Five-membered Ring In Substituent Q Patents (Class 564/189)
-
Patent number: 12024489Abstract: A complex salt formed from a compound of formula (I) and an alkaloid, a preparation method therefor and use thereof are provided. In particular, a complex salt formed from rupestonic acid and matrine, oxymatrine, sophocarpine and sophoridine, or a composition thereof, has potential efficacy in treating a tumor/cancer or preparing related medicaments.Type: GrantFiled: June 1, 2022Date of Patent: July 2, 2024Assignee: XIAMEN INSTITUTE OF RARE EARTH MATERIALSInventors: Jianping Yong, Canzhong Lu
-
Patent number: 12012375Abstract: The invention relates to clinical chemistry, in particular, to new biologically active compounds—amide derivatives of prostaglandin F2?. These compounds have low cytotoxicity and are capable of stimulating formation of endogenous nitrogen oxide in mammal cells. Synthesis of such compounds promotes expansion of nomenclature of biologically active derivatives of prostaglandin F2? capable of reducing intraocular pressure.Type: GrantFiled: May 15, 2019Date of Patent: June 18, 2024Assignee: GURUS BIOPHARM LIMITED LIABILITY COMPANYInventors: Vladimir Vilenovich Bezuglov, Igor Viktorovich Serkov, Igor Ivanovich Lyubimov, Nataliya Mikhailovna Gretskaya
-
Patent number: 11344488Abstract: A cooling agent composition contains a 2,2,6-trimethylcyclohexanecarboxylic acid derivative represented by the following general formula (1). The symbol * represents an asymmetric carbon atom. X represents NH, N(ZAr2), O or S, Z represents a single bond or an alkylene group having 1 to 3 carbon atoms which may have a substituent, Ar2 represents an aryl group having 6 to 20 carbon atoms which may have a substituent or an aromatic heterocyclic group having 2 to 15 carbon atoms which may have a substituent. Y each independently represents a methylene group which may have a substituent, and n represents an integer of 0 to 3. Ar1 represents an aryl group having 6 to 20 carbon atoms which may have a substituent or an aromatic heterocyclic group having 2 to 15 carbon atoms which may have a substituent.Type: GrantFiled: October 16, 2018Date of Patent: May 31, 2022Assignee: TAKASAGO INTERNATIONAL CORPORATIONInventors: Takaji Matsumoto, Hisanori Itoh, Tomoharu Sato, Masashi Otsuka, Makoto Harada
-
Publication number: 20150111969Abstract: Provided is a compound of formula (I): a pharmaceutical composition comprising the compound of formula (I), a pharmaceutical composition comprising anandamide (AEA) and methods of using the same in the treatment of non-melanoma skin cancer (NMSC) and colorectal cancer.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Rukiyah T. Van Dross, Daniel A. Ladin, Colin S. Burns, Allison Stokes Danell
-
Patent number: 9006291Abstract: Compositions for application and methods of application of a composition to modify hair. In one embodiment, a composition includes a compound (molecule) represented by: wherein A and B are individually selected from a hydrogen, a hydroxyl group and a halogen, with the proviso that when one of A and B is a hydroxyl group, the other of A and B is a hydrogen and when one of A and B is a halogen, the other of A and B is a halogen or a hydrogen; wherein Z is, for example, an aryl moiety; and wherein X1 and X2 are, for example, individually selected from a hydrogen and an alkyl moiety, wherein R1 and R2 are individually selected from an oxo, a hydroxyl or an ester group; wherein y is 0 or 1, x is 0 or 1 and x and y are not both 1, or a salt.Type: GrantFiled: September 28, 2012Date of Patent: April 14, 2015Assignee: Pharma Patent Holding Inc.Inventor: Michael C. Brinkenhoff
-
Publication number: 20150031898Abstract: A convergent synthesis of the prostaglandin F2? analogues, travoprost and bimatoprost, was developed employing Julia-Lythgoe olefination of the structurally advanced phenylsulfone with an enantiomerically pure aldehyde ?-chain synthon. The novel convergent strategy allows the synthesis of a whole series of prostaglandin analogues of high purity from a common and structurally advanced prostaglandin intermediate.Type: ApplicationFiled: March 8, 2013Publication date: January 29, 2015Applicant: INSTYTUT FARMACEUTYCZNYInventors: Iwona Dams, Andrzej Kutner, Michal Chodynski, Malgorzata Krupa, Anita Pietraszek, Marta Zezula, Piotr Cmoch, Monika Kosinska
-
Patent number: 8853452Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.Type: GrantFiled: February 9, 2010Date of Patent: October 7, 2014Assignee: The Administrators of the Tulane Educational FundInventors: Barbara S. Beckman, Maryam Foroozesh, Jiawang Liu
-
Publication number: 20140288184Abstract: The present invention provides a glyoxime derivative displaying excellent pesticidal effect or a salt thereof and a pesticide containing the same as an active ingredient. This pesticide is characterized by containing as an active ingredient, a glyoxime derivative expressed by the general formula [I] (in which X represents a cyano group or a carbamoyl group, R1 represents a C1˜C8 alkyl group, a C3˜C6 cycloalkyl C1˜C6 alkyl group, etc, and IV represents a hydrogen atom, a C1˜C8 alkyl group, a C3˜C6 cycloalkyl C1˜C6 alkyl group, etc.) or an agriculturally acceptable salt thereof.Type: ApplicationFiled: November 19, 2012Publication date: September 25, 2014Applicants: IHARA CHEMICAL INDUSTRY CO., LTD., KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Shunichirou Fukumoto, Daisuke Shikama, Toshihiro Nagata, Katsuya Kato, Kei Kawamoto, Masaaki Komatsu, Takeshi Matsuda, Seisuke Ito
-
Patent number: 8809395Abstract: The present invention is directed to compounds, intermediates and methods for making valerenic acid and its derivatives as well as the use of such compounds as GABAA receptor ligands.Type: GrantFiled: January 22, 2010Date of Patent: August 19, 2014Assignee: Valericon GmbHInventors: Johann Mulzer, Jürgen Ramharter, Steffen Hering, Sophia Khom
-
Patent number: 8779003Abstract: Disclosed herein is a method for prolonging analgesic effect of a membrane permeable local anesthetic in a subject in need thereof. The method uses cinnamaldehyde as an adjuvant which, when administered prior to or simultaneously with the administration of a local anesthetic, prolongs the analgesic effect of the local anesthetic. Also disclosed herein is a method for providing analgesic effect in a subject in need thereof. The method uses cinnamaldehyde as an analgesic compound which, when administered alone to the subject in an analgesically effective amount, provides the analgesic effect.Type: GrantFiled: December 29, 2011Date of Patent: July 15, 2014Assignee: Mackay Memorial HospitalInventor: Yu-Chun Hung
-
Patent number: 8716527Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.Type: GrantFiled: March 4, 2009Date of Patent: May 6, 2014Assignee: Edison Pharmaceuticals, Inc.Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
-
Publication number: 20140107124Abstract: Disclosed herein are compositions comprising an amide related to a prostaglandin and a biogenic amine. Other aspects relate to certain chemical compounds, pharmaceutical compositions, and methods of treating glaucoma.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: Allergan, Inc.Inventors: David F. Woodward, Robert M. Burk
-
Publication number: 20140080802Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.Type: ApplicationFiled: October 28, 2013Publication date: March 20, 2014Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
-
Patent number: 8492588Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.Type: GrantFiled: May 29, 2012Date of Patent: July 23, 2013Assignee: Valeant Pharmaceuticals InternationalInventors: Jim Zhen Wu, Jean-Michel Vernier, Huanming Chen, Jianlan Song
-
Patent number: 8466318Abstract: The present invention encompasses a process for preparing compounds of formula (1), wherein a compound of formula (2) is reacted in the presence of a catalyst and a solvent under hydrogen pressure to form a compound of formula (1) and wherein A and R1—R4 are defined herein.Type: GrantFiled: May 15, 2007Date of Patent: June 18, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Guenter Linz, Gerd Kraemer, Zeno A. Leuter, Markus Ostermeier, Werner Rall, Claudia Ochs, Rolf Schmid
-
Patent number: 8426643Abstract: The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect.Type: GrantFiled: August 14, 2009Date of Patent: April 23, 2013Assignee: The Procter & Gamble CompanyInventors: Kenneth Edward Yelm, Gregory Mark Bunke, John Christian Haught
-
Publication number: 20130046024Abstract: Compositions for application and methods of application of a composition to modify hair. In one embodiment, a composition includes a compound (molecule) represented by: wherein A and B are individually selected from a hydrogen, a hydroxyl group and a halogen, with the proviso that when one of A and B is a hydroxyl group, the other of A and B is a hydrogen and when one of A and B is a halogen, the other of A and B is a halogen or a hydrogen; wherein Z is, for example, an aryl moiety; and wherein X1 and X2 are, for example, individually selected from a hydrogen and an alkyl moiety, wherein R1 and R2 are individually selected from an oxo, a hydroxyl or an ester group; wherein y is 0 or 1, x is 0 or 1 and x and y are not both 1, or a salt.Type: ApplicationFiled: September 28, 2012Publication date: February 21, 2013Applicant: PHARMA PATENT HOLDING INC.Inventor: Pharma Patent Holding Inc.
-
Patent number: 8314270Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: GrantFiled: September 9, 2010Date of Patent: November 20, 2012Assignee: Abbott LaboratoriesInventors: James T. Link, Qi Shuai, Martin Winn, Hong Yong
-
Patent number: 8293929Abstract: The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.Type: GrantFiled: October 12, 2010Date of Patent: October 23, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Gerald J. Tanoury, Minzhang Chen, Andrew D. Jones, Philip L. Nyce, Martin Trudeau, David J. Guerin, John R. Snoonian
-
Patent number: 8278483Abstract: The present invention provides processes for the synthesis of novel Shikimic acid head-group containing non-toxic cationic amphiphiles capable of facilitating transport of biological macromolecules into cells.Type: GrantFiled: February 7, 2007Date of Patent: October 2, 2012Assignee: Council of Scientific & Industrial ResearchInventors: Yenugonda Venkata Mahidhar, Arabinda Chaudhuri, Rama Mukherjee
-
Patent number: 8188314Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.Type: GrantFiled: June 24, 2009Date of Patent: May 29, 2012Assignee: Valeant Pharmaceuticals InternationalInventors: Jim Zhen Wu, Jean-Michel Vernier, Huanming Chen, Jianlan Song
-
Patent number: 8163956Abstract: A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.Type: GrantFiled: June 13, 2006Date of Patent: April 24, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Wesley Peter Blackaby, Ian Thomas Huscroft, Linda Elizabeth Keown, Richard Thomas Lewis, Piotr Antoni Raubo, Leslie Joseph Street, Christopher George Thomson, Joanne Thomson
-
Patent number: 8115031Abstract: Disclosed are compounds comprising analogs of quinic acids or shikimic acids having anti-inflammatory properties. The compounds are suitable for oral administration, stable, and demonstrate significant efficacy in inhibiting NF-kB, inhibiting leukocyte adhesion, and inhibiting other factors and cytokines known to be involved in inflammatory disease.Type: GrantFiled: November 10, 2008Date of Patent: February 14, 2012Inventors: Charles R. Yates, Duane D. Miller, Kui Zeng, Karin Emmons Thompson
-
Publication number: 20110230532Abstract: A compound having the structure wherein Y is selected from the group consisting of —C(O)OR2, —C(O)NHR8, —C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: ApplicationFiled: July 27, 2009Publication date: September 22, 2011Inventors: Amjad Ali, Robert K. Baker, Kathleen M. Rupprecht, Michael Man-Chu Lo, Brent Whitehead
-
Patent number: 7989439Abstract: The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.Type: GrantFiled: May 8, 2009Date of Patent: August 2, 2011Assignee: Sanofi-AventisInventors: Kirsten Bjergarde, Mark Dodson, Jacques Mauger, Anil Nair, Marcel Patek, Michel Tabart
-
Patent number: 7947852Abstract: Compounds of formula (I): wherein: R1 represents alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, X represents a group N—OR2 wherein R2 represents a hydrogen atom or an alkyl group. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.Type: GrantFiled: July 1, 2008Date of Patent: May 24, 2011Assignee: Les Laboratoires ServierInventors: Said Yous, Mohamed Ettaoussi, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Philippe Delagrange, Daniel-Henri Caignard, Mark Millan
-
Publication number: 20110052513Abstract: The present patent application relates to novel surface-active cationic compounds, to their use, in particular as hair conditioning agent, to a cosmetic treatment method, in particular for the hair, employing the said compounds, and to the cosmetic or pharmaceutical compositions, in particular hair compositions, comprising the said surfactants.Type: ApplicationFiled: February 3, 2009Publication date: March 3, 2011Applicant: L' OrealInventors: Laure Ramos-Stanbury, Herve Andrean, Christian Blaise
-
Publication number: 20100168216Abstract: The present invention relates to new prostaglandin derivatives having improved pharmacological activity and enhanced tolerability. They can be employed for the treatment of glaucoma and ocular hypertension.Type: ApplicationFiled: March 6, 2008Publication date: July 1, 2010Applicant: CTG PHARMA S.R.L.Inventors: Piero Del Soldato, Giancarlo Santus, Anna Sparatore
-
Publication number: 20100168243Abstract: The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.Type: ApplicationFiled: June 20, 2008Publication date: July 1, 2010Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Alexey V. Ishehenko, Lanqi Jia, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing Yuan, Wei Zhao, Linghang Zhuang, Jing Zhang
-
Patent number: 7728171Abstract: A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.Type: GrantFiled: August 25, 2008Date of Patent: June 1, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Ursula Hoffmann, Goesta Rimmler
-
Publication number: 20100087523Abstract: Rupestonic acid derivatives are rupestonic acid derivative A- or B-type compounds, prepared through a condensation reaction from starting materials, i.e., a monomer compound of rupestonic acid and an aromatic amine or fatty amine or an organic alcohol, i.e., a fatty alcohol or an aromatic alcohol. Rupestonic acid, which is the monomer compound of sesquiterpene isolated from the plant Xinjiang Artemisia rupestric L., is used as a mother compound. Natural anti-virus lead compound with high activity are discovered by modifying the structure of the monomer compound of rupestonic acid. Activity results of the lead compound showed pharmaceutical application of anti-I, II flu virus and anti-I, II herpes simplex virus infection. These compounds can be used alone or in combination with one or more pharmaceutical acceptable, inert and nontoxic excipients or carries in a pharmaceutical composition.Type: ApplicationFiled: September 15, 2009Publication date: April 8, 2010Applicant: Xinjiang Technical Institute of Physics & Chemistry, Chinese Academy of SciencesInventors: Haji Akber Aisa, Jianping Yong, Jiangyu Zhao
-
Publication number: 20090326059Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.Type: ApplicationFiled: June 24, 2009Publication date: December 31, 2009Applicant: VALEANT PHARMACEUTICALS INTERNATIONALInventors: Jim Zhen Wu, Jean-Michel Vernier, Huanming Chen, Jianlan Song
-
Patent number: 7632972Abstract: Compounds and related methods for synthesis, and the use of compounds and combination therapies for the treatment of cancer and modulation of apoptosis in cells are disclosed. The generation of synthetic combinatorial libraries and the evaluation of library member compounds regarding induction of apoptosis selectively in cancer cells are disclosed. Compounds, methods of making the compounds, and therapeutic methods with application against breast cancer cells, melanoma cancer cells, colon cancer cells, and other cancer cells are described.Type: GrantFiled: October 27, 2004Date of Patent: December 15, 2009Assignee: The Board of Trustees of the University of IllionisInventors: Paul J. Hergenrother, Vitaliy Nesterenko, Karson Putt, Brittany Joy Allen, Robin Shane Dothager, Benjamin James Leslie
-
Publication number: 20090306404Abstract: The present invention is aimed at a process for the preparation of compounds of the general formula (I). The objective process is in this case based on the Michael reaction of compounds of the general formula (III) with compounds of the general formula (IV), with subsequent hydrogenation and cyclization of the intermediates of the formula (II) obtained.Type: ApplicationFiled: March 2, 2006Publication date: December 10, 2009Applicant: Degussa GmbHInventors: Günter Knaup, Milan Latinovic
-
Patent number: 7601870Abstract: The present invention relates to aniline derivatives of the general formula I or salts thereof, described therein, and their use.Type: GrantFiled: December 20, 2005Date of Patent: October 13, 2009Assignee: H. Lundbeck A/SInventors: Christian Wenzel Tornøe, Mario Rottländer, Daniel Rodriguez Greve, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
-
Patent number: 7592365Abstract: The disclosure concerns substituted pyrroles of formula (I): wherein A, L, Ar, R1, R2, R5, and Ra are as defined in the disclosure, compositions containing the same, methods for making the same and uses thereof, in particular as anti-cancer agents.Type: GrantFiled: August 1, 2007Date of Patent: September 22, 2009Assignee: Aventis Pharma S.A.Inventors: Baptiste Ronan, Michel Tabart, Catherine Souaille, Fabrice Viviani, Eric Bacque, Jean-Philippe Letallec, Pascal Desmazeau
-
Patent number: 7560591Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta pType: GrantFiled: April 30, 2008Date of Patent: July 14, 2009Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
-
Publication number: 20090088478Abstract: The present invention relates to compounds as inhibitors of enzymes having histone deacetylase activity, to the processes for the preparation of those compounds, and to their use for the treatment of diseases which are associated with hypoacetylation of histones and/or other molecules, or in which induction of hyperacetylation has a beneficial effect for example by inhibition of proliferation and/or induction of differentiation and/or induction of apoptosis in transformed cells, such as cancer. Furthermore, the compounds are useful for the treatment of other proliferative diseases, for therapy or prophylaxis of conditions associated with abnormal gene expression.Type: ApplicationFiled: July 16, 2007Publication date: April 2, 2009Inventors: Alexander B. Maurer, Sascha Hoevelmann, Elke Martin, Bernd Hentsch, Michael Gassen, Juergen Kraus, Rolf Krauss, Adam-Spencer Vincek
-
Patent number: 7511175Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: GrantFiled: January 5, 2006Date of Patent: March 31, 2009Assignee: Abbott LaboratoriesInventors: Jyoti R. Patel, Qi Shuai, James T. Link, Jeffrey J. Rohde, Jurgen Dinges, Bryan K. Sorensen, Martin Winn, Hong Yong, Peer B. Jacobson, Michael E. Brune
-
Patent number: 7511168Abstract: The present invention provides novel processes for the preparation of a cyclopentanone of Formula II and a lactone of Formula I, which are useful in the production of prostaglandins: wherein Z, R2, R3, X1, X2, and are as defined in the specification. The invention also provides novel enantiomerically enriched compounds.Type: GrantFiled: January 18, 2006Date of Patent: March 31, 2009Inventors: Shih-Yi Wei, Yu-Chih Yeh
-
Patent number: 7491844Abstract: Described herein are compounds having a formula and therapeutic methods, compositions, and medicaments, related thereto.Type: GrantFiled: April 20, 2007Date of Patent: February 17, 2009Assignee: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
-
Patent number: 7476755Abstract: Therapeutic substituted cyclopentane compounds, and compositions, medicaments, and therapeutic methods related thereto are disclosed herein.Type: GrantFiled: April 27, 2007Date of Patent: January 13, 2009Assignee: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
-
Patent number: 7435851Abstract: The present invention provides substituted puleganic amides and compositions thereof, which are both useful as a topical treatment for skin, such as a repellant for insects and arthropods.Type: GrantFiled: September 29, 2006Date of Patent: October 14, 2008Assignee: E.I. du Pont de Nemours and CompanyInventor: Mark A. Scialdone
-
Patent number: 7435849Abstract: A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.Type: GrantFiled: October 17, 2006Date of Patent: October 14, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Ursula Hoffmann, Goesta Rimmler
-
Patent number: 7414152Abstract: Cooling compounds are provided having the formula: wherein, m is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, C1-C4 straight or branched alkyl, and a C1-C4 straight or branched alkoxy, X is (CH2)n—R, where n is 0 or 1 and R is a group with non-bonding electrons, with the provisos that: (a) when Y and Z are H, X is not F, OH, MeO or NO2 in the 4-position and is not OH in the 2 or 6-position (b) when Y or Z is H then X, Y and Z are such that (i) the groups in the 3- and 4-positions are not both OMe, (ii) the groups in the 4- and 5-positions are not both OMe, (iii) the groups in 3- and 5-positions are not OMe if the group in the 4-position is OH, and (iv) the groups in the 3- and 5-positions are not OH if the group in the 4-position is methyl.Type: GrantFiled: May 19, 2006Date of Patent: August 19, 2008Assignee: Givaudan, SAInventors: Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack, Lori W. Tigani
-
Publication number: 20080167346Abstract: The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.Type: ApplicationFiled: November 15, 2007Publication date: July 10, 2008Applicant: SANOFI-AVENTISInventors: Michael WAGNER, Matthias URMANN, Volkmar WEHNER, Martin LORENZ, Armin BAUER, Marc NAZARE, Hans MATTER
-
Patent number: 7381827Abstract: The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.Type: GrantFiled: March 11, 2005Date of Patent: June 3, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Gerald J. Tanoury, Minzhang Chen, Andrew D. Jones, Philip L. Nyce, Martin Trudeau, David J. Guerin, John R. Snoonian
-
Publication number: 20080045534Abstract: This invention provides compounds of formula I where X?O or S; Y is O or S; q=1 or 0; and other substituents are defined herein. The invention also provides pharmaceutical compositions comprising compounds of formula I. Such compounds are potassium channel modulators.Type: ApplicationFiled: August 16, 2007Publication date: February 21, 2008Applicant: Valeant Pharmaceuticals North AmericaInventors: Jean-Michel Vernier, Samedy Ouk, Martha Alicia De La Rosa, David Abraham Paisner
-
Patent number: 7220814Abstract: The present invention relates to new hydrophilicized blocked polyisocyanates, a process for preparing them and their use.Type: GrantFiled: December 17, 2003Date of Patent: May 22, 2007Assignee: Bayer MaterialScience AGInventors: Thorsten Rische, Christoph Gürtler, Karin Naujoks, Thomas Feller
-
Patent number: RE44339Abstract: Cooling compounds are provided having the formula: wherein, m is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, C1-C4 straight or branched alkyl, and a C1-C4 straight or branched alkoxy, X is (CH2)n—R, where n is 0 or 1 and R is a group with non-bonding electrons, with the provisos that: (a) when Y and Z are H, X is not F, OH, MeO or NO2 in the 4-position and is not OH in the 2 or 6-position (b) when Y or Z is H then X, Y and Z are such that (i) the groups in the 3- and 4-positions are not both OMe, (ii) the groups in the 4- and 5-positions are not both OMe, (iii) the groups in 3- and 5-positions are not OMe if the group in the 4-position is OH, and (iv) the groups in the 3- and 5-positions are not OH if the group in the 4-position is methyl.Type: GrantFiled: August 31, 2011Date of Patent: July 2, 2013Assignee: Givaudan S.A.Inventors: Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack, Lori W. Tigani