Phthalazines (including Hydrogenated) Patents (Class 544/237)
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Patent number: 6933296Abstract: The compounds of formula I in which Ar1, A, R6, R7, R8 and Ar2 have the meanings as given in the description are novel effective bronchial therapeuticsType: GrantFiled: June 1, 2001Date of Patent: August 23, 2005Assignee: Altana Pharma B.V.Inventor: Geert Jan Sterk
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Patent number: 6924284Abstract: The present invention provides compounds comprising a bicyclic aryl moiety, such as 2H-phthalazin-1-one or derivatives thereof, compositions comprising the same, and methods for producing and using the same. In particular, the present invention provides compounds of the formula: or a pharmaceutically acceptable salt, a hydrate, a solvate, or a prodrug thereof; where Q1, Q2 and Y are those defined herein.Type: GrantFiled: August 15, 2002Date of Patent: August 2, 2005Assignees: ICOS Corporation, Deltagen Research Labs, LLCInventors: Graham Beaton, Wilna J. Moree, Jaimie K. Rueter, Russell S. Dahl, David L. McElligott, Phyllis Goldman, Anthony J. Demaggio, Erik Christenson, Dan Herendeen, Kerry W. Fowler, Danwen Huang, Jaimie E. Bertino, Lisa H. Bourdon, David J. Fairfax, Qin Jiang, Helge A. Reisch, Ren Hua Song, Pavel E. Zhichkin
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Patent number: 6919351Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 9, 2001Date of Patent: July 19, 2005Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young, Melissa S. Egbertson, John S. Wai, Jennifer J. Bennett
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Patent number: 6911440Abstract: The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.Type: GrantFiled: November 26, 2003Date of Patent: June 28, 2005Assignee: Novartis AGInventors: Guido Bold, Janet Dawson King, Jörg Frei, Richard Heng, Paul William Manley, Bernhard Wietfeld, Jeanette Marjorie Wood
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Patent number: 6908919Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: July 15, 2002Date of Patent: June 21, 2005Assignee: Pharmacia CorporationInventors: Michael S. South, Brenda L. Case, Thomas A. Dice, Ricky L. Fenton, Gary W. Franklin, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, Carrie L. Kusturin, Richard J. Lindmark, Scott A. Long, William L. Neumann, David B. Reitz, John I. Trujillo, Ching-Cheng Wang, Rhonda Wood, Qingping Zeng, Matthew W. Mahoney, John J. Parlow, Melvin L. Rueppel
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Patent number: 6906070Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.Type: GrantFiled: August 8, 2001Date of Patent: June 14, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
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Patent number: 6903101Abstract: Substituted and Fused pyridazines having angiogenesis inhibiting activity and the generalized structural formula wherein the ring containing A, B, D, E, and L is a nitrogen-containing heterocycle; groups X and Y may be any of a variety of defined linking units; R1 and R2 may be defined independent substituents or together may be a ring-defining bridge; ring J may be an aryl, pyridyl, or cycloalkyl group; and G groups may be any of a variety of defined substituents. Pharmaceutical compositions containing these materials, and methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermiability processes using these materials are also disclosed.Type: GrantFiled: August 10, 2000Date of Patent: June 7, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Jacques P. Dumas, Stephen James Boyer, Teddy Kite Joe, Holia N. Hatoum-Mokdad, Harold C. E. Kluender, Wendy Lee, Dhanapalan Nagarathnam, Robert N. Sibley, Ning Su
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Patent number: 6903097Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: December 18, 2002Date of Patent: June 7, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Fred L. Ciske, John R. Palmer, Mark E. Schnute, Valerie A. Vaillancourt
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Patent number: 6903098Abstract: The present invention relates to the use of phthalazine derivatives as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30), to the use as inhibitors of PARP-homologous enzymes and, in particular, these phthalazine derivatives also show a selective inhibition of PARP-homologous enzymes.Type: GrantFiled: May 3, 2000Date of Patent: June 7, 2005Assignee: Abbott GmbH & Co.Inventors: Wilfried Lubisch, Jens Sadowski, Michael Kock, Thomas Höger
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Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6894048Abstract: Substituted dihydrophthalazine sulfur containing compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neuropsychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.Type: GrantFiled: September 18, 2003Date of Patent: May 17, 2005Assignee: Transgenomic, Inc.Inventors: Xue-Feng Pei, Baoqing Li, Maria-Luisa Maccecchini
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Patent number: 6894173Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: February 10, 2003Date of Patent: May 17, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Patent number: 6891041Abstract: A process for the production of 4-(heteroaryl-methyl)-halogen-1(2H)-phthalazinones, especially 4-(4-pyridylmethyl)-1(2H)-phthalazinone, is described, which is characterized by the reaction of phthalidyl-3-triphenylphosphonium salt with 4-pyridine aldehyde in the presence of a basic adjuvant, subsequent reaction with hydrazine hydrate and subsequent acid treatment, whereby this process avoids the technical safety and environmental problems of the known processes.Type: GrantFiled: December 20, 2000Date of Patent: May 10, 2005Inventors: Orlin Petrov, Thomas Heiner, Herribert Neh, Martin Kruger
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Patent number: 6890926Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: July 20, 2001Date of Patent: May 10, 2005Assignee: Zentaris AGInventors: Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
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Patent number: 6869945Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems reType: GrantFiled: November 20, 2002Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6846821Abstract: The compounds of formula (I) in which R1, R2, A and Ar have the meanings as given in the description are novel effective PDE4 inhibitors.Type: GrantFiled: February 25, 2003Date of Patent: January 25, 2005Assignee: Altana Pharma, AGInventor: Geert Jan Sterk
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Publication number: 20040259734Abstract: The present invention aims at providing an isoxazoline derivative and a pharmaceutically acceptable salt thereof, both having an excellent herbicidal effect and an excellent selectivity between crop and weed.Type: ApplicationFiled: June 12, 2004Publication date: December 23, 2004Inventors: Masao Nakatani, Minoru Ito, Kyoko Kimijima, Masahiro Miyazaki, Makoto Fujinami, Ryohei Ueno, Satoru Takahashi
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Publication number: 20040254190Abstract: The present invention relates to compounds of the formula I, 1Type: ApplicationFiled: April 14, 2004Publication date: December 16, 2004Applicant: Pfizer IncInventor: Spiros Liras
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Publication number: 20040248225Abstract: The present invention relates to substituted hydrazides of a luciferin dye or to substituted hydrazides of a dye analogous thereto. These chemical compounds comprise the luciferin dye or the dye analogue thereto as a light emitting moiety precursor and the substituted hydrazide as a leaving group precursor, wherein a nitrogen atom of said hydrazide group is bound to a carbonyl group or to a group chemically equivalent to said carbonyl group of said luciferin or said analogue. The invention also relates to conjugates between a biomolecule and these compounds and to the use of such compounds in chemiluminescence procedures.Type: ApplicationFiled: June 25, 2004Publication date: December 9, 2004Inventors: Dieter Heindl, Rupert Herrmann, Hans-Peter Josel, Erasmus Huber, Ursula Klause, Oliver Simon
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Patent number: 6825196Abstract: A method of improving the stability of a hydralazine composition during manufacturing or storage comprising coupling an N-protecting group with hydralazine to produce the compound having the formula: or a compound having the formula: where R1 and R2 are independently H, branched or straight chain alkyl having from 1 to about 7 carbon atoms, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted alkylcycloalkyl, lower alkenyl or R1 and R2 together form part of a substituted or unsubstituted cycloalkyl having from about 4 of about 7 carbon atoms; where R3 is a branched or straight chain alkyl having from 1 to about 7 carbon atoms, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted cycloalkyl, aralkyl, substituted or unsubstituted alkylcycloalkyl or a group having the formula (CH2)nCOOH where n is from 1 to about 7.Type: GrantFiled: March 5, 2002Date of Patent: November 30, 2004Assignee: Barbeau Pharma, Inc.Inventor: Donald L. Barbeau
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Patent number: 6821974Abstract: Pharmaceutical compounds having the general formula: or compounds having the formula: where R1 and R2 are independently H, branched or straight chain alkyl having from 1 to about 7 carbon atoms, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted alkylcycloalkyl, lower alkenyl or R1 and R2 together form part of a substituted or unsubstituted cycloalkyl having from about 4 of about 7 carbon atoms; where R3 is a branched or straight chain alkyl having from 1 to about 7 carbon atoms, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted cycloalkyl, aralkyl, substituted or unsubstituted alkylcycloalkyl or a group having the formula (CH2)nCOOH where n is from 1 to about 7.Type: GrantFiled: November 27, 2002Date of Patent: November 23, 2004Assignee: Barbeau Pharma, IncInventor: Donald L. Barbeau
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Publication number: 20040214999Abstract: The present invention relates to a chemical compound comprising a light emitting moiety precursor and a precursor of a leaving group, bound to each other by an amide or by an ester bond and characterized in that the leaving group precursor upon oxidation is converted into the leaving group. The invention also relates to compounds additionally comprising a coupling group to the use of such compounds for labeling of biomolecules and more generally to the use of such compounds in chemiluminescence detection procedures.Type: ApplicationFiled: June 14, 2004Publication date: October 28, 2004Inventors: Dieter Heindl, Rupert Herrmann, Hans-Peter Josel, Erasmus Huber, Ursula Klause
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Publication number: 20040192695Abstract: A process for the production of 4-(heteroaryl-methyl)-halogen-1(2H)-phthalazinones, especially 4-(4-pyridylmethyl)-1(2H)-phthalazinone, is described, which is characterized by the reaction of phthalidyl-3-triphenylphosphonium salt with 4-pyridine aldehyde in the presence of a basic adjuvant, subsequent reaction with hydrazine hydrate and subsequent acid treatment, whereby this process avoids the technical safety and environmental problems of the known processes.Type: ApplicationFiled: June 11, 2003Publication date: September 30, 2004Inventors: Orlin Petrov, Thomas Heiner, Herribert Neh, Martin Kruger
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Patent number: 6797710Abstract: The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.Type: GrantFiled: June 20, 2002Date of Patent: September 28, 2004Assignee: Akzo Nobel N.V.Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
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Publication number: 20040152708Abstract: The present invention provides new trans-9,10-dehydroepothilone C and trans-9,10-dehydroepothilone D based derivative compounds, compositions and methods of inhibiting cellular hyperproliferation and/or stabilizing microtubules in vitro and of treatment of hyperproliferative diseases in vivo. Also disclosed are methods of making the compounds.Type: ApplicationFiled: November 7, 2003Publication date: August 5, 2004Inventors: Yong Li, Kurt Sundermann, Li Tang, David Myles
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Publication number: 20040142933Abstract: This invention relates to compounds of the formula I 1Type: ApplicationFiled: October 28, 2003Publication date: July 22, 2004Inventors: George William Forrest, Harriet Wall Hamilton
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Publication number: 20040132721Abstract: The compounds of formula I, in which R1, R2, R3, A, X, s and R9 have the meanings as given in the description are novel effecfive PDE4 inhibitors.Type: ApplicationFiled: October 23, 2003Publication date: July 8, 2004Inventors: Gerhard Grundler, Beate Schmidt, Geert Jan Sterk
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Publication number: 20040116694Abstract: The invention relates to quinoline and isoquinoline derivatives of general formula I 1Type: ApplicationFiled: April 2, 2003Publication date: June 17, 2004Applicant: Schering AGInventors: Stefan Jaroch, Manfred Lehmann, Norbert Schmees, Markus Berger, Harmut Rehwinkel, Konrad Krolikiewicz, Werner Skuballa, Heike Schaecke, Arndt J.G. Schottelius
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Patent number: 6750218Abstract: 1,3 Diazines according to formula: and pharmaceutically acceptable salts thereof inhibit phosphorylation of platelet-derived growth factor receptor and thereby hinder abnormal cell growth and cell wandering.Type: GrantFiled: August 26, 2002Date of Patent: June 15, 2004Assignee: Millenniumium Pharmaceuticals, Inc.Inventors: Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shigeki Fujiwara, Shinichi Ide, Eiji Tsukuda, Junko Irie, Shoji Oda
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Patent number: 6740654Abstract: Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the saltType: GrantFiled: July 5, 2001Date of Patent: May 25, 2004Assignee: Celltech R & D LimitedInventors: Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
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Publication number: 20040097510Abstract: The present invention relates to substituted xanthines of general formula 1Type: ApplicationFiled: August 12, 2003Publication date: May 20, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R.H. Lotz, Mohammad Tadayyon
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Publication number: 20040067946Abstract: The compounds of a formula I, in which the given substituents have the meanings as given in the description, are novel effective PDE4 inhibitors.Type: ApplicationFiled: August 13, 2003Publication date: April 8, 2004Inventors: Gerhard Grundler, Beate Schmidt, Geert Jan Sterk
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Publication number: 20040063705Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.Type: ApplicationFiled: August 21, 2002Publication date: April 1, 2004Inventors: Jean-Christophe Harmange, Shon Booker, John L. Buchanan, Stuart Chaffee, Perry M. Novak, Simon Van Der Plas, Xiaotian Zhu
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Patent number: 6710047Abstract: The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etheritied or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, pType: GrantFiled: January 7, 2003Date of Patent: March 23, 2004Assignee: Novartis AGInventors: Guido Bold, Jörg Frei, Peter Traxler, Karl-Heinz Altmann, Helmut Mett, David Raymond Stover, Jeanette Marjorie Wood
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Patent number: 6703390Abstract: Substituted dihydrophthalazine sulfur containing compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neurosychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.Type: GrantFiled: April 12, 2001Date of Patent: March 9, 2004Assignee: Transgenomic, Inc.Inventors: Xue-Feng Pei, Baoqing Li, Maria-Luisa Maccecchini
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Publication number: 20040043999Abstract: A process for preparing a compound of formula I: 1Type: ApplicationFiled: May 20, 2003Publication date: March 4, 2004Applicant: Zambon Group S.p.AInventors: Mauro Napoletano, Gabriele Norcini, Daniela Botta, Giancarlo Grancini, Gabriele Morazzoni, Francesco Santangelo, Jorge G. Siro Herrero, Jose Luis Garcia Navaio, Julio G. Alvarez-Builla
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Publication number: 20040044000Abstract: This invention provides compounds defined by Formula I 1Type: ApplicationFiled: August 5, 2003Publication date: March 4, 2004Inventors: Amy Mae Bunker, Daniel Fred Ortwine
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Patent number: 6699870Abstract: The present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof: wherein R1 and R2 are the same as or different from each other and represent a halogen atom, a C1 to C4 alkyl group which may be substituted with a halogen atom, a C1 to C4 alkoxy group which may be substituted with a halogen atom or a cyano group; X represents a cyano group, a nitro group, a halogen atom, a hydroxyimino group which may be substituted or a heteroaryl group which may be substituted; Y represents a heteroaryl group, an aryl group which may be substituted, an alkynyl group which may substituted, an alkenyl group, an alkyl group, an optionally substituted saturated or unsaturated 4- to 8-membered amine ring, and the cyclic amine compound is a monocyclic compound, bicyclic compound or a spiro compound; l is an integer of 1 to 3; provided that the case where l is 1 or 2, X is aType: GrantFiled: October 28, 2002Date of Patent: March 2, 2004Assignee: Eisai Co., Ltd.Inventors: Nobuhisa Watanabe, Norio Karibe, Kazuki Miyazaki, Fumihiro Ozaki, Atsushi Kamada, Shuhei Miyazawa, Yoshimitsu Naoe, Toshihiko Kaneko, Itaru Tsukada, Tadashi Nagakura, Hiroki Ishihara, Kohtarou Kodama, Hideyuki Adachi
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Patent number: 6699868Abstract: Therapeutically active compounds of formula (I): in which R1 to R4 means hydrogen, alkyl, alkenyl, aryl, arylalkyl, carboxyalkyl, hydroxyalkyl or halogenalkyl, or R2 and R3 form a ring of 5-7 carbon atoms, R5 to R9 means hydrogen, alkyl, alkenyl, aryl, arylalkyl, acyl, hydroxy, alkoxy, alkoxycarbonyl, amino, acylamino, alkylamino, aryloxy, halogen, cyano, nitro, carboxy, alkylsufonyl, sulfonamido or trifluoromethyl, wherein each aryl residue defined above by itself or as a part of another group may be substituted, and pharmaceutically acceptable salts and esters thereof. The compounds increase the calcium sensitivity of contractile proteins of the cardiac muscle and are thus useful in the treatment of congestive heart failure.Type: GrantFiled: December 26, 2002Date of Patent: March 2, 2004Assignee: Orion CorporationInventors: Jarmo Pystynen, Aino Pippuri, Anne Luiro, Pentti Nore, Reijo Bäckström, Kari Lönnberg, Heimo Haikala, Jouko Levijoki, Petri Kaheinen, Juha Kaivola
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Patent number: 6696437Abstract: The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.Type: GrantFiled: March 25, 2002Date of Patent: February 24, 2004Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Michael Kock, Thomas Hoeger, Roland Grandel, Uta Holzenkamp, Sabine Schult, Reinhold Mueller
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Patent number: 6686347Abstract: The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.Type: GrantFiled: September 26, 2001Date of Patent: February 3, 2004Assignee: Novartis AGInventors: Guido Bold, Janet Dawson King, Jörg Frei, Richard Heng, Paul William Manley, Bernhard Wietfeld, Jeanette Marjorie Wood
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Patent number: 6677333Abstract: Poly(ADP-ribose)polymerase inhibitors containing as the active ingredient 2H-phthalazin-1-one derivatives represented by general formula (I) (wherein each symbol is as defined in the description) or salts thereof. The compounds of the general formula (I) inhibit poly(ADP-ribose)polymerase and are useful as preventives and/or remedies for various ischemic diseases (brain, heart, digestive tract, skeletal muscle, retina, etc.), inflammatory diseases (inflammatory intestinal diseases, multiple encephalosclerosis, arthritis, etc.), nerve degeneration diseases (extrapyramidal disorder, Alzheimer's disease, muscular dystrophy, etc.), diabetes, shock, head trauma, renal insufficiency, hyperalgesia, etc. These compounds are also useful as sensitizers for agents against retroviruses (HIV, etc.) and chemotherapy for cancer.Type: GrantFiled: July 25, 2001Date of Patent: January 13, 2004Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Jun Takeuchi, Shinya Takahashi, Masao Naka
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Publication number: 20040006082Abstract: The present invention provides 2-aminopyridine compound having an excellent adenosine receptor (A1, A2a, A2b receptors) antagonism, which is represented by the following formula: 1Type: ApplicationFiled: January 23, 2003Publication date: January 8, 2004Inventors: Hitoshi Harada, Osamu Asano, Shuhei Miyazawa, Masato Ueda, Masahiro Yasuda, Nobuyuki Yasuda
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Publication number: 20040006081Abstract: Compounds of formula (I), compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).Type: ApplicationFiled: December 10, 2002Publication date: January 8, 2004Inventors: Jeremy Burrows, Anne Cooper, John Cumming, Thomas McInally, Howard Tucker
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Publication number: 20030232817Abstract: Compounds of the formula I 1Type: ApplicationFiled: February 24, 2003Publication date: December 18, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventor: Roman Wolfgang Fleck
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Patent number: 6664255Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: May 18, 2000Date of Patent: December 16, 2003Assignee: Pharmacia CorporationInventors: Michael South, John J. Parlow, Darin E. Jones, Brenda Case, Tom Dice, Richard Lindmark, Michael J. Hayes, Melvin L. Rueppel, Horng-Chih Huang, Wei Huang, Scott A. Long, Matthew Mahoney, William L. Neumann, David Reitz, John I. Trujillo, Ching-Cheng Wang, Rhonda Wood, Qingping Zeng, Rick Fenton, Gary W. Franklin, Carrie Kusturin
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Publication number: 20030212072Abstract: This invention relates to [4-oxo-(5-trifluoromethyl-benzothiazol-2-ylmethyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid ethanolamine salt, pharmaceutical compositions thereof and methods of treating diabetic complications in mammals comprising administering to said mammals said salt and said compositions. This invention is also directed to combinations of said diethylamine salt with NHE-1 inhibitors, selective serotonin retuptake inhibitors (SSRIs), glycogen phosphorylase inhibitors (GPIs), sorbitol dehydrogenase inhibitors (SDIs) and antihypertensive agents. Said combinations are useful in treating diabetic complications in mammals.Type: ApplicationFiled: April 1, 2003Publication date: November 13, 2003Inventor: Banavara L. Mylari
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Patent number: 6645965Abstract: Nitric acid salts with medicines having an antihypertensive activity.Type: GrantFiled: December 12, 2000Date of Patent: November 11, 2003Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6635641Abstract: Amide compounds represented by the formula: wherein: R1 is a moiety represented by the formula where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting of CH2, O, and S, provided that at least one of X and Y is CH2, or X and Y together with the bond there-between form a cyclopropyl; are described. These compounds and pharmaceutical compositions containing them modulate and/or inhibit the activity of certain protein kinases and are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation.Type: GrantFiled: January 19, 2001Date of Patent: October 21, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Dilip Bhumralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney