MD20160106A2 - Compuşi aril sau heteroaril biciclici condensaţi şi utilizarea acestora ca inhibitori IRAK4 - Google Patents

Compuşi aril sau heteroaril biciclici condensaţi şi utilizarea acestora ca inhibitori IRAK4 Download PDF

Info

Publication number
MD20160106A2
MD20160106A2 MDA20160106A MD20160106A MD20160106A2 MD 20160106 A2 MD20160106 A2 MD 20160106A2 MD A20160106 A MDA20160106 A MD A20160106A MD 20160106 A MD20160106 A MD 20160106A MD 20160106 A2 MD20160106 A2 MD 20160106A2
Authority
MD
Moldova
Prior art keywords
bicyclic
fused heteroaryl
aryl compounds
irak4 inhibitors
compounds
Prior art date
Application number
MDA20160106A
Other languages
English (en)
Russian (ru)
Other versions
MD4779B1 (ro
Inventor
Дэвид Рэндольф АНДЕРСОН
Марк Эдвард Баннэйдж
Кевин Джозеф КАРРАН
Кристоф Мартин Денхардт
Лори Крим Гаврин
Джоэль Адам ГОЛДБЕРГ
Сониль ХАН
Дэвид Хепуорт
Хонг-Чих ХУАН
Артур Ли
Кэтрин Линь ЛИ
Фрэнк Элдридж ЛАВРИНГ
Майкл Деннис ЛОУ
Джон Пол Матиас
Николаос Папаиоанну
Акшай ПАТНИ
Бетси Сьюзен ПИРС
Эддин САЯХ
Джозеф Уолтер Стробах
Джон Дэвид Трзупек
Ричард Варгас
Сяолунь Ван
Стивен Уэйн РАЙТ
Кристоф Вольфганг Запф
Original Assignee
Pfizer Inc.
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 Pfizer Inc. filed Critical Pfizer Inc.
Publication of MD20160106A2 publication Critical patent/MD20160106A2/ro
Publication of MD4779B1 publication Critical patent/MD4779B1/ro

Links

Classifications

    • 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
    • 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
    • A61K31/40—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
    • A61K31/435—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
    • 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
    • A61K31/4709—Non-condensed quinolines 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
    • A61K31/435—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
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/541—Non-condensed thiazines 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/66—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings being part of condensed ring systems and singly-bound oxygen atoms, bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C07C69/94—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of polycyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of six-membered aromatic rings
    • 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
    • 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
    • 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
    • C07D207/267—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
    • 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
    • C07D207/273—2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen 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
    • 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
    • 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
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • 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
    • C07D498/02—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 two hetero rings
    • C07D498/04—Ortho-condensed systems
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Prezenta invenţie se referă la compuşi, tautomeri şi săruri farmaceutic acceptabile ale compuşilor cu formula generală (Ia),(Ia)aşa cum sunt definiţi în cerere. De asemenea, sunt descrise compoziţii farmaceutice, metode de tratament, metode de sinteză şi intermediari corespunzători.
MDA20160106A 2014-04-04 2015-03-26 Compuşi aril sau heteroaril biciclici condensaţi şi utilizarea acestora ca inhibitori IRAK4 MD4779B1 (ro)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461975473P 2014-04-04 2014-04-04
PCT/IB2015/052251 WO2015150995A1 (en) 2014-04-04 2015-03-26 Bicyclic-fused heteroaryl or aryl compounds and their use as irak4 inhibitors

Publications (2)

Publication Number Publication Date
MD20160106A2 true MD20160106A2 (ro) 2017-03-31
MD4779B1 MD4779B1 (ro) 2021-12-31

Family

ID=52988358

Family Applications (1)

Application Number Title Priority Date Filing Date
MDA20160106A MD4779B1 (ro) 2014-04-04 2015-03-26 Compuşi aril sau heteroaril biciclici condensaţi şi utilizarea acestora ca inhibitori IRAK4

Country Status (46)

Country Link
US (6) US9458168B2 (ro)
EP (2) EP3126330B1 (ro)
JP (2) JP6177456B2 (ro)
KR (1) KR101901044B1 (ro)
CN (1) CN106458912B (ro)
AP (1) AP2016009514A0 (ro)
AR (1) AR099955A1 (ro)
AU (1) AU2015242291B2 (ro)
BR (1) BR112016023117B1 (ro)
CA (1) CA2944475C (ro)
CL (1) CL2016002524A1 (ro)
CR (1) CR20160456A (ro)
CU (1) CU24406B1 (ro)
CY (2) CY1121694T1 (ro)
DK (2) DK3126330T3 (ro)
DO (1) DOP2016000271A (ro)
EA (1) EA032559B1 (ro)
EC (1) ECSP16076566A (ro)
ES (2) ES2910128T3 (ro)
GE (1) GEP20186887B (ro)
GT (1) GT201600215A (ro)
HR (2) HRP20190506T1 (ro)
HU (2) HUE044180T2 (ro)
IL (1) IL248158B (ro)
LT (2) LT3126330T (ro)
MA (2) MA39838B1 (ro)
MD (1) MD4779B1 (ro)
ME (1) ME03599B (ro)
MX (1) MX374729B (ro)
MY (1) MY192521A (ro)
NI (1) NI201600152A (ro)
NZ (1) NZ724578A (ro)
PE (1) PE20161251A1 (ro)
PH (1) PH12016501972B1 (ro)
PL (2) PL3126330T3 (ro)
PT (2) PT3536685T (ro)
RS (2) RS58597B1 (ro)
SG (1) SG11201608110WA (ro)
SI (2) SI3126330T1 (ro)
SV (1) SV2016005295A (ro)
TR (1) TR201904658T4 (ro)
TW (3) TWI623530B (ro)
UA (1) UA121467C2 (ro)
UY (1) UY36056A (ro)
WO (1) WO2015150995A1 (ro)
ZA (1) ZA201606550B (ro)

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2538357T3 (es) 2005-04-11 2015-06-19 Crealta Pharmaceuticals Llc Formas variantes de urato oxidasa y uso de las mismas
US9377454B2 (en) 2009-06-25 2016-06-28 Crealta Pharmaceuticals Llc Methods and kits for predicting infusion reaction risk and antibody-mediated loss of response by monitoring serum uric acid during pegylated uricase therapy
KR20180099933A (ko) 2010-11-19 2018-09-05 리간드 파마슈티칼스 인코포레이티드 복소환 아민 및 이의 용도
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
DK3126330T3 (en) * 2014-04-04 2019-04-23 Pfizer BICYCLE-FUSED HETEROARYL OR ARYL COMPOUNDS AND USE THEREOF AS IRAC4 INHIBITORS
RU2692808C2 (ru) 2014-04-04 2019-06-27 Х. Лундбекк А/С Галогенированные хиназолин-thf-амины в качестве ингибиторов pde1
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
JP2018527337A (ja) 2015-08-13 2018-09-20 ファイザー・インク 二環式縮合ヘテロアリールまたはアリール化合物
WO2017033093A1 (en) 2015-08-27 2017-03-02 Pfizer Inc. Bicyclic-fused heteroaryl or aryl compounds as irak4 modulators
WO2018026877A1 (en) 2016-08-05 2018-02-08 Calitor Sciences, Llc Process for preparing substituted quinolin-4-ol compounds
US11542261B2 (en) 2016-08-17 2023-01-03 Children's Hospital Medical Center Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors
US11254667B2 (en) 2016-08-17 2022-02-22 Children's Hospital Medical Center Substituted imidazo[1,2-A]pyridines as IRAK 1/4 and flt3 inhibitors
CN117085013A (zh) * 2016-10-13 2023-11-21 特拉维尔治疗公司 用于治疗肾脏疾病或病症的联苯磺酰胺化合物
JP2019535819A (ja) 2016-11-11 2019-12-12 ホライゾン ファーマ リューマトロジー リミテッド ライアビリティ カンパニーＨｏｒｉｚｏｎ Ｐｈａｒｍａ Ｒｈｅｕｍａｔｏｌｏｇｙ Ｌｌｃ プレドニゾンおよびウリカーゼ分子の併用療法ならびにその使用
KR20180066296A (ko) * 2016-12-07 2018-06-19 서울대학교산학협력단 토파시티닙을 포함하는 고염증 증상의 예방 또는 치료용 약학적 조성물 및 토파시티닙을 포함하는 고염증 증상의 예방 또는 개선용 건강기능식품 조성물
EP4467565A3 (en) 2016-12-21 2025-03-12 Amgen Inc. Anti-tnf alpha antibody formulations
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
JP7154229B2 (ja) 2017-05-11 2022-10-17 ブリストル－マイヤーズ スクイブ カンパニー Ｉｒａｋ－４阻害剤として有用なチエノピリジンおよびベンゾチオフェン
CN107021960B (zh) * 2017-06-10 2018-07-31 上海普康药业有限公司 一种治疗恶性肿瘤的药物
GB201712282D0 (en) 2017-07-31 2017-09-13 Nodthera Ltd Selective inhibitors of NLRP3 inflammasome
CA3076613A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. Protein degraders and uses thereof
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
CN118063442A (zh) 2017-10-20 2024-05-24 范德比尔特大学 毒蕈碱性乙酰胆碱受体m4的拮抗剂
CA3083959C (en) * 2017-10-30 2023-09-26 Synblia Therapeutics, Inc. Irak4 inhibitors and uses thereof
KR20200081424A (ko) 2017-10-31 2020-07-07 반더빌트유니버시티 무스카린성 아세틸콜린 수용체 m4의 길항제
WO2019099926A1 (en) 2017-11-17 2019-05-23 Arvinas, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
US11485743B2 (en) 2018-01-12 2022-11-01 Kymera Therapeutics, Inc. Protein degraders and uses thereof
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
WO2019149522A1 (en) * 2018-01-31 2019-08-08 Merck Patent Gmbh Quinoline compounds as irak inhibitors and uses thereof
CN111788182B (zh) 2018-02-02 2023-09-26 范德堡大学 毒蕈碱性乙酰胆碱受体m4的拮抗剂
CN111712494A (zh) 2018-02-13 2020-09-25 吉利德科学公司 Pd-1/pd-l1抑制剂
AU2019220632B2 (en) * 2018-02-14 2024-02-22 Dana-Farber Cancer Institute, Inc. IRAK degraders and uses thereof
CN108299397B (zh) * 2018-03-21 2019-01-29 佳木斯大学附属第一医院 一种用于降血压的活性药物及其制备方法
EP4600247A3 (en) 2018-04-19 2025-11-19 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
EP3810144A4 (en) * 2018-06-04 2022-08-17 Chemistryrx Topical compositions for stimulating hair growth
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
TWI842978B (zh) 2018-07-13 2024-05-21 美商基利科學股份有限公司 衍生物
CN109147870A (zh) * 2018-07-26 2019-01-04 刘滨 基于条件随机场的固有无序蛋白质的识别方法
JP7169429B2 (ja) 2018-08-13 2022-11-10 ギリアード サイエンシーズ， インコーポレイテッド ＩＲＡＫ４阻害剤としてのピロロ［１，２－ｂ］ピリダジン誘導体
TWI727392B (zh) 2018-08-13 2021-05-11 美商基利科學股份有限公司 噻二唑irak4抑制劑
KR102659550B1 (ko) 2018-08-13 2024-04-23 길리애드 사이언시즈, 인코포레이티드 Irak4 억제제로서의 피롤로[1,2-b]피리다진 유도체
JP7623943B2 (ja) 2018-11-30 2025-01-29 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ分解剤およびそれらの使用
DE102018221954A1 (de) * 2018-12-17 2020-06-18 Robert Bosch Gmbh Recheneinrichtung und Verfahren zum Betreiben einer Recheneinrichtung
US12121566B2 (en) 2019-01-30 2024-10-22 Horizon Therapeutics Usa, Inc. Methods for treating gout
WO2020160325A1 (en) 2019-01-30 2020-08-06 Horizon Pharma Rheumatology Llc Reducing immunogenicity to pegloticase
CN111662295B (zh) * 2019-03-05 2021-09-10 珠海宇繁生物科技有限责任公司 一种irak4激酶抑制剂及其制备方法
KR102289661B1 (ko) * 2019-05-15 2021-08-17 가톨릭대학교 산학협력단 요산분해효소를 과발현하는 줄기세포를 유효성분으로 포함하는 통풍의 예방 또는 치료용 조성물
JP7570399B2 (ja) 2019-07-18 2024-10-21 ブリストル－マイヤーズ スクイブ カンパニー Ｉｒａｋ４阻害剤として有用な三環式ヘテロアリール化合物
EP3999512B1 (en) 2019-07-18 2023-08-23 Bristol-Myers Squibb Company Pyrazolo[3,4-d]pyrrolo[1,2-b]pyridazinyl compounds useful as irak4 inhibitors
KR20220041124A (ko) 2019-07-23 2022-03-31 브리스톨-마이어스 스큅 컴퍼니 Irak4 억제제로서 유용한 티에노피리디닐 및 티아졸로피리디닐 화합물
CN114616230A (zh) * 2019-07-31 2022-06-10 海洋生物技术与海洋资源有限公司 黄烷类似物化合物及其在治疗慢性和急性疼痛中的用途
ES2983263T3 (es) 2019-08-06 2024-10-22 Bristol Myers Squibb Co Compuestos heterocíclicos bicíclicos útiles como inhibidores de IRAK4
CN112679472A (zh) * 2019-10-17 2021-04-20 北京桦冠医药科技有限公司 具有irak4抑制剂活性的异喹啉类化合物
US20220378707A1 (en) * 2019-11-14 2022-12-01 Pfizer Inc. 1-(((2s,3s,4s)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl)methoxy)-7-methoxyisoquinoline-6-carboxamide combinations and oral dosage forms
US20210154292A1 (en) * 2019-11-21 2021-05-27 Chemocentryx, Inc. Compositions and Methods for Treating CCR9-Mediated Diseases using CCR9 Inhibitor and Anti-TNF-Alpha Blocking Antibodies
KR20220145325A (ko) 2019-12-17 2022-10-28 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
US11591332B2 (en) 2019-12-17 2023-02-28 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
CA3166527A1 (en) * 2020-01-29 2021-08-05 Charbel MOUSSA Compositions and methods for treating neurodegenerative, neurodevelopmental, myodegenerative, and lysosomal storage disorders
US12391702B2 (en) 2020-02-03 2025-08-19 Bristol-Myers Squibb Company Benzo[5,6][1,4]dioxino[2,3-b]pyridine compounds useful as IRAK4 inhibitors
US11618751B1 (en) 2022-03-25 2023-04-04 Ventus Therapeutics U.S., Inc. Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives
CN115715194A (zh) 2020-04-04 2023-02-24 辉瑞公司 治疗冠状病毒疾病2019的方法
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
KR20230084145A (ko) 2020-09-30 2023-06-12 아사히 가세이 파마 가부시키가이샤 피리미딘 함유 함질소 2환 화합물
WO2022070287A1 (ja) 2020-09-30 2022-04-07 旭化成ファーマ株式会社 マクロサイクル化合物
US11866405B2 (en) 2020-12-10 2024-01-09 Astrazeneca Ab Substituted indazoles as IRAK4 inhibitors
AR124547A1 (es) 2020-12-30 2023-04-05 Kymera Therapeutics Inc Degradadores de irak y sus usos
MX2023009527A (es) 2021-02-15 2023-08-24 Kymera Therapeutics Inc Degradadores de la cinasa 4 asociada al receptor de interleucina 1 (irak4) y usos de los mismos.
US11773103B2 (en) 2021-02-15 2023-10-03 Kymera Therapeutics, Inc. IRAK4 degraders and uses thereof
US11319319B1 (en) 2021-04-07 2022-05-03 Ventus Therapeutics U.S., Inc. Compounds for inhibiting NLRP3 and uses thereof
AR125798A1 (es) 2021-05-07 2023-08-16 Kymera Therapeutics Inc Degradadores cdk2 y usos de los mismos
EP4422635A4 (en) * 2021-10-29 2025-11-26 Kymera Therapeutics Inc IRAQ4 DEGRADATION AGENTS AND THEIR SYNTHESIS
CA3243560A1 (en) 2022-01-31 2023-08-03 Kymera Therapeutics, Inc. Iraqi Degradation Agents and Their Uses
CA3250704A1 (en) 2022-02-14 2023-08-17 Astrazeneca Ab IRAK4 INHIBITORS
US12459941B2 (en) 2022-03-31 2025-11-04 Rigel Pharmaceuticals, Inc. Tricyclic IRAK inhibitors
AU2023274390A1 (en) 2022-05-26 2025-01-02 Astrazeneca Ab Solid forms of heterocyclylamides as irak4 inhibitors
US20230391748A1 (en) * 2022-06-01 2023-12-07 Rigel Pharmaceuticals, Inc. Bicyclic inhibitors of irak
US12331048B2 (en) 2022-10-31 2025-06-17 Ventus Therapeutics U.S., Inc. Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 inhibitors
JP2025535830A (ja) 2022-11-04 2025-10-28 領泰生物医薬（紹興）有限公司 Ｉｒａｋ４分解剤及びその使用
WO2024194756A1 (en) 2023-03-17 2024-09-26 Pfizer Inc. Modulating the innate immunity of rna
US12269875B2 (en) 2023-08-03 2025-04-08 Jeff R. Peterson Gout flare prevention methods using IL-1BETA blockers
WO2025036841A1 (en) 2023-08-11 2025-02-20 Astrazeneca Ab Crystalline irak4 inhibitors
CN118978508B (zh) * 2024-08-02 2025-09-16 上海信诺维生物医药有限公司 一种含氮杂环化合物
CN120842197A (zh) * 2025-09-24 2025-10-28 上海市刑事科学技术研究院 一种羟基可替宁-d3的制备方法

Family Cites Families (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3673238A (en) * 1970-02-10 1972-06-27 Usv Pharma Corp 2-naphthoic acid derivatives
JPS528238B2 (ro) 1973-10-11 1977-03-08
DE3065190D1 (en) 1979-11-05 1983-11-10 Beecham Group Plc Enzyme derivatives, and their preparation
DE3882894T2 (de) 1987-10-20 1994-03-17 Mitsui Toatsu Chemicals 1,2-Naphtalocyanine, Infrarotabsorber und sie verwendende Aufzeichnungsmaterialien.
US4861795A (en) * 1988-06-23 1989-08-29 Rorer Pharmaceutical Corporation Treatment of conditions requiring enhanced oxygen availability to mammalian tissues
JP2671059B2 (ja) * 1990-11-30 1997-10-29 富士レビオ株式会社 ナフトエ酸誘導体
JPH05148222A (ja) 1991-11-29 1993-06-15 Fujirebio Inc ナフトエ酸誘導体
US5837689A (en) * 1993-06-16 1998-11-17 Glycomed Incorporated Sialyl lewis-x mimetics containing naphthyl backbones
AU686691B2 (en) 1994-01-12 1998-02-12 F. Hoffmann-La Roche Ag Novel azepanes and homologs thereof
US5612359A (en) 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
TR199600329A2 (tr) 1995-05-05 1997-03-21 Hoffmann La Roche Seker alkollerin yeni sülfürik asit esterleri.
GB9514265D0 (en) * 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
TW536540B (en) 1997-01-30 2003-06-11 Bristol Myers Squibb Co Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe
CN1149196C (zh) 1998-07-06 2004-05-12 布里斯托尔-迈尔斯斯奎布公司 作为血管紧张肽和内皮肽受体双重拮抗剂的联苯基磺酰胺
IL147280A0 (en) * 1999-07-07 2002-08-14 Astrazeneca Uk Ltd Quinazoline derivatives
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
HU230302B1 (hu) * 2000-10-20 2015-12-28 Eisai R&D Management Co., Ltd. Nitrogéntartalmú aromás származékok és ezeket tartalmazó gyógyászati készítmények
HRP20040716A2 (en) 2002-02-27 2005-02-28 Pfizer Products Inc. Acc inhibitors
WO2005080377A1 (ja) * 2004-02-20 2005-09-01 Kirin Beer Kabushiki Kaisha TGFβ阻害活性を有する化合物およびそれを含んでなる医薬組成物
HRP20090471T1 (hr) 2004-05-12 2009-10-31 Pfizer Products Inc. Derivati prolina i njihova upotreba kao inhibitori dipeptidil-peptidaze iv
ES2400371T3 (es) 2005-07-07 2013-04-09 Abbott Laboratories Promotores de la apoptosis
US7572809B2 (en) 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
EP2463283B1 (en) 2006-04-20 2014-06-11 Pfizer Products Inc. Fused phenyl Amido heterocyclic compounds for the prevention and treatment of glucokinase-mediated diseases
CN101541809A (zh) 2006-11-29 2009-09-23 辉瑞产品公司 螺环酮乙酰基-CoA羧化酶抑制剂
US9623021B2 (en) 2007-01-22 2017-04-18 Gtx, Inc. Nuclear receptor binding agents
CN103432133B (zh) 2007-01-22 2016-08-10 Gtx公司 核受体结合剂的用途
US20080200461A1 (en) 2007-02-20 2008-08-21 Cropsolution, Inc. Modulators of acetyl-coenzyme a carboxylase and methods of use thereof
US20090023773A1 (en) 2007-06-27 2009-01-22 Painceptor Pharma Corporation Compositions and methods for modulating gated ion channels
US20090036425A1 (en) 2007-08-02 2009-02-05 Pfizer Inc Substituted bicyclolactam compounds
CN101245022A (zh) * 2008-03-21 2008-08-20 东华大学 3,5-双(2,4-二氨基苯氧基)-2-萘甲酸的制备方法
ES2545231T3 (es) 2008-05-28 2015-09-09 Pfizer Inc. Inhibidores de pirazoloespirocetona acetil-CoA carboxilasa
EP2297164A1 (en) 2008-05-28 2011-03-23 Pfizer Inc. Pyrazolospiroketone acetyl-coa carboxylase inhibitors
DE102008027574A1 (de) 2008-06-10 2009-12-17 Merck Patent Gmbh Neue Pyrrolidinderivate als MetAP-2 Inhibitoren
CN101353307A (zh) * 2008-07-25 2009-01-28 东华大学 3,5-双(2,6-二硝基-4-三氟甲基苯氧基)-2-萘甲酸的制备方法
JP2011529483A (ja) 2008-07-29 2011-12-08 ファイザー・インク フッ素化ヘテロアリール
MX2011002166A (es) 2008-08-28 2011-04-07 Pfizer Derivados de dioxa-biciclo[3.2.1]octano-2,3,1-triol.
TW201038580A (en) 2009-02-02 2010-11-01 Pfizer 4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl derivatives
JP5086480B2 (ja) 2009-03-11 2012-11-28 ファイザー・インク グルコキナーゼ活性化剤として使用されるベンゾフラニル誘導体
CA2754685A1 (en) 2009-03-11 2010-09-16 Pfizer Inc. Substituted indazole amides
US20120095028A1 (en) 2009-03-20 2012-04-19 Pfizer Inc. 3-oxa-7-azabicyclo[3.3.1]nonanes
WO2010128414A1 (en) 2009-05-08 2010-11-11 Pfizer Inc. Gpr 119 modulators
CA2759843A1 (en) 2009-05-08 2010-11-10 Pfizer Inc. Gpr 119 modulators
NZ596467A (en) 2009-06-05 2014-01-31 Pfizer L- ( piperidin-4-yl) -pyrazole derivatives as gpr 119 modulators
WO2011005611A1 (en) 2009-07-09 2011-01-13 Merck Sharp & Dohme Corp. Neuromedin u receptor agonists and uses thereof
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
WO2011159781A2 (en) 2010-06-17 2011-12-22 Senomyx, Inc. Bitter taste modulators
MX336224B (es) 2011-07-26 2016-01-12 Boehringer Ingelheim Int Quinolinas sustituidas y su uso como medicamentos.
WO2013142390A1 (en) 2012-03-21 2013-09-26 Gtx, Inc. Aldo-keto reductase subfamily 1c3 (akr1c3) inhibitors
WO2014039820A1 (en) 2012-09-07 2014-03-13 Gtx, Inc. Aldo-keto reductase subfamily 1c3 (akr1c3) inhibitors
KR101750667B1 (ko) 2013-07-31 2017-07-04 길리애드 사이언시즈, 인코포레이티드 Syk 억제제
DK3126330T3 (en) 2014-04-04 2019-04-23 Pfizer BICYCLE-FUSED HETEROARYL OR ARYL COMPOUNDS AND USE THEREOF AS IRAC4 INHIBITORS
WO2017033093A1 (en) * 2015-08-27 2017-03-02 Pfizer Inc. Bicyclic-fused heteroaryl or aryl compounds as irak4 modulators

Also Published As

Publication number Publication date
KR20160135363A (ko) 2016-11-25
CR20160456A (es) 2016-12-01
US20150284405A1 (en) 2015-10-08
MX374729B (es) 2025-03-06
GT201600215A (es) 2018-10-19
CA2944475A1 (en) 2015-10-08
ECSP16076566A (es) 2017-03-31
JP6492128B2 (ja) 2019-03-27
SI3536685T1 (sl) 2022-05-31
US20160347760A1 (en) 2016-12-01
US11702424B2 (en) 2023-07-18
CN106458912A (zh) 2017-02-22
LT3536685T (lt) 2022-04-25
CY1125110T1 (el) 2024-02-16
EP3536685B1 (en) 2022-02-16
CL2016002524A1 (es) 2017-06-09
MA39838A (fr) 2017-02-08
BR112016023117A2 (ro) 2017-08-15
SV2016005295A (es) 2017-03-28
TWI593683B (zh) 2017-08-01
CN106458912B (zh) 2020-10-27
ME03599B (me) 2020-07-20
MA52856B1 (fr) 2022-03-31
EA201600622A1 (ru) 2017-02-28
JP2017206549A (ja) 2017-11-24
US20190270751A1 (en) 2019-09-05
GEP20186887B (en) 2018-08-27
JP6177456B2 (ja) 2017-08-09
PL3126330T3 (pl) 2019-09-30
HUE044180T2 (hu) 2019-10-28
EP3536685A1 (en) 2019-09-11
BR112016023117B1 (pt) 2023-02-07
TWI580678B (zh) 2017-05-01
HRP20220362T1 (hr) 2022-05-13
RS63024B1 (sr) 2022-04-29
HUE057876T2 (hu) 2022-06-28
ZA201606550B (en) 2018-05-30
LT3126330T (lt) 2019-04-25
WO2015150995A1 (en) 2015-10-08
TR201904658T4 (tr) 2019-04-22
MA39838B1 (fr) 2019-05-31
CU20160149A7 (es) 2017-04-05
US20230339960A1 (en) 2023-10-26
CY1121694T1 (el) 2020-07-31
MD4779B1 (ro) 2021-12-31
SI3126330T1 (sl) 2019-05-31
PE20161251A1 (es) 2016-11-30
MX2016013052A (es) 2017-01-09
TW201722931A (zh) 2017-07-01
PT3536685T (pt) 2022-03-28
US12202836B2 (en) 2025-01-21
UA121467C2 (uk) 2020-06-10
UY36056A (es) 2015-10-30
US10793579B2 (en) 2020-10-06
ES2718552T3 (es) 2019-07-02
HRP20190506T1 (hr) 2019-05-03
AR099955A1 (es) 2016-08-31
US9879022B2 (en) 2018-01-30
AP2016009514A0 (en) 2016-10-31
DOP2016000271A (es) 2017-04-16
MY192521A (en) 2022-08-25
CA2944475C (en) 2018-07-10
PT3126330T (pt) 2019-04-29
US9458168B2 (en) 2016-10-04
MA52856A (fr) 2021-04-21
PH12016501972A1 (en) 2016-12-19
CU24406B1 (es) 2019-05-03
TWI623530B (zh) 2018-05-11
KR101901044B1 (ko) 2018-09-20
SG11201608110WA (en) 2016-10-28
EA032559B1 (ru) 2019-06-28
AU2015242291B2 (en) 2018-08-30
EP3126330B1 (en) 2019-02-27
NZ724578A (en) 2019-05-31
JP2017512809A (ja) 2017-05-25
EP3126330A1 (en) 2017-02-08
IL248158B (en) 2018-06-28
RS58597B1 (sr) 2019-05-31
PH12016501972B1 (en) 2016-12-19
NI201600152A (es) 2016-11-18
US20180127432A1 (en) 2018-05-10
DK3536685T3 (da) 2022-03-07
DK3126330T3 (en) 2019-04-23
TW201630903A (zh) 2016-09-01
US10329302B2 (en) 2019-06-25
US20200377511A1 (en) 2020-12-03
PL3536685T3 (pl) 2022-05-16
ES2910128T3 (es) 2022-05-11
AU2015242291A1 (en) 2016-10-13
TW201540707A (zh) 2015-11-01

Similar Documents

Publication Publication Date Title
MD20160106A2 (ro) Compuşi aril sau heteroaril biciclici condensaţi şi utilizarea acestora ca inhibitori IRAK4
PH12016502382A1 (en) Substituted indazole compounds as irak4 inhibitors
PH12016501977A1 (en) 2-AMINO-6-METHYL-4,4a,5,6-TETRAHYDROPYRANO[3,4-d][1,3]THIAZIN-8a(8H)-YL-1,3-THIAZOL-4-YL AMIDES
PH12017500408A1 (en) Heteroaryl compunds as btk inhibitors and uses thereof
PH12017501191A1 (en) Quinazoline derivatives used to treat hiv
EA201650031A1 (ru) Производные пирролидин-2,5-диона, фармацевтические композиции и способы применения в качестве ингибиторов ido1
MD20170016A2 (ro) Compuşi aminopirimidinici ca inhibitori JAK
MY197698A (en) Oxysterols and methods of use thereof
EA201790246A1 (ru) Гетероциклические карбоновые кислоты в качестве активаторов растворимой гуанилатциклазы
MA40171A (fr) Dérivés d'azamophinan et leur utilisation
PH12016501462A1 (en) Neprilysin inhibitors
TN2017000485A1 (en) Tricyclic compounds and their use as phosphodiesterase inhibitors
PH12017500095A1 (en) Imidazopyridazine compounds
MX2018001992A (es) Compuestos triciclicos heterociclicos como inhibidores de fosfoinositol 3-quinasa.
PH12017500089B1 (en) Aldosterone synthase inhibitors
PH12017500595B1 (en) Aldosterone synthase inhibitors
PH12016502480A1 (en) Compounds, pharmaceutical composition and their use in treating neurodegenerative diseases

Legal Events

Date Code Title Description
KA4A Patent for invention lapsed due to non-payment of fees (with right of restoration)