Chalcogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/236)
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Patent number: 7115610Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.Type: GrantFiled: December 17, 2004Date of Patent: October 3, 2006Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeffrey Zablocki
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Patent number: 7091354Abstract: Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.Type: GrantFiled: July 9, 2004Date of Patent: August 15, 2006Assignee: Adolor CorporationInventors: Bertrand Le Bourdonnec, Roland Ellwood Dolle
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Patent number: 7084144Abstract: A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl group, a phenyl group, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl or, a furyl group; R1 and R2 are, independently, H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group or a lower N-alkyl group, or R1 and R2 taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are one or two oxygen atoms, and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N; n is 0,1,2,3 or 4; m is 0 or 1; and pharmaceutically acceptable salts thereof; with the proviso that said compound is not 1-[(4-methoxyphenyl)sulfonyl]piperazine or 1-(1,3-benzodioxol-5-ylsulfonyl)piperazine.Type: GrantFiled: May 19, 2004Date of Patent: August 1, 2006Assignee: The Jordanian Pharmaceutical MFG & Medical Equipment CO LTDInventor: Adnan Badwan
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Patent number: 7067501Abstract: The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.Type: GrantFiled: May 20, 2004Date of Patent: June 27, 2006Assignee: H. Lundbeck A/SInventors: Garrick P. Smith, Gitte Mikkelsen, Kim Andersen, Daniel Greve, Thomas Ruhland, Stephen P. Wren
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Patent number: 7022880Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings, each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.Type: GrantFiled: August 13, 2004Date of Patent: April 4, 2006Assignee: AMR Technology , Inc.Inventor: Thomas E. D'Ambra
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Patent number: 6992090Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: June 16, 2003Date of Patent: January 31, 2006Assignee: Adolor CorporationInventors: Bertrand Le Bourdonnec, Roland E. Dolle
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Patent number: 6962998Abstract: Disclosed are a method for producing racemic piperidine derivatives by processing optically-active piperidine derivatives in a hydrogen atmosphere in the presence of a reducing catalyst; and a method for producing optically-active piperidine derivatives or their acid salts by optically resolving the racemic piperidine derivatives obtained in the former method.Type: GrantFiled: June 4, 2001Date of Patent: November 8, 2005Assignee: Toray Industries, Inc.Inventors: Toshihiro Fujino, Haruyo Sato
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Patent number: 6953801Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: May 21, 2002Date of Patent: October 11, 2005Assignee: Neurogen CorporationInventors: Alan Hutchison, Linda M. Gustavson, John M. Peterson, Dario Doller, Timothy M. Caldwell, Taeyoung Yoon, Wallace C. Pringle, Yiping Shen, Cheryl Steenstra
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Patent number: 6946475Abstract: The present invention is directed to compounds useful as cancer cell inhibitors, compositions containing such compounds and methods for inhibiting proliferation of electrically non-excitable cells.Type: GrantFiled: April 7, 2000Date of Patent: September 20, 2005Assignee: University of Virginia Patent FoundationInventors: Lloyd S. Gray, Timothy L. Macdonald, Doris Haverstick, Tiffany N. Heady
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Patent number: 6930186Abstract: The present invention is directed to methods for preparing intermediates useful in the synthesis of paroxetine wherein the intermediates are substantially free of alkoxy impurities as well as to methods for preparing paroxetine and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities. The alkoxy impurity is reacted with an ether cleaving agent to generate the corresponding phenol, which is separated, yielding the desired product substantially free of alkoxy impurities. Paroxetine intermediates such as PMA, paroxetine, and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities also form part of the present invention.Type: GrantFiled: June 13, 2002Date of Patent: August 16, 2005Assignee: Teva Pharmacetical Industries Ltd.Inventors: Valerie Niddam, Ilya Avrutov
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Patent number: 6903120Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4,-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.Type: GrantFiled: December 22, 2000Date of Patent: June 7, 2005Assignee: A. Carlsson Research ABInventors: Clas Sonesson, Ingela Marianne Svan, Anders Kristoffer Lilja, Liselott Lilja Rönnqvist, Jenny Maria Carlberg, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
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Patent number: 6903085Abstract: The invention provides compounds of formula (I) wherein R1, R2, R3, R6, Z, Q, m, n, X1, X2, X3, X4 and T are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditionsType: GrantFiled: August 18, 2000Date of Patent: June 7, 2005Assignee: AstraZeneca, ABInventors: Stephen Thom, Andrew Baxter, Nicholas Kindor, Thomas McInally, Brian Springthorpe, Matthew Perry, David Harden, Richard Evans, David Marriott
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Patent number: 6894191Abstract: The present invention provides a process for the preparation of arylamines comprises reacting aryl halide and aryl amine/heterocyclic amine. The said process is carried out in the presence of a solvent, catalyst and a base.Type: GrantFiled: December 10, 2003Date of Patent: May 17, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Ashutosh Anant Kelkar, Nandkumar Manikrao Patil, Raghunath Vitthal Chaudhari
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Patent number: 6881845Abstract: The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX?) methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.Type: GrantFiled: January 4, 2001Date of Patent: April 19, 2005Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Jorge Ramentol, Diego Fernandez-Cano, Miguel P. Armengol, Inés Petschen, Juan Sallares, Francesc X. Camps, Manuel M. Raga, Josep M. Castello
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Patent number: 6875775Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2, which are the same or different are a) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C?CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and ?R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.Type: GrantFiled: April 8, 2003Date of Patent: April 5, 2005Assignee: Hormos Medical Oy LTDInventors: Marja-Liisa Södervall, Arja Kalapudas, Lauri Kangas, Risto Lammintausta, Pirkko Härkönen, Kalervo Väänänen, Arto Karjalainen
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Patent number: 6846835Abstract: 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: July 10, 2001Date of Patent: January 25, 2005Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshio Ogino, Hideki Kurihara, Kenji Matsuda, Tomoshige Numazawa, Norikazu Otake, Kazuhito Noguchi
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Publication number: 20040266822Abstract: The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions containing said compounds and the preparation methods thereof. The invention also relates to the use of the above mentioned compounds in the preparation of drugs for the prophylaxis or treatment of cardiovascular diseases, diabetes, bronchial and urinary smooth muscle spasm as well as ischemic and anoxic nerve injury. The above compounds can be used to treat hypertension, angina diaphragmatic, myocardial infarction, congestive heart failure, arrhythmia, diabetes, spasmodic bronchial diseases, spasmodic bladder or ureter diseases, and depression.Type: ApplicationFiled: August 12, 2004Publication date: December 30, 2004Inventors: Hai Wang, Liuhong Yun, Huasong Feng, Fulin Li, Xingehun Tang, Huamei He, Rifang Yang, Wenyu Cui, Qixiu Gao, Gang Hu, Rusheng Zhao, Wei Liu, Chaoliang Long, Lin Wang, Xinqiang Lu, Lijun Liu, Yuan Yan
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Publication number: 20040266824Abstract: The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: 1Type: ApplicationFiled: March 31, 2004Publication date: December 30, 2004Inventors: Peter A. Crooks, Linda Dwoskin, Marlon D. Jones, Dennis Keith Miller, Seth Davin Norholm, Guangrong Zheng, Sairam Krishamurthy
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Patent number: 6825202Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula (I): wherein Ar, R1, R2, R3 or R4 are as defined in the specification, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: August 9, 2002Date of Patent: November 30, 2004Assignee: Syntex (U.S.A.) LLCInventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
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Publication number: 20040236104Abstract: Substituted 4-aminocyclohexanols, methods of producing the same, pharmaceuticals containing these compounds, the use of substituted 4-aminocyclohexanols for producing pharmaceutical compositions for the treatment of various indications, in particular pain, and for related treatment methods.Type: ApplicationFiled: January 16, 2004Publication date: November 25, 2004Applicant: Gruenenthal GmbhInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Werner Englberger, Stephan Wnendt
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Publication number: 20040229864Abstract: The present invention relates to sulfone derivatives of formula (I):Type: ApplicationFiled: May 14, 2004Publication date: November 18, 2004Inventors: Sylvie Bourrain, Peter Alan Hunt, Ian Thomas Huscroft, Janusz Jozef Kulagowski, Clare London, Elizabeth Mary Naylor, Piotr Antoni Raubo, Eileen Mary Seward
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Publication number: 20040215020Abstract: The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX′) methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.Type: ApplicationFiled: September 15, 2003Publication date: October 28, 2004Inventors: Rafael Foguet, Jorge Ramentol, Diego Fernandez-Cano, Miguel P. Armengol, Ines Petschen, Juan Sallares, Francesc X. Camps, Manuel M. Raga, Josep M. Castello
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Publication number: 20040214822Abstract: 4-aminocyclohexanol compounds, processes for their preparation, pharmaceutical formulations comprising these compounds and the use of substituted 4-aminocyclohexanol compounds for the preparation of pharmaceutical formulations and for the treatment of diverse indications, including, without limitation, pain.Type: ApplicationFiled: January 16, 2004Publication date: October 28, 2004Applicant: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Stephan Wnendt
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Publication number: 20040204583Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): 1Type: ApplicationFiled: May 4, 2004Publication date: October 14, 2004Inventors: Mu-Ill Lim, Yuh-Guo Pan, Gottfried Wenke
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Patent number: 6797826Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.Type: GrantFiled: September 4, 2002Date of Patent: September 28, 2004Assignee: AMR Technology, Inc.Inventor: Thomas E. D'Ambra
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Patent number: 6794510Abstract: Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.Type: GrantFiled: August 8, 2002Date of Patent: September 21, 2004Assignee: Adolor CorporationInventors: Bertrand Le Bourdonnec, Roland Ellwood Dolle
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Publication number: 20040181070Abstract: A novel process is provided for the preparation of 4-aryl piperidines, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, male sexual dysfunction, and female sexual dysfunction.Type: ApplicationFiled: March 8, 2004Publication date: September 16, 2004Inventors: Genevieve N. Boice, Karen M. Conrad, Edward G. Corley, Louis Matty, Jerry A. Murry, Cecile G. Savarin
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Patent number: 6787560Abstract: A serotonin reuptake inhibitor containing a cyclic amine represented by the following formula, a prodrug thereof, or a pharmaceutically acceptable salt of said cyclic amine or prodrug as an active ingredient: wherein R0 is a hydrogen atom, a halogen atom, an alkyl group, a substituted alkyl group, a hydroxyl group, an alkoxy group or the like, R3 is a hydrogen atom or the like, Y is an alkylene group or the like, Z is a hydrogen atom, a cycloalkyl group, an aryl group or the like, n is 1, 2 or 3, and m is 2, 3, 4, 5 or 6.Type: GrantFiled: January 17, 2003Date of Patent: September 7, 2004Assignee: Sumitomo Pharmaceuticals Company LimitedInventors: Toru Kodo, Shuji Masumoto, Koji Koyama, Naoya Kinomura
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Patent number: 6770595Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, 2 or 3, to a plurality of processes for their preparation and to their use as pesticides.Type: GrantFiled: December 19, 2001Date of Patent: August 3, 2004Assignee: Bayer AktiengesellschaftInventors: Andrew Plant, Gerd Kleefeld, Thorsten Pötter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
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Publication number: 20040143122Abstract: The invention provides Zn-chelating compounds that are molecularly engineered to bind to a specific target sequence in a protein of interest. The Zn2+0 ion is far less toxic and promiscuous than nickel and therefore provides an attractive alternative to Ni-based labeling systems. Invention Zn-chelating compounds also do not require oxidizable thiols and therefore can be used in non-reducing environments such as the surface of living cells. In addition, the target sequence is genetically encodable and requires incorporation of only a few amino acids, unlike fusions to fluorescent proteins such as GFP.Type: ApplicationFiled: January 16, 2003Publication date: July 22, 2004Inventors: Roger Y. Tsien, Christina Hauser
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Publication number: 20040142974Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome.Type: ApplicationFiled: November 25, 2003Publication date: July 22, 2004Inventor: Michael Z. Hoemann
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Publication number: 20040122000Abstract: 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: ApplicationFiled: October 21, 2003Publication date: June 24, 2004Applicant: Vertex Pharmaceuticals Incorporated.Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
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Patent number: 6753336Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.Type: GrantFiled: March 11, 2003Date of Patent: June 22, 2004Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
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Patent number: 6750349Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyl-oxy; R2 is hydrogen, C1-6alkyl C1-6alkyloxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk-X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, orType: GrantFiled: June 5, 2002Date of Patent: June 15, 2004Assignee: Janssen Pharmaceutics, N.V.Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
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Publication number: 20040087795Abstract: A process for preparing compound (E) from compound (A), with or without isolation of intermediate products, characterised by one or more of the following steps:Type: ApplicationFiled: June 24, 2003Publication date: May 6, 2004Inventors: Gary Thomas Borrett, Michael Fedouloff, Mark Jason Hughes, Andrew Colin Share, John Bryce Strachan, Peter Szeto, Martyn Voyle
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Patent number: 6723738Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2 , which are the same or different are a) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.Type: GrantFiled: April 8, 2003Date of Patent: April 20, 2004Assignee: Hormos Medical Oy LtdInventors: Marja-Liisa Södervall, Arja Kalapudas, Lauri Kangas, Risto Lammintausta, Pirkko Härkönen, Kalervo Väänänen
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Patent number: 6720336Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.Type: GrantFiled: July 10, 2001Date of Patent: April 13, 2004Assignees: Pfizer, Inc., Pfizer Products, Inc.Inventor: Spiros Liras
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Patent number: 6716986Abstract: The present invention is directed to sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenyl]ester, a metabolite of the 5HT2A antagonist (+)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol and a processes for its preparation and its use in the treatment for a number of disease states.Type: GrantFiled: July 22, 2002Date of Patent: April 6, 2004Assignee: Aventis Pharmaceuticals Inc.Inventors: Ronald Charles Bernotas, Paul Wayne Brown, Gary Thomas Emmons, Chi-Hsin Richard King
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Publication number: 20040048856Abstract: 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: ApplicationFiled: September 4, 2003Publication date: March 11, 2004Applicant: Pfizer IncInventors: Harry R. Howard, Christopher J. Schmidt, Thomas F. Seeger, Mark L. Elliott
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Patent number: 6696469Abstract: Compounds of formula (I): wherein: X represents a heterocycle bonded to the remainder of the molecule by a nitrogen atom of the heterocycle, or an —NR2R3 group wherein R2 represents hydrogen or alkyl, and R3 represents aryl, 1,3 dihydro-2H-benzimidazolyl-2-one or alkyl substituted by a heterocycle, n represents zero or 1, R1 represents hydrogen or alkyl, Ra represents a single bond or an alkylene chain, A represents nitrogen or CH, E represents nitrogen or CRe, wherein Re is as defined in the description, Rb represents a single bond or an alkylene chain as defined in the description, W represents aryl or heteroaryl, Their optical isomers, and addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful for treatment of diseases or pathological conditions in which endothelial dysfunction is known.Type: GrantFiled: October 12, 2001Date of Patent: February 24, 2004Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Jean-Paul Vilaine, Nicole Villeneuve, Catherine Thollon, Marie-Pierre Bourguignon, Christophe Poitevin
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Patent number: 6686473Abstract: The synthesis of paroxetine can be made more convenient by using a solvent system comprising an aliphatic alcohol and a hydrocarbon co-solvent. The solvent system is used particularly in the hydrolysis of paroxetine phenylcarbamate and preferably uses butanol and toluene as the system.Type: GrantFiled: February 15, 2002Date of Patent: February 3, 2004Assignee: Synthon BCT Technologies, LLCInventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Frantisek Picha
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Publication number: 20040006061Abstract: There are described alkoxybenzylamines corresponding to formula 1Type: ApplicationFiled: October 2, 2002Publication date: January 8, 2004Inventors: Wolfgang Haap, Werner Holzl, Karin Petzold
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Patent number: 6673794Abstract: A substituted aminomethyl-phenyl-cyclohexane derivative of formula I or Ia, and their a diastereomer, enantiomer, or of a salt formed with a physiologically tolerated acid. Also disclosed are method for preparing the substituted aminomethyl-phenyl-cyclohexane derivative, pharmaceutical compositions comprising the same and method of using the same for treating pain, urinary incontinence, itching, diarrhea, inflammatory and allergic reactions, depression, drug or alcohol abuse, gastritis, cardiovascular diseases, respiratory tract diseases, coughing, mental illnesses and epilepsy.Type: GrantFiled: July 5, 2002Date of Patent: January 6, 2004Assignee: Gruenenthal GmbHInventors: Claudia Puetz, Wolfgang Strassburger, Babette-Yvonne Koegel
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Publication number: 20030225130Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: 1Type: ApplicationFiled: April 8, 2003Publication date: December 4, 2003Applicant: HORMOS MEDICAL OY LTD.Inventors: Marja-Liisa Sodervall, Arja Kalapudas, Lauri Kangas, Risto Lammintausta, Pirkko Harkonen, Kalervo Vaananen
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Patent number: 6657062Abstract: A process is disclosed for the preparation of compounds of the formula (I), which compounds are useful as intermediates for the preparation of paroxetine of formula(V).Type: GrantFiled: December 28, 1998Date of Patent: December 2, 2003Assignee: Richter Gedeon Vegyesseti Gyar Rt.Inventors: Janos Kreidl, Laszlo Czibula, Andras Nemes, Ida Deutschne Juhasz, Eva Werkne Papp, Juidit Nagyne Bagdy, Laszlo Dobay, Istvan Hegedus, Kalman Harsanyi, Istvan Borza
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Publication number: 20030191126Abstract: A serotonin reuptake inhibitor containing a cyclic amine represented by the following formula, a prodrug thereof, or a pharmaceutically acceptable salt of said cyclic amine or prodrug as an active ingredient: 1Type: ApplicationFiled: January 17, 2003Publication date: October 9, 2003Applicant: SUMITOMO PHARMACEUTICALS COMPANY LIMITEDInventors: Toru Kodo, Shuji Masumoto, Koji Koyama, Naoya Kinomura
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Publication number: 20030191136Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: March 11, 2003Publication date: October 9, 2003Inventors: Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
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Publication number: 20030187269Abstract: A process for the preparation of a compound of formula (1): 1Type: ApplicationFiled: May 8, 2002Publication date: October 2, 2003Inventors: Alan David Curzons, John Edward Richardson, Marian Wladyslaw Wood-Kaczmar
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Publication number: 20030187295Abstract: The invention relates to a method for the production of &OHgr;-aminoalkylsulphonic acids of general formula (I), where R1 and R2=optionally substituted alkyl groups with 1 20 C atoms and n=a whole number from 2 6, whereby an amine of formula (II), where R1 and R2 have the above meanings is reacted with an alkyl dihalide of formula (III), where n has the above meaning and X1 and X2=chlorine or bromine, with addition of alkali hydroxide at a pH of 8 10. The pH is then adjusted to a value of 0 1, by addition of a hydrohalic acid and excess alkyl dihalide is separated off, before the reaction solution is adjusted to a pH of 6 7.5 with alkali liquor, alkali sulphite is added and the product (I) formed at elevated temperate.Type: ApplicationFiled: November 8, 2002Publication date: October 2, 2003Inventors: Volker Schaefer, Wolfgang Knoll, Alexander Schmitt, Christoph Huettner
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Publication number: 20030181483Abstract: The invention is a method for producing &dgr;-aminopentadienoate derivatives of formula (1), the method comprising reacting a streptocyanine derivative of formula (2) with an ester derivative of formula (3) in the presence of an organic base. In formulae (1) to (3), R1 represents an alkyl group or an aryl group; R2, R3, R4 and R5 independently represent a hydrogen atom or an alkyl group; R2 and R3, or R4 and R5 may bond to each other to form a ring; Y represents an electron attractive group; X represents an acid radical; n indicates 0 or a positive number, which is no more than 5; Y may bond to R1 to form a ring.Type: ApplicationFiled: March 25, 2003Publication date: September 25, 2003Inventors: Akihiko Ikegawa, Masuji Motoki, Katsuyoshi Yamakawa