Nitrogen Double Bonded Directly To Carbon (e.g., Amidine, Ketimine, Etc.) Patents (Class 562/440)
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Patent number: 6787668Abstract: The present invention is directed to a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from the group consisting of H and methyl; and R2 is selected from the group consisting of H and methyl. The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.Type: GrantFiled: April 13, 2001Date of Patent: September 7, 2004Assignee: Pharmacia CorporationInventors: Barnett S. Pitzele, James A. Sikorski, Ronald Keith Webber
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Publication number: 20040143009Abstract: The present invention relates to novel secondary or tertiary amines useful for smoothing wrinkles and fine lines, in particular expression wrinkles and fine lines.Type: ApplicationFiled: November 6, 2003Publication date: July 22, 2004Applicant: L'OREALInventors: Maria Dalko, Lionel Breton, Christophe Boulle
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Publication number: 20040110951Abstract: The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands.Type: ApplicationFiled: July 11, 2003Publication date: June 10, 2004Inventor: Yuan-Ching P. Chiang
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Patent number: 6740682Abstract: The novel compound 3-amidinobenzoyl-D-phenylglycine-3-phenylanilide is useful as a serine protease inhibitor.Type: GrantFiled: November 19, 2001Date of Patent: May 25, 2004Assignee: Tularik LimitedInventor: John Walter Liebeschuetz
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Publication number: 20040087556Abstract: This invention relates to compounds which are N-oxides and derivatives thereof, as well as their use to treat HIF related diseases.Type: ApplicationFiled: November 6, 2002Publication date: May 6, 2004Inventors: Lynn Kirkpatrick, Garth Powis, Sarah J. Welsh
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Patent number: 6730807Abstract: Compounds containing carbodiimide units and carboxyl or carboxylate groups (compounds V), derived from a) aliphatic or araliphatic C4 to C20 polyisocyanates (component a) b) amino carboxylic acids or amino carboxylic salts (component b) and c) if desired, further compounds which carry groups able to react with isocyanate groups in an addition reaction (component c) d) if desired, other isocyanates (component d), the carbodiimide units deriving essentially exclusively from the isocyanate groups of component (a).Type: GrantFiled: March 29, 2002Date of Patent: May 4, 2004Assignee: BASF AktiengesellschaftInventors: Karl Häberle, Reinhard Treiber, Christian Lach, Ulrike Licht, Bernd Meyer-Roscher, Peter Weyland
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Publication number: 20040063781Abstract: 1Type: ApplicationFiled: October 14, 2003Publication date: April 1, 2004Inventors: Benjamin Pelcman, Annika Gustafsson, Philip R Kym
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Publication number: 20040059111Abstract: A novel fluorescent group-containing carbodiimide compound having at least one group selected from a carboxyl group, a sulfo group, a phosphono group and a phospho group which have substitution of an alkali metal, an alkaline earth metal or a basic group containing a nitrogen or phosphorus atom, which is prepared by using a novel fluorescent group-containing carbodiimide compound precursor having a halogen atom or a sulfonic acid group; and a method for detecting a nucleic acid by hybridization utilizing a nucleic acid labeled with a labeling substance, which utilizes the fluorescent group-containing carbodiimide compound as the labeling substance.Type: ApplicationFiled: September 2, 2003Publication date: March 25, 2004Inventors: Naoki Kimura, Namiko Shiohata, Yoko Yoshikawa
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Patent number: 6710056Abstract: An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.Type: GrantFiled: June 5, 2002Date of Patent: March 23, 2004Assignee: Ajinomoto Co., Inc.Inventors: Masayuki Sugiki, Kazuyuki Sagi, Kohichi Fujita, Takashi Kayahara, Shunji Takehana, Kuniya Sakurai, Kazumi Tashiro
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Publication number: 20040053892Abstract: The invention provides enantiomers of a joene and derivtives of Z(−)-ajoene. The derivative of Z(−)-ajoene are useful for modulating integrin-mediated functions, for treating disorders, diseases or conditions in which integrins play a role, and for treating tissues to improve their condition for a subsequent use, such as transplantation.Type: ApplicationFiled: June 17, 2003Publication date: March 18, 2004Inventors: John B Davidson, Alexander V Tatarintsev, Ali S Turgiev, James E K Hildreth
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Publication number: 20040034231Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: 1Type: ApplicationFiled: August 12, 2003Publication date: February 19, 2004Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
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Publication number: 20040019072Abstract: Dimer-selective RXR modulator compounds having agonist, partial agonist and/or antagonist activity in the context of an RXR homodimer and/or RXR heterodimers are provided. Also provided are pharmaceutical compositions incorporating such dimer-selective RXR modulator compounds and methods for their therapeutic use.Type: ApplicationFiled: February 5, 2003Publication date: January 29, 2004Inventors: Stacie Canan-Koch, Chan K. Hwang, Marcus F. Boehm, Beth Ann Badea, Laura J. Dardashti, Lin Zhang, Alex M. Nadzan, Richard A. Heyman, Ranjan Mukherjee, Deepak S. Lala, Luc J. Farmer
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Patent number: 6627769Abstract: Novel molecules without intramolecular peptidic bonds, able to mimic the RGD peptide, containing ARG-GLY-ASP motif “arginine-glycine-aspartic acid” (that is a potent inhibitor, in vivo and in vitro, of cellular adhesion) In vitro experimentation demonstrated that said molecules are efficient inhibitors of RASMC adhesion, proliferation and migration.Type: GrantFiled: February 20, 2002Date of Patent: September 30, 2003Assignee: Provincia Italiana Della Congregzaione dei Figli Dell'Immacolata Concezione - Istituto Dermopatico Dell'ImmacolataInventors: Antonio Facchiano, Francesco Facchiano, Ivan Rossi, Rita Casadio
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Patent number: 6627580Abstract: Chelating agents (chelants) of the general structure: wherein: n=2-4 whereby at least two of X are of formula III Y=COOH, —PO3H2 or o-hydroxyphenyl R1, R2 and R3 are independently H or C1-C8 alkyls m=1, 2 or 3 and most preferably m=1 Z and Z1 are unsubstituted or substituted C C+=C or CH or N Z1, Z2, Z′1, and Z′2 are independently selected from H (or nothing for Z2 and Z′2 if C* is N) and C1-C10 groups that optionally contain one or more N atoms (optionally attached directly to C*), whereby one of the pairs Z/Z1, Z/Z2 and Z1/Z2 and one of the pairs Z′/Z′1, Z′1/Z′2 and Z′1/Z′2 may be connected to form substituted or unsubstituted (hetero)(poly)cyclic structures of less than 20 atoms C* is either part of an aromatic (hetero)(poly)cyclic structure or linked by a double bond to Z or Z2 and/or Z′ or Z′2.Type: GrantFiled: April 25, 2002Date of Patent: September 30, 2003Assignee: Akzo Nobel N.V.Inventors: Christer L. Hakanson, Martin Heus
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Patent number: 6608196Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.Type: GrantFiled: May 3, 2002Date of Patent: August 19, 2003Assignee: Galileo Pharmaceuticals, Inc.Inventors: Bing Wang, Satyanarayana Janagani, Wyeth B. Callaway, Jonathan L. Sessler
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Patent number: 6605740Abstract: This invention provides a new class of squaraine dyes having moieties which serve for the covalent attachment to biological substrates and resulting in the fluorescent labeling of the substrates. The labeled substrates are intended for use in analytical techniques for the detection and measurement of biological and clinical compounds of interest.Type: GrantFiled: April 2, 2001Date of Patent: August 12, 2003Inventor: Spyros Theodoropulos
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Patent number: 6603041Abstract: Enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an optionally substituted arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; X is an O or S atom or the group NR30 group; j and k is each zero or the integer 1 or 2 provided that the sum of j and k is zero or the integer 1 or 2; Cy1 is an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof.Type: GrantFiled: September 5, 2001Date of Patent: August 5, 2003Assignee: Celltech R & D LimitedInventors: Timothy John Norman, John Robert Porter, John Clifford Head, Andrew James Ratcliffe
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Patent number: 6599938Abstract: There is disclosed a genus of optionally substituted Schiff base condensation products (and the carba analogs thereof) comprising an amino acid component and a benzaldehyde component, that have MIF (macrophage migration inhibitory factor) antagonist activity. The compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases, asthma, arthritis, EAE, ARDS and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization.Type: GrantFiled: October 27, 2000Date of Patent: July 29, 2003Assignee: The Picower Institute of Medical ResearchInventors: Yousef Al-Abed, Richard J. Bucala
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Patent number: 6548694Abstract: N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: wherein X and R1 to R5 are as defined herein, and includes hydrates or solvates and/or physiologically acceptable salts thereof and/or physiologically acceptable esters thereof.Type: GrantFiled: May 16, 2001Date of Patent: April 15, 2003Assignee: Hoffman-La Roche Inc.Inventors: Leo Alig, Katrin Groebke Zbinden, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Hans Peter Wessel
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Patent number: 6518435Abstract: The present invention provides, as an industrially advantageous production method, a method of producing a compound represented by the formula (III)Type: GrantFiled: April 25, 2002Date of Patent: February 11, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Taihei Yamane, Atsushi Inagaki, Osamu Yabe
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Patent number: 6500951Abstract: A pyridazin-3-on derivative of the formula (1): in which R2 is a hydrogen atom or a C1-C3 alkyl group, R3 is a hydrogen atom or a C1-C3 alkyl group, and Q is an optionally substituted phenyl group can be prepared at a high yield and high purity by ring closing a carboxylic acid derivative of the formula (2): in which R2, R3 and Q are the same as defined above, or its salt in the presence of a nitrogen-containing aromatic compound and a boron compound.Type: GrantFiled: June 28, 2001Date of Patent: December 31, 2002Assignee: Sumitomo Chemical Company, LimitedInventors: Masao Yanagawa, Masahiko Mizuno, Yoshiaki Oda
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Patent number: 6479524Abstract: Compounds that prolong thrombin time. Exemplary are: (a) rac-4-{3-[5-ethoxycarbonylmethyl-2-methyl-4-(2-methyl-pyrrolidinocarbonyl)-phenyl]-propargylamino}benzamidine, (b) rac-4-{3-[2,5-dimethyl-4-(2-methyl-pyrrolidinocarbonyl)-phenyl]-propargylamino}benzamidine, and (c) 4-[3-(2,5-dimethyl-4-isopropylcarbonyl-phenyl)propargyl-amino]benzamidine.Type: GrantFiled: October 18, 2001Date of Patent: November 12, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Henning Priepke, Iris Kauffmann-Hefner, Norbert Hauel, Uwe Ries, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
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Patent number: 6451859Abstract: Compounds having a structure according to the following formula: are effective in treating disorders such as bone disorders and glaucoma in a subject in need thereof.Type: GrantFiled: August 29, 2001Date of Patent: September 17, 2002Assignee: The Procter & Gamble CompanyInventors: Mitchell Anthony deLong, David Lindsey Soper, John August Wos, Biswanath De
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Publication number: 20020072073Abstract: The invention provides solid support synthetic methods for producing combinatorial libraries of modulators of LXRs. The combinatorial libraries thus produced are useful both as diagnostic indicators of LXR&agr; function and as pharmacologically active agents. The combinatorial libraries find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.Type: ApplicationFiled: April 4, 2001Publication date: June 13, 2002Inventors: Julio Medina, Naonori Imazaki
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Patent number: 6395737Abstract: New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.Type: GrantFiled: December 28, 1999Date of Patent: May 28, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Elisabeth Defossa, Uwe Heinelt, Otmar Klingler, Gerhard Zoller, Hans Matter, Fahad A. Al-Obeidi, Armin Walser, Peter Wildgoose
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Publication number: 20020042536Abstract: The invention relates to novel processes for preparing differentially protected lysine derivatives via a novel p-anisaldehyde Schiff base intermediate and the intermediate prepared therein.Type: ApplicationFiled: October 8, 1999Publication date: April 11, 2002Inventor: PRASAD S. RAJE
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Patent number: 6348627Abstract: Compounds with fungicidal and insecticidal properties having formula wherein X is N or CH; Z is O, S or NR8; A is hydrogen, halo, cyano, (C1-C12)alkyl, or (C1-C12)alkoxy; R1 and R8 are independently hydrogen or (C1-C4)alkyl; R2 is hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, halo(C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, aryl, aralkyl, heterocyclic, heterocyclic(C1-C4)alkyl or C(R10)═N—OR9; R3 is hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, halo(C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, aryl, aralkyl, aryl(C3-C7)cycloalkyl, heterocyclic or heterocyclic(C1-C4)alkyl; R4 and R5 are independently hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, halo(C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, halo, cyano, (C1-C4)alkoxycarbonyl, aryl, aralkyl, aryl(C3-C7)cycloalkyl, heterocyclic or heterocyclic(C1Type: GrantFiled: May 15, 2000Date of Patent: February 19, 2002Assignee: Dow AgroSciences LLCInventors: Ronald Ross, Jr., Duyan Vuong Nguyen, Edward Michael Szapacs, Frisby Davis Smith, Steven Howard Shaber
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Patent number: 6348593Abstract: A process for preparing folic acid, which comprises reacting a tetraalkoxypropanol of the general formula I, in which the substituents R are C1-C4-alkyl, with triaminopyrimidone of the formula II and p-aminobenzoyl-L-glutamic acid of the formula IIIType: GrantFiled: February 3, 2000Date of Patent: February 19, 2002Assignee: BASF AktiengesellschaftInventors: Jörg Botzem, Hagen Jaedicke, Michael John, Joachim Paust
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Patent number: 6344483Abstract: The current invention discloses halogenated amidino amino acid derivatives useful as nitric oxide synthase inhibitors, and pharmaceutically acceptable salts thereof.Type: GrantFiled: January 31, 2000Date of Patent: February 5, 2002Assignee: G. D. Searle & Co.Inventors: E. Ann Hallinan, Barnett S. Pitzele, Dale P. Spangler, Mihaly V. Toth, R. Keith Webber, Arija A. Bergmanis, Timothy J. Hagen, Sofya Tsymbalov
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Patent number: 6340420Abstract: This invention relates to methods of controlling the oxidation of hydrocarbons to respective dibasic acids, such as adipic acid for example, by removing the catalyst from the reaction mixture, outside the reaction zone, after the oxidation has taken place at least partially. The catalyst is precipitated substantially in its totality by using a base, preferably sodium hydroxide, to form the catalyst hydroxide, such as cobalt hydroxide for example. Preferably, the precipitated catalyst is recycled to the reaction zone with or without further treatment. The method may also include steps for treatment of the reaction mixture by hydrolysis and/or electrodialysis.Type: GrantFiled: June 30, 1999Date of Patent: January 22, 2002Assignee: RPC Inc.Inventors: Mark W. Dassel, Eustathios Vassiliou
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Publication number: 20020004608Abstract: N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: 1Type: ApplicationFiled: May 16, 2001Publication date: January 10, 2002Inventors: Leo Alig, Katrin G. Zbinden, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Hans Peter Wessl
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Patent number: 6337306Abstract: Phenoxyacetic acid derivatives of the formula: wherein R1, R2, Xn and A are as defined herein, and a process for preparing the derivatives. The derivatives are used as herbicides.Type: GrantFiled: November 5, 1999Date of Patent: January 8, 2002Assignee: Rhone-Poulenc AgroInventors: Norio Sasaki, Atsushi Go, Hideshi Mukaida, Yukiko Oe
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Patent number: 6337350Abstract: Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. Many other phenoxyisobutyric acid derivatives as well as certain other compounds as set out in this disclosure also have been found to inhibit the nonenzymatic glycation of proteins. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences.Type: GrantFiled: April 5, 2000Date of Patent: January 8, 2002Assignee: City of HopeInventors: Samuel Rahbar, Iraj Lalezari
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Publication number: 20010056119Abstract: The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.Type: ApplicationFiled: April 24, 2001Publication date: December 27, 2001Inventor: Pascal Druzgala
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Patent number: 6323227Abstract: This invention relates to compounds of formula which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.Type: GrantFiled: February 26, 1999Date of Patent: November 27, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada, Heinz W. Pauls, Yong Gong, Daniel G. McGarry
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Patent number: 6303818Abstract: The present invention relates to certain oxime ether compounds, compositions containing these compounds, and methods for controlling fungi by the use of a fungitoxic amount of the compounds or compositions.Type: GrantFiled: August 8, 2000Date of Patent: October 16, 2001Assignee: Dow AgroSciences LLCInventors: Lixin Zhang, Steven Howard Shaber
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Patent number: 6291702Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be colorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.Type: GrantFiled: February 8, 2000Date of Patent: September 18, 2001Assignee: Florida International UniversityInventor: David Alan Becker
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Patent number: 6265432Abstract: Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of bums, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: February 11, 2000Date of Patent: July 24, 2001Assignee: Warner-LambertInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Patent number: 6239288Abstract: Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of bums, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: March 2, 1999Date of Patent: May 29, 2001Assignee: Warner-Lambert CompanyInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Publication number: 20010001799Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: 1Type: ApplicationFiled: January 12, 2001Publication date: May 24, 2001Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans P. Wessel
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Publication number: 20010001802Abstract: A process for industrially preparing intermediates of aromatic amidine derivatives having anticoagulant activity (Japanese Patent Application Laid-Open No. 5-208946); i.e., compounds represented by formula (3) or salts thereof by the following reaction scheme including (1), (2), and (3), wherein R1 represents H, an alkanoyl group, an alkoxycarbonyl group, an aralkyl group, an aralkyloxycarbonyl group, or the like; and R3 represents H, an alkyl group, or an alkanoyl group.Type: ApplicationFiled: November 26, 1999Publication date: May 24, 2001Inventors: TORU MAKINO, YUKIO YOKOYAMA
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Patent number: 6225499Abstract: This invention provides a process for preparing aminoarylacetylenes comprising reacting a N-arylmethylidene aminoarylhalide with a terminal acetylene in the presence of a base and a catalyst system comprising a palladium catalyst and a cuprous salt to produce a novel N-arylmethylidene aminoarylacetylene, and hydrolyzing the N-arylmethylidene aminoarylacetylene to the aminoarylacetylene. In one embodiment, the invention provides a process for preparing aminophenylacetylenes comprising reacting a N-benzylidene aminophenylhalide with a terminal acetylene in the presence of a base and the catalyst system to produce a novel N-benzylidene aminophenylacetylene, and hydrolyzing the N-benzylidene aminophenylacetylene to the aminophenylacetylene.Type: GrantFiled: July 14, 1997Date of Patent: May 1, 2001Assignee: Catalytica Pharmaceuticals, Inc.Inventor: John M. Gruber
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Patent number: 6207708Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: March 11, 1998Date of Patent: March 27, 2001Assignee: G. D. Searle & CompanyInventors: Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth
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Patent number: 6160012Abstract: Leukotriene-B.sub.4 derivatives of general formula (I), in which R.sub.1 represents H, CF.sub.3, CH.sub.2 OH, and R.sub.2 represents H or an organic acid radical; R.sup.3 symbolizes H, C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl, or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom; R.sub.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl; A symbolizes a trans, trans--CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramethylene group; B symbolizes a C.sub.1 -C.sub.10 -- straight-chain or branched-chain alkylene group or group (a) or (b); D can mean a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sub.7, or together with B can also mean a direct bond; R.sub.5 and R.sub.6 are the same or different and represent H or C.sub.1 -C.sub.4 alkyl, or R.sub.6 represents H and R.sub.5 represents C.sub.1 -C.sub.15 alkanoyl or R.sub.8 represents SO.sub.2 ; R.sub.7 means H, C.sub.1 -C.sub.5 alkyl, chlorine, bromine; R.sub.Type: GrantFiled: March 27, 2000Date of Patent: December 12, 2000Assignee: Schering AktiengesellschaftInventors: Bernd Buchmann, Wolfgang Frohlich, Claudia Giesen, Hartwig Hennekes, Stefan Jaroch, Werner Skuballa
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Patent number: 6156704Abstract: The invention relates to the compounds of Formula XA ##STR1## wherein X and Y represent independently hydrogen, fluorine or chlorine, Z.sub.1 is fluorine or chlorine and M is hydrogen or a salt forming moiety and Z.sub.2 ' is chlorine or fluorine; and the corresponding herbicidal composition and methods of use. The compounds of the invention are useful as auxin transport inhibitors (i.e. useful as herbicides) and useful as potentiators or enhancers of herbicides.Type: GrantFiled: June 7, 1995Date of Patent: December 5, 2000Assignee: Novartix AGInventors: Richard J. Anderson, Ian S. Cloudsdale, Robert J. Lamoreaux, Kristine J. Schaefer, Jost Harr
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Patent number: 6156924Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: December 5, 2000Assignee: Eli Lilly and CompanyInventors: William J. Hornback, Scott C. Mauldin, John E. Munroe
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Patent number: 6137002Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.Type: GrantFiled: September 23, 1996Date of Patent: October 24, 2000Assignee: Eli Lilly and CompanyInventors: Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, John Michael Morin, Jr., Daniel J. Sall, Marshall A. Skelton, Robert Theodore Vasileff
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Patent number: 6127568Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 and [sic] CHCH.sub.2 CH.sub.3 ;R.sup.1 is hydrogen and [sic] alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl and [sic] alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;R.sup.3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino;R.sup.4 and R.sup.5 are as defined in the specification.Type: GrantFiled: August 18, 1998Date of Patent: October 3, 2000Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 6124494Abstract: The present invention provides compounds which inhibit. an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Scott C. Mauldin, John E. Munroe
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Patent number: 6114554Abstract: A phenylenediamine compound can be converted, with high selectivity, into its corresponding quinonediimine by reacting the phenylenediamine with a hypochlorite oxidation reactant.Type: GrantFiled: June 3, 1998Date of Patent: September 5, 2000Assignee: Flexsys America L.P.Inventors: Jayant Shivji Lodaya, Raymond Anton Lohr, Jr., Donald Lee Fields, Jr.