Abstract

A compound of Formula (I) below, or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof: in which R1, R2, R3, R5, R6, and R7 are defined as in the SUMMARY section. Further disclosed are a method of using the above-described compound, salt, stereoisomer, solvate, or prodrug for treating microbial infections and a pharmaceutical composition containing the same. A compound of Formula (I) below, or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof: in which R1, R2, R3, R5, R6, and R7 are defined as in the SUMMARY section. Further disclosed are a method of using the above-described compound, salt, stereoisomer, solvate, or prodrug for treating microbial infections and a pharmaceutical composition containing the same.

IPC Classes  ?

• C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
• A61P 31/04 - Antibacterial agents

Abstract

Provided herein is a pharmaceutical composition including a solid dispersion containing a cap-dependent endonuclease inhibitor or a pharmaceutically acceptable salt thereof for oral administration.

IPC Classes  ?

• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/503 - PyridazinesHydrogenated pyridazines spiro-condensed
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61K 47/38 - CelluloseDerivatives thereof
• A61K 9/10 - DispersionsEmulsions
• A61K 9/14 - Particulate form, e.g. powders
• C07D 471/04 - Ortho-condensed systems

Abstract

The present disclosure provides a pharmaceutical composition including a solid dispersion containing a cap-dependent endonuclease inhibitor or a pharmaceutically acceptable salt thereof for oral administration.

IPC Classes  ?

• A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
• A61K 9/14 - Particulate form, e.g. powders
• A61K 47/38 - CelluloseDerivatives thereof

Abstract

A compound of Formula (I) below, or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof: (I), in which Ra, Rb, Rc, Rd, X1, X2, R1-R4, W, Z, and L are defined as in the SUMMARY section. Further disclosed are a method of using the above-described compound, salt, stereoisomer, solvate, or prodrug for treating HBV infection and a pharmaceutical composition containing same. A compound of Formula (I) below, or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof: (I), in which Ra, Rb, Rc, Rd, X1, X2, R1-R4, W, Z, and L are defined as in the SUMMARY section. Further disclosed are a method of using the above-described compound, salt, stereoisomer, solvate, or prodrug for treating HBV infection and a pharmaceutical composition containing same.

IPC Classes  ?

• C07D 207/36 - Oxygen or sulfur atoms
• 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 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - 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 three or more hetero rings

Abstract

Provided is an amorphous solid dispersion containing a Cap-dependent endonuclease inhibitor or a pharmaceutically acceptable salt thereof for oral administration, wherein the Cap-dependent endonuclease inhibitor or a pharmaceutically acceptable salt thereof is dispersed in a matrix formed from the pharmaceutically acceptable polymer. Further disclosed are methods for preparing a above amorphous solid dispersion and a use thereof for treating virus infection and a pharmaceutical composition containing same.

IPC Classes  ?

• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/503 - PyridazinesHydrogenated pyridazines spiro-condensed
• A61K 9/14 - Particulate form, e.g. powders
• A61K 9/10 - DispersionsEmulsions
• C07D 471/04 - Ortho-condensed systems
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

The present disclosure provides an amorphous solid dispersion containing a Cap-dependent endonuclease inhibitor or a pharmaceutically acceptable salt thereof for oral administration, wherein the Cap-dependent endonuclease inhibitor or a pharmaceutically acceptable salt thereof is dispersed in a matrix formed from the pharmaceutically acceptable polymer. Further disclosed are methods for preparing a above amorphous solid dispersion and a use thereof for treating virus infection and a pharmaceutical composition containing same.

IPC Classes  ?

• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• A61K 47/38 - CelluloseDerivatives thereof

Abstract

Provided is a stereoselective synthesis of an intermediate for the preparation of the heterocyclic derivative as a Cap-dependent endonuclease inhibitor. The synthesis process has the advantages of simple operation, higher yield and relatively controllable steroselectivity, such that it is suitable for large-scale production.

IPC Classes  ?

• C07D 409/12 - 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 chain containing hetero atoms as chain links
• C07D 471/04 - Ortho-condensed systems
• C07D 337/12 - [b, e]-condensed

Abstract

Provided is a stereoselective synthesis of an intermediate for the preparation of the heterocyclic derivative as a Cap-dependent endonuclease inhibitor. The synthesis process has the advantages of simple operation, higher yield and relatively controllable steroselectivity, such that it is suitable for large-scale production.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 471/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups
• C07D 487/04 - Ortho-condensed systems
• A61K 31/12 - Ketones
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 31/12 - Antivirals

Abstract

1235677 are defined as in the SUMMARY section. Further disclosed are a method of using the above-described compound, salt, stereoisomer, solvate, or prodrug for treating microbial infections and a pharmaceutical composition containing the same.

IPC Classes  ?

• C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Abstract

A compound of Formula (I) below, or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof: (I), in which Ra, Rb, Rc, Rd12144, W, Z, and L are defined as in the SUMMARY section. Further disclosed are a method of using the above-described compound, salt, stereoisomer, solvate, or prodrug for treating HBV infection and a pharmaceutical composition containing same.

IPC Classes  ?

• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• 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 487/04 - Ortho-condensed systems
• C07D 405/14 - 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 three or more hetero rings
• C07D 471/04 - Ortho-condensed systems
• C07D 207/36 - Oxygen or sulfur atoms
• A61K 31/4025 - 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/437 - 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 containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61P 31/20 - Antivirals for DNA viruses

Abstract

Provided is a compound of Formula (I) below, or a pharmaceutically acceptable salt, metabolite, or prodrug thereof: 3-10 heterocyclyl. Further provided are a method of using the above-described compound, or the pharmaceutically acceptable salt, metabolite, or prodrug thereof for treating influenza and a pharmaceutical composition containing same.

IPC Classes  ?

• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

14256735671223345566771-62-62-61-62-61-61-61-63-203-205656553-103-103-10 heterocyclyl. Further provided are a method of using the above- described compound, or the pharmaceutically acceptable salt, metabolite, or prodrug thereof for treating influenza and a pharmaceutical composition containing same.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems

Abstract

115355 cycloalkyl. The trans-isomeric compound has a trans:cis ratio of at least 70:30. Further provided is a method for preparing the trans-isomeric compound.

IPC Classes  ?

• C07D 211/36 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 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 ring carbon atoms
• C07D 211/02 - Preparation by ring-closure or hydrogenation

Abstract

A trans-isomeric compound of formula (I) below or a pharmaceutically acceptable salt thereof: 5 cycloalkyl and the trans-isomeric compound has a trans:cis ratio of at least 70:30. Further disclosed is a method for preparing the trans-isomeric compound.

IPC Classes  ?

• C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Abstract

A spray-dried solid dispersion containing a pharmaceutical compound of formula (I) shown below and a pharmaceutically acceptable polymer, in which the pharmaceutical compound is dispersed in a polymer matrix formed from the pharmaceutically acceptable polymer. Further disclosed are methods for preparing such a solid dispersion and using it for treating hepatitis C virus infection and a pharmaceutical formulation containing same.

IPC Classes  ?

• A61K 31/407 - 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 condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

A spray-dried solid dispersion containing a pharmaceutical compound of formula (I) shown below and a pharmaceutically acceptable polymer, in which the pharmaceutical compound is dispersed in a polymer matrix formed from the pharmaceutically acceptable polymer. Further disclosed are methods for preparing such a solid dispersion and using it for treating hepatitis C virus infection and a pharmaceutical formulation containing same.

IPC Classes  ?

• C07D 473/00 - Heterocyclic compounds containing purine ring systems
• C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
• C07D 471/04 - Ortho-condensed systems
• A61K 31/407 - 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 condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• A61K 31/79 - Polymers of vinyl pyrrolidone
• A61K 31/795 - Polymers containing sulfur
• A61K 31/765 - Polymers containing oxygen
• 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
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61K 9/14 - Particulate form, e.g. powders
• A61K 9/20 - Pills, lozenges or tablets

Abstract

A method of sensitizing a cancer cell to a chemotherapy agent or tracking myocardial infarction. The method includes administering to a subject in need thereof an effective amount of a compound of formula (I), wherein R1 is C3-20 cycloalkyl, each R2 is H or C1-6 alkyl, L1 is C3-20 heterocycloalkyl, L2 is C3-20 cycloalkyl, and m, n, o, p, and q are each independently 0-6.

IPC Classes  ?

• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61P 35/00 - Antineoplastic agents

Abstract

This invention relates to macrocyclic compounds shown in the specification. These compounds can be used to treat hepatitis C virus infection.

IPC Classes  ?

• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• 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
• A61K 31/4355 - 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 containing a five-membered ring having oxygen as a ring hetero atom
• A61P 31/12 - Antivirals

Abstract

This invention relates to macrocyclic compounds of formula (I) shown in the specification. These compounds can be used to treat hepatitis C virus infection.

IPC Classes  ?

• A61K 31/407 - 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 condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• C07D 245/04 - Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
• 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

Abstract

This invention relates to dialdehyde or dinitrile compounds, which are useful for stereoselective synthesis of piperidine, pyrrolidine, and azepane derivatives.

IPC Classes  ?

• C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 215/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
• C07D 213/72 - Nitrogen atoms

Abstract

This invention relates to a pharmaceutical kit containing a lyophilized preparation of a pyrimidine compound described in the specification. Also disclosed is a lyophilization process for making this preparation.

IPC Classes  ?

• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/02 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings
• A61K 9/19 - Particulate form, e.g. powders lyophilised
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

This invention relates to a malic acid salt of (3S, 5R)-7-[3-amino-5-methyl-piperidinyl]-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid. Also disclosed is a method of treating bacterial infection by an effective amount of this salt.

IPC Classes  ?

• C07D 215/233 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
• C07D 215/227 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
• A61K 31/47 - QuinolinesIsoquinolines
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Abstract

This invention relates to a method of treating infection by methicillin-nonsusceptibale bacteria, vancomycin-nonsusceptibale bacteria, penicillin-nonsusceptibale bacteria, clarithromycin-nonsusceptibale bacteria, or metronidazole-nonsusceptibale bacteria by administering to a subject in need thereof an effective amount of a compound of the following formula:

IPC Classes  ?

• A61K 31/47 - QuinolinesIsoquinolines

Abstract

The invention relates to a method of treating pneumonia by orally administering to a subject in need thereof a quinolone compound of formula (I), shown in the disclosure, at a daily dose of 2-30 mg/kg.

IPC Classes  ?

• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61K 47/38 - CelluloseDerivatives thereof
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

This invention relates to a method of treating infection by methicillin-nonsusceptibale bacteria, vancomycin-nonsusceptibale bacteria, penicillin-nonsusceptibale bacteria, clarithromycin-nonsusceptibale bacteria, or metronidazole-nonsusceptibale bacteria by administering to a subject in need thereof an effective amount of a quinolone compound of the formula shown in the specification.

IPC Classes  ?

• A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 31/04 - Antibacterial agents

Abstract

This invention relates to macrocyclic compounds of formula (I) or (II) shown in the specification. These compounds can be used to treat hepatitis C virus infection.

IPC Classes  ?

• C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• 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
• A61P 31/12 - Antivirals

Abstract

This invention relates to heterocyclic compounds of the formulas shown in the specification. It also relates to methods for treating inflammatory diseases or immune diseases, developmental or degenerative diseases, and tissue injuries with one of the heterocyclic compounds

IPC Classes  ?

• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/02 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings

Abstract

Pyrrolidine compounds as shown in the specification. Also disclosed is use of these compounds, alone or in combination with other active agents, to treat hepatitis C virus infection

IPC Classes  ?

• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/02 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings

IPC Classes  ?

• A61K 31/05 - Phenols
• A61K 31/19 - Carboxylic acids, e.g. valproic acid
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters

Abstract

This invention relates to a parenteral formulation containing an effective amount of the compound of the following formula I: water, and an isotonic agent. Also disclosed is a method of treating an infectious disease by administering this formula to a subject via parenteral injection or infusion.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/47 - QuinolinesIsoquinolines
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings

Abstract

This invention relates to the compounds of formula shown in the specification. These compounds can be used to treat a kinesin Eg5 protein-mediated disorder.

IPC Classes  ?

• C07C 305/00 - Esters of sulfuric acids
• C07D 313/00 - Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
• C12Q 1/42 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving phosphatase

Abstract

This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat hepatitis C virus infection.

IPC Classes  ?

• A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
• A61K 31/47 - QuinolinesIsoquinolines

Abstract

This invention relates to the peptide-like compounds of formula (I) as shown herein. These compounds can be used to treat hepatitis C virus infection.

IPC Classes  ?

• A01N 37/18 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N, e.g. carboxylic acid amides or imidesThio-analogues thereof
• A61K 38/00 - Medicinal preparations containing peptides

Abstract

This invention relates to methods for treating retinopathy and repairing tissue damage. The methods include administering to a subject in need thereof an effective amount of one or more compounds of the following formula (I): Each variable in this formula is defined in the specification.

IPC Classes  ?

• A61K 31/40 - 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
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61K 31/18 - Sulfonamides

Abstract

Process for making 7-cycloamino-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acids. Borate ester compounds suitable for use in such process.

IPC Classes  ?

• C07D 401/00 - 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
• C07D 215/00 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems

Abstract

The present invention is directed to malate salts of (3S,5S)-7-[3-amino-5-methyl-piperidinyl]-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid, and its polymorphs. The present invention is also directed to pharmaceutical compositions comprising the described salts and polymorphs.

IPC Classes  ?

• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• C07D 401/02 - 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

Abstract

Hydride process for making acyclic diol intermediates from cyclic intermediates, useful in antibacterial quinolone synthesis.

IPC Classes  ?

• C07D 207/28 - 2-Pyrrolidone-5- carboxylic acidsFunctional derivatives thereof, e.g. esters, nitriles
• C07D 295/00 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms