Two Double Bonds Between Ring Members Of The Diazole Ring (i.e., Pyrazole) Patents (Class 548/373.1)
  • Patent number: 6610726
    Abstract: The invention is directed to pharmaceutical compositions containing small organic molecules having the ability to mimic or agonize hepatocyte growth factor/scatter factor (HGF/SF) activity, useful for promoting, for example, vascularization of tissues or organs for promoting wound or tissue healing, or augmenting or restoring blood flow to ischemic tissues such as the heart following myocardial infarction.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: August 26, 2003
    Assignee: North Shore-Long Island Jewish Research Institute
    Inventors: Sivaram Pillarisetti, Itzhak D. Goldberg
  • Patent number: 6608095
    Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: August 19, 2003
    Assignee: Pfizer Inc.
    Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
  • Patent number: 6599926
    Abstract: The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: July 29, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Donald J. P. Pinto, Mimi L. Quan, Francis J. Woerner
  • Patent number: 6555690
    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: May 8, 2002
    Date of Patent: April 29, 2003
    Assignee: Allergan, Inc.
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Publication number: 20020173662
    Abstract: Compounds of formula (I): 1
    Type: Application
    Filed: April 29, 2002
    Publication date: November 21, 2002
    Inventor: Bernard Joseph Banks
  • Patent number: 6465646
    Abstract: Compounds of Formula 1 and of Formula 2 where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid negative hormone like biological activity.
    Type: Grant
    Filed: August 4, 2000
    Date of Patent: October 15, 2002
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
  • Patent number: 6465647
    Abstract: Compounds of the Formula 1, Formula 2, Formula 3 and Formula 4 wherein the symbols have the meaning assigned to them in the disclosure have retinoid-like biological activity.
    Type: Grant
    Filed: August 4, 2000
    Date of Patent: October 15, 2002
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
  • Publication number: 20020128263
    Abstract: This invention relates to a compound and the use of the compound of the formula 1
    Type: Application
    Filed: November 28, 2001
    Publication date: September 12, 2002
    Inventors: Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
  • Patent number: 6444662
    Abstract: Described are salts of hyperforin and adhyperforin of formula I [A−]m[B]p+  (I) wherein m is an integer from 1 to 3, p is equal to m and gives the total number of positive charges of the residue [B], [A−] is an anion of formula II with n=0 or 1 and [B]p+ is an ion of an alkali metal or an ammonium ion of a salt-forming nitrogen base of formula III wherein R1 through R4 have a variety of meanings including hydrogen, alkyl, cycloalkyl and similar groups which in turn may be substituted with one or more substituents. The salts serve inter alia for enriching or purifying hyperforin and adhyperforin from St. John's Wort extracts. Pharmaceutical preparations containing the salts are used for treating Alzheimer's Disease.
    Type: Grant
    Filed: August 11, 2000
    Date of Patent: September 3, 2002
    Assignee: Willmar Schwabe GmbH & Co.
    Inventors: Shyam Sunder Chatterjee, Clemens Erdelmeier, Klaus Klessing, Dieter Marme, Christoph Schächtele
  • Patent number: 6414011
    Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: July 2, 2002
    Assignee: Euro-Celtique S.A.
    Inventors: Derk Hogenkamp, Ravindra Upasani, Phong Nguyen
  • Patent number: 6407238
    Abstract: Disclosed is a process of making substituted pyrazoles from substituted benzophenone hydrazones with a variety of 1,3-bifunctional substrates under acid conditions. The pyrazole compounds are useful for making pharmaceutical compounds.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: June 18, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: James A. Baron, Vittorio Farina, Nizar Haddad
  • Patent number: 6395724
    Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.
    Type: Grant
    Filed: June 7, 1999
    Date of Patent: May 28, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: J. Kevin Judice, Deborah L. Higgins, John H. Griffin
  • Patent number: 6392048
    Abstract: The present invention provides a process for preparing carbocyclic or heterocyclic nitrites by the vapor phase contact ammoxidation of carbocyclic compounds or heterocyclic compounds, in which the reaction is carried out effectively without the increase of the amount of ammonia or oxygen used or the introduction of steam to give the nitrites as the objective products stably with the passage of time in a high yield with a high selectivity.
    Type: Grant
    Filed: July 31, 2000
    Date of Patent: May 21, 2002
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Yutaka Sasaki, Hiroshi Utsumi, Akimitsu Morii, Kazuo Morishita
  • Patent number: 6380393
    Abstract: Compositions including at least one organic ligand including a first hetero atom and a second hetero atom directly bonded to the first hetero atom or located one carbon atom away from the first hetero atom, with at least one of the hetero atoms being nitrogen, and a transition metal moiety partially complexes by the organic ligand are provided. Such complexes have a controlled adaptable proton transfer ability and/or a hydrogen bonding ability which makes such compositions particularly useful as chemical reaction facilitators. Examples of chemical reactions facilitated by such compositions include hydrolysis reactions and carbon dioxide conversion reactions.
    Type: Grant
    Filed: March 19, 1999
    Date of Patent: April 30, 2002
    Assignee: San Diego State University Foundation
    Inventors: Douglas Bryan Grotjahn, David Combs
  • Patent number: 6372693
    Abstract: The invention relates to 2-(3-alkenylbenzoyl)cyclohexane-1,3-diones of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR6, —OCOR7, —OSO2R7, —SH, —S(O)nR8, —SO2OR6, —SO2NR6R9, —NR9SO2R7 or —NR9COR7; R3 is hydrogen, halogen, alkyl, haloalkyl, alkoxy, alkenyl, alkynyl; R4, R5 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, alkoxy, alkylthio, haloalkoxy, —COR10, —CO2R10, —COSR10, —CONR10R11, —C(R12)═NR13, —PO(OR10)(OR11); unsubstituted or substituted alkyl, heterocyclyl, heterocyclylalkyl, phenyl, phenylalkyl, hetaryl or hetarylalkyl; or R4 and R5 together form an alkanediyl chain which can be substituted and/or can be interrupted by a hetero atom; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring wh
    Type: Grant
    Filed: November 2, 1999
    Date of Patent: April 16, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Baumann, Wolfgang von Deyn, Stefan Engel, Regina Luise Hill, Uwe Kardorff, Guido Mayer, Martina Otten, Michael Rack, Joachim Rheinheimer, Matthias Witschel, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
  • Patent number: 6365738
    Abstract: Described are preferred processes for preparing heterocycles having one or more nitrogen and/or oxygen heteroatoms, utilizing a 1,3-dihalopropene as an effective 3-carbon fragment. Preferred processes yield pyridines, quinolines, oxazoles, pyrimidines and pyrazoles, depending upon the other reactant or reactants utilized with the 1,3-dihalopropene.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: April 2, 2002
    Assignee: Reilly Industries, Inc.
    Inventors: Ramiah Murugan, Eric F. V. Scriven
  • Patent number: 6358631
    Abstract: A light emitting device (LED) structure and devices containing the same in which the LED structure contains a plurality of at least a first and a second light emitting organic device (LED) stacked one upon the other, to form a layered structure, with each LED separated one from the other by a transparent conductive layer to enable each device to receive a separate bias potential to operate to emit light through the stack, at least one of said LED's comprising an emission layer containing an emitting compound, optionally in a matrix of at least one host compound capable of carrying electrons to the emitting compound.
    Type: Grant
    Filed: August 6, 1996
    Date of Patent: March 19, 2002
    Assignee: The Trustees of Princeton University
    Inventors: Stephen Ross Forrest, Mark Edward Thompson, Paul Edward Burrows, Dennis Matthew McCarty, Linda Susan Sapochak, Jon Andrew Cronin
  • Patent number: 6352580
    Abstract: Methods of forming a film on a substrate using chemical vapor deposition techniques and pyrazolyl complexes. The complexes and methods are particularly suitable for the preparation of semiconductor structures.
    Type: Grant
    Filed: August 3, 2000
    Date of Patent: March 5, 2002
    Assignee: Micron Technology, Inc.
    Inventors: Stefan Uhlenbrock, Brian A. Vaartstra
  • Patent number: 6338741
    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: January 31, 2000
    Date of Patent: January 15, 2002
    Assignee: L'Oreal
    Inventors: Laurent Vidal, Agnès Burande, Gérard Malle, Michel Hocquaux
  • Patent number: 6329402
    Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): wherein A represents, for example, a heteroaryl group which contains at least one nitrogen atom and may have a substituent, B represents, for example, a heteroarylene group, a —CONH— group or a group represented by the formula —CR6═CR7— in which R6 and R7 represents H, a lower alkyl group or the like, D represents an arylene group, a heteroarylene group or the like, n1 stands for 0 or 1, M represents, for example, a hydroxyl group or a lower alkoxy group; or a physiologically acceptable salt thereof. As a retinoic-related compound replacing retinoic acid, it permits the provision of a preventive and/or therapeutic for various diseases.
    Type: Grant
    Filed: May 17, 1999
    Date of Patent: December 11, 2001
    Assignee: Eisai Co., Ltd.
    Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
  • Patent number: 6319941
    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: November 20, 2001
    Assignee: American Home Products Corporation
    Inventors: Adam Matthew Gilbert, Zhen-jia Chen
  • Publication number: 20010031878
    Abstract: New leflunomide Form III is disclosed, along with processes for preparing it. The present invention also provides an economic process for preparing leflunomide Form II and a process for preparing leflunomide Form I from leflunomide Form III. Pharmaceutical compositions and dosage forms containing the new form and methods of using them for the treatment of rheumatoid arthritis are also disclosed.
    Type: Application
    Filed: December 14, 2000
    Publication date: October 18, 2001
    Inventors: Ilya Avrutov, Naomi Gershon, Judith Aronhime
  • Publication number: 20010012905
    Abstract: The invention pertains to a method for preparing derivatives of the pyrazolinylnaphthalic acid having the general formula 1
    Type: Application
    Filed: December 21, 2000
    Publication date: August 9, 2001
    Inventors: Victor M. Shershukov, Valentina T. Skripkina
  • Patent number: 6268504
    Abstract: The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated
    Type: Grant
    Filed: December 10, 1999
    Date of Patent: July 31, 2001
    Assignee: American Home Products Corporation
    Inventors: Panolil Raveendranath, Joseph Zeldis, Galina Vid, John R. Potoski, Jianxin Ren, Silvio Iera
  • Patent number: 6265584
    Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.
    Type: Grant
    Filed: May 20, 1999
    Date of Patent: July 24, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventors: Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
  • Patent number: 6265428
    Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1): where X and Y are selected from groups that include O, S, and NH; and Ar1, Ar2 and Ar3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteroaryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.
    Type: Grant
    Filed: June 8, 1999
    Date of Patent: July 24, 2001
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming Fai Chan, Vitukudi Narayanaiyengar Balaji, Rosario Silvestre Castillo, Adam Kois, Bore Gowda Raju, Chengde Wu
  • Patent number: 6229022
    Abstract: Pyrazole derivatives are prepared by reacting carbonyl compounds R1—C(O)—CH(R2)—CH2R3 with hydrazine, its hydrate or its salts in 30 to 100% by weight sulfuric acid in the presence of catalytic amounts of iodine or of an iodine compound.
    Type: Grant
    Filed: December 13, 1999
    Date of Patent: May 8, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans Rupert Merkle, Erich Fretschner
  • Patent number: 6177427
    Abstract: Compositions of non-steroidal glucocorticoid antagonists for treating glaucoma or ocular hypertension and methods for their use are disclosed.
    Type: Grant
    Filed: July 1, 1999
    Date of Patent: January 23, 2001
    Assignee: Alcon Laboratories, Inc.
    Inventors: Abbot F. Clark, Raymond E. Conrow