The Oxygen Is In A Carbonyl Group Patents (Class 544/175)
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Patent number: 9376425Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.Type: GrantFiled: September 26, 2012Date of Patent: June 28, 2016Assignee: Amgen, Inc.Inventors: Michael D. Bartberger, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason A. Duquette, John Eksterowicz, Brian M. Fox, Jiasheng Fu, Ana Gonzalez Buenrostro, Felix Gonzalez Lopez De Turiso, Darin J. Gustin, Julie A. Heath, Michael G. Johnson, Frank Kayser, David John Kopecky, Yihong Li, Zhihong Li, Zhihua Ma, Joel McIntosh, Julio C. Medina, Jeffrey Thomas Mihalic, Steven H. Olson, Yosup Rew, Philip M. Roveto, Michael J. Schmitt, Daqing Sun, Xiaodong Wang, Malgorzata Wanska, Christine Weathers, Xuelei Yan
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Patent number: 9150573Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.Type: GrantFiled: July 1, 2014Date of Patent: October 6, 2015Assignee: Adverio Pharma GmbHInventor: Peter Fey
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Publication number: 20140315926Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: July 1, 2014Publication date: October 23, 2014Inventor: Peter FEY
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Patent number: 8802847Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.Type: GrantFiled: November 26, 2012Date of Patent: August 12, 2014Assignee: Bayer Intellectual Property GmbHInventor: Peter Fey
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Patent number: 8796479Abstract: A process for recovering a lipid from a lipid containing material, comprising subjecting the lipid containing material to superheated steam and recovering the lipid in a liquid state.Type: GrantFiled: July 22, 2005Date of Patent: August 5, 2014Inventor: David Kenneth Pinches
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Publication number: 20140130713Abstract: Partially fluorinated ketones are provided that include a terminal alkyl group having from 1 to 6 carbon atoms bonded to a carbonyl group and a hydrofluoroether moiety having from 2 to 4 carbon atoms that contains at least one hydrogen substituent. The hydrofluoroether moiety is bonded to the carbonyl group with a carbon-carbon bond. The ether oxygen is bonded to a carbon atom that is at least two carbon atoms removed from the carbonyl group. Additionally, a fluorinated alkyl group having from 1 to 10 carbon atoms is bonded to the ether oxygen of the hydrofluoroether moiety. These partially fluorinated ketones can be used in a wide variety of electronics applications.Type: ApplicationFiled: May 22, 2012Publication date: May 15, 2014Applicant: 3M INNOVATIVE PROPERTIES COMPANYInventors: Michael G. Costello, Michael J. Bulinski, Richard M. Flynn
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Publication number: 20140080833Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.Type: ApplicationFiled: November 11, 2013Publication date: March 20, 2014Applicant: MannKind CorporationInventors: Gary A. Flynn, Sandra A. Lee, Mary Faris, David W. Brandt, Subrata Chakravarty
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Patent number: 8617855Abstract: A method for producing starting materials or additives for cosmetics, pharmaceuticals and/or hydrocarbon-based fuels, especially for heating systems or internal combustion engines, takes organic residues or waste materials and decontaminates or sterilizes them with a hydrogenation process. In particular, the materials classified as K1, K2 or K3 according to EU Directive 1774/2002 are used for generating or producing the cited starting materials or additives, whereby an adequate decontamination of the residues or waste materials that are classified as being hazardous to health is ensured.Type: GrantFiled: October 24, 2007Date of Patent: December 31, 2013Inventor: Dieter Tischendorf
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Publication number: 20130172191Abstract: A method to inhibit the ethylene response in plants with cyclopropene compounds by first generating stable cyclopropane precursor compounds and then converting these compounds to the gaseous cyclopropene antagonist compound by use of a reducing or nucleophilic agent.Type: ApplicationFiled: February 25, 2013Publication date: July 4, 2013Inventors: Richard Martin Jacobson, Martha Jean Kelly, William Nixon James
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Publication number: 20130143900Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: November 26, 2012Publication date: June 6, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: BAYER INTELLECTUAL PROPERTY GMBH
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Patent number: 8399662Abstract: The present invention relates to novel O-acyloxime derivatives, a preparation method thereof and a pharmaceutical composition comprising the same for prevention and treatment of cardiovascular disease. The O-acyloxime derivatives according to the present invention may valuably be used for prevention and treatment of cardiovascular diseases such as hyperlipidemia, coronary arterial heart disease, atherosclerosis, and myocardial infarction caused by Lp-PLA2, because they have excellent inhibitory effect of Lp-PLA2.Type: GrantFiled: November 9, 2009Date of Patent: March 19, 2013Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Tae-Sook Jeong, Woo-Song Lee, Hyung-Jae Jeong, Yong-Dae Park, Jong-Min Han, Hyoung-Chin Kim, Og-Sung Moon, Young-Suk Won
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Publication number: 20120329649Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: June 21, 2012Publication date: December 27, 2012Inventors: James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
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Patent number: 8105504Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula (I) wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.Type: GrantFiled: August 22, 2005Date of Patent: January 31, 2012Assignee: BASF SEInventors: Michèle Gerster, Peter Nesvadba
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Publication number: 20110230488Abstract: The present invention relates to the synthesis of a series of ionone and curcumin derivatives as multi-targeting agents effective against both hormone-sensitive and hormone-independent cancers. In particular, the present invention is directed to a distinct class of bifunctional antiandrogens, which inhibit both AR and IKBkinases (IKK). A series of ionone-based chalcones were synthesised and their in vitro cytotoxicity against prostate cancer cell lines were demonstrated. A series of derivatives formed by reacting ionone-based chalcones and hydrazines demonstrate substantial antiproliferative activities in prostate cancer, breast cancer and lung cancer cell lines.Type: ApplicationFiled: November 25, 2009Publication date: September 22, 2011Applicant: TRT PHARMA INC.Inventors: Jian Hui Wu, Gerald Batist, Jinming Zhou, Guoyan Geng, Rongtuan Lin
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Patent number: 7939531Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: February 20, 2009Date of Patent: May 10, 2011Assignee: Roche Palo AltoInventors: Joe Timothy Bamberg, Mark Bartlett, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, Jaehyeon Park, David Bernard Smith, Michael Soth, Hanbiao Yang, Calvin Wesley Yee
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Patent number: 7932254Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1 and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: February 20, 2009Date of Patent: April 26, 2011Assignee: Roche Palo AltoInventors: Daisy Joe DuBois, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Yan Lou, Timothy D. Owens, Calvin Wesley Yee
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Publication number: 20100298329Abstract: The invention provides compositions and methods for treating cancer. Aspects of the invention relate to therapeutic compositions comprising tolperisone and related compounds. Aspects of the invention relate to methods and compositions for treating Ras-associated cancers.Type: ApplicationFiled: September 19, 2008Publication date: November 25, 2010Applicant: Massachusette Institute of TechnologyInventors: Alice T. Shaw, Tyler E. Jacks, Nicola Tolliday
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Publication number: 20100137588Abstract: The present disclosure relates to a method for preparing an ortho-substituted aminoferrocene comprising reacting an aminoferrocene with a Lewis acid and a lithiating reagent in the presence of an electrophile to form the ortho-substituted aminoferrocene.Type: ApplicationFiled: November 24, 2009Publication date: June 3, 2010Applicant: BROCK UNIVERSITYInventor: Costa Metallinos
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Publication number: 20100104979Abstract: Compounds of the Formula (I) wherein x is an integer from 1-4; p is an integer from 1-3; q is an integer from 0-3; Ar is phenyl, naphthyl, anthryl or phenanthryl each of which optionally is substituted by one or more Cl, CN, OR5, C3-C5alkenyl or C1-C6alkyl which optionally is substituted by one or more OR6, COOR or halogen; R1 if x is 1, is ORS, O—X+, NR8R9, C1-C20alkyl optionally substituted by one or more COOR10, or is C2-C20alkyl interrupted by one ore more O, or is C2-C5alkenyl or phenyl-C1-C4alkyl; R1 if x is 2, is for example C1-C20alkylene; R1 if x is 3, is for example a tri-valent radical; R1if x is 4, is for example a tetravalent radical; R2and R3are hydrogen or C1-C8alkyl, or R2and R3 together are O, C1-C3alkylene or CH?CH; R4 is C1-C4alkyl; R5, R6, R7, R8, R9 and R10 are for example hydrogen or C1-C4alkyl; and X is a x-valent cationic counter ion; are in particular suitable as photoinitiators for the curing with UV-A light (320-450 nm).Type: ApplicationFiled: March 25, 2008Publication date: April 29, 2010Inventors: Kurt Dietliker, Peter Murer, Rinaldo Hüsler, Tunja Jung
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Patent number: 7700769Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: August 15, 2008Date of Patent: April 20, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Matthias Hoffmann
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Publication number: 20100093713Abstract: This invention provides beta-carboline compounds of formula wherein Ring A is a substituted pyridinyl, pyrimidinyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, pyranyl, tetrahydrofuranyl, cyclohexyl, cyclopentyl or thiomorpholinyl ring and R1, R2 and R3 are as described in the specification. The compounds are IKK-2 inhibitors that are useful for treating IKK-2-mediated diseases such as inflammatory diseases and cancer.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Michael E. Hepperle, Julie Fields Liu, Francois Soucy, Yingchun Ye, Robert S. Murray, Raman Prakash, Jeremy D. Little, Alfredo Castro, Hormoz Mazdiyasni, Paul E. Fleming, Dominic Reynolds
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Publication number: 20100087437Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives wherein R1, R2, R3, X1, and A are defined herein. The compounds are useful as potassium ion channel inhibitors.Type: ApplicationFiled: August 31, 2009Publication date: April 8, 2010Applicant: Xention LimitedInventors: Derek Edward JOHN, Mushtag MULLA, Richard John HAMLYN, Simon Mark JONES, Derek Roland POLLARD, Basil HARTZOULAKIS, Helen PAYNE, David MADGE, John FORD
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Publication number: 20100056780Abstract: The present invention relates to novel O-acyloxime derivatives, a preparation method thereof and a pharmaceutical composition comprising the same for prevention and treatment of cardiovascular disease. The O-acyloxime derivatives according to the present invention may valuably be used for prevention and treatment of cardiovascular diseases such as hyperlipidemia, coronary arterial heart disease, atherosclerosis, and myocardial infarction caused by Lp-PLA2, because they have excellent inhibitory effect of Lp-PLA2.Type: ApplicationFiled: November 9, 2009Publication date: March 4, 2010Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Tae-Sook JEONG, Woo-Song LEE, Hyung-Jae JEONG, Yong-Dae PARK, Jong-Min HAN, Hyoung-Chin KIM, Og-Sung MOON, Young-Suk WON
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Publication number: 20090299063Abstract: Provided herein are compounds and methods of using compounds that selectively inhibit binding to one or more docking domain regions of an extracellular signal-recognition kinase to inhibit in a cell having an extracellular signal-regulated kinase activity. Such methods may be used to inhibit cell proliferation of a neoplastic cell, to treat a cancer and further may be used in conjunction with administration of an anticancer drug at a reduced dosage to treat a cancer with a concomitant reduction in toxicity to an individual receiving the treatment. Also provided is a method to design and screen for compounds to inhibit binding within the extracellular signal-regulated kinase docking domain region, using at least in part computer-aided drug design modeling.Type: ApplicationFiled: March 29, 2006Publication date: December 3, 2009Inventors: Paul Shapiro, Alexander D. MacKerell, JR.
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Patent number: 7598241Abstract: Novel compounds of the formula (I) in which R1, D, X, W, Y and T have the meaning indicated in Patent Claim (1), e.g. (II), are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.Type: GrantFiled: January 8, 2004Date of Patent: October 6, 2009Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christoph van Amsterdam
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Patent number: 7534880Abstract: The present invention relates to clear photopolymerisable systems for the preparation of high thickness coatings, to a procedure for their application and to the solid surfaces coated with them.Type: GrantFiled: August 3, 2004Date of Patent: May 19, 2009Assignee: Lamberti SpAInventors: Gabriele Norcini, Stefano Romagnano, Marco Visconti, Giuseppe Li Bassi
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Publication number: 20090018333Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: ApplicationFiled: August 15, 2008Publication date: January 15, 2009Applicant: Boehringer Ingelheim International GmbHInventors: Matthias GRAUERT, Matthias HOFFMANN
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Publication number: 20080280883Abstract: This present invention generally relates to muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.Type: ApplicationFiled: September 23, 2005Publication date: November 13, 2008Inventors: Mohammad Salman, Pakala Kumara Savithru Sarma, Sankaranarayanan Dharmarajan, Anita Chugh, Suman Gupta
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Publication number: 20080221106Abstract: Disclosed Arylamine ketones of formula (I), their preparation methods, the pharmaceutical compositions containing them and their use in preventing and/or treating the diseases related to the plaque-activating factors, especially in anti-inflammation and immunization, more especially in the treatment of the acute or chronic inflammation, such as, osteoarthritis, oarthritis deformans, etc.Type: ApplicationFiled: August 5, 2005Publication date: September 11, 2008Inventors: Liya Zhu, Wenjie Wang, Halhong Huang, Ziyun Lin, Liyuan Mou, Zhengui Nie, Yu He, Xueyu Ouyang, Shanying Peng, Dongfong Zhang, Jun Wei
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Patent number: 7414053Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: August 24, 2005Date of Patent: August 19, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Matthias Hoffmann, Martin Steegmaier, Flavio Solca, Jens Juergen Quant
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Patent number: 7291654Abstract: Compounds of formula (I), wherein R1 is hydrogen or alkyl; R2 is C1-C4alkoxy or a morpholino radical; and R3 is hydrogen or C1-C4alkoxy, are suitable for improving the solubility of specific photoinitiators in formulations and accordingly enhance the storage stability of formulations comprising a photoinitiator and compounds of formula (I)Type: GrantFiled: October 17, 2003Date of Patent: November 6, 2007Assignee: Ciba Specialty Chemicals CorporationInventors: Thomas Ulrich, Thomas Bolle, Kurt Dietliker, Jean-Pierre Wolf, André Fuchs
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Patent number: 7030201Abstract: The present invention relates to bottom antireflective coating compositions and polymers useful in making such compositions.Type: GrantFiled: November 26, 2003Date of Patent: April 18, 2006Assignee: AZ Electronic Materials USA Corp.Inventors: Huirong Yao, Shuji Ding-Lee, Hengpeng Wu, Zhong Xiang
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Patent number: 6749988Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.Type: GrantFiled: November 28, 2001Date of Patent: June 15, 2004Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
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Patent number: 6689882Abstract: A new improved process for synthesizing morpholinylbenzenes of the formula I by reacting morpholine of formula II with a substituted benzene of formula III, wherein morpholine is used as a reactant and as the only one solvent.Type: GrantFiled: November 12, 2002Date of Patent: February 10, 2004Assignee: AstraZeneca ABInventor: Wei Tian
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Publication number: 20040024209Abstract: The present invention provides compounds of formula I 1Type: ApplicationFiled: July 21, 2003Publication date: February 5, 2004Inventor: Mark E. Schnute
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Patent number: 6638930Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: April 17, 2001Date of Patent: October 28, 2003Assignee: Merck & Co. Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Patent number: 6562815Abstract: The invention relates to new compounds containing 1-8 active groups of the type 3,3,6,6-polysubstituted 2-morpholinone and having the formula F (A′—Z)m—X (F), wherein m is a number from 1 to 8; X is an organic anchor group of valency m and in case that m is not 1, X may also be a direct bond, SO2, P or PO; A′ is a monovalent group of the formula E containing one linking group; Z is a direct bond, —O—, —S—, —SO—, —SO2— or —NR′14—; provided that Z is —O—, —S—, —SO—, —SO2— or —NR′14— if m is 1 and the linking group in formula E is G3 or G5; G1 is hydrogen; C1-C18alkyl; C2-C18alkyl substituted by OH and/or phenyl; oxyl; OH; C2-C12cyanoalkyl; C2-C12cyanoalkoxy; C1-C18alkoxy; C5-C12cycloalkoxy; C3-C8alkenyl; C3-C8alkynyl; C3-C8alkenyloxy; C7-C12phenylalkyl; C7-C12phenylalkyl substituted by hydroxy, C1-C4alkyl and/or C1-C4Type: GrantFiled: August 16, 2000Date of Patent: May 13, 2003Assignee: Ciba Specialty Chemicals CorporationInventors: Dario Lazzari, Thomas Bolle, Mirko Rossi, Hugh Stephen Laver
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Publication number: 20030088095Abstract: A first process for producing an optically active perfluoroalkylcarbinol derivative includes (a) reacting an optically active imine with a compound that is a hemiacetal of a perfluoroalkylaldehyde or a hydrate of a perfluoroalkylaldehyde to obtain a condensate; and (b) hydrolyzing the condensate under an acid condition. A second process for increasing optical purity of an optically active 4,4,4-trifluoro 3-hydroxy-1-aryl-1-butanone derivative includes (a) precipitating a racemic crystal of the derivative, from the derivative; and (b) removing the racemic crystal from the derivative. A third process for increasing optical purity of the butanone derivative includes recrystallizing the derivative. Novel compounds are optically active and inactive 4,4,4-trifluoro-3-hydroxybutanoic aryl ester derivatives.Type: ApplicationFiled: August 7, 2002Publication date: May 8, 2003Applicant: CENTRAL GLASS COMPANY, LIMITEDInventors: Akihiro Ishii, Masatomi Kanai, Takashi Hayami, Katsuyoshi Shibata, Masaki Matsui, Kazumasa Funabiki, Yokusu Kuriyama, Manabu Yasumoto
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Patent number: 6531471Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: December 14, 2001Date of Patent: March 11, 2003Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6511980Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: April 10, 2001Date of Patent: January 28, 2003Assignee: Ortho McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 6458957Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.Type: GrantFiled: July 12, 2000Date of Patent: October 1, 2002Assignee: Geneva Pharmaceuticals, Inc.Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
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Patent number: 6458781Abstract: The present invention provides compounds that block calcium channels and have the Formula I: The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.Type: GrantFiled: October 25, 1999Date of Patent: October 1, 2002Inventors: David Thomas Connor, Lain-Yen Hu, Thomas Charles Malone, Michael Francis Rafferty, Bruce David Roth, Todd Robert Ryder, Anthony Denver Sercel, Yuntao Song
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Publication number: 20020049202Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.Type: ApplicationFiled: April 13, 2001Publication date: April 25, 2002Inventors: Margaret L. Grapperhaus, James A. Sikorski, Alok K. Awasthi, Lijuan J. Wang, Barnett S. Pitzele, Donald W. Hansen, Pamela T. Manning
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Patent number: 6362182Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: October 30, 2000Date of Patent: March 26, 2002Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6355672Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.Type: GrantFiled: January 30, 2001Date of Patent: March 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Publication number: 20010036942Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: ApplicationFiled: April 26, 2001Publication date: November 1, 2001Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
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Patent number: 6307087Abstract: One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.Type: GrantFiled: January 13, 1999Date of Patent: October 23, 2001Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, David W. Old, John P. Wolfe, Michael Palucki, Ken Kamikawa
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Patent number: 6218390Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: December 17, 1998Date of Patent: April 17, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6200972Abstract: This invention relates to neurotrophic low molecular weight, small molecule heterocyclic esters and amides having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: GrantFiled: February 23, 1998Date of Patent: March 13, 2001Assignee: GPI NIL Holdings, Inc.Inventors: Jia-He Li, Gregory S. Hamilton
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Patent number: 6191182Abstract: A novel process for the preparation of compounds of formula I by aminolysis of a p-halophenyl alkyl ketone of formula II with a cyclic amine of formula III in water at a temperature of at least 130° C., in which formulae X is a halogen atom and R1, R2 and R3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.Type: GrantFiled: June 10, 1999Date of Patent: February 20, 2001Assignee: Ciba Specialty Chemcials CorporationInventors: Rinaldo Hüsler, Rudolf Schwabe, Reto Luisoli