EA201990657A1 - Соединения и композиции в качестве ингибиторов эндосомальных toll-подобных рецепторов - Google Patents

Соединения и композиции в качестве ингибиторов эндосомальных toll-подобных рецепторов

Info

Publication number
EA201990657A1
EA201990657A1 EA201990657A EA201990657A EA201990657A1 EA 201990657 A1 EA201990657 A1 EA 201990657A1 EA 201990657 A EA201990657 A EA 201990657A EA 201990657 A EA201990657 A EA 201990657A EA 201990657 A1 EA201990657 A1 EA 201990657A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
compositions
receptor inhibitors
endosomal toll
endosomal
Prior art date
Application number
EA201990657A
Other languages
English (en)
Other versions
EA036880B1 (ru
Inventor
Филипп Алпер
Джонатан Дин
Сунчунь Цзян
Тао Цзян
Томас Кнепфель
Пьер-Ив Мишелли
Даниел Матник
Вэй Пэй
Питер Сайка
Гобао Чжан
И Чжан
Original Assignee
Новартис Аг
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 Новартис Аг filed Critical Новартис Аг
Publication of EA201990657A1 publication Critical patent/EA201990657A1/ru
Publication of EA036880B1 publication Critical patent/EA036880B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • C07D491/10—Spiro-condensed systems

Abstract

Настоящее изобретение, раскрытое в данном документе, относится к 4,5,6,7-тетрагидро-1H-пиразоло[4,3-c]пиридинильным соединениям и 4,5,6,7-тетрагидро-2H-пиразоло[4,3-c]пиридинильным соединениям формулы (A), фармацевтическим композициям, содержащим такие соединения, и применению таких соединений в лечении аутоиммунных заболеваний.
EA201990657A 2016-09-09 2017-09-06 Соединения и композиции в качестве ингибиторов эндосомальных toll–подобных рецепторов EA036880B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662385726P 2016-09-09 2016-09-09
PCT/IB2017/055375 WO2018047081A1 (en) 2016-09-09 2017-09-06 Compounds and compositions as inhibitors of endosomal toll-like receptors

Publications (2)

Publication Number Publication Date
EA201990657A1 true EA201990657A1 (ru) 2019-07-31
EA036880B1 EA036880B1 (ru) 2020-12-30

Family

ID=60001955

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201990657A EA036880B1 (ru) 2016-09-09 2017-09-06 Соединения и композиции в качестве ингибиторов эндосомальных toll–подобных рецепторов

Country Status (36)

Country Link
US (2) US10954233B2 (ru)
EP (2) EP4059934A1 (ru)
JP (1) JP6779371B2 (ru)
KR (2) KR20190039809A (ru)
CN (2) CN109641899B (ru)
AU (1) AU2017323584C1 (ru)
BR (1) BR112019004597A2 (ru)
CA (1) CA3031585A1 (ru)
CL (1) CL2019000588A1 (ru)
CO (1) CO2019003397A2 (ru)
CR (1) CR20190119A (ru)
CU (1) CU24526B1 (ru)
CY (1) CY1125007T1 (ru)
DK (1) DK3510033T3 (ru)
DO (1) DOP2019000055A (ru)
EA (1) EA036880B1 (ru)
EC (1) ECSP19024046A (ru)
ES (1) ES2905981T3 (ru)
HR (1) HRP20220144T1 (ru)
HU (1) HUE057254T2 (ru)
IL (1) IL265159B (ru)
JO (1) JOP20190041B1 (ru)
LT (1) LT3510033T (ru)
MA (1) MA46196A (ru)
MX (1) MX2019002797A (ru)
MY (1) MY194813A (ru)
PE (1) PE20190732A1 (ru)
PH (1) PH12019500161A1 (ru)
PL (1) PL3510033T3 (ru)
PT (1) PT3510033T (ru)
RS (1) RS62913B1 (ru)
RU (1) RU2759678C2 (ru)
SG (1) SG11201900482SA (ru)
SI (1) SI3510033T1 (ru)
WO (1) WO2018047081A1 (ru)
ZA (1) ZA201900227B (ru)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE063437T2 (hu) 2013-09-24 2024-01-28 Fujifilm Corp Nitrogént tartalmazó vegyületet vagy sóját vagy fémkomplexét tartalmazó gyógyászati készítmény
WO2018009916A1 (en) 2016-07-07 2018-01-11 The Board Of Trustees Of The Leland Stanford Junior University Antibody adjuvant conjugates
EP4059934A1 (en) 2016-09-09 2022-09-21 Novartis AG Compounds and compositions as inhibitors of endosomal toll-like receptors
MA46535A (fr) 2016-10-14 2019-08-21 Prec Biosciences Inc Méganucléases modifiées spécifiques de séquences de reconnaissance dans le génome du virus de l'hépatite b
WO2019123340A1 (en) 2017-12-20 2019-06-27 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
CA3084582A1 (en) 2017-12-20 2019-06-27 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
JP2021507889A (ja) 2017-12-22 2021-02-25 ノバルティス アーゲー ピラゾロピペリジン誘導体の新規な使用
JP7328977B2 (ja) 2018-02-12 2023-08-17 エフ． ホフマン－ラ ロシュ アーゲー ウイルス感染の処置および予防のための新規のスルホン化合物および誘導体
EP3759109B1 (en) 2018-02-26 2023-08-30 Gilead Sciences, Inc. Substituted pyrrolizine compounds as hbv replication inhibitors
WO2019195181A1 (en) 2018-04-05 2019-10-10 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis b virus protein x
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
JP7296398B2 (ja) 2018-04-06 2023-06-22 インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエスシーアール，ヴイ．ヴイ．アイ． ３’３’－環状ジヌクレオチド
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 ２，２，─環二核苷酸
TW201945388A (zh) 2018-04-12 2019-12-01 美商精密生物科學公司 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶
US20190359645A1 (en) 2018-05-03 2019-11-28 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotides comprising carbocyclic nucleotide
AU2019268583B2 (en) * 2018-05-18 2022-01-27 Novartis Ag Crystalline forms of a TLR7/TLR8 inhibitor
CN112313228A (zh) 2018-06-12 2021-02-02 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的新型杂芳基杂环基化合物
US11952363B2 (en) 2018-07-23 2024-04-09 Hoffmann-La Roche Inc. Piperazine compounds for the treatment of autoimmune disease
WO2020028097A1 (en) 2018-08-01 2020-02-06 Gilead Sciences, Inc. Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid
WO2020048583A1 (en) 2018-09-04 2020-03-12 F. Hoffmann-La Roche Ag Benzothiazole compounds for the treatment of autoimmune diseases
EP3847170B1 (en) 2018-09-06 2022-06-22 F. Hoffmann-La Roche AG Novel cyclic amidine compounds for the treatment of autoimmune disease
JP2022501326A (ja) * 2018-09-07 2022-01-06 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 自己免疫疾患の治療のための新規ピロリジンアミン化合物
US11203591B2 (en) 2018-10-31 2021-12-21 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
US20220143061A1 (en) 2019-03-07 2022-05-12 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
EP3934757B1 (en) 2019-03-07 2023-02-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 2'3'-cyclic dinucleotides and prodrugs thereof
EP3935065A1 (en) 2019-03-07 2022-01-12 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
WO2020190725A1 (en) 2019-03-15 2020-09-24 Bolt Biotherapeutics, Inc. Immunoconjugates targeting her2
TW202210480A (zh) 2019-04-17 2022-03-16 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TWI751517B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
WO2020240272A1 (en) * 2019-05-31 2020-12-03 Dr.Reddy's Institute Of Life Sciences Preparation of novel 1 h-pyrazolo[4,3-d]pyrimidines, their compositions, synthesis and methods of using them for treating tuberculosis
WO2021034804A1 (en) 2019-08-19 2021-02-25 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
CR20220129A (es) 2019-09-30 2022-05-06 Gilead Sciences Inc Vacunas para vhb y métodos de tratamiento de vhb
US20230031465A1 (en) 2019-12-06 2023-02-02 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome
CA3169348A1 (en) 2020-03-20 2021-09-23 Gilead Sciences, Inc. Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same
EP4182032A1 (en) 2020-07-14 2023-05-24 F. Hoffmann-La Roche AG Hydroisoquinoline or hydronaphthyridine compounds for the treatment of autoimmune disease
CA3214808A1 (en) 2021-04-16 2022-10-20 Gilead Sciences, Inc. Thienopyrrole compounds
TW202310852A (zh) 2021-05-13 2023-03-16 美商基利科學股份有限公司 ＴＬＲ８調節化合物及抗ＨＢＶ ｓｉＲＮＡ療法之組合
CA3220923A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
US11976072B2 (en) 2021-06-23 2024-05-07 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
AU2022298639A1 (en) 2021-06-23 2023-12-07 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
US11926628B2 (en) 2021-06-23 2024-03-12 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
WO2023046806A1 (en) 2021-09-24 2023-03-30 F. Hoffmann-La Roche Ag Pyrazolo[3,4-b]pyridine compounds for the treatment of autoimmune disease
TW202337443A (zh) 2022-01-11 2023-10-01 瑞士商諾華公司 使用ｔｌｒ７／８拮抗劑治療ｓｊｏｇｒｅｎ氏症候群或混合性結締組織病之方法

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA006381B1 (ru) 2000-08-10 2005-12-29 Фармация Италия С.П.А. Бициклопиразолы, активные в качестве ингибиторов киназы, способ их получения и включающие их фармацевтические композиции
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
MXPA05009719A (es) 2003-03-11 2005-10-18 Pharmacia Italia Spa Derivados de biciclo-pirazol activos como inhibidores de cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden.
CA2585925C (en) 2004-10-27 2014-04-22 Janssen Pharmaceutica, N.V. Tetrahydro-pyridinyl pyrazole cannabinoid modulators
US20070093515A1 (en) * 2005-08-16 2007-04-26 Arrington Mark P Phosphodiesterase 10 inhibitors
US20090118263A1 (en) * 2005-09-22 2009-05-07 Dainippon Sumitomo Pharma Co., Ltd. Novel Adenine Compound
US20070254913A1 (en) 2006-04-19 2007-11-01 Dunn Robert F Phosphodiesterase 4 inhibitors
ES2388315T3 (es) 2007-05-04 2012-10-11 Bristol-Myers Squibb Company Agonistas [6,5]-bicíclicos de receptores GPR119 acoplados a la proteína G
TW200924762A (en) * 2007-11-02 2009-06-16 Vertex Pharma Kinase inhibitors
EP2467380B1 (en) 2009-08-18 2016-11-30 Ventirx Pharmaceuticals, Inc. Substituted benzoazepines as toll-like receptor modulators
JP5694345B2 (ja) * 2009-10-22 2015-04-01 ギリアード サイエンシーズ， インコーポレイテッド Ｔｏｌｌ様受容体の調節因子
WO2011115804A1 (en) 2010-03-17 2011-09-22 Ironwood Pharmaceuticals, Inc. Sgc stimulators
WO2012068450A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2012154608A1 (en) 2011-05-06 2012-11-15 Intellikine, Llc Reactive mtor and pi3 kinase inhibitors and uses thereof
WO2013003383A1 (en) 2011-06-27 2013-01-03 Kyorin Pharmaceutical Co., Ltd. Bridged bicyclic compounds for the treatment of bacterial infections
AU2013218072B2 (en) * 2012-02-08 2017-08-31 Janssen Sciences Ireland Uc Piperidino-pyrimidine derivatives for the treatment of viral infections
JO3407B1 (ar) * 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
JPWO2014034719A1 (ja) 2012-08-29 2016-08-08 興和株式会社 Ｔｌｒ阻害作用を有するキノリン誘導体
HUE037064T2 (hu) 2012-10-10 2018-08-28 Janssen Sciences Ireland Uc Pirrolo[3,2-d]-pirimidin származékok vírusos fertõzések és egyéb betegségek kezelésére
MX2015009270A (es) 2013-01-18 2015-10-30 Hoffmann La Roche Pirazoles sustituidos en posicion 3 y uso de los mismos como inhibidores de la cinasa cremallera de leucinas dual (dlk).
SG11201506800YA (en) 2013-03-14 2015-09-29 Bristol Myers Squibb Co Bicyclo [2.2.2] acid gpr120 modulators
CA2910759C (en) 2013-05-02 2018-01-16 Pfizer Inc. Imidazo-triazine derivatives as pde10 inhibitors
US10471139B2 (en) * 2013-08-15 2019-11-12 The University Of Kansas Toll-like receptor agonists
WO2015024011A2 (en) 2013-08-16 2015-02-19 Duke University Antibacterial compounds
SG11201601199QA (en) 2013-08-19 2016-03-30 Univ Kingston Carbene-functionalized composite materials
JP2016533385A (ja) 2013-08-22 2016-10-27 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ アルキニルアルコール及び使用方法
WO2015036044A1 (en) 2013-09-13 2015-03-19 Telormedix Sa Cationic lipid vehicles for delivery of tlr7 agonists for specific targeting of human cd14+ monocytes in whole blood
CN105636945B (zh) 2013-10-14 2017-11-17 卫材R&D管理有限公司 选择性取代的喹啉化合物
AU2014334554B2 (en) * 2013-10-14 2018-12-06 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
WO2016004272A1 (en) * 2014-07-02 2016-01-07 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
SG11201701169XA (en) 2014-08-15 2017-03-30 Chia Tai Tianqing Pharmaceutical Group Co Ltd Pyrrolopyrimidine compounds used as tlr7 agonist
ES2746839T3 (es) * 2014-12-18 2020-03-09 Pfizer Derivados de pirimidina y triazina y su uso como inhibidores de AXL
AU2015373996B2 (en) 2014-12-30 2020-10-08 Novira Therapeutics, Inc. Derivatives and methods of treating hepatitis B infections
WO2016128908A1 (en) 2015-02-12 2016-08-18 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
WO2016142867A1 (en) 2015-03-12 2016-09-15 Novartis Ag Heterocyclic compounds and methods for their use
JP6919977B2 (ja) 2016-03-16 2021-08-18 クラ オンコロジー，インク． メニン−ｍｌｌの置換された阻害剤及びその使用方法
EP4059934A1 (en) 2016-09-09 2022-09-21 Novartis AG Compounds and compositions as inhibitors of endosomal toll-like receptors

Also Published As

Publication number Publication date
EA036880B1 (ru) 2020-12-30
IL265159B (en) 2021-08-31
KR102411532B1 (ko) 2022-06-22
CO2019003397A2 (es) 2019-06-19
SI3510033T1 (sl) 2022-04-29
RU2019110157A3 (ru) 2020-10-30
CU24526B1 (es) 2021-06-08
MX2019002797A (es) 2019-05-09
CN115215886A (zh) 2022-10-21
SG11201900482SA (en) 2019-03-28
PH12019500161A1 (en) 2019-10-28
CY1125007T1 (el) 2023-01-05
JOP20190041A1 (ar) 2019-03-10
US10954233B2 (en) 2021-03-23
IL265159A (en) 2019-05-30
BR112019004597A2 (pt) 2019-06-11
CU20190018A7 (es) 2019-10-04
MA46196A (fr) 2021-05-19
PL3510033T3 (pl) 2022-03-07
CL2019000588A1 (es) 2019-05-10
ES2905981T3 (es) 2022-04-12
JOP20190041B1 (ar) 2023-03-28
CN109641899B (zh) 2022-07-22
EP4059934A1 (en) 2022-09-21
RU2759678C2 (ru) 2021-11-16
US20190211009A1 (en) 2019-07-11
MY194813A (en) 2022-12-16
CA3031585A1 (en) 2018-03-15
HRP20220144T1 (hr) 2022-04-15
DOP2019000055A (es) 2019-05-31
AU2017323584A1 (en) 2019-01-31
KR20190039809A (ko) 2019-04-15
US20210101902A1 (en) 2021-04-08
CR20190119A (es) 2019-06-03
AU2017323584C1 (en) 2020-09-17
LT3510033T (lt) 2022-02-25
JP6779371B2 (ja) 2020-11-04
RU2019110157A (ru) 2020-10-09
PT3510033T (pt) 2022-02-18
EP3510033B1 (en) 2021-11-24
AU2017323584B2 (en) 2020-03-05
HUE057254T2 (hu) 2022-04-28
EP3510033A1 (en) 2019-07-17
ECSP19024046A (es) 2019-04-30
JP2019531280A (ja) 2019-10-31
DK3510033T3 (da) 2022-02-28
PE20190732A1 (es) 2019-05-23
ZA201900227B (en) 2019-10-30
WO2018047081A1 (en) 2018-03-15
KR20210077014A (ko) 2021-06-24
CN109641899A (zh) 2019-04-16
RS62913B1 (sr) 2022-03-31

Similar Documents

Publication Publication Date Title
EA201990657A1 (ru) Соединения и композиции в качестве ингибиторов эндосомальных toll-подобных рецепторов
EA202091508A1 (ru) 6-азаиндольные соединения
MY196474A (en) [1,2,4]Triazolo[1,5-A]Pyridinyl Substituted Indole Compounds
EA201990169A1 (ru) Диметоксифенилзамещенные соединения индола в качестве ингибиторов tlr7, tlr8 или tlr9
PH12016501570A1 (en) Bicyclic aza compounds as muscarinic m1 receptor and/or m4 receptor agonists
EA202091483A1 (ru) Амидзамещенные индольные соединения, пригодные в качестве ингибиторов tlr
PH12018500259A1 (en) Muscarinic agonists
PH12016501966A1 (en) Compounds and compositions as toll-like receptor 7 agonists
EA202091484A1 (ru) 4-азаиндольные соединения
EA202091530A1 (ru) Диазаиндольные соединения
NZ724878A (en) Compounds and compositions as toll-like receptor 7 agonists
PH12016501791A1 (en) Muscarinic receptor agonists
EA202091480A1 (ru) Аминоиндольные соединения, пригодные в качестве ингибиторов tlr
EA201691674A1 (ru) 1,2-замещенные циклопентаны в качестве антагонистов рецептора орексина
EA202091477A1 (ru) Замещенные соединения простых индольных эфиров
EA201792057A1 (ru) Конденсированные бициклические гетероарильные производные с активностью ингибиторов пролилгидроксилазы
EA201790179A1 (ru) [1,2,4]триазоло[4,3-b]пиридазины для применения в лечении пролиферативных заболеваний
EA201692227A1 (ru) Производные сложных аминоэфиров
MX2016015959A (es) Derivados de carbamato los cuales son tanto inhibidores de la enzima fosfodiesterasa 4 (pde4) como antagonistas del receptor muscarinico m3.
EA201790795A1 (ru) СОЕДИНЕНИЯ 4Н-ПИРИДО[1,2-a]ПИРИМИДИН-4-ОНА
GB2519470A (en) Bicyclic aza compounds as muscarinic M1 receptor agonists
UY37619A (es) Compuestos y composiciones como inhibidores de los receptores endosomales tipo peaje

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): AZ KG TJ TM