EA011130B1 - Ингибиторы сетр - Google Patents

Ингибиторы сетр Download PDF

Info

Publication number
EA011130B1
EA011130B1 EA200700259A EA200700259A EA011130B1 EA 011130 B1 EA011130 B1 EA 011130B1 EA 200700259 A EA200700259 A EA 200700259A EA 200700259 A EA200700259 A EA 200700259A EA 011130 B1 EA011130 B1 EA 011130B1
Authority
EA
Eurasian Patent Office
Prior art keywords
trifluoromethyl
methyl
isopropyl
mmol
methoxy
Prior art date
Application number
EA200700259A
Other languages
English (en)
Russian (ru)
Other versions
EA200700259A1 (ru
Inventor
Амджад Али
Джоанн М. Наполитано
Сяолин Дэн
Чжицзянь Лу
Питер Дж. Синклер
Гейл Э. Тэйлор
Кристофер Ф. Томпсон
Назя Курайши
Камерон Дж. Смит
Джулиан А. Хант
Original Assignee
Мерк Энд Ко., Инк.
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 Мерк Энд Ко., Инк. filed Critical Мерк Энд Ко., Инк.
Publication of EA200700259A1 publication Critical patent/EA200700259A1/ru
Publication of EA011130B1 publication Critical patent/EA011130B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/22—Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • 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
    • A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • A—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
    • A61K31/41—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 being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • 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
    • A61K31/41—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 being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
    • 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
    • A61K31/41—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 being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61K31/41—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 being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/41—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 being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles 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
    • A61K31/41—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 being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/495—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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • 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
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • C07D233/38—One oxygen atom with acyl radicals or hetero atoms directly attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
    • C07D233/50—Nitrogen atoms not forming part of a nitro radical with carbocyclic radicals directly attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
    • C07D233/52—Nitrogen atoms not forming part of a nitro radical with hetero atoms directly attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/24—Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/26—Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/06—1,2,3-Thiadiazoles; Hydrogenated 1,2,3-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/04—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
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/04—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Cephalosporin Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
EA200700259A 2004-07-02 2005-07-01 Ингибиторы сетр EA011130B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US58527404P 2004-07-02 2004-07-02
US64610305P 2005-01-21 2005-01-21
PCT/US2005/023546 WO2006014357A1 (en) 2004-07-02 2005-07-01 Cetp inhibitors

Publications (2)

Publication Number Publication Date
EA200700259A1 EA200700259A1 (ru) 2007-08-31
EA011130B1 true EA011130B1 (ru) 2008-12-30

Family

ID=35045145

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200700259A EA011130B1 (ru) 2004-07-02 2005-07-01 Ингибиторы сетр

Country Status (37)

Country Link
US (5) US7652049B2 (OSRAM)
EP (2) EP1765793B1 (OSRAM)
JP (3) JP4695139B2 (OSRAM)
KR (1) KR101204336B1 (OSRAM)
CN (4) CN104557757A (OSRAM)
AR (2) AR049956A1 (OSRAM)
AU (1) AU2005270058B2 (OSRAM)
BR (1) BRPI0512910A (OSRAM)
CA (1) CA2570717C (OSRAM)
CR (1) CR8808A (OSRAM)
CY (1) CY1117930T1 (OSRAM)
DK (1) DK1765793T3 (OSRAM)
DO (1) DOP2005000123A (OSRAM)
EA (1) EA011130B1 (OSRAM)
EC (1) ECSP067124A (OSRAM)
EG (1) EG27138A (OSRAM)
ES (1) ES2393721T3 (OSRAM)
GE (1) GEP20094694B (OSRAM)
GT (1) GT200500175A (OSRAM)
HR (1) HRP20120993T1 (OSRAM)
IL (2) IL180432A (OSRAM)
JO (1) JO2994B1 (OSRAM)
MA (1) MA28780B1 (OSRAM)
MX (1) MX2007000035A (OSRAM)
MY (1) MY167430A (OSRAM)
NI (1) NI200600322A (OSRAM)
NO (1) NO339808B1 (OSRAM)
NZ (1) NZ552061A (OSRAM)
PA (1) PA8638101A1 (OSRAM)
PE (1) PE20060525A1 (OSRAM)
PL (1) PL1765793T3 (OSRAM)
PT (1) PT1765793E (OSRAM)
RS (1) RS52563B (OSRAM)
SI (1) SI1765793T1 (OSRAM)
SV (1) SV2007002160A (OSRAM)
TW (1) TWI299991B (OSRAM)
WO (2) WO2006014413A1 (OSRAM)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2597266C2 (ru) * 2011-04-12 2016-09-10 Чхон Кхун Дан Фармасьютикал Корп. Циклоалкениларильные производные для ингибирования транспортного белка холестериновых эфиров
RU2627361C2 (ru) * 2013-01-31 2017-08-07 Чонг Кун Данг Фармасьютикал Корп. Биарил- или гетероциклические биарилзамещенные производные циклогексена в качестве ингибиторов сетр

Families Citing this family (119)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7270971B2 (en) * 2003-10-16 2007-09-18 Merck & Co., Inc. Fluorescence assay for measuring the rate of cholesterol ester transfer
DOP2005000123A (es) 2004-07-02 2011-07-15 Merck Sharp & Dohme Inhibidores de cetp
CA2612142A1 (en) 2005-07-01 2007-01-11 Merck & Co., Inc. Process for synthesizing a cetp inhibitor
ATE516016T1 (de) 2005-12-05 2011-07-15 Merck Sharp & Dohme Selbstemulgierende formulierungen von cetp- hemmern
AR057218A1 (es) * 2005-12-15 2007-11-21 Astra Ab Compuestos de oxazolidinona y su uso como pontenciadores del receptor metabotropico de glutamato
US7910592B2 (en) * 2005-12-30 2011-03-22 Merck Sharp & Dohme Corp. CETP inhibitors
US8865707B2 (en) * 2005-12-30 2014-10-21 Merck Sharp & Dohme Corp. Cholesteryl ester transfer protein inhibitors
AU2006332681B2 (en) * 2005-12-30 2011-04-07 Merck Sharp & Dohme Corp. 1, 3-oxazolidin-2-one derivatives useful as CETP inhibitors
EP1973889B1 (en) * 2005-12-30 2016-08-24 Merck Sharp & Dohme Corp. Cetp inhibitors
CN103735515A (zh) 2006-02-09 2014-04-23 默沙东公司 Cetp抑制剂的聚合物制剂
US8383660B2 (en) 2006-03-10 2013-02-26 Pfizer Inc. Dibenzyl amine compounds and derivatives
US7919506B2 (en) 2006-03-10 2011-04-05 Pfizer Inc. Dibenzyl amine compounds and derivatives
WO2007136672A2 (en) * 2006-05-19 2007-11-29 Merck & Co., Inc. Synthesis of a biaryl synthetic intermediate
WO2008082567A1 (en) * 2006-12-29 2008-07-10 Merck & Co., Inc. Process for synthesizing a cetp inhibitor
KR101568799B1 (ko) 2007-01-26 2015-11-12 카네크 파마 인코포레이티드 융합된 방향족 ｐｔｐ-1ｂ 억제제
WO2008115442A1 (en) 2007-03-16 2008-09-25 Concert Pharmceuticals, Inc. Inhibitors of cholesterol ester transfer protein
CA2688187C (en) 2007-05-07 2016-10-11 Merck & Co., Inc. Method of treament using fused aromatic compounds having anti-diabetic activity
EP2520561B1 (en) 2007-06-08 2016-02-10 MannKind Corporation IRE-1A Inhibitors
US8445480B2 (en) * 2007-06-20 2013-05-21 Merck Sharp & Dohme Corp. CETP inhibitors derived from benzoxazole arylamides
US8436028B2 (en) * 2007-06-20 2013-05-07 Merck Sharp & Dohme Corp CETP inhibitors derived from benzoxazole arylamides
EP2166847B1 (en) * 2007-06-20 2014-11-19 Merck Sharp & Dohme Corp. Cetp inhibitors derived from benzoxazole arylamides
AU2008270438B2 (en) 2007-07-02 2013-10-10 F. Hoffmann-La Roche Ag Imidazole derivatives as CCR2 receptor antagonists
EP2183229B1 (en) * 2007-07-26 2012-04-18 Vitae Pharmaceuticals, Inc. Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
AR069207A1 (es) * 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
CA2708303A1 (en) 2007-12-11 2009-06-18 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
TW200934490A (en) * 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
WO2009094169A1 (en) * 2008-01-24 2009-07-30 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2257524B1 (en) 2008-02-01 2016-01-06 Brickell Biotech, Inc. N,n-disubstituted aminoalkylbiphenyl antagonists of prostaglandin d2 receptors
UA98839C2 (en) * 2008-02-01 2012-06-25 Панмира Фармасьютикалз, Ллк. N,n-disubstituted aminoalkylbiphenyl antagonists of prostaglandin d2 receptors
EP2252598A2 (en) * 2008-02-11 2010-11-24 Vitae Pharmaceuticals, Inc. 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP2011512359A (ja) 2008-02-14 2011-04-21 アミラ ファーマシューティカルズ，インク． プロスタグランジンｄ２受容体のアンタゴニストとしての環式ジアリールエーテル化合物
CA2715290A1 (en) * 2008-02-15 2009-08-20 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8497381B2 (en) 2008-02-25 2013-07-30 Panmira Pharmaceuticals, Llc Antagonists of prostaglandin D2 receptors
EP2274287B1 (en) * 2008-03-18 2016-03-09 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
JP2011518130A (ja) 2008-04-02 2011-06-23 アミラ ファーマシューティカルズ，インク． プロスタグランジンｄ２受容体のアミノアルキルフェニルアンタゴニスト
WO2009134392A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8592410B2 (en) 2008-05-01 2013-11-26 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11BETA-hydroxysteroid dehydrogenase 1
ES2421537T3 (es) 2008-05-01 2013-09-03 Vitae Pharmaceuticals Inc Inhibidores cíclicos de la 11beta-hidroxiesteroide deshidrogenasa 1
US8063088B2 (en) * 2008-06-11 2011-11-22 Hoffmann-La Roche Inc. Imidazolidine derivatives
JP5777030B2 (ja) 2008-07-25 2015-09-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤
ES2432150T3 (es) 2008-07-25 2013-12-02 Boehringer Ingelheim International Gmbh Inhibidores cíclicos de la 11 beta-hidroxiesteroide deshidrogenasa 1
EP2323994A1 (en) 2008-07-25 2011-05-25 Boehringer Ingelheim International GmbH Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
GB2463788B (en) 2008-09-29 2010-12-15 Amira Pharmaceuticals Inc Heteroaryl antagonists of prostaglandin D2 receptors
DE102008049675A1 (de) 2008-09-30 2010-04-01 Markus Dr. Heinrich Verfahren zur Herstellung von 3-Aminobiphenylen
WO2010039474A1 (en) * 2008-10-01 2010-04-08 Merck Sharp & Dohme Corp. Prodrugs of oxazolidinone cetp inhibitors
WO2010039977A2 (en) 2008-10-01 2010-04-08 Amira Pharmaceuticals, Inc. Heteroaryl antagonists of prostaglandin d2 receptors
WO2010042652A2 (en) 2008-10-08 2010-04-15 Amira Pharmaceuticals, Inc. Heteroalkyl biphenyl antagonists of prostaglandin d2 receptors
CA2741125A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
CN102271509A (zh) 2008-10-31 2011-12-07 默沙东公司 用于抗糖尿病药的新型环苯并咪唑衍生物
US8383654B2 (en) 2008-11-17 2013-02-26 Panmira Pharmaceuticals, Llc Heterocyclic antagonists of prostaglandin D2 receptors
TW201028414A (en) 2009-01-16 2010-08-01 Merck Sharp & Dohme Oxadiazole beta carboline derivatives as antidiabetic compounds
EP2389368B1 (en) 2009-01-23 2015-06-17 Merck Sharp & Dohme Corp. Bridged and fused antidiabetic compounds
AU2010206786A1 (en) 2009-01-23 2011-07-28 Merck Sharp & Dohme Corp. Bridged and fused heterocyclic antidiabetic compounds
CA2744946A1 (en) 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
TW201040186A (en) 2009-02-05 2010-11-16 Schering Corp Phthalazine-containing antidiabetic compounds
US8680093B2 (en) 2009-04-30 2014-03-25 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8927539B2 (en) 2009-06-11 2015-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 based on the 1,3-oxazinan-2-one structure
WO2011002910A1 (en) 2009-07-01 2011-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2768587A1 (en) 2009-08-05 2011-02-10 Panmira Pharmaceuticals, Llc Dp2 antagonist and uses thereof
JP2011057661A (ja) 2009-08-14 2011-03-24 Bayer Cropscience Ag 殺虫性カルボキサミド類
JP5750449B2 (ja) 2009-11-05 2015-07-22 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規キラルリンリガンド
CN102695414A (zh) 2010-01-15 2012-09-26 默沙东公司 作为抗糖尿病化合物的噁二唑β-咔啉衍生物
AU2011218830B2 (en) 2010-02-25 2014-07-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2011149822A1 (en) 2010-05-26 2011-12-01 Boehringer Ingelheim International Gmbh 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
EP2397473A1 (en) 2010-06-14 2011-12-21 LEK Pharmaceuticals d.d. A stable highly crystalline anacetrapib
EP2582698B1 (en) 2010-06-16 2016-09-14 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
WO2011161128A1 (en) 2010-06-25 2011-12-29 Boehringer Ingelheim International Gmbh Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders
US20130225618A1 (en) 2010-10-04 2013-08-29 Kowa Co., Ltd. Agent for inhibiting expression of lipid metabolism related mrna
AU2011320665B2 (en) 2010-10-29 2015-09-03 Merck Sharp & Dohme Corp. Cyclic amine substituted oxazolidinone CETP inhibitor
EA201300522A1 (ru) 2010-11-02 2013-11-29 Бёрингер Ингельхайм Интернациональ Гмбх Фармацевтические комбинации для лечения метаболических нарушений
EP2468735A1 (en) * 2010-12-23 2012-06-27 LEK Pharmaceuticals d.d. Synthesis of intermediates for preparing anacetrapib and derivates thereof
EP2468736A1 (en) * 2010-12-23 2012-06-27 LEK Pharmaceuticals d.d. Synthesis of intermediates for preparing anacetrapib and derivates thereof
EP2668507B1 (en) 2011-01-26 2017-08-23 INSERM - Institut National de la Santé et de la Recherche Médicale Method for assessing a subject's risk of having a cardiovascular disease.
KR101668514B1 (ko) 2011-02-25 2016-10-21 머크 샤프 앤드 돔 코포레이션 항당뇨병제로서 유용한 신규 시클릭 아자벤즈이미다졸 유도체
CA2840985A1 (en) * 2011-07-07 2013-01-10 Mochida Phamaceutical Co., Ltd. Anti-obesity agent comprising high-purity epa
TWI627167B (zh) 2011-07-08 2018-06-21 諾華公司 用於高三酸甘油酯個體治療動脈粥狀硬化之方法
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
WO2013066768A1 (en) * 2011-10-31 2013-05-10 Merck Sharp & Dohme Corp. Process for a cetp inhibitor
WO2013064188A1 (en) 2011-11-03 2013-05-10 Lek Pharmaceuticals D.D. A stable highly crystalline anacetrapib
US20140303198A1 (en) 2011-11-29 2014-10-09 Kowa Company, Ltd. Agent for inhibiting expression of npc1l1 and/or lipg mrna and agent for preventing and/or treating obesity
RU2604132C2 (ru) * 2011-11-30 2016-12-10 Дэунг Фармасьютикл Ко., Лтд. Фармацевтическая композиция для профилактики или лечения гипертриглицеридемии или вызванных гипертриглицеридемией заболеваний
WO2013091696A1 (en) * 2011-12-21 2013-06-27 Lek Pharmaceuticals D.D. Synthesis of intermediates for preparing anacetrapib and derivatives thereof
WO2013165854A1 (en) * 2012-05-02 2013-11-07 Merck Sharp & Dohme Corp. Cyclic amine substituted heterocyclic cetp inhibitors
MX347400B (es) 2012-06-29 2017-04-18 Univ Nac Autónoma De México Vacuna de aplicacion nasal contra el desarrollo de la enfermedad aterosclerotica y el higado graso.
WO2014012428A1 (zh) * 2012-07-19 2014-01-23 上海恒瑞医药有限公司 噁唑烷酮类衍生物、其制备方法及其在医药上的应用
US9382243B2 (en) 2012-08-22 2016-07-05 Merck Sharp & Dohme Corp. Azabenzimidazole tetrahydropyran derivatives
EP2934518B1 (en) 2012-12-19 2020-02-19 Merck Sharp & Dohme Corp. Spirocyclic cetp inhibitors
EP2934519B1 (en) 2012-12-20 2021-05-12 Merck Sharp & Dohme Corp. Therapeutic thiazolidinone compounds
WO2014111953A1 (en) * 2013-01-17 2014-07-24 Glenmark Pharmaceuticals Limited; Glenmark Generics Limited Process for preparation of anacetrapib and intermediates thereof
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
US9981970B2 (en) 2013-07-30 2018-05-29 Merck Sharp & Dohme Corp. Bicyclic ureas and thiadiazolidine-1, 1-dioxides as CETP inhibitors
WO2015054088A1 (en) 2013-10-10 2015-04-16 Merck Sharp & Dohme Corp. 3,3'-disubstituted indolines as inhibitors of cholesterol ester transfer protein
CN105814064A (zh) 2013-12-17 2016-07-27 默沙东公司 作为胆固醇酯转运蛋白的抑制剂的稠合双环异噁唑啉类
CN104955816B (zh) * 2014-01-14 2016-08-31 杭州普晒医药科技有限公司 一种安塞曲匹的晶型及其制备方法、其药物组合物和用途
CN103923030B (zh) * 2014-03-27 2015-07-22 汕头经济特区鮀滨制药厂 一种安塞曲匹的关键中间体的合成方法
CN103923031A (zh) * 2014-04-01 2014-07-16 汕头经济特区鮀滨制药厂 一种安塞曲匹的中间体的合成方法
EP3174537B1 (en) * 2014-07-29 2021-06-23 Merck Sharp & Dohme Corp. Monocyclic isoxazolines as inhibitors of cholesterol ester transfer protein
EP3795695A1 (en) 2014-07-30 2021-03-24 F. Hoffmann-La Roche AG Genetic markers for predicting responsiveness to therapy
CN104230835B (zh) * 2014-09-01 2017-01-25 福建师范大学 一种合成n‑苯乙烯基恶唑烷‑2‑酮衍生物的方法
WO2016067194A1 (en) * 2014-10-27 2016-05-06 Sun Pharmaceutical Industries Limited Process for the preparation of anacetrapib and an intermediate thereof
CN106032362B (zh) * 2015-03-10 2018-06-19 湖南千金湘江药业股份有限公司 安塞曲匹的制备方法
MX2018015872A (es) 2016-06-29 2019-04-22 Orion Corp Derivados de benzodioxano y su uso farmaceutico.
KR101902002B1 (ko) * 2016-07-19 2018-09-27 재단법인 대구경북첨단의료산업진흥재단 Cetp 억제제로서의 옥사졸리딘온 유도체 화합물
WO2018033866A1 (en) * 2016-08-17 2018-02-22 Novartis Ag New processes and intermediates for nep inhibitor synthesis
CN106496211A (zh) * 2016-10-18 2017-03-15 湖南德魅信息技术有限公司 二氟甲基取代的噁唑烷酮化合物及其用途
CN106496154A (zh) * 2016-10-18 2017-03-15 湖南德魅信息技术有限公司 安塞曲匹的制备方法
CN106749075A (zh) * 2016-11-24 2017-05-31 山东新华制药股份有限公司 阿那曲波的恶唑烷酮中间体的晶型及其制备方法
US20190070178A1 (en) 2017-08-29 2019-03-07 Dalcor Pharma Uk Ltd., Stockport Zug Branch Methods for treating or preventing cardiovascular disorders and lowering risk of cardiovascular events
JOP20180092A1 (ar) 2017-10-13 2019-04-13 Gilead Sciences Inc مثبطات hiv بروتياز
MX2021001520A (es) 2018-08-09 2021-05-27 Dalcor Pharma Uk Ltd Leatherhead Zug Branch Metodos para retardar la ocurrencia de diabetes tipo 2 de nuevo inicio y para desacelerar el progreso de y tratamiento de la diabetes tipo 2.
SG11202107468YA (en) 2019-03-07 2021-08-30 Dalcor Pharma Uk Ltd Leatherhead Methods for treating or preventing heart failure and reducing risk of heart failure
TW202104210A (zh) 2019-04-17 2021-02-01 美商基利科學股份有限公司 Hiv蛋白酶抑制劑
CN114423771A (zh) 2019-07-19 2022-04-29 生物合成股份公司 制备烟酰胺呋喃核糖苷盐的方法、烟酰胺呋喃核糖苷盐本身及其用途
KR20240131463A (ko) 2020-05-05 2024-08-30 뉴베일런트, 아이엔씨. 헤테로방향족 거대환식 에터 화학치료제
EP4146626A4 (en) 2020-05-05 2024-05-29 Nuvalent, Inc. CHEMOTHERAPEUTIC AGENTS BASED ON HETEROAROMATIC MACROCYCLIC ETHERS
WO2022075645A1 (ko) * 2020-10-08 2022-04-14 재단법인 대구경북첨단의료산업진흥재단 Pcsk9 억제제로서 아미노알콜 유도체 및 이를 함유하는 고콜레스테롤 혈증의 예방 또는 치료용 약학적 조성물
US20240360103A1 (en) * 2021-06-30 2024-10-31 Apellis Pharmaceuticals, Inc. Complement inhibition
KR20240087788A (ko) 2021-10-01 2024-06-19 뉴베일런트, 아이엔씨. 헤테로방향족 매크로사이클릭 에테르 화합물의 고체 형태, 약학 조성물 및 제조
WO2025093129A1 (en) 2023-11-01 2025-05-08 Newamsterdam Pharma B.V. Treatment and prevention of age-related macular degeneration using a cetp inhibitor

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0605729A1 (en) * 1992-04-30 1994-07-13 Taiho Pharmaceutical Co., Ltd. Oxazolidine derivative and pharmaceutically acceptable salt thereof
WO1999015487A1 (de) * 1997-09-19 1999-04-01 Bayer Aktiengesellschaft Benzyl-biphenyle und analoge verbindungen und deren verwendung zur behandlung von arteriosklerose und diylipidämien

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4179442A (en) * 1975-08-29 1979-12-18 York Hartleben 4-(Alpha-hydroxy-isopropyl)-5-phenyl-oxazolidin-2-one
DE2655369A1 (de) * 1976-12-03 1978-06-08 Schering Ag 5-(subst. phenyl)-oxazolidinone und deren schwefelanaloga sowie verfahren zu deren herstellung
US4851423A (en) 1986-12-10 1989-07-25 Schering Corporation Pharmaceutically active compounds
WO1988009661A1 (en) * 1987-06-10 1988-12-15 Pfizer Inc. Oxazolidin-2-one derivatives as hypoglycemic agents
US5482971A (en) * 1993-10-01 1996-01-09 American Cyanamid Company Beta3 -adrenergic agents and their use in pharmaceutical compositions
CN1115576A (zh) * 1993-10-15 1996-01-24 盐野义制药株式会社 具有细胞浆磷脂酶a2抑制活性的噁唑啉酮衍生物
AU699085B2 (en) * 1994-04-21 1998-11-19 Schering Aktiengesellschaft PDE IV inhibitors for treating Multiple Sclerosis
FR2729954B1 (fr) * 1995-01-30 1997-08-01 Sanofi Sa Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
CZ290671B6 (cs) * 1995-02-10 2002-09-11 Schering Aktiengesellschaft Farmaceutické preparáty pro inhibici tumornekrosefaktoru
WO1996036616A1 (en) * 1995-05-17 1996-11-21 E.I. Du Pont De Nemours And Company Fungicidal cyclic amides
US5612363A (en) 1995-06-02 1997-03-18 Berlex Laboratories, Inc. N,N-di(aryl) cyclic urea derivatives as anti-coagulants
JPH11508257A (ja) 1995-06-20 1999-07-21 イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー 殺節足動物性及び殺菌・殺カビ性環式アミド
US5846990A (en) * 1995-07-24 1998-12-08 Bristol-Myers Squibb Co. Substituted biphenyl isoxazole sulfonamides
US6310095B1 (en) * 1995-11-06 2001-10-30 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
WO1997028149A1 (en) 1996-02-02 1997-08-07 Merck & Co., Inc. Method for raising hdl cholesterol levels
DE19647380A1 (de) * 1996-11-15 1998-05-20 Hoechst Ag 5-Ring-Heterocyclen als Inhibitoren der Leukozytenadhäsion und VLA-4-Antagonisten
WO1998023155A1 (en) 1996-11-26 1998-06-04 E.I. Du Pont De Nemours And Company Arthropodicidal and fungicidal cyclic amides
DE19704243A1 (de) * 1997-02-05 1998-08-06 Bayer Ag Neue 2-Amino-substituierte Pyridine
BR9811260A (pt) * 1997-03-03 2000-08-08 Boehringer Ingelheim Pharma Pequenas moléculas úteis no tratamento de doença inflamatória
AR015649A1 (es) 1997-05-07 2001-05-16 Univ Pittsburgh Inhibidores de isoprenil-transferasas proteicas, composiciones que los comprenden y el uso de los mismos para la fabricacion de un medicamento
CN1288462A (zh) 1998-01-23 2001-03-21 法玛西雅厄普约翰美国公司 噁唑烷酮组合库、组合物和制备方法
IT1300055B1 (it) * 1998-04-17 2000-04-05 Boehringer Ingelheim Italia Eterocicli con anello a 5 termini difenil-sostituiti loro procedimento di preparazione e loro impiego come farmici
GT199900147A (es) 1998-09-17 1999-09-06 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas.
MX226123B (es) 1999-09-17 2005-02-07 Millennium Pharm Inc Benzamidas e inhibidores del factor xa relacionadas.
HN2000000203A (es) * 1999-11-30 2001-06-13 Pfizer Prod Inc Procedimiento para la obtencion de 1,2,3,4-tetrahidroquinolinas 4-carboxiamino-2- sustituidas.
US6462063B1 (en) 2000-02-04 2002-10-08 Fibrogen, Inc. C-proteinase inhibitors
US6762200B2 (en) 2000-03-28 2004-07-13 Nippon Soda Co. Ltd. Oxa(thia)zolidine derivative and anti-inflammatory drug
CA2431983C (en) * 2000-12-21 2010-06-08 Aventis Pharma Deutschland Gmbh Novel 1,2-diphenylazetidinones, processes for their preparation, medicaments comprising these compounds and their use for treating impaired lipid metabolism
DK1427711T3 (da) 2001-09-11 2005-10-17 Astrazeneca Ab Oxazolidinon og/eller isoxazolinderivater som antibakterielle midler
ATE444065T1 (de) 2001-10-16 2009-10-15 Memory Pharm Corp 4(4-alkoxy-3-hydroxyphenyl)-2-pyrrolidon-deriva e als pde-4-hemmer zur behandlung von neurologischen syndromen
AR043050A1 (es) * 2002-09-26 2005-07-13 Rib X Pharmaceuticals Inc Compuestos heterociclicos bifuncionales y metodos para preparar y usar los mismos
JP5546715B2 (ja) 2003-03-17 2014-07-09 日本たばこ産業株式会社 Ｃｅｔｐ阻害剤の医薬組成物
UA90269C2 (ru) 2004-04-02 2010-04-26 Мицубиси Танабе Фарма Корпорейшн Тетрагидрохинолиновые производные и способ их получения
DOP2005000123A (es) * 2004-07-02 2011-07-15 Merck Sharp & Dohme Inhibidores de cetp
WO2006103527A1 (en) 2005-03-31 2006-10-05 Council Of Scientific And Industrial Research Aromatic substituted pentadienoic acid amide for combination with anti-infective drugs
US7910592B2 (en) * 2005-12-30 2011-03-22 Merck Sharp & Dohme Corp. CETP inhibitors
EP1973889B1 (en) * 2005-12-30 2016-08-24 Merck Sharp & Dohme Corp. Cetp inhibitors
AU2006332681B2 (en) 2005-12-30 2011-04-07 Merck Sharp & Dohme Corp. 1, 3-oxazolidin-2-one derivatives useful as CETP inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0605729A1 (en) * 1992-04-30 1994-07-13 Taiho Pharmaceutical Co., Ltd. Oxazolidine derivative and pharmaceutically acceptable salt thereof
WO1999015487A1 (de) * 1997-09-19 1999-04-01 Bayer Aktiengesellschaft Benzyl-biphenyle und analoge verbindungen und deren verwendung zur behandlung von arteriosklerose und diylipidämien

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2597266C2 (ru) * 2011-04-12 2016-09-10 Чхон Кхун Дан Фармасьютикал Корп. Циклоалкениларильные производные для ингибирования транспортного белка холестериновых эфиров
RU2627361C2 (ru) * 2013-01-31 2017-08-07 Чонг Кун Данг Фармасьютикал Корп. Биарил- или гетероциклические биарилзамещенные производные циклогексена в качестве ингибиторов сетр

Also Published As

Publication number Publication date
BRPI0512910A (pt) 2008-04-15
PE20060525A1 (es) 2006-07-13
US20080119476A1 (en) 2008-05-22
SV2007002160A (es) 2007-03-20
TWI299991B (en) 2008-08-21
IL180432A0 (en) 2007-06-03
AU2005270058A1 (en) 2006-02-09
IL180432A (en) 2012-02-29
EP2415759A1 (en) 2012-02-08
HRP20120993T1 (hr) 2012-12-31
WO2006014357A1 (en) 2006-02-09
GEP20094694B (en) 2009-05-25
EG27138A (en) 2015-08-09
CA2570717C (en) 2011-09-13
AR049956A1 (es) 2006-09-20
EP1765793A1 (en) 2007-03-28
PA8638101A1 (es) 2006-03-24
CN102311401B (zh) 2014-12-03
NO339808B1 (no) 2017-02-06
KR101204336B1 (ko) 2012-11-27
ECSP067124A (es) 2007-01-26
US7652049B2 (en) 2010-01-26
AR087382A2 (es) 2014-03-19
CY1117930T1 (el) 2017-05-17
AU2005270058B2 (en) 2009-04-23
TW200605884A (en) 2006-02-16
JP4491062B1 (ja) 2010-06-30
NO20070607L (no) 2007-04-02
JP5543932B2 (ja) 2014-07-09
CA2570717A1 (en) 2006-02-09
EP1765793B1 (en) 2012-09-26
JP4695139B2 (ja) 2011-06-08
CR8808A (es) 2007-08-28
JP2010150269A (ja) 2010-07-08
CN102304096A (zh) 2012-01-04
US20100099716A1 (en) 2010-04-22
CN104447603A (zh) 2015-03-25
DOP2005000123A (es) 2011-07-15
US8735435B2 (en) 2014-05-27
CN102304096B (zh) 2014-12-03
EA200700259A1 (ru) 2007-08-31
NI200600322A (es) 2007-08-07
JO2994B1 (ar) 2016-09-05
ES2393721T3 (es) 2012-12-27
KR20070039523A (ko) 2007-04-12
US20160075724A1 (en) 2016-03-17
MY167430A (en) 2018-08-28
WO2006014413A1 (en) 2006-02-09
JP2011137006A (ja) 2011-07-14
PT1765793E (pt) 2012-12-06
MX2007000035A (es) 2007-03-07
GT200500175A (es) 2006-03-14
MA28780B1 (fr) 2007-08-01
DK1765793T3 (da) 2013-01-14
US20060040999A1 (en) 2006-02-23
JP2008505120A (ja) 2008-02-21
CN104557757A (zh) 2015-04-29
NZ552061A (en) 2010-09-30
IL217530A0 (en) 2012-02-29
US20140221383A1 (en) 2014-08-07
PL1765793T3 (pl) 2013-03-29
RS52563B (sr) 2013-04-30
SI1765793T1 (sl) 2013-05-31
CN102311401A (zh) 2012-01-11

Similar Documents

Publication Publication Date Title
EA011130B1 (ru) Ингибиторы сетр
US9371294B2 (en) Cycloalkenyl aryl derivatives for CETP inhibitor
JP5793766B2 (ja) 抗菌剤として有用なｎ−結合型ヒドロキサム酸誘導体
US20080261920A1 (en) 2-Aminooxazolines as TAAR1 ligands
KR20180011274A (ko) 사치환된 알켄 화합물 및 그의 용도
US8822510B2 (en) Substituted 3-phenyl-1,2,4-Oxadiazole compounds
US20150376172A1 (en) Fluoro-[1,3]oxazines as bace1 inhibitors
KR101346527B1 (ko) 아민 화합물 및 그 의약 용도
US9233938B2 (en) Inhibitors of cholesterol ester transfer protein
US20170144994A1 (en) Substituted azetidine derivatives
RU2627361C2 (ru) Биарил- или гетероциклические биарилзамещенные производные циклогексена в качестве ингибиторов сетр
CN1980904A (zh) Cetp抑制剂
JP5876419B2 (ja) アリールベンジルアミン化合物
HK1107342A (en) Cetp inhibitors
JPWO2003106423A1 (ja) 環状アミン類およびそれを含む医薬組成物
HK1157767A (en) 4,5-dihydro-oxazol-2-yl derivatives
HK1143811A (en) Oxadiazolidinedione compound

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 KG MD TJ TM

PD4A Registration of transfer of a eurasian patent in accordance with the succession in title
PD4A Registration of transfer of a eurasian patent in accordance with the succession in title
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): BY KZ

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): RU