Chalcogen Bonded Directly To A Piperazine Ring Carbon Patents (Class 514/255.02)
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Publication number: 20030236253Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.Type: ApplicationFiled: March 14, 2003Publication date: December 25, 2003Applicant: Gruenenthal GmbHInventors: Boris Chizh, Matthias Gerlach, Michael Haurand, Claudia Puetz, Gero Gaube, D. Enders
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Publication number: 20030225103Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells.Type: ApplicationFiled: March 25, 2003Publication date: December 4, 2003Applicant: DMI BioSciences, Inc.Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K.R. Rao, Greg Thomas
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Publication number: 20030216375Abstract: 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 17, 2002Publication date: November 20, 2003Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
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Publication number: 20030212062Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: March 11, 2003Publication date: November 13, 2003Applicant: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6642225Abstract: Compounds of formula I wherein R is carboxy, esterified carboxy or amidated carboxy; R1 and R3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di-lower alkylamino or mercapto)-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, cycloalkyl, aryl, biaryl, (cycloalkyl, aryl or biaryl)-lower alkyl, or (carboxy, esterified carboxy or amidated carboxy)-lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, arylaminocarbonyl, or aryl-(oxy, thio or amino); n is 1 or 2; Y is lower-alkylene or lower alkenylene; and pharmaceutically acceptable salts thereof; which are useful as LFA-1 antagonists.Type: GrantFiled: October 2, 2001Date of Patent: November 4, 2003Assignee: Novartis AGInventors: Rainer Albert, Janet Dawson, Claus Ehrhardt, Sompong Wattanasin, Gabriele Weitz-Schmidt, Karl Welzenbach
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Patent number: 6638931Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 28, 2000Date of Patent: October 28, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Publication number: 20030198658Abstract: Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and (b) a carrier of at least one mono-C-substituted or di-C-Substituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.Type: ApplicationFiled: May 21, 2003Publication date: October 23, 2003Applicant: Emisphere Technologies, Inc.Inventor: Samuel J. Milstein
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Publication number: 20030191136Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: March 11, 2003Publication date: October 9, 2003Inventors: Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
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Publication number: 20030181464Abstract: A class of phenylsulphonyl derivatives of the following formula (I) wherein Z represents halogen, cyano, nitro, trifluoromethyl, trifluoromethoxy, —Ra, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb; —CORa; —CO2Ra or —CONRaRb; or Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or Z represents an optionally substituted six-membered heteroaromatic ring selected from pyridine, pyrazine, pyrimidine and pyridazine; Ra and Rb independently represent hydrogen of C1-6 alkyl, or Ra and Rb, when linked through a nitrogen atom, together represent the residue of an azetidine, pyrrolidine, piperidine or morpholine ring; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms, optionally incorporating an oxygType: ApplicationFiled: April 21, 2003Publication date: September 25, 2003Inventors: Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher
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Publication number: 20030171379Abstract: Disclosed herein are Mactanamide compounds having the following structural formula 1Type: ApplicationFiled: December 24, 2002Publication date: September 11, 2003Inventors: Robert S. Jacobs, William H. Fenical, Paul R. Jensen, Peter Lorenz
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Publication number: 20030158186Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: December 20, 2002Publication date: August 21, 2003Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Bradley Paul Morgan, Han-Jie Zhou, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans,
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Publication number: 20030149020Abstract: 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 13, 2002Publication date: August 7, 2003Inventors: Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Andrew Mott, Lori Sutin, Jan Tejbrant
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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: 20030144277Abstract: The present application describes modulators of CCR3 of formula (I): 1Type: ApplicationFiled: September 18, 2002Publication date: July 31, 2003Inventor: George V. DeLucca
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Publication number: 20030139419Abstract: Compounds of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: ApplicationFiled: September 27, 2002Publication date: July 24, 2003Inventors: Bernard Barlaam, Robert Dowell, Nicholas John Newcombe, Howard Tucker, David Waterson
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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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Publication number: 20030114442Abstract: The present invention relates to substituted piperazine derivatives of general formula 1Type: ApplicationFiled: October 8, 2002Publication date: June 19, 2003Inventors: Armin Heckel, Thorsten Lehmann-Lintz, Leo Thomas, Michael Mark
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Publication number: 20030109524Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: November 6, 2002Publication date: June 12, 2003Inventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
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Patent number: 6555543Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.Type: GrantFiled: August 2, 2001Date of Patent: April 29, 2003Assignee: DMI BioSciences, Inc.Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K. R. Rao, Greg Thomas
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Publication number: 20030078237Abstract: Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than hydrogen; A is CH2, SO2 or C═O; X is CO2H, PO3H2, PO2H2, PO2HR5, PO2HOR5, SO3H, SO2H, or tetrazole; and R1, R2, R3, R4 and R5 are independently selected from H, alkyl, alkenyl, alkynyl, aryl and aralkyl; or a pharmaceutically acceptable acid salt or base addition salt or an in vivo hydrolysable ester or amide thereof. Compounds of formula (I) are selective NMDA receptor modulating agents and, therefore, may be used to advantage in vitro in neuroassays and in vivo in the treatment of disorders of the CNS.Type: ApplicationFiled: September 3, 2002Publication date: April 24, 2003Inventors: Daniel T Monaghan, David E Jane, Heong Wai Tse
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Publication number: 20030060418Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: ApplicationFiled: August 10, 2001Publication date: March 27, 2003Inventors: Albert Gyorkos, Lyle W. Spruce
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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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Publication number: 20030050309Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.Type: ApplicationFiled: September 12, 2001Publication date: March 13, 2003Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike Radeke, Fengjiang Wang, Liming Shao
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Publication number: 20030050310Abstract: Compounds of formula (I) are matrix metalloproteinase inhibitors wherein X represents a carboxylic acid group —COOH, or a hydroxamic acid group —CONHOH;R2 represents a radical of formula (II): R3—(ALK)m—(Q)p—(ALK)n—, and W represents a cyclic amino radical of formula (IIIA) or (IIIB): 1Type: ApplicationFiled: September 12, 2002Publication date: March 13, 2003Applicant: British Biotech Pharmaceuticals Ltd.Inventor: Fionna Mitchell Martin
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Patent number: 6525042Abstract: Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: [wherein R1 is hydrogen, hydroxyl, nitro or the like; R2 and R3 are each independently hydrogen, halogeno or the like; R4 and R5 are each dependently hydrogen, halogeno or the like; Q1 is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2 is a single bond, oxygen or the like; Q3 is, e.g., a group represented by formula (a): T1 is carbonyl or the like; and X1 and X2 are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.Type: GrantFiled: March 28, 2000Date of Patent: February 25, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Syozo Kobayashi, Satoshi Komoriya, Masayuki Ito, Tsutomu Nagata, Akiyoshi Mochizuki, Noriyasu Haginoya, Takayasu Nagahara, Haruhiko Horino
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Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
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Patent number: 6509337Abstract: A compound of the formula wherein R1-R9 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidemrolysis bullosa, scleritis and other disease characterized by matrix metalloproteinase activity, as well as AIDS, sepsis, septic shock and other diseases involving the production of TNF.Type: GrantFiled: September 17, 1998Date of Patent: January 21, 2003Assignee: Pfizer Inc.Inventors: Anthony Piscopio, James P. Rizzi
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Publication number: 20030013721Abstract: The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy 1Type: ApplicationFiled: June 17, 2002Publication date: January 16, 2003Inventors: Premji Meghani, Colin Bennion
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Publication number: 20030008882Abstract: The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.Type: ApplicationFiled: May 8, 2002Publication date: January 9, 2003Inventors: Andrew D. Hamilton, Justin Ernst, Brendan P. Orner
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Patent number: 6503910Abstract: Compounds of the formula (B)2N—X—(CH2)n—CR1R2—CO—Y (I) have therapeutic utility as inhibitors of metalloproteinases etc.Type: GrantFiled: August 11, 2000Date of Patent: January 7, 2003Assignee: Darwin Discovery Ltd.Inventors: Andrew Douglas Baxter, David Alan Owen, Robert John Watson, John Gary Montana
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Patent number: 6498162Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: November 1, 2000Date of Patent: December 24, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Gerd Schnorrenberg, Kurt Schromm, Horst Dollinger, Birgit Jung, Georg Speck
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Publication number: 20020193382Abstract: The present invention is to provide a compound or a salt thereof represented by the formula: 1Type: ApplicationFiled: April 24, 2002Publication date: December 19, 2002Inventors: Hiroyuki Tawada, Fumio Itoh, Hiroshi Banno, Zen-Ichi Terashita
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Publication number: 20020177575Abstract: The invention relates to the identification of farnesyl-protein transferase (FPT) as a gene that is upregulated in systemic lupus erythematosus (SLE). Given the widespread availability of inhibitors of FPT, the inventors propose to treat the symptoms of SLE using such inhibitors.Type: ApplicationFiled: May 3, 2002Publication date: November 28, 2002Inventors: Ward Wakeland, Kui Liu
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Patent number: 6472393Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: March 21, 2000Date of Patent: October 29, 2002Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
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Publication number: 20020156064Abstract: This invention relates to certain benzenesulfonamides and their use as PDE7 inhibitorsType: ApplicationFiled: February 28, 2002Publication date: October 24, 2002Applicant: SmithKline Beecham CorpInventors: Kelly M. Aubart, Siegfried B. Christensen, Jack D. Leber
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Publication number: 20020155993Abstract: Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and (b) a carrier of at least one mono-C-substituted or di-C-substituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.Type: ApplicationFiled: April 19, 2002Publication date: October 24, 2002Applicant: Emisphere Technologies, Inc.Inventor: Sam J. Milstein
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Patent number: 6455532Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: A is wherein Y1 and Y2 are independently hydrogen, C1-4 alkyl, C1-4 alkoxy, FuHvC(CH2)0-1 O—, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1, C3-7 cycloalkyl, thio C1-4 alkyl, C1-4 sulfinylalkyl, C1-4 sulfonylalkyl, halogen cyano, or trifluoromethyl, and wherein b is 0 or 1.Type: GrantFiled: June 1, 2000Date of Patent: September 24, 2002Assignee: Merck & Co., Inc.Inventors: Christopher S. Burgey, Kyle A. Robinson, Peter D. Williams, Craig Coburn, Terry A. Lyle, Philip E. Sanderson
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Publication number: 20020128270Abstract: A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R 1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R 2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R 3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued amino, R 4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group, R 5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R 10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 22, 2001Publication date: September 12, 2002Applicant: FUJISAWA PHARMACEUTICAL CO., LTD.Inventors: Masahiro Neya, Hitoshi Yamazaki, Natsuko Kayakiri, Kentaro Sato, Teruo Oku
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Publication number: 20020123492Abstract: The present invention relates beta-amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: September 5, 2002Inventors: David Lauffer, Michael Mullican
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Publication number: 20020099057Abstract: The present invention relates to a method and a medicament for pharmacological treatment of accidental extravasation of topoisomerase II poisons such as anthracyclines. In particular, the invention relates to the use of a topo II catalytic nhibitor such as the bisdioxopiperazine ICRF-187 for the manufacture of a medicament for the treatment of an accidental extravasation of a topoisomerase II poison and a method for treatment of such extravasation of a topoisomerase poison such as the anthracyclines daunorubicin, doxorubicin, epirubicin, or idarubicin. In addition, the invention relates to a kit for such treatment.Type: ApplicationFiled: June 29, 2001Publication date: July 25, 2002Inventors: Seppo W. Langer, Peter B. Jensen, Maxwell Sehested
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Publication number: 20020082263Abstract: Compounds having the structure 1Type: ApplicationFiled: December 11, 2000Publication date: June 27, 2002Inventors: Boliang Lou, Adnan M.M. Mjalli
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Patent number: 6407120Abstract: The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.Type: GrantFiled: January 28, 2000Date of Patent: June 18, 2002Assignee: Pfizer Inc.Inventors: Philip A. Carpino, Marlys Hammond, Richard F. Hank
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Patent number: 6403595Abstract: The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which have activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.Type: GrantFiled: August 3, 2000Date of Patent: June 11, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroyuki Tawada, Fumio Itoh, Hiroshi Banno, Zen-ichi Terashita
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Publication number: 20020068737Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 14, 2001Publication date: June 6, 2002Applicant: Synaptic Pharamceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Publication number: 20020065264Abstract: A class of cysteine protease inhibitors which inactivate a cysteine protease by covalently bonding to the protease and releasing a heterocyclic leaving group is presented. The cysteine protease inhibitors of the present invention comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a heterocyclic leaving group. The heterocyclic leaving group of the protease inhibitor is of the formula: —O— Het, where Het is a heterocycle having 4-7 atoms in the ring, with at least one of the heterocycle atoms being N, O or S.Type: ApplicationFiled: June 11, 2001Publication date: May 30, 2002Inventors: Mary P. Zimmerman, Robert E. Smith
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Publication number: 20020065265Abstract: One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.Type: ApplicationFiled: September 12, 2001Publication date: May 30, 2002Inventors: Xinhe Wu, Brian M. Aquila, Liming Shao, Heike Radeke, Gregory D. Cuny, James R. Hauske, Roger L. Xie
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Publication number: 20020061878Abstract: Compounds of formula I 1Type: ApplicationFiled: October 2, 2001Publication date: May 23, 2002Inventors: Rainer Albert, Janet Dawson, Claus Ehrhardt, Sompong Wattanasin, Gabriele Weitz-Schmidt, Karl Welzenbach
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Publication number: 20020052381Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells.Type: ApplicationFiled: August 2, 2001Publication date: May 2, 2002Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K.R. Rao, Greg Thomas
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Patent number: 6369063Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: April 9, 2002Assignee: Cor Therapeutics, Inc.Inventors: Ting Su, Bing-Yan Zhu, Robert M. Scarborough
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Publication number: 20020035145Abstract: The invention provides methods for treating neuropsychiatric disorders such as schizophrenia, Alzheimer's Disease, autism, depression, benign forgetfulness, childhood learning disorders, close head injury, and attention deficit disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) a therapeutically effective amount of D-alanine (or a modified form thereof), provided that the composition is substantially free of D-cycloserine, and/or (ii) D-serine (or a modified form thereof), and/or (iii) 105 to 500 mg of D-cycloserine (or a modified form thereof), and/or (iv) N-methylglycine (or a modified form thereof).Type: ApplicationFiled: April 13, 2001Publication date: March 21, 2002Applicant: The General Hospital CorporationInventors: Guochuan Tsai, Joseph Coyle