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WO/1997/034865A1 |
Compounds of formula (I), wherein R1, R2, R3, R4, R5 and G are as defined in the description and the dotted lines indicate an optional second bond, as well as the acid, base and ester addition salts thereof, a method for preparing said c...
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WO/1997/033862A1 |
A compound of formula (I) wherein R is a) phenyl; phenyl (C1-C4 alkoxy); phenoxy; or benzyl; the phenyl ring of each substituent being optionally substituted with one or more of halogen, nitro, C1-C8 alkyl, C1-C8 alkoxy, C1-C8 haloalkyl,...
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WO/1997/025309A1 |
Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful...
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WO/1997/023243A1 |
Branched hydrazone linkers for linking a targeting ligand such as an antibody to a therapeutically active drug. The point of branching is at a polyvalent atom and the number of drugs increases by a factor of two for each generation of br...
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WO/1997/023447A1 |
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging) using compounds of formula (I), wherein alk is a straight or branched chain alkylene group containing from 2 to 8 carbon ...
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WO/1997/019935A1 |
Processes are disclosed for preparing compounds of Formula (I), for preparing a compound of Formula (II), for preparing a compound of Formula (III) and for preparing a compound of Formula (IV), wherein R3 and R4 are each independently H,...
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WO/1997/016433A1 |
The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, includin...
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WO/1997/012862A1 |
Analogs of the antitumor antibiotics CC-1065 and the duocarmycins incorporate the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) alkylation subunit. The CBI-based analogs have potent cytotoxic activity and are useful as efficac...
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WO/1997/009303A1 |
An 'alpha'-hydrazino acid derivative of general formula (I) is described, wherein R1, R2, R3 are hydrogen or a carbon radical, such that when R2 and R3 are different, C* is an asymmetric carbon of L, D or DL configuration, and R4 and R5 ...
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WO/1997/007091A1 |
The invention concerns novel fluorobutenic acid hydrazides of formula (I) in which: Y stands for C=O, C=S or SO2; R1 stands for hydrogen or halogen; and R2 stands for alkyl, alkyl halide, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl,...
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WO/1997/003678A1 |
Cyclo-oxygenase inhibitor and amidine derivative salts, preparation methods therefor, pharmaceutical compositions containing said salts and the use thereof particularly as NO synthase and cyclo-oxygenase inhibitors, are disclosed.
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WO/1997/002257A1 |
Compounds having structural formula (I) or (II), wherein R is C1-C6 alkoxy or C1-C6 alkyl; R1 is fluorenyl, thienyl, pyridyl or thiazolyl, unsubstituted or substituted by one or more substituents selected from C1-C4 alkoxy, C1-C4 alkyl, ...
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WO/1997/002255A1 |
Bis-oxime derivatives of formula (I) in which A is (a) or (b), where W is oxygen or sulfur, and the other substituents defined as follows: R1 = hydrogen, C1-C4alkyl; cyclopropyl; R2 = hydrogen, C1-C6alkyl; halo(C1-C6) alkyl; C2-C6alkoxya...
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WO/1997/001543A1 |
The invention concerns 1-amino-3-benzyluracils of formula (I) and their salts. In said formula (I), R1 = halogen; R2, R3 = H, CN, SCN, halogen, C1-C4-alkyl halide, C1-C4-alkoxy halide, C1-C4-alkylthio halide; R4 = R3 + C1-C4-alkyl, C1-C4...
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WO/1997/000853A1 |
Compounds of general formula (I), salts thereof or hydrates thereof wherein (a) represents (b) or (c), for example, the compounds (d) and (e), which are useful as a PGD2 antagonist and thus usable in, for example, a remedy for systemic m...
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WO/1996/040628A1 |
A compound of general formula (I) useful as an anticonvulsant for disorders of the central nervous system wherein: R1, R2, R3 and R4 may be the same or different and each represents a hydrogen or halogen atom, or a C1-9alkyl, C3-9cycloal...
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WO/1996/040663A1 |
The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a di- or tri-aminoguanidine of formula (I), capable o...
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WO/1996/040743A2 |
Novel compounds, 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 disorders.
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WO/1996/040622A1 |
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a bis-(2-aryl)hydrazone capable of inhibiting the formation of a...
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WO/1996/031467A1 |
Provided is a compound of formula (I). This compound is an intermediate to and is used for preparing the arthropodicidal oxidiazine Compound (II) described in the specification.
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WO/1996/030329A1 |
The invention relates to substituted benzenes and derivatives thereof, useful as neuraminidase inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral and other inf...
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WO/1996/021450A2 |
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a dioone bis[hydrazone] capable of inhibiting the formation of a...
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WO/1996/020934A1 |
The invention provides a process for producing lamotrigine of formula (I) which process comprises subjecting a compound of formula (II), wherein R is CN or CONH2, in an organic solvent, to ultraviolet or visible radiation and, when R is ...
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WO/1996/018644A1 |
The present invention discloses peptide aldehydes of formula (I) which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them a...
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WO/1996/016031A1 |
The present invention provides novel compounds of the formulae (I): AG-(CH2)n-CO2R1 and (II) or pharmacologically acceptable salts thereof, wherein AG is: a) N-aminoguanidine, b) N,N'-diaminoguanidine, or c) N,N',N"-triaminoguanidine; an...
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WO/1996/013509A1 |
Fluorinated alkene compounds having structure (I) wherein Q is -(C=S)-R1, -(C=W)-R2, or -(P=W)R3R4; wherein W is O or S; and R1 to R4 are as defined in claim 1; are useful for controlling nematodes, insects, and acarids that prey on agri...
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WO/1996/010560A1 |
A semicarbazone derivative of formula (I), wherein W is an oxygen atom or a sulfur atom; each of X, Y and Z which are independent of one another, is a halogen atom, a hydroxyl group, a cyano group, a nitro group, SCN, a trimethylsilyl gr...
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WO/1996/005180A1 |
A retriviral protease inhibiting compound of formula (A) is disclosed.
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WO/1996/003418A1 |
The present invention relates to novel soluble combinatorial libraries, comprising a soluble phase in solution attached to a core molecule, and allowing the improved high-yield and efficient production of soluble combinatorial libraries....
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WO/1996/001252A1 |
A semicarbazide derivative represented by general formula (1) and a terminally blocked derivative thereof (wherein R1 represents a polyisocyanate residue free from a terminal isocyanate group or a triisocyanate residue free from a termin...
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WO/1995/029889A1 |
Compounds of formula (I) in which X is (a) or (b), n is 0, 1, 2, 3, 4 or 5, where if n is greater than 1, the radicals R2 are identical or different; o is 0, 1, 2, 3 or 4, where if o is greater than 1, the radicals R3 are identical or di...
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WO/1995/029171A1 |
A method for making arthropodicidal oxadiazines and intermediates which are racemic or enantiomerically enriched at their chiral center, the method for making the oxadiazines comprising reaction of an intermediate selected from (II) or (...
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WO/1995/029152A1 |
This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by general formula (I), wherein R1 is aryl optionally substituted with lower alkyl, etc., R2 is lower alkyl, etc., R3 is...
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WO/1995/028377A1 |
Guanidine compounds of formula (I) or a pharmaceutically-acceptable salt, ester, amide or prodrug thereof, which are regulators of nitric oxyde synthase and are useful in the treatment of disorders of the vascular system including hypote...
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WO/1995/024393A1 |
A compound of formula (I) wherein, R1 is carboxy or protected carboxy; R2 is hydrogen, hydroxy or protected hydroxy; R3 is hydrogen, hydroxy, protected hydroxy, etc.; R4 is hydrogen or halogen; A1 is lower alkylene; A2 is bond or lower a...
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WO/1995/019767A1 |
This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More par...
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WO/1995/019960A1 |
Novel monoamine oxidase B inhibitors of formula (I), wherein R1 = H, an optionally substituted benzyloxy or phenylethoxy group; p = 0-3; R3 = H, a CN, OH, CCH group, a C1-C3 alkoxy-carbonyl group, or a C1-C3 alkylated cyanomethyl group; ...
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WO/1995/018832A1 |
This invention describes a series of novel polyamino-carboxylate chelators suitable for attaching metal ions to polypeptide molecules. Polypeptide-polyaminocarboxylate conjugates prepared using the novel chelators form stable complexes w...
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WO/1995/009619A2 |
The use of an N-substituted urea derivative for the manufacture of a medicament for the treatment of a condition where there is an advantage in inhibiting the NO synthase enzyme, in particular cerebral ischemia, and pharmaceutical formul...
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WO/1995/007269A1 |
The invention relates to retroviral protease inhibitors of the general formula (I): W-(A)n-B-(A*)m-V where W, A, B, A*, V, n and m are as defined herein, including related prodrugs of general formula (I) comprising a solubilising group w...
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WO/1995/006251A1 |
A surface of specific reactivity is formed by adsorbing a modified block polymeric surfactant of the Pluronic-type, i.e., containing pendant poly(ethylene oxide) blocks attached at an end to poly(propylene oxide) center blocks and with s...
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WO/1995/004034A1 |
New medicaments containing (thio)carbamidinic acid derivatives having formula (I) are disclosed, as well as new (thio)carbamidinic acid derivatives, a process for preparing the same and medicaments containing these compounds. Medicaments...
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WO/1995/001972A1 |
Inhibitors of nitric oxide formation from arginine useful for treating hypotension, inflammation, stroke and to restore vascular contractile sensitivity to the effects of alpha1 adrenergic agonists are physiologically active compounds in...
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WO/1994/019332A1 |
A retroviral protease inhibiting compound of formula (I) is disclosed.
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WO/1994/017817A1 |
This invention relates to peptide aldehyde analogs that inhibit the thrombin or Factor Xa. The compounds are thought useful for preventing or treating conditions in mammal characterized by abnormal thrombosis.
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WO/1994/011340A1 |
A compound representd by general formula (I), a salt thereof, and a pest control agent, wherein: X represents halogen, alkyl, alkoxy, cycloalkyloxy, alkylsulfonyloxy, alkylthio or alkylsulfonyl; R1 represents hydrogen or alkyl; R2 repres...
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WO/1994/011490A2 |
A solution of one or two molecules of aminoguanidine or other hydrazine type compound incubated with an Amadori product (1-propylamine-1-deoxy-D-fructose) under physiological conditions proceeds through the reactive intermediate 1-propyl...
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WO/1994/008954A1 |
Arthropodicidal compounds: I) 2-(2-ethyl-4-fluoro-2,3-dihydro-1H-inden-1-ylidene)-N-[(4-tr
ifluoromethoxy)phenyl]hydrazinecarboxamide and II) 2-(5-chloro-2,3-dihydro-2-propyl-1H-inden-1-ylidene)-N-[(4-t
rifluoromethoxy)phenyl]hydrazineca...
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WO/1994/007815A2 |
Oligopeptide compounds or oligopeptide analogue compounds of the formula A-B-D are ligands for the anaphylatoxin receptor and are useful in the treatment of inflammatory disease states; also disclosed are anaphylatoxin receptor ligand co...
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WO/1994/006758A1 |
A number of aryl semicarbazones were prepared as candidate anticonvulsants. When administered orally to rats, significant activity was noted in the maximal electroshock (MES) screen and since neurotoxicity was either absent or reduced (a...
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