Chalcogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/248)
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Patent number: 7851487Abstract: Disclosed are methods for alleviating symptoms of neuropsychiatric disorders using tetrahydropyridine derivatives bearing aromatic substituents. The method comprises administering to an individual a tetrahydropyridine derivative bearing aromatic substituents in an amount effective to alleviate symptoms of the neuropsychiatric disorder.Type: GrantFiled: March 12, 2007Date of Patent: December 14, 2010Assignees: The Research Foundation of State University of New York, Chakra Biotech Pte Ltd.Inventors: Huw M. L. Davies, Anil K. Ratty
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Patent number: 7851488Abstract: Provided are novel tetrahydropyridine derivatives bearing substituents. These compounds can be used for alleviating the symptoms of CNS disorders.Type: GrantFiled: March 12, 2007Date of Patent: December 14, 2010Assignee: The Research Foundation of State University of New YorkInventor: Huw M. L. Davies
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Publication number: 20100298347Abstract: Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome.Type: ApplicationFiled: December 1, 2008Publication date: November 25, 2010Applicant: MERCK FROSST CANADA LTDInventors: Michel Belley, Denis Deschenes, Rejean Fortin, Jean-Francois Fournier, Sebastien Gagne, Yves Gareau, Jacques Yves Gauthier, Lianhai Li, Joel Robichaud, Michel Therien, Geoffrey K. Tranmer, Zhaoyin Wang
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Publication number: 20100297077Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: ApplicationFiled: October 3, 2008Publication date: November 25, 2010Applicant: BIONOMICS LIMITEDInventors: Bernard Luke Flynn, Jonathan Bayldon Baell, Jason Hugh Chaplin, Girmit Singh Gill, Damian Wojciech Grobelny, Andrew John Harvey, Jorgen Alvar Mould, Dharam Paul
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Publication number: 20100267770Abstract: The present invention provides piperidine derivatives of formula (I): salts and optical isomers thereof and cosmetic compositions containing them.Type: ApplicationFiled: June 28, 2010Publication date: October 21, 2010Applicant: L'OREALInventors: Alexandre CAVEZZA, Michel Neuwels
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Patent number: 7812100Abstract: The invention relates to new alkoxyamines suitable for hydrosilylation reactions, to siloxane modified alkoxamines and to siloxane modified polymers as well as to their use. The alkoxamines are compounds of formula (I) or (II) wherein A is a group capable of forming a stable free nitroxyl radical A. which is bound via its oxygen atom to the carbon atom; R.sub.1 and R.sub.2 independently of one another are hydrogen, C.sub.1-C.sub.18-alkyl, C.sub.3-C.sub.8cycloalkyl or phenyl which are unsubstituted or substituted by NO.sub.2, halogen, amino, hydroxy, cyano, carboxy, C.sub.1-C.sub.4alkoxy, C.sub.1-C.sub.4alkylthio, C.sub.1-C.sub.4alkylamino or di(C.sub.1-C.sub.4alkyl)amino; R.sub.3, R.sub.4 and R.sub.5 independently of one another are hydrogen or C.sub.1-C.sub.18alkyl or phenyl; or R.sub.3 and R.sub.5 together with the linking group C.dbd.C form a 5 to 12 membered ring; R.sub.6 is X hydrogen or C.sub.1-C.sub.l8alkyl or phenyl; X is O, NH or NR.sub.7, wherein R.sub.7 is C.sub.1-C.sub.18alkyl, C.sub.3-C.sub.Type: GrantFiled: October 16, 2006Date of Patent: October 12, 2010Assignee: Ciba CorporationInventors: Lothar Alexander Engelbrecht, Peter Nesvadba
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Publication number: 20100249423Abstract: A GRDDS (Gastro Retentive Drug Delivery System) containing tolperisone and having a 2-methyl-1-(4-methylphenyl)-propenone (4-MMPPO) fraction of less than 1.5 ppm for the extended release of the active substance tolperisone while avoiding the formation of 4-MMPPO in the gastrointestinal tract.Type: ApplicationFiled: February 19, 2010Publication date: September 30, 2010Applicant: SANOCHEMIA PHARMAZEUTIKA AGInventors: Stefan Welzig, Jan Rothenburger, Beate Kälz, József Gungl, Klaus Gerdes
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Publication number: 20100234604Abstract: The present invention relates to novel substituted aryl sulfone intermediates and processes for preparing the same. An aspect of this invention relates to a process for making substituted aryl sulfone intermediates utilizing a one-pot deacylation-carbon/sulfur bond formation step. The invention also relates to a process for preparing intermediates that are used to make the compounds of formula I. Some of the advantages of the present invention include manufacturing flexibility and efficiency, high yield synthesis using a one pot deacylation and carbon-sulfur bond formation step of a thioester intermediate and the like. This and other aspects of the invention will be realized upon review of the specification as a whole.Type: ApplicationFiled: March 12, 2010Publication date: September 16, 2010Inventors: Xin Linghu, Kathleen Linn, Kevin M. Maloney, Mark McLaughlin, Gang Qian
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Dopamine Transporter Inhibitors for Use in Treatment of Movement Disorders and Other CNS Indications
Publication number: 20100217727Abstract: The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's disease, when assessed by one or more of Hoehn and Yahr Staging of Parkinson's Disease, Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.Type: ApplicationFiled: February 21, 2006Publication date: August 26, 2010Applicant: Prexa Pharmaceuticals, Inc. c/o Advent Healthcare VenturesInventor: James R. Hauske -
Patent number: 7767692Abstract: 4-substituted 1-amidomethylcarbonyl-piperidine compounds having motilin-agonistic properties and their acid addition salts, pharmaceutical compositions containing these compounds, processes and intermediate products for the preparation of these compounds, and methods of treatment utilizing these compounds.Type: GrantFiled: November 10, 2003Date of Patent: August 3, 2010Assignee: Solvay Pharmaceuticals GmbHInventors: Daniel Jasserand, Jochen Antel, Ulf Preuschoff, Reinhard Brueckner, Holger Sann, Michael Wurl, Peter Eickelmann
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Publication number: 20100145003Abstract: Catalytic processes for preparing caprolactam, pipecolinic acid, and their derivatives, from lysine or alpha-amino-epsilon-caprolactam starting materials, and products produced thereby. A process for preparing caprolactam or a derivative thereof, the process comprising contacting a reactant comprising lysine or alpha aminocaprolactam with a catalyst and a gas comprising hydrogen gas, in the presence of a solvent. The catalyst may be provided on a support material, such as a transition metal.Type: ApplicationFiled: February 20, 2008Publication date: June 10, 2010Applicant: BOARD of Trustees of Michigan State UniversityInventor: John W. Frost
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Patent number: 7728008Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.Type: GrantFiled: June 26, 2006Date of Patent: June 1, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
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Publication number: 20100120858Abstract: The invention relates to compounds of Formula (I) and pharmaceutically acceptable acid addition salts thereof, wherein *, X1, X2, R5A, R5B, R6, R7, and R8 are as defined in the specification; pharmaceutical compositions; therapeutic combinations; and methods of treating diseases and disorders.Type: ApplicationFiled: August 13, 2007Publication date: May 13, 2010Inventors: Bradley W. Caprathe, Rocco D. Gogliotti, Rex A. Jennings, Lloyd J. Simons
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Patent number: 7714089Abstract: Rubbery polymers can be formed having the general formula: R1R2N—(CH2)n—X—CH2—CHR3R4 wherein R1 and R2 are independently selected from a group consisting of alkyls, cycloalkyls, alkenyls, cycloalkenyls, aryls, phenyls, heterocycles, acyls, and silanes, or R1 in combination with R2 forms a heterocyclic ring; n is an integer from 1 to 20; X is selected from a group consisting of sulfur, a phosphorus moiety, and a silicon moiety; R3 and R4 are one of hydrogen, alkyls, alkenyls, and at least one of which includes reactive unsaturation such as an alkenyl group. Moreover, this invention discloses a process of making functionalized rubbery polymers from the functionalized monomers.Type: GrantFiled: December 13, 2007Date of Patent: May 11, 2010Assignee: The Goodyear Tire & Rubber CompanyInventors: Adel Farhan Halasa, Wen-Liang Hsu, Leh-Yeh Hsu, legal representative, Shingo Futamura, Joe Zhou, Chad Aaron Jasiunas
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Publication number: 20100105730Abstract: Liquid formulations of the DL-lactic acid, the glutaric acid, the L-aspartic acid and the glutamic acid salts of 4-[2-(4-methylphenylsulfanyl)phenyl]piperidine and their use in the manufacture of a medicament to be used in the treatment of CNS diseases are provided.Type: ApplicationFiled: March 14, 2008Publication date: April 29, 2010Applicant: H. Lundbeck A/SInventors: Gudrun Lasskogen, Tine Bryan Stensbol, Heidi Lopez de Diego
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Patent number: 7692019Abstract: One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.Type: GrantFiled: February 28, 2006Date of Patent: April 6, 2010Assignee: Sepracor Inc.Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Michele L. R. Heffernan, Michael Z. Hoemann, Donald W. Kessler, Liming Shao, Xinhe Wu, Roger L. Xie
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Publication number: 20100081571Abstract: Disclosed herein is a novel purified toxin isolated from Euglena sanguinea. More specifically the toxin, termed euglenophycin, is an alkaloid having herbicidal and cytotoxicity against plant and mammalian cells.Type: ApplicationFiled: September 25, 2009Publication date: April 1, 2010Inventors: Paul V. Zimba, Kevin R. Beauchesne, Peter D. Moeller, Richard E. Triemer
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Publication number: 20100036125Abstract: The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.Type: ApplicationFiled: October 16, 2009Publication date: February 11, 2010Inventors: Xiongwei Shi, Man Zhu, William Leong, Vilas Dahanukar, Ilia A. Zavialov, Cecilia Proietti, Shannon Zhao, Hong-Chang Lee, Yi Liu, Hoa N. Nguyen, Wenxue Wu, Bosco D'Sa, Feng Liang, Loc Thanh Tran
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Patent number: 7655653Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.Type: GrantFiled: October 25, 2007Date of Patent: February 2, 2010Assignee: N.V. OrganonInventor: Hubert Jan Jozef Loozens
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Publication number: 20100016600Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: ApplicationFiled: September 28, 2009Publication date: January 21, 2010Applicant: WAYNE STATE UNIVERSITYInventor: Aloke K. Dutta
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Publication number: 20100010229Abstract: The present invention provides a novel fexofenadine hydrochloride polymorph. The polymorph is particularly useful as a medicament for use as an antihistamine, antiallergy agent or bronchodilator.Type: ApplicationFiled: September 18, 2009Publication date: January 14, 2010Inventor: Frederico Junquera MILLA
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Publication number: 20100004450Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.Type: ApplicationFiled: June 29, 2009Publication date: January 7, 2010Inventors: Sergio Cesco-Cancian, Hongfeng Chen, Jeffrey S. Grimm, Neelakandha S. Mani, Christopher M. Mapes, David C. Palmer, Daniel J. Pippel, Kirk L. Sorgi, Tong Xiao
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Patent number: 7619050Abstract: The instant invention relates to novel alkoxyamine initiators/regulators containing an ethylenically unsaturated, radically polymerizable group. The compounds are useful for the preparation of complex polymeric architectures. Further aspects of the invention are a polymerizable composition and a polymerization process comprising the alkoxyamine initiators/regulators, a macroinitiator obtainable by said polymerization process and a process for polymerizing with the macroinitiator.Type: GrantFiled: May 17, 2005Date of Patent: November 17, 2009Assignee: Ciba Specialty Chemicals CorporationInventors: Peter Nesvadba, Andreas Kramer, Lucienne Bugnon
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Publication number: 20090269673Abstract: The invention relates to a method for producing perfluoroalkanesulfonic acid esters and for further transforming the same into the salts thereof. The invention also relates to the use of the produced compounds in electrolytes, batteries, capacitors, supercapacitors, and galvanic cells.Type: ApplicationFiled: July 8, 2009Publication date: October 29, 2009Inventors: Nikolai Ignatyev, Michael Schmidt, Udo Heider, Peter Sartori, Andry Kucheryna
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Publication number: 20090208413Abstract: The present invention provides compositions and methods for synthesizing labeled drugs. The present invention further provides methods for preventing or stopping prescription drug abuse for all agents registered as a Drug Enforcement Agency (DEA) schedule II through schedule V medications. According to the present invention, methods are provided for monitoring patient compliance with prescribed drug treatment. The present invention also provides methods for facilitating a replacement prescription when a patient is left without access to their prescribed drug. Furthermore, the present invention provides a method to improve employee compliance with an employer's drug policies via either a voluntary or compulsory system for enhanced drug testing.Type: ApplicationFiled: February 23, 2006Publication date: August 20, 2009Inventors: Alan J Reis, Christian Schafmeister
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Patent number: 7572811Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.Type: GrantFiled: February 24, 2005Date of Patent: August 11, 2009Assignee: IRM LLCInventors: Shifeng Pan, Thomas Marsilje, Wenshuo Lu, Wenqi Gao, Nathanael Schiander Gray, Yun He, Yahua Liu, Yuan Mi, Yongping Xie
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Publication number: 20090198033Abstract: The invention relates to new alkoxyamines suitable for hydrosilylation reactions, to siloxane modified alkoxamines and to siloxane modified polymers and to their use as slip and leveling agent or as dispersant. The alkoxamines are compounds of formula (I) or (II) wherein A is a group capable of forming a stable free nitroxyl radical A.Type: ApplicationFiled: October 16, 2006Publication date: August 6, 2009Inventors: Lothar Alexander Engelbrecht, Peter Nesvadba
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Patent number: 7569586Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4,R5, R6, R7, R8a, R8b, W, a, b, c and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: August 15, 2005Date of Patent: August 4, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Trevor Mischki, Adam Hughes, Yu-Hua Ji
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Publication number: 20090163462Abstract: The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: ApplicationFiled: June 11, 2008Publication date: June 25, 2009Applicant: deCODE genetics, ehfInventors: Vincent SANDANAYAKA, Jasbir Singh, Mark Gurney, Bjorn Mamat, Peng Yu, Louis Bedell, Lei Zhao, Rama K. Mishra
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Publication number: 20090137561Abstract: 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 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: October 3, 2008Publication date: May 28, 2009Applicant: Amgen Inc.Inventors: Sean P. Brown, Qiong Cao, Paul John Dransfield, Xiaohui Du, Jonathan Houze, Xian Yun Jiao, Yong-Jae Kim, Todd J. Kohn, SuJen Lai, An-Rong Li, Daniel Lin, Jian Luo, Julio C. Medina, Jeffrey D. Reagan, Vatee Pattaropong, Margrit Schwarz, Wang Shen, Yongli Su, Gayathri Swaminath, Marc Vimolratana, Xiang Wang, Yumei Xiong, Li Yang, Ming Yu, Jie Zhang, Liusheng Zhu
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Patent number: 7521552Abstract: There is provided a process for the preparation of substituted amino alcohols HO—(CH2)n—NR1R2 from haloalcohols HO—(CH2)n—X, where X is Cl, Br or I, by reaction with an amine HNR1R2, in water as solvent at a temperature range of about 20° C. to about 90° C. optionally in the presence of a catalytic amount of an iodide source metal iodides. The haloalcohols are useful in the preparation of 6-[(substituted)phenyl]-triazolopyrimidine compounds which are useful in the treatment of cancer.Type: GrantFiled: December 8, 2004Date of Patent: April 21, 2009Assignee: WyethInventors: Yanzhong Wu, Arkadiy Rubezhov, Jean Schmid, Jay Thomas Afragola
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Publication number: 20090080074Abstract: A polymer film includes: a wavelength dispersion regulator represented by formula (I): wherein R1 and R2 each independently represents a hydrogen atom, an alkyl group or an aryl group, provided that both R1 and R2 are not hydrogen atoms at the same time; and R3 and R4 each independently represents an electron-withdrawing substituent, and R1 and R2, or R3 and R4 may be bonded together to form a ring, and wherein the polymer film has a retardation value that satisfies the following formulae (1) and (2): 70 nm?Rth(548)?300 nm??Formula (1) Rth(628)<Rth(548)<Rth(446)??Formula (2) wherein Rth(?) represents a retardation value expressed in nm in a film thickness direction measured at a wavelength of ? nm.Type: ApplicationFiled: September 4, 2008Publication date: March 26, 2009Applicant: FUJIFILM CorporationInventors: Nobutaka Fukagawa, Masaki Noro, Teruki Niori
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Publication number: 20090074709Abstract: A method of applying a biocidal polymer to a surface including applying a solution of the biocidal polymer to the surface, wherein the biocidal polymer includes biocidal groups and the biocidal polymer is insoluble in water. The biocidal groups can be selected from the group consisting of quaternary salt groups or haloamino groups.Type: ApplicationFiled: September 12, 2008Publication date: March 19, 2009Inventors: RICHARD R. KOEPSEL, ALAN J. RUSSELL, THANGAPPAN RAVIKUMAR
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Patent number: 7470812Abstract: The invention encompasses the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, via the intermediate, (3R)-5-methyl-3-(2-oxo-2{[(1R)-1-phenylethyl]amino}ethyl)hexanoic acid.Type: GrantFiled: August 21, 2007Date of Patent: December 30, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Vinod Kumar Kansal, Brijnath P. Chaurasia, Anand Prakash Tiwari
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Patent number: 7465826Abstract: The invention encompasses the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, via the intermediate, (3R)-5-methyl-3-(2-oxo-2{[(1R)-1-phenylethyl]amino}ethyl)hexanoic acid.Type: GrantFiled: August 21, 2007Date of Patent: December 16, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Vinod Kumar Kansal, Brijnath P. Chaurasia, Anand Prakash Tiwari
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Patent number: 7423012Abstract: The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.Type: GrantFiled: December 2, 2005Date of Patent: September 9, 2008Assignee: AstraZeneca ABInventors: Marcel Linschoten, Magnus Polla
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Publication number: 20080182876Abstract: The present patent application concerns new compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing ring, A is a saturated C1-4 alkylene and B a C3-4 alkylene or alkenylene chain; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.Type: ApplicationFiled: April 26, 2006Publication date: July 31, 2008Inventors: Isabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz
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Patent number: 7368568Abstract: The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroarnides for the synthesis of edothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.Type: GrantFiled: June 10, 2005Date of Patent: May 6, 2008Assignee: Bayer Schering Pharma AGInventors: Jurgen Westermann, Johannes Platzek, Orlin Petrov
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Patent number: 7354895Abstract: The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.Type: GrantFiled: May 3, 2000Date of Patent: April 8, 2008Assignee: AstraZeneca ABInventors: Marcel Linschoten, Magnus Polla
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Patent number: 7351721Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: May 6, 2003Date of Patent: April 1, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Patent number: 7341715Abstract: The preparation for permanently deforming hair has a pH of 6.5 to 9.5 and contains, as keratin-reducing agent, a 2-mercaptopropion-amide of the formula (I): in which R1 and R2, independently of one another, represent H, a linear or branched alkylaminoalkyl group with 2 to 8 carbon atoms, or a morpholinoalkyl group with 2 to 3 carbon atoms in the alkyl portion of the morpholinoalkyl group, with the proviso that R1 and R2 are not simultaneously H, or that R1 and R2, together with the nitrogen atom, form a five-or six-membered heterocyclic ring, which optionally contain an additional N or O and are optionally substituted with one or two OH and/or methyl groups.Type: GrantFiled: May 21, 2001Date of Patent: March 11, 2008Assignee: Wella AGInventors: Beate Dannecker, Ursus Schweizer, Guenther Lang, Regina Ortmann, Wolfgang Hanefeld
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Publication number: 20080009628Abstract: One-pot condensation-reduction methods for preparing substituted allylic alcohols as well as highly selective extractive methods to separate isomeric alcohols produced in the one-pot condensation-reduction processes are provided for preparing, for example, a quinolone.Type: ApplicationFiled: June 13, 2007Publication date: January 10, 2008Inventors: Michael Reuman, Roger Faessler, Armin Roessler, Kirk Sorgi, Xun Li, Jeffrey S. Grimm
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Patent number: 7304155Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.Type: GrantFiled: December 16, 2002Date of Patent: December 4, 2007Assignee: N.V. OrganonInventor: Hubert Jan Jozef Loozen
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Patent number: 7238710Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.Type: GrantFiled: June 7, 2005Date of Patent: July 3, 2007Assignee: Merck Frosst Canada, Ltd.Inventors: Xavier Billot, John Colucci, Yongxin Han, Marie-Claire Wilson, Robert N. Young
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Patent number: 7229803Abstract: The invention relates to methods for reacting (di)amines as substrates in the presence of a lysine oxidase arid a reducing agent, resulting in alcohols, diols or cyclic secondary amines. In a particular embodiment, the invention is directed to methods of preparing cyclic secondary amines suitable for ultimately synthesizing piperidine-2-carboxylic acid and proline derivatives, useful, for example as thrombin inhibitors.Type: GrantFiled: April 8, 2002Date of Patent: June 12, 2007Assignee: BASF AktiengesellschaftInventors: Thomas Friedrich, Norbert Zimmermann, Rainer Stürmer
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Patent number: 7115610Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.Type: GrantFiled: December 17, 2004Date of Patent: October 3, 2006Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeffrey Zablocki
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Patent number: 7078402Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.Type: GrantFiled: May 31, 2001Date of Patent: July 18, 2006Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore
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Patent number: 6933385Abstract: The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.Type: GrantFiled: August 5, 2002Date of Patent: August 23, 2005Assignee: Schering AGInventors: Jurgen Westermann, Johannes Platzek, Orlin Petrov
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Patent number: 6900350Abstract: The invention relates to a method for the production of ?-aminoalkylsulphonic acids of general formula (I), where R1 and R2=optionally substituted alkyl groups with 1 20 C atoms and n=a whole number from 2 6, whereby an amine of formula (II), where R1 and R2 have the above meanings is reacted with an alkyl dihalide of formula (III), where n has the above meaning and X1 and X2=chlorine or bromine, with addition of alkali hydroxide at a pH of 8 10. The pH is then adjusted to a value of 0 1, by addition of a hydrohalic acid and excess alkyl dihalide is separated off, before the reaction solution is adjusted to a pH of 6 7.5 with alkali liquor, alkali sulphite is added and the product (I) formed at elevated temperate.Type: GrantFiled: April 27, 2001Date of Patent: May 31, 2005Assignee: RASCHIG GmbHInventors: Volker Schaefer, Wolfgang Knoll, Alexander Schmitt, Christoph Huettner
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Patent number: 6900329Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: March 19, 2002Date of Patent: May 31, 2005Assignee: Schering CorporationInventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan