Chalcogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding (e.g., 4-hydroxy -3-pyrrolidinemethanol, Etc.) Patents (Class 548/556)
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Publication number: 20090257969Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.Type: ApplicationFiled: April 6, 2009Publication date: October 15, 2009Inventor: Nicholas S. Bodor
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Patent number: 7598250Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.Type: GrantFiled: August 4, 2004Date of Patent: October 6, 2009Assignee: Schering CorporationInventors: Jared N. Cumming, Ying Huang, Guoqing Li, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Jianping Pan, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie
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Publication number: 20090234138Abstract: The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.Type: ApplicationFiled: May 27, 2009Publication date: September 17, 2009Inventors: Mark A. Gallop, Fenmei Yao, Maria J. Ludwikow, Thu Phan, Ge Peng
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Publication number: 20090170870Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: December 12, 2008Publication date: July 2, 2009Inventors: YuHua Ji, Craig Husfeld, Rick Lee, YongQi Mu, Cameron Smith
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Publication number: 20090155862Abstract: A process for the preparation of 2-hydroxymethyl-pyrrolidine-3,4-diols of the formulae: including the steps of: a) bioxidation of N-protected aminotetraols of the formula: b) deprotection of the corresponding 5-amino-5-deoxy-pentulose of the formula: and c) hydrogenation of the corresponding 5-amino-5-deoxy-pentulose of the formula:Type: ApplicationFiled: February 18, 2009Publication date: June 18, 2009Inventors: Ulrich KAMPFEN, Eva Maria URBAN, Claus JESSEN, Martin CLAUSEN
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Publication number: 20090105256Abstract: Prodrugs of ion channeling modulating compounds, including, for example, prodrugs of the ion channel modulating compound of the following formula: are described herein, as well as methods of making and using such prodrugs and pharmaceutical compositions containing such prodrugs.Type: ApplicationFiled: March 31, 2005Publication date: April 23, 2009Applicant: Cardiome Pharma Corp.Inventors: Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Adewale Eniale, Bertrand M.C. Plouvier
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Publication number: 20090075954Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.Type: ApplicationFiled: June 12, 2008Publication date: March 19, 2009Inventor: Nicholas S. BODOR
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Patent number: 7504432Abstract: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X? signifies an anion].Type: GrantFiled: January 3, 2007Date of Patent: March 17, 2009Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshio Ogino, Hideki Kurihara, Kenji Matsuda, Tomoshige Numazawa, Norikazu Otake, Kazuhito Noguchi
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Publication number: 20090069404Abstract: The present application describes deuterium-enriched vemakalant, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 31, 2008Publication date: March 12, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090062372Abstract: A glycopyrronium salt such as glycopyrronium iodide has a lower glass transition temperature than glycopyrronium bromide. It is therefore more suitable for formulation.Type: ApplicationFiled: March 20, 2006Publication date: March 5, 2009Inventor: Andrew Douglas Baxter
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Publication number: 20090053721Abstract: The present invention provides novel methods and compositions for identifying ion channel modulating compounds, including atrial-selective antiarrhythmic agents and ion channel modulating compounds that preferentially modulate K+ channels. The ion channel modulating compounds identified according to these methods are associated with a reduced incidence of ventricular proarrhythmia.Type: ApplicationFiled: August 8, 2008Publication date: February 26, 2009Applicant: CARDIOME PHARMA CORP.Inventor: David Fedida
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Publication number: 20090048329Abstract: Provided herein are substituted pyrrolidines that demonstrate binding at biogenic amine transporters and can be synthesized by a methodology based on a chiral dirhodium catalyst. Compositions comprising substituted pyrrolidines can be used to treat central nervous system disorders such as schizophrenia.Type: ApplicationFiled: June 23, 2008Publication date: February 19, 2009Inventor: Huw M.L. Davies
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Publication number: 20090042942Abstract: The invention provides compounds of formula (I), wherein R1, R2, R3, R4, R5, n and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation.Type: ApplicationFiled: April 18, 2006Publication date: February 12, 2009Applicant: ASTRAZENECA ABInventors: Andrew Bailey, David Donald
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Publication number: 20090012120Abstract: An ylide-based aza-Payne rearrangement of 2,3-aziridin-1-ols leads to an efficient process for the preparation of pyrrolidines. The aza-Payne rearrangement under the basic reaction conditions favors the formation of epoxy amines. Subsequent nucleophilic attack of the epoxide by the ylide yields a bis-anion, which upon a 5-exo-tet ring closure yields the desired pyrrolidine, thus completing the relay of the 3-membered the 5-membered nitrogen containing ring system. This process takes place with complete transfer of stereochemical fidelity, and can be applied to sterically hindered aziridinols.Type: ApplicationFiled: May 9, 2007Publication date: January 8, 2009Applicant: Board of Trustees of Michigan State UniversityInventors: Babak Borhan, Jennifer M. Schomaker, Somnath Bhattacharjee, Keith Korthals
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Publication number: 20080292587Abstract: The present invention discloses compounds of formulae I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 24, 2008Publication date: November 27, 2008Inventors: Ying Sun, Yat Sun Or, Zhe Wang
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Publication number: 20080227988Abstract: A method for the production of crystalline glycopyrronium bromide, comprises the reaction of glycopyrronium base with methyl bromide in a solvent, in which the solvent is selected such that the diastereoisomeric ratio of the product favours the R, S and S, R diastereoisomers over the R, R, and S, S diastereoisomers, and separating the desired diastereoisomers by one or more controlled crystallisation steps. This method gives a product having a particle size of narrow distribution.Type: ApplicationFiled: March 3, 2006Publication date: September 18, 2008Inventors: Andrew Douglas Baxter, Kenneth Walter Sinden, Stefan Kleinebekel
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Publication number: 20080214837Abstract: A method of preparing optically pure (S)-3-hydroxypyrrolidine is disclosed. The present invention provides a method of economically and industrially preparing optically and chemically pure (S)-3-hydroxypyrrolidine, through a process comprising introducing an amine protecting group by using optically pure 4-amino-(S)-2-hydroxybutylic acid as a starting material, reducing a carboxylic acid group into a primary alcohol, removing the amine protecting group to form an amine salt, halogenating the primary alcohol, and amine cyclization; and through a simple purification process, i.e., distillation under reduced pressure. As another method, the present invention provides a method of preparing optically and chemically pure (S)-3-hydroxypyrrolidine, through a process comprising esterifying optically pure 4-amino-(S)-2-hydroxybutylic acid as a starting material, lactam cyclization, and reduction.Type: ApplicationFiled: July 19, 2006Publication date: September 4, 2008Inventors: Kyoung Rok Roh, Ji Sang Yoo, Jong Won Jang, Dae Yon Lee
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Patent number: 7402606Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.Type: GrantFiled: April 1, 2003Date of Patent: July 22, 2008Assignee: SmithKline Beecham CorporationInventors: David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano
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Patent number: 7385065Abstract: The present invention relates to derivatives of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide with covalently bonded acids, and to the salts, solvates and prodrugs thereof, to the derivatives as medicaments, to the use of these derivatives for the preparation of a medicament, to the use of these derivatives for the preparation of a pharmaceutical composition, to a process for the preparation of the pharmaceutical compositions, to pharmaceutical compositions obtainable by this process, and to a process for the treatment of diseases which comprises the administration of the pharmaceutical composition.Type: GrantFiled: November 25, 2003Date of Patent: June 10, 2008Assignee: Tioga Pharmaceuticals, Inc.Inventors: Matthias Wiesner, Christoph Seyfried
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Publication number: 20080039470Abstract: The present invention discloses compounds of formulae I and II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: August 11, 2006Publication date: February 14, 2008Inventors: Deqiang Niu, Joel D. Moore, Dong Liu, Yonghua Gai, Zhigang Chen, Yat Sun Or, Zhe Wang
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Patent number: 7314932Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrite groups, are provided.Type: GrantFiled: April 7, 2005Date of Patent: January 1, 2008Assignee: WyethInventor: Bogdan Kazimierz Wilk
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Patent number: 7232817Abstract: ?- and ?-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 27, 2005Date of Patent: June 19, 2007Assignees: G.D. Searle & Co., Monsanto CompanyInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 7230119Abstract: Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from benzylamine instead of phenethylamine (Scheme 3) which provides a crystalline intermediate. The synthesis of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is achieved from (S)-diethylmalate as described in Scheme 4. A process for preparing camphor sultam is also provided.Type: GrantFiled: August 25, 2005Date of Patent: June 12, 2007Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Pooran Chand, Yahya El-Kattan, Pravin L. Kotian
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7160902Abstract: Amide derivatives of the general formulae Ia and Ib: are disclosed. Pharmaceutical compositions containing these compounds, and methods for their use, inter alia, for treating and/or preventing gastrointestinal disorders, pain, and pruritus are also disclosed.Type: GrantFiled: November 14, 2003Date of Patent: January 9, 2007Assignee: Adolor CorporationInventors: Roland E. Dolle, Guo-Hua Chu, Minghua Gu
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Patent number: 7135578Abstract: Designed imminocyclitols have potent inhibition activity with respect to hexoaminidases and glycosidases.Type: GrantFiled: March 10, 2004Date of Patent: November 14, 2006Assignee: The Scripps Research InstituteInventors: Chi-Huey Wong, Junjie Liu
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Patent number: 7132543Abstract: The present disclosure relates to a novel a para-phenylenediamine derivative substituted with a pyrrolidinyl group of formula (I) and the addition salts thereof. The present disclosure also relates to a dyeing composition for keratin fibers comprising the paraphenylene derivative as at least one oxidation base, and to a process for dyeing keratin fibers and a multi-compartment kit using the claimed dye composition. Such a composition makes it possible to obtain a chromatic, powerful, unselective and fast coloration of keratin fibers.Type: GrantFiled: March 29, 2004Date of Patent: November 7, 2006Assignee: L'Oreal S.A.Inventors: Laure Ramos, Stéphane Sabelle
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Patent number: 7091204Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.Type: GrantFiled: May 7, 2002Date of Patent: August 15, 2006Assignee: SmithKline Beecham CorporationInventors: Dashyant Dhanak, Timothy F. Gallagher, Steven D. Knight
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Patent number: 7084165Abstract: The present invention relates to compounds that are useful exhibit activity as serotonin, norepinephrine and dopamine reuptake inhibitors, and their pharmaceutically acceptable salts, and their use in the treatment of central nervous system and other disorders.Type: GrantFiled: September 4, 2003Date of Patent: August 1, 2006Assignee: Pfizer IncInventors: Harry Ralph Howard, Jr., Christopher Joseph Schmidt, Thomas Francis Seeger, Mark Leonard Elliot
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Patent number: 7026094Abstract: New oxime sulfonate compounds of the formula (I) and (II), wherein R1 is C1-C12alkyl, C1C4haloalkyl, hydrogon, OR9, NR10R11, SR12 or is phenyl which is unsubstituted or substituted by OH, C1-C18alkyl, halogen and/or C1-C12alkoxy; R2, R3, R4 and R5 are for example hydrogen or C1-C12alkyl; R6 is for example is C1-C18alkylsulfonyl, phenyl-C1-C3alkylsulfonyl or phenylsulfonyl; R?6 is for example phenylenedisulfonyl or diphenylenedisulfonyl; R7, R8 and R9 for example are hydrogen or C1-C6alkyl; R10 and R11, are for example hydrogen or C1-C18alkyl; R12 is for example hydrogen, phenyl or C1-C18alkyl; A is S, O, NR13, or a group of formula A1, A2 or A3, R21 and R22 independently of one other have one of the meanings given for R7; R23, R24, R25 and R26 independently of one another are for example hydrogen, C1-C4alkyl, halogen or phenyl; Z is CR22 or N; and Z1 is CR22 or N; and Z1 is CR22 or N; and Z1 is CH2, S, O or NR13 are particularly suitable as photo-latent acids in resist applications.Type: GrantFiled: May 23, 2002Date of Patent: April 11, 2006Assignee: Ciba Specialty Chemicals Corp.Inventors: Akira Matsumoto, Hitoshi Yamato, Toshikage Asakura, Masaki Ohwa, Peter Murer
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Patent number: 6946468Abstract: The present invention relates to inhibitors of ras farnesylation of the Formula I wherein: R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CH2—NH— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing upto 5 heteroatoms where the heteroatoms are independently selected from O, N & S; or a —S—S— dimer thereof when R2?H; or a N-oxide or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation their use as therapeutic agents and pharmaceutical compositions containing them.Type: GrantFiled: August 13, 1997Date of Patent: September 20, 2005Assignee: Zeneca LimitedInventors: Francis Thomas Boyle, James Michael Wardleworth
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Patent number: 6936597Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.Type: GrantFiled: March 21, 2002Date of Patent: August 30, 2005Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe
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Patent number: 6933390Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.Type: GrantFiled: July 15, 2004Date of Patent: August 23, 2005Assignee: Warner-Lambert CompanyInventors: Hubert Barth, Klaus Steiner, Simon Schneider, Ulrich Bayer, Manfred Westermayer, Ulrike Wolfsperger, Hans-Jürgen Betche
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Patent number: 6923835Abstract: The invention relates to novel bis-para-phenylenediamine derivatives containing a pyrrolidyl group substituted with a cationic radical, to dye compositions containing them and to the process of dyeing keratin fibres using these compositions. The present invention makes it possible to obtain a chromatic, powerful, sparingly selective and colourfast coloration of keratin fibres.Type: GrantFiled: September 9, 2003Date of Patent: August 2, 2005Assignee: L'Oreal S.A.Inventors: Stéphane Sabelle, Laure Ramos, Madeleine Leduc
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Patent number: 6900322Abstract: A method for stereochemically controlled production of azacyclic compounds of general formula (I) in which the substituents have the meanings given in the specification. The invention also relates to intermediate products of this method and to novel azacyclenes.Type: GrantFiled: May 10, 1999Date of Patent: May 31, 2005Assignee: Solvay Pharmaceuticals GmbHInventors: Michael Reggelin, Timo Heinrich, Bernd Junker, Jochen Antel, Ulf Preuschoff
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Publication number: 20040242672Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.Type: ApplicationFiled: June 30, 2004Publication date: December 2, 2004Inventors: Johannes Aebi, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow, Eric Argirios Kitas, Ulrike Obst, Hans Peter Wessel
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Patent number: 6794519Abstract: Sulfonic acid ester derivatives represented by the general formula (4) or (5) are produced by reacting an amino alcohol derivative represented by the general formula (1) or (2) with an organic sulfonyl halide represented by the general formula (3), in a mixed solvent composed of an aprotic organic solvent and water in the presence of a non-water-prohibiting inorganic base. This procedure can be carried out in a simple, easy, safe and economical manner while reducing the load on the environment. Wherein n represents an integer of 0 to 5, A represents a phenyl group, which may be substituted, R represents a methanesulfonyl, ethanesulfonyl, p-toluenesulfonyl or p-nitrobenzenesulfonyl group and X represents a chloride, bromine or iodine atom.Type: GrantFiled: February 8, 2002Date of Patent: September 21, 2004Assignee: Kaneka CorporationInventors: Fumihiko Kano, Shigeki Kunihiro, Noritaka Yoshida, Natsuki Mori
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Patent number: 6774140Abstract: Designed iminocylitols that have potent inhibition activity with respect to hexominidases and glycosides are disclosed.Type: GrantFiled: February 12, 2002Date of Patent: August 10, 2004Assignee: The Scripps Research InstituteInventors: Chi-Huey Wong, Jungie Liu
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Patent number: 6770764Abstract: A compound of the formula (I) wherein R1 is a protecting group for N&agr;, R2 is a protecting group for NG, and R3 is aryl, and wherein the compound of formula (I) is a trypsin substrate such that trypsin cleaves the O—C single bond, which liberates R3—OH; a diagnostic device comprising same; a method for preparing the diagnostic device; and a method of using the diagnostic device to detect levels of urinary trypsin inhibitor in a biological sample; and a diagnostic kit for detecting levels of urinary trypsin inhibitor in a biological sample.Type: GrantFiled: April 30, 2001Date of Patent: August 3, 2004Assignee: Bayer CorporationInventors: Paul F. Corey, Steven W. Felman, Gary E. Rehm, Michael J. Pugia
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Publication number: 20040122017Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: ApplicationFiled: December 3, 2002Publication date: June 24, 2004Applicant: Schering CorporationInventors: John W. Clader, Anandan Palani, Ruo Xu, Mark D. McBriar, Jing Su, Haiqun Tang
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Patent number: 6720335Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: March 8, 2002Date of Patent: April 13, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger D. Tung, Mark A. Murcko, Govinda Rao Bhisetti
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Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6624314Abstract: A pyrrolesulfonamide derivative having the following formula (I): wherein the ring P represented by is a pyrrole ring having the following structure: wherein R represents alkyl, cycloalkyl, cycloalkylalkyl or aralkyl; the dashed line indicates the presence or absence of a bond; l stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W represents CH, C═ or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C═; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.Type: GrantFiled: June 4, 2001Date of Patent: September 23, 2003Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 6624142Abstract: The invention is directed primarily to compounds of Formula I: wherein: R1 is a polymeric residue; L1 is a bifunctional linking group; Y1 and Y2 are independently O, S or NR7; R2-7 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; D is a moiety that is a leaving group or a residue of a compound to be delivered into a cell; Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; and (y) is a positive integer greater than or equal to 1. Methods of making and using the same are also disclosed.Type: GrantFiled: May 9, 2001Date of Patent: September 23, 2003Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Hong Zhao
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Patent number: 6590106Abstract: Disclosed are novel compounds represented by Structural Formula II, IX or XXVIII: R1, R2, and R22 are independently an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. R2 is —NR4R5 or —N+≡C−. Alternatively, R1, and R2, taken together with the methine group to which they are bonded, are a moiety represented by the following structural formula: R3 is —NH2, —OH, —OC(O)H or —OR9. R5, R6 and R7 are independently —H or an amine protecting group. R8 is —H, —OH or —OR8. R9 is an alcohol protecting group. Also disclosed are methods of preparing these compounds.Type: GrantFiled: June 21, 2002Date of Patent: July 8, 2003Assignee: Pharm-Eco Laboratories, Inc.Inventors: Richard L. Gabriel, Jurjus Jurayj
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Patent number: 6576780Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: October 13, 2000Date of Patent: June 10, 2003Assignee: GD Searle & CompanyInventors: Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth
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Patent number: 6541491Abstract: Pharmaceutical compositions comprising an inhibitor of ras farnesylation of formula (I) wherein, R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CO—NH2— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a —S—S-dimer thereof when R2=H; or an enantiomer, diastereoisomer, pharmaceutically acceptable salt, prodrug or solvate thereof together with a pharmaceutically acceptable diluent or carrier. A particular use is cancer therapy.Type: GrantFiled: November 30, 2000Date of Patent: April 1, 2003Assignee: Zeneca LimitedInventors: David Huw Davies, Francis Thomas Boyle, James Michael Wardleworth, Peter Wedderburn Kenny, Peter Beverley Scholes, Zbigniew Stanely Matusiak
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Patent number: 6534523Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl oType: GrantFiled: March 5, 2002Date of Patent: March 18, 2003Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Elise Ghiro, Nathalie Goudreau, Marc-Andre Poupart, Jean Rancourt, Youla S. Tsantrizos, Anne-Marie Faucher, Teddy Halmos, Dominik M. Wernic
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Patent number: 6518437Abstract: Processes for the preparation of pyrrolidones (7 and 8) and pyrrolidines (9 and 10) from tri-O-acetyl-D-erythro-4-pentulosonic acid esters are described. The compounds are aza sugar analogs of D-ribofuranoside and are intermediates to drugs which regulate nucleoside and nucleic acid synthesis.Type: GrantFiled: September 4, 2001Date of Patent: February 11, 2003Assignee: Board of Trustees of Michigan State UniversityInventor: Rawle I. Hollingsworth
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Patent number: RE38133Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formulae I, II, III and IV have the structure: wherein: X, X4, X5, X7, X9; R1, R2, R3, R4; and Y, Z and n are as described in the specification.Type: GrantFiled: February 4, 2002Date of Patent: June 3, 2003Assignee: Adolor CorporationInventors: Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang