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WO/2002/028839A1 |
Benzimidazole and indole derivatives of the formula (I) that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and peripheral disorders, particularly stress, anxie...
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WO/2002/026727A2 |
Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid...
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WO/2002/024686A2 |
This invention comprises the novel compounds of formula (I) wherein r, t, Y?1¿-Y?2¿, R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?6¿ and R?7¿ have defined meanings, having farnesyl transferase inhibiting activity; their preparation, composit...
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WO/2002/024693A1 |
This invention is to provide a process for producing 3,4-dihydro naphthyridinone analogs and salts thereof containing the structure shown by the following structural formula (I).The naphthyridinone analogs with an electrowithdrawing grou...
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WO/2002/024660A1 |
Imidazole derivatives of the general formula (1) or salts thereof, medicines containing the derivatives or the salts, and intermediates for the synthesis of the derivatives or the salts (wherein R?1¿ is lower alkyl; R?2¿ is alkyl or ar...
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WO/2002/024682A1 |
This invention comprises the novel compounds of formula (I)wherein r, s, t, Y?1¿-Y?2¿, R?1¿, R?2¿, R?3¿, R?4¿, R?5¿ and R?7¿ have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions ...
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WO/2002/024200A1 |
The present invention relates to thiazoles, oxazoles, imidazoles and pharmaceutical compositions comprising said compounds antagonizing the corticotropin releasing factor receptor ('CRF receptor') and useful for the treatment of depressi...
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WO/2002/024679A1 |
Pyridine compounds of general formula (I) wherein -R?1¿ represents, or in which R?11¿ is hydrogen, C¿1-6? alkyl, halogen, hydroxy, C¿1-12? alkoxy, nitro, amino, C¿1-6? alkylsulfonylamino, C¿1-6? alkoxycarbonyl, C¿1-6? alkylamino, ...
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WO/2002/024651A1 |
This invention is to provide a process for producing 2-amino-4,6-disubstituted nicotinic acid ester analogs and salts thereof, comprising the reaction shown by the following scheme. The ester analogs can be prepared in one pot, and in go...
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WO/2002/024666A2 |
Quinazolines of the formula I, in which R, R?1¿, R?2¿, R?3¿, R?4¿ and Y have the meaning indicated in Patent Claim 1, and their salts or solvates as glycoprotein IbIX antagonists.
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WO/2002/024685A1 |
The invention concerns novel indole derivatives, their preparation method and their pharmacological activity as antimycotic and/or antiparasitic compounds.
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WO/2002/024687A1 |
This invention comprises the novel compounds of formula (I) wherein r, t, Y?1¿-Y?2¿, R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?6¿ and R?7¿ have defined meanings, having farnesyl transferase inhibiting activity; their preparation, composit...
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WO/2002/022556A1 |
Amide derivatives represented by the following general formula (1) which have a C5$g(a) receptor antagonism, wherein each symbol has the meaning as defined in the description. These amide derivatives, optically active isomers thereof or ...
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WO/2002/022605A1 |
This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII, wherein Z?1¿ is N or C-R?9¿, Z?2¿ is N or CH, and Z?3¿ is N or C-R?x¿, provided that one of Z?1¿ ...
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WO/2002/022603A1 |
This invention provides novel pyrazole compounds that are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3. The compounds may be used to treat abnormal physiological function leading to diseases such as...
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WO/2002/022604A1 |
This invention describes novel pyrazole compounds of formula III:wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R?x¿ and R?y¿ are taken toget...
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WO/2002/022608A1 |
This invention describes novel protein kinase inhibitors of formula (VII): wherein G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Rind C has ...
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WO/2002/022601A1 |
This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula (V) wherein Z?1¿ is N, CR?a¿, or CH, and Z?2¿ is N or CH, provided one of Z?1¿ and Z?2¿ is nitrogen; G i...
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WO/2002/022607A1 |
This invention describes novel pyrazole compounds of formula II:wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1, 2, 4-triazinyl ring, and R?2¿, R?2¿, R?x¿, and R?y¿ are as described in t...
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WO/2002/022584A1 |
Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: where R?1¿ is hydrogen, or C¿1-4? alkyl, (CH¿2?)¿0-1?CN, C(O)R?14¿, (CH¿2?)Â...
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WO/2002/022606A1 |
This invention describes novel pyrazole compounds of formula (IV) wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R?x¿ and R?y¿ are independen...
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WO/2002/022550A2 |
The disclosed invention comprises a compound having the formula (I), in which R?1¿ and R?2¿ independently represent a hydrogen or an alkyl group of 4 carbon atoms or greater. Further disclosed is a process for the preparation of the di...
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WO/2002/022602A2 |
This invention describes novel triazole compounds of formula (IX): wherein Z?1¿ is nitrogen or CR?9¿ and Z?2¿ is nitrogen or CH, provided that at least one of Z?1¿ and Z?2¿ is nitrogen; G is Ring C or Ring D; Ring C is selected from...
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WO/2002/020472A1 |
The invention relates to substituted phenylcyclohexane carboxylic acid amides of formula (I), a method for the production thereof and the use thereof in medicaments, especially in the prevention and/or treatment of cardiovascular diseases.
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WO/2002/020500A2 |
Compounds of Formula (I) that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to po...
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WO/2002/018349A2 |
The instant invention provides processes and intermediates employed in the synthesis of ((2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)-amino-3-hydroxy-5-
(2S-(1-tetrahydropyrimid-2-onyl)-3-methyl-butanoyl)amino-1,6
-diphenylhexane and analogs...
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WO/2002/018368A1 |
The present invention discloses novel tricyclic compounds represented by the formula (1.0), a prodrug thereof, or a pharmaceutically acceptable salt or solvate of the compound or of said prodrug useful for inhibiting farnesyl protein tra...
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WO/2002/016308A1 |
The invention relates to compounds of the general formula (1), wherein A, R?1¿, R?2¿, R?3¿, R?4¿, R?5¿ and R?6¿ are defined as in the description and the claims. The invention further relates to a method for producing said compound...
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WO/2002/016324A1 |
The present invention relates to compounds of the general formula (I) wherein a.o. 5 R is hydrogen or halogen; R and R?2¿ or R?4¿ and R?4'¿ may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from...
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WO/2002/013824A1 |
The present invention is directed to compounds of the formula I (wherein R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?6¿ and X are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are...
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WO/2002/014269A2 |
Disclosed are compounds of the formula (I) or pharmaceutically acceptable salts thereof wherein: (i) represents: (ii, iii, iv, v) and A, B, G, D, E, R¿a?, R¿b?, W, and Z are defined herein. These compounds are agonists, antagonists or ...
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WO/2002/014311A2 |
Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptabl...
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WO/2002/014276A1 |
Benzoylaminoisoindoline compounds of the general formula [I] useful as drugs, or pharmacologically acceptable salts thereof; processes for the preparation of the compounds or the salts; and intermediates for the synthesis thereof; [I] wh...
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WO/2002/012224A2 |
Substituted N-substituted alkoxyphenyl compounds, compositions containing them, and methods of making and using them.
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WO/2002/012190A2 |
Substituted non-imidazole aryloxypiperidine compounds, compositions containing them, and methods of making and using them to treat or prevent histamine-mediated conditions.
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WO/2002/012214A2 |
Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
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WO/2002/012197A1 |
The invention relates to 1H-pyrazol derivatives corresponding to general formula (I), wherein R?1¿ and R?3¿, independently of each other, represent H or a C¿1?-C¿4?-alkyl radical, R?2¿ represents H, halogen or a C¿1?-C¿4?-alkyl ra...
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WO/2002/010140A2 |
The present invention is directed to imidazolyl derivatives of formula (I) where the substituents are defined in the specification, which are useful as agonists or antagonists of somatostatin receptors.
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WO/2002/010161A1 |
The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R?1¿, R?2¿, R?3¿, R?4¿...
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WO/2002/010163A1 |
The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R, R?1¿, R?2¿, R?3...
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WO/2002/008211A2 |
Compounds, pharmaceutical compositions, and methods for the treatment of a hyperlipidemic condition in a subject. The compounds of the present invention are apical sodium co-dependent bile acid transport inhibitors and are 1,4-benzothiaz...
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WO/2002/008213A1 |
The invention related to colchinol derivatives of the formula (I): Wherein: R?1¿, R?2¿ and R?3¿ are each independently hydroxy, phosphoryloxy (-OPO¿3?H¿2?), C¿1-4?alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso...
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WO/2002/008232A1 |
The invention relates to compounds of general formulas (IA) or (IB) wherein R?1¿ is (a), (b), (c), (d) or is -NH(CH¿2?)¿2?OH, -NR?3¿C(O)CH¿3? or -NR?3¿C(O)-cyclopropyl; R?2¿ is methyl or chloro; R?3¿ is hydrogen or methyl; R is h...
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WO/2002/008199A2 |
The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa...
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WO2001053268B1 |
Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating , e.g., kinases-dependent...
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WO/2002/006255A2 |
The invention provides compounds of Formula (I) having the structure wherein A, B, Z, R and R?1¿ are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders ...
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WO/2002/006237A1 |
A 3,5-dicyanopyridine derivative or a salt thereof. The compound exhibits excellent activity of opening the maxi-K channel and bladder smooth muscle contracting activity based on the maxi-K opening activity, and thus can be used in the t...
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WO/2002/003912A2 |
Novel C-4 substituted all-trans retinoic acid analogs are synthesized and used to treat various cancers and dermatological diseases and conditions. These novel C-4 substituted all-trans retinoic acid analogs inhibit all-trans retinoic ac...
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WO/2002/002538A1 |
Amino acid-N-carboxy anhydrides having an N-acyl substituent at nitrogen which are represented by the following general formula (1); and a process for producing the same. These compounds easily react with free amino acids, alcohols or nu...
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WO/2002/002542A1 |
A five-membered-ring compound represented by the formula or a salt thereof: wherein X represents oxygen or sulfur; R?1¿ represents hydrogen, (un)substituted alkyl, etc.; R?2¿ represents hydrogen, (un)substituted alkyl, (un)substituted ...
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