Plural Nitrogens In The Polycyclo Ring System Patents (Class 540/577)
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Patent number: 10435408Abstract: Azepine derivatives acting on 5-HT7 receptors and pharmaceutically acceptable salts thereof are disclosed. The azepine derivatives and the pharmaceutically acceptable salts thereof have high binding affinities for and high antagonistic activities on 5-HT7 receptors. Due to these advantages, the azepine derivatives and the pharmaceutically acceptable salts thereof can be applied to therapeutic or prophylactic agents for central nervous system diseases, such as depression, migraine, anxiety, pain, inflammatory pain, neuropathic pain, body temperature dysregulation, biorhythm dysregulation, sleep disturbance, and smooth muscle diseases where 5-HT7 receptors antagonistic activity is required.Type: GrantFiled: November 6, 2017Date of Patent: October 8, 2019Assignee: Korea Institute of Science and TechnologyInventors: Hyunah Choo, Youngjae Kim, Jihye Seong, Ghil Soo Nam, Yong Seo Cho
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Patent number: 9944636Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: GrantFiled: December 10, 2014Date of Patent: April 17, 2018Assignee: Celgene Quanticel Research, Inc.Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
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Publication number: 20150045351Abstract: The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action. The present invention relates to a compound represented by the formula (1) wherein ring A is an aromatic carbocycle optionally having substituent(s) or an aromatic heterocycle optionally having substituent(s), X is —N(R1)—, —O— or the like, when ring A is an aromatic carbocycle optionally having substituent(s), then R1 is a hydrogen atom, an alkyl group optionally having substituent(s), or the like, and when ring A is an aromatic heterocycle optionally having substituent(s), then R1 is a hydrogen atom, an alkyl group optionally having substituent(s), a cycloalkyl group optionally having substituent(s), or the like, is a single bond or a double bond, and n is an integer of 0, 1 or 2, or a salt thereof.Type: ApplicationFiled: March 6, 2013Publication date: February 12, 2015Applicant: Takeda Pharmaceutical Company LimitedInventors: Tomokazu Kusumoto, Shigekazu Sasaki, Hironobu Maezaki
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Publication number: 20150038438Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.Type: ApplicationFiled: August 29, 2012Publication date: February 5, 2015Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
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Publication number: 20140371207Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.Type: ApplicationFiled: December 13, 2013Publication date: December 18, 2014Applicants: Kyowa Hakko Kirin Co., Ltd., Millennium Pharmaceuticals, Inc.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C.B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
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Patent number: 8846951Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: GrantFiled: November 19, 2010Date of Patent: September 30, 2014Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
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Patent number: 8563541Abstract: The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: May 23, 2012Date of Patent: October 22, 2013Assignee: Incyte CorporationInventors: Argyrios G. Arvanitis, James D. Rodgers, Andrew P. Combs, Richard B. Sparks, Darius J. Robinson
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PROCESS FOR THE PREPARATION OF TETRACYCLIC DERIVATIVES AND INTERMEDIATE PRODUCTS USED IN THE PROCESS
Publication number: 20130274466Abstract: A process for preparation of a compound of formula I or a pharmaceutically acceptable salt thereof, is disclosed. The process involves subjecting a compound of formula II to Ullmann-type conditions to effect an intra-molecular ring closure reaction to form the compound of formula I. The different substituents are as described in the specification. Further, the process can provide an alternate route for the synthesis of asenapine from starting materials that can be readily available.Type: ApplicationFiled: September 26, 2011Publication date: October 17, 2013Applicant: Alphora Research Inc.Inventors: Boris Gorin, Craig Edward Dixon, Yang Qu -
Publication number: 20130102590Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicant: AbbVie IncInventor: AbbVie Inc.
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Publication number: 20120277216Abstract: The present invention relates to novel 1,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.Type: ApplicationFiled: December 29, 2009Publication date: November 1, 2012Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Ishtiyaque Ahmad, Pradeep Jayarajan, Nagaraj Vishwottam Kandikere, Anil Karbhari Shinde, Rama Sastri Kambhampati, Gopinadh Bhyrapuneni, Jyothsna Ravula, Sriramachandra Murthy Patnala, Venkateswarlu Jasti
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Publication number: 20120220572Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: February 28, 2012Publication date: August 30, 2012Applicant: ABBOTT LABORATORIESInventors: Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
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Patent number: 8138333Abstract: The present invention relates to novel compounds of formula (I): wherein R1, R2, R3, R4, and R5 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: GrantFiled: March 13, 2008Date of Patent: March 20, 2012Assignee: Proximagen LimitedInventors: Johan Angbrant, Peter Brandt, Rune Ringom, Bengt Lindqvist
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Publication number: 20110269744Abstract: [Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. [Means for Solution] The present inventors have investigated compounds having a 5-HT2C receptor agonist activity, which is promising as an active ingredient of a pharmaceutical composition for treating or preventing incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like, and have found that the benzazepine compounds of the present invention have an excellent 5-HT2C receptor agonist activity, thereby completing the present invention.Type: ApplicationFiled: March 9, 2011Publication date: November 3, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Hiroyuki KOSHIO, Norio ASAI, Taisuke TAKAHASHI, Takafumi SHIMIZU, Yasuhito NAGAI, Keiko KAWABATA, Karl Bruce THOR
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Patent number: 8048895Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.Type: GrantFiled: April 18, 2008Date of Patent: November 1, 2011Assignee: Research Triangle InstituteInventors: Frank Ivy Carroll, Hernan A. Navarro, James B. Thomas, Tingwei Cai
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Patent number: 7994314Abstract: The invention relates to the preparation of mirtazapine precursors and mirtazapine preferably having a substantial enantiomeric excess.Type: GrantFiled: April 7, 2008Date of Patent: August 9, 2011Assignee: N.V. OrganonInventors: Gerardus Johannes Kemperman, Johannes Paulus Gerardus Seerden
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Publication number: 20110160451Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: March 8, 2011Publication date: June 30, 2011Inventors: Hui CAI, Frank CHAVEZ, James P. EDWARDS, Anne E. FITZGERALD, Jing LIU, Neelakandha S. MANI, Danielle K. NEFF, Michele C. RIZZOLIO, Brad M. SAVALL, Deborah M. SMITH, Jennifer D. VENABLE, Jianmei WEI, Ronald L. WOLIN
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Patent number: 7956066Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: GrantFiled: February 8, 2007Date of Patent: June 7, 2011Assignee: Janssen Pharmaceutica NVInventors: Daniel J. Buzard, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20110118231Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: ApplicationFiled: November 19, 2010Publication date: May 19, 2011Applicants: ABBOTT LABORATORIES, ABBOTT GMBH & CO. KGInventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
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Publication number: 20100240637Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, R20, X, Y, Q and Z have defined meanings.Type: ApplicationFiled: September 18, 2008Publication date: September 23, 2010Applicant: JANSSEN PHARMACEUTICAL NVInventors: Virginie Sophie Poncelet, Sophie Coupa, Pierre-Henri Storck, Bruno Schoentjes
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Patent number: 7790709Abstract: In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl.Type: GrantFiled: December 5, 2003Date of Patent: September 7, 2010Assignee: Affinium Pharmaceuticals, Inc.Inventors: Judd M. Berman, Peter Sampson, Heinz W. Pauls, Jailall Ramnauth, David Douglas Manning, Matthew D. Surman, Dejian Xie, Helene Y. Decornez
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Patent number: 7749994Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.Type: GrantFiled: August 14, 2006Date of Patent: July 6, 2010Assignees: Genentech, Inc., Hoffman-LaRoche, Inc. (US Only), F. Hoffman-LaRoche, AG (EX-US)Inventors: Thomas E. Rawson, Brian Safina, Jennafer Dotson, Aihe Zhou, Ignacio Aliagas-Martin, Jason Halladay, Jun Liang, Matthias Rueth, Bing-Yan Zhu, Frederick Brookfield, Michael Prime, Birong Zhang, Jun M. Li
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Publication number: 20100130420Abstract: The present invention provides novel chimeric receptors that have unique pharmacology. In particular, the chimeric receptors comprise a mutated ligand binding domain of the ?7 nicotinic acetylcholine receptor fused to a transmembrane or channel domain from a ligand-gated ion channel protein. The mutations in the ligand binding domain confer selective binding of compounds. Methods of using the novel chimeric receptors of the invention as well as compounds that preferentially bind and activate the chimeric receptors are also disclosed.Type: ApplicationFiled: October 9, 2009Publication date: May 27, 2010Applicant: Howard Hughes Medical InstituteInventors: Scott STERNSON, Loren Looger, Peter Lee
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Patent number: 7718648Abstract: This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.Type: GrantFiled: August 6, 2007Date of Patent: May 18, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher F. Claiborne, Todd B. Sells, Stephen G. Stroud
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Patent number: 7704991Abstract: This invention relates to novel substituted diazabicyclo derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: GrantFiled: April 3, 2006Date of Patent: April 27, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Elsebet Østergaard Nielsen, John Paul Redrobe
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Publication number: 20090270370Abstract: Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: ApplicationFiled: July 2, 2009Publication date: October 29, 2009Inventors: Nicholas I. Carruthers, Wenying Chai, Xiaohu Deng, Curt A. Dvorak, Annette K. Kwok, Jimmy T. Liang, Neelakandha Mani, Dale A. Rudolph, Victoria D. Wong
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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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Publication number: 20090062255Abstract: The invention relates to a method for evaluating a chemotherapeutic potential of a candidate molecule. In evaluating the candidate molecule, the candidate molecule is tested for its ability to inhibit the in vitro growth of a cancer cell; to bind a cellular receptor produced by a cancer cell, wherein said receptor, such as a peripheral benzodiazepine receptor, is produced in a greater amount by said cancer cell than by a normal cell; and to inhibit the activity of at least one protein member of the MAPK pathway. The invention further relates to dibenzodiazepinone analogues and derivatives thereof.Type: ApplicationFiled: August 15, 2008Publication date: March 5, 2009Applicant: THALLION PHARMACEUTICALS INC.Inventors: Henriette GOURDEAU, Pierre FALARDEAU, My-Anh WIOLAND, Nadia BOUFAIED, James B. MCALPINE, Mustapha AOUIDATE, Thierry BERTOMEU, Ashraf IBRAHIM
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Publication number: 20090005556Abstract: Disclosed is a process for producing pure form of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine. The process comprises of reacting 2-(2-aminoanilino)-5-methylthiophene-3-carbonitrile with N-methyl piperazine in conjunction with N-methylpiperazine acid salt, to produce 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine. Also disclosed is a process for obtaining the Polymorphic Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine by crystallizing the crude 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine in a mixture of solvents.Type: ApplicationFiled: July 14, 2004Publication date: January 1, 2009Inventors: Jwalant Ashesh Shastri, Akshat Bhatnagar, Rajesh Kumar Thaper, Sushil Kumar Dubey
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Patent number: 7465722Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturatedType: GrantFiled: August 11, 2006Date of Patent: December 16, 2008Assignee: WyethInventors: Amedeo A. Failli, John P. Dusza, Thomas J. Caggiano, Jay S. Shumsky, Kevin A. Memoli, Eugene J. Trybulski
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Publication number: 20080293694Abstract: The present invention relates to novel compounds of formula (I): wherein R1, R2, R3, R4, and R5 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: ApplicationFiled: March 13, 2008Publication date: November 27, 2008Applicant: Biovitrum AB (publ.)Inventors: Johan Angbrant, Peter Brandt, Rune Ringom, Bengt Lindqvist
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Patent number: 7456567Abstract: An organic electroluminescent device having a pair of electrodes, and at least one organic layer interposed between the pair of electrodes, with the organic layer containing at least one compound represented by formula (1): wherein L11, L13, and L14 each independently represent an o-arylene group, an o-heteroarylene group, or a vinylene group; L12 represents an o-arylene group, an o-heteroarylene group, a vinylene group, or an ethylene group; and L15 represents a trivalent or higher aromatic ring or a trivalent or higher aromatic heterocyclic ring; and a compound represented by formula (2): wherein L21, L22, L23, L24, and L25 each independently represent a group necessary for forming an aromatic ring or a group necessary for forming an aromatic heterocyclic ring; and a method for producing a compound represented by formula (2).Type: GrantFiled: September 12, 2005Date of Patent: November 25, 2008Assignee: Fujifilm CorporationInventor: Jun Ogasawara
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Publication number: 20080280882Abstract: This invention relates to novel substituted diazabicyclo derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: April 3, 2006Publication date: November 13, 2008Applicant: NEUROSEARCH A/SInventors: Dan Peters, Elsebet Ostergaard Nielsen, John Paul Redrobe
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Patent number: 7407949Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.Type: GrantFiled: February 12, 2004Date of Patent: August 5, 2008Assignee: Ferring B.V.Inventors: Peter Hudson, Andrzej Roman Batt, Celine Marguerite Simone Heeney, Andrew John Baxter, Michael Bryan Roe, Peter Andrew Robson
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Patent number: 7329653Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.Type: GrantFiled: April 11, 2006Date of Patent: February 12, 2008Assignee: WyethInventors: Amedeo A. Failli, Jay S. Shumsky, Thomas J. Caggiano, John P. Dusza, Kevin A. Memoli
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Patent number: 6974824Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors relative to nor-BNI, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.Type: GrantFiled: January 8, 2001Date of Patent: December 13, 2005Assignee: Research Triangle InstituteInventors: F. Ivy Carroll, James B. Thomas, S. Wayne Mascarella
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Patent number: 6875867Abstract: A process is provided for preparing chiral diol sulfones of the structure where R3 is preferably where R4a is preferably aryl such as phenyl, and R1a is preferably alkyl such as t-butyl, which are intermediates used in preparing HMG CoA reductase inhibitors.Type: GrantFiled: May 30, 2002Date of Patent: April 5, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Paul R. Brodfuehrer, Thomas R. Sattelberg, Joydeep Kant, Xinhua Qian
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Publication number: 20040248879Abstract: Pharmaceutically acceptable salts of compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.Type: ApplicationFiled: March 29, 2004Publication date: December 9, 2004Applicant: Agouron Pharmaceuticals, Inc.Inventors: Stacie Canan-Koch, Jan-Jon Chu, Jia Liu, Jean Matthews
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Publication number: 20040248880Abstract: The present invention discloses radioligands of 9-arylsulfone of the formula (X) 1Type: ApplicationFiled: April 12, 2004Publication date: December 9, 2004Inventors: Eric Jon Jacobsen, Kalpana M. Merchant
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Publication number: 20040242623Abstract: The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof: 1Type: ApplicationFiled: July 29, 2004Publication date: December 2, 2004Inventors: Romano Difabio, Collin F. Regan, Yves St-Denis, Fabrizio Micheli, Michael K. Schwaebe
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Patent number: 6815440Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.Type: GrantFiled: March 3, 2003Date of Patent: November 9, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
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Publication number: 20040204398Abstract: Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: February 27, 2004Publication date: October 14, 2004Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
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Patent number: 6800656Abstract: The present invention provides a compound of the formula and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. Wherein: X=O, (CH2)m, S, SO, SO2, NH, NR8; Y=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Z=NH, O, NR8, S, SO, SO2; The remaining substituents are described in the specification.Type: GrantFiled: July 5, 2002Date of Patent: October 5, 2004Assignee: Warner Lambert CompanyInventors: Richard John Booth, Vara Prasad Venkata Nagendra Josyula, Annette Lynn Meyer, Bruce Allan Steinbaugh
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Patent number: 6765004Abstract: The invention is directed to tricyclic indoloazepine compounds useful as vasopressin receptor antagonists, pharmaceutical compositions comprising the compounds of the present invention and methods of treating conditions involving increased vascular resistance and cardiac insufficiency which include hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis or water retention in a subject in need thereof.Type: GrantFiled: June 12, 2000Date of Patent: July 20, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: William J. Hoekstra, Michael N. Greco, Leonard R. Hecker, Bruce E. Maryanoff, Jay M. Matthews
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Publication number: 20040058906Abstract: The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: ApplicationFiled: August 27, 2003Publication date: March 25, 2004Applicant: Schering CorporationInventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee, Thavalakulam K. Sasikumar
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Publication number: 20040038963Abstract: The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.Type: ApplicationFiled: November 12, 2002Publication date: February 26, 2004Inventor: Jiabing Wang
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Patent number: 6693101Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.Type: GrantFiled: January 23, 2001Date of Patent: February 17, 2004Assignee: Merck & Co., Inc.Inventors: Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
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Publication number: 20040023947Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.Type: ApplicationFiled: May 27, 2003Publication date: February 5, 2004Applicant: X-Ceptor Therapeutics Inc.Inventors: Richard Martin, Tie-Lin Wang, Brenton T. Flatt, Xiao-Hui Gu, Ronald Griffith
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Publication number: 20040019037Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.Type: ApplicationFiled: July 10, 2003Publication date: January 29, 2004Inventors: Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
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Publication number: 20030216568Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.Type: ApplicationFiled: December 12, 2002Publication date: November 20, 2003Applicant: WOCKHARDT LIMITEDInventors: Noel John De Souza, Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Shiv Kumar Agarwal, Kandepu Sreenivas, Sheela Chandrasekharan Nair, Yati Chugh, Milind Chintaman Shukla
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Patent number: 6627636Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.Type: GrantFiled: December 4, 2001Date of Patent: September 30, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl