Chalcogen Attached Indirectly To The Morpholine Ring By Acyclic Nonionic Bonding Patents (Class 514/238.8)
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Patent number: 6677338Abstract: The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.Type: GrantFiled: February 28, 2002Date of Patent: January 13, 2004Assignees: President and Fellows of Harvard College, Organix, Inc.Inventors: Bertha K. Madras, Peter C. Meltzer
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Publication number: 20040002496Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: March 14, 2003Publication date: January 1, 2004Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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Publication number: 20030232063Abstract: Aminosulfonic acid compounds having the structural formula (I): 1Type: ApplicationFiled: May 19, 2003Publication date: December 18, 2003Applicant: SOCIETE L'OREAL S.A.Inventors: Jean-Baptiste Galey, Dominique Bernard, Lucie Simonetti
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Patent number: 6664254Abstract: The present invention relates to odor eliminating compositions, including air fresheners, and methods of eliminating odors. The inventive compositions comprise soyaethyl morpholinium ethosulfate, benzethonium chloride, and Ordenone®.Type: GrantFiled: February 16, 2000Date of Patent: December 16, 2003Inventor: Wallace Rogozinski
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Patent number: 6649616Abstract: The present invention relates to substituted phenylcyclohexanecarboxamides of the formula (I) to processes for their preparation and to their use in medicaments, in particular for the prevention and/or treatment of cardiovascular disorders.Type: GrantFiled: August 30, 2001Date of Patent: November 18, 2003Assignee: Bayer AktiengesellschaftInventors: Erwin Bischoff, Thomas Krahn, Stephan-Nicholas Müller, Holger Paulsen, Joachim Schuhmacher, Henning Steinhagen, Wolfgang Thielemann
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Patent number: 6638930Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: April 17, 2001Date of Patent: October 28, 2003Assignee: Merck & Co. Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Publication number: 20030181450Abstract: The invention relates to the use of at least one substituted 1-amino-5-phenylpentane-3-ol and/or 1-amino-6-phenyl-hexane-3-ol compound and/or one of the enantiomers thereof and/or one of the diastereomers thereof and/or one of the physiologically acceptable salts thereof for producing a medicament that has an N-methyl-D-aspartate-(NMDA)-antagonistic effect.Type: ApplicationFiled: November 18, 2002Publication date: September 25, 2003Inventors: Bernd Sundermann, Werner Engleberger, Boris Chizh
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Aminothiolester compounds, pharmaceutical and cosmetic compositions containing same and uses thereof
Publication number: 20030181443Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): 1Type: ApplicationFiled: May 6, 2003Publication date: September 25, 2003Inventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore -
Publication number: 20030158151Abstract: The novel active compound combinations of methoximinoacetamide derivatives of the general formula (I), 1Type: ApplicationFiled: October 16, 2002Publication date: August 21, 2003Inventors: Ulrike Wachendorff-Neumann, Thomas Seitz, Herbert Gayer, Ulrich Heinemann, Bernd-Wieland Kruger, Wolfgang Kramer, Lutz Assmann
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Publication number: 20030149019Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), 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 system.Type: ApplicationFiled: May 10, 2002Publication date: August 7, 2003Inventors: Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Lori Sutin, Andrew Mott, Jan Tejbrant
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Publication number: 20030149021Abstract: In accordance with the present invention, there is provided a new class of compounds, i.e., mono(dithio)carbamate esters of piperazine and analogs thereof, with or without substituents. Also provided are methods for the preparation of invention compounds and the pharmaceutical use thereof in the treatment of a variety of pathological conditions, especially for the treatment of cancers. A lead compound has shown good anticancer activity with low toxicity.Type: ApplicationFiled: May 28, 2002Publication date: August 7, 2003Applicant: Medinox, Inc.Inventors: Runtao Li, Tieming Cheng, Jingrong Cui, Tingmin Wang
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Patent number: 6599920Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides naphthalene compounds, intermediates, formulations, and methods.Type: GrantFiled: August 26, 1997Date of Patent: July 29, 2003Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
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Publication number: 20030139402Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: September 20, 2002Publication date: July 24, 2003Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Publication number: 20030134827Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1Type: ApplicationFiled: March 12, 2002Publication date: July 17, 2003Inventors: Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie
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Patent number: 6586431Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.Type: GrantFiled: May 31, 2000Date of Patent: July 1, 2003Assignee: Pfizer IncInventors: Spiros Liras, Martin P. Allen, Barbara E. Segelstein
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Patent number: 6586427Abstract: This patent application describes the treatment of Addictive disorders, Psychoactive Substance Use disorders, Intoxication disorders, Inhalation disorders, Alcohol addiction, Tobacco addiction and or Nicotine addiction; and Attention Deficit Hyperactivity Disorder (ADHD); comprising administering a therapeutically effective, nontoxic dose of Reboxetine and derivatives and or pharmaceutically acceptable salts thereof to a patient.Type: GrantFiled: August 13, 2001Date of Patent: July 1, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Fred Hassan, John Michael McCall, Duncan Paul Taylor, Philip F. Von Voigtlander, Erik Ho Fong Wong
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Publication number: 20030105095Abstract: The present invention relates to a novel 4′-methanesulfonyl-biphenyl derivative having a structure of formula 1 and its pharmaceutically acceptable salts as a highly selective cyclooxygenase-2 inhibitor.Type: ApplicationFiled: October 3, 2002Publication date: June 5, 2003Applicant: CHEIL JEDANG CorporationInventors: Il Hwan Cho, Jee Woong Lim, Ji Young Noh, Jong Hoon Kim, Sang Wook Park, Hyung Chul Ryu, Je Hak Kim, Hyung Ok Chun, So Young Wang, Eun Young Lee
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Publication number: 20030105132Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: ApplicationFiled: March 12, 2002Publication date: June 5, 2003Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
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Patent number: 6562817Abstract: The present invention provides a compound of the formula (I): wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.Type: GrantFiled: July 21, 2000Date of Patent: May 13, 2003Assignee: Shionogi & Co., Ltd.Inventors: Norihiko Tanimoto, Yasushi Hasegawa, Nobuhiro Haga
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Publication number: 20030087934Abstract: The present invention relates to certain substituted polyketides of formula I, 1Type: ApplicationFiled: August 5, 2002Publication date: May 8, 2003Inventors: Frederick R. Kinder, Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Publication number: 20030083330Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, addiction to cocaine or nicotine-containing (especially tobacco) products, or addiction to alcohol using such compound, salts, solvates or compositions.Type: ApplicationFiled: May 17, 2002Publication date: May 1, 2003Inventor: John Joseph Partridge
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Publication number: 20030078262Abstract: This patent application describes, a new combination treatment of selective, noradrenaline-reuptake inhibitors (NARI) and specifically, reboxetine, and pindolol to provide rapid relief to patients suffering from depression, general anxiety, attention deficit hyperactivity disorder (ADHD), anxiety disorders such as obsessive compulsive disorders (OCD), panic disorders (PD), social phobia (SD) and the like.Type: ApplicationFiled: November 5, 2002Publication date: April 24, 2003Applicant: Pharmacia & Upjohn CompanyInventor: Duncan Paul Taylor
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Patent number: 6552225Abstract: A compound of formula (I) wherein: R1, R2, R3, R4, R5, R6 and R7 are as defined within; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.Type: GrantFiled: June 17, 2002Date of Patent: April 22, 2003Assignee: AstraZeneca ABInventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows
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Patent number: 6548679Abstract: The present invention provides compounds of general formula I or II: wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.Type: GrantFiled: August 17, 2000Date of Patent: April 15, 2003Assignee: The Regents of the University of CaliforniaInventors: Trevor C. McMorris, Michael J. Kelner
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Publication number: 20030064988Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation and use; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.Type: ApplicationFiled: May 17, 2002Publication date: April 3, 2003Inventors: Phillip Frederick Morgan, David Lee Musso, John Joseph Partridge
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Publication number: 20030050298Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: September 5, 2002Publication date: March 13, 2003Inventors: Michael R Palovich, Katherine L Widdowson, Hong Nie
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Patent number: 6518265Abstract: 1H-Imidazopyridine derivatives represented by the following general formula or salts thereof: wherein R1 represents hydrogen atom, hydroxyl group, an alkyl group, a cycloalkyl group, styryl group, or an aryl group; R2 represents hydrogen atom, an alkyl group, a halogen atom, hydroxyl group, amino group, a cyclic amino group, or phenoxy group; ring A represents a homocyclic or heterocyclic ring which may be substituted; R3 represents a saturated nitrogen-containing heterocyclic group; and m represents an integer of from 0 to 3. The derivatives have excellent inhibitory actions against production of TNF or IL-1 and are extremely useful as preventive or therapeutic agents for diseases in which a cytokine is mediated.Type: GrantFiled: May 2, 2001Date of Patent: February 11, 2003Assignee: Hokuriku Seiyaku Co., Ltd.Inventors: Hideo Kato, Jun Sakaguchi, Makoto Aoyama, Tomoyuki Izumi, Ken-ichi Kato
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Publication number: 20030027827Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, methods for preparing them, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.Type: ApplicationFiled: May 17, 2002Publication date: February 6, 2003Inventors: Toby Broom, Monica Delpogetto, Richard Atkins, Alan Negus, Paul William Oxley
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Patent number: 6503905Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.Type: GrantFiled: August 6, 1999Date of Patent: January 7, 2003Assignee: Pfizer IncInventors: Spiros Liras, Martin P. Allen, Barbara E. Segelstein
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Patent number: 6498158Abstract: The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 4; —A—B— represents —(CH2)r—, —(CH2)t—O—, —(CH2)t—S(═O)u— or —(CH2)t—NR3—; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is aryl, Het1, C3-7cycloalkyl, cyano, optionally substituted C1-6alkyl, —C(═Q)—X2—R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloalkyl, aryl; where X2 is a direct bond, R15 may also be halo or Het1; where X2 is NR5, R15 may also be hydroxy; where X2 is C(═O)—NH—NH or NH—NH—C(&boType: GrantFiled: May 22, 2001Date of Patent: December 24, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Jean Fernand Armand Lacrampe, Yannick Ligny, Eddy Jean Edgard Freyne, Frederik Dirk Deroose
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Patent number: 6489119Abstract: Disclosed is a method of selecting analgesic agents based on their selective ability to block tetrodotoxin-insensitive sodium channels, particularly in comparison to blocking tetrodotoxin-sensitive sodium channels. Also disclosed is a novel class of compounds that is selective for blocking tetrodotoxin-insensitive sodium channels.Type: GrantFiled: December 6, 1999Date of Patent: December 3, 2002Assignee: Elan Pharmaceuticals, Inc.Inventors: James L. Miller, George P. Miljanich, Stephen S. Bowersox, Laszlo Nadasdi
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Publication number: 20020177593Abstract: Agents for improving potentcy of the urinary bladder which comprises an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action. Particularly, crystals of a tricyclic, condensed, heterocyclic derivative are provided, which possess an excellent action to inhibit acetylcholine esterase and an action to improve the excretory potency of urinary bladder. As an example, crystals of of 8-[3-[1-[(3-fluorophenyl)-methyl]-4-piperidinyl]-1-oxopropyl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one or a salt thereof and pharmaceutical compositions containing them are disclosed.Type: ApplicationFiled: September 24, 2001Publication date: November 28, 2002Inventors: Yuji Ishihara, Takayuki Doi, Hiroshi Nagabukuro, Yuji Ishichi
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Patent number: 6479491Abstract: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.Type: GrantFiled: November 13, 2000Date of Patent: November 12, 2002Assignee: Neurosearch A/SInventors: Oskar Axelsson, Dan Peters, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
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Publication number: 20020147187Abstract: Molecules demonstrating anti-proliferative effects against epithelial cancer cell lines, human estrogen-dependent cancer cells and endothelial cells are disclosed. The molecules are intended for use in therapeutic preparations for the treatment of various cancers. The compounds specified are 1,2-diphenyl-1-naphthyl ethene derivatives.Type: ApplicationFiled: August 21, 2001Publication date: October 10, 2002Inventors: Jonathan Martin Schmidt, Julie Mercure, Shuguang Zhu, John Whelan, Natalie Lazarowych
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Publication number: 20020142985Abstract: A method for treating a glycolipid storage-related disorder, comprising administering a therapeutically effective amount of an inhibitor of glycolipid synthesis in combination with an agent capable of increasing the rate of glycolipid degradation or in combination with bone marrow transplantation. Inhibitors of glycolipid synthesis include N-butyldeoxynojirimycin (NB-DNJ), N-butyldeoxygalactonojirimycin (NB-DGJ) or N-nonyldeoxynojirimycin (NN-DNJ). Glycolipid storage-related disorders include Gaucher disease, Sandhoff's disease, Fabry's disease, Tay-Sach's disease, Niemann-Pick C storage disease, GM1 gangliosidosis, genetic disorders in which neuronal glycolipid accumulation contributes to disease pathology.Type: ApplicationFiled: October 19, 2001Publication date: October 3, 2002Inventors: Raymond A. Dwek, Terence D. Butters
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Patent number: 6432982Abstract: The invention provides novel benzothiophenes of the formula: wherein R1 is —H, —OH, —O(C1-C4 alkyl), —O—CO(C1-C6 alkyl), —OSO2(C4-C6 alkyl, or —OCOAr where Ar is optionally substituted phenyl; R2 is —H, —OH, —Cl, —Br, —O(C1-C4 alkyl), —OCO(C1-C6 alkyl), —OSO2(C4-C6 alkyl, or —OCOAr where Ar is optionally substituted phenyl; R3 is —H, —F, —Cl, —(C1-C4 alkyl), —CN, or —O(C1-C3 alkyl); R4 is —H, —F, —Cl, —(C1-C4 alkyl), —CN or —O(C1-C3 alkyl); R5 is —H, —F, —Cl, —(C1-C4 alkyl), or —O(C1-C3 alkyl); and R6 is —H, —F, —Cl, —(C1-C4 alkyl), or —O(C1-C3 alkyl); with the provisos that R3, R4, R5 and R6 can not all be hydrogen, and that when one of R3, R4, R5 or R6 is C1-C4 alkyl, no more than two of R3, R4, R5 and R6 can be hydrogen; Y is —CO—, —CHOH—, or &mdaType: GrantFiled: January 14, 1997Date of Patent: August 13, 2002Assignee: Eli Lilly and CompanyInventors: George Joseph Cullinan, Kennan Joseph Fahey
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Publication number: 20020099035Abstract: Compounds of the formula: 1Type: ApplicationFiled: January 24, 2001Publication date: July 25, 2002Inventors: Vincent P. Sandanayaka, Arie Zask, Aranapakam M. Venkatesan, Jannie L. Baker, Lalitha Krishnan, Sreenivasulu Megati, Joseph Zeldis
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Patent number: 6417199Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzothiophenes which are a-substituted with ether, thioether amino, hydrazino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.Type: GrantFiled: September 29, 1995Date of Patent: July 9, 2002Assignee: Eli Lilly and CompanyInventor: Brian S. Muehl
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Patent number: 6395755Abstract: The present invention provides a compound of formula I wherein R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2; R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol; R3 is O(CH2)2 or O(CH2)3; R4 and R5 are optionally CO(CH2)3, CO(CH2)4, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline; R6 is and pharmaceutically acceptable salts thereof; useful in treating estrogen deficient pathology.Type: GrantFiled: March 10, 1995Date of Patent: May 28, 2002Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Jeffrey A. Dodge
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Patent number: 6391875Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.Type: GrantFiled: June 22, 2001Date of Patent: May 21, 2002Assignee: SmithKline Beecham CorporationInventors: Phillip Frederick Morgan, David Lee Musso, John Joseph Partridge
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Patent number: 6392040Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: GrantFiled: March 9, 2001Date of Patent: May 21, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert H. Chen, Min A. Xiang
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Publication number: 20020052341Abstract: Methods and compositions are disclosed which utilize metabolites of bupropion for treating disorders ameliorated by inhibition of neuronal monoamine reuptake. Such disorders include, but are not limited to, sexual dysfunction, affective disorders, cerebral function disorders, cigarette smoking, and incontinence. Methods of making optically pure bupropion metabolites are also disclosed.Type: ApplicationFiled: November 16, 2001Publication date: May 2, 2002Applicant: SEPRACOR INC.Inventors: Kevin Qun Fang, Chrisantha Hugh Senanayake, Paul Grover
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Publication number: 20020042410Abstract: Compounds of formula 1, 1Type: ApplicationFiled: July 24, 2001Publication date: April 11, 2002Inventors: Klaus Fuchs, Werner Stransky, Matthias Grauert, Adrian Carter, Wolfram Gaida, Thomas Weiser, Helmut Ensinger
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Patent number: 6355632Abstract: The present invention provides pharmaceutically active compounds formula I wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R2 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl), or halo; R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; and n is 2 or 3; and or a pharmaceutically acceptable salt thereof. Also provided are compounds of formula II wherein R1a is —H or —OR5 in which R5 is a hydroxy protecting group. R2a is —H, halo, or —OR6 in which R6 is a hydroxy protecting group; and R4 is —OH or —CHO; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 3, 2000Date of Patent: March 12, 2002Assignee: Eli Lilly and CompanyInventor: Alan D. Palkowitz
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Patent number: 6352986Abstract: This patent application describes the treatment of Addictive Disorders, Psychoactive Substance Use Disorders, Intoxication disorders, Inhalation disorders, Alcohol addiction, Tobacco Addiction and or Nicotine Addiction; and Attention Deficit Hyperactivity Disorder (ADHD); comprising administering a therapeutically effective, nontoxic dose of Reboxetine and derivatives and or pharmaceutically acceptable salts thereof to a patient.Type: GrantFiled: May 5, 2000Date of Patent: March 5, 2002Assignee: Pharmacia & Upjohn CompanyInventors: Fred Hassan, John Michael McCall, Duncan Paul Taylor, Philip F. Von Voigtlander, Erik Ho Fong Wong
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Patent number: 6352985Abstract: A benzimidazole compound represented by the formula (I): wherein R3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.Type: GrantFiled: January 28, 2000Date of Patent: March 5, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Noritsugu Yamasaki, Takafumi Imoto, Yoshiyuki Murai, Takahiro Hiramura, Teruo Oku, Kouzou Sawada
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Publication number: 20020019396Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.Type: ApplicationFiled: June 22, 2001Publication date: February 14, 2002Inventors: Phillip Frederick Morgan, David Lee Musso, John Joseph Partridge
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Patent number: 6316484Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: August 7, 2000Date of Patent: November 13, 2001Assignee: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
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Patent number: 6274579Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholino and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.Type: GrantFiled: January 20, 1999Date of Patent: August 14, 2001Assignee: Glaxo Wellcome Inc.Inventors: Phillip Frederick Morgan, David Lee Musso, John Joseph Partridge
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Patent number: 6211172Abstract: The present invention relates to a method to inhibit bacteria from adhering to a submergible surface. The method contacts the submergible surface with an effective amount of at least one sulfonamide to inhibit bacterial adhesion to the submergible surface. The present invention also relates to a method for controlling biofouling of an aqueous system. This method adds an effective amount of at least one sulfonamide to inhibit bacteria from adhering to a submerged surface within the aqueous system. This method effectively controls biofouling without substantially killing the fouling organisms. The sulfonamide used in the method of the invention has the following formula: The present invention also relates to a composition containing the sulfonamides and useable in the above methods. The compositions comprise at least one sulfonamide in an amount effective to inhibit bacteria from adhering to submergible or submerged surfaces.Type: GrantFiled: April 26, 1999Date of Patent: April 3, 2001Assignee: Buckman Laboratories International, Inc.Inventors: Mark L. Zollinger, Daniel E. Glover, Marilyn S. Whittemore, Stephen D. Bryant