TW202417000A - Tlr7/tlr8抑制劑之晶型 - Google Patents
Tlr7/tlr8抑制劑之晶型 Download PDFInfo
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- TW202417000A TW202417000A TW112150642A TW112150642A TW202417000A TW 202417000 A TW202417000 A TW 202417000A TW 112150642 A TW112150642 A TW 112150642A TW 112150642 A TW112150642 A TW 112150642A TW 202417000 A TW202417000 A TW 202417000A
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- methyl
- pyridin
- pyrazolo
- crystalline form
- octan
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- 230000003595 spectral effect Effects 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000000859 sublimation Methods 0.000 description 1
- 230000008022 sublimation Effects 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 229960001940 sulfasalazine Drugs 0.000 description 1
- NCEXYHBECQHGNR-QZQOTICOSA-N sulfasalazine Chemical compound C1=C(O)C(C(=O)O)=CC(\N=N\C=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-QZQOTICOSA-N 0.000 description 1
- NCEXYHBECQHGNR-UHFFFAOYSA-N sulfasalazine Natural products C1=C(O)C(C(=O)O)=CC(N=NC=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-UHFFFAOYSA-N 0.000 description 1
- MLKXDPUZXIRXEP-MFOYZWKCSA-N sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 description 1
- 229960000894 sulindac Drugs 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 206010043207 temporal arteritis Diseases 0.000 description 1
- LZNWYQJJBLGYLT-UHFFFAOYSA-N tenoxicam Chemical compound OC=1C=2SC=CC=2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 LZNWYQJJBLGYLT-UHFFFAOYSA-N 0.000 description 1
- 229960002871 tenoxicam Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 238000002076 thermal analysis method Methods 0.000 description 1
- 229960001017 tolmetin Drugs 0.000 description 1
- UPSPUYADGBWSHF-UHFFFAOYSA-N tolmetin Chemical compound C1=CC(C)=CC=C1C(=O)C1=CC=C(CC(O)=O)N1C UPSPUYADGBWSHF-UHFFFAOYSA-N 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 208000006961 tropical spastic paraparesis Diseases 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- 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
Landscapes
- 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)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2018087448 | 2018-05-18 | ||
| WOPCT/CN2018/087448 | 2018-05-18 |
Publications (1)
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| TW202417000A true TW202417000A (zh) | 2024-05-01 |
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| TW112150642A TW202417000A (zh) | 2018-05-18 | 2019-05-16 | Tlr7/tlr8抑制劑之晶型 |
| TW108116864A TWI826446B (zh) | 2018-05-18 | 2019-05-16 | Tlr7/tlr8抑制劑之晶型 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
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| TW108116864A TWI826446B (zh) | 2018-05-18 | 2019-05-16 | Tlr7/tlr8抑制劑之晶型 |
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| US (2) | US12084460B2 (enExample) |
| EP (1) | EP3793998A1 (enExample) |
| JP (2) | JP7407740B2 (enExample) |
| KR (1) | KR20210013554A (enExample) |
| CN (1) | CN112119078A (enExample) |
| AR (1) | AR117573A1 (enExample) |
| AU (1) | AU2019268583B2 (enExample) |
| BR (1) | BR112020022738A2 (enExample) |
| CA (1) | CA3097312A1 (enExample) |
| CL (1) | CL2020002967A1 (enExample) |
| MX (2) | MX2020012259A (enExample) |
| TW (2) | TW202417000A (enExample) |
| WO (1) | WO2019220390A1 (enExample) |
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| WO2019155042A1 (en) | 2018-02-12 | 2019-08-15 | F. Hoffmann-La Roche Ag | Novel sulfone compounds and derivatives for the treatment and prophylaxis of virus infection |
| US12157746B2 (en) | 2018-06-05 | 2024-12-03 | Hoffmann-La Roche Inc. | Tetrahydro-1H-pyrazino[2,1-a]isoindolylquinoline compounds for the treatment of autoimmune disease |
| 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 |
| CN112638908A (zh) | 2018-09-04 | 2021-04-09 | 豪夫迈·罗氏有限公司 | 用于治疗自身免疫性疾病的苯并噻唑类化合物 |
| WO2020048596A1 (en) | 2018-09-06 | 2020-03-12 | F. Hoffmann-La Roche Ag | Novel pyrazolopyridine compounds for the treatment of autoimmune disease |
| EP3847170B1 (en) | 2018-09-06 | 2022-06-22 | F. Hoffmann-La Roche AG | Novel cyclic amidine compounds for the treatment of autoimmune disease |
| CN114599652B (zh) | 2019-10-31 | 2024-07-12 | 豪夫迈·罗氏有限公司 | 用于治疗自身免疫性疾病的氢吡嗪并[1,2-d][1,4]二氮杂䓬化合物 |
| EP4061816A1 (en) | 2019-11-19 | 2022-09-28 | F. Hoffmann-La Roche AG | Hydro-1h-pyrrolo[1,2-a]pyrazine compounds for the treatment of autoimmune disease |
| EP4061821B1 (en) | 2019-11-20 | 2025-08-06 | F. Hoffmann-La Roche AG | Spiro(isobenzofuranazetidine) compounds for the treatment of autoimmune disease |
| JP2023533807A (ja) | 2020-07-14 | 2023-08-04 | 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イソキノリン又はヒドロナフチリジン化合物 |
| US11661431B2 (en) | 2021-04-16 | 2023-05-30 | Gilead Sciences, Inc. | Thienopyrrole compounds |
| TW202440078A (zh) | 2021-09-10 | 2024-10-16 | 美商基利科學股份有限公司 | 噻吩并吡咯化合物 |
| PE20250401A1 (es) * | 2021-09-24 | 2025-02-11 | Hoffmann La Roche | Compuestos de pirazolo[3,4-b]piridina para el tratamiento de enfermedades auto/inmunitarias |
| AU2023207313A1 (en) * | 2022-01-11 | 2024-06-13 | Novartis Ag | Tlr7/8-antagonist for treating sjögren's syndrome or mixed connective tissue disease |
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| JPH11507052A (ja) | 1995-06-07 | 1999-06-22 | スージェン・インコーポレーテッド | キナゾリンおよび医薬組成物 |
| EP1940819A1 (en) | 2005-08-16 | 2008-07-09 | Memory Pharmaceuticals Corporation | Phosphodiesterase 10 inhibitors |
| EP3238722B1 (en) | 2011-01-10 | 2019-03-13 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinones |
| EA039373B1 (ru) | 2012-02-08 | 2022-01-19 | Янссен Сайенсиз Айрлэнд Юси | Производные пиперидино-пиримидина для лечения вирусных инфекций |
| EA029281B1 (ru) | 2013-07-30 | 2018-03-30 | Джилид Коннектикут, Инк. | Полиморф ингибиторов syk |
| AU2016312011B2 (en) * | 2015-08-25 | 2021-02-04 | Beigene, Ltd. | Process for preparing Parp inhibitor, crystalline forms, and uses thereof |
| BR112018074911B1 (pt) * | 2016-06-30 | 2023-01-17 | Kimberly-Clark Worldwide, Inc. | Processo para fabricar um compósito de espuma e fibra, compósito de espuma e fibra, e, artigo absorvente |
| EP4059934B1 (en) * | 2016-09-09 | 2026-07-29 | Novartis AG | Compounds and compositions as inhibitors of endosomal toll-like receptors |
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2019
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- 2019-05-16 KR KR1020207032942A patent/KR20210013554A/ko not_active Ceased
- 2019-05-16 BR BR112020022738-2A patent/BR112020022738A2/pt not_active IP Right Cessation
- 2019-05-16 CN CN201980032642.0A patent/CN112119078A/zh active Pending
- 2019-05-16 EP EP19735624.9A patent/EP3793998A1/en not_active Withdrawn
- 2019-05-16 AR ARP190101308A patent/AR117573A1/es not_active Application Discontinuation
- 2019-05-16 AU AU2019268583A patent/AU2019268583B2/en not_active Ceased
- 2019-05-16 MX MX2020012259A patent/MX2020012259A/es unknown
- 2019-05-16 US US17/056,351 patent/US12084460B2/en active Active
- 2019-05-16 TW TW112150642A patent/TW202417000A/zh unknown
- 2019-05-16 JP JP2020564243A patent/JP7407740B2/ja active Active
- 2019-05-16 TW TW108116864A patent/TWI826446B/zh active
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2023
- 2023-12-18 JP JP2023212606A patent/JP2024037930A/ja active Pending
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2024
- 2024-08-06 US US18/795,371 patent/US20240391938A1/en active Pending
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| EP3793998A1 (en) | 2021-03-24 |
| CN112119078A (zh) | 2020-12-22 |
| CL2020002967A1 (es) | 2021-04-30 |
| MX2020012259A (es) | 2021-01-29 |
| MX2023013584A (es) | 2023-11-30 |
| JP7407740B2 (ja) | 2024-01-04 |
| TWI826446B (zh) | 2023-12-21 |
| CA3097312A1 (en) | 2019-11-21 |
| KR20210013554A (ko) | 2021-02-04 |
| WO2019220390A1 (en) | 2019-11-21 |
| AU2019268583A1 (en) | 2020-10-29 |
| JP2024037930A (ja) | 2024-03-19 |
| US20210206783A1 (en) | 2021-07-08 |
| US20240391938A1 (en) | 2024-11-28 |
| TW202015698A (zh) | 2020-05-01 |
| US12084460B2 (en) | 2024-09-10 |
| AU2019268583B2 (en) | 2022-01-27 |
| AR117573A1 (es) | 2021-08-18 |
| BR112020022738A2 (pt) | 2021-02-02 |
| JP2021523918A (ja) | 2021-09-09 |
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