Abstract

Compounds and their use in treating a condition, disease, or disorder associated with an increased neutral sphingomyelinase 2 (nSMase2) activity or expression are disclosed.

Abstract

Prodrugs of itaconic acid and 1- and 4-methyl itaconic acid and their use for treating a disease, disorder, or condition associated with inflammation are disclosed.

IPC Classes  ?

• C07C 69/593 - Dicarboxylic acid esters having only one carbon-to-carbon double bond
• C07C 69/90 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with esterified hydroxyl and carboxyl groups
• C07C 229/36 - 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 containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
• C07C 237/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
• C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups

Abstract

Conjugates comprising one or more therapeutic agents or a prodrug thereof, such as the glutamine antagonist 6-diazo-5-oxo-L-norleucine (DON) and prodrugs or derivatives thereof, conjugated to an avidin through biotin, wherein the avidin is further linked to an antibody, and use of the conjugates for treating a disease, condition, or disorder, including cancer, are disclosed.

IPC Classes  ?

• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• A61K 31/42 - Oxazoles
• C07D 261/04 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/66 - Phosphorus compounds
• A61K 31/7076 - 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 containing purines, e.g. adenosine, adenylic acid
• A61P 35/00 - Antineoplastic agents
• C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
• C07D 317/40 - Vinylene carbonateSubstituted vinylene carbonates

Abstract

Novel N4-substituted decitabine analogs are disclosed that exhibit promising in vitro and in vivo therapeutic activity. These novel compounds were shown to be resistant to deamination via cytidine deaminase (CDA) metabolism and provide a unique pharmacokinetic profile versus decitabine, while retaining the ability to induce DNA demethylation in target cells. These novel compounds can be used for treating hematological cancers, as well for new therapeutic interventions, including bacterial or viral pneumonia, acute respiratory distress syndrome, pulmonary fibrosis, transplantation and checkpoint inhibitor-induced adverse events, including pneumonitis.

IPC Classes  ?

• C07H 19/12 - Triazine radicals
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/706 - 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

Abstract

The present disclosure describes 3′3′ cyclic phosphonate dinucleotides of general formula (J), their pharmaceutically acceptable salts, their pharmaceutical composition and combinations of substances and other medicaments or pharmaceuticals. The disclosure also describes the use of compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. These substances can be used as adjuvants in vaccines. The present disclosure describes 3′3′ cyclic phosphonate dinucleotides of general formula (J), their pharmaceutically acceptable salts, their pharmaceutical composition and combinations of substances and other medicaments or pharmaceuticals. The disclosure also describes the use of compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. These substances can be used as adjuvants in vaccines.

IPC Classes  ?

• C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
• A61P 37/02 - Immunomodulators

Abstract

Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.

IPC Classes  ?

• C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
• C07F 9/38 - Phosphonic acids [R—P(:O)(OH)2]Thiophosphonic acids
• C07F 9/40 - Esters thereof
• C07F 9/44 - Amides thereof

Abstract

Prodrugs of itaconic acid and 1- and 4-methyl itaconic acid and their use for treating a disease, disorder, or condition associated with inflammation are disclosed.

IPC Classes  ?

• C07C 69/593 - Dicarboxylic acid esters having only one carbon-to-carbon double bond
• C07C 69/90 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with esterified hydroxyl and carboxyl groups
• C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
• C07C 237/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
• C07C 229/36 - 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 containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton

Abstract

Provided herein are carbohydrate derivatives of general formula (I) bearing a trans-cyclooctene moiety usable in covalently binding active moieties to cell surfaces in vitro and/or in vivo and their use for therapeutic or nontherapeutic purposes. Furthermore, compounds of general formula (II) are used together with the derivatives of general formula (I) in a method of binding active moieties to the cell surface. The compounds may be combined to form a kit for forming a covalent attachment of active moieties to the cell surface.

IPC Classes  ?

• C07H 13/12 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by acids having the group —X—C (=X)—X—, or halides thereof, in which X means nitrogen, oxygen, sulfur, selenium, or tellurium, e.g. carbonic acid, carbamic acid
• C12N 5/071 - Vertebrate cells or tissues, e.g. human cells or tissues
• A61K 31/7012 - Compounds having a free or esterified carboxyl group attached, directly or through a carbon chain, to a carbon atom of the saccharide radical, e.g. glucuronic acid, neuraminic acid
• A61K 35/12 - Materials from mammalsCompositions comprising non-specified tissues or cellsCompositions comprising non-embryonic stem cellsGenetically modified cells
• C07H 13/04 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms

Abstract

transin vitroin vivoin vivo and their use for therapeutic or nontherapeutic purposes. Furthermore, compounds of general formula (II) are used together with the derivatives of general formula (I) in a method of binding active moieties to the cell surface. The compounds may be combined to form a kit for forming a covalent attachment of active moieties to the cell surface.

IPC Classes  ?

• C07H 13/04 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
• A61K 31/7012 - Compounds having a free or esterified carboxyl group attached, directly or through a carbon chain, to a carbon atom of the saccharide radical, e.g. glucuronic acid, neuraminic acid
• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids

Abstract

The present disclosure relates to 3'3' cyclic dinucleotides containing isonucleotidic units, their pharmaceutically acceptable salts, their pharmaceutical composition and combinations of said substances and other medicaments or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. In addition, these substances can be used as adjuvants in vaccines. The compounds have formula (J):

IPC Classes  ?

• C07H 19/11 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
• C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
• A61P 35/00 - Antineoplastic agents
• A61P 37/04 - Immunostimulants
• A61P 31/12 - Antivirals

Abstract

The present disclosure relates to 3'3' cyclic dinucleotides containing isonucleotidic units, their pharmaceutically acceptable salts, their pharmaceutical composition and combinations of said substances and other medicaments or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. In addition, these substances can be used as adjuvants in vaccines. The compounds have formula (J):

IPC Classes  ?

• C07H 19/11 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
• A61P 31/12 - Antivirals
• A61P 37/04 - Immunostimulants
• C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate

Abstract

Prodrugs of 6-mercaptopurine (6-MP) and methods of their use for treating cancers and autoimmune diseases are disclosed.

IPC Classes  ?

• C07F 9/28 - Phosphorus compounds with one or more P—C bonds
• C07D 487/04 - Ortho-condensed systems
• C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
• C07H 19/16 - Purine radicals
• A61K 31/7076 - 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 containing purines, e.g. adenosine, adenylic acid
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

N44in vitroin vivoin vivo therapeutic activity. These novel compounds were shown to be resistant to deamination via cytidine deaminase (CDA) metabolism and provide a unique pharmacokinetic profile versus decitabine, while retaining the ability to induce DNA demethylation in target cells. These novel compounds can be used for treating hematological cancers, as well for new therapeutic interventions, including bacterial or viral pneumonia, acute respiratory distress syndrome, pulmonary fibrosis, transplantation and checkpoint inhibitor-induced adverse events, including pneumonitis.

IPC Classes  ?

• C07H 19/12 - Triazine radicals
• 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
• A61P 35/00 - Antineoplastic agents
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present disclosure relates to 3'3' cyclic phosphonate dinucleotides of general formula (J), their pharmaceutically acceptable salts, their pharmaceutical composition and combinations of said substances and other medicaments or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. In addition, these substances can be used as adjuvants in vaccines. (Formula (J))

IPC Classes  ?

• C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
• A61P 35/00 - Antineoplastic agents
• A61K 31/7084 - Compounds having two nucleosides or nucleotides, e.g. nicotinamide-adenine dinucleotide, flavine-adenine dinucleotide
• A61P 31/12 - Antivirals

Abstract

The present disclosure relates to 3'3' cyclic phosphonate dinucleotides of general formula (J), their pharmaceutically acceptable salts, their pharmaceutical composition and combinations of said substances and other medicaments or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. In addition, these substances can be used as adjuvants in vaccines. (Formula (J))

IPC Classes  ?

• C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
• A61P 31/12 - Antivirals

Abstract

Prodrugs of hydroxamate-based GCPII inhibitors and methods of their use for treating a disease or condition are disclosed.

IPC Classes  ?

• C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
• A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
• C07C 259/08 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07D 317/38 - Ethylene carbonate

Abstract

GCPII inhibitors comprising 2-(phosphonomethyl) pentanedioic acid (2-PMPA) conjugated to a bile acid and their use for treating a disease or condition associated with elevated levels of GCPII, including inflammatory bowel disease.

IPC Classes  ?

• C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
• C07J 33/00 - Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

Prodrugs of itaconic acid and 1- and 4-methyl itaconic acid and their use for treating a disease, disorder, or condition associated with inflammation are disclosed.

IPC Classes  ?

• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
• A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil

Abstract

Prodrugs of itaconic acid and 1- and 4-methyl itaconic acid and their use for treating a disease, disorder, or condition associated with inflammation are disclosed.

IPC Classes  ?

• C07C 69/593 - Dicarboxylic acid esters having only one carbon-to-carbon double bond
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
• A61K 31/225 - Polycarboxylic acids
• A61K 31/235 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
• A61K 31/25 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids with polyoxyalkylated alcohols, e.g. esters of polyethylene glycol
• A61K 31/265 - Esters, e.g. nitroglycerine, selenocyanates of carbonic, thiocarbonic or thiocarboxylic acids, e.g. thioacetic acid, xanthogenic acid, trithiocarbonic acid
• A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
• C07C 69/86 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with esterified hydroxyl groups
• C07C 69/96 - Esters of carbonic or haloformic acids
• C07C 233/49 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a carbon atom of an acyclic unsaturated carbon skeleton
• C07C 233/51 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
• C07C 237/20 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
• C07C 271/16 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
• C07D 307/60 - Two oxygen atoms, e.g. succinic anhydride

Abstract

Prodrugs of mebendazole and methods for their use in treating a disease, disorder, or disorder, including cancer, are disclosed.

IPC Classes  ?

• C07D 235/32 - Benzimidazole-2-carbamic acids, unsubstituted or substitutedEsters thereofThio-analogues thereof
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/661 - Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion
• A61P 35/00 - Antineoplastic agents
• C07D 405/12 - 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 chain containing hetero atoms as chain links
• C07F 9/09 - Esters of phosphoric acids

Abstract

Prodrugs of mebendazole and methods for their use in treating a disease, disorder, or disorder, including cancer, are disclosed.

IPC Classes  ?

• C07D 235/32 - Benzimidazole-2-carbamic acids, unsubstituted or substitutedEsters thereofThio-analogues thereof
• C07D 405/12 - 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 chain containing hetero atoms as chain links
• C07F 9/09 - Esters of phosphoric acids
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/661 - Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion
• A61P 35/00 - Antineoplastic agents

Abstract

Prodrugs of glutamine analogs, such as prodrugs of acivicin, are disclosed.

IPC Classes  ?

• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• A61K 31/42 - Oxazoles
• C07D 261/04 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member

Abstract

Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer, are provided.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 35/00 - Antineoplastic agents

Abstract

Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer, are provided.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 35/00 - Antineoplastic agents

Abstract

Prodrugs of hydroxamate-based GCPII inhibitors and methods of their use for treating a disease or condition are disclosed.

IPC Classes  ?

• C07C 239/20 - Hydroxylamino compounds or their ethers or esters having oxygen atoms of hydroxylamino groups etherified
• C07D 307/34 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members

Abstract

Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.

IPC Classes  ?

• C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
• C07F 9/38 - Phosphonic acids [R—P(:O)(OH)2]Thiophosphonic acids
• C07F 9/40 - Esters thereof
• C07F 9/44 - Amides thereof

Abstract

Prodrugs of glutamine analogs, such as prodrugs of aza-serine, and 6-diazo-5-oxo-norleucine (DON), and 5-diazo-4-oxo-L-norvaline (L-DONV) are disclosed.

IPC Classes  ?

• C07C 227/14 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
• C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
• C07F 9/06 - Phosphorus compounds without P—C bonds
• C07D 317/40 - Vinylene carbonateSubstituted vinylene carbonates
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/66 - Phosphorus compounds
• A61K 31/7076 - 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 containing purines, e.g. adenosine, adenylic acid

Abstract

Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.

IPC Classes  ?

• C07F 9/28 - Phosphorus compounds with one or more P—C bonds
• A61K 31/66 - Phosphorus compounds
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• C07F 9/02 - Phosphorus compounds

Abstract

Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.

IPC Classes  ?

• C07F 9/28 - Phosphorus compounds with one or more P—C bonds
• C07F 9/02 - Phosphorus compounds
• A61K 31/66 - Phosphorus compounds
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The present invention relates to a compound or a pharmaceutically acceptable salt or solvate thereof for use in inhibiting HIV capsid assembly, the compound comprising the core structure wherein E is CR7or S, and wherein f is 0 or 1, and wherein in case E is S, f is 0, and wherein the core structure is at least substituted in 2 and 4 position, and wherein the residue R6 and R7, are, independently of each other, selected from the group consisting of -H, -D, -alkyl, alkoxy, alkenyl, alkynyl, halides, -NO2, - OH, -NH2, -NHR4#, -CN, - S(O)R4#, -SO2R4#, -P(O)R4#R5#, -P(O)(OR4#)R5#, -P(O)(OR4#)(OR5#), -C(O)NR4#R5#, - C(O)SR4#, -C(O)R4#, -C(O)O-R4#, alkoxy and glycol chains; and wherein R6 may optionally form a cyclic residue, with a further substituent present 5 or 6 position, and wherein R4# and R5# are, independently of each other, selected from the group consisting of -H, -alkyl, -alkenyl, -heterocyclo alkyl, aryl and heteroaryl.

IPC Classes  ?

• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

The present invention relates a compound or a pharmaceutically acceptable salt or solvate thereof for use in inhibiting HIV capsid assembly, wherein the compound is a pyrimidine being at least substituted in two positions, preferably in 2 and 4 position or in 4 and 6 position, more preferably in 2 and 4 position.

IPC Classes  ?

• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

This invention involves two novel peptides of the formulas (1) H-Gly -Met-Trp -Ser-Lys- -Ile-Leu-Gly -His-Leu-Ile-Arg -NH2 and (2), H-Gly -Lys-Trp -Met-Ser-Leu-Leu-Lys -His-Ile-Leu-Lys-NH2 isolated from natural sources and their synthetic analogs of general formula (1-A) [Xaan]m -Gly-Met-Trp-Ser-Lys-Ile-Leu-Gly-His-Leu-Ile-Arg-NH2 and (2-A), [Xaan]m -Gly-Lys-Trp-Met-Ser-Leu-Leu-Lys-His-Ile-Leu-Lys-NH2 where Xaa represents, independently from each other, proteinogenic amino acid, D-amino acid, non- standard amino acid or amino acid with the side chain modification, n means position of the amino acid replacement and m means the number of the replacements in the peptide chain. Described is also their use for the preparation of medicaments for the treatment of microbial, parasitic and fungal diseases and for the cancer treatment.

IPC Classes  ?

• A61K 38/10 - Peptides having 12 to 20 amino acids
• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans

Abstract

The invention provides compounds of formula (I), wherein R1 and R2 have any of the values defined in the specification and salts thereof, as well as composi-tions comprising such compounds and therapeutic methods that utilize such compounds.

IPC Classes  ?

• C07H 19/14 - Pyrrolo-pyrimidine radicals
• A61K 31/7064 - 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

Abstract

The invention provides compounds of formula (I), wherein R1 and R2 have any of the values defined in the specification and salts thereof, as well as compositions comprising such compounds and therapeutic methods that utilize such compounds.

IPC Classes  ?

• C07H 19/14 - Pyrrolo-pyrimidine radicals
• A61K 31/7064 - 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