Abstract: A compound of the formula:
[wherein R1 is a hydrocarbon group which may be substituted;
R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted;
R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group;
R4 is hydrogen atoms or a hydroxy group;
n is 0 or 1; and
p is 0 or 1 to 4];
or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.
Abstract: A serotonin reuptake inhibitor containing a cyclic amine represented by the following formula, a prodrug thereof, or a pharmaceutically acceptable salt of said cyclic amine or prodrug as an active ingredient:
wherein R0 is a hydrogen atom, a halogen atom, an alkyl group, a substituted alkyl group, a hydroxyl group, an alkoxy group or the like, R3 is a hydrogen atom or the like, Y is an alkylene group or the like, Z is a hydrogen atom, a cycloalkyl group, an aryl group or the like, n is 1, 2 or 3, and m is 2, 3, 4, 5 or 6.
Type:
Grant
Filed:
January 17, 2003
Date of Patent:
September 7, 2004
Assignee:
Sumitomo Pharmaceuticals Company Limited
Inventors:
Toru Kodo, Shuji Masumoto, Koji Koyama, Naoya Kinomura
Abstract: The present invention relates to a process for preparing perfluoroalkylanilines and to their use for preparing active ingredients, in particular for agrochemicals.
Abstract: Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.
Type:
Grant
Filed:
December 3, 2002
Date of Patent:
July 13, 2004
Assignee:
Novo Nordisk A/S
Inventors:
Janos Tibor Kodra, Peter Madsen, Jesper Lau, Anker Steen Jorgensen, Inge Thoger Christensen
Abstract: Hindered amine compounds which are substituted by a long hydrocarbon chain are useful in a number of applications where the solubility or compatibility afforded by said substitution is needed. This is seen particularly for example with white, dyed, dipped, unscented and/or scanted candle wax which is effectively stabilized against discoloration and fading by the incorporation therein of a long chain hindered amine alone or in combination with a UV absorber and/or an antioxidant.
Type:
Grant
Filed:
September 6, 2002
Date of Patent:
June 29, 2004
Assignee:
Ciba Specialty Chemicals Corporation
Inventors:
Mervin G. Wood, Andrea R. Smith, James P. Galbo
Abstract: This invention discloses a process for synthesizing an amine functionalized monomer that comprises (1) reacting a secondary amine with a 2,3-dihalopropene to produce a vinyl halide containing secondary amine having a structural formula selected from the group consisting of 1
Type:
Application
Filed:
December 9, 2003
Publication date:
June 24, 2004
Applicant:
The Goodyear Tire & Rubber Company
Inventors:
Adel Farhan Halasa, Wein-Liang Hsu, Jin-Ping Zhou, Chad Aaron Jasiunas, Corey Stanton Yon
Abstract: This invention provides 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.
Type:
Application
Filed:
October 29, 2003
Publication date:
June 24, 2004
Inventors:
Mathai Mammen, Richard Wilson, Yan Chen, Sarah Dunham, Adam Hughes, Craig Husfeld, Yu-Hua Ji, Li Li, Trevor Mischki, Ioanna Stergiades
Abstract: The present invention relates to vulcanization accelerators constituted by compounds, derived from secondary amines, belonging to the class of enamines and to a process for their preparation.
Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I;
wherein X, Y, Z, D and R3 are as defined in the specification.
Abstract: Disclosed is a compound represented by Structural Formula (I):
R1 is a substituted or unsubstituted 2-imidazolyl group which is optionally fused to a substituted or unsubstituted aryl group.
Z1 is ═O, ═S, ═NOR11, or ═NR11.
R is represented by a Structural Formula selected from (II)-(VII):
The variables in Structural Formulas (II)-(VII) are described below.
Abstract: Vinylic hindered amine light stabilizers as novel polylmerizable light stabilizers are disclosed and have the general formula (I):
wherein:
R1 is C1 to C8: alkyl, alkoxy, alkyl phenyl, hydroxy alkyl (all linear and branched), allyl, acyl, cycloalkyl (cyclopentyl, cyclohexyl or curnyl: linear and branched); R2 is hydrogen and methyl, R3 is vinyl, C1-C4 vinyl alkyl [H2C═C(R4)C1-C4], R4 is H, C1-C4 alky and alkyl phenyl and R5 is H, C1-C4 alkyl, X is O, NH, C1-C8 alkyloxy and alkylamino: (linear or branched).
Type:
Grant
Filed:
February 22, 2001
Date of Patent:
May 18, 2004
Assignee:
Council of Scientific and Industrial Research
Inventors:
Shrojal Mohitkumar Desai, Raj Pal Singh
Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII):
useful in treating Alzheimer's disease and other similar diseases.
Type:
Grant
Filed:
March 23, 2001
Date of Patent:
May 18, 2004
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.
Type:
Grant
Filed:
February 13, 2003
Date of Patent:
May 4, 2004
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
Abstract: A compound of the structure
A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1(vascular cell adhesion molecule-1) and fibronectin; pharmaceutically active compositions comprising these compounds; and the use of these compounds for the control or prevention of diseases states in which &agr;4&bgr;1 is involved are also disclosed.
Type:
Grant
Filed:
October 9, 2001
Date of Patent:
April 20, 2004
Assignee:
Texas Biotechnology Corporation
Inventors:
Ronald J. Biediger, Brian Dupre, Linda K. Hamaker, George W. Holland, Jamal M. Kassir, Wen Li, Robert V. Market, Noel Nguyen, Ian L. Scott, Chengde Wu, E. Radford Decker
Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula:
wherein R1 and R2 , which are the same or different are
a) H, halogen, OCH3, OH; or
where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H,
—CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or
c) —Y—(CH2)nCH2—O—R6
where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or
d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and
R3 is H, halogen, OH or —OCH3;
stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.
Type:
Grant
Filed:
April 8, 2003
Date of Patent:
April 20, 2004
Assignee:
Hormos Medical Oy Ltd
Inventors:
Marja-Liisa Södervall, Arja Kalapudas, Lauri Kangas, Risto Lammintausta, Pirkko Härkönen, Kalervo Väänänen
Abstract: This invention discloses a rubbery polymer which is comprised of repeat units that are derived from (1) at least one conjugated diolefin monomer, and (2) at least one functionalized monomer having of the structural formula: 1
Type:
Application
Filed:
June 30, 2003
Publication date:
April 1, 2004
Inventors:
Stephan Rodewald, Steven Kristofer Henning, Brian Earl Burkhart
Abstract: The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group. X is O or S, preferably O.R1 is hydrogen or a C1-C6-alkyl group, preferably H.R2 is hydrogen, —COOR3, —CONR3R3′, OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.
Type:
Application
Filed:
September 8, 2003
Publication date:
March 18, 2004
Inventors:
Serge Halazy, Dennis Church, Stephen J. Arkinstall, Marco Biamonte, Montserrat Camps, Jean-Pierre Gotteland, Thomas Rueckle
Abstract: The present invention relates to a biphenylamidine derivative of the general formula (1):
or a pharmaceutically acceptable salt thereof, which is a novel compound functioning as a clinically applicable FXa inhibitor.
Abstract: A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca2+ overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I):
wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH2)n— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.
Abstract: Compounds used for treating dependence on or withdrawal from a drug of abuse, for an eating disorder or for a CNS disease or pathology having the following formulas:
Type:
Grant
Filed:
June 7, 2002
Date of Patent:
March 9, 2004
Assignee:
University of Kentucky Research Foundation
Inventors:
Peter A. Crooks, Linda Dwoskin, Dennis Keith Miller, Vladimir P. Grinevich, Seth Davin Norrholm, Guangrong Zheng
Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.
Type:
Grant
Filed:
August 25, 2000
Date of Patent:
February 17, 2004
Assignee:
Theravance, Inc.
Inventors:
James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1):
wherein Y is CH or N and Z is H, OCH3, NH2 and alkyl of from 1 to 4 carbon atoms, with the proviso that when Y is N the 2,4-diaminophenoxy moieties are positioned at the 4 and 6 positions on the pyrimidine ring.
Type:
Grant
Filed:
January 18, 2002
Date of Patent:
February 17, 2004
Assignee:
The Procter & Gamble Company
Inventors:
Mu-III Lim, Yuh-Guo Pan, James S. Anderson
Abstract: The invention relates to methods of synthesizing libraries of diverse and complex highly substituted 2,4-dioxopiperidine compounds of the general formula:
wherein R1, R2 and R3 are as herein described, novel intermediates useful for synthesizing such 2,4-dioxopiperidine compounds and methods for identifying and isolating the compounds.
Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula:
wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
Type:
Grant
Filed:
October 4, 2002
Date of Patent:
January 27, 2004
Assignee:
Hoffman-La Roche Inc.
Inventors:
Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
Abstract: The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.
Type:
Grant
Filed:
February 28, 2002
Date of Patent:
January 13, 2004
Assignees:
President and Fellows of Harvard College, Organix, Inc.
Abstract: A medicinal composition containing one or more compounds selected from the compounds represented by the following formula (I), salts of these compounds, solvates of these compounds and solvates of these salts and being capable of reducing the contact of the compounds with the components in the bile or pancreatic juice.
Abstract: A substituted aminomethyl-phenyl-cyclohexane derivative of formula I or Ia,
and their a diastereomer, enantiomer, or of a salt formed with a physiologically tolerated acid. Also disclosed are method for preparing the substituted aminomethyl-phenyl-cyclohexane derivative, pharmaceutical compositions comprising the same and method of using the same for treating pain, urinary incontinence, itching, diarrhea, inflammatory and allergic reactions, depression, drug or alcohol abuse, gastritis, cardiovascular diseases, respiratory tract diseases, coughing, mental illnesses and epilepsy.
Type:
Grant
Filed:
July 5, 2002
Date of Patent:
January 6, 2004
Assignee:
Gruenenthal GmbH
Inventors:
Claudia Puetz, Wolfgang Strassburger, Babette-Yvonne Koegel
Abstract: The invention relates to new compounds of formula I
or the pharmaceutically acceptable salts thereof,
wherein
R1, R2, R3, R4, X and Ar1 have the meanings given in the specification, as well as the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
Type:
Grant
Filed:
October 16, 2001
Date of Patent:
December 16, 2003
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Horst Dollinger, Franz Esser, Birgit Jung, Gerd Schnorrenberg, Kurt Schromm, Georg Speck
Abstract: The present invention provides certain sulfonamide derivatives useful for potentiating glutamate receptor function in a patient and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
Type:
Application
Filed:
August 15, 2002
Publication date:
December 4, 2003
Inventors:
Joshua Zwick Davison, Winton Dennis Jones, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.
Type:
Application
Filed:
February 6, 2003
Publication date:
November 27, 2003
Inventors:
Simon Bailey, Elisabeth C. L. Gautier, Alan J. Henderson, Thomas V. Magee, Anthony Marfat, John P. Mathias, Dale G. McLeod, Sandra M. Monaghan, Blanda L. C. Stammen
Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
Type:
Grant
Filed:
July 28, 2000
Date of Patent:
November 25, 2003
Assignee:
Telik, Inc.
Inventors:
Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
Abstract: Described are piperidines of Formula I
and pharmaceutically acceptable salts thereof. The compounds of Formula I are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, central nervous system disorders, depression, trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, pain, especially chronic pain, neuropathic pain, or surgical pain, or urinary incontinence.
Type:
Grant
Filed:
November 30, 2001
Date of Patent:
November 4, 2003
Assignee:
Warner-Lambert Company LLC
Inventors:
Brian Edward Kornberg, Russell Andrew Lewthwaite, David Manning, Sham Shridhar Nikam, Ian Leslie Scott
Abstract: This invention encompasses a method for the treatment or prevention of prostaglandin mediated diseases comprising administering to a mammalian patient a compound of formula I:
in an amount that is effective to treat or prevent said prostaglandin mediated disease. Novel compounds are also disclosed.
Type:
Grant
Filed:
April 24, 2001
Date of Patent:
September 30, 2003
Inventors:
Michel Gallant, Nicolas Lachance, Marc Labelle, Robert Zamboni, Helene Juteau, Yves Gareau, Patrick Lacombe
Abstract: The present invention provides a process for the preparation of amine oxide by reacting a tertiary or a secondary amine with hydrogen peroxide as an oxidant in the presence of a recyclable heterogeneous catalyst comprising a layered double hydroxide exchanged with an anion in the presence of an additive selected from the group consisting of benzonitrile, propionitrile, isobutyronitrile, benzamide and isobutyraride.
Type:
Grant
Filed:
March 28, 2002
Date of Patent:
September 9, 2003
Assignee:
Council of Scientific and Industrial Research
Abstract: Unsaturated 1-Amino-alkylcyclohexane compounds which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.
Type:
Application
Filed:
November 6, 2002
Publication date:
September 4, 2003
Inventors:
Markus Henrich, Wojciech Danysz, Christopher Graham Raphael Parsons, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons, Markus Gold
Abstract: Novel quaternary ammonium compounds of the formula 1
Type:
Application
Filed:
October 25, 2002
Publication date:
August 21, 2003
Inventors:
Ivan Richards, Sue K. Cammarata, Craig D. Wegner, Michael Hawley, Mark Peter Warchol, Mark Kontny, Walter Morozowich, Karen Patrice Kolbasa, Malcolm Wilson Moon, Dominique Bonafoux, Sergey Gregory Wolfson, Patrick James Lennon
Abstract: Compounds and methods are provided for the alleviation or treatment of diseases or conditions in which modification of muscarinic m1 receptor activity has a beneficial effect. In the method, a therapeutically effective amount of a selective muscarinic m1 agonist compound is administered to a patient in need of such treatment.
Type:
Application
Filed:
January 7, 2003
Publication date:
July 31, 2003
Inventors:
Mark Brann, Terri Messier, Erika Currier, Kate Duggento, Tracy Spalding, Mikael Friberg, Niels Skjaerbaek
Abstract: An image forming material includes an image forming layer containing a water-insoluble and alkali-soluble resin, a light-heat converting agent and a compound represented by the following general formula (1). In general formula (1), R1 to R3 independently represent an organic group, where R1 represents a residue forming a ring containing a N1 atom, R2 and R3 may bond to each other to form a ring or at least one of R2 and R3 may bond to R1 to form a ring and X− represents a conjugate base of an organic acid or inorganic acid. The ring containing the N1 atom is preferably a piperidine ring.
Abstract: Disclosed are a method for producing racemic piperidine derivatives by processing optically-active piperidine derivatives in a hydrogen atmosphere in the presence of a reducing catalyst; and a method for producing optically-active piperidine derivatives or their acid salts by optically resolving the racemic piperidine derivatives obtained in the former method.
Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula:
wherein R1 and R2, which are the same or different are
a) H, halogen, OCH3, OH; or
where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or
c) —Y—(CH2)nCH2—O—R6
where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or
d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and
R3 is H, halogen, OH or —OCH3;
stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.
Type:
Grant
Filed:
November 15, 2000
Date of Patent:
June 10, 2003
Assignee:
Hormos Medical Oy Ltd
Inventors:
Marja-Liisa Södervall, Arja Kalapudas, Lauri Kangas, Risto Lammintausta, Pirkko Härkönen, Kalervo V{umlaut over (aa)}nänen
Abstract: Disclosed are compounds of the formula:
and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein.
These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.
Type:
Grant
Filed:
July 6, 2001
Date of Patent:
May 27, 2003
Assignee:
Neurogen Corporation
Inventors:
Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
Abstract: 1 The present invention provides a process for preparing a compound of formula (I), wherein R represents C1-C4 alkyl; and X represents an alkyl, alkenyl, cycloalkyl, aryl, substituted aryl, heterocycle, or substituted heterocycle, comprising treating a compound of formula (II), with a suitable crown ether and a suitable base followed by addition of a compound of formula R−M+ wherein M+ is a suitable cation.
Type:
Application
Filed:
September 9, 2002
Publication date:
May 15, 2003
Inventors:
Marvin Martin Hansen, Perry Clark Heath, Sandra Sabol Keast