Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/371.7)
  • Patent number: 7425630
    Abstract: The present invention relates to processes for preparing pyrazolo[3,4-d]pyrimidine ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: September 16, 2008
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Tawfik Gharbaoui, Dipanjan Sengupta, Edward A. Lally, Naomi S. Kato, Marlon Carlos, Natalie Rodriguez
  • Patent number: 7425640
    Abstract: The present invention provides compounds of formula I wherein X, Y, R1-R7 are as defined herein. Compositions containing these compounds, and methods for inhibiting HCV RNA-dependent RNA polymerase and treating hepatitis C and related disorders using these compounds and compositions are also provided.
    Type: Grant
    Filed: October 26, 2005
    Date of Patent: September 16, 2008
    Assignee: Schering Corporation
    Inventors: Alan B. Cooper, Hugh Y. Zhu, James J-S Wang, Jagdish A. Desai, Gerald W. Shipps, Jr., Patrick J. Curran, D. Allen Annis, Huw M. Nash, Viyyoor M. Girijavallabhan
  • Publication number: 20080214559
    Abstract: Compounds with a combination of cannabinoid CB1 antagonism and serotonin re-uptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed. In at least one embodiment, the invention relates to compounds of the general formula (1); wherein the substitutents have the definitions given in the specification.
    Type: Application
    Filed: January 7, 2008
    Publication date: September 4, 2008
    Inventors: Josephus H.M. Lange, Cornelis G. Kruse
  • Publication number: 20080207725
    Abstract: A compound of formula (I): wherein A represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; and R1 and R2 each independently represent hydrogen, fluorine or chlorine; or a physiologically functional derivative thereof.
    Type: Application
    Filed: June 27, 2006
    Publication date: August 28, 2008
    Inventors: Michael David Barker, David House, Haydn Terence Jones, Simon John Fawcett MacDonald, Iain McFarlane Mclay
  • Publication number: 20080200519
    Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.
    Type: Application
    Filed: February 15, 2008
    Publication date: August 21, 2008
    Inventors: Markus BERGER, Hartmut Rehwinkel, Heike Schacke, Ekkehard May, Werner Skuballa, Hermann Kunzer
  • Publication number: 20080176865
    Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.
    Type: Application
    Filed: December 13, 2007
    Publication date: July 24, 2008
    Applicant: PFIZER LIMITED
    Inventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
  • Patent number: 7399884
    Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen; R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3-12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.
    Type: Grant
    Filed: November 7, 2006
    Date of Patent: July 15, 2008
    Assignee: Takeda San Diego, Inc.
    Inventors: Jerome C. Bressi, Sheldon X. Cao, Jeffrey A. Stafford, Phong H. Vu
  • Publication number: 20080146643
    Abstract: Compounds of formula (I) are used in combination with a second antiparasitic agent for the treatment of parasitic infestations in a host animal.
    Type: Application
    Filed: December 13, 2007
    Publication date: June 19, 2008
    Applicant: PFIZER LIMITED
    Inventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
  • Publication number: 20080103313
    Abstract: The present invention relates to dyes of formula (1) that are soluble in organic solvents, wherein Cat+ is an organic cation, to a process for their preparation and to their use in the production of colored plastics or polymeric color particles, printing colorants, printing pastes and printing inks.
    Type: Application
    Filed: December 19, 2005
    Publication date: May 1, 2008
    Inventors: Thomas Ruch, Ursula Luterbacher
  • Patent number: 7342037
    Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: March 11, 2008
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Peter A. Petillo
  • Patent number: 7329670
    Abstract: The compounds are aryl and heteroaryl substituted heterocyclic ureas of the formula A—NH—C(O)—NH—B where A is the aryl or hetaryl substituted heterocyclic group and B is an aryl or heteroaryl moiety. The compounds inhibit raf kinase and are useful in the treatment of RAF kinase mediated diseases.
    Type: Grant
    Filed: December 27, 1999
    Date of Patent: February 12, 2008
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Jacques Dumas, Uday Khire, Timothy B. Lowinger, Bernard Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, Holia Hatoum-Mokdad, Jeffrey Johnson, Aniko Redman, Robert Sibley
  • Patent number: 7307097
    Abstract: Pyrazole derivatives are described herein. The described invention also includes methods of making such pyrazole derivatives as well as methods of using the same in the treatment of diseases.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: December 11, 2007
    Assignee: SmithKline Beechman Corporation
    Inventors: Jerry Leroy Adams, Jiri Kasparec, Domingos J. Silva
  • Patent number: 7303592
    Abstract: Hair dyeing compositions are provided which comprise at least one coupler selected from N-aryl-m-phenylenediamine derivatives, 2-substituted N-aryl-m-phenylenediamine derivatives, and N-aryl-m-diaminopyridine derivatives, in combination with and at least one diaminopyrazole primary intermediate.
    Type: Grant
    Filed: March 11, 2005
    Date of Patent: December 4, 2007
    Assignee: The Procter & Gamble Company
    Inventors: Mu'lll Lim, Guiru Zhang, Bryan Patrick Murphy
  • Patent number: 7271191
    Abstract: The compounds of formula I: inhibit gamma secretase and hence are of utility in the treatment or prevention of Alzheimer's Disease.
    Type: Grant
    Filed: April 1, 2004
    Date of Patent: September 18, 2007
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Michela Bettati, Mark Stuart Chambers, Peter Alan Hunt, Philip Jones, Angus Murray MacLeod, Helen Jane Szekeres, Martin Richard Teall
  • Patent number: 7268235
    Abstract: A method for the preparation of N-pyrazolylamidoximes of the general formula I R1 and R2 independently represent an alkyl, aryl, or heteroaryl group, comprises reacting a 5-(?-ketoalkyl)-3-substituted-1,2,4-oxadiazoles of the general formula II with hydrazine.
    Type: Grant
    Filed: September 30, 2004
    Date of Patent: September 11, 2007
    Assignee: Eastman Kodak Company
    Inventors: Francesco DeBellis, Alice J. Kim, legal representative, Chang-Kyu Kim, deceased
  • Patent number: 7244757
    Abstract: The present invention relates to compounds of the Formula wherein R1, R3, R4, R5, R6, R7 and R8 are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods of treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.
    Type: Grant
    Filed: March 11, 2005
    Date of Patent: July 17, 2007
    Assignee: Pfizer Inc
    Inventors: Yuhpyng L. Chen, Lei Zhang
  • Patent number: 7202257
    Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.
    Type: Grant
    Filed: July 6, 2004
    Date of Patent: April 10, 2007
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Peter A. Petillo
  • Patent number: 7183306
    Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.
    Type: Grant
    Filed: November 14, 2003
    Date of Patent: February 27, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Fumiyuki Shirai, Hidenori Azami, Natsuko Kayakiri, Kazuo Okumura, Katsuya Nakamura
  • Patent number: 7176210
    Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein
    Type: Grant
    Filed: January 21, 2004
    Date of Patent: February 13, 2007
    Assignee: Pfizer Inc.
    Inventor: David A. Griffith
  • Patent number: 7154002
    Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen; R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3–12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.
    Type: Grant
    Filed: October 7, 2003
    Date of Patent: December 26, 2006
    Assignee: Takeda San Diego, Inc.
    Inventors: Jerome C. Bressi, Sheldon X. Cao, Jeffrey A. Stafford, Phong H. Vu
  • Patent number: 7144911
    Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.
    Type: Grant
    Filed: December 24, 2003
    Date of Patent: December 5, 2006
    Assignee: Deciphera Pharmaceuticals LLC
    Inventors: Daniel L. Flynn, Peter A. Petillo
  • Patent number: 7091350
    Abstract: The invention relates to diaminopyrazole derivatives having the following structure (I), wherein R1 represents an alkyl or alkenyl radical bearing at least one substituent selected from among OR, NRR?, SR, SOR, SO2R, COOR, CONRR?, PO(OH)2, SO3X, NHCONRR, a non-cationic heterocycle, an aryl, a halogen. R2 and R3 are different from H and represent, independently of each other, an alkyl or alkenyl group; R2 and R3, together with the nitrogen atom to which they are attached, can form a heterocycle possibly comprising at least one other heteroatom selected from among N, O and S; R2 and R3 or the heterocycle that they form with the nitrogen to which they are attached can be substituted by at least one substituent defined above.
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: August 15, 2006
    Assignee: L'Oreal
    Inventors: Thilo Fessmann, Eric Terranova
  • Patent number: 7060718
    Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: March 11, 2003
    Date of Patent: June 13, 2006
    Assignee: Amgen Inc.
    Inventor: Jonathan B. Houze
  • Patent number: 7001905
    Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: February 21, 2006
    Assignee: Warner-Lambert Company
    Inventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
  • Patent number: 6974829
    Abstract: This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting ?-amyloid peptide release and/or synthesis, a method for inhibiting ?-secretase activity and a method for treating neurological disorders associated with ?-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.
    Type: Grant
    Filed: May 7, 2003
    Date of Patent: December 13, 2005
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Jay S. Tung, Ashley C. Guinn, Eugene D. Thorsett, Michael A. Pleiss
  • Patent number: 6962915
    Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts or prodrugs thereof, are useful as kinase inhibitors, wherein Y is —C(?O)NR1—, —NR1C(?O)—, —NR1C(?O)NR1—, —NR1SO2—, —SO2NR1—, —C(?O)—, —OC(?O)—, or —CO2—; B is alkyl, substituted alkyl, alkenyl, substituted alkenyl, hydroxy, alkoxy, aryl, cycloalkyl, heteroaryl, and heterocyclo; or when Y is —C(?O)NR1—, B also may be selected from —C(?O)R8, —C(?O)NR8R9, and —CO2R8; R1 is hydrogen, C1-4alkyl, or substituted C1-4alkyl; R2 is hydrogen or C1-4alkyl; R3 is hydrogen, methyl, perfluoromethyl, hydroxy, methoxy, halogen, cyano, NH2, or NH(CH3); and R4, R5, R6, R7, R8, and R9 are as defined in the specification.
    Type: Grant
    Filed: May 19, 2003
    Date of Patent: November 8, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Chunjian Liu, Robert V. Moquin, Katerina Leftheris
  • Patent number: 6960661
    Abstract: [7-(3-chloro-4-methoxybenzylamino)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-ylmethoxy]acetic acid, is disclosed, as well as a process for its preperation and intermediates in the process of preparing the same.
    Type: Grant
    Filed: December 29, 2001
    Date of Patent: November 1, 2005
    Assignee: Merck Patent GmbH
    Inventor: Hans-Michael Eggenweiler
  • Patent number: 6949578
    Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.
    Type: Grant
    Filed: July 14, 2004
    Date of Patent: September 27, 2005
    Assignee: Pharmacia Corporation
    Inventors: Ish Kumar Khanna, Michael Clare, Alan F. Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu
  • Patent number: 6919462
    Abstract: A process for preparing pesticides or pesticidal intermediates, particularly 5-amino-1 aryl-3-cyanopyrazoles, having the formula said process comprising reacting a compound having the formula with a cyanide salt.
    Type: Grant
    Filed: July 18, 2003
    Date of Patent: July 19, 2005
    Assignee: BASF Agro B.V., Amhem (NL) - Wadenswil Branch
    Inventor: Jean-Erick Ancel
  • Patent number: 6916924
    Abstract: This invention relates to novel processes for preparing heteroaryl-substituted urea compounds of formula (I): which are useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. X, Ar, L, Q and are described herein.
    Type: Grant
    Filed: February 12, 2002
    Date of Patent: July 12, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Zhulin Tan, Jinhua J. Song
  • Patent number: 6887280
    Abstract: Novel compositions for use in oxidative hair coloring compositions are provided. The compositions comprise one or more oxidative hair coloring N-aryl-m-phenyldiamine derivatives as couplers and one or more diaminopyrazole primary intermediates in combination.
    Type: Grant
    Filed: March 4, 2002
    Date of Patent: May 3, 2005
    Assignee: The Procter & Gamble Company
    Inventors: Mu-Ill Lim, Yuh-Guo Pan, Sabina Burdzovic
  • Patent number: 6881735
    Abstract: The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.
    Type: Grant
    Filed: November 28, 2001
    Date of Patent: April 19, 2005
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel
  • Patent number: 6852717
    Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: February 8, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, John Robinson Regan
  • Patent number: 6838458
    Abstract: The present invention relates to 5-(alkylidene-cycloalkyl)-pyrazoles and 5-(alkylidene-heterocyclyl)-pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, ring G, R1 through R7 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.
    Type: Grant
    Filed: November 1, 2002
    Date of Patent: January 4, 2005
    Assignee: Pfizer, Inc.
    Inventor: Subas M. Sakya
  • Publication number: 20040198986
    Abstract: Pyrazole derivatives are described herein. The described invention also includes methods of making such pyrazole derivatives as well as methods of using the same in the treatment of diseases.
    Type: Application
    Filed: March 26, 2004
    Publication date: October 7, 2004
    Inventors: Jerry Leroy Adams, Jiri Kasparec, Domingo J Silva
  • Patent number: 6706711
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein R1, R2, T, n and Q are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases, such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: March 16, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: Michael R. Hale
  • Publication number: 20040029883
    Abstract: The present invention relates to compounds of general formula (I), wherein the residues R represent organic radicals, X represents a bond, oxygen or —NR12 and Y represents oxygen or sulfur, processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory, autoimmune and immune diseases.
    Type: Application
    Filed: November 19, 2002
    Publication date: February 12, 2004
    Inventors: Markus Albers, Thomas Lehmann, Thomas Rlle, Gerhard Mller, Gerhard Hessler, Masaomi Tajimi, Karl Ziegelbauer, Hiromi Okigami, Haruki Hasegawa
  • Patent number: 6686318
    Abstract: The invention relates to new substituted aromatic amino compounds of the general formula (I) in which R1, R2, R3, R4 and Z have the meanings given in the description, to a process for their preparation, and to their use as herbicides.
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: February 3, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Kurt Findeisen, Joachim Kluth, Karl-Heinz Linker, Klaus-Helmut Müller, Otto Schallner, Markus Dollinger
  • Patent number: 6677335
    Abstract: Compounds of the formula (I): wherein R1, R2, R4 and R13 are as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a pharmaceutically or veterinarily acceptable solvate or pro-drug thereof: are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: January 13, 2004
    Assignee: Pfizer Inc
    Inventors: Mark Edward Bunnage, Keith Michael DeVries, Laurence James Harris, Philip Charles Levett, John Paul Mathias, Joanna Teresa Negri, Stephen Derek Albert Street, Albert Shaw Wood
  • Patent number: 6677353
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 13, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Publication number: 20030232865
    Abstract: Disclosed are 1,4-disubstituted benzo-fused urea compounds of formula (I): 1
    Type: Application
    Filed: February 19, 2003
    Publication date: December 18, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, John Robinson Regan
  • Patent number: 6660732
    Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: September 25, 2001
    Date of Patent: December 9, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashehar Betageri, Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, Thomas M. Kirrane, Monica H. Moriak, Neil Moss, Usha R. Patel, John R. Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi
  • Patent number: 6660046
    Abstract: The invention concerns novel pyrazole derivatives comprising at least a cationic group Z, Z being selected among the quaternized aliphatic chains, aliphatic chains comprising at least a saturated quaternized cycle, and aliphatic chains comprising at least an unsaturated quaternized cycle, their use as oxidation base for dyeing keratin fibres, dyeing compositions containing them, and dyeing methods using them.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: December 9, 2003
    Assignee: L'Oreal S.A.
    Inventors: Eric Terranova, Alain Lagrange
  • Patent number: 6656933
    Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: September 25, 2001
    Date of Patent: December 2, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Eugene R. Hickey
  • Patent number: 6645258
    Abstract: The invention relates to novel compositions for the oxidation dyeing of keratin fibers, comprising at least one specific diaminopyrazole derivative, to the dyeing process using this composition, to novel diaminopyrazole derivatives and to a process for their preparation.
    Type: Grant
    Filed: October 18, 2001
    Date of Patent: November 11, 2003
    Assignee: L'Oreal, S.A.
    Inventors: Laurent Vidal, Agnès Burande, Gérard Malle, Michel Hocquaux
  • Patent number: 6620944
    Abstract: A process for preparing pesticides or pesticidal intermediates, particularly 5-amino-1 aryl-3-cyanopyrazoles, having the formula said process comprising reacting a compound having the formula with a cyanide salt.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: September 16, 2003
    Assignee: Aventis CropScience S.A.
    Inventor: Jean-Erick Ancel
  • Patent number: 6608077
    Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: August 19, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Qi Jin
  • Patent number: 6600050
    Abstract: Diaminopyrazole derivatives of the general Formula (I) or their physiological tolerated, water-soluble salts with inorganic or organic acids, and agents, containing these compounds, for the oxidative dyeing of fibers.
    Type: Grant
    Filed: September 9, 2002
    Date of Patent: July 29, 2003
    Assignee: Wella AG
    Inventors: Laurent Chassot, Hans-Juergen Braun
  • Patent number: 6596878
    Abstract: The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.
    Type: Grant
    Filed: September 18, 2001
    Date of Patent: July 22, 2003
    Assignees: Yissum Research & Development Company of the Hebrew University, Sugen, Inc.
    Inventors: Hui Chen, Aviv Gazit, Alexander Levitzki, Klaus Peter Hirth, Elaina Mann, Laura K. Shawver, Jianming Tsai, Peng Cho Tang
  • Patent number: 6596863
    Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formula
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: July 22, 2003
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo