Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperidine Ring Patents (Class 546/245)
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Patent number: 7683168Abstract: Diarylmethylpiperazine compounds are described, which are useful as mu and/or delta receptor opioid compounds, without central side effects. Pharmaceutical compositions containing such compounds are variously useful for peripheral or non-centrally mediated indications, including peripherally mediated and neuropathic pain, urogenital tract disorders, overactive bladder, urinary incontinence, sexual disorders, premature ejaculation, cough, lung edema, cardiac disorders, cardioprotection, gastro-intestinal disorders, diarrhea, irritable bowl syndrome, functional distention, immuno-modulation and anti-tumor activity.Type: GrantFiled: April 14, 2006Date of Patent: March 23, 2010Assignee: Mount Cook Bio Sciences, Inc.Inventors: Shyi-Tai Jan, Kwen-Jen Chang, Kestutis P. Biciunas, Xin Ma
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Patent number: 7678785Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.Type: GrantFiled: July 24, 2007Date of Patent: March 16, 2010Assignee: UCB Pharma S.A.Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
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Publication number: 20100063081Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.Type: ApplicationFiled: June 29, 2006Publication date: March 11, 2010Inventor: Stuart Edward Bradly
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Publication number: 20100063095Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.Type: ApplicationFiled: February 27, 2009Publication date: March 11, 2010Inventors: James J. KOWALCZYK, Galina KUZNETSOV, Shawn SCHILLER, Boris M. SELETSKY, Mark SPYVEE, Hu YANG
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Patent number: 7662812Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: February 13, 2006Date of Patent: February 16, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B Timmermann, Gunnar Olsen, Elsebet Østergaard Nielsen, Tino Dyhring
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Publication number: 20100016295Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: July 31, 2006Publication date: January 21, 2010Applicant: Bayer Healthcare LLCInventors: Roger A. Smith, Derek Lowe, Tatiana Shelekhin, Georgiy Bondar, Philip Coish, Stephen J. O'Connor
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Publication number: 20100010228Abstract: Disclosed is a process for the asymmetric preparation of a phenyl(3-piperidinyl)methanol represented by Formula (I): wherein R is an optionally substituted phenyl and E is an amine protecting group.Type: ApplicationFiled: June 24, 2009Publication date: January 14, 2010Applicant: Vitae Pharmaceuticals, Inc.Inventor: Mark B. Mitchell
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Publication number: 20090318432Abstract: The application relates to novel nitrate ester derivatives of substituted aminoalcohols of the general formula (I), wherein R1, R2, R3, V, X, Y and Z0 have the meanings explained in more detail in the description, to a process for their preparation and to the use of these compounds as therapeutics in cardiovascular diseases, in particular in high blood pressure and vascular and organ damage age accompanying high blood pressure.Type: ApplicationFiled: September 11, 2007Publication date: December 24, 2009Applicant: SPEEDEL EXPERIMENTA AGInventors: Peter Herold, Robert Mah, Christiane Marti, Nathalie Jotterand
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Publication number: 20090281085Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: February 3, 2009Publication date: November 12, 2009Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
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Publication number: 20090253919Abstract: Chiral thioureas are effective catalysts for the borane reduction of prochiral ketones to optically active alcohols. A prochiral ketone may be reduced to an optically active alcohol in the presence of a substantially sub-stoichiometric amount of chiral thiourea. The asymmetric thiourea compound of the present invention may be produced according to a production method described herein.Type: ApplicationFiled: April 3, 2008Publication date: October 8, 2009Applicant: Board of RegentsInventors: Derun Li, John R. Falck
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Patent number: 7585856Abstract: The present invention is generally drawn to novel isolated therapeutic agents, termed resolvins, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenase-II (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or tri-hydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.Type: GrantFiled: August 12, 2003Date of Patent: September 8, 2009Assignee: The Brigham and Women's Hospital, Inc.Inventor: Charles N. Serhan
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Publication number: 20090209520Abstract: A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; Y is —CRRC2—(CH2)m—, where m is 0 or 1, RC1 is selected from H, CH3 and CF3, and RC2 is selected from H and CH3, or RC1 and RC2? together with the carbon atom to which they are attached form the 1,1-cyclopropylene group formula (A): RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; Het is formula (ii): where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F.Type: ApplicationFiled: June 15, 2007Publication date: August 20, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Muhammad Hashim Javaid, Sylvie Gomez, Xiao-Ling Fan Cockcroft, Keith Allan Menear, Niall Morrison Barr Martin
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Publication number: 20090203905Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.Type: ApplicationFiled: September 27, 2006Publication date: August 13, 2009Inventors: Jorgen Blixt, Michael David Golden, Philip John Hogan, David Michael Glanville Martin, Francis Joeph Montgomery, Zakariya Patel, John David Pittam, George Joseph Sependa, Christopher John Squire, Nicholas Cartwright Alexander Wright
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Publication number: 20090198065Abstract: To provide a resist polymer comprising, as a structural unit, an acid-decomposable unit having a structure represented by formula (1) or (2) which exhibits a small line edge roughness and produces little defects in DUV excimer laser lithography or the like.Type: ApplicationFiled: March 26, 2009Publication date: August 6, 2009Applicant: Mitsubishi Rayon Co., Ltd.Inventors: Hikaru Momose, Atsushi Ootake, Tadashi Nakamura, Akifumi Ueda
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Publication number: 20090192192Abstract: The present invention relates to the use of compounds as broad spectrum inhibitors of bacterial biofilm formation. In particular the invention refers to a family of compounds that block the quorum sensing system of Gram-negative and Gram-positive bacteria, a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of bacterial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.Type: ApplicationFiled: December 17, 2008Publication date: July 30, 2009Inventors: Aldo Ammendola, Tanja Wieber, Andreas Wuzik, Martin Lang
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Publication number: 20090186874Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B and ring C are each an aromatic ring optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), Z is an optionally halogenated C1-6 alkyl group, Y is a methylene group optionally having substituent(s), m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof. The compound of the present invention has a superior tachykinin receptor antagonistic action, particularly an SP receptor antagonistic action, and is useful as a pharmaceutical agent, for example, a tachykinin receptor antagonist, an agent for the prophylaxis or treatment of an abnormality of lower urinary tract functions, a digestive organ disease or a central nerve disease, and the like.Type: ApplicationFiled: January 13, 2005Publication date: July 23, 2009Inventors: Yoshinori Ikeura, Junya Shirai
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Patent number: 7560549Abstract: A compound having the formula (I) wherein R1 is a substituted phenyl, R2 is a phenyl substituted with halogen atoms, R3 is a substituted phenyl, D is an oxygen or a methylene, and n is 0 or 1. The compound is a synthetic intermediate for a neurokinin receptor antagonist.Type: GrantFiled: February 23, 2005Date of Patent: July 14, 2009Assignee: Sankyo Company, LimitedInventors: Hiroshi Tomori, Hiroshi Miyamoto, Keijiro Kobayashi
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Publication number: 20090170901Abstract: The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independently are hydrogen atom, hydroxy, benzyloxy, amino, nitro, C1-C4 alkylsulfonamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkoxy, aroyl-carbamoyl optionally substituted with halogen atom or C1-C4 alkyl or C1-C4 alkoxycarbonyl group, or the neighboring X and Y groups optionally form together with one or more identical or different additional hetero atom and —CH? and/or —CH2— groups an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably morpholine, pyrrole, pyrrolidine, oxo- or thioxo-pyrrolidine, pyrazole, pyrazolidine, imidazole, imidazolidine, oxo- or thioxo-imidazole or imidazolidine, 1,4-oxazine, oxazole, oxazolidine, triazole, oxo- or thioxo-oxazolidine, or 3-oxo-1,4-oxazine ring, V and Z independently are hydrogen or halogen atom, cyano, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl, hydroxy oType: ApplicationFiled: July 21, 2005Publication date: July 2, 2009Inventors: Istvan Borza, Gizella Bartané Szalai, Eva Bozo, Csilla Acsné Kiss, Csilla Horvath, Sandor Farkas, Jozsef Nagy, Sandor Kolok
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Patent number: 7534814Abstract: A compound of formula wherein R2 is arylene or heterocyclene; or R and R2 together with the nitrogen atom to which they are attached form non-aromatic heterocyclene; and the other residues have various meanings, useful as pharmaceuticals, e.g. antimicrobials.Type: GrantFiled: June 14, 2004Date of Patent: May 19, 2009Assignee: Nabriva Therapeutics AGInventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
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Patent number: 7528152Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.Type: GrantFiled: February 2, 2007Date of Patent: May 5, 2009Assignee: Eisai Co., Ltd.Inventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
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Publication number: 20090099186Abstract: The embodiments provide compounds of the general Formulas I-IV, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: October 10, 2006Publication date: April 16, 2009Inventors: Leonid Beigelman, Steven W. Andrews, Kevin R. Condroski, Indrani Gunawaradana, Julia Haas
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Publication number: 20090093520Abstract: Compounds of the following formula (I), for example: wherein R1, R2, R3, and R4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: ApplicationFiled: December 11, 2008Publication date: April 9, 2009Inventors: Brad BUCKMAN, Kumar Emayan, Imadul Islam, Karen May, Judi Bryant, Raju Mohan, Christopher West, Shendon Yuan
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Publication number: 20090069331Abstract: Compounds of formula (I) have been found to be useful as inhibitors of DDAH.Type: ApplicationFiled: November 11, 2005Publication date: March 12, 2009Applicant: UCL Biomedica PLC c/o Finance Division University College of LondonInventors: Patrick John Thompson Vallance, James Mitchell Leiper, David Lawrence Selwood, Sharon Rossiter, Basil Hartzoulakis
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Patent number: 7488844Abstract: The present invention provides a compound of formula I processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.Type: GrantFiled: December 30, 2004Date of Patent: February 10, 2009Assignee: AstraZeneca ABInventors: Eva-Lotte Lindstedt Alstermark, Anna Christina Olsson, Lanna Li
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Publication number: 20090036423Abstract: 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: ApplicationFiled: February 1, 2008Publication date: February 5, 2009Inventors: Shifeng Pan, Wenqi Gao, Nathanael S. Gray, Yuan Mi, Yi Fan
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Publication number: 20080275086Abstract: The invention relates to compounds of formula (I) wherein Z, R1-7, X and n have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.Type: ApplicationFiled: February 20, 2006Publication date: November 6, 2008Inventors: Paul John Edwards, Silvia Cerezo-Galvez, Meritxell Lopez-Canet, Victor Giulio Matassa, Claudia Rosenbaum, Christian Rummey, Sonja Nordhoff
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Publication number: 20080262234Abstract: The present invention relates to a new and useful process for preparing N,N-substituted carbamoyl halides from secondary amines, carbon dioxide, trialkylsilyl chloride and a halogenating agent.Type: ApplicationFiled: October 26, 2006Publication date: October 23, 2008Inventors: Ilaria Bientinesi, Zadeo Cimarosti, Giuseppe Guercio, Corinne Leroi, Alcide Perboni
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Publication number: 20080132544Abstract: An object of the present invention is to provide a peroxisome proliferator-activated receptor ? (PPAR?) ligand derived from a natural product and to provide a composition for prevention or improvement of insulin resistant syndrome, diabetes mellitus, obesity, or visceral fat obesity, characterized by comprising the ligand as an active ingredient. The present invention provides a PPAR? ligand comprising as an active ingredient, at least one compound selected from the group consisting of coumaperine and derivatives thereof. The present invention also provides a composition for prevention or improvement of insulin resistant syndrome, diabetes mellitus, obesity, or visceral fat obesity comprising the compound as an active ingredient.Type: ApplicationFiled: December 19, 2005Publication date: June 5, 2008Applicant: KANEKA CORPORATIONInventors: Mitsuaki Kitano, Misuzu Tsukagawa, Eisaku Konishi, Tatsumasa Mae, Kazunori Hosoe
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Publication number: 20080108820Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.Type: ApplicationFiled: September 22, 2004Publication date: May 8, 2008Inventors: Silvio A. Campagna, Francis G. Fang, James J. Kowalczyk, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
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Patent number: 7345174Abstract: The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.Type: GrantFiled: June 22, 2006Date of Patent: March 18, 2008Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Ronald Breslow, Sandro Belvedere, Leland Gershell, Thomas A. Miller, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
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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: 7276610Abstract: The invention provides novel GlyT2 inhibiting compounds useful in modulating, treating, or preventing: anxiolytic disorders; a condition requiring treatment of injured mammalian nerve tissue; a condition amenable to treatment through administration of a neurotrophic factor; a neurological disorder; or obesity; an obesity-related disorder.Type: GrantFiled: August 17, 2004Date of Patent: October 2, 2007Assignee: Janssen Pharaceutica, NVInventors: Charles Q. Huang, Timothy W. Lovenberg, Alejandro Santillán, Jr., Liu Y. Tang, Ronald L. Wolin
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Patent number: 7262211Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.Type: GrantFiled: December 4, 2002Date of Patent: August 28, 2007Assignee: Dendreon CorporationInventors: Amir P. Tamiz, L. Josue Alfaro-Lopez, Odile Esther Levy, Joseph Edward Semple
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Patent number: 7241902Abstract: Compounds which are the reaction product of allicin and ACE-inhibiting compounds are useful in treating hypertension, elevated triglycerides, and elevated insulin.Type: GrantFiled: May 30, 2002Date of Patent: July 10, 2007Assignee: Yeda Research and Development Co. Ltd.Inventors: Talia Miron, Aharon Rabinkov, David Mirelman, Meir Wilchek
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Patent number: 7192972Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1–R7, X1, X2, R, Q, and n are as defined herein.Type: GrantFiled: March 21, 2003Date of Patent: March 20, 2007Assignee: Eisai Co., Ltd.Inventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
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Patent number: 7148219Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: April 29, 2005Date of Patent: December 12, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Rongliang Lou, Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Patent number: 7125895Abstract: This invention relates to novel arylalkyl cyclic amine derivatives. This invention also relates to chemokine receptor antagonists that are be effective as therapeutic agents and/or preventive agents for diseases such as atherosclerosis, rheumatoid arthritis, transplant rejection, psoriasis, asthma, ulcerative colitis, glomerulonephritis, multiple sclerosis, pulmonary fibrosis, and myocarditis, in which tissue infiltration of blood monocytes and lymphocytes plays a major role in the initiation, progression or maintenance of the disease. Furthermore, chemokine receptor antagonists also inhibit the interaction of viruses, which attack blood monocytes and lymphocytes, through the use of a chemokine receptor. One such example is the HIV virus.Type: GrantFiled: May 12, 2000Date of Patent: October 24, 2006Assignee: Bristol-Myers Squibb Pharma Research Labs, Inc.Inventors: Christine M. Tarby, Wilna Moree
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Patent number: 7094909Abstract: The present invention concerns processes for preparing compounds of formula (I-H), or a prodrug, pharmaceutically active metabolite, or pharmaceutically active salt or solvate thereof, which are useful as inhibitors of the HIV protease enzyme.Type: GrantFiled: December 4, 2003Date of Patent: August 22, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: David John Kucera, Robert William Scott
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Patent number: 7087604Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis, asthma, restinosis, organ transplantation, and cancer.Type: GrantFiled: March 7, 2003Date of Patent: August 8, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Robert J. Cherney
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Patent number: 7084277Abstract: This invention relates to 3-amino piperidine derivatives, their intermediates and methods of manufacture. As such, the present invention includes methods of making a compound of the formulas (Ia) and (Ib) wherein R1, R2, R3, R4, R14, and n are herein defined. The present invention also relates to the compounds used in such processes, as well as the compounds made by the processes.Type: GrantFiled: November 20, 2003Date of Patent: August 1, 2006Assignee: Pfizer Inc.Inventor: David H. B. Ripin
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Patent number: 7084120Abstract: Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy.Type: GrantFiled: December 22, 2000Date of Patent: August 1, 2006Assignee: Probiodrug AGInventors: Hans-Ulrich Demuth, Dagmar Schlenzig, Torsten Hoffmann, Susanne Manhart
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Patent number: 7060836Abstract: Compounds of the formula (I): or a pharmaceutically acceptable salt, prodrug, solvate or polymorph thereof, wherein R, R1, and Z are as defined herein, are useful in treating or preventing a condition for which an NK2 antagonist is efficacious.Type: GrantFiled: December 17, 2002Date of Patent: June 13, 2006Assignee: Pfizer, IncInventors: Donald Stuart Middleton, Alan Stobie
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Patent number: 7056709Abstract: Recombinant microbial strains are provided that express nitrilase enzyme and are useful as biocatalysts for the hydrolysis of nitrile-containing substrates. The recombinant cells are transformed with a foreign gene isolated from Acidovorax facilis 72W encoding a thermostable nitrilase enzyme that catalyzes the hydrolysis of nitrile-containing substrates to carboxylic acids under mild reaction conditions. The nucleotide sequence of the nitrilase gene and the deduced amino acid sequence encoded by the nitrilase gene are provided.Type: GrantFiled: February 27, 2003Date of Patent: June 6, 2006Assignee: E. I. du Pont de Nemours and CompanyInventors: Sarita Chauhan, Robert Dicosimo, Robert D. Fallon, John E. Gavagan, Mark S. Payne
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Patent number: 7041678Abstract: The present invention provides an alkaloid compound that is an inhibitor of mycotoxin biosynthesis. The alkaloid is an alkenyl piperidine amide wherein the alkenyl is a C18 alkenyl with one or more double bonds. The alkaloid inhibits transcription of the fungus genes nor-1, tri5, and ipnA. The present invention further provides a method for identifying compounds, which inhibit biosynthesis of aflatoxin in Aspergillus spp. and deoxynivalenol in Gibberella spp. without inhibiting growth of the fungus in vitro.Type: GrantFiled: September 17, 2004Date of Patent: May 9, 2006Assignee: Board of Trustees of Michigan State UniversityInventors: Frances Trail, Raymond Hammerschmidt, John E. Linz, Haixin Xu, Luis Velasquez, Seanna L. Annis
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Patent number: 7034184Abstract: A process comprising allowing a peroxide compound represented by following Formula (2): wherein Ra, Rb, Rc and Rd are the same or different and are each a hydrogen atom or a hydrocarbon group, and wherein Ra and Rb, Rc and Rd may be combined to form a ring together with the adjacent carbon atom, respectively, to react with ammonia and water to yield an azine compound represented by following Formula (3): wherein Ra, Rb, Rc and Rd have the same meanings as defined above, or oxime compounds represented by following Formulae (4a) and/or (4b): wherein Ra, Rb, Rc and Rd have the same meanings as defined above, in the presence of a nitrogen-containing cyclic compound constitutively having a skeleton represented by following Formula (A) in its ring: wherein X is one of an oxygen atom and an —OR group, and wherein R is one of a hydrogen atom and a hydroxyl-protecting group.Type: GrantFiled: March 6, 2003Date of Patent: April 25, 2006Assignee: Daicel Chemical Industries, Ltd.Inventors: Yasutaka Ishii, Tatsuya Nakano
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Patent number: 7019003Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: March 1, 2002Date of Patent: March 28, 2006Assignee: Smithkline Beecham CorporationInventors: Jia-Ning Xiang, Siegfried B. Christensen, IV, Jinhwa Lee, Daniel J. Mercer
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Patent number: 6930186Abstract: The present invention is directed to methods for preparing intermediates useful in the synthesis of paroxetine wherein the intermediates are substantially free of alkoxy impurities as well as to methods for preparing paroxetine and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities. The alkoxy impurity is reacted with an ether cleaving agent to generate the corresponding phenol, which is separated, yielding the desired product substantially free of alkoxy impurities. Paroxetine intermediates such as PMA, paroxetine, and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities also form part of the present invention.Type: GrantFiled: June 13, 2002Date of Patent: August 16, 2005Assignee: Teva Pharmacetical Industries Ltd.Inventors: Valerie Niddam, Ilya Avrutov
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Patent number: 6927290Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p??(1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH??(2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX??(3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.Type: GrantFiled: May 10, 2004Date of Patent: August 9, 2005Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Miki, Hideki Ushio, Isao Kurimoto
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Patent number: 6921822Abstract: The present invention relates to a process for preparing stereoisomerically enriched 4-aryl-4-hydroxybutanoic acid derivatives by reducing 4-aryl-4-ketobutanoic acid derivatives in the presence of ruthenium-containing catalysts.Type: GrantFiled: June 9, 2003Date of Patent: July 26, 2005Assignee: Bayer AktiengesellschaftInventors: Hans-Christian Militzer, Boris Bosch, Markus Eckert, Benjamin Meseguer
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Patent number: 6875870Abstract: Hindered amine compounds which are substituted by a long hydrocarbon chain are useful in a number of applications where the solubility or compatibility afforded by said substitution is needed. This is seen particularly for example with white, dyed, dipped, unscented and/or scented candle wax which is effectively stabilized against discoloration and fading by the incorporation therein of a long chain hindered amine alone or in combination with a UV absorber and/or an antioxidant.Type: GrantFiled: December 18, 2003Date of Patent: April 5, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Mervin G. Wood, Andrea R. Smith, James P. Galbo