Tricyclo Ring System Having The Seven-mmbered Hetero Ring As One Of The Cyclos Patents (Class 514/211.11)
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Publication number: 20080261950Abstract: Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The compounds of the invention are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.Type: ApplicationFiled: February 4, 2008Publication date: October 23, 2008Applicant: CoLucid Pharmaceuticals, Inc.Inventors: Nadia M. J. Rupniak, James F. White, Kazumi Shiosaki, J. David Leander, Shoucheng Du, Daniel J. Coughlin
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Patent number: 7429577Abstract: The present invention relates to pharmaceutical compositions comprising an antipsychotic agent in combination with a chromium salt, which are used for minimizing side effects in a patient taking an antipsychotic agent.Type: GrantFiled: November 9, 2004Date of Patent: September 30, 2008Assignee: Comprehensive Neuroscience, Inc.Inventor: John Docherty
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Publication number: 20080207590Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.Type: ApplicationFiled: October 26, 2007Publication date: August 28, 2008Applicant: METHYLGENE INC.Inventors: Robert Deziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
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Publication number: 20080194540Abstract: The invention teaches the use of a tricyclic compound for promoting the endocytotic uptake of macromolecular active ingredients.Type: ApplicationFiled: February 17, 2004Publication date: August 14, 2008Applicant: RINA NETZWERK RNA-TECHNOLOGIEN GMBHInventors: Birgit Neukamm, Christine Lang, Reinhard Gessner
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Publication number: 20080188455Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 29, 2007Publication date: August 7, 2008Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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Publication number: 20070249583Abstract: Compounds are provided of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia and dyslipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis wherein A is chosen from B is chosen from wherein the variables R1 to R7, m, n, are as defined herein. A method for treating the above diseases employing the above compounds is also provided.Type: ApplicationFiled: April 24, 2007Publication date: October 25, 2007Inventors: Philip D. Stein, Steven P. Seitz, David J. Carini, Yan Shi, Jeffrey A. Robl, Jay A. Markwalder, Chunhong He
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Patent number: 7235541Abstract: The present application relates to internally cyclized naphthamide compounds of the formula Ia (wherein R1a, R1b, R1c, R2, R3, R4, R5, R6, R7, R8, X1, X2, Y, Z, and n are as defined herein), which are useful, for example, for antagonizing the pharmacological actions of the neurokinin 1 (NK1) receptor.Type: GrantFiled: January 24, 2005Date of Patent: June 26, 2007Assignee: Astrazeneca ABInventors: Jeffrey Scott Albert, Peter Bernstein, Cyrus Ohnmacht, Jr., Keith Russell, Ashokkumar Bhikkappa Shenvi
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Patent number: 7229984Abstract: Compounds of the Formula I: wherein m, n, k, A, X, Y, Z, Ar, R1, R2, R3, and R4 are as defined herein. The compounds are useful as 5-HT6 receptor antagonists. Also provided are compositions comprising, methods of using, and methods of making the subject compounds.Type: GrantFiled: December 9, 2005Date of Patent: June 12, 2007Assignee: Roche Palo Alto LLCInventors: Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
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Patent number: 7041661Abstract: The invention relates to the use of compound of Formula I in treating patients for inflammatory or neuropathic pain as well as various symptoms of multiple sclerosisType: GrantFiled: December 16, 2003Date of Patent: May 9, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Bin Zhu, Joseph Wettstein, Margaret A. Petty
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Patent number: 6989379Abstract: This invention is directed to triazine derivatives, bicyclic compounds and tricyclic compounds which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. This invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.Type: GrantFiled: April 21, 2000Date of Patent: January 24, 2006Assignee: H. Lundbick A/SInventors: Mohammad R. Marzabadi, Wai C. Wong, Stewart A. Noble, Manesh N. Desai
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Patent number: 6943156Abstract: The present invention relates to a novel dibenzoxazepine derivative, its synthesis, and its use as an ?v integrin receptor antagonist. More particularly, the compound of the present invention is an antagonist of the integrin receptors ?v?3 and ?v?5 and therefor useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, artheroscietosis, inflammatory arthritis, cancer and metastatic tumor growth.Type: GrantFiled: October 19, 2001Date of Patent: September 13, 2005Assignee: Merck & Co., IncInventor: Michael A. Patane
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Patent number: 6908926Abstract: Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial. These imidazoles compounds have the formula I wherein R1, R2, R3, R4, R5, R6, A, X, Y and Z are as defined in the specification.Type: GrantFiled: April 12, 2000Date of Patent: June 21, 2005Assignee: Novo Nordisk A/SInventors: Florencio Zaragoza Dörwald, Knud Erik Andersen, Tine Krogh Jørgensen, Bernd Peschke, Birgitte Schjellerup Wulff, Ingrid Pettersson, Klaus Rudolf, Dirk Stenkamp, Rudolf Hurnaus, Stephan Georg Müller, Bernd Krist
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Patent number: 6900315Abstract: The present invention relates to novel compounds, compositions and methods for inhibiting the growth, elaboration and/or replication of HIV in human patients and to the prevention and treatment of human acquired immunodeficiency syndrome (AIDS) and other diseases caused by retroviral infection. More particularly, in preferred aspects, the present invention provides a method for the use of novel prodrug forms of 9-(2,3-Dideoxy-?-D-glycero-pent-2-enofuranosyl) guanine (d4G) for the prevention and treatment of both wild type and drug-resistant Human Immunodeficiency Virus (HIV), the causative pathogen of AIDS. Compounds according to the present invention are based upon the chemical formula: where X is OCH3, N3, NHCH3, N(CH3)2 or an aminocyclopropyl group; R1 is H or a C1 to C20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; and R2 is H or a C1 to C20 acyl or alkyl group.Type: GrantFiled: February 5, 2002Date of Patent: May 31, 2005Assignees: Yale University, University of Georgia Research Foundation, Inc.Inventors: Karen S. Anderson, Adrian Staffin Ray, Chung K. Chu, Yang Zhenjun
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Patent number: 6846814Abstract: Compounds having the general formula wherein R1a, R1b, R1c, R2, R3, R4, R5, R6, R7, R8, X1, X2, Y, Z and n are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: April 5, 2001Date of Patent: January 25, 2005Assignee: Astra Zeneca ABInventors: Jeffrey Scott Albert, Peter Bernstein, Cyrus Ohnmacht, Jr., Keith Russell, Ashokkumar Bhikkappa Shenvi
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Patent number: 6831077Abstract: The present invention relates to pharmaceutical compositions comprising an atypical antipsychotic agent in combination with a chromium salt, which are used for treating atypical depression, as well as minimizing side effects in a patient taking an atypical antipsychotic agent.Type: GrantFiled: July 25, 2002Date of Patent: December 14, 2004Assignee: Comprehensive Neuroscience, Inc.Inventor: John Docherty
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Publication number: 20040110742Abstract: The present invention provides dihydrodiaryloxazepine derivative represented by the following formula [1], analogs thereof and pharmaceutical compositions containing them. Those compounds have an excellent effect of improving functional diseases of gastrointestinal tracts.Type: ApplicationFiled: December 1, 2003Publication date: June 10, 2004Applicant: Ajinomoto Co., Inc.Inventors: Katsutoshi Sakata, Takashi Tsuji, Munetaka Tokumasu, Kazuyoshi Takahashi, Shigeo Hirasawa, Junko Ezaki
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Patent number: 6710041Abstract: A compound of formula (I): where: R=H, Cl, Br, F, I, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, or C5-C6 cycloalkyl; R1 =C1-C4 dialkylamine, where the alkyl groups are the same or different from one another, 4-alkyl-1-piperazinyl, 4-hydroxyalkyl-1-piperazinyl, 1-imidazolyl, 4-alkyl-1-piperidinyl, or 4-alkyl-1-homopiperazinyl; R2 =H, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, CHO, or CH=NOH; R3 =H, CHO; or the pharmaceutically acceptable salts thereof.Type: GrantFiled: February 3, 2003Date of Patent: March 23, 2004Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Patrizia Minetti, Assunta Di Cesare, Domenico Mastroianni, Giuseppe Campiani, Vito Nacci
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Publication number: 20040048847Abstract: An agent for increasing the sugar-transporting capacity and an agent for preventing and/or treating diabetes, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, impaired glucose tolerance or adiposis, which contains a lactam compound or a pharmaceutically acceptable salt thereof as the active ingredient.Type: ApplicationFiled: June 2, 2003Publication date: March 11, 2004Applicant: AJINOMOTO CO. INCInventors: Yukio Iino, Takao Ikenoue, Nobuo Kondo, Hiroyuki Matsueda, Toshihiro Hatanaka, Ryusuke Hirama, Yoko Masuzawa, Fumio Ohta, Akiyo Yamazaki
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Publication number: 20040038962Abstract: Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9-11) are new. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.Type: ApplicationFiled: June 13, 2003Publication date: February 26, 2004Inventors: Doreen Ashworth, Gary R W Pitt, Peter Hudson, Christopher Yea, Richard J Franklin, Graeme Semple, David Paul Jenkins
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Publication number: 20040029860Abstract: The present invention relates to methods for the treatment of diseases associated with hyper-proliferation of cells by administering to a subject in need a therapeutically effective amount of at least one psychotropic agent. Specific proliferative diseases against which psychotropic agents were found to be effective are cancer, including multi-drug resistant cancer and diseases associated with hyper-proliferation of the skin cells, such as psoriasis and hyperkeratosis.Type: ApplicationFiled: September 16, 2003Publication date: February 12, 2004Inventors: Irit Gil-Ad, Abraham Weizman
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Publication number: 20040019035Abstract: The present invention relates to a novel dibenzoxazepine derivative, its synthesis, and its use as an &agr;v integrin receptor antagonist. More particularly, the compound of the present invention is an antagonist of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;5 and therefor useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, artheroscietosis, inflammatory arthritis, cancer and metastatic tumor growth.Type: ApplicationFiled: April 23, 2003Publication date: January 29, 2004Inventor: Michael A Patane
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Publication number: 20030219718Abstract: Compounds that bind S100 and inhibit the S100-p53 protein-protein interaction and activate the tumor suppressor activity of p53, and thus which have an antineoplastic effect are disclosed, as well as methods for identifying these compounds, compositions comprising the same, and methods of using the same to treat cancer.Type: ApplicationFiled: March 27, 2003Publication date: November 27, 2003Applicant: UNIVERSITY OF MARYLAND, BALTIMOREInventors: David J. Weber, Joseph Markowitz, France Carrier, Alexander D. MacKerell
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Patent number: 6642222Abstract: The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.Type: GrantFiled: May 3, 2000Date of Patent: November 4, 2003Assignee: Abbott LaboratoriesInventors: William A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
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Publication number: 20030096805Abstract: Methods and compositions of antidepressants and analogs thereof for inducing local long-lasting anesthesia and analgesia are provided. The methods and compositions are useful for alleviating acute and chronic pain, particularly useful for treating a localized pain.Type: ApplicationFiled: April 4, 2002Publication date: May 22, 2003Inventors: Ging Kuo Wang, Peter Gerner, Donald K. Verrecchia
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Patent number: 6537987Abstract: This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, anti-Alzheimer's agents or anti-acne agents.Type: GrantFiled: December 18, 1998Date of Patent: March 25, 2003Assignee: Pfizer Inc.Inventors: Ernest S. Hamanaka, Cheryl M. Hayward
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Publication number: 20030055035Abstract: 1Type: ApplicationFiled: May 3, 2000Publication date: March 20, 2003Inventors: Willilam A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
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Patent number: 6528504Abstract: The present invention provides (R)-5,11-dihydro-5-[1-(4-methoxyphenethyl)piperidine-2-ylmethyl]dibenzo[b,e][1,4]oxazepine, (R)-5,11-dihydro-5-[1-(4-dimethylaminophenethyl)piperidine-2-ylmethyl]dibenzo[b,e][1,4]oxazepine, compounds analogous to them and pharmaceutical compositions containing such a compound. These compounds are useful for treating or preventing abnormal motor functions of gastrointestinal tracts, particularly irritable bowel syndrome.Type: GrantFiled: July 9, 2001Date of Patent: March 4, 2003Assignee: Ajinomoto Co., Inc.Inventors: Katsutoshi Sakata, Takashi Tsuji, Noriko Sasaki, Kazuyoshi Takahashi
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Patent number: 6476017Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R1 represents hydrogen atom or a C1-6 alkyl group; R2 and R3 independently represent a hydrogen atom or a C1-6 alkyl group, or R2 and R3 may combine together to represent a 5- or 6-membered cycloalkyl group; R4 represents, for example, a hydrogen atom or a C1-6 alkyl group; R5 represents, for example, a hydrogen atom or a C1-6 alkyl group; R6 represents a hydrogen atom or a C1-6 alkyl group; X represents —NR7—, —O—, —CHR7— or —S— in which R7 represents, for example, a hydrogen atom or a C1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.Type: GrantFiled: April 20, 2001Date of Patent: November 5, 2002Assignee: Institute of Medicinal Molecular Design, Inc.Inventor: Koichi Shudo
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Publication number: 20020156052Abstract: Methods and pharmaceutical compositions for the treatment of pain, preferably with lowered risk of induction of seizure in a patient.Type: ApplicationFiled: November 16, 2001Publication date: October 24, 2002Inventors: Robert DeHaven, Erin Gauntner, Patrick Little, Wei Y. Zhang
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Patent number: 6436922Abstract: Disclosed are 5,11-Dihydrodibenzo[b,e][1,4]oxazepine derivatives such as (R)-(+)-5,11-dihydro-5-[1-(4-methoxyphenethyl)-2-pyrrolidinylmethyl]dibenzo[b,e][1,4]oxazepine and (R)-(+)-5,11-dihydro-5-[1-(4-fluorophenethyl)-2-pyrrolidinylmethyl]dibenzo[b,e][1,4]oxazepine, stereoisomers thereof, pharmacologically acceptable salts thereof, or hydrates thereof and a pharmaceutical composition conating the 5,11-Dihydrodibenzo[b,e][1,4]oxazepine derivatives. The derivatives have an excellent activity of improving a digestive tract moving function and are free of side effect.Type: GrantFiled: June 19, 2000Date of Patent: August 20, 2002Assignee: Ajinomoto Co., Inc.Inventors: Yuji Tanaka, Keiji Misumi, Yoshinari Kawakami, Masahiko Moriguchi, Kazuyoshi Takahashi, Hiroki Okamoto, Toshiaki Kamisaki, Kimihiro Inoue, Makoto Sato
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Publication number: 20020099047Abstract: The present invention provides (R)-5,11-dihydro-5-[1-(4-methoxyphenethyl)piperidine-2-ylmethyl]dibenzo[b,e][1,4]oxazepine, (R)-5,11-dihydro-5-[1-(4-dimethylaminophenethyl)piperidine-2-ylmethyl]dibenzo[b,e][1,4]oxazepine, compounds analogous to them and pharmaceutical compositions containing such a compound. These compounds are useful for treating or preventing abnormal motor functions of gastrointestinal tracts, particularly irritable bowel syndrome.Type: ApplicationFiled: July 9, 2001Publication date: July 25, 2002Applicant: Ajinomoto Co., Inc.Inventors: Katsutoshi Sakata, Takashi Tsuji, Noriko Sasaki, Kazuyoshi Takahashi
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Publication number: 20020094975Abstract: Methods and compositions of tricyclic antidepressants for inducing local long-lasting anesthesia and analgesia are provided. The methods and compositions are useful for alleviating acute and chronic pain, particularly useful for treating a localized pain.Type: ApplicationFiled: September 26, 2001Publication date: July 18, 2002Applicant: The Brigham and Woman's Hospital, Inc.Inventors: Ging Kuo Wang, Peter Gerner
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Patent number: 6417180Abstract: The invention relates to antimicrobial compounds which interact with zinc in a zinc finger of a bacterial DNA polymerase, methods of screening for such compounds, and methods of using such compounds to inhibit polymerase activity or bacterial growth.Type: GrantFiled: October 7, 1998Date of Patent: July 9, 2002Assignee: University of MassachusettsInventors: Neal C. Brown, Marjorie H. Barnes, George E. Wright
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Publication number: 20020045610Abstract: The present invention relates to the use of N-substituted azaheterocyclic compounds or salts thereof, for the treatment of conditions related to angiogenesis.Type: ApplicationFiled: June 1, 2001Publication date: April 18, 2002Inventors: Anker Jon Hansen, Tine Krogh Jorgensen, Uffe Bang Olsen
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Patent number: 6362176Abstract: Disclosed are methods of treating rheumatoid arthritis by coadministering synergistic effective amounts of pentostatin and methotrexate to a host in need thereof, and kits and compositions that include pentostatin and methotrexate.Type: GrantFiled: July 20, 2000Date of Patent: March 26, 2002Assignee: Super Gen, Inc.Inventor: Daniel A. Albert
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Publication number: 20020010171Abstract: The present invention relates to compounds of the general formula (I) 1Type: ApplicationFiled: June 11, 2001Publication date: January 24, 2002Inventors: Lone Jeppesen, Per Sauerberg, Anthony Murray, Paul Stanley Bury
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Publication number: 20010039272Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R1 represents hydrogen atom or a C1-6 alkyl group; R2 and R3 independently represent a hydrogen atom or a C1-6 alkyl group, or R2 and R3 may combine together to represent a 5- or 6-membered cycloalkyl group; R4 represents, for example, a hydrogen atom or a C1-6 alkyl group; R5 represents, for example, a hydrogen atom or a C1-6 alkyl group; R6 represents a hydrogen atom or a C-1-6 alkyl group; X represents —NR7—, —O—, —CHR7— or —S— in which R7 represents, for example, a hydrogen atom or a C1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.Type: ApplicationFiled: April 20, 2001Publication date: November 8, 2001Inventor: Koichi Shudo
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Publication number: 20010029256Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: March 14, 2001Publication date: October 11, 2001Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6235730Abstract: 3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases.Type: GrantFiled: October 26, 1999Date of Patent: May 22, 2001Assignee: Japan Tobacco, Inc.Inventors: Motohide Sato, Takeo Katsushima, Hajime Kinoshita
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Patent number: 6214820Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 19, 1999Date of Patent: April 10, 2001Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6191140Abstract: The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.Type: GrantFiled: October 20, 1999Date of Patent: February 20, 2001Assignee: Abbott LaboratoriesInventors: William A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort