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| Number | Title | Issue Date |
| 7678923 | Method for synthesizing 5-chloro-1-aryl-4-(4,5-dicyano-1h-imidazol-2-yl)-3-alkyl-1h-pyrazole derivatives Method for synthesising 1-aryl-4-(imidazol-2-yl)-3-alkyl-1H-pyrazole derivatives from 1-aryl-3-alkyl-1H-pyrazo-line-5-one derivatives. ... | 03/16/2010 |
| 7429581 | Pyrazole-derivatives as factor Xa inhibitors The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is... | 09/30/2008 |
| 7417152 | 4-bromo-5-(2-chloro-benzoylamino)-1H-pyrazole-3-carboxylic acid amide derivatives and related compounds as bradykinin Breceptor antagonists for the treatment of inflammatory diseases Disclosed are compounds of formula I and II that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certa... | 08/26/2008 |
| 7358052 | Catalytic amplification of multiplexed assay signals Methods, compositions, kits, and a system are disclosed for detecting one or more analytes in a sample. A mixture comprising the (i) sample, (ii) a first binding reagent comprising a cleavage-inducing moiety and a first binding agent specific for an analyte, and (ii... | 04/15/2008 |
| 7291642 | Bradykinin-B1 antagonists, process for their preparation and their use as medicaments The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and ... | 11/06/2007 |
| 7285554 | Pyrazole derivative Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors conta... | 10/23/2007 |
| 7255999 | Methods and compositions for analyzing proteins Methods, compositions and kits are disclosed for determining one or more target polypeptides in a sample where the target polypeptides have undergone a post-translational modification. A mixture comprising the sample and a first reagent comprising a cleavage-inducin... | 08/14/2007 |
| 7253169 | Aza compounds, pharmaceutical compositions and methods of use The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities. ... | 08/07/2007 |
| 7247635 | Pyrazole derivative Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors conta... | 07/24/2007 |
| 7217677 | Method for producing coupling compound A method is provided for producing a specific crosscoupling compound and a specific catalyst for producing the compound. The method includes reacting in the presence of a base and a nickel compound catalyst organic halide of the formula n′(R1X1 | 05/15/2007 |
| 7214802 | Anti-cytokine heterocyclic compounds Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chr... | 05/08/2007 |
| 7160735 | Tagged microparticle compositions and methods Compositions and methods are disclosed for detecting multiple target analytes in a sample using microparticles having molecular tags attached by cleavable linkages. Generally, an assay mixture is formed comprising a sample and a reagent comprising multiple such micr... | 01/09/2007 |
| 7141581 | Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit un... | 11/28/2006 |
| 7129261 | Cytotoxic agents The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as ot... | 10/31/2006 |
| 7091350 | Diaminopyrazole derivatives and their use for oxidation dyeing of keratinous fibres The invention relates to diaminopyrazole derivatives having the following structure (I), wherein R1 represents an alkyl or alkenyl radical bearing at least one substituent selected from among OR, NRR′, SR, SOR, SO2R, COOR, CONRR′, PO(OH) | 08/15/2006 |
| 7087378 | Design, synthesis and use of specific polyamide DNA-binding ligands The invention encompasses improved selective polyamides for binding to specific nucleotide sequences of double stranded DNA as well as methods for designing and synthesizing polyamide DNA binding ligands that are selective for an identified specific nucleotide seque... | 08/08/2006 |
| 7087600 | Peptidyl prodrugs and linkers and stabilizers useful therefor The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as ot... | 08/08/2006 |
| 7078536 | Charged compounds comprising a nucleic acid binding moiety and uses therefor Charged compounds are provided that comprise one or more regions of localized positive charge, compositions comprising such compounds, methods of synthesizing such compounds, methods of screening such compounds to identify those having anti-infective activity, and m... | 07/18/2006 |
| 7041459 | Analyzing phosphorylated proteins Methods, compositions and kits are disclosed for determining one or more target polypeptides in a sample where the target polypeptides have undergone phosphorylation. A mixture comprising the sample and a first reagent comprising a cleavage-inducing moiety and an IM... | 05/09/2006 |
| 7041669 | 1,4-benzofused urea compounds useful in treating cytokine mediated diseases Disclosed are 1,4-disubstituted benzo-fused urea compounds of formula (I): wherein Ar, X, A, L, and Q of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes an... | 05/09/2006 |
| 6958339 | Pyrazole derivative The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal co... | 10/25/2005 |
| 6955874 | Kits employing oligonucleotide-binding e-tag probes Kits for the multiplexed detection of known, selected nucleotide target sequences are provided. Detection involves the release of identifying tags as a consequence of target recognition. The kits include sets of electrophoretic tag probes or e-tag probes, capture ag... | 10/18/2005 |
| 6906199 | Process for preparing distamycin derivatives It is described a process for preparing, in high yields and purity and without the need of carrying out several steps and/or isolating many intermediates which could lead to undesired by-products, a distamycin derivative of formula | 06/14/2005 |
| 6794518 | Vitronectin receptor antagonist pharmaceuticals The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer ... | 09/21/2004 |
| 6753316 | Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring of the polyetherocyclic chain, from N and CH; R1 | 06/22/2004 |
| 6746989 | Substituted benzoylpyrazoles as herbicides The invention relates to novel substituted benzoylpyrazoles of the general formula (I), in which n represents the numbers 0, 1, 2 or 3, A represents a single bond or represents alkanediyl(alkylene), ... | 06/08/2004 |
| 6723743 | High affinity small molecule C5a receptor modulators This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as anta... | 04/20/2004 |
| 6706711 | Pyrazole derived kinase inhibitor Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein R1, R2, T, n and Q are as described in the specification. The compounds are useful for treatin... | 03/16/2004 |
| 6686368 | Inhibitors of factor Xa 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.... | 02/03/2004 |
| 6673940 | Compositions and methods relating to cyclic compounds that undergo nucleotide base pair-specific interactions with double-stranded nucleic acids The design, synthesis, and use of cyclic compounds, including cyclic polyamides, is described. Such compounds comprise at least two polymer portions, one of which comprises at least three molecular units, and the other comprises at least four molecular un... | 01/06/2004 |
| 6649643 | Imidazol-4-ylmehanols and their use as inhibitors of steroid C17-20 lyase Imidazol-4-ylmethanols and their uses for preventing and treating primary tumors, metastasis and recurrence of tumors, various symptoms accompanying tumors, prostatic hypertrophy, virilism, hirsutism, male pattern alopecia, precocious puberty, endometrios... | 11/18/2003 |
| 6620826 | Endothelin receptor antagonists Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.... | 09/16/2003 |
| 6593477 | Synthesis of 3-acylaminopyrazoles Disclosed is a process for forming an N-acylamino pyrazole comprising contacting a N-acyl-3-oxo-imino ether compound either with a salt of hydrazine in the presence of a base or with hydrazine.... | 07/15/2003 |
| 6545162 | Method for the synthesis of pyrrole and imidazole carboxamides on a solid support The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise ... | 04/08/2003 |
| 6534524 | Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or... | 03/18/2003 |
| 6528509 | Pyrazole compositions useful as inhibitors of ERK Described herein are compounds that are useful as protein kinase inhibitors having the formula: ##STR1## where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviate... | 03/04/2003 |
| 6506906 | Preparation and use of bifunctional molecules having DNA sequence binding specificity Small molecule polyamides that specifically bind with subnanomolar affinity to any predetermined sequence in the human genome with potential use in molecular biology and human medicine are described. Further, the designed compounds which target the minor ... | 01/14/2003 |
| 6503912 | Substituted guanidine derivatives The present application relates to novel guanidine derivatives of the formula (I) ##STR1## in which R1 represents a five- or six-membered heterocyclic group; R2 represents hydrogen or alkyl, R3 represents the groupings --OR | 01/07/2003 |
| 6492393 | Compounds useful as anti-inflammatory agents Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammat... | 12/10/2002 |
| 6492346 | Hybridization and mismatch discrimination using oligonucleotides conjugated to minor groove binders Conjugates between a minor groove binding molecule, such as the trimer of 1,2-dihydro-(3H)-pyrrolo[3,2-e]indole-7-carboxylate (CDPI3), and an oligonucleotide form unusually stable hybrids with complementary target sequences, in which the tether... | 12/10/2002 |
