Tricyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/547)
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Patent number: 9532959Abstract: Methods and compositions for reducing frequency of urination are disclosed. The methods comprise administering to a subject having a condition that resulting in undesired frequency of urination an effective amount of a pharmaceutical composition comprising one or more prostaglandin pathway inhibitors. The pharmaceutical compositions comprise one or more prostaglandin pathway inhibitors and a pharmaceutically acceptable carrier.Type: GrantFiled: June 6, 2014Date of Patent: January 3, 2017Assignee: WELLESLEY PHARMACEUTICALS, LLCInventors: David A. Dill, Frank J. Rauscher, III
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Publication number: 20140288050Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: November 7, 2012Publication date: September 25, 2014Inventors: Scott Malcolm, Carrie Bowen, Laurence Melnick, Linghong Xie
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Publication number: 20140046053Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: October 10, 2013Publication date: February 13, 2014Applicant: THERAVANCE, INC.Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
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Publication number: 20140011988Abstract: 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: February 14, 2013Publication date: January 9, 2014Inventors: Robert Deziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
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Patent number: 8461145Abstract: The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use as pharmacological tools, or as irritant incapacitants, or in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.Type: GrantFiled: December 4, 2008Date of Patent: June 11, 2013Assignee: Janssen Pharmaceutica NVInventors: Henricus Jacobus Maria Gijsen, Marc Hubert Mercken
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Publication number: 20130116238Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: November 8, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: VERTEX PHARMACEUTICALS INCORPORATE
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Publication number: 20110136782Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof (wherein, R1 to R6 each independently represents a hydrogen atom, unsubstituted or substituted C1-20 alkyl group and the like, R1 and R2, R3 and R4, or R5 and R6 may together form an unsubstituted or substituted 5- to 8-membered ring, A-B, in which A represents a carbon atom and B represents a nitrogen atom, represents the formula: C?N and the like, Y represents an oxygen atom and the like, X and X? each independently represent an unsubstituted or substituted C1-20 alkyl group and the like, m represents an integer of 0 to 2, and n represents an integer of 0 to 4), and a fungicide for agricultural and horticultural use that contains at least one of these compounds as an active ingredient thereof, demonstrates reliable effects and can be used safely.Type: ApplicationFiled: August 10, 2009Publication date: June 9, 2011Applicant: Nippon Soda Co., LtdInventors: Akira Mitani, Jun Inagaki, Raito Kuwahara, Masahiro Yokoyama, Kotaro Shibayama, Motoaki Sato
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Publication number: 20110021771Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.Type: ApplicationFiled: November 3, 2008Publication date: January 27, 2011Applicant: METHYLGENE INC.Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Roger Machaalani, Silvana Leit, Patrick Beaulieu, Robert Déziel, John Mancuso
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Publication number: 20100273774Abstract: A compound of formula (I), wherein R, R1, R2, ring A, which ring contains one or two nitrogen atoms, and ring B are as defined in the Specification, pharmaceutical compositions containing these compounds, and uses for these compounds and compositions, in particular, in transplantation.Type: ApplicationFiled: July 9, 2010Publication date: October 28, 2010Inventors: Jürgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
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Publication number: 20100273773Abstract: The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use as pharmacological tools, or as irritant incapacitants, or in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.Type: ApplicationFiled: December 4, 2008Publication date: October 28, 2010Inventors: Henricus Jacobus Maria Gijsen, Marc Hubert Mercken
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Publication number: 20100144703Abstract: 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: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Applicant: 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: 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: 20090227788Abstract: The invention provides a process for preparing a 2,3,4,5-tetrahydro[1,4]benzothiazepine of formula: by reacting a [2-(acylaminoethyl)thio]arene of formula with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reacting the [2-(acylaminoethyl)thio]arene with the aldehyde or multimer thereof and a base to form an [N-hydroxymethyl-2-[acylaminoethyl)thio]arene of formula then treating the [N-hydroxymethyl-2-(acylaminoethyl)thio]arene with the acid to form the 2,3,4,5-tetrahydro[1,4]benzothiazepine.Type: ApplicationFiled: March 3, 2009Publication date: September 10, 2009Inventors: Shixian Deng, Sandro Belvedere, Jiaming Yan, Donald Landry
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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: 20090181942Abstract: The present invention relates to tricyclic compounds each represented by the following formula (I): (wherein, R1, R2, R2?, R3, R4, X, Y and Z have the same meanings as defined in the specification); and a drug containing the compound. Since the compounds according to the present invention exhibit an excellent squalene synthetase inhibitory effect and cholesterol synthesis inhibitory effect so that they are useful as a drug such as preventive and/or remedy for diseases in mammals including humans such as hyperlipemia, e.g., hypercholesterolemia, hypertriglyceridemia, and low HDL cholesterolemia and/or arteriosclerosis.Type: ApplicationFiled: October 23, 2006Publication date: July 16, 2009Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kazuyuki Sugita, Masami Otsuka, Hitoshi Oki, Noriyasu Haginoya, Masanori Ichikawa, Masao Itoh
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Publication number: 20090076262Abstract: The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][1,4]thiazepin-11(10H)-one) with phosphorous oxychloride in the presence of triethylamine in an aromatic organic solvent such as toluene or, preferably, xylene at reflux temperature to obtain an aromatic hydrocarbon solution of 11-chloro-dibenzo[bf][1,4]thiazepine. Thereafter, the 11-chloro-dibenzo[bf][1,4]thiazepine is reacted with 2-(2-piperazin-1-ylethoxy)-ethanol to yield, following several processing steps, quetiapine. Compound I can then be further reacted with fumaric acid at elevated temperature to yield quetiapine fumarate. The resulting quetiapine fumarate obtained is suitable for use in pharmaceutical preparations.Type: ApplicationFiled: April 21, 2006Publication date: March 19, 2009Applicant: MEDICHEM, S.A.Inventors: Jordi Bosch I Llado, Maria Carmen Burgarolas Montero, Iolanda Chamorro Gutierrez
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Publication number: 20080275023Abstract: New N-hydroxyamides of n-alkyl carboxylic acids omega substituted with suitable tricyclic systems characterised by a central 7-membered ring, having activity as inhibitors of histone deacetylase (HDAC).Type: ApplicationFiled: March 13, 2006Publication date: November 6, 2008Inventors: Antonio Guidi, Tula Dimoulas, Danilo Giannotti, Nicholas Harmat
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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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Publication number: 20080241949Abstract: Provided is an improved synthesis of quetiapine and pharmaceutically acceptable salts.Type: ApplicationFiled: March 31, 2008Publication date: October 2, 2008Inventors: Vinod Kumar Kansal, Suhail Ahmad, Kanhaiya Lal, Bhatu Tumba Patil
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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: 20080200671Abstract: The invention relates to an orthorhombic crystal form of compound trans-5-chloro-2,3,3a, 12b-tetrahydro-2-methyl-1H-dibenz [2,3:6,7] oxepino [4,5-c] pyrrole (Z)-2-butenedioate, to methods for the preparation of this crystal form and to pharmaceutical compositions comprising an orthorhombic crystal form.Type: ApplicationFiled: November 13, 2007Publication date: August 21, 2008Applicant: N.V. OrganonInventor: Gerhardus Johannes Heeres
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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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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: 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: 7078521Abstract: A process is described for the preparation of compounds with the following formula where the groups are as defined below; in particular, R1 is a substituted amine; said process includes essentially the reaction of pyrrolobenzothiazepin-9-one with amine R1H to give the corresponding enamine, which is subsequently transformed into the final compoundType: GrantFiled: July 20, 2001Date of Patent: July 18, 2006Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Patrizia Minetti, Domenico Mastrojanno
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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: 6887838Abstract: Formulation components such as bleach boosting compounds selected from the group consisting of bleach boosters comprising quaternary imine cations, zwitterions, polyions having a net charge of from about +3 to about 3 and mixtures thereof, bleaching species comprising oxariridinium cations, zwitterions, polyions having a net charge of from about +3 to about ?3 and mixtures thereof, and mixtures thereof are disclosed. The bleach boosting compounds increase bleaching effectiveness even in lower temperature solutions and provides improved stability toward unwanted boosting compound decomposition. The bleach boosting compounds are ideally suited for inclusion into bleaching compositions including those with detersive surfactants and enzymes. Also provided is a method for laundering a fabric employing the bleach compounds, a laundry additive product employing the bleach boosting compounds.Type: GrantFiled: May 26, 2004Date of Patent: May 3, 2005Assignee: Procter & Gamble CompanyInventors: Robert Richard Dykstra, Gregory Scot Miracle
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Patent number: 6887868Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.Type: GrantFiled: September 19, 2002Date of Patent: May 3, 2005Assignee: Pharmacia & Upjohn CompanyInventor: Jian-Min Fu
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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: 6806267Abstract: The present invention relates to pyrrolobenzoxazepines, pyrrolobenzthiazepines and related compounds having the ability to induce apoptosis, to pharmaceutical compositions comprising these compounds and to their use as anti-tumour agents.Type: GrantFiled: February 16, 2000Date of Patent: October 19, 2004Assignees: The Universita'di Siena, The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen Elizabeth Near DublinInventors: David Clive Williams, Daniela M. Zisterer, Vito Nacci, Giuseppe Campiani
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Patent number: 6794391Abstract: The invention provides compounds or salts thereof of the general formula (I): wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; X represents OCH2 or a group CR3R4; wherein each of R3 or R4 independently represents a hydrogen atom or a C1-3 alkyl group; R5 represents a hydrogen atom or a C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl group; R6 represents a hydrogen atom or a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, amino, C1-6 alkylamino, di(C1-6) alkylamino or C2-7 acylamino group; each of R7 and R8 independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkylthio, C1-6 alkoxy, C3-6 cycloalkyl; and R9 represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkylthio, C1-6 alkoxy or C3-6 cycloalkyl group. The compounds or salts thereof are useful for treatment of respiratory disorders such as asthma.Type: GrantFiled: September 26, 2001Date of Patent: September 21, 2004Assignee: Vernalis LimitedInventors: Alexander William Oxford, David Jack
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Publication number: 20040167118Abstract: The invention relates to a compound represented by the following general formula (1) or its analogue, which selectively inhibit N-type calcium channels or its analogue, and to a method for treating pain etc.Type: ApplicationFiled: February 27, 2004Publication date: August 26, 2004Applicant: AJINOMOTO CO., INC.Inventors: Takashi Yamamoto, Seiji Niwa, Kayo Otani, Seiji Ohno, Hajime Koganei, Satoshi Iwayama, Akira Takahara, Yukitsugu Ono, Tomoko Takeda, Shinichi Fujita, Keiko Moki
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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: 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: 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: 20030186959Abstract: Compounds with formula (I) are described where the groups are as defined here below, as well as processes for their preparation, pharmaceutical compositions containing them and their use for the preparation of medicaments with antipsychotic activity.Type: ApplicationFiled: February 3, 2003Publication date: October 2, 2003Inventors: Patrizia Minetti, Assunta Di Cesare, Domenico Mastroianni, Giuseppe Campiani, Vito Nacci
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Publication number: 20030181437Abstract: A process is described for the preparation of compounds with the following formula where the groups are as defined below; in particular, R1 is a substituted amine; said process includes essentially the reaction of pyrrolobenzothiazepin-9-one with amine R1H to give the corresponding enamine, which is subsequently transformed into the final compound.Type: ApplicationFiled: February 3, 2003Publication date: September 25, 2003Inventors: Patrizia Minetti, Domenico Mastrojanno
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Patent number: 6624159Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: June 22, 2001Date of Patent: September 23, 2003Assignee: Pharmacia & Upjohn CompanyInventors: David John Anderson, Gordon L. Bundy, Fred L. Ciske, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
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Publication number: 20030171358Abstract: The present invention relates to compounds of the general formula (I) 1Type: ApplicationFiled: January 27, 2003Publication date: September 11, 2003Inventors: Lone Jeppesen, Per Sauerberg, Anthony Murray, Paul Stanley Bury
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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: 20030036542Abstract: The invention provides compounds or salts thereof of the general formula (I): 1Type: ApplicationFiled: September 26, 2001Publication date: February 20, 2003Inventors: Alexander William Oxford, David Jack
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Patent number: 6521769Abstract: Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include chiral C1-C6 TunaPhos ligands. The ruthenium TunaPhos complex reduces ketones to the corresponding alcohols with 95-99.6% enantioselectivity. The transition metal complexes of the chiral ligands are useful in asymmetric reactions such as asymmetric hydrogenation, hydride transfer, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, isomerization, allylic alkylation, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition and epoxidation reactions.Type: GrantFiled: September 19, 2000Date of Patent: February 18, 2003Assignee: The Penn State Research FoundationInventor: Xumu Zhang
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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: 20020151539Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula 1Type: ApplicationFiled: March 14, 2002Publication date: October 17, 2002Inventors: Tine Krogh Jorgensen, Knud Erik Andersen, Rolf Hohlweg, Uffe Bang Olsen, Erik Fischer, Zdenek Polivka, Kaler Sindelar
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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: 20020091090Abstract: Compounds according to the formula A-B-Z-W, whereinType: ApplicationFiled: September 14, 2001Publication date: July 11, 2002Inventors: Bridget M. Cole, Anthony P. Ricketts, Bruce A. Hay
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Patent number: 6387893Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.Type: GrantFiled: September 27, 2000Date of Patent: May 14, 2002Assignee: Merck & Co., Inc.Inventors: Ben E. Evans, Jacob M. Hoffman, Kevin F. Gilbert, Kenneth E. Rittle
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Publication number: 20020055499Abstract: Compounds of the formula (I) are disclosed which are dual fibrinogen receptor and vitronectin receptor antagonists and are useful in the treatment of atherosclerosis, in the prevention of restenosis and in the prevention of tumor metastasis and tumor growth: 1Type: ApplicationFiled: December 12, 2001Publication date: May 9, 2002Inventors: Dirk Heerding, James Martin Samanen
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Publication number: 20020035104Abstract: Provided are compounds of formula (I) 1Type: ApplicationFiled: August 16, 2001Publication date: March 21, 2002Applicant: GENENTECH, INC.Inventors: Dean R. Artis, David Y. Jackson, Thomas E. Rawson, Mark E. Reynolds, Daniel P. Sutherlin, Mark S. Stanley