Inventor: Stephen D. Hsu
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Patent number: 7385083Abstract: A potassium channel opener comprising a compound (e.g., pimaric acid) represented by the formula [I]: wherein R1, R2, R3, R4, R5, R6 and R7 are each independently hydrogen, alkyl, alkenyl, halogen, hydroxy, halogenated alkyl, hydroxyalkyl, aminoalkyl, alkoxy, aryl, heteroaryl, acyl, carboxyl, alkoxycarbonyl, hydroxamate, sulfo, carbamoyl, sulfonamide, aldehyde, or nitrile; or R4 and R5 may be bonded to each other to form a ring; or R6 and R7 may be bonded to each other to form a ring; and all of three bonds represented by are single bonds, or one of the three bonds is double bond and the other bonds are single bonds, or a physiologically acceptable salt thereof as an effective ingredient.Type: GrantFiled: September 17, 2003Date of Patent: June 10, 2008Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Yuji Imaizumi, Tomohiko Ohwada
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Patent number: 7321050Abstract: The present invention provides novel diphenyl ethene compounds and pharmaceutically-acceptable salts thereof. Also provided are methods for making the compounds of the invention as well as methods for the use thereof in the treatment of immune, inflammatory, and auto-immune diseases.Type: GrantFiled: July 15, 2004Date of Patent: January 22, 2008Assignee: Welichem Biotech Inc.Inventors: Genhui Chen, John M. Webster, Jianxiong Li, Kaji Hu, Wei Liu, Jiang Zhu
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Patent number: 7304091Abstract: The present invention relates to compounds with structures resembling natural statins isolated from Penicillium sp.Type: GrantFiled: December 3, 2002Date of Patent: December 4, 2007Assignee: Myco TeO A/SInventors: Jens Christian Frisvad, Lene Lange, Kirk Schnorr, Steen Stender, Thomas Ostenfeld Larsen
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Publication number: 20070276042Abstract: The present disclosure is directed to modulators of cyclooxygenase (COX) enzymes and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of the severity and duration of non-specific pain, tension-type pain, headache, migraine, lower back pain, sciatica, dental pain, muscular pain, pain associated with acute soft tissue injuries, bursitis, tendonitis, lumbago, periarthritis, tennis elbow, sprains, strains, muscular problems associated with sports injuries, muscular problems associated with accidents, period pain, primary dysmenorrhoea, acute sore throat pain, osteoarthritis, rheumatoid arthritis, cancer, any disorder requiring analgesic response, any disorder requiring anti-inflammatory response, any disorder requiring antipyretic response, any conditions mediated by cyclooxygenase, cystic fibrosis, dementia, Alzheimer's disease, and/or conditions mediated by levels of ?-amyloid are described.Type: ApplicationFiled: May 22, 2007Publication date: November 29, 2007Applicant: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar, Soon Hyung Woo
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Publication number: 20070265332Abstract: Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.Type: ApplicationFiled: May 11, 2007Publication date: November 15, 2007Inventors: Min Ge, Jiafang He, Fiona Wai Yu Lau, Gui-Bai Liang, Songnian Lin, Weiguo Liu, Shawn P. Walsh, Lihu Yang
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Patent number: 7179817Abstract: Compounds represented by formula (I), prodrugs thereof and salts thereof, and pharmaceutical compositions comprising the same as an active ingredient (wherein each symbol has the meaning as defined in the specification.).Type: GrantFiled: May 9, 2002Date of Patent: February 20, 2007Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masahiko Terakado, Hiroshi Kohno, Shinya Takahashi
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Patent number: 7160732Abstract: The present invention is directed, in part, to fluorescein-based ligands for detection of metal ions, and methods of making and using the same.Type: GrantFiled: July 9, 2001Date of Patent: January 9, 2007Assignee: Massachusetts Institute of TechnologyInventors: Stephen J. Lippard, Shawn Burdette, Scott Hilderbrand, Roger Y. Tsien, Grant K. Walkup
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Patent number: 7148245Abstract: Compounds of formula (I): in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2 and R3 represent, in particular, H or alkyl, or R2 and R3, taken together, form a 5- or 6-membered ring, R4 and R5 represent, in particular, H or halogen, R6 represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.Type: GrantFiled: July 7, 2003Date of Patent: December 12, 2006Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Philippe Nedoncelle
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Patent number: 7019152Abstract: The present invention relates to the field of organic synthesis and more particularly to a new process for the optical resolution of a precursor of sclareolide. This process includes the reaction of [(1RS,2RS,4aSR,8aSR)-2-hydroxy-2,5,5,8a-tetramethyldecahydronaphthalen-1-yl]acetic acid, or an alkaline salt thereof, with an enantiomer of the 2-(methylamino)-1-phenyl-1-propanol, or an ammonium salt thereof respectively, which is used as resolving agent.Type: GrantFiled: April 9, 2004Date of Patent: March 28, 2006Assignee: Firmenich SAInventor: Alexandre Huboux
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Patent number: 7019034Abstract: Diabetic mammals are treated with compounds that are significantly more efficacious as agonists of RXR? retinoid receptors than as agonists of RXR? or RXR? retinoid receptors. The treatment reduces serum glucose and triglyceride levels of the mammals without the undesirable side effects of reducing serum thyroxine levels and a transient increase in serum triglyceride levels Compounds suitable for use in the methods of treatments of the present invention are selected by testing and identifying compounds of selective or specific efficacy as agonists of RXR? retinoid receptors in preference over RXR? and/or RXR? retinoid receptors. Novel compounds used in the methods of the invention have Formula 1 where the variables are defined as disclosed in the specification.Type: GrantFiled: December 17, 2003Date of Patent: March 28, 2006Assignee: Allergan, Inc.Inventors: Yang-Dar Yuan, Richard L. Beard, Roshantha A. Chandraratna
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Patent number: 6939988Abstract: Novel ?-aryl-?-oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them. The compounds have hypolipidemic, antihyperglycemic uses.Type: GrantFiled: November 23, 1999Date of Patent: September 6, 2005Assignee: Dr. Reddy's Laboratories LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 6936636Abstract: Compounds of the formula: where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.Type: GrantFiled: June 26, 2003Date of Patent: August 30, 2005Assignee: Allergan, Inc.Inventors: Santosh Sinha, Kwok Yin Tsang, Smita Bhat, Roshantha A. Chandraratna
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Patent number: 6924390Abstract: Compounds useful as surface coating agents, including compounds of the formula: wherein X1 comprises a first photoreactive species; X2 comprises a second photoreactive species; Y comprises a nonpolymeric core molecule comprising an aromatic group; and Z comprises at least one charged group. The Y core can include an aromatic group such as a benzene radical, the charged groups Z can be independently selected from the organic acids that include sulfonic acid, carboxylic acid, and phosphoric acid, and the photoreactive species of X1 and X2 can independently be aryl ketones, such as those selected from the group acetophenone, benzophenone, anthraquinone, anthrone, and anthrone-like heterocycles, and their substituted derivatives.Type: GrantFiled: July 14, 2003Date of Patent: August 2, 2005Assignee: SurModics, Inc.Inventor: Dale G. Swan
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Patent number: 6887896Abstract: Compounds of the formula where the variations have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of transiently increasing triglyceride levels and reducing serum thyroxine levels.Type: GrantFiled: October 29, 2003Date of Patent: May 3, 2005Assignee: Allergan, Inc.Inventors: Richard L. Beard, Tien T. Duong, Janet A. Takeuchi, Ling Li, Kwok Yin Tsang, Xiaoxia Liu, Jayasree Vasudevan, Liming Wang, Santosh C. Sinha, Haiqing Yuan, Roshantha A. Chandraratna
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Patent number: 6884820Abstract: Compounds of the formula where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effect of reducing serum thyroxine levels.Type: GrantFiled: April 3, 2003Date of Patent: April 26, 2005Assignee: Allergan, Inc.Inventors: Richard L. Beard, Haiqing Yuan, Roshantha A. Chandratratna
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Patent number: 6878842Abstract: The invention relates to a novel process for synthesizing organic compounds of general formula (I): said process may be carried out on an industrial scale and makes it possible to obtain from a mixture of racemic alcohols of formula (II), the corresponding chiral alcohols of R configuration, in a high chemical yield.Type: GrantFiled: April 25, 2003Date of Patent: April 12, 2005Assignee: Galderma Research & Development, S.N.C.Inventor: Alain Chenede
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Patent number: 6869967Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? suptype.Type: GrantFiled: July 18, 2002Date of Patent: March 22, 2005Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg