Benzo Is The Other Cyclo Patents (Class 544/62)
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Patent number: 7388095Abstract: The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: November 27, 2006Date of Patent: June 17, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Publication number: 20080132496Abstract: Substituted carboxylic acid amides of general formula wherein A, B, and R1 to R5 are as defined herein, and the tautomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, such as antithrombotic activity and factor Xa-inhibiting activity.Type: ApplicationFiled: November 30, 2007Publication date: June 5, 2008Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: James Gillard, Sandra Ruth Handschuh, Herbert Nar, Roland Pfau, Henning Priepke, Wolfgang Wienen, Annette Mario Schuler-Metz, Eckhart Bauer, Georg Dahmann, Kai Gerlach
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Patent number: 7351704Abstract: The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: February 17, 2005Date of Patent: April 1, 2008Assignee: Theravance, Inc.Inventors: Daniel Marquess, Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Adam A. Goldblum, Daniel D. Long, S. Derek Turner, Jyanwei Liu
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Patent number: 7205309Abstract: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3 and A have the significance given in the specification are provided. The compounds can be used for the treatment or prevention of obesity.Type: GrantFiled: July 3, 2003Date of Patent: April 17, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Patrizio Mattei, Werner Mueller, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger
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Patent number: 7196109Abstract: The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(?NH)R1 or C(?NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essentialType: GrantFiled: November 23, 2005Date of Patent: March 27, 2007Assignee: Aventis Pharma SAInventors: Dominique Lesuisse, Gilles Dutruc-Rosset, Franck Halley, Didier Babin, Thomas Rooney, Gilles Tiraboschi
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Patent number: 7163949Abstract: Provided herein are compounds of the formulae IA–IF. These compounds are tetrahydroisoquinolines of the following structure: wherein R1–R8 for compounds of each of the formulae IA, IB, IC, ID, IE and IF are as described herein. Said compounds are particularly useful in the treatment of various neurological and psychiatric disorders, e.g., ADHD.Type: GrantFiled: November 2, 2000Date of Patent: January 16, 2007Assignee: AMR Technology, Inc.Inventors: James P. Beck, Mark A. Smith
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Patent number: 7109338Abstract: The present invention relates to substituted 1,4-dihydro-4-oxoquinolines having antiviral activity. The substituents are present at positions 1, 2 and at least one of 5-8 positions of the quinoline ring.Type: GrantFiled: February 21, 2003Date of Patent: September 19, 2006Assignee: Maruishi Pharmaceutical Co., Ltd.Inventors: Takashi Tamura, Haruo Kuriyama, Masanobu Agoh, Yumi Agoh, Manabu Soga, Teruyo Mori
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Patent number: 7067532Abstract: The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt pro-drug or solvate thereof. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) and methods for the treatment or prevention of cancer comprising administering an effective amount of a compound of Formula (Ia).Type: GrantFiled: October 26, 2001Date of Patent: June 27, 2006Assignee: AstraZenecaInventors: Francis Thomas Boyle, Keith Hopkinson Gibson, Kevin Michael Foote
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Patent number: 7049309Abstract: This invention describes compounds of Formula (I) which are modulators of potassium channels and are useful for treating conditions affected by abnormal potassium channel activity including erectile dysfunction and irritable bowel syndrome.Type: GrantFiled: October 13, 2004Date of Patent: May 23, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Piyasena Hewawasam, Sing-Yuen Sit, Kai Xie
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Patent number: 7026314Abstract: Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.Type: GrantFiled: January 15, 2002Date of Patent: April 11, 2006Assignee: AstraZeneca ABInventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
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Patent number: 7015217Abstract: The present application describes novel cyclic sulfone derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof. In formula I, A is selected from —COR5, —CO2H, —CO2R6, —C(O)NHOH, —C(O)NHOR5, —C(O)NHOR6, —NHRa, —N(OH)COR5, —N(OH)CHO, —SH, —CH2SH, —S(O)(?NH)Ra, —S(?NH)2Ra, —SC(O)Ra, —PO(OH)2, and —PO(OH)NHRa; B is a thiomorpholine ring; X is absent or is CR3R4; and Ua, Xa, Ya, Za, R1, R2, Rb, and q are defined in the present specification.Type: GrantFiled: October 7, 2002Date of Patent: March 21, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Chu-Biao Xue
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Patent number: 7002015Abstract: This invention describes compounds of Formula (I) which are modulators of potassium channels and are useful for treating conditions affected by abnormal potassium channel activity including erectile dysfunction and irritable bowel syndrome.Type: GrantFiled: October 13, 2004Date of Patent: February 21, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Kenneth M. Boy
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Patent number: 6992092Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1, R2, Ra, Rb, X, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.Type: GrantFiled: April 15, 2004Date of Patent: January 31, 2006Assignee: Pfizer Inc.Inventors: Donald L. Bussolotti, Ronald B. Gammill
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Patent number: 6969730Abstract: Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.Type: GrantFiled: February 25, 2002Date of Patent: November 29, 2005Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Youssef L. Bennani, Ramin Faghih, Gregory A. Gfesser, Lawrence A. Black
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Patent number: 6949579Abstract: The present invention relates to the novel indazole derivatives of general formula (I): in which: R is either O, S or NH; R3 is an alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, aryl, heterocycle, cycloalkyl, alkenyl, etc. radical; these radicals being optionally substituted with one or more substituents; R4, R5, R6 and R7 are chosen, independently of each other, from the following radicals: hydrogen, halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycle, cycloalkyl, alkenyl, etc.; these radicals being optionally substituted with one or more substituents.Type: GrantFiled: March 11, 2003Date of Patent: September 27, 2005Assignee: Aventis Pharma S.A.Inventors: Gilles Dutruc-Rosset, Dominique Lesuisse, Thomas Rooney, Franck Halley
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Patent number: 6930118Abstract: The invention provides aminoalkylindole compounds of Formula (I), wherein R1-R5, n and p are as described. Also provided are compositions containing compounds of Formula (I) and the use of compounds of Formula (I) in modulating the activity of a cannabinoid receptor in a subject.Type: GrantFiled: November 2, 2001Date of Patent: August 16, 2005Assignee: Amrad Operations Pty. Ltd.Inventors: Peter Gerard Moloney, Alan Duncan Robertson
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Patent number: 6924278Abstract: This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.Type: GrantFiled: November 24, 2003Date of Patent: August 2, 2005Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroshi Miyake, Kazuhiko Take, Shinji Shigenaga, Hidenori Azami, Hiroshi Sasaki, Yoshiteru Eikyu, Kazuo Nakai, Junya Ishida, Takashi Manabe, Nobukiyo Konishi, Tadashi Terasaka
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Patent number: 6908916Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: November 14, 2002Date of Patent: June 21, 2005Assignee: Bristol Myers Squibb CompanyInventors: Harold Mastalerz, Guifen Zhang, James G. Tarrant, Gregory D. Vite
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Patent number: 6897210Abstract: The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selectedType: GrantFiled: November 3, 2003Date of Patent: May 24, 2005Assignees: Zeneca Limited, Zeneca Pharma S. A.Inventors: Andrew Peter Thomas, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Patent number: 6855710Abstract: The present invention relates to new substituted indolinones of general formula wherein X and R1 to R5 are defined as in claim 1, the isomers and the salts thereof which have valuable properties. The above compounds of general formula I wherein R1 denotes a hydrogen atom, a C1-3-alkyl group or a prodrug group have valuable pharmacological properties, particularly an inhibiting effect on various kinases, on viral cyclin and on receptor tyrosine kinases, and the other compounds of the above general formula I wherein R1 does not represent a hydrogen atom, a C1-3-alkyl group or a prodrug group are valuable intermediate products for the preparation of the abovementioned compounds.Type: GrantFiled: September 19, 2003Date of Patent: February 15, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Rainer Walter, Wolfgang Grell, Armin Heckel, Frank Himmelsbach, Wolfgang Eberlein, Gerald Roth, Jacobus C.A. van Meel, Norbert Redemann, Walter Spevak, Ulrike Tontsch-Grunt, Thomas von Rueden
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Patent number: 6846817Abstract: The invention provides nicotine receptor agonists of formula I: wherein R1, x, y, and n have any of the values given in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising such a compound or salt, methods for preparing such a compound or salt, and methods for modulating (e.g. antagonizing or activating) nicotine receptors with such a compound or salt.Type: GrantFiled: November 30, 2001Date of Patent: January 25, 2005Assignee: Regents of the University of MinnesotaInventor: S. Mbua Ngale Efange
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Patent number: 6846818Abstract: The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I: pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The compounds of the invention are particularly useful in the treatment or alleviation of inflammation and inflammation associated disorders, such as, for example, rheumatoid arthritis and osteoarthritis, and in the relief of pain, such as, for example, pain associated with surgery or trauma, in mammals, preferably felines and canines.Type: GrantFiled: April 16, 2003Date of Patent: January 25, 2005Assignee: Pfizer Inc.Inventors: Kristin Lundy DeMello, Brian S. Bronk, Rhonda Marie Crosson
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Patent number: 6844336Abstract: This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, in which Z is a straight-chain or branched-chain alkyl group with up to 5 carbon atoms that is fluorinated in at least one place, preferably a trifluoromethyl group, and R1, R2, X, Y and n have the meanings that are indicated in the description. The new compounds have at their disposal strong antiestrogenic action. In addition, they can have at their disposal estrogenic action that occurs in a tissue-selective manner. They can be used for the production of pharmaceutical agents, especially for the treatment of estrogen-dependent diseases and tumors and pharmaceutical agents for hormone replacement therapy (HRT) as well as for the prevention and treatment of osteoporosis.Type: GrantFiled: March 15, 2001Date of Patent: January 18, 2005Assignee: Schering AGInventors: Hermann Kuenzer, Rolf Jautelat, Ludwig Zorn, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
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Patent number: 6774233Abstract: 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: August 10, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Patent number: 6770641Abstract: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.Type: GrantFiled: June 10, 2003Date of Patent: August 3, 2004Assignees: Yamanouchi Pharmaceutical Co., Ltd., Ludwig Institute for Cancer Research, Imperial Cancer Research Technology Ltd.Inventors: Masahiko Hayakawa, Hiroyuki Kaizawa, Hiroyuki Moritomo, Ken-Ichi Kawaguchi, Tomonobu Koizumi, Mayumi Yamano, Koyo Matsuda, Minoru Okada, Mitsuaki Ohta
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Patent number: 6743788Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: May 17, 2002Date of Patent: June 1, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
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Patent number: 6730670Abstract: A compound of the formula Compounds of formula I have a good affinity to the A2A receptor and are useful for the treatment of diseases mediated by this receptor.Type: GrantFiled: December 10, 2002Date of Patent: May 4, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Alexander Flohr
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Patent number: 6716837Abstract: Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c aType: GrantFiled: November 13, 2000Date of Patent: April 6, 2004Assignee: NPS Allelix Biopharmaceuticals, Inc.Inventors: Louise Edwards, Methvin Isaac, Shawn Maddaford, Abdelmalik Slassi, Tao Xin
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Patent number: 6713651Abstract: Disclosed are multibinding compounds which are &bgr;2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: November 1, 2000Date of Patent: March 30, 2004Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
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Patent number: 6706757Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: October 2, 2002Date of Patent: March 16, 2004Assignee: WyethInventors: Lynne Padilla Greenblatt, Michael Gerard Kelly
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Patent number: 6703397Abstract: This invention relates to indole derivatives of the general formula (I) wherein R1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfonyl, dialkylsulfamoyl, N-cycloalkyl-N-alkylsulfamoyl, heterocyclylalkyl or phenylalkyl; R2 is hydrogen, halogen, alkyl, alkanoyl, phenyl, phenylalkyl or heterocyclylalkyl; R3 is hydrogen, alkyl; and R4 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfonyl, dialkylsulfamoyl, N-cycloalkyl-N-alkylsulfamoyl, heterocyclylalkyl, or phenylalkyl; and pharmaceutically acceptable acid addition salts of these compounds, there use as therapeutically active substances; medicaments based on these substances, optionally in combination with sulphonamides, and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula (I) and their pharmaceutically acceptabType: GrantFiled: October 25, 2002Date of Patent: March 9, 2004Assignee: Basilea Pharmaceutica AGInventors: Patrizio Mattei, Philippe Pflieger
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Patent number: 6686351Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: February 27, 2002Date of Patent: February 3, 2004Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Qi Chao
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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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Patent number: 6673803Abstract: The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl);R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl groupType: GrantFiled: February 25, 2002Date of Patent: January 6, 2004Assignee: Zeneca LimitedInventors: Andrew Peter Thomas, Craig Johnstone, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Patent number: 6649609Abstract: The present invention relates to novel 1-phenylbenzimidazole derivatives having particular alkoxycarbonyl substituents in the 5-position of the benz ring and having particular cyclic substituents in the meta-position of the phenyl ring, as well as to pharmaceutical compositions containing these compounds and to methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of GABAA receptor complex, and in particular for inducing and maintaining anaesthesia, sedation, and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.Type: GrantFiled: December 12, 2001Date of Patent: November 18, 2003Assignee: Neurosearch A/SInventors: Lene Teuber, Frank Watjen
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Patent number: 6635771Abstract: Compounds of the formula in which R, R′, R7-R11, X, n1 and n3 are as defined herein. These compounds are useful as intermediates for preparing pharmaceutical compounds having pharmacological activity as chemical inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes.Type: GrantFiled: November 22, 2002Date of Patent: October 21, 2003Assignee: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
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Patent number: 6632813Abstract: The invention provides compounds with antagonism against excitatory amino acid receptors, in particular, AMPA receptor having 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives and addition salts thereof as effective ingredients, and processes for the preparation of both. The compounds are 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives represented by the formula (1) where A denotes a single bond or methylene (CH2), Y denotes a nitrogen atom or ═CH—, V denotes a single bond or methylene (CH2), T denotes a hydroxyl group, amino group, lower alkoxycarbonyl group, carboxyl group, aldehyde group or the like, Q denotes a halogen atom, lower alkyl group or lower alkoxy group, and R1 denotes a hydroxyl group, lower alkoxy group or the like, and addition salts thereof.Type: GrantFiled: August 22, 2001Date of Patent: October 14, 2003Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasuo Takano, Futoshi Shiga, Tsuyoshi Anraku, Kazunori Fukuchi
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Patent number: 6627624Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.Type: GrantFiled: March 31, 2000Date of Patent: September 30, 2003Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Alan Hutchison, Kenneth Shaw, Daniel L. Rosewater
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Patent number: 6624160Abstract: This invention provides compounds of formula I; which are useful as antiviral agents.Type: GrantFiled: March 15, 2001Date of Patent: September 23, 2003Assignee: Pharmacia & Upjohn Co.Inventors: Valerie A. Vaillancourt, Scott D. Larsen, Sajiv K. Nair
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Patent number: 6613760Abstract: The present invention relates to certain novel compounds, including their production, their formulation as pharmaceutical compositions, and their therapeutic uses. In particular, the invention discloses certain indole derivatives and their function as inhibitors of monocyte chemoattractant protein-1 (MCP-1) and RANTES induced chemotaxis. The invention also discloses the use of the novel compounds in the treatment of inflammatory disease.Type: GrantFiled: July 2, 2001Date of Patent: September 2, 2003Assignee: AstraZeneca ABInventors: Jason Kettle, Alan W Faull
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Patent number: 6613772Abstract: Compounds of the formula I in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular diseases such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance.Type: GrantFiled: June 16, 2000Date of Patent: September 2, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel, Peter Schindler
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Patent number: 6593497Abstract: The present invention is directed to multibinding compounds which are &bgr;2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: February 14, 2000Date of Patent: July 15, 2003Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Edmund J. Moran
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Patent number: 6593322Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-&bgr;. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: September 21, 2000Date of Patent: July 15, 2003Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah Marie Gayo-Fung, Bernd M. Stein, Qi Chao, Anthony R. Gangloff, Jeffrey A. McKie, Kenneth D. Rice
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Patent number: 6590099Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.Type: GrantFiled: December 6, 2001Date of Patent: July 8, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Jinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
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Patent number: 6579885Abstract: Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being aryl or heteroaryl Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine or dopamine.Type: GrantFiled: March 6, 2002Date of Patent: June 17, 2003Assignee: Albany Molecular Research, Inc.Inventors: James P. Beck, Matt A. Curry, Mark A. Smith
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Patent number: 6548667Abstract: The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP.Type: GrantFiled: December 6, 2001Date of Patent: April 15, 2003Assignee: Samsung Electronics Co. Ltd.Inventors: Young-Jun Park, Hae-Young Bae, Ji-Uk Yoo, Myeong-Yun Chae, Sang-Hyun Paek, Hye-Kyung Min, Hyun-Gyu Park, Choon-Ho Ryu, Kyung-Chul Kim, Jeoung-Wook Lee
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Patent number: 6541499Abstract: The invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts, as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: April 1, 2003Assignee: Eli Lilly and CompanyInventors: Jolie A Bastian, Nickolay Y Chirgadze, Michael L Denney, Matthew J Fisher, Robert J Foglesong, Richard W Harper, Mary G Johnson, Valentine J Klimkowski, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Shawn C Miller, Jeffrey T Mullaney, Michael E Richett, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Jennifer M Tinsley, Michael R Wiley, Minsheng Zhang
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Patent number: 6541470Abstract: The present invention relates to substituted 1,4-dihydro-4-oxoquinolines having antiviral activity. The substituents are present at positions 1, 2 and at least one of 5-8 positions of the quinoline ring.Type: GrantFiled: August 29, 2000Date of Patent: April 1, 2003Assignee: Maruishi Pharmaceutical Co., Ltd.Inventors: Takashi Tamura, Haruo Kuriyama, Masanobu Agoh, Yumi Agoh, Manabu Soga, Teruyo Mori
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Patent number: 6514971Abstract: The invention relates to the use of cinnoline derivatives of formula (I) wherein Z represents —O—, —NH—, —S— or —CH2—; m is a n integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, cyano, trifluoromethyl, Cp1-3alkyl, C1-3alkoxy, C1-3alkylthio or NR6R7 (wherein R6 and R7, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, auoro, chioro, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R4 represents hydrogen, hydroxy, halogeno, cyano, nitro, amino, trifluoromethyl, C1-3alkyl or a group R5—X1 (wherein X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR8CO—, —CONR9—, —SO2NR10—, —NR11SO2— or NR12— (wherein R8, R9, R10, R11 and R12 each independently represents hydrogen, C1-Type: GrantFiled: April 13, 1999Date of Patent: February 4, 2003Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Andrew Peter Thomas, Laurent Francois Andre Hennequin
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Patent number: 6498159Abstract: 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: March 8, 2000Date of Patent: December 24, 2002Assignee: 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