Three Or More Hetero Atoms In The Tetracyclo Ring System Patents (Class 514/287)
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Publication number: 20080125452Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5 and X have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: January 26, 2006Publication date: May 29, 2008Applicant: ALTANA PHARMA AGInventors: Matthias Vennemann, Thomas Bar, Jurgen Braunger, Petra Gimmnich, Thomas Beckers, Mathias Schmidt, Thomas Ciossek, Sandra Nappe
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Publication number: 20080119505Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R31, R4, R5, R51 and Har have the meanings indicated in the description, are novel effective PDE4 inhibitors.Type: ApplicationFiled: January 31, 2006Publication date: May 22, 2008Applicant: ALTANA Pharma AGInventors: Ulrich Kautz, Beate Schmidt, Dieter Flockerzi, Maria Vittoria Chiesa, Armin Hatzelmann, Christof Zitt, Johannes Barsig, Andrea Wohlsen, Degenhard Marx, Hans-Peter Kley
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Publication number: 20080114016Abstract: The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by ad-ministering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: January 5, 2006Publication date: May 15, 2008Inventors: Edward J. Brnardic, Mark E. Fraley, Robert M. Garbaccio, Justin T. Steen
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Publication number: 20080114017Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and X have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: January 26, 2006Publication date: May 15, 2008Inventors: Matthias Vennemann, Thomas Bar, Jurgen Braunger, Petra Gimmnich
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Patent number: 7329676Abstract: The compounds of formula I in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings as indicated in the description, are novel effective PDE4 inhibitors.Type: GrantFiled: August 28, 2003Date of Patent: February 12, 2008Assignee: Nycomed GmbHInventors: Ulrich Kautz, Beate Schmidt
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Patent number: 7291627Abstract: The invention concerns dihydroimidazo[5,1-a]-?-carboline compounds of general formula (I) wherein in particular, R1, R2, R3, R4, R6 and R7, identical or different, independently of one another, present a hydrogen, halogen atom, an alkyl, hydroxyl, alkoxy, trihalogenoalkyl, alkylamino, dialkylamino, aryl, arylalkyl, carboxy, alkylcarbonyloxy, acyl, aryloxy or arylalkoxy group; R5 represents a hydrogen atom, an alkyl or arylalkyl group; and their isomers as well as their addition salts to a pharmaceutically acceptable acid. The inventive compounds are for use in medicine, in particular as hypnotics.Type: GrantFiled: May 16, 2002Date of Patent: November 6, 2007Assignee: MACEFInventors: Jean-Bernard Fourtillan, Marianne Fourtillan, Omar Karam, Fabien Zunino, Jean-Claude Jacquesy, Jean-Pierre Tafani
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Patent number: 7144843Abstract: An objective of the present invention is to provide a harmful organism control agent that possesses excellent control effect against harmful organisms and can be safely used. The present invention provides a compound of formula (1) or a salt thereof. The present invention also provides a harmful organism control agent comprising the compound of formula (1). wherein R1, n, R2, and R3 are as defined in the specification.Type: GrantFiled: January 31, 2002Date of Patent: December 5, 2006Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kazuhiko Oyama, Takeshi Teraoka, Kazumi Yamamoto
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Patent number: 7138408Abstract: Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.Type: GrantFiled: October 14, 2005Date of Patent: November 21, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Atsuo Kuki, Xinqiang Li, Michael Bruno Plewe, Hai Wang, Junhu Zhang
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Patent number: 7122534Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.Type: GrantFiled: January 23, 2004Date of Patent: October 17, 2006Assignee: Pfizer IncInventor: Jotham Wadsworth Coe
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Patent number: 7001912Abstract: Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.Type: GrantFiled: January 26, 2004Date of Patent: February 21, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Atsuo Kuki, Xinqiang Li, Michael Bruno Plewe, Hai Wang, Junhu Zhang
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Patent number: 6967215Abstract: Tetrahydrocarbazoles of formula where Q is —SO2—; —O—; or —(CO)—; X is —(CH)—; or —N—; m is from 1 to 3; t is 0 or 1 and the remaining substituents are as defined herein, are useful as antimicrobial active ingredients.Type: GrantFiled: September 11, 2001Date of Patent: November 22, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Wolfgang Haap, Andreas Mehlin, Karin Petzold, Dietmar Ochs, Werner Hölzl
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Patent number: 6960585Abstract: Compounds of formula (I), or pharmaceutically-acceptable salts thereof, are useful in treating inflammatory and immune diseases and disorders, wherein X, Y1, Y2, and R2-4 are as defined in the specification.Type: GrantFiled: September 27, 2001Date of Patent: November 1, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Francis Beaulieu, Carl Quellet, Makonen Belema, Yuping Qiu, Xuejie Yang, Fred C. Zusi
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Patent number: 6949646Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.Type: GrantFiled: December 3, 2004Date of Patent: September 27, 2005Assignee: 3M Innovative Properties Co.Inventors: John F. Gerster, Kyle J. Lindstrom, Stephen L. Crooks, Philip D. Heppner, Gregory J. Marszalek, Peter V. Maye, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
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Patent number: 6936622Abstract: Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in the description, are novel effective PDE3/4 Inhibitors.Type: GrantFiled: February 21, 2002Date of Patent: August 30, 2005Assignee: Altana Pharma AGInventor: Dieter Flockerzi
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Patent number: 6930114Abstract: The present invention relates to pyrrolo[2.1-a]dihydroisoquinolines which are inhibitors of phosphodiesterase 10a and can be used for combating cancer.Type: GrantFiled: December 4, 2001Date of Patent: August 16, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Maria Theresia Niewöhner, Marcus Bauser, Jens-Kerim Ergüden, Dietmar Flubacher, Paul Naab, Thorsten-Oliver Repp, Jürgen Stoltefuss, Nils Burkhardt, Andrea Sewing, Michael Schauer, Karl-Heinz Schlemmer, Olaf Weber, Stephen J. Boyer, Mark Miglarese, Ulrich Niewöhner
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Patent number: 6858620Abstract: Compounds of general structural formula (I), and use of the compounds or salts or solvates thereof as therapeutic agents, are disclosedType: GrantFiled: September 17, 2001Date of Patent: February 22, 2005Assignee: Lilly ICOS, LLCInventors: Mark W. Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan, Romain Luc Marie Gosmini, Lisa M. Schultze
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Patent number: 6852727Abstract: Benzimidazo[4,5-f]isoquinolinone derivatives are inhibitors of Janus protein tyrosine kinases (Jak), and as such are useful as immunosuppressants, and in the treatment of diseases including asthma, allergies, autoimmune diseases.Type: GrantFiled: July 26, 2002Date of Patent: February 8, 2005Assignee: Merck & Co., Inc.Inventors: Joung L. Goulet, Rose M. Cubbon, Richard T. Cummings, Xingfang Hong, Peter J. Sinclair, James E. Thompson
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Patent number: 6838456Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: GrantFiled: September 17, 2001Date of Patent: January 4, 2005Assignee: Lilly ICOS LLCInventors: Mark W. Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan, Françoise Gellibert, Romain Luc Marie Gosmini
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Patent number: 6809096Abstract: A pharmaceutical composition including an efficient amount of a compound selected among the compounds of formulae (I) and (Ia). The compounds have interesting cytotoxic properties leading to a therapeutic use as antitumoral medicines.Type: GrantFiled: February 13, 2002Date of Patent: October 26, 2004Assignee: Laboratoire L. LafonInventors: Evelyne Delfourne, Francis Darro, Jean Bastide, Robert Kiss, Armand Frydman
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Patent number: 6803366Abstract: Disclosed is an agent for improving learning and/or memory, which is useful for therapy of dementia accompanying disorder of memory due to a cerebrovascular disease, neurodegenerative disease such as Alzheimer's disease, endocrine disease, nutritional or metabolic disorder, infectious disease, drug addiction or the like. The agent for improving learning and/or memory according to the present invention comprises as an effective ingredient an isoquinoline derivative having a specific structure, such as (4aR, 12aR)-2-methyl-4a-(3-hydroxyphenyl)-1,2,3,4,4a,5,12,12a-octahydro-quinoline[2,3-g]isoquinoline or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 30, 2002Date of Patent: October 12, 2004Assignee: Toray Industries, Inc.Inventors: Kuniaki Kawamura, Hiroshi Nagase, Noriyuki Hirano, Junzo Kamei
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Patent number: 6747039Abstract: The present invention relates to a group of aza-anthrapyrazole compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-anthrapyrazole compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.Type: GrantFiled: March 12, 2002Date of Patent: June 8, 2004Assignee: Albany Molecular Research, Inc.Inventor: Simon N. Haydar
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Patent number: 6720348Abstract: This invention relates to pharmaceutical compositions comprising combinations of a GABA agonist, a prodrug thereof or a pharmaceutically acceptable salt of said GABA agonist or said prodrug and an ARI, a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug, kits containing such combinations and methods of using such combinations to treat mammals, including humans, suffering from diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic retinopathy, diabetic microangiopathy, diabetic macroangiopathy, cataracts or foot ulcers.Type: GrantFiled: November 29, 2001Date of Patent: April 13, 2004Assignee: Pfizer IncInventor: Banavara L. Mylari
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Patent number: 6713471Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: June 15, 2000Date of Patent: March 30, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Simon Haydar, Wenting Chen, Christopher D. Mc Clung, Emilie J. B. Calvello, David M. Zawrotny
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Patent number: 6706702Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.Type: GrantFiled: August 13, 2002Date of Patent: March 16, 2004Assignee: Pfizer Inc.Inventor: Jotham Wadsworth Coe
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Patent number: 6699899Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.Type: GrantFiled: December 21, 1999Date of Patent: March 2, 2004Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
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Publication number: 20030207906Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: ApplicationFiled: February 28, 2003Publication date: November 6, 2003Inventors: Mark W. Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan, Francoise Gellibert, Romain Luc Marie Gosmini
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Patent number: 6630483Abstract: N-oxides of the compounds of formula (I) in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, or in which R1 and R2 together are a 1-2C-alkylenedioxy group, R6 is an R7- and R8-substituted phenyl radical, they are active bronchial therapeutics.Type: GrantFiled: June 18, 2002Date of Patent: October 7, 2003Assignee: Altana Pharma AGInventor: Beate Schmidt
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Publication number: 20030091505Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: October 15, 2002Publication date: May 15, 2003Inventor: Jian-Min Fu
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Patent number: 6559160Abstract: The invention provides compounds and compositions of the formula: wherein the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; R1 is a member selected from the group consisting of substituted or unsubstituted (C5-C15)alkyl; R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl; each R3 is independently a substituent selected from -halogen, —OR′, —OC(O)R′, —NR′R″, —SR′, —R′, —CN, —NO2, —CO2R′, —CONR′R″, —C(O)R′, —OC(O)NR′R″, —NR″C(O)R′, —NR″C(O)2R′, , —NR′—C(O)NR″R′″, —NH—C(NH2)═NH, —NR′C(NH2)═NH, —NH—C(NH2)═NR—, —S(O)R′, —S(O)2R′, —Type: GrantFiled: August 25, 2000Date of Patent: May 6, 2003Assignee: Chemocentryx, Inc.Inventors: Thomas J. Schall, Daniel J. Dairaghi, Brian E. McMaster
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Patent number: 6548515Abstract: The invention relates to compound of formula (I): wherein: represents a single or double bond, R0 represents hydrogen or hydroxy or alkoxy, R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its opType: GrantFiled: November 22, 2000Date of Patent: April 15, 2003Assignee: Les Laboratories ServierInventors: Henri-Philippe Husson, Sylviane Giorgi-Renault, Christophe Tratrat, Ghanem Atassi, Alain Pierre, Pierre Renard, Bruno Pfeiffer
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Publication number: 20030065005Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and heterocyclyl or heteroaryl functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.Type: ApplicationFiled: December 6, 2001Publication date: April 3, 2003Inventors: Leslie J. Charles, Joseph F. Dellaria, George W. Griesgraber, Philip D. Heppner, Karl J. Manske, John W. Mickelson, Michael J. Rice
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Patent number: 6541484Abstract: A class of substituted and/or ring-fused pyrazolo[3,4-b]pyridine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent on the pyrazole nitrogen atom adjacent the pyridine nucleus, and an optionally substituted cycloalkyl-alkoxy, aryl-alkoxy or heteroaryl-alkoxy substituent on the carbon atom adjacent the pyridine ring nitrogen atom, are selective ligands for GABAA receptors, in particular having high affinity for the &bgr;2 and/or &bgr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse neurological disorders, including anxiety and convulsions.Type: GrantFiled: June 14, 2002Date of Patent: April 1, 2003Assignee: Merck Sharp & Dohme LimitedInventors: Ian James Collins, Linda Elizabeth Keown, Leslie Joseph Street
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Patent number: 6538011Abstract: Cosmetic or dermatological compositions for washing and/or antidandruff treatment of hair and/or scalp comprising at least one antidandruff agent chosen from pyridinethione salts, at least 1% by weight of at least one hydroxy acid, and at least one amphoteric surface-active agent or nonionic surface-active agent of the alkyl(poly)glycoside type.Type: GrantFiled: July 10, 2000Date of Patent: March 25, 2003Assignee: L'Oreal, S.A.Inventors: Véronique Maurin, Bernard Beauquey
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Patent number: 6538005Abstract: The N-oxides of the compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, arm novel active bronchial therapeutics.Type: GrantFiled: July 12, 2001Date of Patent: March 25, 2003Assignee: ALTANA Pharma AGInventor: Beate Gutterer
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Patent number: 6534519Abstract: The N-oxides of the compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel active bronchial therapeutics.Type: GrantFiled: July 12, 2001Date of Patent: March 18, 2003Assignee: Altana Pharma AGInventor: Beate Gutterer
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Patent number: 6534518Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel active bronchial therapeutics.Type: GrantFiled: July 12, 2001Date of Patent: March 18, 2003Assignee: Altana Pharma AGInventor: Beate Gutterer
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Patent number: 6521635Abstract: This invention provides methods that are useful for inhibiting a MXR transporter in a cell overexpressing a MXR gene but not overexpressing a Pgp gene by contacting the cell with an acridine derivative. The invention also provides for a method of treating a mammal suffering from a cancer, which overexpressing a MXR gene but not overexpress a Pgp gene, by the co-administration of a chemotherapeutic and an acridine derivative.Type: GrantFiled: January 22, 2001Date of Patent: February 18, 2003Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Susan Bates, Robert Robey
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Patent number: 6479505Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and Ar have the meanings indicated in the description, are novel active bronchial therapeutics.Type: GrantFiled: July 12, 2001Date of Patent: November 12, 2002Assignee: Altana Pharma AGInventor: Beate Gutterer
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Patent number: 6476025Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51, R6, R13 and R20 have the meaning indicated in the description, are novel active bronchial therapeuticsType: GrantFiled: July 12, 2001Date of Patent: November 5, 2002Assignee: Altana Pharma AGInventor: Beate Gutterer
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Patent number: 6476021Abstract: Novel fused tetracyclic heterocyclic compounds having a potent and highly selective effect of inhibiting cyclic GMP phosphodiesterase (cGMP-PDE) and a high safety; a process for producing the same; drugs characterized by containing at least one of these compounds as the active ingredient, in particular, preventives and/or remedies for pulmonary hypertension, ischemic heart diseases, erectile insufficiency, female sexual dysfunction or diseases against which cGMP-PDE inhibitory effects are efficacious and intermediates useful in producing the above compounds.Type: GrantFiled: May 26, 2000Date of Patent: November 5, 2002Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Masayuki Ohashi, Hidemitsu Nishida, Toshiyuki Shudo
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Patent number: 6469021Abstract: Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.Type: GrantFiled: October 26, 2001Date of Patent: October 22, 2002Assignee: Agouron Pharmaceuticals, Inc.Inventors: Larry Kenneth Truesdale, Richard A. Bychowski, Javier Gonzalez, Atsuo Kuki, Ranjan Jagath Rajapakse, Min Teng, Dan Kiel, Daljit S. Dhanoa, Yufeng Hong, Tso-sheng Chou, Anthony L. Ling, Michael David Johnson, Vlad Edward Gregor
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Patent number: 6451807Abstract: The present invention relates to highly selective phosphodiesterase (PDE) enzyme inhibitors and to their use in methods of treating sexual dysfunction in individuals suffering from a retinal disease, class 1 congestive heart failure, or myocardial infarction.Type: GrantFiled: April 26, 2000Date of Patent: September 17, 2002Assignee: Lilly Icos, LLC.Inventors: Jeffrey T. Emmick, Kenneth M. Ferguson, William E. Pullman, John S. Whitaker
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Patent number: 6436952Abstract: Compounds of the formula I, in which R1, R2, R3 and R4 have the meanings indicated in the description, are novel active bronchial therapeutics.Type: GrantFiled: February 15, 2001Date of Patent: August 20, 2002Assignee: BYK Gulden Lomberg Chemische Fabrik GmbHInventor: Dieter Flockerzi
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Patent number: 6384045Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.Type: GrantFiled: June 24, 1999Date of Patent: May 7, 2002Assignee: Kansas State University Research FoundationInventors: Duy H. Hua, Jean-Pierre Perchellet
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Patent number: 6310208Abstract: Since the compounds in accordance with the invention can bind to serotonin receptors (5HT2), they are especially suitable for the treatment or prevention of central nervous disorders such as depressions, bipolar disorders, anxiety states, sleep and sexual disorders, psychoses, schizophrenia, migraine and other conditions associated with cephalic pain or pain of a different kind, personality disorders or obsessive-compulsive disorders, social phobias or panic attacks, mental organic disorders, mental disorders in childhood, aggressivity, age-related memory disorders and behavioral disorders, addiction, obesity, bulimia etc., nervous system damage caused by trauma, stroke, neurodegenerative diseases etc.; cardiovascular disorders such as hypertension, thrombosis, stroke etc.; and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: January 6, 1998Date of Patent: October 30, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Heinz Stadler, Jürgen Wichmann
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Patent number: 6306869Abstract: N-oxides of formula 1 wherein R1, R2, R3 and R4 have the meanings given in the description, are selective inhibitors of types 3 and 4 of cyclic nucleotide phosphodiesterase (PDE3, PDE4); they are useful on the one hand as bronchial therapeutics but on the other hand especially for the treatment of disorders of inflammatory nature.Type: GrantFiled: November 1, 2000Date of Patent: October 23, 2001Assignee: Byk Gulden Lomberg Chemische Febrik GmbHInventor: Dieter Flockerzi
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Patent number: 6218400Abstract: A compound of formula and salts and solvates thereof, wherein R0, R1, and R2 are defined in the specification. A compound of the present invention is a potent and selective inhibitor of cGMP-specific PDE and has utility in a variety of therapeutic areas where such inhibition is beneficial.Type: GrantFiled: August 24, 1999Date of Patent: April 17, 2001Assignee: ICOS CorporationInventors: Alain Claude-Marie Daugan, Richard Frederic LaBaudiniere
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Patent number: 6214839Abstract: Compounds of formula I pharmaceutically acceptable salts thereof and compositions of either are useful for treating conditions amenable to treatment with a phosphodiesterase inhibitor type 4.Type: GrantFiled: January 24, 2000Date of Patent: April 10, 2001Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Beate Gutterer
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Patent number: 6191138Abstract: Compounds of formula (I), where R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings given in the description, are new active bronchial therapeutic agents.Type: GrantFiled: July 31, 1998Date of Patent: February 20, 2001Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Beate Gutterer
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Patent number: RE39679Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: February 16, 2006Date of Patent: June 5, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emile J. B. Calvello, David M. Zawrotny, Parthasarathl Rajagopalan