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Patent # Description
US-1,028,0177 Use of polyols to obtain stable polymorphous forms of rifaximin
Polyols stabilize polymorphous form of rifaximin, in particular the .beta. form. When polyols having at least two hydroxy groups are added to rifaximin powder,...
US-1,028,0176 Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their...
US-1,028,0175 Hepatitis B antiviral agents
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y--Z--R (I) which inhibit the...
US-1,028,0174 Salt of fused pyrimidine compound and crystal thereof
Provided is a salt having a high selectivity to BTK and is useful as a drug ingredient for a pharmaceutical product. It has been found that fumarate of Compound...
US-1,028,0173 Ibrutinib solid forms and production process therefor
Provided are ibrutinib polymorphs, e.g., crystalline ibrutinib Forms III, IV, V, VI, VII, VIII and Form IX and processes for producing these crystalline forms,...
US-1,028,0172 Inhibitors of KRAS G12C mutant proteins
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): ##STR00001## or a...
US-1,028,0171 Heterocyclic inhibitors of PTPN11
The present invention relates to compounds which may be useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated...
US-1,028,0170 Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and ...
The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and 5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a][1,4]diazepine...
US-1,028,0169 Biaryl bruton's tyrosine kinase inhibitors
The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable...
US-1,028,0168 Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof
The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazopyrimidine compounds) that act as...
US-1,028,0167 Purine derivatives for the treatment of viral infections
The present invention relates to purine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
US-1,028,0166 2-(1H-indazol-3-yl)-3H-imidazo[4,5-B]pyridine and therapeutic uses thereof
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole...
US-1,028,0165 Pyridopyrimidinones and methods of use thereof
The invention relates to pyridopyrimidinone compounds of formula I ##STR00001## or pharmaceutically acceptable salts thereof, wherein X, R.sup.1, R.sup.2,...
US-1,028,0164 Pyrazolopyridone compounds and uses thereof
Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds....
US-1,028,0163 5 or 8-substituted imidazo[1, 5-a] pyridines as indoleamine and/or tryptophane 2, 3-dioxygenases
Disclosed herein are 5 or 8-substituted imidazo[1,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted...
US-1,028,0162 Pyridopyrimidines derivatives compounds
The present invention describes new pyridopyrimidine derivatives compounds with structure represented by General Formula (I): ##STR00001## or pharmaceutically...
US-1,028,0161 Aztreonam derivatives and uses thereof
Disclosed herein are aztreonam derivatives, therapeutic methods of using the aztreonam derivatives, particularly in combination with .beta.-lactamase...
US-1,028,0160 Phthalazinone compounds and methods for the treatment of cystic fibrosis
The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in...
US-1,028,0159 Fused (hetero)cyclic compounds as S1P modulators
The invention relates to (hetero)cyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment,...
US-1,028,0158 Immune adjustment compound, use thereof and pharmaceutical composition comprising same
The present invention provides a compound represented by formula I, wherein R is a halogen element or a C1-C6 alkyl group. The compound has S1P1 receptor...
US-1,028,0157 Process for the synthesis of an indoleamine 2,3-dioxygenase inhibitor
The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl- ...
US-1,028,0156 Heteroaromatic chalcone derivatives and their medical use
The present invention relates to heteroaromatic chalcone derivatives, particularly the compounds of formula (I) as described and defined herein, pharmaceutical...
US-1,028,0155 Process for preparing 4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluoro-pheny- ...
A process for preparing a compound of formula (I): ##STR00001## or a pharmaceutically acceptable salt thereof includes reacting a compound of formula (6): ...
US-1,028,0154 Pyrimidine compound and pharmaceutical use thereof
Provided are a pyrimidine compound represented by Formula 1, a method of preparing the same, and a pharmaceutical use of the pyrimidine compound for the...
US-1,028,0153 Process for the preparation of pure nilotinib and its salt
Object of the present invention is a process for the preparation of the pharmaceutical active ingredient Nilotinib free base or Nilotinib dihydrochloride...
US-1,028,0152 Imaging of glycogen synthase kinase 3
Provided herein are radiolabelled compounds useful for imaging GSK-3 kinase. An exemplary radiolabelled compound provided herein is useful as a radiotracer for...
US-1,028,0150 Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation...
US-1,028,0149 Therapeutic compounds and uses thereof
The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM2b. The invention also provides pharmaceutically...
US-1,028,0148 Electroconductive member for electrophotography and quaternary ammonium salt
Provided is an electroconductive member for electrophotography in which movement of a quaternary ammonium salt toward the surface of a binder resin is...
US-1,028,0147 Solid-supported palladium (II) complex as a heterogeneous catalyst for cross coupling reactions and methods thereof
A solid-supported catalyst ligand which chelates palladium (II) species to form a complex that functions as a heterogeneous catalyst that is stable and can be...
US-1,028,0146 Pyrimidone compounds used as Lp-PLA2 inhibitors and pharmaceutical compositions thereof
The present invention relates to pyrimidone compounds used as Lp-PLA.sub.2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone...
US-1,028,0145 Urea derivative and use therefor
A compound has inhibitory activity on Discoidin Domain Receptor 1. A urea derivative is represented by the formula (I) or a pharmaceutically acceptable salt...
US-1,028,0144 Pyridazine derivatives as RORc modulators
Compounds of formula I: ##STR00001## or pharmaceutical salts thereof, wherein m, A, X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined...
US-1,028,0143 Process for preparing deuterated desmosine and derivatives thereof
There is provided a process for preparing a compound represented by the following general formula (1) or a salt thereof, which comprises exchanging one or more...
US-1,028,0142 Bipyridyl compound
There are provided a compound capable of being a novel ligand allowing regioselective borylation to be performed in the aromatic borylation reaction, and a...
US-1,028,0141 Crystalline compounds
The present invention relates to crystalline forms of (1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane hydrochloride and compositions comprising the same...
US-1,028,0140 Production of pyrrolidine derivatives
The present invention relates to a method for the production of a pyrrolidine derivative.
US-1,028,0139 Cytotoxic peptides and conjugates thereof
Disclosed herein are novel compounds of formula (I) as described herein: ##STR00001## and the use of such peptides in making immunoconjugates (i.e Antibody...
US-1,028,0138 Nitric oxide donating derivatives of fluprostenol
The present invention relates to 15-nitrooxyderivatives of fluprostenol, their use for the treatment of glaucoma and ocular hypertension and formulation...
US-1,028,0136 Process for preparing esters of .alpha.-hydroxy methionine from sugars
A continuous flow process for the preparation of one or more esters of lactic acid and 2-hydroxy-3-butenoic acid or .alpha.-hydroxy methionine analogs from a...
US-1,028,0135 Method for producing isocyanates
The invention relates to a continuously operated method for producing isocyanates by reacting the corresponding amines with phosgene. When changing the target...
US-1,028,0134 Potent cytotoxic agent against human hepatocellular carcinoma cell line based on 2-aryl hydrazonopropanal...
The invention is directed to 2-aryl hydrazonopropanals that exert anti-tumor activity and methods for using them to prevent, inhibit and treat cancer. It also...
US-1,028,0133 Process for the manufacture of 4-aminobenzoamidine dihydrochloride
The present invention relates to a process for the preparation of 4-aminobenzoamidine (4-AMBA) salts of general formula (I) ##STR00001## preferably the salts...
US-1,028,0132 Process for catalytic transvinylation of carboxylic acids
A carboxylic acid is transvinylated with vinyl ester to give a vinyl ester product and the corresponding acid of the vinyl ester in the presence of a catalyst,...
US-1,028,0131 Terpene-derived acids and esters and methods for preparing and using same
The invention relates to terpene-derived acids and esters thereof as well as to processes for synthesizing them.
US-1,028,0130 Polyisobutylene-based thermoplastic elastomers
The present invention is directed to a new class of thermoplastic elastomers (TPEs) and processes for making them. In some embodiments of the present invention,...
US-1,028,0128 Aromatics alkylation process
In a process for alkylating an aromatic hydrocarbon feedstock with an olefin feedstock, at least one of the aromatic hydrocarbon and olefin feedstocks is passed...
US-1,028,0127 Integrated gas turbine and conversion system process
An integrated process and system to generate power and convert acyclic C5 feedstock to non-aromatic, cyclic C5 hydrocarbon. A combustion device, such as a...
US-1,028,0126 Method for producing conjugated diene
A method for producing a conjugated diene according to one aspect of the present invention comprises a step of contacting a raw material gas containing an...
US-1,028,0125 Process for selective ethylene oligomerization with antifouling components
A process for selectively producing 1-butene comprises contacting at least one antifouling agent with at least one aluminum alkyl compound to form at least one...
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