Nitrogen In Alcohol Moiety Patents (Class 560/49)
  • Patent number: 10023680
    Abstract: An isocyanate reactive composition for making a polyurethane foam includes a tertiary amine urethane catalyst comprising a di(C1-C4)alkyl fatty alkyl amine and a polyester polyol. The use of one or more of fatty alkyl tertiary amine serves to reduce hydrolysis of the polyester polyol in the isocyanate reactive composition.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: July 17, 2018
    Assignee: Evonik Degussa GmbH
    Inventors: Gary Dale Andrew, Juan Jesus Burdeniuc, Goran Zarkov
  • Publication number: 20150094469
    Abstract: A borate moiety-contained linker and a bio-sensing element containing the same are disclosed. The borate moiety-contained linker can be used to modify a sensing molecule and connect the sensing molecule to a substrate to form the bio-sensing element.
    Type: Application
    Filed: December 4, 2014
    Publication date: April 2, 2015
    Inventors: Yaw-Kuen LI, Mo-Yuan SHEN, Yu-Ju PIEN
  • Publication number: 20140378541
    Abstract: Synthetic polyphenolic compounds of formula (I), their modes of synthesis, and pharmaceutical compositions thereof are provided herein. Use of the compounds and compositions described herein for treating cancer and for treating metabolic disorders is also provided.
    Type: Application
    Filed: June 15, 2012
    Publication date: December 25, 2014
    Applicants: WAYNE STATE UNIVERSITY, THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIVERSITY, HONG KONG POLYTECHNIC UNIVERSITY
    Inventors: Tak-Hang Chan, Sreedhar Pamu, Qing Ping Dou, Di Chen
  • Publication number: 20140163253
    Abstract: The present invention relates to the discovery of new class of linear and multiarmed hydrolysable linkers and cross linkers for use in the synthesis of biodegradable polymers such as, polyesters, polyurethanes, polyamides, polyureas and degradable epoxy amine resin. The linear and multiarmed hydrolysable linkers of the present invention include symmetrical and/or unsymmetrical ether carboxylic acids, amines, amide diols, amine polyols and isocyanates.
    Type: Application
    Filed: February 14, 2014
    Publication date: June 12, 2014
    Applicant: BEZWADA BIOMEDICAL, LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20140018422
    Abstract: Disclosed herein are derivatives of tetracaine that, among other things, block cyclic nucleotide gated (CNG) channels and are useful in the treatment of diseases characterized by overactive CNG channels such as retinal degeneration diseases.
    Type: Application
    Filed: December 14, 2012
    Publication date: January 16, 2014
    Inventors: Jeffrey Karpen, Sarah Kirk, Adriana Andrade, Michelle Schaffer, Kenneth Melich
  • Publication number: 20130310596
    Abstract: The present invention relates to the discovery of new class of linear and multiarmed hydrolysable linkers and cross linkers for use in the synthesis of biodegradable polymers such as, polyesters, polyurethanes, polyamides, polyureas and degradable epoxy amine resin. The linear and multiarmed hydrolysable linkers of the present invention include symmetrical and/or unsymmetrical ether carboxylic acids, amines, amide diols, amine polyols and isocyanates.
    Type: Application
    Filed: November 8, 2012
    Publication date: November 21, 2013
    Applicant: BEZWADA BIOMEDICAL, LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20130096151
    Abstract: The present invention relates to the use of an anesthetic agent for killing clinically latent microorganisms associated with microbial infections and to novel combinations comprising an anesthetic agent and an antimicrobial agent for the treatment of microbial infections.
    Type: Application
    Filed: March 29, 2011
    Publication date: April 18, 2013
    Applicant: HELPERBY THERAPEUTICS LIMITED
    Inventors: Yanmin Hu, Anthony M.R. Coates
  • Publication number: 20110300567
    Abstract: A method for identifying the redox activity of a subject compound is disclosed. The method can be performed aerobically and can include forming a mixture comprising a free-radical precursor and a compound to be tested, and converting the free-radical precursor into a free-radical anion and a free-radical cation. After the free radical cation and the free radical anion have been formed, the relative redox activity of the subject compound may cause a difference in the rate of photo-bleaching of the mixture and/or the rate of superoxide generation. These differences can be quantified and used to identify the redox activity of the subject compound. This sensitive technique for measuring redox activity can be used to screen compounds for various biological applications. Drugs also can be developed based on the relationship between redox activity and biological activity for particular biological applications.
    Type: Application
    Filed: August 9, 2011
    Publication date: December 8, 2011
    Inventors: Jonathan J. Abramson, Benjamin S. Marinov
  • Publication number: 20110152210
    Abstract: Synthetic polyphenolic compounds of formula (I), their modes of synthesis, and pharmaceutical compositions thereof are provided herein. Use of the compounds and compositions described herein for inhibiting proteasomal activity and for treating cancer is also provided.
    Type: Application
    Filed: December 15, 2010
    Publication date: June 23, 2011
    Applicants: THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/McGILL UNIVERSITY, THE HONG KONG POLYTECHNIC UNIVERSITY, WAYNE STATE UNIVERSITY
    Inventors: Tak-Hang CHAN, Q. Ping DOU
  • Patent number: 7928141
    Abstract: Taught is a composition for enhancing potency and/or for prolonging the duration of action of an anesthetic comprising dexamethasone, compound vitamin B, metronidazole, berberine, etamsylate, gentamicin, chymotrypsin, methylene blue trihydrate, and 5% sodium bicarbonate aq. When administered with an anesthetic, the composition shortens the onset time of the anesthetic, and prolongs the duration of anesthesia.
    Type: Grant
    Filed: January 14, 2008
    Date of Patent: April 19, 2011
    Inventor: Fuchao Li
  • Patent number: 7589124
    Abstract: The invention provides novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions and kits comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
    Type: Grant
    Filed: April 4, 2007
    Date of Patent: September 15, 2009
    Assignee: NicOx, S.A.
    Inventors: L. Gordon Letts, David S. Garvey
  • Publication number: 20080317729
    Abstract: This invention relates to ammonium salts and stable storable ammonium salts and ammonium salt/mineral salt clathrate compounds (inclusion compounds, clusters) having acid dibasic anionic acid residues such as bicarbonate, to methods for producing them and to pharmaco-medical and chemical synthetic applications for said compounds.
    Type: Application
    Filed: July 20, 2005
    Publication date: December 25, 2008
    Inventors: Helmut Kasch, Uwe Reuter, Ralf Oettmeier
  • Patent number: 7371831
    Abstract: Compounds of formula (I) wherein all substituents have the meanings as defined in the Specification, their production and their use.
    Type: Grant
    Filed: February 11, 2002
    Date of Patent: May 13, 2008
    Assignee: Clariant Finance (BVI) Limited
    Inventors: Martin Oberholzer, J├╝rgen Geiwiz
  • Publication number: 20080032409
    Abstract: The invention describes fluorescent biomolecule labeling reagents (I-SHark and phI-SHark) and their model compounds. Further described are methods of preparing and using the same.
    Type: Application
    Filed: August 7, 2007
    Publication date: February 7, 2008
    Applicant: California Institute of Technology
    Inventors: Jay R. Winkler, Jennifer C. Lee, Seth B. Harkins, Harry B. Gray
  • Patent number: 7220749
    Abstract: The invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent. The invention also provides novel compositions comprising at least one COX-2 selective inhibitor, that is optionally sitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.
    Type: Grant
    Filed: June 10, 2003
    Date of Patent: May 22, 2007
    Assignee: NitroMed, Inc.
    Inventors: L. Gordon Letts, David S. Garvey
  • Patent number: 7019104
    Abstract: An object of present invention is to provide a diamine and an acid dianhydride having photoreactivity and thermoreactivity and a polyimide composition containing the diamine and the acid dianhydride as monomer components, and specifically to synthesize a diamine and an acid dianhydride having a photoreactive and thermoreactive group containing a double bond or triple bond such as cinnamic acid, chalcone, benzalacetophenone, stilbene, coumarin, pyrone, allyl, propargyl, and acetylene or a derivative skeleton thereof so as to exhibit photoreactivity and thermoreactivity specific to the reactive group, thereby providing a polyimide composition containing the diamine and the acid dianhydride.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: March 28, 2006
    Assignee: Kaneka Corporation
    Inventors: Koji Okada, Shoji Hara, Hitoshi Nojiri
  • Patent number: 6602869
    Abstract: This invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 represents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an aryl or alkyl halogen, R4 represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e. to increase and/or stimulate the growth of said hair.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: August 5, 2003
    Assignee: L'Oreal S.A.
    Inventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
  • Patent number: 6576747
    Abstract: Disclosed is a process for preparing dianthranilate compounds which comprises (a) admixing reactants as follows: (1) a diol of the formula R1(OH)2, wherein R1 is an alkylene group having at least about 20 carbon atoms, and wherein the —OH groups are primary or secondary, (2) isatoic anhydride, present in an amount of at least, about 2 moles of isatoic anhydride per every one mole of diol, (3) a catalyst which is 1,4-diazabicyclo [2.2.2]octane, N,N,N′,N′-tetramethylethylene diamine, or a mixture thereof, said catalyst being present in an amount of at least about 0.
    Type: Grant
    Filed: June 27, 2002
    Date of Patent: June 10, 2003
    Assignee: Xerox Corporation
    Inventors: Rina Carlini, James M. Duff, Stephen G. Robinson, George Liebermann, Roger E. Gaynor, Tania Pereira, Jeffrey H. Banning, James D. Mayo
  • Publication number: 20020019558
    Abstract: The present invention provides a novel diamine and a novel acid anhydride which are applicable for a polyimide and includes a cinnamoyl group or a derived cinnamoyl group. The novel diamines and acid anhydrides have photo-reactivity and heat-reactivity inherent to the cinnamoyl group.
    Type: Application
    Filed: August 17, 2001
    Publication date: February 14, 2002
    Applicant: Kanegafuchi Kagaku Kogyo Kabushiki Kaisha
    Inventors: Kohji Okada, Hitoshi Nojiri
  • Patent number: 6262114
    Abstract: Novel amidinophenol derivatives of formula (IB) and processes for the preparation thereof; compositions containing a compound of formula (IB) as active ingredient useful as antagonists of leukotine B4 and inhibitors of phospholipase A2 and/or trypsin; methods for preventing or treating diseases induced by phospholipase A2 and/or trypsin comprising administering to a patient a compound of formula (IB); and methods for treating diseases induced by leukotine B4 comprising administering to a patient a compound of formula (IB) or a known amidinophenol derivative of formula (IA)
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: July 17, 2001
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hisao Nakai, Koumei Kamiyasu
  • Patent number: 6143734
    Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a compound comprising an enolic anilide non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO.sub.2 group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.
    Type: Grant
    Filed: January 31, 2000
    Date of Patent: November 7, 2000
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Patent number: 6054457
    Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: December 9, 1997
    Date of Patent: April 25, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
  • Patent number: 5985919
    Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: November 16, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Grote, Reinhard Kirstgen, Bernd Muller, Hubert Sauter, Albrecht Harreus, Hartmann Konig, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Franz Rohl
  • Patent number: 5948922
    Abstract: Compounds containing two cyclic hydrocarbon moieties which are substituted to provide crosslinking functionality and which are linked to each other by secondary or tertiary oxycarbonyl containing moiety are basis for compositions which are cured to provide cured thermosets for encapsulation and underfill for electronic components that are thermally decomposable to allow repair, replacement, recovery or recycling of operative electronic components from assemblies that are inoperative.
    Type: Grant
    Filed: February 20, 1997
    Date of Patent: September 7, 1999
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Christopher K. Ober, Hilmar Koerner
  • Patent number: 5885990
    Abstract: Substituted amidinonaphthyl ester compounds effective for treatment of thrombosis are represented by the following formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1## wherein R.sub.1 represents (4,5-dihydro-1H-imidazol-2-yl)amino group, (4,5-dihydro-1,3-thiazol-2-yl)amino group, amidino group, morpholinomethyl group, nitro group, amino group, dimethylamino group, ##STR2## R.sub.3 represents hydrogen, methoxy group, hydroxyl group, acetylamino group, morpholino group, piperidino group, 1-pyrrolidinyl group or dimethylamino group,m represents 0-4,R.sub.4 represents hydrogen or methyl group,R.sub.2 represents NH.sub.2 CO(CH.sub.2).sub.n --, 2-(carbamoyl)vinyl group or R.sub.5 OOC(CH.sub.2).sub.n --,R.sub.5 represents dimethylcarbamoylmethyl group, hydrogen or lower alkyl group, andn represents 0-2.
    Type: Grant
    Filed: June 12, 1997
    Date of Patent: March 23, 1999
    Assignee: Torii Pharmaceutical Co., Ltd.
    Inventors: Toyoo Nakayama, Hiroyuki Kawamura, Hiroyuki Uchiyama
  • Patent number: 5861534
    Abstract: A diaminobenzene derivative of the formula (I): ##STR1## wherein each of P and Q which may be the same or different from each other, is a single bond, or a bivalent organic group selected from the group consisting of --O--, --COO-- and --CONH--, R.sub.1 is a C.sub.2-22 straight chain alkylene group, and R.sub.2 is a cyclic group selected from the group consisting of an aromatic ring, an aliphatic ring, a heterocyclic ring and substituted forms of such rings.
    Type: Grant
    Filed: September 10, 1996
    Date of Patent: January 19, 1999
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Takayasu Nihira, Yoshio Miyamoto, Hideyuki Endo, Toyohiko Abe
  • Patent number: 5783593
    Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: April 29, 1996
    Date of Patent: July 21, 1998
    Assignee: Abbott Laboratories
    Inventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
  • Patent number: 5648513
    Abstract: The invention relates to a method of suppressing human body malodor by utilizing a deodorant composition containing a competitive substrate for the enzymatic creation of axillary body malodor. The compound is present in a dermatologically acceptable vehicle, and in an amount effective to reduce the conversion of malodor producing precursor. The present invention also relates to novel O-acylated serine compounds and method for the production thereof.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: July 15, 1997
    Inventor: Judith Wolfe Laney
  • Patent number: 5639746
    Abstract: The invention provides hydroxamic acid-containing compounds which are useful as inhibitors of matrix metalloproteases and which are effective in treating conditions associated with excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula I ##STR1## wherein (A)R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently selected from various substituents; and(B) where R.sup.3 and R.sup.4 or R.sup.4 and R.sup.5 may together comprise a cyclic moiety; or a pharmaceutically-acceptable salt, biohydrolyzable amide or biohydrolyzable ester thereof.In other aspects, the invention is directed to pharmaceutical compositions containing the compounds of Formula (I), and to methods of treating diseases characterized by matrix metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: June 17, 1997
    Assignee: The Procter & Gamble Company
    Inventor: Kenneth Edward Yelm
  • Patent number: 5527689
    Abstract: The invention relates to a process for the preparation of N-benzyloxycarbonyl-.alpha.-L-aspartyl-L-phenylalanine methyl ester by enzymatic coupling of N-benzyloxycarbonyl-L-aspartic acid and L-phenylalanine methyl ester in an aqueous medium with formation of a precipitate, the coupling reaction being effected with (virtually) equimolar quantities of N-benzyloxycarbonyl-L-aspartic acid and L-phenylalanine methyl ester under the influence of a neutral protease at an initial pH of from 4.5 to 6.0 and in the presence of from 3 to 25%, calculated as per cent by weight based on the total reaction mixture, of an alkali metal salt, alkaline earth metal salt or ammonium salt.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: June 18, 1996
    Assignee: Holland Sweetener Company V.o.F.
    Inventors: Shigeaki Irino, Shin-ichiro Nakamura, Kiyotaka Oyama, Peter J. L. M. Quaedflieg, Theodorus J. G. M. Van Dooren
  • Patent number: 5514794
    Abstract: Derivatized drugs are prepared with a linker consisting of a malonate, wherein the drug is linked through a methylene to the 2-position carbon of the malonate.
    Type: Grant
    Filed: January 22, 1991
    Date of Patent: May 7, 1996
    Assignee: Eli Lilly and Company
    Inventor: Russell L. Barton
  • Patent number: 5453532
    Abstract: A novel crystalline modification of 2-dimethylaminoethyl-n-butylaminobenzoate hydrochloride is characterized by a melting point of 148.6.degree..+-.0.3.degree. C. and has an interplanar spacing d and relative intensities defined herein, and a method for making said crystal. The compound of the invention is has local anaesthetic activity and is an active principle of a pharmaceutical preparation for the eyes.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: September 26, 1995
    Inventor: Nikolai B. Leonidov
  • Patent number: 5424474
    Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphono- and phosphinocarboxylic acids containing hydroxyl and/or mercapto groups, their use as waterproofing and/or oil-repellency agents, and a method for their preparation.
    Type: Grant
    Filed: December 23, 1993
    Date of Patent: June 13, 1995
    Assignee: Bayer AG
    Inventors: Klaus Pohmer, Rainer Weber, Hans-Dieter Block, Hans-Heinrich Moretto
  • Patent number: 5414102
    Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphonocarboxylic acids containing acrylate and/or methacrylate groups, their use as waterproofing or oil-repellency agents, and a method for their preparation.
    Type: Grant
    Filed: December 27, 1993
    Date of Patent: May 9, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Pohmer, Rainer Weber, Hans-Dieter Block, Hans-Heinrich Moretto
  • Patent number: 5403951
    Abstract: A novel crystalline modification of 2-dimethylaminoethyl-n-butylaminobenzoate hydrochloride and a method for production of said compound residing in that a solution of 2-dimethylaminoethyl-n-butylaminobenzoate hydrochloride of polymorphic form in water or organic solvent, or in their mixture, is cooled by a cooling agent at a rate of no less than 8.degree. C./min till complete crystallization of the solution with subsequent drying of obtained crystals.Compound of the invention has a local anaesthetic activity and is an active principle of a pharmaceutical preparation for anaesthesia of eyes (content of active principle is from 0.05 to 0.5% by mass).
    Type: Grant
    Filed: December 22, 1992
    Date of Patent: April 4, 1995
    Inventor: Nikolai B. Leonidov
  • Patent number: 5395853
    Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.
    Type: Grant
    Filed: November 24, 1993
    Date of Patent: March 7, 1995
    Assignee: Burroughs Wellcome Co.
    Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
  • Patent number: 5302743
    Abstract: Disclosed is an improved process for the preparation of an N-protected .alpha.-L-aspartyl-L-phenylalanine methyl ester from an N-protected L-aspartic anhydride and L-phenylalanine methyl ester, the improvement which comprises employing the L-phenylalanine methyl ester in the form of a mineral acid salt thereof and conducting the reaction either (a) in an organic solvent and in the presence of a salt of an organic carboxylic acid, or (b) in an organic solvent comprising an organic carboxylic acid and in the presence of at least one member of the group consisting of an alkali metal or an alkaline earth metal inorganic base, an ammonium alkali metal or alkaline earth metal salt of an organic carboxylic acid and ammonium carbonate. The starting N-protected aspartic anhydride, e.g., N-benzyloxycarbonyl-L-aspartic anhydride, can be produced by the reaction of N-protected aspartic acid with phosgene.
    Type: Grant
    Filed: January 21, 1992
    Date of Patent: April 12, 1994
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Toshio Katoh, Chojiro Higuchi, Takeshi Oura, Masanobu Ajioka, Akihiro Yamaguchi
  • Patent number: 5298647
    Abstract: Aromatic compounds absorbing UVB and/or UVA, substituted with an amide function, selected from the group consisting of ##STR1## whose variable substituents are as defined in the specification, e.g. ##STR2## are useful as photoprotective agents or tanning accelerators.
    Type: Grant
    Filed: December 14, 1987
    Date of Patent: March 29, 1994
    Inventors: Dominique Robert, Louis Jung
  • Patent number: 5290814
    Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, or Ph(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, or R.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, or R.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; X is ##STR2## where A is halogen; Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: March 1, 1994
    Assignee: Burroughs Wellcome Co.
    Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
  • Patent number: 5283258
    Abstract: A procaine acid addition salt, wherein the acid is attached to the diethylamino nitrogen, is complexed with a biologically active organic acid such as a vitamin acid, essential unsaturated fatty acid, C.sub.4 to C.sub.6 hydroxycarboxylic acid or alpha amino acid in stoichiometric ratios of organic acid to procaine acid addition salt to form a double salt complex wherein the organic acid attaches to the p-amino nitrogen. Such double salt complexes protect the procaine molecule from cholinesterase hydrolysis when orally administered to warm blooded animals allowing the complex to be carried intact to the site of damaged cells and across the cell membrane where the double salt complex is disassociated in the cell releasing the organic acid and procaine for cellular repair and regeneration. Procaine hydrochloride is the preferred procaine salt. Preferred acids are citric and vitamin acids including nicotinic acid, ascorbic acid, biotin and folic acid.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: February 1, 1994
    Inventor: Robert Koch
  • Patent number: 5218137
    Abstract: Light activated acyl-enzymes of the formula: ##STR1## are disclosed. In the compounds of Formula (III), ENZ is an enzyme, X is O or S, Y is --NR.sub.3 R.sub.4, --OR.sub.5, or --SR.sub.5, and Z is a nucleophile. m is 0 to 3 and n is 1 or 2. Y is substituted on the ring at either or both of the 4 and 6 position.R.sub.1 and R.sub.2 are each independently H, C1 to C4 alkyl, C3 to C4 unconjugated alkenyl, or C3 to C4 unconjugated alkynyl.R.sub.3 and R.sub.4 are each independently H, C1 to C4 alkyl, C3 to C4 unconjugated alkenyl, or C3 to C4 unconjugated alkynyl, except that R.sub.3 and R.sub.4 are not simultaneously both H. R.sub.5 is C1 to C4 alkyl, C3 to C4 unconjugated alkenyl, or C3 to C4 unconjugated alkynyl.Methods of using the acyl-enzymes and intermediates for making the acyl-enzymes are disclosed.
    Type: Grant
    Filed: March 25, 1992
    Date of Patent: June 8, 1993
    Assignee: Duke University
    Inventors: Ned A. Porter, John D. Bruhnke
  • Patent number: 5102911
    Abstract: HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed.
    Type: Grant
    Filed: July 6, 1990
    Date of Patent: April 7, 1992
    Assignee: Merck & Co, Inc.
    Inventors: Ta J. Lee, Wilbur J. Holtz
  • Patent number: 5087726
    Abstract: This invention relates to novel compounds which are ACAT inhibitors rendering them useful in lowering blood cholesterol levels. The compounds are carbamates represented by the general formula ##STR1## wherein Ar and Ar' represent phenyl or naphthyl each of which may be substituted; m and n each represent zero or one; Z and Y are hydrogen, aliphatic hydrocarbon, heterocyclic, aryl or carbocyclic containing groups.
    Type: Grant
    Filed: February 13, 1990
    Date of Patent: February 11, 1992
    Assignee: Warner-Lambert Company
    Inventors: Patrick M. O'Brien, Drago R. Sliskovic
  • Patent number: 5073641
    Abstract: Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R.sub.1 and R.sub.2 are the same or different and are selected from a group consisting of an alkyl, an alkenyl, an aryl, an aralkyl, a cycloalkyl and which group may be unsubstituted or substituted, or R.sub.1 and R.sub.2 together with the N forms a 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and which heterocyclic group may be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and are highly susceptible to undergoing enzymatic hydrolysis in vivo whereas they are highly stable in aqueous solution.
    Type: Grant
    Filed: April 26, 1988
    Date of Patent: December 17, 1991
    Inventors: Hans Bundgaard, Niels M. Nielsen
  • Patent number: 5001148
    Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.
    Type: Grant
    Filed: June 7, 1989
    Date of Patent: March 19, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey O. Saunders, Eric M. Gordon
  • Patent number: 5001156
    Abstract: Lipophilic quaternary ammonium salicylate, characterized in that it corresponds to the formula: ##STR1## in which: (i) R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote an alkyl or alkylcycloalkyl radical, optionally substituted or interrupted;(ii) R.sub.3 and/or R.sub.4 denote(s) a group:R.sub.8 [OC.sub.2 H.sub.3 R.sub.7 ].sub.n [OCH.sub.2 CHOH--CH.sub.2 ].sub.pin which 0.ltoreq.n.ltoreq.4 and p denotes 0 or 1; R.sub.8 denotes H or an alkyl, alkenyl, alkylcycloalkyl or alkylaryl radical;(iii) R.sub.4 denotes an alkylphenyl radical;(iv), (v) R.sub.1 and R.sub.2 can form a saturated or unsaturated aromatic or non-aromatic heterocycle;(vi) R.sub.1, R.sub.2 and R.sub.3 form polycyclic derivatives with the nitrogen atoms; R.sub.5 denotes a group corresponding to the formula: ##STR2## in which n is an integer varying between 0 and 10.
    Type: Grant
    Filed: December 1, 1987
    Date of Patent: March 19, 1991
    Assignee: L'Oreal
    Inventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
  • Patent number: 4999186
    Abstract: The present invention relates to novel sunscreen agents which have the ability to absorb both UVA and UVB wavelength radiation. The sunscreen agents comprise a specific type of UVA-absorbing chromophore covalently bonded to a specific type of UVB-absorbing chromophore. The chromophore moieties are covalently bonded together such that the electron systems of these moieties are not directly coupled.The present invention further relates to sunscreen compositions containing the hereinbefore described type of sunscreen agents. Furthermore, the present invention relates to methods for protecting the skin of humans or lower animals from the effects of UVA and UVB wavelength radiation. This method comprises topically applying to the skin an effective coating of a sunscreen composition of the present invention.
    Type: Grant
    Filed: June 2, 1987
    Date of Patent: March 12, 1991
    Assignee: The Procter & Gamble Company
    Inventors: Anthony D. Sabatelli, Josephine A. Spirnak
  • Patent number: 4992575
    Abstract: N,N'-dimethyl aromatic diamines are prepared from the corresponding diprimary amines via a two step synthesis forming first the corresponding di-succinylimidomethylamine and then reductively cleaving the succinylimido group. The products are useful, e.g., as epoxy curing agents.
    Type: Grant
    Filed: September 30, 1988
    Date of Patent: February 12, 1991
    Assignee: American Cyanamid Company
    Inventor: Dalip K. Kohli
  • Patent number: 4940813
    Abstract: A process is described for the preparation of an optically active carboxylic acid or ester derivative thereof from a ketene and an optically active .alpha.-hydroxyester or an .alpha.-hydroxy amide.
    Type: Grant
    Filed: March 31, 1989
    Date of Patent: July 10, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Edward G. Corley, Robert D. Larsen, Edward J. J. Grabowski, Paul Reider
  • Patent number: 4937370
    Abstract: The present invention relates to novel chromophore-containing compounds useful as sunscreen agents which have the ability to absorb both UVA and UVB wavelength radiation. These compounds comprise a specific type of UVA-absorbing chromophore covalently bonded to a specific type of UVB-absorbing chromophore. The chromophore moieties are covalently bonded together such that the electron systems of these moieties are directly coupled to thereby form a new chromophore.The present invention further relates to sunscreen compositions containing the hereinbefore described type of sunscreen agents. Furthermore, the present invention relates to methods for protecting the skin or humans or lower animals from the effects of UVA and UVB wavelength radiation. This method comprises topically applying to the skin an effective coating of a sunscreen composition of the present invention.
    Type: Grant
    Filed: June 2, 1987
    Date of Patent: June 26, 1990
    Assignee: The Procter & Gamble Company
    Inventor: Anthony D. Sabatelli