The Oxygen Is In A Carbonyl Group Patents (Class 544/175)
  • Patent number: 9376425
    Abstract: 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: Grant
    Filed: September 26, 2012
    Date of Patent: June 28, 2016
    Assignee: 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
  • Patent number: 9150573
    Abstract: 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: Grant
    Filed: July 1, 2014
    Date of Patent: October 6, 2015
    Assignee: Adverio Pharma GmbH
    Inventor: Peter Fey
  • Publication number: 20140315926
    Abstract: 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: Application
    Filed: July 1, 2014
    Publication date: October 23, 2014
    Inventor: Peter FEY
  • Patent number: 8802847
    Abstract: 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: Grant
    Filed: November 26, 2012
    Date of Patent: August 12, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventor: Peter Fey
  • Patent number: 8796479
    Abstract: 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: Grant
    Filed: July 22, 2005
    Date of Patent: August 5, 2014
    Inventor: David Kenneth Pinches
  • Publication number: 20140130713
    Abstract: 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: Application
    Filed: May 22, 2012
    Publication date: May 15, 2014
    Applicant: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Michael G. Costello, Michael J. Bulinski, Richard M. Flynn
  • Publication number: 20140080833
    Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.
    Type: Application
    Filed: November 11, 2013
    Publication date: March 20, 2014
    Applicant: MannKind Corporation
    Inventors: Gary A. Flynn, Sandra A. Lee, Mary Faris, David W. Brandt, Subrata Chakravarty
  • Patent number: 8617855
    Abstract: 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: Grant
    Filed: October 24, 2007
    Date of Patent: December 31, 2013
    Inventor: Dieter Tischendorf
  • Publication number: 20130172191
    Abstract: 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: Application
    Filed: February 25, 2013
    Publication date: July 4, 2013
    Inventors: Richard Martin Jacobson, Martha Jean Kelly, William Nixon James
  • Publication number: 20130143900
    Abstract: 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: Application
    Filed: November 26, 2012
    Publication date: June 6, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventor: BAYER INTELLECTUAL PROPERTY GMBH
  • Patent number: 8399662
    Abstract: 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: Grant
    Filed: November 9, 2009
    Date of Patent: March 19, 2013
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Tae-Sook Jeong, Woo-Song Lee, Hyung-Jae Jeong, Yong-Dae Park, Jong-Min Han, Hyoung-Chin Kim, Og-Sung Moon, Young-Suk Won
  • Publication number: 20120329649
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: 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
  • Patent number: 8105504
    Abstract: 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: Grant
    Filed: August 22, 2005
    Date of Patent: January 31, 2012
    Assignee: BASF SE
    Inventors: Michèle Gerster, Peter Nesvadba
  • Publication number: 20110230488
    Abstract: 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: Application
    Filed: November 25, 2009
    Publication date: September 22, 2011
    Applicant: TRT PHARMA INC.
    Inventors: Jian Hui Wu, Gerald Batist, Jinming Zhou, Guoyan Geng, Rongtuan Lin
  • Patent number: 7939531
    Abstract: 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: Grant
    Filed: February 20, 2009
    Date of Patent: May 10, 2011
    Assignee: Roche Palo Alto
    Inventors: 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
  • Patent number: 7932254
    Abstract: 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: Grant
    Filed: February 20, 2009
    Date of Patent: April 26, 2011
    Assignee: Roche Palo Alto
    Inventors: Daisy Joe DuBois, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Yan Lou, Timothy D. Owens, Calvin Wesley Yee
  • Publication number: 20100298329
    Abstract: 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: Application
    Filed: September 19, 2008
    Publication date: November 25, 2010
    Applicant: Massachusette Institute of Technology
    Inventors: Alice T. Shaw, Tyler E. Jacks, Nicola Tolliday
  • Publication number: 20100137588
    Abstract: 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: Application
    Filed: November 24, 2009
    Publication date: June 3, 2010
    Applicant: BROCK UNIVERSITY
    Inventor: Costa Metallinos
  • Publication number: 20100104979
    Abstract: 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: Application
    Filed: March 25, 2008
    Publication date: April 29, 2010
    Inventors: Kurt Dietliker, Peter Murer, Rinaldo Hüsler, Tunja Jung
  • Patent number: 7700769
    Abstract: 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: Grant
    Filed: August 15, 2008
    Date of Patent: April 20, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Matthias Hoffmann
  • Publication number: 20100093713
    Abstract: 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: Application
    Filed: December 17, 2009
    Publication date: April 15, 2010
    Applicant: 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
  • Publication number: 20100087437
    Abstract: 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: Application
    Filed: August 31, 2009
    Publication date: April 8, 2010
    Applicant: Xention Limited
    Inventors: Derek Edward JOHN, Mushtag MULLA, Richard John HAMLYN, Simon Mark JONES, Derek Roland POLLARD, Basil HARTZOULAKIS, Helen PAYNE, David MADGE, John FORD
  • Publication number: 20100056780
    Abstract: 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: Application
    Filed: November 9, 2009
    Publication date: March 4, 2010
    Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Tae-Sook JEONG, Woo-Song LEE, Hyung-Jae JEONG, Yong-Dae PARK, Jong-Min HAN, Hyoung-Chin KIM, Og-Sung MOON, Young-Suk WON
  • Publication number: 20090299063
    Abstract: 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: Application
    Filed: March 29, 2006
    Publication date: December 3, 2009
    Inventors: Paul Shapiro, Alexander D. MacKerell, JR.
  • Patent number: 7598241
    Abstract: 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: Grant
    Filed: January 8, 2004
    Date of Patent: October 6, 2009
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christoph van Amsterdam
  • Patent number: 7534880
    Abstract: 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: Grant
    Filed: August 3, 2004
    Date of Patent: May 19, 2009
    Assignee: Lamberti SpA
    Inventors: Gabriele Norcini, Stefano Romagnano, Marco Visconti, Giuseppe Li Bassi
  • Publication number: 20090018333
    Abstract: 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: Application
    Filed: August 15, 2008
    Publication date: January 15, 2009
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias GRAUERT, Matthias HOFFMANN
  • Publication number: 20080280883
    Abstract: 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: Application
    Filed: September 23, 2005
    Publication date: November 13, 2008
    Inventors: Mohammad Salman, Pakala Kumara Savithru Sarma, Sankaranarayanan Dharmarajan, Anita Chugh, Suman Gupta
  • Publication number: 20080221106
    Abstract: 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: Application
    Filed: August 5, 2005
    Publication date: September 11, 2008
    Inventors: Liya Zhu, Wenjie Wang, Halhong Huang, Ziyun Lin, Liyuan Mou, Zhengui Nie, Yu He, Xueyu Ouyang, Shanying Peng, Dongfong Zhang, Jun Wei
  • Patent number: 7414053
    Abstract: 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: Grant
    Filed: August 24, 2005
    Date of Patent: August 19, 2008
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Matthias Hoffmann, Martin Steegmaier, Flavio Solca, Jens Juergen Quant
  • Patent number: 7291654
    Abstract: 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: Grant
    Filed: October 17, 2003
    Date of Patent: November 6, 2007
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Thomas Ulrich, Thomas Bolle, Kurt Dietliker, Jean-Pierre Wolf, André Fuchs
  • Patent number: 7030201
    Abstract: The present invention relates to bottom antireflective coating compositions and polymers useful in making such compositions.
    Type: Grant
    Filed: November 26, 2003
    Date of Patent: April 18, 2006
    Assignee: AZ Electronic Materials USA Corp.
    Inventors: Huirong Yao, Shuji Ding-Lee, Hengpeng Wu, Zhong Xiang
  • Patent number: 6749988
    Abstract: 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: Grant
    Filed: November 28, 2001
    Date of Patent: June 15, 2004
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
  • Patent number: 6689882
    Abstract: 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: Grant
    Filed: November 12, 2002
    Date of Patent: February 10, 2004
    Assignee: AstraZeneca AB
    Inventor: Wei Tian
  • Publication number: 20040024209
    Abstract: The present invention provides compounds of formula I 1
    Type: Application
    Filed: July 21, 2003
    Publication date: February 5, 2004
    Inventor: Mark E. Schnute
  • Patent number: 6638930
    Abstract: 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: Grant
    Filed: April 17, 2001
    Date of Patent: October 28, 2003
    Assignee: 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
  • Patent number: 6562815
    Abstract: 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-C4
    Type: Grant
    Filed: August 16, 2000
    Date of Patent: May 13, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Dario Lazzari, Thomas Bolle, Mirko Rossi, Hugh Stephen Laver
  • Publication number: 20030088095
    Abstract: 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: Application
    Filed: August 7, 2002
    Publication date: May 8, 2003
    Applicant: CENTRAL GLASS COMPANY, LIMITED
    Inventors: Akihiro Ishii, Masatomi Kanai, Takashi Hayami, Katsuyoshi Shibata, Masaki Matsui, Kazumasa Funabiki, Yokusu Kuriyama, Manabu Yasumoto
  • Patent number: 6531471
    Abstract: 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: Grant
    Filed: December 14, 2001
    Date of Patent: March 11, 2003
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
  • Patent number: 6511980
    Abstract: 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: Grant
    Filed: April 10, 2001
    Date of Patent: January 28, 2003
    Assignee: Ortho McNeil Pharmaceutical, Inc.
    Inventors: Sigmond G. Johnson, Ralph A. Rivero
  • Patent number: 6458781
    Abstract: 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: Grant
    Filed: October 25, 1999
    Date of Patent: October 1, 2002
    Inventors: David Thomas Connor, Lain-Yen Hu, Thomas Charles Malone, Michael Francis Rafferty, Bruce David Roth, Todd Robert Ryder, Anthony Denver Sercel, Yuntao Song
  • Patent number: 6458957
    Abstract: 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: Grant
    Filed: July 12, 2000
    Date of Patent: October 1, 2002
    Assignee: Geneva Pharmaceuticals, Inc.
    Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
  • Publication number: 20020049202
    Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.
    Type: Application
    Filed: April 13, 2001
    Publication date: April 25, 2002
    Inventors: Margaret L. Grapperhaus, James A. Sikorski, Alok K. Awasthi, Lijuan J. Wang, Barnett S. Pitzele, Donald W. Hansen, Pamela T. Manning
  • Patent number: 6362182
    Abstract: 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: Grant
    Filed: October 30, 2000
    Date of Patent: March 26, 2002
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
  • Patent number: 6355672
    Abstract: 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: Grant
    Filed: January 30, 2001
    Date of Patent: March 12, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
  • Publication number: 20010036942
    Abstract: 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: Application
    Filed: April 26, 2001
    Publication date: November 1, 2001
    Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
  • Patent number: 6307087
    Abstract: 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: Grant
    Filed: January 13, 1999
    Date of Patent: October 23, 2001
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, David W. Old, John P. Wolfe, Michael Palucki, Ken Kamikawa
  • Patent number: 6218390
    Abstract: 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: Grant
    Filed: December 17, 1998
    Date of Patent: April 17, 2001
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
  • Patent number: 6200972
    Abstract: 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: Grant
    Filed: February 23, 1998
    Date of Patent: March 13, 2001
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Jia-He Li, Gregory S. Hamilton
  • Patent number: 6191182
    Abstract: 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: Grant
    Filed: June 10, 1999
    Date of Patent: February 20, 2001
    Assignee: Ciba Specialty Chemcials Corporation
    Inventors: Rinaldo Hüsler, Rudolf Schwabe, Reto Luisoli