Abstract: Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a —N=atom or a —N(Rb)—, —C(Rb)═ or —C(Rb)(RC)— group; Ra, Rb and Rc is each independently a hydrogen atom or an optionally substituted C1-6alkyl group; X is an —O— or —S— atom or —NH— group or substituted N atom; each Y is independently a N atom or CH group or substituted C atom; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof; The compounds are potent inhibitors of p38 kinase and are use in the prophylaxis or treatment of p38 kinase med
Type:
Application
Filed:
July 20, 2004
Publication date:
December 16, 2004
Inventors:
Jeremy Martin Davis, Daniel Christopher Brookings, Barry John Langham
Abstract: Methods and novel intermediates for the preparation of acyclic nucleoside derivatives of the formula: 1
Type:
Application
Filed:
June 17, 2004
Publication date:
December 9, 2004
Applicant:
Medivir AB
Inventors:
M. Robert Leanna, Steven M. Hannick, Michael Rasmussen, Jien-Heh J. Tien, Lakshmi Bhagavatula, Pulla Reddy Singam, Bradley D. Gates, Lawrence Kolaczkowski, Ramesh R. Patel, Greg Wayne, Greg Lannoye, Weijiang Zhang, Zhenping Tian, Kirill A. Lukin, Bikshandarkoil A. Narayanan, David A. Riley, Howard Morton, Sou-Jen Chang, Cynthia B. Curty, Daniel Plata, John Bellettini, Bhadra Shelat, Tiffany Spitz, Cheng-Xi Yang
Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures:
wherein:
V=
NH;
O;
S; or
CH2;
R7 is a heterocycle selected from the group consisting of:
thiophene;
furan;
pyrrole;
thiazole;
pyrazole;
imidazole;
isoxazole;
isothiazole; and
1,3,4-thiadiazole;
and Y, A, R1, R2, R3, R4, and n1 are defined herein.
Abstract: Processes are disclosed for preparing the antiviral agent entecavir. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various intermediates useful in the preparation of entecavir are also disclosed.
Type:
Application
Filed:
December 11, 2003
Publication date:
September 30, 2004
Inventors:
Yadagiri R. Pendri, Chung-Pin H. Chen, Sunil S. Patel, Jeffrey M. Evans, Jing Liang, David R. Kronenthal, Gerald L. Powers, Siva Josyula Prasad, Jeffrey T. Bien, Zhongping Shi, Ramesh N. Patel, Amit Banerjee, Yeung Yu Chan, Sushil K. Rijhwani, Ambarish K. Singh, Shaopeng Wang, Milan Stojanovic, David J. Kucera, Richard P. Polniaszek, Charles Lewis, John Thottathil, Dhileepkumar Krishnamurty, Maotang X. Zhou, Purushotham Vemishetti
Abstract: Compounds of the following formula are provided:
wherein:
R1 is —X—R1′; in which R1′ is alkyl, cycloalkyl, aryl, aralkyl, hetaryl, or heterocyclyl, all of which are optionally substituted;
X is —NH;
R2 is optionally substituted lower alkyl; and
R3 is —NR4R5; in which R4 and R5 independently are hydrogen or lower alkyl optionally substituted by hydroxy or amino; or acid addition salts or cationic salts thereof. The compounds inhibit CDK-2 activity and are useful for treating disorders characterized by undesirable cell proliferation.
Type:
Grant
Filed:
August 14, 2001
Date of Patent:
September 14, 2004
Inventors:
Robert T. Lum, Cheri Lynn Blum, Richard Mackman, Michael M. Wick, Steven R. Schow, Jeffery A. Zablocki, Prabbha Ibrahim
Abstract: Compounds which are active against viruses have the following Formulas:
wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1 and R2 are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.
Type:
Grant
Filed:
January 14, 2002
Date of Patent:
September 14, 2004
Assignees:
Wayne State University, The Regents of the University of Michigan
Inventors:
Jiri Zemlicka, Yao-Ling Qiu, John C. Drach, Roger G. Ptak
Abstract: The present invention is concerned with pharmaceutical compositions containing certain adenosine derivatives having an acetylene group in the 4′ position, which are adenosine A1 agonists, and to their use in therapy.
Type:
Application
Filed:
March 4, 2004
Publication date:
August 19, 2004
Inventors:
Adrian Hall, Karamjit Singh Jandu, Christopher James Lunniss, Maria Victoria Vinader, Robert Ian West
Abstract: The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage.
Type:
Application
Filed:
October 15, 2003
Publication date:
August 12, 2004
Applicants:
IRM LLC, The Scripps Research Institute
Abstract: Compound of general formula I:
wherein R1, R2, R3, R4, X, Y and R5 have the meanings given herein which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
Type:
Grant
Filed:
March 12, 2002
Date of Patent:
August 3, 2004
Assignee:
Pfizer Inc.
Inventors:
Stephen Martin Denton, Mark Ian Kemp, Sandra Dora Newman, David James Rawson
Abstract: Disclosed are novel A2B adenosine receptor antagonists of Formula I: A compound of the formula:
wherein:
R1 is optionally substituted alkyl or a group —Y—Z, in which Y is a covalent bond or optionally substituted alkylene, and Z is optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted alkenyl or optionally substituted alkynyl, with the proviso that when Y is a covalent bond Z cannot be alkenyl or alkynyl; and
X is oxygen, sulfur, or NH—,
or a pharmaceutically acceptable salt, ester, or prodrug thereof. The compounds are particularly useful for treating asthma and diabetic retinopathy.
Type:
Grant
Filed:
June 27, 2002
Date of Patent:
August 3, 2004
Inventors:
Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki, Dengming Xiao
Abstract: A method for the preparation of acyclic nucleosides such as valomaciclovir stearate comprising the acid hydrolysis of an intermediate of the formula II: where X is a leaving group or an optionally protected guanine moiety, R1 is a hydroxy protecting group or a —C(═O)C1-C22 alkyl ester group; R2 and R3 are independently lower alkyl or benzyl, or R2 and R3 taken together are —CH2CH2— or —CH2CH2CH2— or —CH2CH2CH2CH2—; to the corresponding aldehyde of the formula III: and the reduction of the aldehyde to the corresponding alcohol of the formula IV: by the addition of a borohydride or borane aldehyde reducing agent, characterised in that the borohydride or borane aldehyde reducing agent is introduced under acid conditions.
Abstract: The present invention relates to modified nucleotides and nucleosides and reagents to produce these. The modified nucleotides and nucleotides are assembled to larger oligonucleotides and oligonucleosides, which, for example, may be used for diagnostics of polymorphisms and for antisense therapy of various conditions. The oligonucleotides and oligonucleosides described in the invention have very good endonuclease resistance without compromising the RNA cleavage properties of RNase H wherein combinations of modifications with Y, Z, R or B are claimed: X=O or S, NH or NCH3, CH2 Or CH(CH3), Y=O, S, or NH or NCH3, CH2or CH(CH3); Z=O, S, or NH or NCH3, CH2 or CH(CH3); R=O or S, or NH or NCH3, CH2 or CH(CH3); B=A, C, G, T; 5-F/cl/BrU or —C, 6-thioguanine, 7-deazaguanine; &agr;- or &bgr;-D- (or L)ribo, xylo, arabino or lyxo configuration.
Abstract: The present invention relates to 1,7 disubstituted guanines inhibitors possessing antitumor activity and to a process for preparing the same. Furthermore, these compounds are expected to enhance the efficacy of other chemotherapeutic agents, in the treatment of cancer.
Type:
Application
Filed:
March 15, 2004
Publication date:
July 15, 2004
Inventors:
Alberto Bargiotti, Antonella Ermoli, Maria Menichincheri, Ermes Vanotti, Luisella Bonomini, Antonella Fretta
Abstract: This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): 1
Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.
Type:
Grant
Filed:
December 7, 2000
Date of Patent:
June 15, 2004
Assignee:
MBC Research, Inc.
Inventors:
Nelly Padioukova, Sergey Mikhailov, H. B. F. Dixon, Grigorii Tzeitline
Abstract: The present invention relates to a series of CDK-inhibiting purine derivatives of structural formula (I), or a pharmaceutically acceptable salt and/or prodrug form thereof, wherein: X is O, S or CHRX where RX is H or C1-14 alkyl; D is NZ1Z2 where Z1 is selected from H, C1-4 alkyl, C1-4 hydroxyalkyl, an unsubstituted or substituted aryl or heteroaryl, and an unsubstituted or substituted aralkyl or heteroaralkyl group, and Z2 is selected from an unsubstituted or substituted aryl or heteroaryl, and an unsubstituted or substituted aralkyl or heteroaralkyl group; A is selected from H, C1-4 alkyl, C1-4 alkoxy, hydroxy, CH2(CH2)nOH (n=1-4), and NRa1Ra2 where Ra1 and Ra2 are each independently H or C1-4 alkyl; B is selected from H, halo, C1-4 alkyl, C1-4 alkoxy, CF3, an optionally substituted aryl or an optionally substituted aralkyl, and a hydroxy group that may undergo a C═O tautomeric rearrangement; and Y comprises an unsubstituted or substituted 4- to 8-membered carbocyclic or heterocyclic ring, optio
Type:
Application
Filed:
January 6, 2004
Publication date:
June 10, 2004
Inventors:
Roger John Griffin, Alan Hilary Calvert, Nicola Jane Curtin, Bernard Thomas Golding, Ian Robert Hardcastle, David Richard Newell, Philip John Jewsbury, Francis Thomas Boyle, Jane Anne Endicott, Martin Edward Mantyla Noble
Abstract: The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R1, R2 and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonist and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or prolifertion of cells of the vascular smooth musculature.
Type:
Grant
Filed:
March 6, 2002
Date of Patent:
June 8, 2004
Assignees:
Aventis Pharma Deutschland GmbH, Genetech Inc.
Inventors:
Anuschirwan Peyman, Jochen Knolle, Thomas R Gadek, Jean-Francois Gourvest, Jean-Marie Ruxer
Abstract: The L-monovaline ester derived from 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
Type:
Application
Filed:
June 24, 2003
Publication date:
May 27, 2004
Inventors:
John J. Nestor, Scott W. Womble, Hans Maag, Charles A. Dvorak, Paul R. Fatheree
Abstract: Purine derivatives represented by the following formula and salts thereof:
wherein R1 represents a C1-C4 alkyl group or difluoromethyl group; R2 represents tetrahydrofuranyl group, a C1-C7 alkyl group and the like; X represents hydrogen atom, a halogen atom or nitro group; and A represents a group represented by the following formula:
wherein R3 represents hydrogen atom, a halogen atom and the like; R4 and R5 represent hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxyl group and the like, which are useful as active ingredients of medicaments such as antiasthmatic agents.
Abstract: The invention provides new methods for synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications, including treatment of viral or bacterial infections and associated diseases and disorders.
Type:
Application
Filed:
April 28, 2003
Publication date:
May 6, 2004
Applicant:
Micrologix Biotech Inc.
Inventors:
Wenqiang Zhou, Yi Jin, Arlene Roland, Radhakrishnan Parameswaran Iyer
Abstract: The present invention relates to compounds of the formulae I and Ia
in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their prodrugs, their preparation, their use, in particular as pharmaceutical active compounds, and pharmaceutical preparations comprising them. The compounds of the formula I are vitronectin receptor antagonists and can be employed, for example, as inhibitors of bone resorption and for the treatment of osteoporosis.
Type:
Grant
Filed:
June 15, 2000
Date of Patent:
April 20, 2004
Assignees:
Hoechst Aktiengesellschaft, Genentech
Inventors:
Anuschirwan Peyman, Jochen Knolle, Volkmar Wehner, Gerhard Breipohl, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek
Abstract: Oligonucleotide analogue arrays attached to solid substrates and methods related to the use thereof are provided. The oligonucleotide analogues hybridize to nucleic acids with either higher or lower specificity than corresponding unmodified oligonucleotides. Target nucleic acids which comprise nucleotide analogues are bound to oligonucleotide and oligonucleotide analogue arrays.
Type:
Application
Filed:
August 22, 2003
Publication date:
April 15, 2004
Inventors:
Glenn Hugh McGall, Charles Garrett Miyada, Maureen T. Cronin, Jennifer Dee Tan, Mark S. Chee
Abstract: Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates.
Type:
Grant
Filed:
November 13, 2001
Date of Patent:
March 30, 2004
Assignee:
Pharmasset, Ltd.
Inventors:
Krzysztof W. Pankiewicz, Krystyna Lesiak, Kyoichi A. Watanabe
Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) 1
Type:
Application
Filed:
October 24, 2002
Publication date:
March 11, 2004
Inventors:
Michael L. Edwards, Paul J. Cox, Shelley Amendola, Stephanie D. Deprets, Timothy A. Gillespy, Christopher D. Edlin, Andrew D. Morley, Charles J. Gardner, Brian Pedgrift, Herve Bouchard, Didier Babin, Laurence Gauzy, Alain Le-Brun, Tahir N. Majid, John C. Reader, Lloyd J. Payne, Nawaz M. Khan, Michael Cherry
Abstract: Methods and novel intermediates for the preparation of and the treatment with acyclic nucleoside derivatives of the formula:
where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a —C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl and
R3 is OH or H.
Abstract: The invention relates to pharmaceutically active substances from the group comprising midazolam and compounds with a methyl-substituted nitrogen atom that is the ring atom of a nitrogenous heterocycle. These substances are used to reduce the oxygen consumption during a physical activity. They can be administered together with an effective amount of D-glucose, D-maltose, ethanol, a glucogenic amine, a glucogenic amino acid or an amino acid metabolizable via glyoxylate or a dipeptide or a pharmaceutically acceptable salt of such an amino acid and an effective amount of thiamine, of a pharmaceutically acceptable thiamine salt or of a combination of folic acid and cyanocobalamine, with the proviso that the third component is thiamine or a pharmaceutically acceptable thiamine salt if the second component is D-glucose, D-maltose, a glucogenic amine, a glucogenic amino acid non-metabolizable via glyoxylate, or a dipeptide or a pharmaceutically acceptable salt of such an amino acid.
Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (−)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.
Type:
Application
Filed:
August 20, 2003
Publication date:
February 26, 2004
Inventors:
Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
Abstract: The present invention relates to novel types of peptide nucleic acids (PNAS) with improved properties. In particular, it relates to positively charged PNA units having an ethylene linker between the backbone and the nucleobase, to oligonucleotide analogs comprising these units, to oligomers comprising these units, and to the use of positively charged PNAs as novel delivery agents with therapeutic and diagnostic applications including for antisense therapy.
Type:
Application
Filed:
June 2, 2003
Publication date:
February 19, 2004
Inventors:
Jehoshua Katzhendler, Ada Schlossmann, Yousuf Najajreh, Dan Gibson
Abstract: The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as &agr;-L-oxy-LNA, amino-LNA, &agr;-L-amino-LNA, thio-LNA, &agr;-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
Type:
Application
Filed:
May 8, 2003
Publication date:
January 22, 2004
Inventors:
Mads Detlef Sorensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
Abstract: The invention features 2,7-disubstituted purines and their isosteres such as the corresponding 3-deazapurines and 3-deaza-8-azapurines. The compounds disclosed herein have potent anti-microbial, e.g., anti-bacterial and anti-mycoplasmal properties. The compounds described herein inhibit DNA polymerase IIIC and DNA polymerase IIIE species; the compounds thus inhibit the growth of bacteria and mycoplasmata. The compounds can be administered to prevent or to treat Gram-positive or Gram-negative bacterial or mycoplasmal infections, e.g., in eukaryotic cell cultures, animals, or humans.
Type:
Application
Filed:
February 10, 2003
Publication date:
January 22, 2004
Inventors:
George E. Wright, Wei-Chu Xu, Neal C. Brown
Abstract: The invention is a compound, composition, use for and a method of treating Flaviviridae (Hepacivirus, Flavirius, Pestivirus) infections, including BVDV and HCV, or abnormal cellular proliferation, including malignant tumors, in a host including animals, and especially humans, using a &bgr;-D or &bgr;-L nucleoside of general formula (I)-(XX), or their pharmaceutically acceptable salt or prodrug thereof.
Type:
Application
Filed:
February 13, 2003
Publication date:
January 1, 2004
Inventors:
Lieven J. Stuyver, Junxing Shi, Kyoichi A. Watanabe
Abstract: N-Heterocyclic derivatives of the formula (I):
are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
Type:
Grant
Filed:
April 12, 2002
Date of Patent:
December 30, 2003
Assignees:
Berlex Laboratories, Inc., Pharmacopeia, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, 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
Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures:
with X, Y, D, Q, V, A, R1, R2, R3, R4, and n1 defined herein.
Abstract: &bgr;-lactamases are the most widespread resistance mechanism to &bgr;-lactam antibiotics, such as penicillins and cephalosporins. In response to these enzymes, inhibitors have been introduced. Unfortunately, these inhibitors are also &bgr;-lactams, and resistance to them has developed rapidly. Consequently, the present invention provides a novel structure-based approach to inhibitors of these enzymes.
Abstract: A novel method for synthesizing functional PNA having superior cost performance and which enables functional molecules to be-introduced extremely rapidly, and compounds used therein. Disclosed is a method for producing a functional PNA oligomer; wherein a PNA monomer unit having adenine, guanine, cytosine or thymine protected by a protecting group is reacted with. Fmoc-&ohgr;-amino acid-BocPNA-OH, and after synthesizing PNA oligomer, a functional molecule having free carboxylic acid is introduced into that PNA oligomer followed by deprotecting the protecting group; compounds synthesized by the method; and, Fmoc-&ohgr;-amino acid-BocPNA-OH that functions as a precursor PNA monomer unit.
Abstract: Dihydrate of 4-[[9-[(3-cyclopentyloxy-4-methoxy)benzyl]-6,8-dimethylpurin]-2-yl-3-oxypropyl]pyridine N-oxide, drugs containing the same and a compound useful as an intermediate in the production of this dihydrate.
Because of having a phosphodiesterase IV inhibitory effect, this dihydrate is useful as a preventive and/or remedy for asthma, chronic obstructive lung disease and/or other inflammatory diseases.
Abstract: The present invention relates to acylguanidino derivatives of formula (I), in which R1, R2, R3, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles.
Type:
Application
Filed:
January 27, 2003
Publication date:
October 30, 2003
Inventors:
Anurschirwan Peyman, David Will, Thomas R Gadek, Jochen Knolle, Robert McDowell, Jean-Francois Gourvest, Jean-Marie Ruxer
Abstract: Disclosed are (i) compounds of a steroid, a &bgr;-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, &bgr;-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.
Type:
Application
Filed:
May 5, 2003
Publication date:
October 23, 2003
Inventors:
David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Stewart K. Richardson