Bicyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/376)
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Patent number: 7189726Abstract: The invention is directed to methods to inhibit p38-? kinase using compounds which contain an aromatic residue coupled to an benzofuran moiety through a piperidine.Type: GrantFiled: May 14, 2002Date of Patent: March 13, 2007Assignee: Scios, Inc.Inventors: Babu J. Mavunkel, Sarvajit Chakravarty, John J. Perumattam, Sundeep Dugar, Qing Lu, Xi Liang
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Patent number: 7186724Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: GrantFiled: April 6, 2004Date of Patent: March 6, 2007Assignee: Aventis Pharmaceuticals Inc.Inventors: James A Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M Shutske, Jospeh T Strupczewski, Kenneth J Bordeau, John G Jurcak, Thaddeus Nieduzak, Sharon A Jackson, Paul Angell, James P Carey, George Lee, David Fink, Jean-Fancois Sabuco, Yulin Chiang, Nicola Collar
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Patent number: 7144883Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous systemType: GrantFiled: June 11, 2002Date of Patent: December 5, 2006Assignee: Biovitrum ABInventors: Patrizia Caldirola, Gary Johansson, Andrew Mott, Katarina Beierlien, Markus Thor, Lars Tedenborg, Ulf Bremberg, Annika Jenmalm Jensen
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Patent number: 7135473Abstract: A cyclic diamine compound of formula (1): wherein R1 and R2 are individually a hydrogen atom or a methoxy group, provided R1 is a methoxy group when R2 is a hydrogen atom, or a hydrogen atom when R2 is a methoxy group; A is an oxygen atom, a sulfur atom, CH?CH, CH?N or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; B is a nitrogen atom, CH or CR4, in which R4 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; m is 1 or 2; and n is a number of 1 to 5, an acid-addition salt thereof, or a hydrate thereof. The compound has inhibitory effects on cell adhesion and is useful for treatment of allergy, asthma, rheumatism, arteriosclerosis, and inflammation.Type: GrantFiled: August 13, 2003Date of Patent: November 14, 2006Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Takeshi Doi, Yoshinori Kyotani
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Patent number: 7115607Abstract: Selected substituted piperazine compounds of Formula I are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: July 24, 2002Date of Patent: October 3, 2006Assignee: Amgen Inc.Inventors: Christopher H. Fotsch, Premilla Arasasingham, Yunxin Bo, Ning Chen, Martin H. Goldberg, Nianhe Han, Feng-Yin Hsieh, Michael G. Kelly, Qingyian Liu, Mark H. Norman, Duncan M. Smith, Markian Stec, Nuria Tamayo, Ning Xi, Shimin Xu
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Patent number: 7094779Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity.Type: GrantFiled: July 3, 2002Date of Patent: August 22, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Wouter I. Iwema Bakker, Jan H. van Maarseveen, Hein K. A. C. Coolen, Martinus Th. M. Tulp, Arnoldus H. J. Herremans, Andrew C. Mccreary, Gustaaf J. M. van Scharrenburg, Adrianus van den Hoogenband
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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: 7067513Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.Type: GrantFiled: August 22, 2000Date of Patent: June 27, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G Kruse, Jacobus Tipker, Martinus T. M Tulp, Gerben M Visser, Bernard J Van Vliet
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Patent number: 7056921Abstract: The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1–C6 alkyl; R1 is H, C1–C6 alkyl or C3–C6 cycloalkyl; R3 is C1–C6 alkyl, C3–C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0–4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.Type: GrantFiled: November 13, 2003Date of Patent: June 6, 2006Assignee: Astrazaneca ABInventors: Stefan Berg, Martin Nylöf, Svante Ross, Seth-Olov Thorberg
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Patent number: 7030241Abstract: The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step.Type: GrantFiled: February 14, 2002Date of Patent: April 18, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Marcel P. M. van Aar, Stefanus J. Schouten, Jan Zorgdrager, Michiel C. Heslinga
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Patent number: 7026314Abstract: Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.Type: GrantFiled: January 15, 2002Date of Patent: April 11, 2006Assignee: AstraZeneca ABInventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
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Patent number: 7026352Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer.Type: GrantFiled: February 1, 2002Date of Patent: April 11, 2006Assignees: Mercian Corporation, Eisai Co., Ltd.Inventors: Yoshiharu Mizui, Takashi Sakai, Satoshi Yamamoto, Keisuke Komeda, Masanori Fujita, Akifumi Okuda, Kumiko Kishi, Jun Niijima, Mitsuo Nagai, Kiyoshi Okamoto, Masao Iwata, Yoshihiko Kotake, Toshimitsu Uenaka, Naoki Asai, Motoko Matsufuji, Tomohiro Sameshima, Naoto Kawamura, Kazuyuki Dobashi, Takashi Nakashima, Masashi Yoshida, Toshio Tsuchida, Susumu Takeda, Tomonari Yamada, Koji Norihisa, Takao Yamori
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Patent number: 6967201Abstract: The present invention provides serotonergic benzofurylpiperazines of Formula I: where: A is a piperazine of formula: and R, R1, R2, R3, R4, R5, R5?, R6, R6?, R7, R7?, R8, and R8? are as described in the specification.Type: GrantFiled: July 21, 2000Date of Patent: November 22, 2005Assignee: Eli Lilly and CompanyInventors: Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Brian Eugene Cunningham, Matthew Joseph Fisher, William Harlan Gritton, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Matthew Robert Reinhard, Dennis Charles Thompson, Leonard Larry Winneroski, Yanping Xu
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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: 6916812Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.Type: GrantFiled: October 4, 2002Date of Patent: July 12, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Graham S. Poindexter, Guanglin Luo, Ling Chen
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Patent number: 6916797Abstract: The invention relates to new ?-arylethylpiperazine of the formula wherein Z represents 0 or S; n? represents 1 or 2; R2 represents a hydrogen atom or a methyl group; W, Ar1 and Ar2 represent various substituents as defined herein; or non-toxic pharmaceutically acceptable salt, individual optical isomer, or individual diastereoisomer thereof, which are useful as neurokinin receptor antagonists (NK1 antagonists). It also relates to processes for their preparation and use in methods for treatment of asthma and/or allergic rhinitis.Type: GrantFiled: December 14, 2000Date of Patent: July 12, 2005Assignee: UCB, S.A.Inventors: Françoise Stiernet, Christophe Genicot, Marie-Agnes Lassoie, Florence Moureau, Thomas Ryckmans, Thierry Taverne, Jean-Pierre Henichart, Michel Neuwels, Solo Goldstein
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Patent number: 6855822Abstract: Benzo[b]furan dimers and processes for their preparation are provided. The invention provides a synthetic process for the preparation of benzo[b]furan dimer using mild reaction conditions, which provides a high substituent tolerance and is appropriate for use in solid phase syntheses for producing a library of benzo[b]furan dimers for biological screening.Type: GrantFiled: June 23, 2003Date of Patent: February 15, 2005Assignee: VivoQuest, Inc.Inventors: Yun Liao, Reza Fathi, Zhen Yang
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Patent number: 6846825Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C4 alkenyloxy, amino, C1-C4 alkylamino, or di-(C1-C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: GrantFiled: August 10, 2000Date of Patent: January 25, 2005Assignee: British Biotech Pharmaceuticals LimitedInventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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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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Patent number: 6825201Abstract: The invention comprises substituted indole, azaindole and related heterocyclic amidopiperazine derivatives of general Formula I wherein: Q is —may represent a bond; A is selected from the group consisting of C1-6alkoxy, C1-6alkyl, C3-7cycloalkyl, phenyl, and heteroaryl; wherein said heteroaryl may be monocyclic or bicyclic and may be comprised of three to eleven atoms selected from the group consisting of C, N, NR9, O, and S, and wherein each ring of said phenyl and heteroaryl is optionally substituted with one to five same or different substituents selected from the group consisting of R19-R23; T is U is NR7, O, or S; V is C(H)kR1, O or N(R7′)k; W is CR3 or NR10; X is CR4 or NR10; Y is CR5 or NR10; Z is CR6 or NR10; k is 0 or 1; and m, n, and p are each independently 0, 1, or 2 provided that the sum of m, n, and p must equal 1 or 2; compositions thereof and their use as antiviral agents, particularly for treating HIV infection.Type: GrantFiled: April 22, 2002Date of Patent: November 30, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Owen B. Wallace, Nicholas A. Meanwell, Zhongxing Zhang, John A. Bender, John F. Kadow, Kap-Sun Yeung
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Patent number: 6780859Abstract: This invention relates to novel benzofuran and dihydrobenzofuran compounds, pharmaceutical compositions containing such compounds, and methods of treating beta-3 adrenoreceptor-mediated conditions with such compositions.Type: GrantFiled: September 10, 2002Date of Patent: August 24, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Gaetan H. Ladouceur, William R. Schoen, Michael J. Burke
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Publication number: 20040157857Abstract: The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) 1Type: ApplicationFiled: November 13, 2003Publication date: August 12, 2004Inventors: Stefan Berg, Martin Nylof, Svante Ross, Seth-Olov Thorberg
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Patent number: 6770650Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 29, 2001Date of Patent: August 3, 2004Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Donald Roy Hirschfeld, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Patent number: 6767907Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cykcloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7 membered ring; R8 is hydrogen or alkyl; have effects at cType: GrantFiled: April 14, 2000Date of Patent: July 27, 2004Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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Publication number: 20040138225Abstract: Compounds of general formula (I), wherein R1 is selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl and triazolyl; where each R1 phenyl ring and R1 heteroaromatic ring optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo.Type: ApplicationFiled: November 17, 2003Publication date: July 15, 2004Applicant: AstraZeneca ABInventors: William Brown, Christopher Walpole, Niklas Plobeck
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Patent number: 6762300Abstract: Process for the preparation of 5-(1-piperazinyl)benzofuran-2-carboxamide in which, as intermediate step, 5-bromosalicylaldehyde or one of its derivatives is reacted in a transition metal-catalysed amination with R2-piperazine, in which R2 is as defined in claim 1.Type: GrantFiled: October 10, 2002Date of Patent: July 13, 2004Assignee: Merck Patent GmbHInventors: Andreas Bathe, Steffen Emmert, Bernd Helfert, Henning Boettcher
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Patent number: 6753331Abstract: The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.Type: GrantFiled: January 4, 2001Date of Patent: June 22, 2004Assignee: AstraZeneca ABInventors: Peter WR Caulkett, Roger James, Stuart E Pearson, Anthony M Slater, Rolf P Walker
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Publication number: 20040110949Abstract: Benzo[b]furan dimers and processes for their preparation are provided. The invention provides a synthetic process for the preparation of benzo[b]furan dimer using mild reaction conditions, which provides a high substituent tolerance and is appropriate for use in solid phase syntheses for producing a library of benzo[b]furan dimers for biological screening.Type: ApplicationFiled: June 23, 2003Publication date: June 10, 2004Inventors: Yun Liao, Reza Fathi, Zhen Yang
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Publication number: 20040110750Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: March 31, 2003Publication date: June 10, 2004Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
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Publication number: 20040110745Abstract: Provided herein is a compound represented by the Formula (I) wherein said compounds are useful for the treatment of migraine. Also provided are processes for the preparation of compounds of Formula (I) and intermediates.Type: ApplicationFiled: July 16, 2003Publication date: June 10, 2004Inventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
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Publication number: 20040087575Abstract: Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.Type: ApplicationFiled: July 16, 2003Publication date: May 6, 2004Inventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
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Patent number: 6730670Abstract: A compound of the formula Compounds of formula I have a good affinity to the A2A receptor and are useful for the treatment of diseases mediated by this receptor.Type: GrantFiled: December 10, 2002Date of Patent: May 4, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Alexander Flohr
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Publication number: 20040077861Abstract: An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.Type: ApplicationFiled: August 25, 2003Publication date: April 22, 2004Inventors: William Brown, Niklas Plobeck
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Patent number: 6723730Abstract: Disclosed are diaryl piperazines and related compounds of the following Formula: wherein the variables are as defined in the specification. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.Type: GrantFiled: July 20, 2001Date of Patent: April 20, 2004Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Alan Hutchinson, Robert W. DeSimone, Kevin J. Hodgetts, James E. Krause, Geoffrey G. White
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Publication number: 20040072828Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.Type: ApplicationFiled: September 17, 2003Publication date: April 15, 2004Applicant: Bayer Pharmaceuticals CorporationInventors: Stephen J. O'Connor, Gaetan H. Ladouceur, William H. Bullock, Ann-Marie Campbell, Miao Dai, Robert Dally, Jacques Dumas, Holia N. Hatoum-Mokdad, Uday Khire, Wendy Lee, Qingjie Liu, Derek B. Lowe, Steven R. Magnuson, Ning Qi, Tatiana E. Shelekhin, Quanrong Shen, Roger A. Smith, Ming Wang
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Publication number: 20040072843Abstract: This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.Type: ApplicationFiled: September 19, 2003Publication date: April 15, 2004Inventors: Gaetan H. Ladouceur, Richard D. Connell, Jeremy Baryza, Ann-Marie Campbell, Timothy G. Lease, James H. Cook
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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: 20040058931Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure 1Type: ApplicationFiled: November 15, 2002Publication date: March 25, 2004Inventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
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Publication number: 20040053940Abstract: Benzofuran derivatives represented by formula (I) or salts thereof: 1Type: ApplicationFiled: June 26, 2003Publication date: March 18, 2004Inventors: Nobuyuki Kawakatsu, Takayuki Namiki, Norihisa Yamazaki, Masayuki Yuasa, Toyohiko Miki, Noriko Suenobu, Tomomasa Shimanuki
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Patent number: 6699864Abstract: The present invention provides compounds of the formula: wherein R1-R8, X, Y, Z, n and m are defined in the application. The compounds of the invention have affinity for the 5-HT1A receptor.Type: GrantFiled: June 20, 2002Date of Patent: March 2, 2004Assignee: H. Lundbeck A/SInventors: Thomas Ruhland, Christian Krog-Jensen, Mario Rottländer, Gitte Mikkelsen, Ejner Knud Moltzen, Kim Andersen
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Patent number: 6700025Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.Type: GrantFiled: January 5, 2001Date of Patent: March 2, 2004Assignee: United Therapeutics CorporationInventors: Robert M. Moriarty, Hitesh Batra
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Publication number: 20040034017Abstract: This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, 1Type: ApplicationFiled: January 7, 2003Publication date: February 19, 2004Inventors: Hermann Kuenzer, Rolf Jautelat, Ludwig Zorn, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
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Publication number: 20040030131Abstract: A compound of the formula in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholino group, said group being optionally substituted with 1 to 3 substituents selected from C1-4 alkyl, hydroxymethyl, C1-4 alkoxymethyl and amido, R3 is a naphthyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; and m is 0 or 1, provided that when m is 1 then n is 1; or a salt or ester thereof.Type: ApplicationFiled: September 3, 2003Publication date: February 12, 2004Inventors: Martine Keenan, Vincent Patrick Rocco, Kumiko Takeuchi, David Edward Tupper, Vincent Vivien
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Publication number: 20040029914Abstract: Novel compounds are useful as chemotherapeutic, chemopreventative, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones.Type: ApplicationFiled: April 18, 2003Publication date: February 12, 2004Inventors: Nurulain Zaveri, Wan-Ru Chao
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Patent number: 6680318Abstract: The present application is directed to compounds having the general formula: and to the use of these compounds in therapeutic methods.Type: GrantFiled: October 21, 2002Date of Patent: January 20, 2004Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole, Niklas Plobeck
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Publication number: 20040009969Abstract: This invention relates to new piperazine derivatives of general formula I, 1Type: ApplicationFiled: November 22, 2002Publication date: January 15, 2004Applicant: Schering AGInventors: Arwed Cleve, Christoph Huwe, Volker Schulze, Helmut Morack, Dieter Zopf, Jens Hoffmann, Andreas Reichel
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Publication number: 20040006090Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: ApplicationFiled: June 9, 2003Publication date: January 8, 2004Inventors: John F. Kadow, Alicia Regueiro-Ren, Qiufen May Xue
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Publication number: 20030232819Abstract: The present invention provides novel tropane compounds and methods for their use.Type: ApplicationFiled: March 27, 2003Publication date: December 18, 2003Inventors: Paul Blundell, Peter C. Meltzer, Bertha K. Madras
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Publication number: 20030229083Abstract: The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I), 1Type: ApplicationFiled: November 27, 2002Publication date: December 11, 2003Applicant: DR. REDDY'S LABORATORIES LIMITEDInventors: Bhuniya Debnath, Saibal Kumar Das, Gurram Ranga Madhavan, Javed Iqbal, Ranjan Chakrabarti, Reeba Kannimel Vikramadithyan
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Publication number: 20030229069Abstract: The present invention provides a compound of the formula: 1Type: ApplicationFiled: June 4, 2003Publication date: December 11, 2003Applicant: Roche Palo Alto LLCInventors: Robin Douglas Clark, Shu-Hai Zhao