1,4-benzothiazines Patents (Class 544/51)
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Patent number: 11944613Abstract: The present invention pertains to novel treatments of neuropathic pain; in particular chemotherapy induced peripheral neuropathic pain (CIPNP). The invention provides antagonists cytochrome P450 epoxygenases (CYP), and more specifically antagonists of CYP2J2, as therapeutics for use in the treatment of neuropathic pain such as CIPNP. CYP2J2 antagonists were identified to alleviate CIPNP in-vivo, and therefore are provided additionally in combination with chemotherapeutics for the treatment of diseases such as cancer or other proliferative disorders. The CYP2J2 antagonists reduce chemotherapeutic induced pain and therefore allow for a higher dosing of the chemotherapeutic during cancer treatment. In addition the invention relates to the use of CYP2J2 agonists, or metabolites of CYP2J2, for sensitizing TRPV1.Type: GrantFiled: October 7, 2019Date of Patent: April 2, 2024Assignee: FRAUNHOFER-GESELLSCHAFT ZUR FÖRDERUNG DER ANGEWANDTEN FORSCHUNG E.V.Inventors: Marco Sisignano, Christian Brenneis, Klaus Scholich, Gerd Geisslinger, Sebastian Zinn, Michael John Parnham
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Patent number: 9334250Abstract: The present disclosure provides compounds of formula (I): compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.Type: GrantFiled: October 2, 2013Date of Patent: May 10, 2016Assignee: Arizona Board of Regents, A Body Corporate of the State of Arizona Acting For and on Behalf of Arizona State UniversityInventors: Sandipan Roy Chowdhury, Omar Khdour, Sidney Hecht
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Patent number: 9328079Abstract: A process for producing an optically active amine compound, characterized by asymmetrically hydrogenating a prochiral carbon-nitrogen double bond in the presence of a ruthenium complex represented by general formula (1) or (2) (wherein P represents an optically active diphosphine, X represents an anionic group, and Ar represents an optionally substituted arylene group).Type: GrantFiled: September 6, 2013Date of Patent: May 3, 2016Assignee: TAKASAGO INTERNATIONAL CORPORATIONInventors: Takeshi Ohkuma, Noriyoshi Arai, Kazuhiko Matsumura
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Patent number: 9120822Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.Type: GrantFiled: November 18, 2014Date of Patent: September 1, 2015Assignee: BASILEA PHARMACEUTICA AGInventors: Berangere Gaucher, Jr., Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin Xu
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Patent number: 8999976Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.Type: GrantFiled: December 9, 2013Date of Patent: April 7, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Dennis Hurley, Lev T. D. Fanning, Peter D. J. Grootenhuis, Martyn Botfield, Fredrick Van Goor
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Publication number: 20140330007Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: July 16, 2014Publication date: November 6, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Patent number: 8771648Abstract: There are provided pharmaceutical compositions comprising greater than 15% w/w of a compound of Formula (I) as defined herein and/or hydrate thereof and an amount of one or more effervescent agents that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.Type: GrantFiled: July 27, 2012Date of Patent: July 8, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Bindhumadhavan Gururajan, Farhan Abdul Karim Alhusban, Ian Paul Gabbott, David Bradley Brook Simpson, Dawn Sievwright
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Patent number: 8765741Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is CR3, and A is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: GrantFiled: September 30, 2013Date of Patent: July 1, 2014Assignee: Anadys Pharmaceuticals, Inc.Inventor: Peter Dragovich
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Publication number: 20140163016Abstract: The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.Type: ApplicationFiled: December 11, 2013Publication date: June 12, 2014Applicant: NeurAxon, Inc.Inventors: Jailall RAMNAUTH, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
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Patent number: 8716280Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.Type: GrantFiled: January 21, 2010Date of Patent: May 6, 2014Assignee: Basilea Pharmaceutica AGInventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
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Patent number: 8697911Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: June 29, 2011Date of Patent: April 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
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Patent number: 8618286Abstract: The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. Exemplary compounds are of the formula: The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.Type: GrantFiled: January 27, 2012Date of Patent: December 31, 2013Assignee: NeurAxon, Inc.Inventors: Jailall Ramnauth, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
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Patent number: 8309734Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: GrantFiled: October 19, 2009Date of Patent: November 13, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Henrietta Dehmlow, Rainer E. Martin, Ulrike Obst Sander, Hans Richter, Christoph Ullmer
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Publication number: 20120253039Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: ApplicationFiled: April 9, 2012Publication date: October 4, 2012Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Patent number: 8188073Abstract: The present invention relates to a compound, useful as a mineralocorticoid receptor-modulating agent, of the following formula [I]: wherein Ring A is a benzene ring optionally having a substituent(s) other than R1 etc, R1 is a group of the formula: RaSO2NH— etc, Ra is an alkyl group etc, R2 and R3 are each a hydrogen atom, a phenyl group, an optionally substituted alkyl group etc, X is an oxygen atom etc, Y is a group of the formula: —C(?O)— etc, Ar is an optionally substituted aryl group or an optionally substituted heteroaryl group, Q is a single bond, an alkylene group etc, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 24, 2011Date of Patent: May 29, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Toru Iijima, Yasuo Yamamoto, Hidenori Akatsuka, Takayuki Kawaguchi
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Publication number: 20120122855Abstract: The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.Type: ApplicationFiled: January 27, 2012Publication date: May 17, 2012Applicant: NeurAxon, Inc.Inventors: Jailall RAMNAUTH, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
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Patent number: 8178671Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: July 30, 2004Date of Patent: May 15, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Patent number: 8114867Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CRa, Ra being halogen, and, in the case of W, may also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH, or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, provided R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent(s) CRC and the remaining each represent CH, Rb being alkoxy, alkoxycarbonyl or alkoxyalkoxy and Rc being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are selected from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to saltsType: GrantFiled: April 10, 2008Date of Patent: February 14, 2012Assignee: Actelion Pharmaceuticals LtdInventors: Markus Gude, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 8106043Abstract: The present invention features benzothiazines that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms, and that have the formula: The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.Type: GrantFiled: July 6, 2009Date of Patent: January 31, 2012Assignee: NeurAxon, Inc.Inventors: Jailall Ramnauth, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
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Patent number: 8044044Abstract: The invention relates to compounds of formula (I) wherein R0 represents H or OH; R1 represents alkoxy; U and W represent N, V represents CH and R2 represents H or F, or U and V represent CH, W represents N and R2 represents H or F, or U and V represent N, W represents CH and R2 represents H, or U represents N, V represents CH, W represents CRa and R2 represents H; Ra represents CH2OH or alkoxycarbonyl; A represents the group CH?CH—B or a binuclear heterocyclic system D, B representing a mono- or di-substituted phenyl group wherein the substituents are halogen atoms and D representing one of the following groups wherein Z represents CH or N, and Q represents O or S; and to salts of such compounds. These compounds are useful as antibacterial agents.Type: GrantFiled: December 21, 2007Date of Patent: October 25, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 8012961Abstract: The invention relates to antibacterial compounds of formula (I) wherein U represents CH or N; W represents CH or N; R1 represents alkoxy, halogen or CN; ring A represents a pyrrolidin-1,3-diyl-, a piperidin-1,3-diyl or a morpholin-2,4-diyl group and B represents CH2; or ring A is selected from the groups drawn below: wherein R2 represents H, F or hydroxymethyl, and B is absent; G represents a group selected from the group consisting of ?—CH?CH-E, wherein Y1, Y2, Y3 and Z independently represent CH or N; Q represents O or S; and E represents phenyl which is mono- or di-substituted wherein the substituents are each independently halogen; and to pharmaceutically acceptable salts of such compounds.Type: GrantFiled: April 14, 2009Date of Patent: September 6, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 7981886Abstract: The invention relates to antibiotic derivatives of formula I wherein: A represents —O—, S, —C(?O)—, —C(?NOR6)—; Z—B represents NCH2CH2, NCOCH2, NCH2CO, NCH2CH(OH), CHN(R8)CH2 or CHN(R8)CO; D represents binuclear heteroaryl; Y1 represents —CR1— or —N—, Y2 represents —CR2— or —N—, Y3 represents —CR3— or —N— and Y4 represents —CR4— or —N—; U represents —NH—, —O— or —S— and V represents —N— or —CH—; W represents —CH2—, —O— or —NR7—; R1 represents H, methyl, ethyl or halogen; R2, R3 and R4 each represent independently H, C1-C4 alkyl, halogen, or C1-C4 alkoxy; R5 represents H, C1-C4 alkyl or fluorine; R6 represents H, C1-C4 alkyl or aryl-C1-C4 alkyl; R7 represents H, C1-C4 alkyl, aryl-C1-C4 alkyl or —CH2—COOH; R8 represents H, C1-C4 alkyl or —CH2—COOH; with the provisos that if Z—B represents NCH2CH2, NCOCH2, NCH2CO or NCH2CH(OH), then W represents —CH2—; if A represents O or S, then W represents —CH2—; and only one or two of Y1, Y2, Y3 and Y4 can represent N at the same time.Type: GrantFiled: May 24, 2006Date of Patent: July 19, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Daniel Bur, Christian Hubschwerlen, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 7960376Abstract: The present invention provides benzo-fused heterocyclic compounds having the structure of formula I, as well as prodrugs, stereoisomers, racemates, salts, hydrates, solvates, acid salt hydrates and isomorphic crystalline forms thereof. The compounds directly or indirectly modulate the activity of one or more cannabinoid receptors and can be incorporated into pharmaceutical preparations that are useful for the prevention and treatment of a variety of diseases and conditions, including pain, inflammation and pruritis.Type: GrantFiled: September 10, 2008Date of Patent: June 14, 2011Assignee: Cara Therapeutics, Inc.Inventors: Jason S. Newcom, Carla M. Gauss, Gary R. Gustafson
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Patent number: 7932254Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1 and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: February 20, 2009Date of Patent: April 26, 2011Assignee: Roche Palo AltoInventors: Daisy Joe DuBois, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Yan Lou, Timothy D. Owens, Calvin Wesley Yee
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Publication number: 20110082133Abstract: [Problems] A useful compound which can be used as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease is provided. [Means for Solution] The present inventors have conducted extensive studies on EP4 receptor agonists, and as a result, have found that a novel pyridone compound, in which a group having an acidic group is substituted at the 1-position of the pyridone ring, the 6-position is bonded with an aromatic ring group via a linking part, and the linking part contains a nitrogen atom, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action, it is useful as a pharmaceutical, in particular, as an agent for treating peripheral arterial occlusive disease.Type: ApplicationFiled: June 16, 2009Publication date: April 7, 2011Inventors: Takashi Kamikubo, Masanori Miura, Takao Okuda, Keisuke Maki, Fukushi Hirayama, Ayako Moritomo, Yuriko Komiya, Keisuke Matsuura, Ryotaro Ibuka
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PROCESS FOR PREPARING BENZOMORPHOLINE DERIVATIVES BY HYDROGENATING O-NITROPHENOXY CARBONYL COMPOUNDS
Publication number: 20110040089Abstract: A process for preparing benzomorpholine derivatives is described, in which an o-nitrophenoxy carbonyl compound is hydrogenated in the presence of extraneous metal-doped sponge metal catalysts based on nickel or cobalt with ring formation.Type: ApplicationFiled: December 18, 2009Publication date: February 17, 2011Applicant: SALTIGO GMBHInventors: MATTHIAS BOLL, BURKHARD KOCH -
Patent number: 7879845Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: GrantFiled: January 29, 2010Date of Patent: February 1, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Publication number: 20110003795Abstract: The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.Type: ApplicationFiled: May 6, 2010Publication date: January 6, 2011Applicant: Gruenenthal GmbHInventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100197670Abstract: Amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,1-4H-benzothiazines and 3-amino-1,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: and the use of the products and the corresponding pharmaceutical formulations for the treatment of neurodegenerative pathologies such as cerebral ischemia, neurodegeneration induced by cranial trauma, Alzheimer's disease, Multiple Sclerosis and Amyotrophic Lateral Sclerosis.Type: ApplicationFiled: September 22, 2008Publication date: August 5, 2010Inventors: Maurizio Anzini, Antonio Giordani, Francesco Makovec, Andrea Cappelli, Salvatore Vomero, Gianfranco Caselli, Lucio Claudio Rovati
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Publication number: 20100179135Abstract: Antibacterial compounds including 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives are provided, and methods of treatment or prevention of bacterial infection with such compounds are provided.Type: ApplicationFiled: June 13, 2008Publication date: July 15, 2010Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20100168418Abstract: A nitrogen-containing heterocyclic compound represented by the general formula: wherein the dashed line represents a single bond or a double bond; R1, R2, R3, R4 and R5 independently represent a hydrogen atom, halogen atom, a lower alkyl, aryl, lower alkoxy or monocyclic heterocyclic group which may be substituted or the like; R6 represents a lower alkyl, aryl, monocyclic heterocyclic, bicyclic heterocyclic or tricyclic heterocyclic group which may be substituted; X1 represents a lower alkylene group or the like; X2 represents a lower alkylene, lower alkenylene or lower alkynylene group which may be substituted; X3 represents an oxygen atom, sulfur atom, a sulfinyl group, sulfonyl group or the like; Y1 represents a bivalent cyclic group, containing a nitrogen, which may be substituted or the like; and Z1 represents a nitrogen atom, a carbon atom which may be substituted or the like, or a salt thereof.Type: ApplicationFiled: June 22, 2006Publication date: July 1, 2010Applicants: Toyama Chemical Co., Ltd., Taisho Pharmaceutical Co. Ltd.Inventors: Taro Kiyoto, Tadashi Tanaka, Yasuhiro Tsutsui, Junichi Ando, Mai Motono, Yasuko Kawaguchi, Toshiya Noguchi, Yasunobu Ushiki, Fumihito Ushiyama, Hiroki Urabe
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Publication number: 20100137290Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CRa, Ra being halogen, and, in the case of W, may also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH, or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, provided R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent(s) CRC and the remaining each represent CH, Rb being alkoxy, alkoxycarbonyl or alkoxyalkoxy and Rc being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are seleted from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to salts ofType: ApplicationFiled: April 10, 2008Publication date: June 3, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Markus Gude, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 7713987Abstract: The present invention relates to diaryl pyrimidine-2,4-diamines, pharmaceutical compositions thereof, and the use of the compounds and compositions for the inhibition of kinases. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: GrantFiled: December 6, 2005Date of Patent: May 11, 2010Assignee: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Rajinder Singh
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Publication number: 20100093707Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji NAKAMURA, Masayuki Morita, Tetsuo Yoneda, Kenji Izakura
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Publication number: 20100009975Abstract: The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.Type: ApplicationFiled: July 6, 2009Publication date: January 14, 2010Inventors: Jailall Ramnauth, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
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Publication number: 20100004229Abstract: The present invention relates to pyridin-3-yl pyridin-3-amine compounds and derivatives thereof having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: ApplicationFiled: January 29, 2007Publication date: January 7, 2010Inventors: Mark T. Bilodeau, Jacob M. Hoffman, M. Brad Nolt
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Publication number: 20090318687Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: ApplicationFiled: June 18, 2009Publication date: December 24, 2009Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Publication number: 20090275565Abstract: The present invention relates to novel substituted aralkyl derivatives of the general formula (I) and (IIIa), their derivatives, their analogs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, pharmaceutical compositions containing them, use of these compounds in medicine and the intermediates involved in their preparation.Type: ApplicationFiled: July 8, 2009Publication date: November 5, 2009Applicant: CADILA HEALTHCARE LIMITEDInventors: Braj B. Lohray, Vidya B. Lohray, Mukul R. Jain, Sujay Basu, Harikishore Pingali, Saurin K. Raval, Preoti S. Raval
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Publication number: 20090258856Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
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Publication number: 20090253687Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.Type: ApplicationFiled: December 27, 2006Publication date: October 8, 2009Inventors: Shoji Fukumoto, Nobuyuki Matsunaga, Taiichi Ohra, Norio Ohyabu, Tomoaki Hasui, Takashi Motoyaji, Christopher Stephen Siedem, Tony Pisal Tang, Lisa A. Demeese, Cassandra Gauthier
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Patent number: 7576078Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: GrantFiled: May 3, 2006Date of Patent: August 18, 2009Assignee: Acadia Pharmaceuticals, Inc.Inventors: Niels Skjaerbaek, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
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Publication number: 20090192144Abstract: The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof in which R, R1, R2, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.Type: ApplicationFiled: April 12, 2007Publication date: July 30, 2009Applicant: SPEEDEL EXPERIMENTA AGInventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stjepan Jelakovic, Stefan Stutz
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Patent number: 7566707Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: June 10, 2004Date of Patent: July 28, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Norbert Hauel, Elke Langkopf, Frank Himmelsbach, Iris Kauffmann-Hefner, Mohammad Tadayyon, Michael Mark
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Patent number: 7560466Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: October 6, 2006Date of Patent: July 14, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Publication number: 20090137566Abstract: The invention relates to substituted 3,4- or higher substituted piperididine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds preferably have the formula I, wherein the moieties R1, R2, R11 and W are as defined in the specification.Type: ApplicationFiled: May 24, 2006Publication date: May 28, 2009Inventors: Takeru Ehara, Yuko Hitomi, Kazuhide Konishi, Kelichi Masuya
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Publication number: 20090093469Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: ApplicationFiled: December 15, 2008Publication date: April 9, 2009Applicant: WYETHInventors: Callain Younghee Kim, Paige Erin Mahaney, Eugene John Trybulski, Puwen Zhang, Eugene Anthony Terefenko, Casey Cameron McComas, Michael Anthony Marella, Richard Dale Coghlan, Gavin David Heffernan, Stephen Todd Cohn, An Thien Vu, Joseph Peter Sabatucci, Fei Ye
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Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Publication number: 20090012069Abstract: Disclosed are novel compounds of general formula (I) where the symbols are as defined in the specification, their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The compounds are useful in the treatment of diabetes and related diseases.Type: ApplicationFiled: June 24, 2005Publication date: January 8, 2009Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Harikishore Pingali
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Publication number: 20090012055Abstract: Novel substituted piperidines of the general formulae (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.Type: ApplicationFiled: February 6, 2008Publication date: January 8, 2009Inventors: Peter Herold, Robert Mah, Stefan Stutz, Aleksandar Stojanovic, Vincenzo Tschinke, Nathalie Jotterand