Chalcogen Bonded Directly To The Bicyclo-carbocyclic Ring System Patents (Class 546/206)
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Publication number: 20040192688Abstract: This invention relates to novel {overscore (&ohgr;)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.Type: ApplicationFiled: October 27, 2003Publication date: September 30, 2004Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Devdutt Chaturvedi, Atul Kumar, Reema Rastogi, Arvind Srivastava, Priti Tewari, Rehan Ahmad, Ramesh Chander, Anju Puri, Geetika Bhatia, Farhan Rizvi, Anil Kumar Rastogi, Suprabhat Ray
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Publication number: 20040158070Abstract: A process for the preparation of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl] methyl piperidine hydrochloride (Donepezil HCl) is disclosed. 5,6-Dimethoxy-2-(pyridin-4-yl) methylene inda-1-one is hydrogenated with a noble metal catalyst or a non-oxide derivative of a noble metal catalyst in a solvent at 20-100° C. and 10-90 psi gauge pressure. The resulting 4-[(5,6-dimethoxy-1-indanon)-2-yl] methyl piperidine is alkylated with an alkylating agent in an organic solvent at 20-80° C.Type: ApplicationFiled: November 17, 2003Publication date: August 12, 2004Inventors: Tarur Venkatasubramanian Radhakrishnan, Sathe Dhanajay Govind, Naidu Avinash Venkatraman
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Patent number: 6774136Abstract: The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.Type: GrantFiled: June 27, 2002Date of Patent: August 10, 2004Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul
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Publication number: 20040143121Abstract: An efficient process for preparation of donepezil is provided.Type: ApplicationFiled: July 24, 2003Publication date: July 22, 2004Applicants: DR. REDDY'S LABORATORIES LIMITED, DR. REDDY'S LABORATORIES, INC.Inventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Mathad Vijayavitthal Thippannachar, Elati Ravi Rama Chandrashekar, Podichetty Anil Kumar, Kolla Naveen Kumar
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Patent number: 6753429Abstract: Compounds of formula I: wherein A, B, D, and R are as defined herein and their agriculturally acceptable salts are disclosed as effective insecticides. In addition, compositions comprising an insecticidally effective amount of a compound of Formula I in admixture with at least one agriculturally acceptable extender or adjuvant and methods of controlling insects comprising applying said compositions to locus on crops where control is desired are disclosed. It is emphasized that this abstract is provided to comply with the rules requiring an abstract that will allow a searcher or other reader to quickly ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope or meaning of the claims (see 37 C.F.R. 1.72(b)).Type: GrantFiled: August 29, 2001Date of Patent: June 22, 2004Assignee: FMC CorporationInventors: George Theodoridis, Edward Barron, Daniel H. Cohen, Ellen M. Crawford, Thomas G. Cullen, Hongyan Qi, Elizabeth Rowley, Syed F. Ali, Walter H. Yeager, Christina B. Duggan
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Patent number: 6734195Abstract: The invention provides a pharmaceutical composition for the treatment of dementia or Alzheimer's disease in which the active therapeutical agent is donepezil hydrochloride in an amorphous state.Type: GrantFiled: August 1, 2002Date of Patent: May 11, 2004Assignee: Chemagis Ltd.Inventors: Alexander Weisman, Chalil Abu Gnim, Rina Uzan, Joseph Kaspi
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Publication number: 20040082611Abstract: Described in the present invention are a sulfonyl derivative represented by the following formula (I):Type: ApplicationFiled: October 9, 2003Publication date: April 29, 2004Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Syozo Kobayashi, Satoshi Komoriya, Noriyasu Haginoya, Masanori Suzuki, Toshiharu Yoshino, Takayasu Nagahara, Tsutomu Nagata, Haruhiko Horino, Masayuki Ito, Akiyoshi Mochizuki
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Publication number: 20040077867Abstract: A compound of the formula: 1Type: ApplicationFiled: August 21, 2003Publication date: April 22, 2004Inventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Publication number: 20040072820Abstract: The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.Type: ApplicationFiled: May 27, 2003Publication date: April 15, 2004Inventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones, Alan David Palkowitz
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Publication number: 20040048893Abstract: The invention provides a process for the preparation of a compound of the formula 6 comprising the hydrolysis and decarboxylation of a compound of the formula 5 according to the reaction: 1Type: ApplicationFiled: June 11, 2003Publication date: March 11, 2004Applicant: CHEMAGIS LTDInventors: Ori Lerman, Joseph Kaspi, Oded Arad, Mohammed Alnabari, Yana Sery
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Patent number: 6677330Abstract: The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a 4-substituted piperidine compound fluoride represented by the following formula, a pharmaceutically acceptable salt thereof or hydrates thereof (provided that 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine, a pharmaceutically acceptable salt thereof and hydrates thereof are excluded). wherein R1 and R2 represent substituents.Type: GrantFiled: August 30, 2001Date of Patent: January 13, 2004Assignee: Eisai Co., Ltd.Inventors: Yoichi Iimura, Takashi Kosasa, Yoshiharu Yamanishi, Hachiro Sugimoto, Yoshio Takeuchi, Tetsuo Shibata, Emiko Suzuki
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Publication number: 20040002517Abstract: The invention provides a pharmaceutical composition for the treatment of dementia or Alzheimer's disease in which the active therapeutical agent is donepezil hydrochloride in an amorphous state.Type: ApplicationFiled: August 1, 2002Publication date: January 1, 2004Applicant: Chemagis Ltd.Inventors: Alexander Weisman, Chalil Abu Gnim, Rina Uzan, Joseph Kaspi
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Publication number: 20030232801Abstract: The invention features compounds for the treatment of cancer and other proliferative diseases. These compounds were identified in screening assays that contact candidate compounds with a cell containing a nucleic acid that includes a HER2 regulatory element and a reporter sequence. The invention further features compounds structurally related to those identified by the screening assays. Finally, the invention features methods of treating or preventing a proliferative disease using the compounds of the invention.Type: ApplicationFiled: April 15, 2003Publication date: December 18, 2003Inventors: Michael Alan Sturgess, Ke Yang
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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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Patent number: 6653321Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: July 28, 2000Date of Patent: November 25, 2003Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
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Patent number: 6649765Abstract: A process for the preparation of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride (Donepezil HCl). 5,6-Dimethoxy-2-(pyridin-4-yl)methylene inda-1-one is hydrogenated with a noble metal oxide catalyst in an organic solvent at 20-50° C. and 10-45 psi gauge pressure. The resulting 4-[(5,6-dimethoxy-1-indanon)-2-yl]methyl piperidine is alkylated with an alkylating agent in an organic solvent at 30-80° C.Type: GrantFiled: February 12, 2003Date of Patent: November 18, 2003Assignee: USV Limited, BSD MARG.Inventors: Joshi Shreerang Vidyadhar, Naidu Avinash Venkatraman, Sutar Rajiv Pandurang
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Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6635650Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: August 8, 2001Date of Patent: October 21, 2003Assignee: Les Laboratoires ServierInventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
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Publication number: 20030181519Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1Type: ApplicationFiled: December 11, 2002Publication date: September 25, 2003Applicant: WyethInventors: Richard E. Mewshaw, Richard J. Edsall, Cuijian Yang, Heather A. Harris, James C. Keith, Leo M. Albert
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Publication number: 20030176461Abstract: Described herein are compounds having general formula (1), wherein groups R1, R2, R3, Ar1, Ar2, Ar3, X, Y, p and n are as defined in the specification, and a salt, solvate and hydrate thereof. Such compounds inhibit glycine transport (or reuptake) via the GlyT-1 transporter, or are precursors (for example, pro-drugs) of such compounds and, thus, are useful in the treatment of schizophrenia, as well as other CNS-related disorders such as dementia, Alzheimer's disease, attention deficit disorder and depression.Type: ApplicationFiled: October 21, 2002Publication date: September 18, 2003Inventors: Ian R. Egle, Jennifer Frey, Methvin B. Isaac, Abdelmalik Slass, Leah E. Begleiter, Louise G. Edwards, Tomislav Stefanac, Ashok Tehim, Shewn P. Maddaford, Hoi Lun Allan Tse
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Publication number: 20030171362Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: December 2, 2002Publication date: September 11, 2003Inventors: Ann Marie Madera, Robert James Weikert
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Patent number: 6617324Abstract: A class of pyrazole derivatives described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.Type: GrantFiled: April 2, 2002Date of Patent: September 9, 2003Assignee: G. D. Searle & CompanyInventors: Ashok S. Naraian, Michael Clare, Paul W. Collins, Joyce Zuowu Crich, Rajesh Devraj, Daniel L. Flynn, Lifeng Geng, Matthew J. Graneto, Cathleen E. Hanau, Gunnar J. Hanson, Susan J. Hartmann, Michael Hepperle, He Huang, Francis J. Koszyk, Shuyuan Liao, Suzanne Metz, Richard A. Partis, Thao D. Perry, Shashidhar N. Rao, Shaun Raj Selness, Michael S. South, Michael A. Stealey, John Jeffrey Talley, Michael L. Vazquez, Richard M. Weier, Xiangdong Xi, Ish K. Khanna, Yi Yu
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Publication number: 20030166925Abstract: The present invention provides a novel compound having a superior acetylcholinesterase inhibitory action.Type: ApplicationFiled: November 25, 2002Publication date: September 4, 2003Inventors: Yoichi Iimura, Takashi Kosasa
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Publication number: 20030166643Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1Type: ApplicationFiled: December 11, 2002Publication date: September 4, 2003Applicant: WyethInventors: Robert E. McDevitt, Folake O. Adebi, Heather A. Harris, James C. Keith, Leo M. Albert
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Patent number: 6613805Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: August 16, 2001Date of Patent: September 2, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Publication number: 20030158225Abstract: The invention provides compounds of general formula (I) wherein Q, R, R2, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: October 21, 2002Publication date: August 21, 2003Inventors: Peter Hansen, Lars Pettersson
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Patent number: 6608089Abstract: Compounds having the formula (I) Z—OCH2—C≡CCH2—NRR1 (I) or a pharmaceutically acceptable salt or solvate thereof wherein Z can represent the formula (1A) or (1B). The compounds possess antiproliferative activity and are useful as modulators of multiple drug resistance in cancer chemotherapy. The compounds may also be useful for the manufacture of a medicament for the treatment or prevention of neoplasms, menopausal disorders and osteoporosis.Type: GrantFiled: February 15, 2002Date of Patent: August 19, 2003Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Piero Valenti
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Publication number: 20030100754Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides naphthalene compounds, intermediates, formulations, and methods.Type: ApplicationFiled: August 26, 1997Publication date: May 29, 2003Inventors: HENRY UHLMAN BRYANT, THOMAS ALAN CROWELL, CHARLES DAVID JONES
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Publication number: 20030087903Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.Type: ApplicationFiled: July 11, 2002Publication date: May 8, 2003Inventors: Rolf Baenteli, Wilfried Bauer, Sylvain Cottens, Claus Ehrhardt, Ulrich Hommel, Jorg Kallen, Josef Gottfried Meingassner, Francois Nuninger, Gabriele Weitz Schmidt
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Patent number: 6531472Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, X and Y have the meanings defined in the specification. The compounds have histone deacetylase (HDAC) inhibitory activity which is useful in cancer treatment. Also provided is a process for making a compound of formula I by reacting a compound of formula III with a compound of formula IV wherein A is a displaceable group and PG is a protecting group.Type: GrantFiled: December 4, 2001Date of Patent: March 11, 2003Assignee: Hoffman-La Roche Inc.Inventors: Guy Georges, Adelbert Grossmann, Tim Sattelkau, Wolfgang Schaefer, Ulrich Tibes
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Patent number: 6521758Abstract: Tosylate salts are useful in purifying 4-(fluorophenyl)-3-carbinol-piperidines from the corresponding des-fluoro impurity. The purified compounds are advantageously used in paroxetine synthesis.Type: GrantFiled: May 14, 2001Date of Patent: February 18, 2003Assignee: Synthon BVInventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Pavel Slanina
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Patent number: 6500818Abstract: Compounds having the following formula wherein L, M, R2, R3, R4, R5, R6, R7, X1 and X2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for treating depression, anxiety, asthma, rheumatoid arthritis, Alzheimer's disease, cancer, schizophrenia, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, emesis, Huntington's disease, psychoses, hypertension, migraine, bladder hypermotility, or urticaria, compositions including such compounds and processes for making such compounds.Type: GrantFiled: March 30, 2001Date of Patent: December 31, 2002Assignee: Astrazeneca ABInventors: Peter Robert Bernstein, Robert Frank Dedinas, Cyrus John Ohnmacht, Keith Russell
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6492522Abstract: The present invention relates to a new process for the preparation of acetylcholinesterase inhibitors of formula (I) or a salt thereof, wherein: R1 is N-acyl-4-piperidyl; N-alkoxycarbonyl-4-piperidyl; N-alkyl-4-piperidyl; N-benzyl-4-piperidyl; N-(&ohgr;-aralkyl)-4-piperidyl; 4-pyridyl; R4, R5, R6, and R7 are identical or different and each represents hydrogen, straight-chain or branched alkyl, aryl, hydroxy, alkoxy, aryloxy, benzyloxy, acyloxy, alkylthio, arylthio, benzylthio, acylamino, phthalimido or halogen; n is 1, 2 or 3; m is 1, 2, 3, 4, or 5. This process comprises cyclisation of a compound of formula (II) or salts thereof, wherein R1, R4, R5, R6 and R7, m and n are as defined above; R2 is selected from a derivatised or non-derivatised carboxyl, cyano, N-substituted aminocarbonyl groups or hydrogen; R3 is selected from a derivatised or non-derivatised carboxyl, cyano or N-substituted aminocarbonyl groups, optionally in the presence of acids and/or solvents.Type: GrantFiled: May 24, 2001Date of Patent: December 10, 2002Assignee: Finetech Laboratories Ltd.Inventors: Arie L. Gutman, Eleonora Shkolnik, Boris Tishin, Genady Nisnevich, Igor Zaltzman
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Publication number: 20020183512Abstract: Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.Type: ApplicationFiled: May 6, 2002Publication date: December 5, 2002Applicant: SLIL Biomedical CorporationInventors: Andrei V. Blokhin, Benjamin Frydman, Laurence J. Marton, Karen M. Neder, Jerry Shunneng Sun
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Patent number: 6486129Abstract: The present invention relates to compounds of formula (1), wherein R1 is phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (iso)quinolinyl, tetrahydro(iso)quinolinyl, 3,4-dihydro-1H-isoquinolinyl, chromanyl or the camphor group, which groups may optionally be substituted with one or more substitutents selected from (1-8C)alkyl or (1-8C)alkoxy; R2 and R3 are independently H or (1-8C)alkyl; R4 is (1-8C)alkyl or (3-8C)cycloalkyl; or R3 and R4 together with the nitrogen atom to which they are bonded are a nonaromatic (4-8)membered ring optionally containing another heteroatom, the ring optionally being substituted with (1-8C)alkyl or SO2-(1-8C)alkyl; Q is a spacer having a chain length of 10 to 70 atoms; and Z is a negatively charged oligosaccharide residue comprising two to six monosaccharide units, the charge being compensated by positively charged counterions; or a pharmaceutically acceptable salt thereof or a prodrug thereof.Type: GrantFiled: December 18, 2000Date of Patent: November 26, 2002Assignees: Akzo Nobel N.V., University LeidenInventors: Cornelia Maria Tromp, Johannes Egbertus Maria Basten, Constant Adriaan Anton van Boeckel, Rogier Christian Buijsman
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Patent number: 6469029Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1-3 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 13, 2000Date of Patent: October 22, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6455531Abstract: Compounds having therapeutic utility are of the formula wherein NB2 is heterocycloalkyl and R1 and R2 are each various substituents or a cyclic group.Type: GrantFiled: March 28, 2001Date of Patent: September 24, 2002Assignee: Darwin Discovery, Ltd.Inventors: David Alan Owen, Andrew Douglas Baxter, Robert John Watson, Duncan Robert Hannah, John Gary Montana
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Publication number: 20020128208Abstract: The disclosed invention is a composition agonists and/or antagonists of V2, V1a or both receptors, in a host, including animals, and especially humans, using a small molecule or its pharmaceutically acceptable salt or prodrug.Type: ApplicationFiled: December 17, 2001Publication date: September 12, 2002Inventors: James P. Snyder, Dennis C. Liotta, Hariharan Venkatesan, Minmin Wang, Matthew C. Davis
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Patent number: 6429317Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.Type: GrantFiled: September 5, 2000Date of Patent: August 6, 2002Assignee: Eli Lilly and CompanyInventors: Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
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Patent number: 6423713Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.Type: GrantFiled: July 31, 2001Date of Patent: July 23, 2002Assignee: G. D. Searle & CompanyInventors: Ashok Anantanarayan, Michael Clare, Paul W. Collins, Joyce Zuowu Crich, Rajesh Devraj, Daniel L. Flynn, Lifeng Geng, Matthew J. Graneto, Cathleen E. Hanau, Gunnar J. Hanson, Susan J. Hartmann, Michael Hepperle, He Huang, Francis J. Koszyk, Shuyuan Liao, Suzanne Metz, Richard A. Partis, Thao D. Perry, Shashidhar N. Rao, Shaun Raj Selness, Michael S. South, Michael A. Stealey, John Jeffrey Talley, Michael L. Vazquez, Richard M. Weier, Xiangdong Xi, Ish K. Khanna, Yi Yu
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Patent number: 6420415Abstract: Compounds represented by general formula (1) or salts thereof which have a matrix metalloprotease inhibitory activity and are useful as drugs, wherein the rings A and B represent each an optionally substituted homocycle or heterocycle, etc.; R1s are the same or different and each represents hydrogen, optionally substituted hydrocarbyl, acyl, etc.; X1 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, etc.; X2 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, —O—, etc.; Ys are the same or different represents hydrogen, optionally substituted hydrocarbyl, oxo, etc.; m is 0 or 1; n is an integer of 1 to 3; q1 is an integer of 1 to 2n+4; and q2 is an integer of 0 to 2n+3, provided that q1+q2 is 2n+4.Type: GrantFiled: March 20, 2001Date of Patent: July 16, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
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Publication number: 20020087002Abstract: Piperidine derivatives, their manufacture and use as medicaments is described. The compounds are useful for treating diseases associated with restenosis, glaucoma, cardiac infarct, high blood pressure and end organ damage, e.g. cardiac insufficiency and kidney insufficiency.Type: ApplicationFiled: December 18, 2001Publication date: July 4, 2002Inventors: Volker Breu, Hans-Peter Marki, Eric Vieira, Wolfgang Wostl
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Patent number: 6413986Abstract: Novel [[(aminocarbonyloxy)-1-indan]-2-yl]methylpiperidines of the formula wherein R is hydrogen, loweralkyl, or a group of the formula R1 is hydrogen or a group of the formula W, X and Y are hydrogen, loweralkyl, loweralkoxy, halogen, nitrogen, or trifluoromethyl; n is 1 or 2; the pharmaceutically acceptable acid addition salts thereof intermediates of the formula and process for the preparation thereof, and a method of relieving memory dysfunction, employing compounds and compositions thereof are disclosed.Type: GrantFiled: May 8, 1995Date of Patent: July 2, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl, Richard C. Effland
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Patent number: 6410530Abstract: New piperidinyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, where 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; n is 0-4; as (R)-enantiomer, (S)-enantiomer or a racemate in the form of the free base or a pharmaceutically acceptable salt or hydrate thereof; a pharmaceutical formulation containing the compounds, use of the compounds in the treatment of 5-hydroxytryptamine mediated disorders, processes for the preparation of the compounds and intermediates for the preparation of the compounds.Type: GrantFiled: August 31, 2000Date of Patent: June 25, 2002Assignee: AstraZeneca ABInventors: Stefan Berg, Lennart Florvall, Svante Ross, Seth-Olov Thorberg
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Publication number: 20020065282Abstract: The present invention provides compounds of formula I 1Type: ApplicationFiled: December 4, 2001Publication date: May 30, 2002Inventors: Guy Georges, Adelbert Grossmann, Tim Sattelkau, Wolfgang Schaefer, Ulrich Tibes
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Patent number: 6369074Abstract: The present invention relates to novel aminomethylene substituted non-aromatic heterocycles and, specifically, to compounds of the formula wherein W, R1, R2, R3, A, X′, Y′ and Z′ are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formulae Ia and Ib are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: October 1, 1999Date of Patent: April 9, 2002Assignee: Pfizer Inc.Inventors: Harry R. Howard, Brian T O'Neill
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Publication number: 20020037895Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.Type: ApplicationFiled: August 13, 2001Publication date: March 28, 2002Inventors: Rolf Baenteli, Wilfried Bauer, Sylvain Cottens, Claus Ehrhardt, Ulrich Hommel, Joerg Kallen, Josef Gottfried Meingassner, Francois Nuninger, Gabriele Weitz Schmidt
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Patent number: 6359138Abstract: The present invention relates to 4-hydroxy-piperidine derivatives of the general formula wherein X denotes —O—, —NH—, —CH2—, —CH═, —CHOH—, —CO—, —S—, —SO— or —SO2—; R1-R4 are, independently from each other, hydrogen, hydroxy, lower-alkyl-sulfonylamino, 1- or 2-imidazolyl or acetamido; R5-R8 are, independently from each other, hydrogen, hydroxy, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or trifluoromethyloxy; a and b may be a double bond, provided that when “a” is a double bond, “b” cannot be a double bond; n is 0-2; m is 1-3; p is 0 or 1 and to pharmaceutically acceptable addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers, which can be used in mediating processes underlying development of CNS including learning and memory formation and function.Type: GrantFiled: November 24, 1997Date of Patent: March 19, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Büttelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, René Wyler
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Patent number: 6333337Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: January 13, 1999Date of Patent: December 25, 2001Assignee: ICAgen, Inc.Inventors: Michael F. Gross, Neil A. Castle