CN112119078A - Tlr7/tlr8抑制剂的晶型 - Google Patents

Tlr7/tlr8抑制剂的晶型 Download PDF

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Publication number
CN112119078A
CN112119078A CN201980032642.0A CN201980032642A CN112119078A CN 112119078 A CN112119078 A CN 112119078A CN 201980032642 A CN201980032642 A CN 201980032642A CN 112119078 A CN112119078 A CN 112119078A
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China
Prior art keywords
degrees
crystalline form
methyl
pyridin
pyrazolo
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Pending
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CN201980032642.0A
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English (en)
Chinese (zh)
Inventor
N·比厄里
A·柯迪考斯基
李斌
P·卢斯滕贝格尔
R·拉莫斯
V·塞图拉曼
张思思
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Novartis AG
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Novartis AG
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Publication of CN112119078A publication Critical patent/CN112119078A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/41—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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • A61K31/4353—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Steroid Compounds (AREA)
CN201980032642.0A 2018-05-18 2019-05-16 Tlr7/tlr8抑制剂的晶型 Pending CN112119078A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2018/087448 2018-05-18
CN2018087448 2018-05-18
PCT/IB2019/054066 WO2019220390A1 (en) 2018-05-18 2019-05-16 Crystalline forms of a tlr7/tlr8 inhibitor

Publications (1)

Publication Number Publication Date
CN112119078A true CN112119078A (zh) 2020-12-22

Family

ID=67145832

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980032642.0A Pending CN112119078A (zh) 2018-05-18 2019-05-16 Tlr7/tlr8抑制剂的晶型

Country Status (13)

Country Link
US (2) US12084460B2 (https=)
EP (1) EP3793998A1 (https=)
JP (2) JP7407740B2 (https=)
KR (1) KR20210013554A (https=)
CN (1) CN112119078A (https=)
AR (1) AR117573A1 (https=)
AU (1) AU2019268583B2 (https=)
BR (1) BR112020022738A2 (https=)
CA (1) CA3097312A1 (https=)
CL (1) CL2020002967A1 (https=)
MX (2) MX2020012259A (https=)
TW (2) TW202417000A (https=)
WO (1) WO2019220390A1 (https=)

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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
KR20210018818A (ko) 2018-06-05 2021-02-18 에프. 호프만-라 로슈 아게 자가면역 질환의 치료를 위한 테트라하이드로-1H-피라지노[2,1-a]이소인돌릴퀴놀린 화합물
EP3807270B1 (en) 2018-06-12 2023-09-13 F. Hoffmann-La Roche AG Novel heteroaryl heterocyclyl compounds for the treatment of autoimmune disease
US11952363B2 (en) 2018-07-23 2024-04-09 Hoffmann-La Roche Inc. Piperazine compounds for the treatment of autoimmune disease
WO2020048583A1 (en) 2018-09-04 2020-03-12 F. Hoffmann-La Roche Ag Benzothiazole compounds for the treatment of autoimmune diseases
WO2020048595A1 (en) 2018-09-06 2020-03-12 F. Hoffmann-La Roche Ag Novel cyclic amidine compounds for the treatment of autoimmune disease
JP7367004B2 (ja) 2018-09-06 2023-10-23 エフ． ホフマン－ラ ロシュ アーゲー 自己免疫疾患の処置のための新規のピラゾロビリジン化合物
US12421240B2 (en) 2019-10-31 2025-09-23 Hoffmann-La Roche Inc. Hydropyrazino[1,2-d][1,4]diazepine compounds for the treatment of autoimmune disease
JP2023502087A (ja) 2019-11-19 2023-01-20 エフ．ホフマン－ラ ロシュ アーゲー 自己免疫疾患の処置のためのヒドロ－１Ｈ－ピロロ［１，２－ａ］ピラジン化合物
JP7649306B2 (ja) 2019-11-20 2025-03-19 エフ． ホフマン－ラ ロシュ アーゲー 自己免疫疾患の処置のためのスピロ（イソベンゾフラナゼチジン）化合物
WO2022013136A1 (en) 2020-07-14 2022-01-20 F. Hoffmann-La Roche Ag Hydroisoquinoline or hydronaphthyridine compounds for the treatment of autoimmune disease
KR20230171469A (ko) 2021-04-16 2023-12-20 길리애드 사이언시즈, 인코포레이티드 티에노피롤 화합물
EP4398989A1 (en) 2021-09-10 2024-07-17 Gilead Sciences, Inc. Thienopyrrole compounds
AU2022351495A1 (en) 2021-09-24 2024-02-01 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

Citations (1)

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WO2018047081A1 (en) * 2016-09-09 2018-03-15 Novartis Ag Compounds and compositions as inhibitors of endosomal toll-like receptors

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MX2008002207A (es) 2005-08-16 2008-03-27 Memory Pharm Corp Inhibidores de fosfodiesterasa 10.
ES2637113T3 (es) 2011-01-10 2017-10-10 Infinity Pharmaceuticals, Inc. Procedimientos para preparar isoquinolinonas y formas sólidas de isoquinolinonas
SG11201404743TA (en) 2012-02-08 2014-09-26 Janssen R & D Ireland Piperidino-pyrimidine derivatives for the treatment of viral infections
KR101810798B1 (ko) 2013-07-30 2017-12-19 질레드 코네티컷 인코포레이티드 Ｓｙｋ 억제제의 다형체
EA037366B1 (ru) 2015-08-25 2021-03-18 Бейджин, Лтд. Способ получения ингибитора parp, кристаллические формы и их применения
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WO2018047081A1 (en) * 2016-09-09 2018-03-15 Novartis Ag Compounds and compositions as inhibitors of endosomal toll-like receptors

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TW202417000A (zh) 2024-05-01
AR117573A1 (es) 2021-08-18
JP2021523918A (ja) 2021-09-09
WO2019220390A1 (en) 2019-11-21
AU2019268583A1 (en) 2020-10-29
MX2023013584A (es) 2023-11-30
US12084460B2 (en) 2024-09-10
TWI826446B (zh) 2023-12-21
CA3097312A1 (en) 2019-11-21
EP3793998A1 (en) 2021-03-24
MX2020012259A (es) 2021-01-29
AU2019268583B2 (en) 2022-01-27
BR112020022738A2 (pt) 2021-02-02
JP2024037930A (ja) 2024-03-19
TW202015698A (zh) 2020-05-01
CL2020002967A1 (es) 2021-04-30
JP7407740B2 (ja) 2024-01-04
US20210206783A1 (en) 2021-07-08
US20240391938A1 (en) 2024-11-28
KR20210013554A (ko) 2021-02-04

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