Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To A Piperdine Ring By Nonionic Bonding Patents (Class 546/190)
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Patent number: 7368461Abstract: NK2R binding compounds in accord with structural diagram I useful for the treatment or prevention of OAB or UI in mammals, particularly humans are disclosed: wherein in said compounds D, A, R1, R3 and R4 are as defined in the specification. Pharmaceutically-advantageous salts of the compounds, methods of use of the compounds, either alone or in combination with other pharmacological agents, and pharmaceutical compositions useful in practicing the methods of the invention are also disclosed.Type: GrantFiled: November 1, 2002Date of Patent: May 6, 2008Assignee: AstraZeneca ABInventors: Russell Bialecki, Cathy Dantzman, Keith Herzog
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Patent number: 7358359Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: July 22, 2005Date of Patent: April 15, 2008Assignee: University of WashingtonInventors: Niels H. Andersen, Jason Bowman
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Patent number: 7348324Abstract: A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Type: GrantFiled: October 18, 2002Date of Patent: March 25, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Shinichi Imamura, Shohei Hashiguchi, Taeko Hattori, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba, Yoshihiro Sugihara
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Patent number: 7335788Abstract: Dithiocarbonate derivatives are disclosed, along with a process for preparing the same. The dithiocarbonate compounds can be utilized as initators, chain transfer agents and/or terminators in controlled free radical polymerizations. The dithiocarbonates can be used to produce polymers having narrow molecular weight distribution. Advantageously, the compounds of the present invention can also introduce functional groups into the resulting polymers. The dithiocarbonate compounds have low odor and are substantially colorless.Type: GrantFiled: October 8, 2003Date of Patent: February 26, 2008Assignee: Lubrizol Advanced Materials, Inc.Inventor: John Ta-Yuan Lai
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Patent number: 7253186Abstract: Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.Type: GrantFiled: June 20, 2003Date of Patent: August 7, 2007Inventors: Carl-Magnus Andersson, Nathalie Schlienger, Alma Fejzic, Eva Louise Hansen, Jan Pawlas
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Patent number: 7105507Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: May 16, 2001Date of Patent: September 12, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
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Patent number: 7084140Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: September 5, 2002Date of Patent: August 1, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Franz Esser, Gerd Schnorrenberg, Kurt Schromm, Horst Dollinger, Birgit Jung, Georg Speck
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Patent number: 7074795Abstract: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17 ?-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with type 3 17 ?-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions. In one embodiment, the present invention discloses a compound having the general structure shown in Formula I: wherein the various moieties are as defined herein.Type: GrantFiled: November 14, 2003Date of Patent: July 11, 2006Assignee: Schering CorporationInventors: Kamil Paruch, Timothy J. Guzi
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Patent number: 6987188Abstract: Compounds of the formula: are disclosed as ligands for neuropeptide Y receptors and as such are useful in the treatment of obesity and disorders of the central nervous system.Type: GrantFiled: July 28, 2004Date of Patent: January 17, 2006Inventors: Scott Dax, James McNally
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Patent number: 6936718Abstract: In one embodiment, the present invention discloses a process to directly prepare an unequal ratio of specific, preferred rotamer or rotameric pair of an acid salt from a basic compound, by creative choice of a solvent medium. The process is particularly useful in preparing desired rotamers of pharmaceutically useful salts.Type: GrantFiled: November 26, 2002Date of Patent: August 30, 2005Assignee: Schering CorporationInventors: Minzhang Chen, Bosco D'sa, William Leong, Suhan Tang
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Patent number: 6930200Abstract: Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R2 and/or R3) as shown in Formula 1: N(R4R5)C(R2R3)CO(OR1).Type: GrantFiled: June 26, 2003Date of Patent: August 16, 2005Assignee: Pharmacore, Inc.Inventor: Adnan M. M. Mjalli
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Patent number: 6900326Abstract: A method of producing an N-alkoxycarbonylpiperidine derivative, comprising reacting an N-aralkylpiperidine derivative represented by the following general formula (1): wherein R1 represents an aralkyl group which may have a substituent, with a mesyl halide in the presence of a base, thereby obtaining a mesylated product represented by the following general formula (2): wherein R1 represents an aralkyl group which may have a substituent and Ms represents a mesyl group, and reacting the mesylated product with a dicarbonate represented by the following general formula (3): wherein R4 represents an alkyl group, in the presence of hydrogen and a catalyst containing palladium, thereby obtaining an N-alkoxycarbonylpiperidine derivative represented by the following general formula (4): wherein R4 represents an alkyl group and Ms represents a mesyl group.Type: GrantFiled: September 17, 2003Date of Patent: May 31, 2005Assignee: Yuki Gosei Kogyo Co., Ltd.Inventor: Kiyono Nakagawa
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Patent number: 6852725Abstract: The present invention is directed to imidazolyl derivatives of the formula: where the substituents are defined in the specification, or a pharmaceutically acceptable salt thereof. The derivatives bind selectively to the somatostatin subtype receptors and elicit either an agonist or antagonist effect from the somatostatin subtype receptors.Type: GrantFiled: June 8, 1999Date of Patent: February 8, 2005Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, S. A. S.Inventors: Christophe Alain Thurieau, Lydie Francine Poitout, Marie-Odile Galcera, Christophe Philippe Moinet, Thomas D. Gordon, Barry A. Morgan
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Patent number: 6841552Abstract: Compounds of the formula: are disclosed as ligands for neuropeptide Y receptors and as such are useful in the treatment of obesity and disorders of the central nervous system.Type: GrantFiled: April 20, 2000Date of Patent: January 11, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Scott Dax, James McNally
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Patent number: 6787522Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, anType: GrantFiled: April 30, 2002Date of Patent: September 7, 2004Assignee: British Biotech PharmaceuticalsInventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
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Patent number: 6787650Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.Type: GrantFiled: April 5, 2002Date of Patent: September 7, 2004Assignee: Takeda Chemical Industries, Ltd.Inventors: Osamu Kurasawa, Shinichi Imamura, Shohei Hashiguchi, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba
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Publication number: 20040132694Abstract: This invention relates to the novel use of amide squaramides in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: July 16, 2003Publication date: July 8, 2004Inventors: Michael R. Palovich, Katherine L. Widdowson
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Patent number: 6737527Abstract: The present invention relates to 4-formylamino-N-methylpiperidine derivatives of the formula (I) where the variables are as defined in the Description, to a process for preparing these piperidine derivatives, to the use of these piperidine derivatives of the invention, or prepared according to the invention, for stabilizing organic material, in particular for stabilizing plastics or coating materials, and also to the use of these piperidine derivatives of the invention, or prepared according to the invention, as light stabilizers or stabilizers for wood surfaces. The present invention further relates to stabilized organic material which comprises these piperidine derivatives of the invention or prepared according to the invention.Type: GrantFiled: September 27, 2002Date of Patent: May 18, 2004Assignee: BASF AktiengesellschaftInventors: Sylke Haremza, Jürgen Krockenberger, Manfred Appel, Hubert Trauth, Alexander Aumüller
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Patent number: 6716987Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z representsType: GrantFiled: December 20, 2001Date of Patent: April 6, 2004Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
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Publication number: 20040044215Abstract: The invention relates to crystalline forms of (R)-(+)-N-[[3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1-yl]-4-phenylpiperidin-4-yl]-N-methylacetamide and to processes for preparing them.Type: ApplicationFiled: August 28, 2003Publication date: March 4, 2004Inventors: Alain Alcade, Gilles Anne-Archard, Patrick Gros-Claude, Olivier Monnier, Jerome Roche
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Patent number: 6696570Abstract: Oligomeric compounds and methods of making the compound having the formula: T—&Parenopenst;E—F&Parenclosest;i—&Parenopenst;E—F′&Parenclosest;j—&Parenopenst;E′—F&Parenclosest;k—&Parenopenst;E′—F′&Parenclosest;l—S (II) wherein i, j, k, and l are integers from about 0 to 300 and the sum of i, j, k, and l is greater than 2, wherein the units F, F′ and T are derived from one or more multi-functional carbonyl compounds of general structure DO—CO—CRaRb—(—CRcRd—)n—NH—(Y)m—CO—OD (IV) wherein n is an integer from 1 to 15, m is either 0 or 1; Ra, Rb, Rc, and Rd, are each a hydrogen or a hydrocarbyl group; Y is CO—(CReRf)p, wherein Re and Rf are each a hydrogen or hydrocarbyl group and p is zero or an integer from 1 to 20 or CO—C6H4—, wherein the substitution pattern on the phenylene group is an ortho, meta, or para substitution pattern, andType: GrantFiled: October 25, 2001Date of Patent: February 24, 2004Assignee: Cytec Technology Corp.Inventors: Thomas P. Sassi, Ram. B. Gupta
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Patent number: 6693117Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: August 19, 2002Date of Patent: February 17, 2004Assignee: AstraZeneca Canada Inc.Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
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Patent number: 6693202Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.Type: GrantFiled: August 25, 2000Date of Patent: February 17, 2004Assignee: Theravance, Inc.Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
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Publication number: 20040010147Abstract: A cyclic amine compound represented by the following general formula (1): 1Type: ApplicationFiled: July 10, 2002Publication date: January 15, 2004Applicant: KOWA CO., LTD.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Shunji Takemura, Takeshi Doi, Yoshinori Kyotani, Masao Ohkuchi
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Publication number: 20030232837Abstract: There are disclosed compounds of the formula (I): 1Type: ApplicationFiled: October 15, 2002Publication date: December 18, 2003Applicant: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch
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Publication number: 20030207917Abstract: The present invention discloses compounds, which are novel muscarinic receptor antagonists, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such muscarinic receptor antagonists as well as methods for using them to treat cognitive disorders such as Alzheimer's disease.Type: ApplicationFiled: October 8, 2002Publication date: November 6, 2003Applicant: Schering CorporationInventors: Yuguang Wang, Samuel Chackalamannil
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Patent number: 6613769Abstract: The invention relates to bifunctional tryptase inhibitors of formula (I) wherein H1 and H2 comprise a Q group and L is a linker of formula and the conformation of the H1, H2 and L groups is such that the groups are separated by a distance of from 20 to 45 Å. Pharmaceutical compositions and crystal forms of the compounds are described in addition to methods for producing and identifying such compounds, as well as the use of such compounds in methods of treating allergic and inflammatory diseases.Type: GrantFiled: January 22, 2001Date of Patent: September 2, 2003Assignees: Max-Planck-Gesellschaft zur Föderung der Wissenschaften. e.V., Altana Pharma AGInventors: Wolfram Bode, Luis Moroder, Pedro Jose Barbosa Pereira, Andreas Bergner, Robert Huber, Christian Sommerhoff, Norbert Schaschke, Thomas Bär, Thomas Martin, Josef Stadlwieser, Wolf-Rüdiger Ulrich, Andreas Dominik, Ulrich Thibaut, Daniela Bundschuh, Rolf Beume, Karl-Josef Goebel
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Publication number: 20030078427Abstract: The present invention of compounds of formula (I) 1Type: ApplicationFiled: June 5, 2002Publication date: April 24, 2003Inventors: Jean-Paul Rene Marie Andre Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
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Patent number: 6518283Abstract: Squaric acid Derivatives of formula (1) are described: wherein R1 is an integrin binding group; R2 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic chain; R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune of inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.Type: GrantFiled: May 25, 2000Date of Patent: February 11, 2003Assignee: Celltech R&D LimitedInventors: Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
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Patent number: 6514996Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CType: GrantFiled: November 19, 1997Date of Patent: February 4, 2003Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
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Patent number: 6492521Abstract: Compounds and methods of preparing compounds of the formula: RZ—CO—CRaRb—(CRcRd)n—NH—(Y)m—CO—A (I) wherein n is an integer from 1 to 15, m is either 0 or 1; Ra, Rb, Rc, and Rd are each a hydrogen or a hydrocarbyl group; Y is CO—(CReRf)p, wherein Re and Rf are each a hydrogen or hydrocarbyl group and p is zero or an integer from 1 to 20 or CO—C6H4—, wherein the substitution pattern on the phenylene group is an ortho, meta, or para substitution pattern and one or more of the hydrogens of the phenylene group may be substituted by a hydrocarbyl group or a functional group; Z is —O— or —NG—, wherein G is H, C1-C12 alkyl or the radical R; wherein R is wherein R1 is hydrogen, C1-C18 alkyl, O, OH, CH2CN, C1-C18 alkoxy, C1-C18 hydroxyalkoxy, C5-C12 cycloalkoxy, C5-C12 hydroxycycloalkoxy, C3-C6 alkenyl, C1-C18 alkynyl, C7-C9 phenylalkyl, unsubstituted or substituted on the phenyl with 1, 2 or 3 C1-C4 alkylType: GrantFiled: October 25, 2001Date of Patent: December 10, 2002Assignee: Cytec Technology Corp.Inventors: Thomas P. Sassi, Ram B. Gupta
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Hindered amine compound, resin composition, polyurethane fiber and production method and use thereof
Patent number: 6486238Abstract: A hindered amine compound having thesolubility in an acidic solution of 5.0×10−3 eq./liter or less comprising at least two specific organic groups in a specific weight ratio in a molecule, or at least two specific monomeric units, which can be used as a stabilizer of a resin.Type: GrantFiled: December 20, 1999Date of Patent: November 26, 2002Assignee: Toyo Boseki Kabushiki KaishaInventors: Kota Kitamura, Chihiro Oshimo, Genei Matsukawa, Futoshi Ishimaru -
Patent number: 6462041Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I-III are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled cell growth and spread of abnormal cells occurs.Type: GrantFiled: February 1, 2000Date of Patent: October 8, 2002Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Han-Zhong Zhang, Yan Wang, Ben Tseng, Shailaja Kasibhatla, John A. Drewe
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Patent number: 6455545Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: January 18, 2001Date of Patent: September 24, 2002Assignee: AstraZeneca Canada Inc.Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
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Patent number: 6423714Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: GrantFiled: March 9, 2001Date of Patent: July 23, 2002Assignee: Ortho McNeil-Pharmaceutical, Inc..Inventors: Robert H. Chen, Min A. Xiang
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Patent number: 6414155Abstract: Oligomeric compounds and methods of making the compound having the formula: wherein i, j, k, and l are integers from about 0 to 300 and the sum of i, j, k, and l is greater than 2, wherein the units F, F′ and T are derived from one or more multi-functional carbonyl compounds of general structure DO—CO—CRaRb—(—CRcCRd—)n—NH—(Y)m—CO—OD (IV) wherein n is an integer from 1 to 15, m is either 0 or 1; Ra, Rb, Rc, and Rd, are each a hydrogen or a hydrocarbyl group; Y is CO—(CReRf)p, wherein Re and Rf are each a hydrogen or hydrocarbyl group and p is zero or an integer from 1 to 20 or CO—C6H4—, wherein the substitution pattern on the phenylene group is an ortho, meta, or para substitution pattern, and one or more of the hydrogens of the phenylene group may be substituted by a hydrocarbyl group or a functional group; and D is a hydrocarbyl group and the units E, E′ and S are derived from one or more 1-subType: GrantFiled: November 3, 2000Date of Patent: July 2, 2002Assignee: Cytec Technology Corp.Inventors: Thomas Patrick Sassi, Ram Baboo Gupta
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Patent number: 6380215Abstract: This invention relates to &bgr;-alanine derivatives represented by the following formula: wherein each symbol is as defined in the specification and pharmaceutically acceptable salt thereof which is glycoprotein IIb/IIIa antagonist, inhibitor of blood platelets aggregation and inhibitor of the binding of fibrinogen to blood platelets, 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: August 4, 1995Date of Patent: April 30, 2002Assignee: Fujisawa Pharmaceutical Co., LtdInventors: Mitsuru Ohkubo, Fumie Takahashi, Toshio Yamanaka, Hiroyoshi Sakai, Masayuki Kato
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Patent number: 6376584Abstract: Hindered amines substituted on the N-atom with an hydroxy-substituted alkoxy moiety are particularly effective in stabilizing organic polymer compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not otherwise attainable.Type: GrantFiled: February 27, 2001Date of Patent: April 23, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: James Peter Galbo, Gerald A. Capocci, Nancy N. Cliff, Robert E. Detlefsen, Michael P. DiFazio, Ramanathan Ravichandran, Peter Solera, Christophe Bulliard
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Patent number: 6348597Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.Type: GrantFiled: April 4, 2001Date of Patent: February 19, 2002Assignee: Merrell Pharmaceuticals, Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6333338Abstract: Novel compounds which are inhibitors of the binding of fibrinogen to the Gp IIb/IIIa platelet receptors, and which can be used therepeutically as antithrombotic agentsType: GrantFiled: January 17, 2001Date of Patent: December 25, 2001Assignee: Laboratoire L. LafonInventors: Christophe Yue, Marguerite Henry, Thierry Giboulot, Brigitte Lesur
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Patent number: 6331545Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: December 17, 1999Date of Patent: December 18, 2001Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 6323315Abstract: The present invention provides compounds of the formula where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocylic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or —C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.Type: GrantFiled: March 31, 2000Date of Patent: November 27, 2001Assignees: BASF Aktiengesellschaft, Arizona Board of RegentsInventors: George R. Pettit, Jayaram K. Srirangam, Michael D. Williams, Kieran P. M. Durkin, Teresa Barlozzari, Andreas Kling, Bernd Janssen, Andreas Haupt
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Publication number: 20010039353Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided.Type: ApplicationFiled: February 21, 2001Publication date: November 8, 2001Inventors: Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
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Patent number: 6313097Abstract: Compounds of the formula (I) wherein A, R, R1, R2, X1, X2, X3, and Y are as defined herein, and the tautomers and the pharmaceutically acceptable salts thereof, including pharmaceutical compositions containing these compounds, and their use in the selective antagonization of calcitonin gene-related peptide (CGRP) and in the treatment or prophylaxis of migraine or cluster headaches, non-insulin-dependent diabetes mellitus, inflammation, allergic rhinitis, asthma, morphine tolerance, menopausal hot flashes, and diseases characterized by excessive vasodilatation and consequent reduction in blood-flow.Type: GrantFiled: March 10, 2000Date of Patent: November 6, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Wolfgang Eberlein, Klaus Rudolf, Wolfhard Engel, Henri Doods, Gerhard Hallermayer
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Patent number: 6307048Abstract: Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.Type: GrantFiled: November 18, 1999Date of Patent: October 23, 2001Assignee: Schering CorporationInventors: Shen-Chun Kuo, Charles F. Bernard, Frank Xing Chen, Donald Hou, Agnes S. Kim-Meade, George G. Wu
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Patent number: 6303601Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula wherein is 2 or 3 and X denotes oxygen, N(CH2)nR6 or CR7R8, and R34 R5 R6 R7, R8, Ar and n have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin)-antagonists.Type: GrantFiled: January 3, 2001Date of Patent: October 16, 2001Assignee: Boehringer Ingelheim KGInventors: Gerd Schnorrenberg, Horst Dollinger, Franz Esser, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 6294556Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula wherein p is 2 or 3 and X denotes oxygen, N(CH2)nR6 or CR7R8, and R3, R4, R5, R6, R7, R8, Ar and n have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin)-antagonists.Type: GrantFiled: February 18, 2000Date of Patent: September 25, 2001Assignee: Boehringer Ingelheim KGInventors: Gerd Schnorrenberg, Horst Dollinger, Franz Esser, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 6294555Abstract: Compound of the formula (I): wherein Ar is a group of the following formula (Ar-1) or (Ar-2): A is a group of the formula: —Z—N(Q1)(Q2), —CO—R7 or —(CH2)p—CH(R8)—COR9, or a pharmaceutically acceptable acid addition salt thereof, a process for preparing the same, a pharmaceutical composition containing the same, and intermediates therefor. The compounds of the present invention show a potent affinity for 5-HT4 receptors, and they are useful as a gastrointestinal motility enhancer or a gastrointestinal prokinetic agent.Type: GrantFiled: October 27, 2000Date of Patent: September 25, 2001Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Shiro Kato, Yoshihito Toyotomi, Hirotake Tateishi, Hiroshi Harada, Naoyuki Yoshida, Kazuo Morikage, Yukiko Morikage
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Patent number: 6291478Abstract: The present application relates to novel compounds belonging to the benzylaminodiacetamide family which have good anti-irritant and soothing properties. The invention also relates to their use in a composition comprising a physiologically acceptable medium, in particular in order to prevent and/or treat certain cutaneous disorders and more particularly in order to treat sensitive skins.Type: GrantFiled: March 13, 2000Date of Patent: September 18, 2001Assignee: L'OrealInventors: Jean-Baptiste Galey, Maria Dalko
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Patent number: 6288234Abstract: Disclosed are multibinding compounds which inhibit microsomal triglyceride transferase protein (MTP), a protein which mediates the transfer of lipids during the assembly of lipoproteins and related biomolecules. The multibinding compounds contain from 2 to 10 ligands covalently attached to one or more linkers. The multibinding compounds of this invention are useful for lowering serum lipid, cholesterol and/or triglyceride levels, and for preventing and treating disorders associated with hyperlipemia, hyperlipidemia, hyperlipoproteinemia, hypercholestrolemia, hypertriglyceridemia and the like, such atherosclerosis.Type: GrantFiled: June 4, 1999Date of Patent: September 11, 2001Assignee: Advanced Medicine, Inc.Inventor: John H. Griffin