The invention relates to an engineered PETase enzyme comprises an amino acid sequence having at least 70% or 80%, 90%, 95%, 99% or 100% sequence identity to SEQ ID NO: 1. Preferably, the PETase enzyme comprises SEQ ID NO.1 with at least four mutations. The invention also refers to a composition and to a method for decomposing plastics.
A62D 3/02 - Processes for making harmful chemical substances harmless, or less harmful, by effecting a chemical change in the substances by biological methods, i.e. processes using enzymes or microorganisms
B09B 3/60 - Biochemical treatment, e.g. by using enzymes
C08J 11/10 - Recovery or working-up of waste materials of polymers by chemically breaking down the molecular chains of polymers or breaking of crosslinks, e.g. devulcanisation
C12N 15/52 - Genes encoding for enzymes or proenzymes
Institute of Solid State Physics, University of Latvia (Latvia)
Inventor
Leduskrasts, Kaspars
Suna, Edgars
Vembris, Aivars
Maurucaite, Adriana
Abstract
The present invention relates to multi-layered light emitting electrochemical cell (LEC) and preparation thereof. The present invention also relates to the composition of the light emitting layer (3) of a light emitting electrochemical cell (LEC). The light emitting layer (3) of the light emitting electrochemical cell consists of a neutral polymer and a pyridinium luminophore. The pyridinium luminophores used are non-polymeric small molecule compounds.
The present invention relates to a novel N-aryl lysine derivatives and isosteres as cardioprotective agents by inhibiting trimethyllysine hydroxylase (TMLH) activity, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of various diseases and disorders by administration of such substances.
C07D 317/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07C 229/26 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
4.
BENZO[b]SELENOPHENES AS NOVEL SELECTIVE ESTROGEN RECEPTOR MODULATORS
The present invention relates to a novel benzoselenophenes as anticancer agents by modulating estrogen receptor alpha (ERα) activity, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of various diseases and disorders by administration of such substances.
INSTITUTE OF SOLID STATE PHYSICS, UNIVERSITY OF LATVIA (Latvia)
Inventor
Leduskrasts, Kaspars
Suna, Edgars
Vembris, Aivars
Maurucaite, Adriana
Abstract
The present invention relates to multi-layered light emitting electrochemical cell (LEC) and preparation thereof. The present invention also relates to the composition of the light emitting layer (3) of a light emitting electrochemical cell (LEC). The light emitting layer (3) of the light emitting electrochemical cell consists of a neutral polymer and a pyridinium luminophore. The pyridinium luminophores used are non-polymeric small molecule compounds.
The present invention relates to light emitting pyridinium salts and synthesis thereof. The synthesis encompases the formation of the pyridine luminophores, their alkylation, an optional ion exchange sequence and purification. The present invention also relates to the application of the light emitting pyridinium salts, for example in light emitting electrochemical cells (LEC).
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C09K 11/00 - Luminescent, e.g. electroluminescent, chemiluminescent, materials
INSTITUTE OF SOLID STATE PHYSICS, UNIVERSITY OF LATVIA (Latvia)
LATVIAN INSTITUTE OF ORGANIC SYNTHESIS (Latvia)
Inventor
Vembris, Aivars
Suna, Edgars
Maurucaite, Adriana
Leduskrasts, Kaspars
Abstract
The present invention relates to multi-layered light emitting electrochemical cell (LEC) and preparation thereof. The present invention also relates to the composition of the light emitting layer (3) of a light emitting electrochemical cell (LEC). The light emitting layer (3) of the light emitting electrochemical cell consists of a neutral polymer and a pyridinium luminophore. The pyridinium luminophores used are non-polymeric small molecule compounds.
H05B 33/14 - Light sources with substantially two-dimensional radiating surfaces characterised by the chemical or physical composition or the arrangement of the electroluminescent material
C09K 11/02 - Use of particular materials as binders, particle coatings or suspension media therefor
The present invention relates to recombinant spidroin bioconjugates (chemically modified engineered spider silk proteins). More particularly, the invention relates to recombinant spidroin bioconjugates with poly-ethyleneglycol polymers and their use in regenerative medicine.
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
9.
[1,2]SELENAZOLO[2,3-A]PYRIDIN-8-IUM INHIBITORS OF PYRUVATE KINASE ISOFORM M2
The present invention relates to a novel isoselenazolopyridinium salts as anticancer agents by inhibiting pyruvate kinase isoform M2 (PKM2) activity, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of various diseases and disorders by administration of such substances.
A61K 31/4353 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
10.
An assay for measuring binding affinity for cardiolipin of biologically active compounds
The present invention relates to a method for the evaluation of binding affinity of biologically active substances for cardiolipin based on acridinium salt utilization as a fluorescent probe.
The present invention relates to a novel substituted acridinium salts as fluorescent dyes, as well as methods of their manufacturing and use of the disclosed compounds for the detection of cardiolipin.
The present invention relates to a novel cancer curing deuterated selenopheno [h] chromene derivatives, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of cancer by administration of such substances.
The present invention relates to medicine, and in particular to the treatment of viral infections, more particularly to inhibitors of viral mRNA cap methyltransf erases (MTases). Even more particularly, the invention relates to adenosylmercaptane derivatives and pharmaceutical compositions thereof and their use as inhibitors for viral mRNA cap methyltransferases.
The present invention relates to a method for the evaluation of binding affinity of biologically active substances for cardiolipin based on acridinium salt utilization as a fluorescent probe.
This invention relates to the preparation of novel substituted acetamides of formula la-c and their use as anticonvulsants (I) a) R=Ph, R1=Me; b) R=Ph, R1=i-Pr; c) R=EtO, R1=Et.
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
16.
2-(2-OXO-3-PYROLIN-1-YL)ACETAMIDES AS ANTICONVULSANTS
This invention relates to the preparation of novel substituted acetamides of formula la-c and their use as anticonvulsants (I) a) R=Ph, R1=Me; b) R=Ph, R1ii-Pr; c) R=EtO, R1=Et.
C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
C07D 207/273 - 2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
The present invention relates to a novel selenophenochromene hydroxamic acids as angiogenesis inhibitors, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment or prevention of various diseases and disorders by administration of such substances.
The present invention includes DHPDO curcumin derivatives (6) having the following general structure: These DHPDO curcumin derivatives have pronounced anti-cancer activity with lower toxicity on normal cells. Specifically, these compounds can be used in the treatment of breast cancer and colorectal cancer.
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
The present invention includes DHPDO curcumin derivatives (6) having the following general structure: These DHPDO curcumin derivatives have pronounced anti-cancer activity with lower toxicity on normal cells. Specifically, these compounds can be used in the treatment of breast cancer and colorectal cancer.
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
A compound with general formula (I) R1 is H, C1-6alkyl, C2-6alkeny, C2-6alkynyl, aryl, biary1, ary1C1 -6alkyl, arylC2-6alkenyl, arylC2-6alkynyl, heteroaryl, heteroary1Ci-ealkyl, or heteroarylC2-6alkenyl; R2is H, C16alkyl, C2 6alkcny, C2 6alkynyl, aryl, biary1, ary1C 1 6alkyl, arylC2 6alkcnyl, arylC2 6alkynyl, heteroaryl, heteroary1C1-6alkyl, or heteroarylC2-ealkenyl; R3 is-F, -Cl,- CN, -C(=O)R4,-C(=O)OR4,-CR5R6OR4, or -CR5R6N(R7)R8. R4, R5, R6, R7 and R8 independently represent H, C1-6alkyl, C2-6alkeny, C2 6alkynyl, aryl, biary1, ary1C1- 6alkyl, arylC2 6alkenyl, arylC2-6alkynyl, heteroaryl, heteroary1C1-6alkyl, or heteroarylC2 6alkenyl; any of R5 and R6, R7 and R8 are linked together to form, together with the atom to which they are attached, a 3- to 6-membered ring, X is a direct bond or C1-4 alkylene group; or an optical isomer, stereoisomer, racemate, enantiomer, diastereomer, or mixtures thereof; or a pharmaceutically acceptable salt, hydrate, or solvate thereof. The disclosed compounds are useful in the treatment of metastatic tumors, including breast cancer and brain tumors.
The present invention relates to medicine and in particular to the treatment of metastatic tumors, more particularly to antimitotic agents and microtubule polymerization inhibitors. Even more particularly, the invention relates to novel analogs of natural antimitotic agent diazonamide A and pharmaceutical compositions thereof and the use of the novel analogs as inhibitors of microtubule polymerization. Formula (I):
hh] chromene derivatives, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of cancer by administration of such substances.
A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
23.
MACROCYCLIC AMIDES ACTING AS PLASMEPSIN INHBITORS FOR THE TREATMENT OF MALARIA
The present invention relates to medicine and in particular to the treatment of malarial infections, more particularly to inhibitors of malarial aspartic proteases - plasmepsins. Even more particularly, the invention relates to macrocyclic amides and pharmaceutical compositions thereof and their use as inhibitors for plasmepsins (Plm).
Disclosed are new metal- organic frameworks (MOFs) based on tetradentate anthraquinone ligand and method of making and using the same. Disclosed is its ability to adsorb dye molecules from solution. In the formed host-guest complex dye is encapsulated inside MOF pores in such a way, that dye fluorescence is completely quenched. After liberation of the dye its fluorescence is fully restored.
Disclosed are new metal- organic frameworks (MOFs) based on tetradentate anthraquinone ligand and method of making and using the same. Disclosed is its ability to adsorb dye molecules from solution. In the formed host-guest complex dye is encapsulated inside MOF pores in such a way, that dye fluorescence is completely quenched. After liberation of the dye its fluorescence is fully restored.
C07F 1/00 - Compounds containing elements of Groups 1 or 11 of the Periodic Table
B01J 20/22 - Solid sorbent compositions or filter aid compositionsSorbents for chromatographyProcesses for preparing, regenerating or reactivating thereof comprising organic material
The present invention relates to a novel substituted acridinium salts as fluorescent dyes, as well as methods of their manufacturing and use of the disclosed compounds for the detection of cardiolipin.
The present invention relates to a novel selenophenochromene phosphonic acids as antiproliferative agents, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment or prevention of various diseases and disorders by administration of such substances.
C07F 9/6564 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
28.
NOVEL BORONIC ACID CONTAINING PEPTIDOMIMETICS AS MALARIAL SERINE PROTEASE INHIBITORS
The invention relates to novel boric acid-containing peptidomimetics I, (I) acting as inhibitors of the malaria subtilisin-related serine protease (SUB). They are useful as medicinal preparations or as ingredients for the treatment of malaria.
The invention relates to novel boric acid-containing peptidomimetics I, (I) acting as inhibitors of the malaria subtilisin-related serine protease (SUB). They are useful as medicinal preparations or as ingredients for the treatment of malaria.
This invention relates to the novel potentially therapeutic compounds that contain l-acyl derivatives of aziridine-2-carboxamide and their analogues with the anticancer and/or antiproliferative, and/or antimetastatic properties and/or those with the thioredoxin reductase inhibitory activity as well as the application of these compounds in cancer treatment and/or prophylaxis and in the treatment of such diseases where thioredoxin reductase inhibition is crucial.
C07D 203/18 - Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with acylated ring nitrogen atoms by carboxylic acids, or by sulfur or nitrogen analogues thereof
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/396 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having three-membered rings, e.g. aziridine
The present invention relates to a novel selenophenochromene hydroxamic acids as angiogenesis inhibitors, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment or prevention of various diseases and disorders by administration of such substances.
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
The present invention relates to a novel selenophenochromene hydroxamic acids as angiogenesis inhibitors, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment or prevention of various diseases and disorders by administration of such substances.
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
33.
1-ACETYL-5-NITRO-4-PHENYL-3-PYRROLIN-2-ONE FOR USE IN CANCER TREATMENT
The invention relates to medicine, in particular to medical use of 1-acetyl-5-nitro-4- phenyl-3-pyrrolin-2-one exhibiting metalloproteinase and angiogenesis inhibiting properties for the treatment of cancer.
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
The present invention relates to a novel cancer metastasis preventing and curing selenopheno[h]chromene derivatives, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment and/or prevention of primary cancer and its metastasis by administration of such substances.
The present invention relates to novel aminoalkylazoles acting as inhibitors of malarial protease plasmepsin II. These can be used as medicines or as constituent of medicines for the treatment of malaria infection.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
C07D 207/20 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 207/333 - Radicals substituted by oxygen or sulfur atoms
C07D 249/06 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
36.
SUBSTITUTED AMINOALKYLAZOLES AS MALARIAL ASPARTIC PROTEASE INHIBITORS
The present invention relates to novel aminoalkylazoles acting as inhibitors of malarial protease plasmepsin II. These can be used as medicines or as constituent of medicines for the treatment of malaria infection.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 249/06 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
C07D 207/20 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 207/333 - Radicals substituted by oxygen or sulfur atoms
A method for the preparation of ibrutinib's precursor, 3-(4-phenoxypheny1)-1- ((3R)- piperidin-3-y1)-1H-pyrazolo[3,4-cillpyrimidin-4-amine, involving arylation of N-protected 1- (piperidin-3-y1)pyrazo1o[3,4-alpyrimidin-4-amine in the presence of palladium catalyst, nitrogen-containing ligand, and base, with subsequent removal of the protecting groups by known methods, is reported.
A method for the preparation of ibrutinib's precursor, 3-(4-phenoxyphenyl)-1-((3R)-piperidin-3-il)-1H-pyrazolof [3,4-d]|pyrimidin-4-amine, involving arylation of N-protected 1-(piperidin-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine in the presence of palladium catalyst, nitrogen-containing ligand, and base, with subsequent removal of the protecting groups by known methods, is reported. (Formula (II))
Use of 2-(5S-Methyl-2-oxo-4R-phenyl-pyrrolidin-1-yl)-acetamide or its pharmaceutically acceptable salt in manufacture of a medicament for prophylaxis and treatment of seizure.
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
The present invention relates to ethynylxanthine derivatives of formula (l) which exhibit high antiproliferative activity against various tumour cell lines, methods for their synthesis and use for the treatment and/or prevention of cancer.
The present invention relates to novel ethynylxanthine derivatives of formula (I) which exhibit high antiproliferative activity against various tumor cell lines, methods for their synthesis and use for the treatment and/or prevention of cancer.
The present invention relates to novel pharmaceutical compounds, which exhibit ability to act as calcium ion channel modulators, methods for their synthesis and the treatment and/or prevention of various diseases and disorders including deregulated calcium ion channel activity.
The present invention relates to a novel ethynylxanthine derivatives of formula (I) which exhibit ability selectively suppress matrix metalloproteinases and therefore may act as inhibitors of angiogenesis, methods for their synthesis and use for the treatment and/or prevention of various diseases and disorders caused by overexpression of matrix metalloproteinases by administration of such substances.
The thieno[2,3-b]pyridines of general formula (I),
as multidrug resistance modulators to increase the effectiveness of chemotherapy in cancer treatment.
The invention relates to application of well-defined air and moisture stable hydridopalladium(ll) halides LnPd(H)(X), where L is ligand and X is halide, as preformed catalysts in the Suzuki-Miyaura cross-coupling reactions between arylboron derivatives (boronic acids, pinacolylboronates) and aryl halides in the production of biaryl compounds.
B01J 31/12 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides containing organo-metallic compounds or metal hydrides
46.
NOVEL SUBSTITUTED 2-AMINOQUINAZOLIN-4(3H)-ONE DERIVATIVES AS MALARIAL ASPARTIC PROTEASE INHIBITORS
The present invention discloses novel substituted 2-aminoquinazolin-4(3H)-one derivatives and their use as inhibitors of malarial aspartic protease plasmepsin I,II,IV or related malarial aspartic proteases, as well as pharmaceutical compositions thereof for treatment of malaria.
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
The invention relates to medicine, in particular S-Phenotropil ((S)-2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide) containing pharmaceutical compositions and their use in control of body mass gain.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A method for the preparation N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)- quinazolin-4-amine (erlotinib) from 6,7-bis(2-methoxyethoxy)quinazolin-4(3H)-one and 3-aminophenylacetylene in the presence of titanium(IV) chloride and anisole is reported.
The thieno[2,3-b]pyridines of general formula (I), wherein R1 is Me, C6H5, 3,4,5-(OMe)3C6H2, NH2; R2 is H, CN, COMe, COOC1-4 alkyl, COOC2H4OMe, COOC2H4 OPr(n); R3 is C6H4R6, 3,4-OCH2O-C6H3; 2-furanyl; R6 is 4-Cl, 4-NO2, 4-N(C1-4alkyl)2, 3-(C1-4alkyloxy), 4-(C1-4alkyloxy), 3,4-(C1-4 alkyloxy)2, 3,4,5-(C1-4alkyloxy)3; R4 is NH2, NHCOMe; R5 is CN, COMe, COC6H4 R7; CO-(2-naphthyl); R7 is H, 4-F, 4-Cl, 3-OMe, 4-OMe, 2,4-(OMe)2, 3,4,5-(OMe)3 as multidrug resistance modulators to increase the effectiveness of chemotherapy in cancer treatment.
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
50.
PHARMACEUTICAL COMPOSITION FOR REDUCING THE TRIMETHYLAMINE N-OXIDE LEVEL
The invention discloses the use of pharmaceutical compositions containing 3-(2,2,2-trimethylhydrazinium)propionate, its dihydrate or pharmaceutically acceptable salts thereof for trimethylamine N-oxide level decrease in a body.
A61K 31/205 - Amine addition salts of organic acidsInner quaternary ammonium salts, e.g. betaine, carnitine
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
51.
PHARMACEUTICAL COMPOSITION ON BASIS OF REVERSE TRANSCRIPTASE INHIBITOR AND MELDONIUM
Novel pharmaceutical compositions which contain one of the reverse transcriptase inhibitors, viz., Zidovudine, Lamivudine or Stavudine in clinically efficacious amount and Meldonium as well as pharmaceutically applicable excipients. It has been proved that inclusion of Meldonium in these pharmaceutical compositions essentially diminishes the cardio- and neuro-toxicity of the reverse transcriptase inhibitor.
A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
patents
