Chalcogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 540/570)
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Patent number: 8962615Abstract: The described invention relates to compounds (I) which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis. All definitions as in claim 1.Type: GrantFiled: June 29, 2012Date of Patent: February 24, 2015Assignee: University of DundeeInventors: Ana Maria Schor, Seth Lawrence Schor, Rodolfo Marquez, David George Norman
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Patent number: 8791104Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides novel 1,4-benzodiazepine-2,5-dione compounds, and methods of using novel 1,4-benzodiazepine-2,5-dione compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.Type: GrantFiled: May 17, 2013Date of Patent: July 29, 2014Assignee: The Regents of the University of MichiganInventor: Gary D. Glick
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Publication number: 20140171423Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, treat pain; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: December 10, 2013Publication date: June 19, 2014Applicant: ABBVIE INC.Inventors: Pramila A. Bhatia, John T. Randolph, Michael R. Schrimpf, Quinwei I. Zhang
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Patent number: 8673898Abstract: Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.Type: GrantFiled: April 12, 2012Date of Patent: March 18, 2014Assignee: Array BioPharma Inc.Inventors: George A. Doherty, Zachary Jones
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Publication number: 20130324521Abstract: A medical product (1) introducible into a blood vessel (2) comprising a drug (3) for the treatment of an aneurysm and of arteriosclerotic diseases. The drug (3) is a farnesyltransferase inhibitor.Type: ApplicationFiled: November 24, 2011Publication date: December 5, 2013Inventor: Reza Ghotbi
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Publication number: 20130261110Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides novel 1,4-benzodiazepine-2,5-dione compounds, and methods of using novel 1,4-benzodiazepine-2,5-dione compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.Type: ApplicationFiled: May 17, 2013Publication date: October 3, 2013Applicant: The Regents of the University of MichiganInventor: Gary D. Glick
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Publication number: 20120264746Abstract: The described invention relates to compounds (I) which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis. All definitions as in claim 1.Type: ApplicationFiled: June 29, 2012Publication date: October 18, 2012Inventors: Ana Maria Schor, Seth Lawrence Schor, Rodolfo Marquez, David George Norman
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Publication number: 20120232067Abstract: The invention provides 1,4-benzodiazepinone compounds, pharmaceutical compositions, and methods of treating autoimmune disorders, chronic inflammatory disorders, and hyperproliferative disorders. For example, the 1,4-benzodiazepinone compounds and pharmaceutical compositions are contemplated to be useful for treating rheumatoid arthritis, graft-versus-host disease, inflammatory bowel disease, and the like.Type: ApplicationFiled: September 17, 2010Publication date: September 13, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Gary D. Glick, Alexander Ross Hurd, Chad Alan Van Huis
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Publication number: 20120225866Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.Type: ApplicationFiled: August 20, 2010Publication date: September 6, 2012Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kunio Oshima, Shuuji Matsumura, Hokuto Yamabe, Naohiro Isono, Noriaki Takemura, Shinichi Taira, Takashi Oshiyama, Yasuhiro Menjo, Tsuyoshi Nagase, Masataka Ueda, Yasuo Koga, Sunao Nakayama, Kenji Tsujimae, Toshiyuki Onogawa, Kuninori Tai, Motohiro Itotani
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Patent number: 8227504Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.Type: GrantFiled: March 15, 2010Date of Patent: July 24, 2012Assignee: SanofiInventors: Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin
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Publication number: 20100152171Abstract: CGRP antagonists of the formula of which the following are exemplary: (1) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amide, (2) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amide.Type: ApplicationFiled: February 17, 2010Publication date: June 17, 2010Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Klaus RUDOLF, Stephan Georg MUELLER, Dirk STENKAMP, Philipp LUSTENBERGER, Alexander DREYER, Eckhart BAUER, Marcus SCHINDLER, Kirsten ARNDT, Henri DOODS
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Publication number: 20100113391Abstract: [Problem] Provided is a compound, which exhibits a P2Y12 inhibitory action and is useful as a medical drug, particularly, as a platelet aggregation inhibitor. [Means for Solution] The inventors have eagerly investigated P2Y12 inhibitors. As a result, the inventors have found that a bicyclic heterocyclic compound such as quinazolinedione, isoquinolone, and the like having an amino group substituted with lower alkyl, cycloalkyl, or lower alkylene-cycloalkyl at the specific position exhibits an excellent platelet aggregation inhibitory action, thereby completing the present invention. Since the compound of the invention exhibits excellent P2Y12 inhibitory action and platelet aggregation inhibitory action, it is useful as a platelet aggregation inhibitor.Type: ApplicationFiled: April 17, 2008Publication date: May 6, 2010Applicant: Astellas Pharma Inc.Inventors: Yuji Koga, Takao Okuda, Takashi Kamikubo, Michihito Kageyama, Hiroyuki Moritomo
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Methods and compositions for treating diseases and conditions associated with mitochondrial function
Publication number: 20090275099Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, mitochondrial F1F0 ATP hydrolase associated disorders, and the like.Type: ApplicationFiled: March 21, 2007Publication date: November 5, 2009Applicant: Regents of the University of MichiganInventor: Gary D. Glick -
Publication number: 20090208413Abstract: The present invention provides compositions and methods for synthesizing labeled drugs. The present invention further provides methods for preventing or stopping prescription drug abuse for all agents registered as a Drug Enforcement Agency (DEA) schedule II through schedule V medications. According to the present invention, methods are provided for monitoring patient compliance with prescribed drug treatment. The present invention also provides methods for facilitating a replacement prescription when a patient is left without access to their prescribed drug. Furthermore, the present invention provides a method to improve employee compliance with an employer's drug policies via either a voluntary or compulsory system for enhanced drug testing.Type: ApplicationFiled: February 23, 2006Publication date: August 20, 2009Inventors: Alan J Reis, Christian Schafmeister
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Publication number: 20090176770Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: ApplicationFiled: October 6, 2008Publication date: July 9, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Alexander DREYER, Kirsten ARNDT, Henri DOODS, Gerhard SCHAENZLE, Marco SANTAGOSTINO, Fabio PALEARI
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Publication number: 20090143361Abstract: The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical compositions which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating central nervous system disorders, obesity, and metabolic disorders.Type: ApplicationFiled: November 25, 2008Publication date: June 4, 2009Applicants: ELBION GMBH, WYETHInventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Hans Stange, Rudolf Schindler, Norbert Hofgen, Ute Egerland, Barbara Langen
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Publication number: 20090143366Abstract: The present invention relates to dihydrobenzodiazepine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dihydrobenzodiazepine derivatives are useful in the treatment of diseases associated with inappropriate ROCK kinase.Type: ApplicationFiled: October 18, 2005Publication date: June 4, 2009Inventors: Michael John Alberti, David Kendall Jung
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Publication number: 20090118244Abstract: The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.Type: ApplicationFiled: November 6, 2008Publication date: May 7, 2009Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventor: Gary D. Glick
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Publication number: 20080221087Abstract: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: ApplicationFiled: April 19, 2007Publication date: September 11, 2008Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANYInventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
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Patent number: 7282496Abstract: Compounds of the formula are useful in treating disease conditions mediated by TNF-?, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, graft rejection, cachexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease and HIV.Type: GrantFiled: November 1, 2002Date of Patent: October 16, 2007Assignee: Wyeth Holdings CorporationInventors: Vincent Premaratna Sandanayaka, Efren Guillermo Delos Santos
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Patent number: 6878821Abstract: The invention concerns a method for chemoselective oxidation of an organic compound comprising several potentially oxidizable groups whereof at least one is a nitrogen group. Said method is characterised in that it consists in using at least a protic solvent, which is a good donor of hydrogen bonds, enabling to limit N-oxidation.Type: GrantFiled: March 22, 2001Date of Patent: April 12, 2005Assignee: Warner-Lambert LLCInventor: Patrick Bernardelli
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Patent number: 6858599Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.Type: GrantFiled: December 27, 2001Date of Patent: February 22, 2005Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
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Patent number: 6140322Abstract: There are provided novel compounds of formula (I) ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the specification and optical isomers and racemates thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy.Type: GrantFiled: January 20, 1999Date of Patent: October 31, 2000Assignee: Astra AktiebolagInventors: James MacDonald, James Matz, William Shakespeare
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Patent number: 6121258Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: August 26, 1997Date of Patent: September 19, 2000Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
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Patent number: 6071903Abstract: Compounds are provided having the following formula: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are defined in the specification, which have matrix metalloproteinase inhibiting activity.Type: GrantFiled: May 26, 1999Date of Patent: June 6, 2000Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Efren G. Delos Santos, Xuemei Du
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Patent number: 5977101Abstract: Vitronectin receptor antagonists having the formula: ##STR1## which are useful for the treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporsis.Type: GrantFiled: December 20, 1996Date of Patent: November 2, 1999Assignee: SmithKline Beecham CorporationInventors: Fadia El-Fehail Ali, William Bondinell, William Francis Huffman, M. Amparo Lago, Richard McCulloch Keenan, Chet Kwon, William Henry Miller, Thomas Nguyen, Dennis T. Takata
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Patent number: 5614543Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: March 25, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
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Patent number: 5580979Abstract: The present invention makes available novel compounds represented by the general formula ##STR1## wherein Y represents a phosphate analog. Which compounds are useful for inhibiting an interaction between a protein containing an SH2 domain and a phophotyrosine-containing polypeptide.Type: GrantFiled: March 15, 1994Date of Patent: December 3, 1996Assignee: Trustees of Tufts UniversityInventor: William W. Bachovchin
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Patent number: 5389631Abstract: Fibrinogen receptor antagonists of the ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets wherein G is: ##STR2## for example, ##STR3##Type: GrantFiled: March 22, 1993Date of Patent: February 14, 1995Assignee: Merck & Co., Inc.Inventors: David A. Claremon, Nigel Liverton
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Patent number: 5175159Abstract: Compounds of Formula I are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for stoppage of labor prepatory to Caesarean delivery.Type: GrantFiled: December 28, 1990Date of Patent: December 29, 1992Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Ben E. Evans, Roger M. Freidinger
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Patent number: 5141735Abstract: Novel substituted 2-amino-5-(1H-pyrrol-2-yl)-3H-1,4-benzodiazepines and compositions containing same for treatment and prophylaxis of viral infections, including HIV infections.Type: GrantFiled: June 18, 1990Date of Patent: August 25, 1992Assignee: Hoffman-La Roche, Inc.Inventors: Anne R. Bellemin, James V. Earley, Ming-Chu Hsu, Steve Yik-Kai Tam
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Patent number: 5142048Abstract: The invention relates to novel intermediate compounds for preparation of novel amino acid derivatives having renin inhibiting activity.Type: GrantFiled: January 8, 1990Date of Patent: August 25, 1992Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Keiji Hemmi, Masahiro Neya, Hiroshi Marusawa, Keisuke Imai, Natsuko Kayakiri, Masashi Hashimoto
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Patent number: 4906630Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of benzodiazinone-pyridazinone and hydroxy-pyrazolyl compounds and pharmaceutical compositions including the same.Type: GrantFiled: October 11, 1988Date of Patent: March 6, 1990Assignee: Rorer Pharmaceutical CorporationInventors: William L. Studt, William C. Faith, Bruce F. Molino
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Patent number: 4877785Abstract: Non-peptidyl compounds characterized generally as .beta.-succinamidoacyl aminodios are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: October 31, 1989Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 4859771Abstract: An economical, one-pot process for resolution-racemization of primary amines with .alpha.-hydrogens via selective crystallization of diastereomeric chiral sulfonic acid salts and the subsequent in situ racemization of the other enantiomer by the catalytic addition of aromatic aldehydes, and a key process intermediate thereof.Type: GrantFiled: January 19, 1989Date of Patent: August 22, 1989Assignee: Merck & Co., Inc.Inventors: Paul J. Reider, Edward J. J. Grabowski
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Patent number: 4820834Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).Type: GrantFiled: March 16, 1987Date of Patent: April 11, 1989Assignee: Merck & Co., Inc.Inventors: Ben E. Evans, Roger M. Freidinger, Mark G. Bock
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Patent number: 4785101Abstract: Benzodiazinone-pyridazinone and -hydroxypyrazolyl compounds possess cardiotonic activity and are included in therapeutic cardiotonic compositions useful in methods for increasing cardiac contractility and for the treatment of congestive heart failure.Type: GrantFiled: June 17, 1987Date of Patent: November 15, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, William C. Faith, Bruce F. Molino
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Patent number: 4755508Abstract: Benzodiazepines of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).Type: GrantFiled: February 27, 1987Date of Patent: July 5, 1988Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Ben E. Evans, Roger M. Freidinger