Abstract: Disclosed are compounds of the formulas (I) & (II) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds.
wherein G, X, A and Q are described herein.
Type:
Grant
Filed:
October 11, 2002
Date of Patent:
November 30, 2004
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Pier Francesco Cirillo, Abdelhakim Hammach, John R. Regan
Abstract: The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel bicyclic diamide compounds that are neuroprotective and/or neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
November 21, 2000
Date of Patent:
November 16, 2004
Assignee:
Bristol-Myers Squibb Company
Inventors:
Gene Michael Dubowchik, David Paul Provencal
Abstract: The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-&agr;, NFK-&bgr; and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library and as individual compounds. In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-&agr;, TNF-&bgr; and also apoptosis.
Type:
Grant
Filed:
December 28, 2001
Date of Patent:
November 9, 2004
Assignee:
Celltech R & D, Inc.
Inventors:
Jim P. Boyce, J. Jeffry Howbert, John C. Tabone
Abstract: The present invention provides a novel a condensed polycyclic compound useful as a phosphodiesterase 4 inhibitor, which is shown by the formula [I]: 1
Type:
Application
Filed:
February 6, 2004
Publication date:
October 14, 2004
Inventors:
Tatsuzo Ukita, Yoshihiro Terakawa, Kazuteru Wada, Aya Nakata, Atsuko Sakai, Koji Ogawa
Abstract: The present invention refers to the use of novel molecules able to bind tenaciously to silica, borosilicate and silicate surfaces, and thus to modify their properties and characteristics. When applied to silica-based chromatography, it offers important advantages in all cases in which it is necessary to modulate the interaction of analytes with the stationary phase. In capillary zone electrophoresis (CZE), such compounds will eliminate or invert the electroendoosmostic (EEO) flow, greatly simplifying the analysis of negatively-charged compounds and permitting the analysis of bio(macro)molecules via the direct use of naked capillaries.
Type:
Grant
Filed:
July 3, 2002
Date of Patent:
August 17, 2004
Inventors:
Attilio Citterio, Roberto Sebastiano, Cecilia Gelfi, Pier Giorgio Righetti
Abstract: The object of the present invention is to provide soluble &bgr;-amyloid precursor protein secretory stimulators, which are effective in treating neurodegenerative diseases as well as cerebrovascular disorder-induced neuronopathy.
Abstract: The invention discloses compounds that are selective &agr;7 nAChR agonists and 5-HT3 antagonists. The compounds are useful for treating many CNS diseases.
Type:
Application
Filed:
October 31, 2003
Publication date:
July 29, 2004
Inventors:
Erik Ho Fong Wong, Luz A. Cortes-Burgos, Bruce Nelson Rogers, David W. Piotrowski, Daniel Patrick Walker, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka
Abstract: The present invention provides a compound of formula I 1
Type:
Application
Filed:
December 23, 2003
Publication date:
July 22, 2004
Inventors:
Gordon L. Bundy, Fred L. Ciske, Michael J. Genin, Steven E. Heasley, Scott D. Larsen, Byung Hyun Lee, Paul D. May, John R. Palmer, Mark E. Schnute, Valerie A. Vaillancourt, Atli Thorarensen, Allison J. Wolf, Nancy Anne Wicnienski, David Wilhite
Abstract: The invention relates to compounds of the general formula (I):
wherein
Ar is optionally substituted aryl or heteroaryl;
A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members;
B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—;
R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl;
R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ri
Type:
Grant
Filed:
October 11, 2002
Date of Patent:
July 6, 2004
Assignee:
Biovitrum AB
Inventors:
Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
Abstract: The invention provides a compound of formula I
wherein X, R1, R2 and Het are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.
Abstract: This invention relates to a novel class of heterocyclic compounds that bind chemokine receptors, inhibiting the binding of their natural ligands thereby. These compounds result in protective effects against infection by HIV through binding to chemokine receptors, including CXCR4 and CCR5, thus inhibiting the subsequent binding by these chemokines.
Type:
Grant
Filed:
March 24, 2000
Date of Patent:
June 15, 2004
Assignee:
AnorMED, Inc.
Inventors:
Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols
Abstract: The present invention provides monocyclic, bicyclic and oligomeric amine compounds with at least two sites of diversity. These compounds are formed from monocyclic scaffolds which can be cyclized to form bicyclic amine scaffolds. These can then be reacted with building blocks to form the amine compounds of the invention. This invention further provides libraries or monocyclic, bicyclic and oligomeric amine compounds. Also provided are methods for preparing monocyclic, bicyclic and oligomeric amine compounds and libraries thereof. The present invention also provides pharmaceutical compositions of the monocyclic, bicyclic and oligomeric amine compounds.
Type:
Grant
Filed:
September 5, 1997
Date of Patent:
June 15, 2004
Assignee:
ISIS Pharmaceuticals, Inc.
Inventors:
Eric Edward Swayze, Peter William Davis, Robert Jay Tinder, Kelly G. Sprankle
Abstract: The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.
Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.
Type:
Grant
Filed:
April 2, 2002
Date of Patent:
May 11, 2004
Assignee:
Synaptic Pharmaceutical Corporation
Inventors:
Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
Abstract: Compounds of general structural formula (1) are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of behaviors dependent upon AMPA receptors, and in treating conditions, such as memory impairment, in which AMPA receptors, or synapses utilizing these receptors, are reduced in numbers or efficiency. They may also be used to enhance excitatory synaptic activity in order to restore an imbalance between brain subregions, as in treatment of schizophrenia or schizophreniform behavior.
Type:
Grant
Filed:
April 27, 2001
Date of Patent:
May 4, 2004
Assignee:
The Regents of the University of California
Abstract: The use of substituted imidazoazines of the formula I, 1
Type:
Application
Filed:
June 4, 2003
Publication date:
March 25, 2004
Inventors:
Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Bernd Muller, Hubert Sauter, Andreas Gypser, Thomas Grote, Joachim Rheinheimer, Ingo Rose, Frank Schieweck, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
Abstract: The present invention relates to compounds of Formula (I):
wherein A1 is methylene, ethylene or propylene group and A2 is N or CR5, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Abstract: Compounds represented by formula I:
as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat caspase-3 mediated diseases and conditions.
Type:
Grant
Filed:
July 25, 2002
Date of Patent:
March 2, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
Abstract: The present invention relates to the preparation of synthons that are used to form modules that, in turn, are used to form two-dimensional close-packed planar arrays, referred to as nanomembranes. In a presently preferred embodiment, a nanomembrane herein constitutes a filter.
Type:
Application
Filed:
February 7, 2002
Publication date:
February 19, 2004
Applicant:
CoValent Partners, LLC.
Inventors:
Timothy B. Karpishin, Josh Kriesel, Grant Merrill, Donald B. Bivin, Thomas H. Smith, Martin Stuart Edelstein
Abstract: Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1 ,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
Abstract: A compound of formula (I):
wherein:
R1 represents hydrogen, or linear or branched (C1-C6)alkyl optionally substituted by one or more identical or different groups selected from aryl, heteroaryl, cycloalkyl and heterocycloalkyl,
represents a saturated ring having from 4 to 7 ring members that may contain, in addition to nitrogen, one or two hetero atoms selected from O, S and —NR3 groups, wherein R3 represents hydrogen or linear or branched (C1-C6)alkyl,
n represents an integer such that 1≦n≦6,
R2 represents any one of the groups described in the description,
their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as inhibitor of trypsin-related serine proteases and thrombin.
Type:
Grant
Filed:
December 14, 2001
Date of Patent:
February 3, 2004
Assignee:
Les Laboratoires Servier
Inventors:
Guillaume De Nanteuil, Philippe Gloanec, Tony Verbeuren, Alain Rupin, Marie-Odile Vallez
Abstract: The invention relates to phenyl-propargylether derivatives of the general formula I
including the optical isomers thereof and mixtures of such isomers, wherein
R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl,
R2 and R3 are each independently hydrogen or alkyl,
R4 is alkyl, alkenyl or alkynyl,
R5, R6, R7, and R8 are each independently hydrogen or alkyl,
R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl,
R10 is optionally substituted aryl or optionally substituted heteroaryl, and
Z is halogen, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkenyloxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkenylthio; optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenylsulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfon
Type:
Grant
Filed:
November 15, 2002
Date of Patent:
January 27, 2004
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
Clemens Lamberth, Martin Zeller, Walter Kunz, Fredrik Cederbaum
Abstract: A method of synthesis of a bicyclic or polycyclic compound of formula (I) or formula (II) in which: E represents an electrophile; each of R, R1, R2, R3, R6, R7, R8, R9 and X independently represents the common organic substituent groups defined in claim 1; Y represents C(r12)R13, O, NR14, or S; Z represents O, NR15, S or CR16W; G represents W or X; W represents an electron withdrawing group; X has the same definition as R, and W═W; and each of n and m represents an integer from 0 to 100. The method comprises the steps of (a) activating a compound of formula (III); 8b) subjecting a compound of formula (IV) to nucleophilic addition with the activated form of compound III; (c) subjecting the product of step (b) to ring closing metathesis; and (d) subjecting the product of step (c) to stereoselective ring closure. The methods of invention are useful in the synthesis of candidate pharmaceutical agents or intermediates in drugs synthesis.
Type:
Application
Filed:
April 25, 2003
Publication date:
January 15, 2004
Inventors:
Patrick Perlmutter, Mark Rose, Neeranat Thienthong
Abstract: Phenylalanine derivatives of formula (1) are described:
in which:
Ar1 is an aromatic or heteroaromatic group;
L1 is a linker atom or group;
R is a carboxylic acid or a derivative thereof;
Ar2 is an optionally substituted aromatic or heteroaromatic group;
and the salts, solvates, hydrates and N-oxides thereof.
The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
Type:
Grant
Filed:
August 10, 2001
Date of Patent:
January 13, 2004
Assignee:
Celltech R & D Limited
Inventors:
John Clifford Head, John Robert Porter, Graham John Warrellow, Sarah Catherine Archibald, Brian Woodside Hutchinson
Abstract: The invention provides a process for the optical resolution of a racemic mixture, or an optically enriched mixture, of trans-7-(hydroxymethyl)octa-hydro-2H-pyrido-1,2a)pyrazine, a key intermediate for preparing pharmacologically active 2,7-substituted octahydro-1H-pyrido[1,2-a]pyrazine derivatives useful in the treatment of disorders of the dopamine system. The process of the invention involves use of D-(−) or L-(+)naproxen as a resolving agent.
Abstract: The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
Abstract: The present invention relates to hydroxyproline derivatives represented by the following general formulas and the therapeutic agent containing the same for the impaired organs and tissues.
(wherein R is hydrogen or optionally substituted alkyl)
The hydroxyproline derivatives of the present invention possess cell-proliferative and cell-protective activities, and are effectively applied for the restoration and regeneration of impaired organs and tissues.
Abstract: Compounds of formula (I) wherein R and R1, which are different from each other, are a straight or branched C2-C8 acyl group, have analgesic activity.
Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them 1
Type:
Application
Filed:
November 13, 2002
Publication date:
October 9, 2003
Inventors:
Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
Abstract: Compounds that inhibit the peptidyl-prolyl isomerase (rotamase) enzyme activity of the FK-506 binding protein (FKBP) and compositions comprising these compounds are described. The FKBP-inhibiting compounds have a bicyclic [3.3.1], [4.3.1] or polycyclic azaamide nucleus. Pharmaceutical compositions containing such compounds help stimulate the outgrowth of neurites in nerve cells and augmenting nerve regeneration. Methods of treating nerve cells with such compositions are useful to promote repair of neuronal damage caused by disease and physical trauma.
Type:
Grant
Filed:
July 16, 1999
Date of Patent:
October 7, 2003
Assignee:
Pfizer Inc
Inventors:
Susumu Katoh, Hiroshi Kawakami, Hiroki Tada, Maria Angelica Linton, Vincent Kalish, John Howard Tatlock, Jesus Ernesto Villafranca
Abstract: A compound of the formula (I): in which Z, R1, R2, R8, R10, R11, R12, R13 and R14 are each as defined in the description, or a salt thereof. The object compound of the present invention has pharmacological activities such as Tachykinin antagonism, and is useful for manufacture of a medicament for treating or preventing Tachykinin-mediated diseases.
Abstract: The present invention relates to novel aryl and heteroaryl diazabicycloalkane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
Type:
Application
Filed:
November 13, 2002
Publication date:
September 18, 2003
Inventors:
Dan Peters, Gunnar M Olsen, Elsebet Ostergaard Nielsen, Philip K Ahring, Simon Feldb?aelig;k Nielsen, Tino Dyhring Jorgensen
Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
Type:
Application
Filed:
October 28, 2002
Publication date:
July 17, 2003
Inventors:
Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, John Michael Morin, Daniel J. Sall, Marshall A. Skelton, Robert Theodore Vasileff
Abstract: This invention is directed to compounds of the formula
and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.
Type:
Grant
Filed:
October 15, 2002
Date of Patent:
June 1, 2004
Assignee:
Pfizer Inc.
Inventors:
Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker