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WO/2003/016306A1 |
This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a?1¿=a?2...
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WO/2003/011210A2 |
There are provided novel compounds of formula (I), wherein R1, R2, R3, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes...
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WO/2003/008393A1 |
The invention relates to a method for producing 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine (lamotrigine) by ring closure reaction from $g(a)-oxo-2,3-dichlorophenyl acetamidino-aminoguanidino hydrazone.
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WO/2003/006444A2 |
Amide, sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having t...
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WO/2003/000653A1 |
The invention relates to novel substituted N-acyl aniline derivatives of general formula (I), where R?1¿ to R?5¿, A, X, Y and Z are as defined in claim 1, the tautomers, stereoisomers, mixtures, prodrugs, derivatives with a group, nega...
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WO/2002/091989A2 |
Methods for treating viral diseases are provided, using conjugates in which polyamine analogs are conjugated to an amino acid.
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WO/2002/083630A1 |
Novel compounds of the formula (I) in which R?1¿, R?2¿, R?3¿, R?4¿, X and Z are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders ...
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WO/2002/083030A2 |
Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed. In preferred aspects, examples of such compositions include Formulae (A) and (B).
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WO/2002/079145A1 |
Novel benzamide compounds of formula (I), 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 disorde...
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WO/2002/076395A2 |
Agents and methods for chemoprevention and treatment of neoplasia are described, the agents including a selective inhibitor of inducible nitric oxide synthase and a combination of a selective inhibitor of inducible nitric oxide synthase ...
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WO/2002/070468A2 |
Compounds which can be represented by the general formula (I) and in which A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, -R¿1? is selected from an alkyl group having from 1 to...
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WO/2002/070471A1 |
Compounds of the formula (I) in which R?1¿ is CN, or C(=NH)-NH¿2?, CON(R?3¿)¿2? or [C(R?4¿)¿2?]¿n?N(R?3¿)¿2?, each of which is unsubstituted or monosubstituted by C(=O)R?3¿, COOR?3¿, or?3¿ or by a conventional amino-protectin...
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WO/2002/066418A2 |
An improved process for preparing arylethanoldiamines is described. Compounds of this type are known to be useful as agonists at atypical beta-adrenoceptors (also known as beta-3-adrenoceptors).
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WO/2002/064136A2 |
The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases m...
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WO/2002/062766A2 |
MC4-R binding compounds of the formula: B-Z-E (I) wherein B is an anchor moiety, Z is a central moiety, and E is a MC4-R interacting moiety are discussed. Methods of using the compounds to treat MC4-R associated disorders, such as disord...
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WO/2002/062778A2 |
The invention relates to anti-thrombotic compounds of general formula (I), where R¿1? to R¿4?, Ar, A, m and n are as defined in claim 1, the tautomers, stereoisomers, mixtures, pro-drugs and salts thereof which have worthwhile properti...
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WO/2002/060861A1 |
A process for the production of amidine derivatives represented by the general formula (II) or salts thereof, characterized by reducing an amidoxime derivative represented by the general formula (I) with zinc in an acetic acid solvent: (...
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WO/2002/058690A2 |
The present invention relates to methods for the prophylaxis, management and treatment of certain diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD) by the administration ...
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WO/2002/057236A1 |
Novel compounds of the formula I in which W, X, Y, T, R?1¿ and R2 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.
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WO/2002/042273A2 |
Compounds having the formula (I), are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, Ixa, Xa, and/or Xia, wherein ring B is phenyl or pyridyl, W is preferably C(=O)NR¿4?R¿5?, L is a linker group, XÂ...
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WO/2002/042248A2 |
The present invention relates to naphthalene derivatives of formula (I), wherein X is S, S(O), S(O)¿2?, S(O)¿2?NH, P(O)OCH¿3?, P(O)OH, NH, N(CH¿3?), NHC(O)NH, C(O), C(O)O, NHC(O), CH(OH), CH=N, CH=CH, CH¿2?NH, C(=NH); R?1¿ is aryl ...
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WO/2002/038105A2 |
Conjugates in which polyamine analogs are conjugated to an amino acid are provided, as well as compositions comprising these conjugates. Methods of using these conjugates as anticancer treatments are also provided.
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WO/2002/037937A2 |
Compounds of formula I and II, or pharmaceutically-acceptable salts thereof , are useful as inhibitors of Factor VIIa, Factor IXa, Factor Xa, Factor FXIa, tryptase, and urokinase, wherein ring B is phenyl or pyridyl, L is a linker, and R...
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WO/2002/038553A2 |
he present invention is directed to compounds represented by the following structural formula (I'), and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C¿1?-C¿8...
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WO/2002/034711A1 |
Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as...
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WO/2002/028823A1 |
The present invention relates to compounds of formula (I), in which R1, R1, A and B have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmacologically active compounds. They exhibit a strong antithromb...
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WO/2002/022561A1 |
The present invention relates to 2-amino-2-alkyl-3 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
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WO/2002/022562A1 |
The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
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WO/2002/022559A2 |
The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
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WO/2002/022553A2 |
This invention relates to positively charged non-natural amino acids, methods of making thereof, and utilization thereof in peptides.
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WO/2002/022558A2 |
The present invention relates to 2-amino-2-alkyl-3 heptenoic and heptynoic as derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
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WO/2002/022557A2 |
The present invention relates to 2-amino-2-alkyl-4 heptenoic and heptynoic ac derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
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WO/2002/022694A1 |
Catalyst compositions useful for the polymerization of olefins are disclosed. These compositions comprise a Group 8-10 metal complex comprising a bidentate or variable denticity ligand comprising two nitrogen donor atoms independently su...
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WO/2002/020526A2 |
Disclosed are cyclic and acyclic amidines, pharmaceutical compositions containing such amidines, and their use in treating or preventing progesterone receptor mediated diseases or conditions, such as osteopenia and osteoporosis.
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WO/2002/010127A1 |
The invention relates to novel compounds of formula (I) wherein R, R?1¿ and R?2¿ have the designation cited in patent claim 1. Said compounds are inhibitors of the coagulation factors Xa and VIIa, and can be used to treat thromboses, m...
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WO/2002/002516A2 |
The present invention is a series of novel and effective inhibitors of integrase, an essential in the life cycle of retroviruses. These compounds were designed to have a restricted conformation for the determination of the integrase bind...
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WO/2001/098262A1 |
A class of styryl amidine derivatives which are antagonists of the hum NMDA receptor, being selective for those containing the NR2B subunit, are active in the treatment and/or prevention of neurological and neurodegenerative disorders, i...
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WO/2001/096366A2 |
The invention relates to derivatives of amidino-benzylamine, especially derivatives of 4-amidino-benzylamine, with two bonded amino acids. These derivatives represent a novel group of highly active and very selective F Xa-inhibitors for ...
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WO/2001/094333A2 |
Disclosed are processes for coupling amino substituted 2-chromanyl derivatives and benzoyl derivatives via an amide bond, and intermediates for producing platelet aggregation inhibitors and for producing potent platelet aggregation inhib...
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WO/2001/092207A1 |
A process of reacting a compound having an NH group with a thiocyanate, a cyanamide, a nitrile, or an ester in the presence of a silylating agent to thereby obtain the corresponding nitrogen-containing addition or substitution product. T...
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WO/2001/090051A1 |
The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula (I) wherein X and R?1¿ to R?5¿ are as defined in the description and in the claims, as well as hydrates or solvates and/or physiologica...
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WO/2001/085674A1 |
The present invention relates to a process for the preparation of both the phenyl pyrazine derivative 2,6-diamino-3-(2,3,5-trichlorophenyl)pyrazine and an intermediate in the synthesis of 2,6-diamino-3-(2,3,5-trichlorophenyl)pyrazine, 2-...
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WO/2001/083571A2 |
Catalyst compositions useful for the polymerization or oligomerization of olefins are disclosed. Certain of the catalyst compositions comprise N-pyrrolyl substituted nitrogen donors. Also disclosed are processes for the polymerization or...
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WO/2001/079156A1 |
The present invention contains halogenated 2-amino-4, 5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.
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WO/2001/078719A1 |
The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.
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WO/2001/078654A2 |
The present invention contains halogenated 2-amino-3, 4 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.
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WO/2001/079155A2 |
The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treat...
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WO/2001/070678A2 |
The invention relates to compounds of general formula (I) where R?1¿ = -C(=NH)NH¿2 ?optionally substituted with COA, -CO-, [C(R?7¿)¿2?]¿n?-Ar', -COOA, OR?7¿, OCOA, OCO-[C(R?7¿)¿2?]¿n?-Ar', -OH or by a conventional amino protecti...
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WO/2001/068605A1 |
The invention relates to polycyclic aryl and heteroaryl substituted benzene compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment...
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WO/2001/068585A1 |
A compound represented by the general formula (I) and a salt thereof: R?1¿-A-X-NHCO-Y-R?2¿ wherein R?1¿ is an optionally substituted heterocyclic group or optionally substituted phenyl; R?2¿ is optionally substituted fused phenyl, op...
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