EA201490919A1 - Производные бетулина - Google Patents

Производные бетулина

Info

Publication number
EA201490919A1
EA201490919A1 EA201490919A EA201490919A EA201490919A1 EA 201490919 A1 EA201490919 A1 EA 201490919A1 EA 201490919 A EA201490919 A EA 201490919A EA 201490919 A EA201490919 A EA 201490919A EA 201490919 A1 EA201490919 A1 EA 201490919A1
Authority
EA
Eurasian Patent Office
Prior art keywords
betulina
derivatives
present
compounds
treating
Prior art date
Application number
EA201490919A
Other languages
English (en)
Other versions
EA027363B1 (ru
Inventor
Марк Эндрю Хэтчер
Брайан Элвин Джонс
Майкл Толар Мартин
Эли Амин Табет
Цзюнь Тан
Original Assignee
ГЛАКСОСМИТКЛАЙН ЭлЭлСи
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by ГЛАКСОСМИТКЛАЙН ЭлЭлСи filed Critical ГЛАКСОСМИТКЛАЙН ЭлЭлСи
Publication of EA201490919A1 publication Critical patent/EA201490919A1/ru
Publication of EA027363B1 publication Critical patent/EA027363B1/ru

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/225—Polycarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/02—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C211/03—Monoamines
    • C07C211/04—Mono-, di- or tri-methylamine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/02—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C211/09—Diamines
    • C07C211/10—Diaminoethanes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/34—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton
    • C07C211/38—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/08—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with only one hydroxy group and one amino group bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C217/26—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is further substituted by halogen atoms or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/02—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C219/04—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C219/06—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having the hydroxy groups esterified by carboxylic acids having the esterifying carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/24—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups or amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/02—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C225/14—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/30—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 doubly-bound oxygen atoms
    • C07C233/33—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 doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/34—Esters of acyclic saturated polycarboxylic acids having an esterified carboxyl group bound to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—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
    • C07D207/04—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
    • C07D207/08—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
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • C07D413/06—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 only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002—Carbocyclic rings fused
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/52—Ortho- or ortho- and peri-condensed systems containing five condensed rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

Настоящее изобретение относится к соединениям, характеризующимся тем, что они имеют структуру в соответствии с приведенной ниже формулой I, или к их фармацевтически приемлемым солям. Соединения по настоящему изобретению пригодны для лечения или предупреждения ВИЧ-инфекции.
EA201490919A 2011-12-16 2012-12-14 Производные бетулина EA027363B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161576448P 2011-12-16 2011-12-16
PCT/US2012/069637 WO2013090664A1 (en) 2011-12-16 2012-12-14 Derivatives of betulin

Publications (2)

Publication Number Publication Date
EA201490919A1 true EA201490919A1 (ru) 2014-11-28
EA027363B1 EA027363B1 (ru) 2017-07-31

Family

ID=48613199

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201490919A EA027363B1 (ru) 2011-12-16 2012-12-14 Производные бетулина
EA201790923A EA201790923A1 (ru) 2011-12-16 2012-12-14 Производные бетулина

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA201790923A EA201790923A1 (ru) 2011-12-16 2012-12-14 Производные бетулина

Country Status (38)

Country Link
US (6) US20150218142A1 (ru)
EP (2) EP2791103B1 (ru)
JP (2) JP6300730B2 (ru)
KR (1) KR101953869B1 (ru)
CN (2) CN107501383A (ru)
AR (1) AR089285A1 (ru)
AU (1) AU2012352110B2 (ru)
BR (1) BR112014014769A2 (ru)
CA (1) CA2859030C (ru)
CL (1) CL2014001585A1 (ru)
CO (1) CO6970600A2 (ru)
CR (1) CR20140301A (ru)
CY (1) CY1119422T1 (ru)
DK (1) DK2791103T3 (ru)
DO (1) DOP2014000121A (ru)
EA (2) EA027363B1 (ru)
ES (1) ES2644578T3 (ru)
HK (1) HK1210180A1 (ru)
HR (1) HRP20171512T1 (ru)
HU (1) HUE034877T2 (ru)
IL (1) IL233081A (ru)
JO (1) JO3387B1 (ru)
LT (1) LT2791103T (ru)
MA (1) MA35833B1 (ru)
ME (1) ME02895B (ru)
MX (1) MX360679B (ru)
PE (1) PE20141788A1 (ru)
PH (3) PH12014501362B1 (ru)
PL (1) PL2791103T3 (ru)
PT (1) PT2791103T (ru)
RS (1) RS56373B1 (ru)
SG (1) SG11201402707PA (ru)
SI (1) SI2791103T1 (ru)
TW (2) TW201730202A (ru)
UA (1) UA116978C2 (ru)
UY (1) UY34523A (ru)
WO (1) WO2013090664A1 (ru)
ZA (1) ZA201404135B (ru)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3387B1 (ar) * 2011-12-16 2019-03-13 Glaxosmithkline Llc مشتقات بيتولين
CN103242413B (zh) * 2012-02-08 2015-08-26 江西青峰药业有限公司 Lupane三萜系衍生物及其药学用途
CA2893959A1 (en) * 2012-12-14 2014-06-19 Shenshen Cai Pharmaceutical compositions
US9637516B2 (en) 2012-12-31 2017-05-02 Hetero Research Foundation Betulinic acid proline derivatives as HIV inhibitors
US9863858B2 (en) * 2014-02-12 2018-01-09 Ofi Testing Equipment, Inc. Heating and cooling jacket for test cell
US20170129916A1 (en) 2014-06-26 2017-05-11 Hetero Research Foundation Novel betulinic proline imidazole derivatives as hiv inhibitors
BR112017006005A2 (pt) 2014-09-26 2017-12-19 Glaxosmithkline Ip No 2 Ltd composição farmacêutica, e, método de prevenção ou tratamento de uma infecção por hiv.
CN107250153A (zh) * 2014-11-14 2017-10-13 Viiv保健英国第五有限公司 氧代羽扇豆烯衍生物
CA2967601A1 (en) * 2014-11-14 2016-05-19 VIIV Healthcare UK (No.5) Limited Extended betulinic acid analogs
MA40886B1 (fr) 2015-02-09 2020-03-31 Hetero Research Foundation Nouveau triterpénone en c-3 avec des dérivés d'amide inverse en c-28 en tant qu'inhibiteurs du vih
WO2016147099A2 (en) 2015-03-16 2016-09-22 Hetero Research Foundation C-3 novel triterpenone with c-28 amide derivatives as hiv inhibitors
EP3328876A1 (en) * 2015-07-28 2018-06-06 Glaxosmithkline Intellectual Property (No. 2) Limited Betuin derivatives for preventing or treating hiv infections
BR112018001537A2 (pt) 2015-07-28 2018-09-18 Glaxosmithkline Ip No 2 Ltd composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica, métodos para tratamento e para prevenção de uma infecção por hiv em um indivíduo, e, uso de um composto ou sal
US20180273579A1 (en) 2015-09-24 2018-09-27 Glaxosmithkline Intellectual Property (No.2) Limited Compounds with hiv maturation inhibitory activity
WO2017125870A1 (en) 2016-01-20 2017-07-27 Glaxosmithkline Intellectual Property (No.2) Limited Amine derivatives of lupanes with hiv maturation inhibitory activity
WO2018042332A1 (en) 2016-08-31 2018-03-08 Glaxosmithkline Intellectual Property (No.2) Limited Combinations and uses and treatments thereof
WO2018044853A1 (en) * 2016-08-31 2018-03-08 Viiv Healthcare Conpany Combinations and uses and treatments thereof
WO2018042331A1 (en) 2016-08-31 2018-03-08 Glaxosmithkline Intellectual Property (No.2) Limited Combinations and uses and treatments thereof
WO2018044838A1 (en) * 2016-08-31 2018-03-08 Viiv Healthcare Company Combinations and uses and treatments thereof
WO2019150300A1 (en) 2018-02-02 2019-08-08 Glaxosmithkline Intellectual Property (No.2) Limited Crystalline forms of 4-(((3ar,5ar,5br,7ar,9s,11ar,11br,13as)-3a-((r)-2-((4-chlorobenzyl)(2-(dimethylamino)ethyl)amino)-1-hydroxyethyl)-1-isopropyl-5a,5b,8,8,11a-pentamethyl-2-oxo-3,3a,4,5,5a,5b,6,7,7a,8,9,10,11,11a,11b,12,13,13a-octadecahydro-2h-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid
WO2019186342A1 (en) 2018-03-27 2019-10-03 Glaxosmithkline Intellectual Property (No.2) Limited Ionic liquid salts of 4-(((3ar,5ar,5br,7ar,9s,11ar,11br,13as)-3a-((r)-2-((4-chlorobenzyl)(2-(dimethylamino)ethyl)amino)-1-hydroxyethyl)-1-isopropyl-5a,5b,8,8,11a-pentamethyl-2-oxo-3,3a,4,5,5a,5b,6,7,7a,8,9,10,11,11a,11b,12,13,13a-octadecahydro-2h-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid
PT3784349T (pt) 2018-04-24 2024-01-22 Viiv Healthcare Uk No 5 Ltd Compostos com atividade inibidora de maturação do hiv
KR101909885B1 (ko) * 2018-05-25 2018-10-19 김예원 살리드로사이드 또는 베툴린을 이용한 뇌수막종 개선용 조성물
PL237998B1 (pl) 2018-05-28 2021-06-28 Narodowy Inst Lekow Fosfonowe pochodne kwasu 3-karboksyacylobetulinowego, sposób ich otrzymywania oraz ich zastosowanie

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB427857A (en) 1934-08-02 1935-05-01 Newsum Sons & Company Ltd H A new or improved system of construction for skeleton structures, particularly vehicle body frames and door frames
US4107288A (en) 1974-09-18 1978-08-15 Pharmaceutical Society Of Victoria Injectable compositions, nanoparticles useful therein, and process of manufacturing same
GB8815265D0 (en) 1988-06-27 1988-08-03 Wellcome Found Therapeutic nucleosides
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
US5358721A (en) 1992-12-04 1994-10-25 Alza Corporation Antiviral therapy
AU2001262489A1 (en) 2000-05-23 2001-12-03 Univerzita Karlova V Praze Triterpenoid derivatives
HUP0400241A2 (hu) 2001-03-19 2004-06-28 Ono Pharmaceutical Co., Ltd. Hatóanyagként triaza-spiro[5.5]undekán-származékokat tartalmazó gyógyszerkészítmények
US7163700B2 (en) 2001-07-31 2007-01-16 Capricorn Pharma, Inc. Amorphous drug beads
US20080206161A1 (en) 2002-10-25 2008-08-28 Dov Tamarkin Quiescent foamable compositions, steroids, kits and uses thereof
EP1569931B1 (en) 2002-12-13 2008-10-08 Smithkline Beecham Corporation Heterocyclic compounds as ccr5 antagonists
CA2509711A1 (en) 2002-12-13 2004-07-01 Smithkline Beecham Corporation Piperidine derivatives as ccr5 antagonists
AU2003296992A1 (en) 2002-12-13 2004-07-09 Smithkline Beecham Corporation Pyrrolidine and azetidine compounds as ccr5 antagonists
ATE384724T1 (de) 2002-12-13 2008-02-15 Smithkline Beecham Corp Cyclopropylverbindungen als ccr5 antagonisten
AU2003297048A1 (en) 2002-12-13 2004-07-09 Smithkline Beecham Corporation Cyclohexyl compounds as ccr5 antagonists
JP2006512339A (ja) 2002-12-13 2006-04-13 スミスクライン ビーチャム コーポレーション Ｃｃｒ５アンタゴニストとしてのインダン化合物
US20050142205A1 (en) 2003-07-18 2005-06-30 Julia Rashba-Step Methods for encapsulating small spherical particles prepared by controlled phase separation
WO2005112929A2 (en) 2004-05-20 2005-12-01 Cornell Research Foundation, Inc. Anti-hiv-1 activity of betulinol derivatives
TW200628161A (en) * 2004-11-12 2006-08-16 Panacos Pharmaceuticals Inc Novel betulin derivatives, preparation thereof and use thereof
CN101142227A (zh) * 2004-11-12 2008-03-12 帕纳克斯医药公司 新颖的桦木醇衍生物、其制备和其用途
US20090023698A1 (en) 2005-03-29 2009-01-22 Krasutsky Pavel A Methods of manufacturing bioactive 3-esters of betulinic aldehyde and betulinic acid
TW201414495A (zh) 2005-04-04 2014-04-16 Tibotec Pharm Ltd Ｈｉｖ-感染之預防
WO2006117666A2 (en) 2005-04-29 2006-11-09 Pfizer Inc. Dosage forms, pharmaceutical compositions and methods for sub-tenon delivery
JP2009527563A (ja) 2006-02-21 2009-07-30 アキリオン ファーマシューティカルズ，インコーポレーテッド ウイルス感染症を治療するのに有用な置換タラキサスタン
FI121468B (fi) * 2006-06-07 2010-11-30 Valtion Teknillinen Betuliiniperäiset yhdisteet antimikrobisina aineina
CL2007001847A1 (es) 2006-06-23 2008-02-08 Tibotec Pharm Ltd Composicion farmaceutica intramuscular o subcutanea que comprende tmc278 (rilpivirina); proceso para preparar la composicion; y uso para el tratamiento o prevencion de infeccion por vih.
WO2008127364A2 (en) 2006-10-13 2008-10-23 Myriad Genetics, Inc. Antiviral compounds and use thereof
AR063546A1 (es) * 2006-11-03 2009-01-28 Panacos Pharmaceuticals Inc DERIVADOS DE TRITERPENO, METODOS PARA SU PREPARACION, COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN Y SU USO EN LA FABRICACION DE MEDICAMENTOS PARA EL TRATAMIENTO DE INFECCIoN POR EL VIRUS VIH.
AU2008342536A1 (en) * 2008-01-03 2009-07-09 Virochem Pharma Inc. Novel C-21-keto lupane derivatives preparation and use thereof
CA2711424A1 (en) 2008-01-03 2009-07-09 Virochem Pharma Inc. Novel lupane derivatives
DE102008037025C5 (de) 2008-08-08 2016-07-07 Jesalis Pharma Gmbh Verfahren zur Herstellung kristalliner Wirkstoff-Mikropartikel bzw. einer Wirkstoffpartikel-Festkörperform
WO2010053817A1 (en) 2008-11-04 2010-05-14 Trustees Of Dartmouth College Betulinic acid derivatives and methods of use thereof
CZ2008723A3 (cs) 2008-11-13 2010-01-13 Univerzita Palackého v Olomouci 2-Deoxyglykosidy triterpenoidu, zpusob jejich prípravy a jejich použití jako lécivo
KR101847887B1 (ko) 2008-12-11 2018-04-11 시오노기세야쿠 가부시키가이샤 카르바모일피리돈 ｈｉｖ 인테그라제 억제제 및 중간체의 합성
US8802727B2 (en) 2009-07-14 2014-08-12 Hetero Research Foundation, Hetero Drugs Limited Pharmaceutically acceptable salts of betulinic acid derivatives
US9067966B2 (en) * 2009-07-14 2015-06-30 Hetero Research Foundation, Hetero Drugs Ltd. Lupeol-type triterpene derivatives as antivirals
FR2948132B1 (fr) 2009-07-20 2011-08-26 Inst Francais Textile & Habillement Association de produits cationiques et anioniques naturels comme liant pour support textile
BR112012019762A2 (pt) 2010-02-11 2016-02-23 Glaxosmithkline Llc composto, composição, e, método para tratar uma doença.
TWI577377B (zh) 2010-09-16 2017-04-11 Ｖｉｉｖ醫療保健公司 醫藥組合物
WO2013020245A1 (en) * 2011-08-08 2013-02-14 Glaxosmithkline Llc Carbonyl derivatives of betulin
WO2013020246A1 (en) * 2011-08-08 2013-02-14 Glaxosmithkline Llc Methylene derivatives of betulin
IN2014CN04449A (ru) 2011-12-14 2015-09-04 Glaxosmithkline Llc
WO2013091144A1 (en) 2011-12-21 2013-06-27 Glaxosmithkline Llc Propenoate derivatives of betulin
CN104844679B (zh) * 2011-12-16 2017-03-01 葛兰素史克有限责任公司 白桦脂醇的衍生物
JO3387B1 (ar) 2011-12-16 2019-03-13 Glaxosmithkline Llc مشتقات بيتولين
US20150209273A1 (en) 2012-08-28 2015-07-30 Glaxosmithkline Llc Pharmaceutical Compositions
CA2893959A1 (en) 2012-12-14 2014-06-19 Shenshen Cai Pharmaceutical compositions
BR112017006005A2 (pt) 2014-09-26 2017-12-19 Glaxosmithkline Ip No 2 Ltd composição farmacêutica, e, método de prevenção ou tratamento de uma infecção por hiv.

Also Published As

Publication number Publication date
TWI583696B (zh) 2017-05-21
AU2012352110A1 (en) 2014-07-10
TW201730202A (zh) 2017-09-01
PH12014501362A1 (en) 2014-09-22
TW201336862A (zh) 2013-09-16
JP2015501845A (ja) 2015-01-19
EP2791103B1 (en) 2017-08-02
US10064873B2 (en) 2018-09-04
JP2018065867A (ja) 2018-04-26
US20140357643A1 (en) 2014-12-04
KR101953869B1 (ko) 2019-03-04
CN107501383A (zh) 2017-12-22
CA2859030C (en) 2020-06-16
US20160120878A1 (en) 2016-05-05
JP6300730B2 (ja) 2018-03-28
BR112014014769A2 (pt) 2017-06-13
RS56373B1 (sr) 2017-12-29
AU2012352110B2 (en) 2016-05-12
CN105008322B (zh) 2017-09-26
MX2014007280A (es) 2014-07-22
CN105008322A (zh) 2015-10-28
EP3263580A1 (en) 2018-01-03
US20170252356A1 (en) 2017-09-07
PT2791103T (pt) 2017-11-09
CA2859030A1 (en) 2013-06-20
HK1210180A1 (en) 2016-04-15
WO2013090664A1 (en) 2013-06-20
UY34523A (es) 2013-07-31
EA201790923A1 (ru) 2017-09-29
MA35833B1 (fr) 2014-12-01
HRP20171512T1 (hr) 2017-11-17
LT2791103T (lt) 2017-10-25
UA116978C2 (uk) 2018-06-11
SG11201402707PA (en) 2014-09-26
EA027363B1 (ru) 2017-07-31
KR20140104037A (ko) 2014-08-27
DOP2014000121A (es) 2014-07-31
US20130184263A1 (en) 2013-07-18
NZ625516A (en) 2016-01-29
PL2791103T3 (pl) 2018-02-28
EP2791103A4 (en) 2015-05-06
DK2791103T3 (en) 2017-10-02
SI2791103T1 (sl) 2017-11-30
US20170348324A1 (en) 2017-12-07
PH12014501362B1 (en) 2014-09-22
US9102685B2 (en) 2015-08-11
CR20140301A (es) 2014-08-21
ZA201404135B (en) 2019-04-24
PH12017501429A1 (en) 2019-02-27
IL233081A (en) 2017-11-30
PH12017501426A1 (en) 2020-07-13
IL233081A0 (en) 2014-08-03
EP2791103A1 (en) 2014-10-22
US20150218142A1 (en) 2015-08-06
JO3387B1 (ar) 2019-03-13
HUE034877T2 (hu) 2018-03-28
PE20141788A1 (es) 2014-12-10
CO6970600A2 (es) 2014-06-13
ME02895B (me) 2018-04-20
MX360679B (es) 2018-11-13
AR089285A1 (es) 2014-08-13
CL2014001585A1 (es) 2015-02-27
CY1119422T1 (el) 2018-03-07
ES2644578T3 (es) 2017-11-29

Similar Documents

Publication Publication Date Title
EA201490919A1 (ru) Производные бетулина
CY1120480T1 (el) Ενωσεις πυραζολοπυριμιδινης
EA201590321A1 (ru) Дейтерированный барицитиниб
EA201590224A1 (ru) Имидазотриазинкарбонитрилы, используемые в качестве ингибиторов киназы
CR20140231A (es) Derivados de ácido benzotiazol-6-il acético y su uso para tratar una infección por vih
EA201490724A1 (ru) Замещенные соединения тетрагидроизохинолина в качестве ингибиторов фактора xia
EA201290632A1 (ru) Производные бетулина
CR20150078A (es) Análogos de piridazina 1,4-disustituida y métodos para el tratamiento de condiciones relacionadas con la deficiencia de smn
TN2016000090A1 (en) Substituted quinolizine derivatives useful as hiv integrase inhibitors.
UA107954C2 (en) Substituted pyrrolidin-2-carboxamide
EA201391615A1 (ru) Дейтерированные потенциаторы cftr
IN2014MN02652A (ru)
EA201492205A1 (ru) Макроциклические ингибиторы вирусов flaviviridae
EA201290800A1 (ru) Гетероциклическое соединение
MD20140136A2 (ru) Ингибиторы вируса гепатита С
EA201590296A1 (ru) Дейтерированный ибрутиниб
CO6561783A2 (es) Inhibidores del virus flaviviridae
EA201390917A1 (ru) Дигетероарильные соединения в качестве ингибиторов vps34
EA201590862A1 (ru) Фармацевтические композиции
DK2997033T3 (da) Kondenserede tricykliske heterocykliske forbindelser som hiv- integrasehæmmere
EA201591024A1 (ru) Димерные соединения
EA201690894A1 (ru) Феноксиэтилы
EA201500931A1 (ru) Производные пиридин-4-ила
WO2014172188A3 (en) 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
IN2014CN04449A (ru)

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU