Tricyclo Ring System Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.03)
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Publication number: 20090023722Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain amide 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: June 30, 2008Publication date: January 22, 2009Inventors: Patrick L. Coleman, Stephen L. Crooks, George W. Griesgraber, Kyle J. Lindstrom, Bryon A. Merrill, Michael J. Rice
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Publication number: 20090018122Abstract: Imidazoquinoline compounds with an aryloxy or arylalkyleneoxy or hydroxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: August 27, 2004Publication date: January 15, 2009Inventors: Kyle J. Lindstrom, Hugues M.H. Martin, Bryon A. Merrill, Michael J. Rice, Joshua R. Wurst, Chad A. Haraldson, Tushar A. Kshirsagar, Philip D. Heppner, Shri Niwas, George W. Griesgraber, Matthew R. Radmer
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Publication number: 20090005365Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: ApplicationFiled: June 6, 2008Publication date: January 1, 2009Applicant: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
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Publication number: 20080306049Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
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Publication number: 20080306048Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta
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Patent number: 7462717Abstract: The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising themType: GrantFiled: August 19, 2003Date of Patent: December 9, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Encarnacion Matesanz-Ballesteros, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Petrus Megens
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Publication number: 20080293712Abstract: The present invention relates to Benzo[c][2,7]naphthyridine Derivatives, compositions comprising an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for treating or preventing a proliferative disorder or an autoimmune disease, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for modulating PDK-1 activity, PKA activity, Akt activity, S6K activity, or PKC activity, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative. The invention also relates to processes for preparing a Benzo[c][2,7]naphthyridine Derivative.Type: ApplicationFiled: March 4, 2008Publication date: November 27, 2008Applicant: WYETHInventors: Allan WISSNER, Middleton Brawner FLOYD, JR., Russell DUSHIN, Heidi L. FRASER, Yongbo HU, Andreas MADERNA, Thomas NITTOLI, Yanong Daniel WANG
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Publication number: 20080287432Abstract: The invention provides a novel class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.Type: ApplicationFiled: August 15, 2006Publication date: November 20, 2008Applicants: IRM LLC, The Scripps Research InstituteInventors: Barun Okram, Pingda Ren, Nathanael S. Gray
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Publication number: 20080255110Abstract: This invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Z, m, n, o, p and r are as defined herein, its preparation, pharmaceutical composition and use as an adenosine A3 receptor ligand preferably an antagonist.Type: ApplicationFiled: June 17, 2008Publication date: October 16, 2008Applicant: SANOFI-AVENTISInventors: Peter ARANYI, Laszlo BALAZS, Maria BALOGH, Sandor BATORI, Lajos T. NAGY, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin GERBER, Judit VARGANE SZEREDI, Katalin URBAN-SZABO, Erzsebet WALCZ
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Publication number: 20080221118Abstract: Compounds of the formula I, in which s, k, I, W, R1, R2, R3, and U have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 31, 2006Publication date: September 11, 2008Inventors: Wolfgang Staehle, David Bruge, Kai Schiemann, Dirk Finsinger, Hans-Peter Buchstaller, Frank Zenke, Christiane Amendt
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Publication number: 20080214536Abstract: Compounds of a certain formula (I) in which R1, R2, R3, R31, R4, R5, R51, R6 and R7 have the meanings indicated in the description, are novel effective PDE4 inhibitors.Type: ApplicationFiled: March 9, 2006Publication date: September 4, 2008Applicant: NYCOMED GmbhInventors: Ulrich Kautz, Beate Schmidt, Dieter Flockerzi, Maria Vittoria Chiesa, Armin Hatzelmann, Christof Zitt, Johannes Barsig, Degenhard Marx, Hans-Peter Kley
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Publication number: 20080194579Abstract: The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.Type: ApplicationFiled: May 18, 2006Publication date: August 14, 2008Inventors: Carlos Garcia-Echeverria, Frederic Stauffer, Pascal Furet
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BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20080176847Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 28, 2007Publication date: July 24, 2008Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20080171744Abstract: The present invention is directed to a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.Type: ApplicationFiled: January 11, 2008Publication date: July 17, 2008Applicant: 6441513 CANADA INC.Inventors: Wayne R. Danter, Martyn Brown, Franck LePifre
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Publication number: 20080146546Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.Type: ApplicationFiled: February 4, 2008Publication date: June 19, 2008Inventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
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Publication number: 20080146557Abstract: The invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the spiro-piperidine head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, methods for preparing the compounds and pharmaceutical compositions, and their use in the treatment of dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxious and depressive disorders.Type: ApplicationFiled: January 24, 2008Publication date: June 19, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080146568Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety, depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein R1 to R1, X and Y are as defined in the specification.Type: ApplicationFiled: November 30, 2007Publication date: June 19, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080139553Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety, depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein R1 to R1, X and Y are as defined in the specification.Type: ApplicationFiled: November 30, 2007Publication date: June 12, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080139554Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety, depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein R1 to R1, X and Y are as defined in the specification.Type: ApplicationFiled: November 30, 2007Publication date: June 12, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080113962Abstract: The invention relates to condensed tricyclic benzimidazoles of formula (I) in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.Type: ApplicationFiled: September 30, 2005Publication date: May 15, 2008Applicant: Aitana Pharma AGInventors: Peter Jan Zimmermann, Wilm Buhr, Christof Brehm, Andreas Palmer, M. Vittoria Chiesa, Wolfgang-Alexander Simon, Stefan Postius, Wolfgang Kromer
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Publication number: 20080108627Abstract: The present invention relates to a quinoline derivative having the general formula (A): in which R1, R2, X, Y and Z are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).Type: ApplicationFiled: June 20, 2007Publication date: May 8, 2008Inventors: Olaf Prien, Knut Eis, Wolfgang Schwede, Judith Guenther, Dieter Zopf
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Patent number: 7312209Abstract: Compounds having the formula (I), wherein R3 is selected from H, OH and NH2; R30 is selected from ?O and ?S; W is —C(?O)—, —S(?O)—, or —S(O)2—; or W may be —CH2— if X is —C(?O)—; X is selected from —CH2—, —N(R4)—, and —O—, except that when W is —CH2—, X is —C(?O)—; Y is a bond or —C(R40)(R45)—; Q is a linker; Z is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; and R1, R2, R24, and R25 are as defined in the specification.Type: GrantFiled: December 20, 2002Date of Patent: December 25, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Edwin J. Iwanowicz, Scott H. Watterson, Ping Chen, T. G. Murali Dhar, Henry H. Gu, Yufen Zhao
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Patent number: 7291612Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.Type: GrantFiled: May 30, 2006Date of Patent: November 6, 2007Assignee: Active Biotech A.B.Inventors: Ian Richard Matthews, Thomas Stephen Coutler, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Goran Pettersson, Dorthe da Graca Thrige, Philip Huxley
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Publication number: 20070213341Abstract: The present invention relates to spiroindolinone derivatives of the formula and enantiomers and pharmaceutically acceptable salts and esters thereof which have utility as antiproliferative agents, especially, as anticancer agents.Type: ApplicationFiled: March 1, 2007Publication date: September 13, 2007Inventors: Li Chen, Qingjie Ding, Jin-Jun Liu, Song Yang, Zhuming Zhang
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Patent number: 7265103Abstract: The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with primary, secondary and/or tertiary amino groups, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2 and R3 are certain specific substituents, with the proviso that at least one of R1 and R2 is an amino radical of formula N—R10R11 wherein R10 and R11 are each a variety of radicals, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutiType: GrantFiled: March 27, 2003Date of Patent: September 4, 2007Assignee: Janssen Pharmaceutica NV.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Margaretha Henrica Maria Bakker, Ana Isabel De Lucas Olivares
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Patent number: 7235557Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: GrantFiled: February 21, 2006Date of Patent: June 26, 2007Assignee: MGI GP, Inc.Inventors: Dana Victor Ferraris, Jia-He Li, Vincent Kalish, Jie Zhang
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Patent number: 7226928Abstract: The disclosure provides methods for the treatment and prevention of periodontal disease. In preferred embodiments, the invention provides for local treatment of periodontal tissues with a pharmaceutical composition including an immune response modifier (IRM) selected from the group of immune response modifiers comprising imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, imidazonaphtyridine amines, oxazoloquinoline amines, thiazoloquinoline amines and 1,2-bridged imidazopyridine amines.Type: GrantFiled: June 14, 2002Date of Patent: June 5, 2007Assignee: 3M Innovative Properties CompanyInventors: Sumita B. Mitra, Charles E. Shelburne, Mark A. Tomai
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Patent number: 7199128Abstract: The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, A8, R2, R3, R5, R6, R7, and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.Type: GrantFiled: February 1, 2006Date of Patent: April 3, 2007Assignee: Achillion Pharmaceuticals, Inc.Inventors: Barton J. Bradbury, Jason Allan Wiles, Milind Deshpande, Qiuping Wang, Akihiro Hashimoto, Edlaine Lucien
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Patent number: 7169786Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonine (5-HT) reuptake inhibitor activity in combination with additional ?2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative.Type: GrantFiled: February 13, 2002Date of Patent: January 30, 2007Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Manuel Jesús Alcázar-Vaca, José Maria Cid-Nuñez, Joaquin Pastor-Fernandez, Antonius Adrianus Hendrikus Petrus Megens, Godelieve Irma Christine Maria Heylen, Xavier Jean Michel Langlois, Margaretha Henrica Maria Bakker, Thomas Horst Wolfgang Steckler
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Patent number: 7153849Abstract: Compounds of the formula I: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: September 10, 2003Date of Patent: December 26, 2006Assignee: WyethInventors: Deborah Ann Evrard, Dahui Zhou, Gary Paul Stack, Aranapakam Madumbai Venkatesan, Amedeo A. Failli, Susan Christman Croce
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Patent number: 7153859Abstract: The present invention provides a novel a condensed polycyclic compound useful as a phosphodiesterase 4 inhibitor, which is shown by the formula [I]: or a pharmaceutically acceptable salt thereof and a pharmaceutical composition containing the same.Type: GrantFiled: July 31, 2002Date of Patent: December 26, 2006Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tatsuzo Ukita, Yoshihiro Terakawa, Kazuteru Wada, Aya Nakata, Atsuko Sakai, Koji Ogawa
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Patent number: 7115621Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disordersType: GrantFiled: April 2, 2002Date of Patent: October 3, 2006Assignee: Lilly Icos LLCInventors: Jason S. Sawyer, Mark W. Orme, James D. Copp
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Patent number: 7081456Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.Type: GrantFiled: November 21, 2003Date of Patent: July 25, 2006Assignee: Active Biotech ABInventors: Ian Richard Matthews, Thomas Stephen Coulter, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Göran Pettersson, Dorthe da Graca Thrige, Philip Huxley
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17 ?-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
Patent number: 7053091Abstract: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17?-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with type 3 17?-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.Type: GrantFiled: December 15, 2003Date of Patent: May 30, 2006Assignee: Schering CorporationInventors: Timothy J. Guzi, Yi-Tsung Liu, Ronald J. Doll, Anil Saksena, Viyyoor M. Girijavallabhan, Jonathan A. Pachter -
Patent number: 6989390Abstract: Disclosed is a salt of amonafide or amonafide analogs represented Structural Formula (I): R1 is —(CH2)nN+HR3R4 X? or R1 is —(CH2)nN+HR3R4 X? or —(CH2)nNR3R4 when R2 is —N+HR6R7. R2 is —OR5, halogen, —NR6R7, —N+HR6R7 X?? sulphonic acid, nitro, —NR5COOR5, —NR5COR5 or —OCOR5; R3 and R4 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; each R5 is independently —H or a C1-C4 alkyl group; R6 and R7 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; n is an integer from 0-3; and X? is the carboxylate anion of an organic carboxylic acid compound. Also disclosed are methods of preparing certain compounds represented by Structural Formula (I).Type: GrantFiled: October 20, 2003Date of Patent: January 24, 2006Assignee: Xanthus Life Sciences, Inc.Inventors: Alfred M. Ajami, David O. Barlow
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Patent number: 6939881Abstract: Methods for preventing ulcers, such as gastric ulcers, in a horse about to undergo stress that causes gastric ulcers and prior to occurrence of a gastric ulcer condition in the horse involving administering a proton pump inhibitor (PPI) are disclosed and claimed.Type: GrantFiled: May 29, 2001Date of Patent: September 6, 2005Inventor: Frank Pipers
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Patent number: 6924289Abstract: The present invention relates to lactam derivatives of the formula wherein R1, R2, R3, A, X, Z, n and the dashed line are defined herein, and pharmaceutical compositions thereof, to processes and intermediates for their preparation, and to their medicinal use as selective agonists and antagonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1D receptors. These compounds are useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.Type: GrantFiled: August 15, 2002Date of Patent: August 2, 2005Assignee: Pfizer IncInventor: Harry R. Howard
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Patent number: 6875761Abstract: Condensed pyridine compounds represented by formula (I): wherein: R1 and R3 are, independently, hydrogen, lower alkyl, or lower alkoxy; R2 represent an amino substituent; ring A is a benzene ring, pyridine ring, thiophene ring, or furan ring; and B represents a substituent containing a ring structure. Also, pharmaceutically acceptable salt and hydrates thereof. These compounds are clinically useful medicaments having serotonin antagonism, and in particular, for treating, ameliorating, or preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.Type: GrantFiled: March 10, 2004Date of Patent: April 5, 2005Assignee: Eisai Co., Ltd.Inventors: Kohshi Ueno, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Noritaka Kitazawa, Keiko Takahashi, Noboru Yamamoto, Yuichi Suzuki, Manabu Matsunaga, Atsuhiko Kubota
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Publication number: 20040235839Abstract: This invention provides beta-carboline compounds of formula I: 1Type: ApplicationFiled: April 9, 2004Publication date: November 25, 2004Applicant: Millennium Pharmaceuticals, Inc.Inventors: Michael E. Hepperle, Julie Fields Liu, Francois Soucy, Yingchun Ye, Robert S. Murray, Raman Prakash, Jeremy D. Little, Alfredo Castro, Hormoz Mazdiyasni, Paul E. Fleming, Dominic Reynolds
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Patent number: 6815449Abstract: Compounds having immunosuppressive activity, cell growth inhibitory activity, anti-tumor activity, etc. are represented by formula I: and pharmaceutically acceptable salts thereof.Type: GrantFiled: November 7, 2002Date of Patent: November 9, 2004Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tsutomu Akama, Hiroyuki Nagata, Atsuhiro Hasegawa, Harumi Ue, Isami Takahashi, Yutaka Saitoh, Kenichi Mochida, Shun-ichi Ikeda, Yutaka Kanda
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Publication number: 20040214826Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) 1Type: ApplicationFiled: May 24, 2004Publication date: October 28, 2004Applicant: Pharmacia & Upjohn CompanyInventors: Robert M. McCall, Martin Durham Meglasson
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Publication number: 20040214823Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) 1Type: ApplicationFiled: May 14, 2004Publication date: October 28, 2004Applicant: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Publication number: 20040214825Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) 1Type: ApplicationFiled: May 24, 2004Publication date: October 28, 2004Applicant: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Publication number: 20040214815Abstract: The present invention provides compounds of formula (I): 1Type: ApplicationFiled: May 7, 2004Publication date: October 28, 2004Applicant: Pharmacia & Upjohn CompanyInventors: William W. McWhorter, Valentina Badescu
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Patent number: 6800624Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide 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: GrantFiled: December 21, 2001Date of Patent: October 5, 2004Assignee: 3M Innovative Properties CompanyInventors: Stephen L. Crooks, Kyle J. Lindstrom, Bryon A. Merrill, Michael J. Rice
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Publication number: 20040186103Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject.Type: ApplicationFiled: January 6, 2004Publication date: September 23, 2004Applicant: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, John M. Wetzel, Chien-An Chen, Yu Jiang, Kai Lu
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Patent number: 6794382Abstract: The invention relates to benzimidazole derivatives of general formula in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom: R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist, to give the compounds of formula (I) comprising a secondary or tertiary amine; R4 represents a hydrogen atom or a C1-C6 alkyl, C3-C7 cycloalkyl, optionally substituted C3-C7 heterocycloalkyl, —(CH2)p-heteroaryl, heteroaryl-carbonyl, phenylcarbonyl, (C1-C6)alkylcarbonyl, —(CH2)pCOOR, optionally substituted phenylsulphonyl or optionally substituted —(CH2)p-phenyl group, and, when X represents a carbon atom: R3 represents a hydrogen atom or a group —NR5R6, —N(R5)3+, —NHCOR7, —CONHR5, —COR7, —NHCONH2, —OH or —CH2OH, R4 represents a hydrogen atom or an optionally substituted —(CH2)p-phenyl, —(CH2)p-heteroaryl or —(CH2)tNR7R8 group.Type: GrantFiled: January 30, 2003Date of Patent: September 21, 2004Assignee: Sanofi-SynthelaboInventors: Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
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Publication number: 20040180875Abstract: The present invention is directed to novel compounds represented by structural Formula (I): 1Type: ApplicationFiled: December 19, 2003Publication date: September 16, 2004Inventors: Taekyu Lee, Wenting Chen, Wei Deng, Albert J. Robichaud, Ruth R. Wexler
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Patent number: 6790844Abstract: Condensed pyridine compounds represented by formula (I): wherein: R1 and R3 are, independently, hydrogen, halogen, lower alkyl, or lower alkoxy; R2 represents an amino substituent; ring A is a benzene ring, pyridine ring, thiophene ring, or furan ring; and B represents a substituent containing a ring structure. Also, pharmaceutically acceptable salt and hydrates thereof. These compounds are clinically useful medicaments having; serotonin antagonism, and in particular, for treating, ameliorating, or preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.Type: GrantFiled: May 11, 2001Date of Patent: September 14, 2004Assignee: Eisai Co., LtdInventors: Kohshi Ueno, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Noritaka Kitazawa, Keiko Takahashi, Noboru Yamamoto, Yuichi Suzuki, Manabu Matsunaga, Atsuhiko Kubota
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Publication number: 20040176367Abstract: 1-Amino 1H-imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: March 5, 2004Publication date: September 9, 2004Applicant: 3M Innovative Properties CompanyInventors: George W. Griesgraber, Karl J. Manske