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Tricyclic heterocycles as BET protein inhibitors
The present disclosure relates to tricyclic heterocycles of Formula I, which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful...
Thieno-indole moieties and methods of treating using the same
The present invention relates to a novel class of alkylating agents comprising a thieno-indole moiety linked to a DNA-binding moiety, which have cytotoxic...
Compounds of chiral aromatic spiroketal diphosphine ligands, preparation
methods and uses thereof
Disclosed are aromatic spiroketal diphosphine ligands, preparation methods and uses thereof. The ligands have the structure of formula (I), in which R.sup.1,...
Production method for anhydro sugar alcohol having markedly reduced ion
content and improved colour characteristics
The present invention relates to a production method for an anhydro sugar alcohol having a markedly reduced ion content and improved color characteristics, and,...
Chromane-like cyclic prenylflavonoids for the medical intervention in
The present invention relates to certain chromane-like cyclic prenylflavonoids, in particular the compounds of formulae (I), (II) and (III) as described and...
Amidopyridine derivative and use thereof
The present invention relates to novel amidopyridine derivatives. More specifically, the present invention provides a medicinal agent which is useful as a...
Compounds and compositions for use in phototherapy and in treatment of
ocular neovascular disease and cancers
The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including...
HSPC-sparing treatments for RB-positive abnormal cellular proliferation
This invention is in the area of improved compounds for and methods of treating selected RB-positive cancers and other Rb-positive abnormal cellular...
Oxindole compounds carrying a CO-bound spiro substituent and use thereof
for treating vasopressin-related diseases
The present invention relates to novel substituted oxindole derivatives of formula I ##STR00001## wherein the variables are as defined in the claims and the...
Process for preparing chiral dipeptidyl peptidase-IV inhibitors
A process for the preparation of pyrazolopyrolidines of structural formula I: ##STR00001## and W is ##STR00002## or P, wherein in P is an amine protecting...
Compounds and methods for treatment of hypertension
Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor...
Fused triazole derivatives as gamma secretase modulators
The present invention provides fused bicyclic triazole derivatives of Formula (I) useful as gamma secretase modulators (GSM), for the treatment of Alzheimer's...
Phenyl-urea and phenyl-carbamate derivatives as inhibitors of protein
The present invention relates to certain phenyl-urea and phenyl-carbamate derivatives comprising a bicyclic heteroaryl group, pharmaceutical compositions...
Pyrrole six-membered heteroaryl ring derivative, preparation method
thereof, and medicinal uses thereof
The present invention relates to a pyrrole six-membered heteroaryl ring derivative, the preparation method therefor, and the medicinal uses thereof....
Benzyl piperidine compounds as lysophosphatidic acid (LPA) receptor
The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their...
Salt and polymorph of pyrazolopyrimidinone compound, and pharmaceutical
composition containing the same,...
The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate,...
N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
The present invention provides N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks)...
Treatment of lupus, fibrotic conditions, and inflammatory myopathies and
other disorders using PI3 kinase...
Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory...
Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR00001## wherein R.sup.2, W, A, Y and R.sup.1 are as defined in the specification,...
Derivatives and methods of treating hepatitis B infections
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of...
Naphthyridine derivative compounds
The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of...
Heteroaromatic compounds and their use as dopamine D1 ligands
The present invention provides, in part, compounds of Formula I: ##STR00001## and pharmaceutically acceptable salts thereof and N-oxides of the foregoing;...
Inhibitors of human immunodeficiency virus replication
The disclosure generally relates to compounds of formula (I), including compositions and methods for treating human immunodeficiency virus (HIV) infection. The...
Substituted pyrido[2,3-b]pyrazines as phosphodiesterase 2A inhibitors
The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of...
Substituted-quinoxaline-type piperidine compounds and the uses thereof
The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type...
Benzimidazole tetrahydropyran derivatives
Novel compounds described herein are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the...
2-pyridinecarboxamide derivatives, compositions containing such compounds,
and methods of treatment
Novel pyridine-2-carboxamide derivatives of formula I and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2...
Inhibitors of EZH2
The present invention relates to compounds that inhibit activity of the histone lysine N-methyltransferase, Enhancer of Zeste Homolog 2 (EZH2), pharmaceutical...
Crystal having specific crystal habit and pharmaceutical composition
containing the crystal as active ingredient
An object is to provide a crystal having a new crystal habit of luliconazole and expand the possibility of application to pharmaceuticals. Disclosed is a...
Cyclopropylamines as LSD1 inhibitors
The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
Substituted 1-benzylquinoxalin-2(1H)-one analogs as positive allosteric
modulators of muscarinic acetylcholine...
The invention relates to substituted 1-benzylquinoxalin-2(1H)-one analogs, which are useful as positive allosteric modulators of the muscarinic acetylcholine...
Stable crystal form of tipiracil hydrochloride and crystallization method
for the same
An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride....
Substituted condensed pyrimidine compounds
The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) ##STR00001## in which the chemical groupings, substituents...
Heteroaromatic compounds and their use as dopamine D1 ligands
The present invention provides, in part, compounds of Formula I: ##STR00001## and pharmaceutically acceptable salts thereof; processes for the preparation of;...
Inhibitors of the renal outer medullary potassium channel
This invention relates to compounds having structural Formula I: ##STR00001## and pharmaceutically acceptable salts thereof which are inhibitors of the Renal...
Histone demethylase inhibitors
The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted ...
Method for expanding hematopoietic stem cells using heterocyclic compound
An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful for improvement in the efficiency of gene transfer into...
C-9 oxygen functionalized labdane derivates
This invention relates to diterpenes of general formula (1) belonging to labdane class, isolated from Leucas stelligera, being useful for prevention, treatment,...
Single step process for conversion of furfural to tetrahydrofuran
The present patent discloses a one step process for the synthesis of THF and related ring hydrogenated products form furfural using Palladium metal based carbon...
Purification of taxanes
Disclosed is a method of crystallizing docetaxel comprising combining docetaxel and at least one solubilizing solvent to obtain a solution, wherein the...
Pharmaceutical composition for preventing or treating cognitive
impairment-related disease comprising...
Provided is a pharmaceutical composition for preventing or treating a cognitive impairment-related disease, the pharmaceutical composition including...
Hydroxybupropion analogues for treating drug dependence
The invention provides hydroxybupropion analogs capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic...
Method for preparing 3-trifluoromethyl chalcones
Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture...
Deprotection method for tetrazole compound
The present invention relates to a method of deprotecting a tetrazole compound, useful as an intermediate for angiotensin II receptor blockers, and provides a...
Diethylammonium salts of phenyl-substituted thiobarbituric acid as
The diethylammonium salts of phenyl-substituted thiobarbituric acid as anti-diabetic agents include compounds having the formula: ##STR00001## wherein X is: ...
Pyridazine compounds, compositions and methods
The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine...
Method for producing sulfonyl amidine compound
Provided are a method for producing a sulfonyl amidine compound, which has an excellent gonadotropin releasing hormone receptor antagonism and is useful as a...
Compounds for treating peripheral; neuropathies and other
Compounds and methods for treating or preventing a neurodegenerative disease, disorder or condition associated with the overall activity of hsp90 but not with...
Method of modulating stress-activated protein kinase system
Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency...
Hydroxypyridone derivatives, pharmaceutical compositions thereof, and
their therapeutic use for treating...
Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods...