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Class 548/362.5 - Having chalcogen or nitrogen attached indirectly to the diazole ring by acyclic nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen or chalcogen (i.e., oxygen, sulfur,
No. of patents: 196
Last issue date: 10/18/2011


1          
NumberTitleIssue Date
8039639Kinase inhibitors and methods of use thereof
A compound of Formula II and salts thereof are useful in the preparation of a compound of Formula I and pharmaceutically acceptable salts and prodrugs thereof. ...
10/18/2011
7741494Histone deacetylase inhibitors
Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein. ...
06/22/2010
7622594Glucocortioid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
Compounds of Formula (IA) and (IB) wherein R1, R2, R3, A, B, C, D, and E are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such ...
11/24/2009
7605272IGF-1R inhibitor
The present invention provides a type I insulin-like growth factor receptor (IGF-1R) inhibitor comprising, as an active ingredient, an indazole derivative represented by Formula (I): {wherein R1 represents —NR
10/20/2009
7449586Processes for the preparation of CGRP-receptor antagonists and intermediates thereof
The invention relates to novel processes for the preparation of small molecule antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”) and intermediates thereof. ...
11/11/2008
7419989Indazole-carboxamide compounds
The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 recep...
09/02/2008
7402606Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss
Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle ...
07/22/2008
7399765Substituted diazabicycloalkane derivatives
Compounds of formula (I) Z-Ar1—Ar2  (I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substitute...
07/15/2008
7396833Indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, and preparation and uses thereof
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of ...
07/08/2008
7365211Heterocyclic 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
7332149Vitronectin 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 in a patient...
02/19/2008
7304060Indazolyl-substituted pyrroline compounds as kinase inhibitors
The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or am...
12/04/2007
7271190Indazole compounds as β3 adrenoceptor agonist
A compound represented by the general formula I: I wherein R1 represents hydrogen, etc. R2 represents NHSO2R3, etc., provided that R3 represents C1-6 alkyl, etc. R5 represents hydrogen, etc. R6
09/18/2007
7250436Indazole-aminoacetonitrile derivatives having special pesticidal activity
The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances gi...
07/31/2007
7232912Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
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 diseases to modulate and/or i...
06/19/2007
7223772Pyrazolopyridine derivatives as selective cox-2 inhibitors
The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from the gr...
05/29/2007
7217728Diaminopropionic acid derivatives
A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds. ...
05/15/2007
7214699Indazole derivatives as CRF antagonists
This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein R3 is optionally substituted aryl or heteroaryl, R1...
05/08/2007
7211594Indazole compounds and compositions thereof as JNK inhibitors and for the treatment of diseases associated therewith
This invention is generally directed to Indazole Derivatives having the following structure: or pharmaceutically acceptable salt thereof, wherein R1, R2 and A are as defined herein. Such com...
05/01/2007
7205299Indole derivatives having an apoptosis-inducing effect
The invention relates to indole derivatives which are used as drugs for treating tumor diseases, in particular when there is drug resistance against other active compounds and where there is a metastasizing carcinoma. ...
04/17/2007
7199147Rho kinase inhibitors
A compound represented by the formula (1): wherein R1—X— indicates that 1 to 4 R1—X— groups are present which may be the same or different, the rin...
04/03/2007
7196082Ophthalmic 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 us...
03/27/2007
7141587Indazole 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
7125863Inhibitors 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
RE39265Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compound...
09/05/2006
7060841Process for preparing 1-methylindazole-3-carboxylic acid
The invention provides a process for preparing 1-methylindazole-3-carboxylic acid of formula (I): which comprises reacting a methylating agent with indazole-3-carboxylic acid of formula (VI): ...
06/13/2006
7053107Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
Indazole compounds that modulate and/or inhibit the ophthalmic diseases and the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereb...
05/30/2006
6998489Methods of making indazoles
Methods of making indazoles are described. The methods involved reacting an aromatic aldehyde with a nitrogen source to form a nitroso aromatic aldehyde. The nitroso aromatic aldehyde is reacted with a reducing agent to form an indazole which ultimately can be used ...
02/14/2006
6962929Pentafluorobenzenesulfonamides and analogs
The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states...
11/08/2005
69560366-hydroxy-indazole derivatives for treating glaucoma
Substituted 1-(α-alkyl-ethylamino)-1H-indazol-6-ols useful for lowering and controlling IOP and treating glaucoma are disclosed ...
10/18/2005
6943186Methods of treating sepsis
The present invention features a method for treating sepsis. The method includes administrating to a subject in need thereof an effective amount of a fused pyrazolyl compound of formula (I): A is H, C1˜C
09/13/2005
6933390Process 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
6919461Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
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 diseases to modulate and/or i...
07/19/2005
6897231Indazole derivatives as JNK inhibitors and compositions and methods related thereto
Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: wherein R1, R2 and A are as defined...
05/24/2005
6891044Indazole 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...
05/10/2005
6884890Indazole 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...
04/26/2005
6875765Arylsulfonamide ethers, and methods of use thereof
The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1β converting enzyme and other cysteine proteases in the ICE family are described. In one embodiment, the compound is described by the generalized s...
04/05/2005
6864254Inhibitor for 20-hete-yielding enzyme
An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular dis...
03/08/2005
6858638Substituted 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
6794518Vitronectin 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
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