Patents Examined by Alan L. Rotman
  • Patent number: 7235576
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Grant
    Filed: January 11, 2002
    Date of Patent: June 26, 2007
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
  • Patent number: 7223772
    Abstract: The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from the group consisting of H, halogen, C1-6alkyl, C1-6alkoxy, and C1-6alkoxy substituted by one or more fluorine atoms; R2 is selected from the group consisting of H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, and C1-6alkoxy substituted by one or more fluorine atoms; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
    Type: Grant
    Filed: November 1, 1999
    Date of Patent: May 29, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: Ian Baxter Campbell, Alan Naylor
  • Patent number: 7173025
    Abstract: Compounds of formula (I), wherein G1 is CH or N; G2 is CH or N; R1 is a variety of optional substituents; L1 is (1-4C)alkylene; T1 is CH or N; R2 and R3 are independently hydrogen or (1-4C)alkyl or are joined to form a ring; X1 and X2 represent various linking groups; Ar is phenylene or certain heteroaryl rings and Q represents a variety of aromatic or heterocyclic rings systems, and pharmaceutically acceptable salts thereof are described as useful antithrombotic and anticoagulant agents, and are selective Factor Xa inhibitors. Processes for their preparation and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: January 31, 1997
    Date of Patent: February 6, 2007
    Assignee: Zeneca Limited
    Inventors: Andrew Stocker, John Preston, Michael James Smithers
  • Patent number: 7005521
    Abstract: Complexes of a selected class of chiral ligands with molybdenum, tungsten or chromium, preferably molybdenum, are effective as catalysts in highly enantioselective and regioselective alkylation of allylic substrates. Such compositions provide a versatile and low-cost alternative to existing catalysts.
    Type: Grant
    Filed: February 7, 2000
    Date of Patent: February 28, 2006
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Barry M. Trost, Iwao Hachiya
  • Patent number: 6946565
    Abstract: A process for the preparation of methyl 2-(3-chloropropoxy)-indole-3-carboxylate, which comprises reacting a 3-chloro-3-carboxylate indole compound with 3-chloropropanol in the presence of an acid having a pKa of from 0 to 2.
    Type: Grant
    Filed: January 30, 2003
    Date of Patent: September 20, 2005
    Assignee: SmithKline Beecham PLC
    Inventors: Michael Fedouloff, John Bryce Strachan
  • Patent number: 6908928
    Abstract: Crystalline monohydrate of (1?,2?,4?,5?,7?)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: June 21, 2005
    Assignee: BI Pharma KG.
    Inventors: Rolf Banholzer, Peter Sieger, Christian Kulinna, Michael Trunk, Manfred Graulich, Peter Specht, Helmut Meissner, Andreas Mathes
  • Patent number: 6897312
    Abstract: A method for producing ? crystals of ethyl (R)-2-[4-(6-chloro-2-quinoxalin-2-yloxy)phenoxy]propionate, which is characterized by heating ? crystals, or ? crystals and ? crystals, within a range of from 50° C. to lower than the melting point of the ? crystals.
    Type: Grant
    Filed: December 4, 2001
    Date of Patent: May 24, 2005
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Masami Yasukawa, Shinji Kuwahara
  • Patent number: 6878728
    Abstract: The invention provides novel compounds of formula (I) wherein all variables are as defined in the specification, that are useful as inhibitors of aspartyl proteases.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: April 12, 2005
    Assignee: Vertex Pharmaceutical Incorporated
    Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger
  • Patent number: 6875775
    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 5, 2005
    Assignee: Hormos Medical Oy LTD
    Inventors: Marja-Liisa Södervall, Arja Kalapudas, Lauri Kangas, Risto Lammintausta, Pirkko Härkönen, Kalervo Väänänen, Arto Karjalainen
  • Patent number: 6855832
    Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: February 15, 2005
    Assignee: Allergan, Inc.
    Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
  • Patent number: 6849646
    Abstract: The invention relates to compounds having formula (I), wherein R1, R2, R3, R4, R5, R7, R8, R11, Z, m and n have the meaning cited in claim 1, and to the physiologically acceptable salts and solvates which can be used as integrin inhibitors, especially in the prophylaxis and treatment of circulatory diseases, in case of thrombosis, myocardial infarction, coronary heart diseases, arteriosclerosis, osteoporosis, pathologic processes caused or propagated by angiogenesis and in tumor therapy.
    Type: Grant
    Filed: October 14, 1999
    Date of Patent: February 1, 2005
    Assignee: Merck Patent GmbH
    Inventors: Claus Fittschen, Simon Goodman, Joachim März, Peter Raddatz, Matthias Wiesner
  • Patent number: 6838466
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: January 4, 2005
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
  • Patent number: 6831193
    Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: December 14, 2004
    Assignee: Abbott Laboratories
    Inventors: Chih-Hung Lee, Richard J. Perner, Daniel P. Larson, John R. Koenig, Arthur R. Gomtsyan, Guo Zhu Zheng, Stanley DiDomenico, Andrew O. Stewart, Erol K. Bayburt
  • Patent number: 6825181
    Abstract: Aminoisoquinoline derivatives of the following formulae or analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an excellent effect of inhibiting activated blood-coagulation factor X, and they are useful as anticoagulants or agents for preventing or treating thrombi or emboli.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: November 30, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Tadakiyo Nakagawa, Shingo Makino, Kazuyuki Sagi, Masaru Takayanagi, Takashi Kayahara, Shunji Takehana
  • Patent number: 6806275
    Abstract: The present invention provides an arylpiperidine derivative of the formula (I) or a pharmaceutically acceptable salt thereof, which has antipsychotic effect: wherein D is a carbon atom or a nitrogen atom, E is a CH group or a nitrogen atom, G is an oxygen atom, a sulfur atom, a nitrogen atom or an NH group, Y1 is a hydrogen atom or a halogen atom, n is an integer of 1 to 4, and R1 is a group represented by any of the formulas (i) to (iv) defined in the specification.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: October 19, 2004
    Assignees: Nihon Nohyaku Co., Ltd., Taisho Pharmaceutical Co., Ltd.
    Inventors: Masashi Nagamine, Makoto Gotoh, Masanori Yoshida, Atsuro Nakazato, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa
  • Patent number: 6794392
    Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.
    Type: Grant
    Filed: October 13, 1999
    Date of Patent: September 21, 2004
    Assignee: Schering Aktiengesellschaft
    Inventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
  • Patent number: 6794399
    Abstract: The invention disclosed some 1,4-dihydropiridine derivative chemically with guaiacoxypropanolamine based phenoxypropanolamine moiety and pharmacologically with &bgr;-adrenoceptor blocking and partial &bgr;2-agonist activities, is now emerging. The compound of 1,4-dihydropiridine derivative wherein has the formula I, wherein R selected from four group as follow R1 selected from X, H, NO2 saturated C1-C6 alkyl chain, unsaturated C6-C6 alkyl chain, R2 selected from H, CH3 R3 and R4 are individually selected from saturated C1-C6 alkyl chain, unsaturated C1-C6 alkyl chain; R5 selected from OH, saturated C1-C6 alkyl chain, unsaturated C1-C6 alkyl chain.
    Type: Grant
    Filed: April 11, 2002
    Date of Patent: September 21, 2004
    Inventor: Ing-Jun Chen
  • Patent number: 6787528
    Abstract: The compounds of formula (I) are hydrophilic aryl phosphate, thiophosphate, and aminophosphate intestinal apical membrane Na-mediated phosphate co-transportation inhibitors. The compounds can be administered orally, where they act to inhibit Na-dependent phosphate uptake in the intestines, or internally, where they interact with the phosphate control functions of the kidneys and parathyroid. They are therefore useful for inhibiting sodium-mediated phosphate uptake, reducing serum PTH, calcium, calcitriol, and phosphate, and treating renal disease in an animal, including a human.
    Type: Grant
    Filed: January 7, 2002
    Date of Patent: September 7, 2004
    Assignee: Board of Regents, The University of Texas System
    Inventor: Brian E. Peerce
  • Patent number: 6780874
    Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in, which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
    Type: Grant
    Filed: June 10, 2003
    Date of Patent: August 24, 2004
    Assignee: Celltech R & D Limited
    Inventors: Timothy John Norman, John Robert Porter, Brian Woodside Hutchinson, Andrew James Ratcliffe, John Clifford Head, Rikki Peter Alexander, Barry John Langham, Graham John Warrellow, Sarah Catherine Archibald, Janeen Marsha Linsley
  • Patent number: 6777432
    Abstract: A compound of the formula and pharmaceutically acceptable salts thereof, wherein R1 is selected from (R3)C(═O)—N(R4)— and (R3)(R4)N—C(═O)—; R2 is selected from —OR5 and —N(R5)(R6); n is 0, 1, 2 or 3; X is selected from oxygen and sulfur; and R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, heteroalkyl, aryl, aryl(akylene), heteroaryl, heteroaryl(alkylene), carbocycle, carbocycle(alkylene), heterocycle, and heterocycle(alkylene); as well as pharmaceutical compositions containing said compound. The compounds and compositions are useful in, for example, the treatment of inflammatory events in an animal subject.
    Type: Grant
    Filed: September 4, 2002
    Date of Patent: August 17, 2004
    Assignee: Darwin Molecular Corporation
    Inventors: Neil S. Cutshall, Scott C. Jeffrey