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| Number | Title | Issue Date |
| 7960563 | Indazoles used to treat estrogen receptor beta mediated disorders The present invention relates to novel indazole derivatives having pharmacological activity, processes for their preparation, compositions containing them and uses of these compounds in the treatment of estrogen receptor beta mediated diseases. ... | 06/14/2011 |
| 7868184 | Multicore indazolinone library There is provided a method to convert O-functionalized indazolinone-derivatives to the corresponding N2-functionalized indazolinone derivatives, by use of microwave energy or a transition metal catalyst. A preferred catalyst is palladium tetrakis. The method describ... | 01/11/2011 |
| 7449585 | Indazol-3-ones and analogues and derivatives thereof which modulate the function of the vanilloid-1 receptor (VR1) Compounds of formula (I), which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1). ... | 11/11/2008 |
| 7429609 | Pyrazole compound and medicinal composition containing the same The present invention provides a novel compound having an excellent JNK inhibitory effect. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 des... | 09/30/2008 |
| 7410992 | Ophthalmic compositions for treating ocular hypertension This invention relates to potent potassium channel blocker compounds of Formula (I) or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the ... | 08/12/2008 |
| 7365211 | Heterocyclic GABAA subtype selective receptor modulators This invention relates to a method for modulating α2 subtype GABAA receptors with heterocyclic compounds of formula I, and salts, solvates and prodrugs thereof. The invention further relates to said heterocyclic compounds and pharmaceutical co... | 04/29/2008 |
| 7262200 | Indazolinone compositions useful as kinase inhibitors The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK... | 08/28/2007 |
| 7125863 | Inhibitors of dipeptidyl peptidase IV Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of t... | 10/24/2006 |
| 7078425 | Preparation of phosphatase inhibitors Disclosed are compounds of the Formula (I) and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, R1, R2, R3, and R4 are as defined in the specification. Such compounds are tyrosine phosphatase inhibitor... | 07/18/2006 |
| 6943170 | N-cycloalkylglycines as HIV protease inhibitors This invention relates generally to N-cycloalkylglycines of the Formula (I): or a stereoisomeric form, a mixture of stereoisomeric forms, or a pharmaceutically acceptable salt thereof, which are useful as HIV protease ... | 09/13/2005 |
| 6933390 | Process for the arylation of aza-heterocycles with activated aromatics in presence of caesium carbonate The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of fur... | 08/23/2005 |
| 6858638 | Substituted indazoles, compositions containing them, method of production and use Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particlar in oncology. ... | 02/22/2005 |
| 6727246 | 1-(aminoalkyl)-3-sulfonylindole-and-indazole derivatives as 5-hydroxytryptamine-6 ligands The present invention provides compounds of formula I and the use thereof for the treatment of central nervous system disorders related to or affected by the 5-HT6 receptor. ... | 04/27/2004 |
| 6297260 | Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least o... | 10/02/2001 |
| 6288063 | Substituted 4-biarylbutyric and 5-biarylpentanoic acid derivatives as matrix metalloprotease inhibitors Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)x A--B--D--E--G whe... | 09/11/2001 |
| 6258819 | Substituted 2(4-piperidyl)-4(3H)-quinazolinones and 2-(4-piperidyl)-4(3H)-azaquinazolinones This invention relates to compounds which are generally alpha1A/B -receptor antagonists and which are represented by Formula I: ##STR1## wherein the substituents are as defined in the specification; or pharmaceutically acceptable salts, hydrate... | 07/10/2001 |
| 6214834 | Integrin inhibitor prodrugs This invention relates to novel heterocycles which are useful as antagonists of the vଲ.sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, to iontophoretic d... | 04/10/2001 |
| 6180637 | 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones having anti-asthmatic, anti-allergic, anti-inflammatory, immunomodulating and neuroprotective action, process for their preparation and their use as medicaments The invention relates to 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones of formula (I) ##STR1## wherein X is --SO2 --, --SO--, --(CH2)p --, --(CH2)p --O--, --(CH2)p --(C.dbd.O)--... | 01/30/2001 |
| 6166023 | 1,5- and 3-O-substituted 1H-indazoles having anti-asthmatic, anti-allergic, anti-inflammatory, immunomodulating and neuroprotective action, process for their preparation and their use as medicaments The invention relates to 1,5- and 3-O-substituted 1H-indazoles of formula (I) ##STR1##... | 12/26/2000 |
| 5990145 | Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I, A--B--D--E--F--G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compound... | 11/23/1999 |
| 5928998 | Arylindazoles and their use as herbicides Substituted arylindazoles of the formula: ##STR1## wherein X is CR14 and R14 is hydrogen, halogen, haloalkyl, cyano, nitro, alkylthio, alkylsulfonyl, alkylsulfinyl or alkoxy; and substituents R1, R2, R... | 07/27/1999 |
| 5925637 | Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## wherein r is 0-2, T is selec... | 07/20/1999 |
| 5840738 | Selective ଲ-3 adrenergic agonists The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective 댣 adrenergic receptor agonists useful in the treatment of Type II diabet... | 11/24/1998 |
| 5821256 | Endothelin receptor antagonists Novel compounds of the formula I ##STR1## in which R1, R2, R3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.... | 10/13/1998 |
| 5776932 | 1,3,5-tribsubstituted indazole derivatives, processes for preparing, and for pharmacological treatment therewith 1,3,5-trisubstituted indazole derivatives of the formula ##STR1## wherein R1 is H, (b) a C1-6 straight or branched, substituted or unsubstituted alkyl residue, (c) a C3-7 cycloalkyl residue, (d) an unsustituted or substituted ph... | 07/07/1998 |
| 5763616 | Indazolesulfonylurea derivative, its use and intermediate for its production The present invention provides an indazolesulfonylurea derivative represented by the general formula: ##STR1## wherein R1 is a hydrogen atom or an alkyl group, etc., R2 and R3 are the same or different and represent... | 06/09/1998 |
| 5756532 | Aminomethyl-2 3 8 9-tetrahydro-7H-1 4-dioxino2 3-E!-indol-8-ones and derivatives The compounds of formula I: ##STR1## wherein R1 and R2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R1 and R2, taken together, are benzylidene optionally substituted with R3 as defin... | 05/26/1998 |
| 5726198 | N,N-di(aryl) cyclic urea derivatives as anti-coagulants N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## wherein R1 is --C(NH)NH2, --C(NH)N(H)OR11, --C(NH)N(H)C(O)R9, or --C(NH)N(H)C(O)OR11 ; R2... | 03/10/1998 |
| 5714606 | Pyrrolidine-containing monomers and oligomers The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.... | 02/03/1998 |
| 5635537 | 8-substituted-2-aminotetralins A compound of the formula ##STR1## Z is hydrogen or halogen, Q is COR1 or 5-or 6-membered aryl which may contain 1 or 2 heteroatoms selected from N, 0 or S and may be substituted or fused wherein R is hydrogen or C1 -methyl (cis... | 06/03/1997 |
| 5631381 | Process for the preparation of pesticidal 1-(haloaryl) heterocyclic compounds Process for preparing complex pesticidal 1-(haloaryl)heterocyclic compounds by reacting 1-(nitroaryl)heterocycles with metallic halide salts.... | 05/20/1997 |
| 5576343 | Aromatic amidine derivatives and salts thereof An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from ... | 11/19/1996 |
| 5541214 | N-polyhalobenzyl-pyrazole carboxamides endowed with acaricidal and insecticidal activity Amides of pyrazolecarboxy acids having the general formula (I): ##STR1## exhibiting a high insecticidal and acaricidal activity.... | 07/30/1996 |
| 5519134 | Pyrrolidine-containing monomers and oligomers Novel pyrrolidine monomers bearing various functional groups are used to prepare oligomeric structures. The pyrrolidine monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups... | 05/21/1996 |
| 5508450 | Benzopyran derivatives Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, c... | 04/16/1996 |
| 5506243 | Sulfonamide derivatives Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infar... | 04/09/1996 |
| 5440035 | Heterocyclic amide derivatives The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R1, R2, L, X,... | 08/08/1995 |
| 5374644 | Fungicides Compounds of formula: ##STR1## and stereoisomers thereof, wherein X, Y and Z, which are the same or different, are hydrogen, halogen, hydroxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally ... | 12/20/1994 |
| 5312820 | Substituted carbamoyl and oxycarbonyl derivatives of biphenylmethylamines Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT1 and AT2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. ... | 05/17/1994 |
| 5306692 | Herbicidal indazole and benzimidazole compounds A herbicidal compound of formula (I): ##STR1## or N-oxide or quaternised derivative thereof; Ar is an optionally substituted aryl or heterocyclic ring system; W is O or NR1 where R1 is H or lower alkyl; A, B, D are independently sele... | 04/26/1994 |
