Isoquinolines (including Hydrogenated) Patents (Class 514/253.05)
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Publication number: 20040077656Abstract: Piperazine derivatives, containing a quinoline analog moiety, of formula (I) and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammal, particularly in man.Type: ApplicationFiled: November 13, 2003Publication date: April 22, 2004Inventors: Roger Edward Markwell, Neil David Pearson, Christian Smethurst
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Publication number: 20040072850Abstract: The present invention relates to compounds of formula I: 1Type: ApplicationFiled: June 27, 2003Publication date: April 15, 2004Inventors: Ronald Knegtel, Michael Mortimore, John Studley, David Millan
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Publication number: 20040067960Abstract: This invention relates to compounds of the formula 1 1Type: ApplicationFiled: September 26, 2003Publication date: April 8, 2004Inventors: Jamie Marie Davis, Tracy Fay Gregory, Michael Anthony Walters
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Publication number: 20040038969Abstract: Compounds having the general structure 1Type: ApplicationFiled: May 20, 2003Publication date: February 26, 2004Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Vassil I. Ognyanov, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Liping H. Pettus, Hui-Ling Wang, Xianghong Wang, Premilla Arasasingham
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Patent number: 6696480Abstract: A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell Nitric Oxide Synthase activity. As a result, agents that disrupt actin cytoskeletal organization are useful in treating or preventing conditions that result from the abnormally low expression and/or activity of endothelial cell Nitric Oxide Synthase. Such conditions include hypoxia-induced conditions. Subjects thought to benefit mostly from such treatments include nonhyperlipidemics and nonhypercholesterolemics, but not necessarily exclude hyperlipidemics and hypercholesterolemics.Type: GrantFiled: May 13, 2002Date of Patent: February 24, 2004Assignee: Brigham and Women's Hospital, Inc.Inventor: James K. Liao
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Publication number: 20040034011Abstract: Compounds of formula (I′), wherein A, R1 to R3 and t are as defined in the disclosure, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: July 9, 2003Publication date: February 19, 2004Inventors: Reijo Bckstrm, Jarmo Pystynen, Timo Lotta, Martti Ovaska, Jyrki Taskinen
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Publication number: 20040029841Abstract: The present invention provides methods for treating individuals suffering from depression. The methods are based on the administration of a therapeutically effective amount of a substance that lowers the circulating concentration of a purinergic compound or that acts as an antagonist to a purinergic receptor.Type: ApplicationFiled: April 15, 2003Publication date: February 12, 2004Inventor: Perry F. Renshaw
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Patent number: 6686351Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: February 27, 2002Date of Patent: February 3, 2004Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Qi Chao
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Patent number: 6683083Abstract: Disclosed herein is a method for suppressing the growth of cancer cells in a mammal in need of such treatment comprising administering to said mammal a cancer cell suppressing amount of a diphenylmethylpiperazine represented by the following general formula [1]: wherein R represents: or a pharmaceutically acceptable salt thereof. Compared with conventional anticancer agents, these agents are less toxic and exert an excellent carcinostatic effect on various solid cancers. Moreover, these anticancer agents inhibit the proliferation of fibroblasts, which makes them efficacious against pulmonary fibrosis and proliferative keloid lesions.Type: GrantFiled: August 2, 2002Date of Patent: January 27, 2004Inventors: Noboru Kaneko, Kazuto Nishio
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Publication number: 20040009985Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. 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: March 20, 2003Publication date: January 15, 2004Inventors: Tao Wang, Owen B. Wallace, Nicholas A. Meanwell, John F. Kadow, Zhongxing Zhang, Zhong Yang
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Publication number: 20040006069Abstract: 1Type: ApplicationFiled: March 27, 2003Publication date: January 8, 2004Inventors: Kyungae Lee, Scott Mitchell, Robert Ohliger, Lu Yan Zhang, He Zhao, Kevin Currie
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Publication number: 20030232822Abstract: An indole derivative having the formula 1Type: ApplicationFiled: December 17, 2002Publication date: December 18, 2003Applicant: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jakob Felding, Jan Kehler
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Publication number: 20030229077Abstract: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of PDGF receptor to hinder abnormal cell growth and cell wandering and thus are useful for the prevention or treatment of cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.Type: ApplicationFiled: August 26, 2002Publication date: December 11, 2003Inventors: Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shigeki Fujiwara, Shinichi Ide, Eiji Tsukuda, Junko Irie, Shoji Oda
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Publication number: 20030216385Abstract: The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.Type: ApplicationFiled: November 18, 2002Publication date: November 20, 2003Inventors: Takahiko Tobe, Takashi Sugane, Wataru Hamaguchi, Itsuro Shimada, Kyoichi Maeno, Junji Miyata, Tetsuya Kimizuka, Takeshi Suzuki, Atsuyuki Kohara, Takuma Morita, Michael Arlt, Hartmut Greiner
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Publication number: 20030203905Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: March 25, 2003Publication date: October 30, 2003Inventors: John Cochran, Roger Tung
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Publication number: 20030199495Abstract: Disclosed are compounds having the formula: 1Type: ApplicationFiled: March 29, 2002Publication date: October 23, 2003Inventor: Laszlo Prokai
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Patent number: 6635647Abstract: The invention provides compounds of formula (I) wherein A, B and R are as defined herein and the preparation thereof. The compounds of formula (I) are useful as somatostatin antagonists.Type: GrantFiled: September 18, 2002Date of Patent: October 21, 2003Assignee: Novartis AGInventor: Thomas J. Troxler
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Publication number: 20030176441Abstract: The invention provides compounds of Formula (I): 1Type: ApplicationFiled: November 29, 2002Publication date: September 18, 2003Inventors: Daisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
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Publication number: 20030176424Abstract: Regenerative growth of an adult mammalian central nervous system neuron axon subject to growth inhibition by endogenous, myelin growth repulsion factors is promoted by delivering to the axon a therapeutically effective amount of a specific inhibitor of protein kinase C, whereby regenerative growth of the axon is promoted and a resultant promotion of the regenerative growth of the axon is detected.Type: ApplicationFiled: March 14, 2003Publication date: September 18, 2003Applicant: Children's Medical Center CorporationInventors: Zhigang He, Vuk Koprivica, Rajeev Sivasankaran
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Publication number: 20030176423Abstract: Regenerative growth of an adult mammalian central nervous system neuron axon subject to growth inhibition by endogenous, myelin growth repulsion factors is promoted by delivering to the axon a therapeutically effective amount of a specific inhibitor of protein kinase C, whereby regenerative growth of the axon is promoted and a resultant promotion of the regenerative growth of the axon id detected.Type: ApplicationFiled: March 14, 2002Publication date: September 18, 2003Applicant: Children's Medical Center CorporationInventors: Zhigang He, Vuk Koprivica, Rajeev Sivasankaran
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Publication number: 20030158198Abstract: Compound of formula (I) 1Type: ApplicationFiled: February 11, 2003Publication date: August 21, 2003Inventors: Chih-Hung Lee, Erol K. Bayburt, Stanley DiDomenico, Irene Drizin, Arthur R. Gomtsyan, John R. Koenig, Richard J. Perner, Robert G. Schmidt, Sean C. Turner, Tammie K. White, Guo Zhu Zheng
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Publication number: 20030158188Abstract: Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.Type: ApplicationFiled: February 20, 2002Publication date: August 21, 2003Inventors: Chih-Hung Lee, Erol K. Bayburt, Stanley DiDomenico, Irene Drizin, Arthur R. Gomtsyan, John R. Koenig, Richard J. Perner, Robert G. Schmidt, Sean C. Turner, Tammie K. White, Guo Zhu Zheng
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Publication number: 20030158177Abstract: A melanin-concentrating hormone antagonist comprising a compound of the formula: 1Type: ApplicationFiled: November 12, 2002Publication date: August 21, 2003Inventors: Yuji Ishihara, Jun Terauchi, Nobuhiro Suzuki, Shiro Takekawa, Kazuyoshi Aso
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Publication number: 20030153580Abstract: The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity.Type: ApplicationFiled: December 11, 2002Publication date: August 14, 2003Inventors: Norman Kong, Emily Aijun Liu, Binh Thanh Vu
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Patent number: 6602867Abstract: Triazole compounds of the following formula where R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3 receptor and can therefore be used for treating diseases which respond to the influence of dopamine D3 ligands.Type: GrantFiled: July 11, 2001Date of Patent: August 5, 2003Assignee: Abbott LaboratoriesInventors: Dorothea Starck, Hans-Jörg Treiber, Liliane Unger, Barbara Neumann-Schultz, Kai Blumbach, Dietmar Schöbel
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Patent number: 6593322Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-&bgr;. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: September 21, 2000Date of Patent: July 15, 2003Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah Marie Gayo-Fung, Bernd M. Stein, Qi Chao, Anthony R. Gangloff, Jeffrey A. McKie, Kenneth D. Rice
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Publication number: 20030130276Abstract: The present invention provides methods of treating cancer of the liver, ovarian cancer, a desmoid tumor, glioma, pancreatic cancer, or renal cell carcinoma using an estrogen agonist/antagonist. The present invention also provides kits that contain an estrogen agonist/antagonist for treating cancer of the liver, ovarian cancer, a desmoid tumor, glioma, pancreatic cancer, or renal cell carcinoma.Type: ApplicationFiled: January 23, 2002Publication date: July 10, 2003Inventor: Robert L. Rosati
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Patent number: 6583155Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.Type: GrantFiled: February 13, 2002Date of Patent: June 24, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Christopher R. Butler, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Clark A. Sehon, Siquan Sun, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei
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Publication number: 20030114423Abstract: Methods for treating CMV and CMV-related diseases are provided that use compounds having the formula: 1Type: ApplicationFiled: August 29, 2002Publication date: June 19, 2003Applicant: ChemoCentryx, Inc.Inventors: Brian E. McMaster, Thomas J. Schall, Mark Penfold, J.J. Wright, Daniel J. Dairaghi
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Publication number: 20030105102Abstract: Compounds, compositions containing compounds, methods of sing compounds, and processes of making compounds, of formula I containing at least one ring nitrogen: 1Type: ApplicationFiled: April 1, 2002Publication date: June 5, 2003Applicant: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Kevin Leonard Tays, Jie Zhang
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Patent number: 6573262Abstract: The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I, compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.Type: GrantFiled: December 19, 2001Date of Patent: June 3, 2003Assignee: Bristol-Myers Sqibb CompanyInventors: Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin
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Publication number: 20030087901Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: ApplicationFiled: February 27, 2002Publication date: May 8, 2003Applicant: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Qi Chao
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Patent number: 6559186Abstract: Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an &agr;-1-adrenergic antagonist, &agr;-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.Type: GrantFiled: August 5, 1994Date of Patent: May 6, 2003Assignee: Arc 1, Inc.Inventor: James N. Campbell
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Publication number: 20030073669Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: April 17, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20030069245Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. 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: December 19, 2001Publication date: April 10, 2003Inventors: Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin
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Patent number: 6518273Abstract: The present invention relates to compounds of the formula (I): wherein R1a, R1b, R2, R3, R4, R5, X and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.Type: GrantFiled: September 4, 2001Date of Patent: February 11, 2003Assignee: Merck Sharp & Dohme Ltd.Inventors: Kevin Tyler Chapman, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Steven Michael Hutchins, Duncan Edward Shaw, Christopher Alan Willoughby
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Patent number: 6518272Abstract: This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5-7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionallyType: GrantFiled: March 27, 2002Date of Patent: February 11, 2003Assignee: WyethInventors: Wayne E. Childers, Michael G. Kelly, Yvette L. Palmer, Edward J. Podlesny
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Publication number: 20030027832Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I 1Type: ApplicationFiled: June 27, 2002Publication date: February 6, 2003Applicant: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler, Jakob Felding
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Publication number: 20030013703Abstract: A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell Nitric Oxide Synthase activity. As a result, agents that disrupt actin cytoskeletal organization are useful in treating or preventing conditions that result from the abnormally low expression and/or activity of endothelial cell Nitric Oxide Synthase. Such conditions include hypoxia-induced conditions. Subjects thought to benefit mostly from such treatments include nonhyperlipidemics and nonhypercholesterolemics, but not necessarily exclude hyperlipidemics and hypercholesterolemics.Type: ApplicationFiled: May 13, 2002Publication date: January 16, 2003Inventor: James K. Liao
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Publication number: 20020165203Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: November 7, 2002Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Patent number: 6472392Abstract: Triazole compounds of the following formula: where Ar1, A, B and Ar2 have the meanings given in the description, possess a high affinity for the dopamine D3 receptor and can therefore be used for treating diseases which respond to dopamine D3 ligands.Type: GrantFiled: December 28, 1999Date of Patent: October 29, 2002Assignee: Abbott LaboratoriesInventors: Dorothea Starck, Stefan Blank, Hans-Jörg Treiber, Liliane Unger, Barbara Neumann-Schultz, Theophile-Marie Le Bris, Hans-Jürgen Teschendorf, Karsten Wicke
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Patent number: 6462048Abstract: The present invention relates to lactam derivatives of the formula wherein R1, R2, R3, A, X, Z, n and the dashed line are defined herein, and pharmaceutical compositions thereof, to processes and intermediates for their preparation, and to their medicinal use as selective agonists and antagonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1D receptors. These compounds are useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.Type: GrantFiled: September 24, 1998Date of Patent: October 8, 2002Assignee: Pfizer Inc.Inventor: Harry R. Howard
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Patent number: 6448244Abstract: The present invention concerns novel water-soluble azole compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof; as antifungals; their processes for preparation, composition containing them and their use as a medicine.Type: GrantFiled: November 9, 2000Date of Patent: September 10, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken
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Patent number: 6436923Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: March 17, 2000Date of Patent: August 20, 2002Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Bernd M. Stein, Qi Chao, Anthony R. Gangloff, Jeffrey A. McKie, Kenneth D. Rice
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Publication number: 20020111358Abstract: The present invention relates to a phenoxypropylamine compound of the formula (I) 1Type: ApplicationFiled: November 23, 2001Publication date: August 15, 2002Inventors: Akira Nishiyama, Masahiro Bougauchi, Takanobu Kuroita, Masanori Minoguchi, Yasunori Morio, Kouji Kanzaki
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Patent number: 6423751Abstract: A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell Nitric Oxide Synthase activity. As a result, agents that disrupt actin cytoskeletal organization are useful in treating or preventing conditions that result from the abnormally low expression and/or activity of endothelial cell Nitric Oxide Synthase. Such conditions include pulmonary hypertension, ischemic stroke, impotence, heart failure, hypoxia-induced conditions, insulin deficiency, progressive renal disease, gastric or esophageal motility syndrome, etc. Subjects thought to benefit mostly from such treatments include nonhyperlipidemics and nonhypercholesterolemics, but not necessarily exclude hyperlipidemics and hypercholesterolemics.Type: GrantFiled: July 14, 1998Date of Patent: July 23, 2002Assignee: The Brigham and Women's Hospital, Inc.Inventor: James K. Liao
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Patent number: 6417362Abstract: Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia.Type: GrantFiled: November 30, 1999Date of Patent: July 9, 2002Assignee: Meiji Seika Kaisha, Ltd.Inventors: Naoto Ohkura, Takashi Tsuruoka, Takayuki Usui, Yukiko Hiraiwa, Tetsuya Matsushima, Masaharu Shiotani, Tetsutaro Niizato, Yuuko Nakatani, Shigeki Suzuki, Chidsuko Kuroda, Kiyoaki Katano
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Publication number: 20020072520Abstract: Sulfonylcarboxamide derivatives of formula I, their physiologically acceptable salts and/or physiologically functional derivatives, methods of making these compounds, their use for preparing medicines for the prevention and treatment of hyperlipidemia and arteriosclerotic disorders.Type: ApplicationFiled: September 27, 2001Publication date: June 13, 2002Inventors: Reinhard Kirsch, Hans-Ludwig Schaefer, Eugen Falk, Horst Hemmerle
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Patent number: 6399617Abstract: The invention provides a method of treatment or prophylaxis of obesity, comprising administering to a patient in need of such treatment a therapeutically effective amount of an aryl sulfonamide compound of formula (I) or formula (II) wherein the substituents are as described in the specification.Type: GrantFiled: July 20, 2001Date of Patent: June 4, 2002Assignee: Biovitrum ABInventors: Patrizia Caldirola, Sukhwinder Jossan, Kjell S. Sakariassen, Jan Svartengren
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Patent number: 6387389Abstract: The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using such sustained-release derivatives to bind the dopamine transporter to achieve a desired effect, such as antagonism of dopamine reuptake inhibitors, such as cocaine, or dopamine releasers or norepinephrine and/or serotonin reuptake inhibitors, such as methamphetamine.Type: GrantFiled: June 30, 1999Date of Patent: May 14, 2002Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Richard B. Rothman, Kenner C. Rice, David Lewis, Dorota Matecka, John R. Glowa