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WO/2001/090717A2 |
This invention generally relates to nanocrystal compounds, and linker arm for nanocrystal compounds that attach the nanocrystals to the organic compounds. The nanocrystal compound comprises a nanocrystal, linker arm, and organic compound...
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WO/2001/090106A2 |
The present invention provides compounds of the formula (I): wherein R?1¿ is C¿3-6? cycloalkyl optionally substituted by one or more fluorine atoms, or C¿1-6? alkyl optionally substituted by one or more fluorine atoms, or C¿3-6? cycl...
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WO/2001/089524A1 |
A method of training a smoker to cease smoking by administering tropane compounds is provided.
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WO/2001/087846A2 |
This invention relates to compounds of formula I which are inhibitors of protein kinase activity, of which some are novel compounds, to pharmaceutical compositions containing these pyrazoles and to processes for preparing these pyrazoles.
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WO/2001/087299A1 |
The present invention describes a method for programming a specific course and rate of metabolism for a parent drug compound that leads to an inactive or very weakly active and nontoxic metabolite when the modified drug compound is admin...
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WO/2001/080905A2 |
The present invention provides novel sigma-2 ligands (labeled and unlabeled) and the use of the compounds in medical therapy or diagnosis (I).
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WO/2001/077100A2 |
The present invention relates to certain benzoamide piperidine containing compounds of formula I and related compounds that exhibit activity as NK-1 receptor antagonists, (e.g., substance P receptor antagonists), to pharmaceutical compos...
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WO/2001/072303A1 |
Ligands which are selective for the delta opioid receptor. The ligands may be used for treating a variety of disease states.
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WO/2001/070734A2 |
The present application describes novel β-amino acid derivatives of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, U?a�, X?a�, Y?a�, Z?a�, R?1�, R?2�, R?3�, R?4�, and R?4a� a...
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WO/2001/066543A2 |
This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as $g(d)-opioid or $g(m)-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, imm...
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WO/2001/066521A1 |
Compound and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound of formula (II) is administered t...
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WO/2001/057008A1 |
The present invention is directed to a compound of formula (I), racemic-diastereomeric mixtures thereof, optical isomers thereof, prodrugs thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, prodrugs...
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WO/2001/046187A1 |
The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.
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WO/2001/046186A1 |
The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.
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WO/2001/046191A1 |
4-[aryl(8-azabicyclo[3.2.1]octan-3yl)]aminobenzoic acid derivatives are delta-opioid receptor modulators. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their antagonist effect, such compounds ma...
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WO/2001/043746A1 |
A medicinal composition comprising as the active ingredient an amide derivative represented by formula [1] or a pharmacologically acceptable salt thereof, (wherein R?1¿ and R?2¿ are the same or different and each represents hydrogen, o...
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WO/2001/043745A1 |
The use of scopolamine salts for preventing the onset of epilepsy that might ensue after the condition of status epileticus, major head trauma, including those occasioned by neurosurgical trauma, and acute lesional events to the brain.
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WO/2001/036417A1 |
This invention relates to new use of a compound of general formula (I) wherein: A represents (II), (III), (IV), (V), (VI); D represents oxygen, or sulfur; R?1¿ represents hydrogen or methyl; R?2¿ represents hydrogen, or C¿1?-C¿4? alk...
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WO/2001/032649A1 |
The invention relates to compounds of general formula R-Z?1¿-Z?2¿-Z?3¿-R?1¿ wherein R. R?1¿ and Z?1¿ -Z?3¿ are defined as in Claim 1, the tautomers thereof, diastereomers thereof, enantiomers thereof, mixtures and salts thereof, e...
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WO/2001/032179A1 |
Novel 3-substituted 8-aza-bicyclo[3.2.1]octanes (commonly known as 'tropanes') substituted in the 8-position are effective as NMDA NR2B antagonists useful for relieving pain.
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WO/2001/029000A2 |
The present application describes modulators of CCR3 of formula (I): A-E-NR?1¿-G, or pharmaceutically acceptable salt forms thereof, wherein: A is selected from (a), (b), (c) and (d). G is selected from -C(O)R?3¿, -C(O)NR?2¿R?3¿, -C(...
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WO/2001/029034A1 |
A compound of formula (I) wherein A represents (II), (III), (IV), (V) or (VI); R represents hydrogen or methyl; R?1¿ and R?2¿ are independently hydrogen, or C¿1?-C¿4? alkyl; R?3¿ and R?4¿ are independently hydrogen, C¿1?-C¿4? alk...
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WO/2001/025236A2 |
A one-step stereoselective process for the preparation of endo-3-aminoazabicycloalkanes from azabicycloalkanones by means of reductive amination is described.
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WO/2001/019816A1 |
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for makin...
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WO/2001/016121A1 |
In accordance with the present invention, there are provided novel class of heterocyclic compounds and methods of use thereof. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring th...
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WO/2001/015532A1 |
The use of azabicyclo and azacyclo oxime and amine compounds of the formula (I) to (IV) wherein the symbols and indices have the meanings given in the specification for controlling animal pests.
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WO/2001/014333A1 |
The invention provides compounds of formula (I) wherein R?1¿, R?2¿, R?3¿, R?6¿, Z, Q, m, n, X?1¿, X?2¿, X?3¿, X?4¿ and T are as defined in the specification, processes for their preparation, pharmaceutical compositions containing...
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WO/2001/014374A2 |
Novel processes for the stereoselective preparation of exo- and endo- indolotropanes of formulae (IA) and (IB) wherein: R?1¿ is hydrogen or (C¿1-6?)alkyl; R?2¿ and R?3¿, which may be the same or different, are selected from the group...
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WO/2001/009119A2 |
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by (...
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WO/2000/078725A1 |
The present invention provides a process for preparing amidines starting from carboxylic acid derivatives, in which the carboxylic acid containing moiety is attached to a sp?3¿-, or sp?2¿- or sp?1¿-hybridized carbon atom. The sp?2¿-h...
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WO/2000/078724A2 |
This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present,...
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WO/2000/071519A2 |
Novel compounds and methods for preparing same, immunopotentiating compositions, and a method for potentiating the immune system of a host animal. The method comprises administering to the animal an effective amount of an immunopotentiat...
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WO/2000/064490A1 |
Provided are compounds of formula (I) wherein R is C2-C6 mono- or multi-unsaturated hydrocarbon having one or more ethylene, acetylene or allene groups, A is 18 or 19, and X is H or halogen. The compounds of the invention bind to dopamin...
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WO/2000/064491A1 |
A series of compounds in the 4-fluoroalkyl-3-halophenyl nortropanes family are described as diagnostic and therapeutic agents for diseases associated with serotonin transporter dysfunction. These compounds bind to serotonin transporter p...
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WO/2000/063215A2 |
The invention concerns a compound of general formula (I) wherein: R¿1? represents a hydrogen atom, a halogen, a C¿1?-C¿4? alkoxyl, methyl, hydroxy or amino group; R¿2? represents -(CH¿2?)¿2?-OH or-CH¿2?-C(O)OH when R¿3? represent...
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WO/2000/063204A2 |
Compounds of formula (I) wherein the symbols have meaning as defined herein, are p38 MAP kinase inhibitors, and are useful pharmaceutically for treating TNF$g(a) and IL-1 mediated diseases, such as rheumatoid arthritis, and diseases of b...
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WO/2000/061569A1 |
The invention provides compounds of general formula (I) in which m, A, R?1¿ and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the...
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WO/2000/059510A1 |
This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula (I), wherein R?1¿, R?2¿ and R?3¿ are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those...
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WO/2000/056729A1 |
This invention relates to a novel class of heterocyclic compounds that bind chemokine receptors, inhibitng the binding of their natural ligands thereby. These compounds result in protective effects against infection by HIV through bindin...
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WO/2000/051608A1 |
The present invention is directed to pyrrolidine compounds of the formula (I): (wherein R?1¿, R?2¿, R?3¿, R?4c¿, R?4d¿, and R?4f¿ are defined herein) which are useful as modulators of chemokine receptor activity. In particular, the...
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WO/2000/050396A1 |
A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-...
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WO/2000/048597A1 |
The present invention relates to a new use for compounds having 5-HT¿3?(serotonin M) receptor antagonist activity, especially tropisetron, for the manufacture of a pharmaceutical composition for the systemic treatment of an inflammatory...
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WO/2000/047571A1 |
A compound of formula (I) wherein X is (II) or (III) wherein R' is a group (a), R is a group (e) or (f) wherein n is 0 to 3. In particular the agents of the invention inhibit the formation of $g(b)-amyloid (A$g(b)) peptide into neurotoxi...
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WO/2000/047200A1 |
A medicament containing, separately or together, (A) formoterol or a pharmaceutically acceptable salt thereof or a solvate of formoterol or said salt and (B) a tiotropium salt of a pharmaceutically acceptable acid, for simultaneous, sequ...
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WO/2000/044747A1 |
Biologically active derivatives of the tropane ring system are provided having formula (1) wherein R¿1? is selected from the group consisting of hydrogen and C¿1? to C¿8? alykl; R¿2? is selected from the group consisting of hydrogen,...
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WO/2000/044743A1 |
Amide derivatives represented by general formula [1] or pharmaceutically acceptable salts thereof, and drug compositions containing both as the active ingredient: (wherein R?1¿ and R?2¿ are each independently hydrogen, optionally subst...
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WO/2000/044746A1 |
The present invention relates to 8-azabicyclo[3.2.1]oct-2-ene derivatives in their labelled form. Furthermore, the present invention relates to the use of said derivatives in their labelled or unlabelled form in diagnostic methods, in pa...
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WO/2000/044728A1 |
The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R?1¿, R?3¿ and R?4¿ are as defined herein. The invention also relates to methods of treating abnormal cell ...
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WO/2000/039125A1 |
Compounds of formula 1: [Region$g(a)] - [Region$g(b)] - [Region$g(g)] - [Region$g(d)] which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these comp...
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WO/2000/038680A1 |
Compounds of the Formula (I) [Region $g(a)] - [Region $g(b)] - [Region $g(g)] - [Region $g(d)] which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formlations and methods of treatment using th...
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