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WO/2003/086314A2 |
The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a co...
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WO/2003/087059A2 |
(E)-oxime ether derivative of 5,6-dihydro-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one, compound of formula (I): wherein R in formula (I) is selected from formula (a, b, c, d, e, f, g, h, i) and their pharmaceutically acceptable salts usefu...
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WO/2003/086393A1 |
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including serotonin r...
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WO/2003/084956A1 |
The invention concerns derivatives of formula (I), wherein R1 represents -OH, (C1-C5) alkoxy, carboxyl, (C2-C6) alkoxycarbonyl, -NR5R6, -NH-SO2-Alk, -NH-SO2-Ph, -NH-CO-Ph, -N(Alk)-CO-Ph, -NH-CO-NH-Ph, -NH-CO-Alk, -NH-CO2-alk,-O-(CH2)n-cA...
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WO/2003/084931A1 |
Benzo [4,5]cyclohepta[1,2-b]pyridines represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
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WO/2003/082828A1 |
Substituted tetrahydroisoquinolines of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with ...
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WO/2003/082350A2 |
The present invention is concerned with radiolabelled quinoline and quinolinone derivatives according Formula (I-A)* or (I-B)* showing metabotropic glutamate receptor antagonistic activity, in particular mGlu1 receptor activity, and thei...
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WO/2003/080582A2 |
The invention relates to novel fredericamycin derivatives, to drugs containing said derivatives or the salts thereof, and to the use of the fredericamycin derivatives for treating diseases, especially cancer diseases.
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WO/2003/080581A1 |
A compound of the formula (I):whereinring A is a carbocyclic group, R1 is hydrogen or a halogen atom or a lower alkyl group,R2 is a di(lower)alkylamino group or N-containing heterocyclic group, among which the N-containing heterocyclic g...
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WO/2003/080046A1 |
Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes of formula I (N, Y, Z,, R, R1-R5 as defined in the claims) which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical comp...
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WO2002036573B1 |
8-Substituted-2,6-methano-3-benzazocines of general structure (I) in which A is -CH2-OH, -CH2NH2, -NHSO2CH3, and Y is O, S NR<17> or NOH bind to opioid receptors and are useful as analgesics, anti-diarrheal agents, anticonvulsants, antit...
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WO/2003/077919A1 |
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a...
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WO/2003/076416A1 |
A compound selected from those of formula (I): formula (I) wherein: - X1, X2, and X3, represent N or CR3 in which R3 is as described in the description, - G1 represents a group selected from those of formulae (i/a) and (i/b): formula (II...
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WO/2003/076417A2 |
A compound selected from those of formula (I) wherein: X1, X2, and X3, represent N or -CR3 in which R3 is as described in the description, G1 represents a group selected from those of formulae (i/a) and (i/b) in which R4, R5, and R6 are ...
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WO2002058695A9 |
Compounds described by the chemical formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of p38 useful in the treatment of inflammatory diseases such as arthritis.
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WO/2003/072549A1 |
Disclosed are novel tricyclic compounds represented by the formula (1.0) and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical c...
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WO/2003/070690A2 |
The invention relates to compounds of formula (I): where R1 = an aryl, heteroaryl or alkyl group, optionally substituted with a group of formula -(CO)-CR6R7NR8R9, where R6, R7, R8 and R9 are as defined in the description, R2 = H or optio...
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WO/2003/070277A1 |
It is intended to provide antipruritics (drugs to control itching, antiitch agents and drugs to stop itching). It is found out that a compound having a cannabinoid receptor agonism shows an antipruritic effect.
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WO/2003/068212A1 |
Inhibitors of cellular sodium/hydrogen exchangers display an inhibiting effect on the secretion of von-Willebrand factor and/or increased expression of P-selektin. Said inhibitors can thus be used for the treatment of thrombotic and infl...
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WO/2003/066597A2 |
A variety of small, guanidino group−containing molecules capable of acting as MC4−R agonists are provided. The compounds have various structures provided herein. The compounds are useful in treating MC4−R mediated diseases and may ...
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WO/2003/066599A1 |
The invention relates to 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-10-ols of general formula (1) wherein the radicals R1, R2, R3, R4, R5, R6, R7, R8 and R9 can have the designations cited in the description and in the claims. The in...
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WO/2003/062202A2 |
The invention relates to a method for the production of substituted 1,2,3,4-tetrahydroisoquinoline-2-carboxylic acids, i.e.7,9-dichlor-3a,4,5,9b-tetrahydro-3H-cyclopental[c]quinol
ine-4-carboxylic acid.
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WO/2003/057145A2 |
This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
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WO/2003/057697A1 |
The invention relates to compounds having general formula (I), wherein R denotes a halogen atom, a phenyl group which is substituted by one or more groups selected from among halogen atoms and the (Cl-C6) alkyl, (C1-C6) alcoxy, nitro, am...
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WO/2003/053915A2 |
This invention relates to compounds of the Formula (I):(Chemical formula should be inserted here as it appears on abstract in paper form)(I)or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the tre...
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WO/2003/051826A1 |
A compound of formula (I); wherein R1 represents chloro, fluoro or hydroxy as well as optical isomers and racemates thereof as well as pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, to processes for ...
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WO/2003/051880A1 |
This invention comprises the novel compounds of formula (I) wherein r, s, A, X, Y1, Y2, R1, R2, R3, and R4 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their ...
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WO/2003/051841A2 |
Carbamates and related compounds of formula R1 R2NCO-Y or R1 R2NCS-Y wherein R1 and R2 are hydrogen, alkyl, aryl, heteroaryl or may together form a piperidine, piperazine, morpholine or other heterocyclic ring, are inhibitors of hormone ...
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WO/2003/051842A2 |
Carbamates and related compounds of formula R1R2NCO-Y or R1R2NCS-Y wherein R1 and R2 may form a ring, are inhibitors of hormone sensitive lipase and are useful for the treatment of any disorder where it is desirable to modulate the plasm...
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WO2000077000A9 |
There is provided compounds of formula (I), wherein R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, R<41>, R<42>, R<43>, R<44>, R<45>, R<46>, A and B have meanings given in the description, which are useful in the prophylaxis and in the treatm...
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WO/2003/043618A2 |
The present invention relates to the treatment of Alzheimer's disease and other similar diseases, and more specifically to the use of compounds that inhibit beta-secretase, an enzyme that cleaves amyloid precursor protein to produce A be...
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WO/2003/043582A2 |
Compounds of formula (1) modulate the activily of Rho C, wherein R¿1? is H, OH, or lower alkyl; R¿2?, R¿3?, R¿4?, R¿5? and R¿6? are each independently H, halo, lower alkyl, OH, lower alkoxy, NH¿2?, lower alkylamino, di(lower alkyl...
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WO/2003/042135A2 |
Chiral ligands and metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The metal complexes according to the present invention are useful as catalysts in asymmetric reactions, such as, hydrigenation,...
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WO/2003/040140A1 |
A process and new oxazolinic intermediates for the preparation of 4-(8-chloro-5,6-dihydro-11H-benzo-[5,6]-ciclohepta-[1,2-b]-p
yridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester (loratadine) is described. The process starts from ...
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WO/2003/037329A1 |
This invention relates to the use of nicotinic acetylcholine receptor agonists for the treatment of restless legs syndrome (RLS). The invention further relates to the use of a nicotinic acetylcholine receptor agonist in the manufacture o...
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WO/2003/035069A1 |
Impotence can be ameliorated without substantial undesirable side effects by nasal administration of apomorphine, optionally with an antiemetic agent present in an amount sufficient to substantially reduce nausea symptons that may be ass...
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WO/2003/031397A1 |
A compound of formula (I), wherein R¿1? is haloalkyl, alkenyl, phenyl, thienyl, pyridine, benzthiazolyl, chromanyl (1,2-dihydrobenzopyranyl) or (C¿6-18?)aryl, and R¿1? or R¿2? independently of each other are substituted (C¿4-8?)cycl...
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WO/2003/029221A1 |
The invention relates to novel tetrahydroisochinolines according to formula (I), to methods for the production thereof and to their use for producing medicaments that are used in the treatment and/or prophylaxis of illnesses, particularl...
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WO/2003/022785A2 |
This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. A...
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WO/2003/020700A2 |
The invention provides novel classes of substituted Indeno[1,2-c]isoquinoline Compounds. Pharmaceutical compositions and methods of making and using the compounds, are also described.
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WO/2003/018537A1 |
Compounds of the formula (I) wherein: X and Y are hydroxy or H. A' and A'' are terminal amine functions such valinamide or indanolamine. Z' and Z'' along with the adjacent ()n groups are independently alkylaryl have utility as HIV aspart...
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WO/2003/016281A1 |
In one embodiment, the present invention describes the synthesis of a compound of Formula III, wherein X is halogen, 'Chemical formula should be inserted here as it appears on abstract in paper form'and intermediates therefor from easily...
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WO/2003/015715A2 |
This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; ...
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WO/2003/013532A1 |
The present invention relates to the preparation of the optical isomer (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de
]isoquinoline. This invention also relates to the use of pharmaceutical compositions comprising (R)-(+)-8...
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WO/2003/013530A2 |
The invention relates to salts of substituted 1, 2, 3, 4-tetrahydroquinoline-2-carboxylic acid derivatives of formula (I), in addition to methods for the production thereof, the use thereof in he production of medicaments and medicaments...
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WO/2003/011302A1 |
Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the ...
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WO/2003/000261A1 |
Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula (I) wherein X, Y, Z, R?1¿, R...
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WO/2003/000661A1 |
A metal coordination compound having a basic structure expressed by general formula MLmL’n (1) [wherein M represents a metal atom of Ir, Pt, Rh, or Pd, L and L’ represent mutually different bidentate ligands, m is 1, 2, or 3, n is 0,...
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WO/2003/000688A1 |
The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs...
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WO/2002/102803A1 |
The invention relates to a method for the synthesis of galanthamine, the derivatives and analogues thereof of formula (1) where R¿1? = a hydrogen atom, R¿2? = a hydroxy group, R¿1? and R¿2? together form =0, R¿3?, R¿4?, and R¿5? i...
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