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WO/2005/018545A2 |
The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. ...
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WO/2005/007618A1 |
The invention relates to a method for production of $g(a),$g(b)-unsaturated amide compounds of general formula (I): whereby (A) a protective group is introduced into a molecule of general formula (II) to give a compound of formula (III),...
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WO/2004/093796A2 |
Lactam derivatives of the general formula (I), are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.
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WO/2004/087672A1 |
In one aspect, the present invention provides pharmaceutical compositions comprising a therapeutically effective amount of a compound of general formula (I), wherein R1-R6, Ra-RC, Q, Y1, Y2 and n are as defined herein, whereby the compos...
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WO/2004/084809A2 |
Embodiments of this invention provide novel peptidomimetics that contain a macrocycle. Such compounds are neuroprotective and have utility as therapeutic agents for treatment of diseases, injuries and other conditions characterised by ne...
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WO/2004/082357A2 |
The invention relates to a method of the synthesis of compounds of formula (I), where R1 = H, alkyl or benzyl and R2 = an amine protecting group. The above is of application to the synthesis of perindopril and the pharmaceutically-accept...
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WO/2004/083237A1 |
The invention relates to a method for the synthesis of derivatives of formula (I), where R= H or an acid-protecting group. Of application to the synthesis of perindopril and the pharmaceutically-acceptable salts thereof.
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WO/2004/080391A2 |
This invention relates to novel macrolides, to the preparation of novel macrolides, to the use of such novel macrolides for preventing, treating, or ameliorating various conditions, and to the use of such novel macrolides as antibacteria...
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WO/2004/054624A1 |
Cytotoxic compounds and diagnostic imaging agents comprising HSP90-ligands and methods of use thereof are described.
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WO/2004/050623A1 |
Methods of making substituted phenylalkynes of formula (I).
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WO/2004/034970A2 |
Compounds represented by Formula (I), acid-addition salts and pro-drugs are disclosed, wherein the ring structure includes no substitutions, one substitution, or more than one substitution; and wherein n is equal to an integer greater th...
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WO/2003/106390A1 |
A polymerisation inhibitor comprising a non-hindered cyclic hydroxylamine either alone or in combination with an additional inhibitor.
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WO/2003/106653A2 |
Abstract The invention relates to recombinant polyketide synthase enzymes, polyketide modifying proteins, and other proteins involved in polyketide biosynthesis or function. The invention provides domains of geldanamycin and herbimycin p...
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WO2003014105A9 |
The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula (I) wherein: R?1¿ is ...
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WO/2003/076411A1 |
A process for producing an optically active sulfoxide derivative (I) having CCR5 antagonistic activity without causing side reactions such as racemization and Pummerer rearrangement, which comprises reacting a compound (II) with a compou...
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WO/2003/076478A1 |
Novel arene-ruthenium complexes immobilized on polymers as represented by the following formula: [wherein A is an organic polymer whose aromatic rings on the side chains coordinate to Ru; X1 and X2 are each independently halogeno; and R ...
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WO2002002488A9 |
The present invention relates to methods and agonist/antagonist compounds for modulating nuclear receptor coactivator binding. The invention includes a method for identifying residues comprising a coactivator binding site for a nuclear r...
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WO/2003/072794A1 |
The present invention relates to a process of preparing geldanamycin by culturing Streptomyces hygroscopicus in an aqueous nutrient medium. The aqueous nutrient medium can comprise starch, a starch conversion enzyme, an assimilable sourc...
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WO/2003/066005A2 |
Ansamycins and methods of preparing and using the same are described. At least some of these ansamycins exhibit one or more of improved aqueous formulation ability, chemical stability, and bioavailability. Some of the derivatives describ...
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WO/2003/053927A1 |
A piperazine derivative represented by the formula (1) [wherein n is an integer of 1 to 8&semi R1 represents hydrogen or C1−10 alkyl&semi A represents CH or nitrogen&semi Ar1 represents phenyl or substituted phenyl&semi and Y represent...
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WO/2003/050295A2 |
Ligand binding assays as applied to HSP90s as receptors or ligands, and reagents useful therefore, are described and claimed, as are methods of assaying for HSP90 modulators and methods of using the resulting products identified thereby.
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WO/2003/026571A2 |
Efficient chemical processes for preparing high yields, purities, and different polymorphic forms of 17-allyl amino geldanamycin (17-AAG) and other ansamycins are described and claimed.
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WO/2003/013430A2 |
The invention relates to benzoquinone ansamycin analogs useful for the treatment of cancer and other diseases or conditions characterized by undesired cellular proliferation or hyperproliferation. Therapies involving the administration o...
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WO/2002/086078A2 |
The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R¿1? is selected from the group consisting of...
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WO/2002/079167A1 |
A geldanamycin derivative exhibiting significant preliminary in vivo activity, particularly significant oral in vivo activity, and a method of treating or preventing cancer in a host comprising administrering a geldanamycin derivative to...
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WO/2002/058679A2 |
This invention provides the use of macrocyclic amines for inhibition of cellular invasion or angiogenesis. Compounds and pharmaceutical compositions of this invention are useful in the treatment of conditions characterized by cellular in...
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WO/2002/057218A1 |
The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I, Formula (I) wherein R¿1? is (C¿1-3?)alkyloxy, (C¿1-3?)alkyloxy(C¿1-3?)alkyl, (C¿1-3?)alkylthio, (C¿1-3?)alkylthio(C¿1-3?)a...
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WO/2002/036574A1 |
A geldanamycin derivative of general formula (I) and in vitro and in vivo methods of selectively inhibiting Hsp90 in a cell without substantially inhibiting Grp94 comprising administering to a cell comprising Hsp90 and Grp94, or to a hos...
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WO/2002/026705A2 |
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one s...
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WO/2002/026750A2 |
Disclosed are substantially enantiomerically pure bis-phosphine compounds comprising a substantially enantiomerically pure chiral backbone linking two phosphine residues wherein one of the phosphine residues has three phosphorus-carbon b...
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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/2002/017712A2 |
Compounds of formula (I): wherein A, B, D, and R are as defined herein and their agriculturally acceptable salts are disclosed as effective insecticides. In addition, compositions comprising an insecticidally effective amount of a compou...
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WO/2002/016369A2 |
The present invention relates to compounds having the structure (1) (and pharmaceutically acceptable derivatives thereof), wherein R¿1?-R¿4?, Z, X, A-B, D-E, G-J, and K-L are as defined herein, the synthesis thereof and the use of thes...
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WO/2002/012185A1 |
The invention relates to a process for producing 2,3-diaminopropanol of formula (II) from aziridine of formula (I) wherein, R?1¿ is selected from a group consisting of hydrogen, alkyl, cycloalkyl, acyl, aryl, hydrocarbon residues, aralk...
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WO/2002/009696A1 |
The present invention concerns methods for treating cell proliferative diseases, tumors associated with viral infections, and certain viral infections. The disclosed methods use compounds which inhibit heat shock protein 90 proteins. Suc...
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WO/2002/007761A1 |
The present invention features methods for inhibiting HCV replication and processing by targeting heat shock protein 90 (HSP90). HSP90 is a cellular chaperone protein that was found to be an essential factor in NS2/3 self-cleavage. HSP90...
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WO/2001/096342A1 |
Thirteen-membered ring containing terpenoid analog compounds are synthesized from analinogeranylpyrophosphate using 5-epi-aristolochene synthase as a reaction catalyst. The method provides a generalized procedure for making high-ordered ...
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WO/2001/090082A1 |
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula (1) wherein one of X, Y, or Z is independently -S-, -O-, or > N-R?4¿, the others are-CH¿2-;? (p) is an i...
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WO/2001/090081A1 |
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula (I) wherein one of X, Y or Z is independently -S-,-0- CH¿2?- or $m(g)N-R?6¿, the others are -CH¿2?-; m ...
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WO/2001/083444A1 |
The invention relates to a method for producing cyclic lactams of the formula (II), wherein n and m may each represent 0, 1, 2, 3, 4, 5, 6, 7, 8 and 9 and the sum of n + m is at least 3, preferably at least 4, R?1¿ and R?2¿ represent C...
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WO/2001/060768A1 |
A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a...
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WO/2001/047558A1 |
Preventives/remedies for diseases associated with the denaturation or death of nerve cells characterized by containing a growth hormone liberation promoter as the active ingredient.
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WO/2001/000583A1 |
UCF116 derivatives represented by formula (I), wherein Q represents (a) or (b) and R represents hydrogen, C(=O)R?1a¿, C(=X)NHR?1b¿ or SO¿2?R?1c¿ or salts thereof which have antitumor and antibacterial activities and are useful as ant...
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WO/2000/061578A1 |
Bifunctional molecules comprising two hsp-binding moieties which bind to hsp90 in the pocket to which ansamycin antibiotics bind connected via a linker are effective for inducing the degradation and/or inhibition of HER-family tyrosine k...
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WO/2000/058294A1 |
Compounds of formula (I) are antibacterial agents wherein: R¿3? and R¿4?, taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 1...
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WO2000003737A9 |
the present invention provides water-soluble drugs, in particular, water-soluble analogues of geldanamycin, and compositions comprising the same. This invention also provides a method of rendering water-insoluble drugs soluble in water t...
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WO/2000/039115A1 |
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediat...
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WO/2000/020398A1 |
The present invention relates to biphenylene lactams of Formula (II) which are ligands at the prostaglandin receptors, as well as a method for treating prostaglandin mediated diseases comprising administration to a patient in need of suc...
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WO/2000/018724A1 |
The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, ...
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WO/2000/018721A1 |
The invention relates to substituted polycyclic aryl and heteroaryl $i(tertiary)-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions an...
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