EA202091641A1 - 2,4,6,7-ТЕТРАГИДРОПИРАЗОЛО[4,3-d]ПИРИМИДИН-5-ОНОВЫЕ ПРОИЗВОДНЫЕ И РОДСТВЕННЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА C5a ДЛЯ ЛЕЧЕНИЯ ВАСКУЛИТА И ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ - Google Patents
2,4,6,7-ТЕТРАГИДРОПИРАЗОЛО[4,3-d]ПИРИМИДИН-5-ОНОВЫЕ ПРОИЗВОДНЫЕ И РОДСТВЕННЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА C5a ДЛЯ ЛЕЧЕНИЯ ВАСКУЛИТА И ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙInfo
- Publication number
- EA202091641A1 EA202091641A1 EA202091641A EA202091641A EA202091641A1 EA 202091641 A1 EA202091641 A1 EA 202091641A1 EA 202091641 A EA202091641 A EA 202091641A EA 202091641 A EA202091641 A EA 202091641A EA 202091641 A1 EA202091641 A1 EA 202091641A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- derivatives
- tetrahydropyrazolo
- vasculitis
- treatment
- inflammatory diseases
- Prior art date
Links
Classifications
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- 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
-
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Eye Examination Apparatus (AREA)
- Oscillators With Electromechanical Resonators (AREA)
- Heat Sensitive Colour Forming Recording (AREA)
Abstract
Настоящее изобретение относится к производным формулы (I)где кольцо A, X, Y, Z, RA, R1, R2, R3 и R4 являются такими, как указано в описании и, в частности, к 2,4,6,7-тетрагидропиразоло[4,3-d]пиримидин-5-оновым производным и родственным соединениям, их получению, их фармацевтически приемлемым солям, их применению в качестве лекарственных препаратов, фармацевтическим композициям, содержащим одно или несколько соединений формулы (I) и, в особенности, к их применению в качестве модуляторов C5a рецепторов для лечения, например, васкулита и воспалительных заболеваний.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2018050598 | 2018-01-10 | ||
| PCT/EP2019/050372 WO2019137927A1 (en) | 2018-01-10 | 2019-01-09 | 2,4,6,7-tetrahydro-pyrazolo[4,3-d]pyrimidin-5-one derivatives and related compounds as c5a receptor modulators for treating vasculitis and inflammatory diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA202091641A1 true EA202091641A1 (ru) | 2020-11-17 |
Family
ID=65012016
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA202091641A EA202091641A1 (ru) | 2018-01-10 | 2019-01-09 | 2,4,6,7-ТЕТРАГИДРОПИРАЗОЛО[4,3-d]ПИРИМИДИН-5-ОНОВЫЕ ПРОИЗВОДНЫЕ И РОДСТВЕННЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА C5a ДЛЯ ЛЕЧЕНИЯ ВАСКУЛИТА И ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ |
Country Status (29)
| Country | Link |
|---|---|
| US (2) | US11608341B2 (ru) |
| EP (1) | EP3737684B1 (ru) |
| JP (1) | JP7014914B2 (ru) |
| KR (1) | KR102574564B1 (ru) |
| CN (1) | CN111566109B (ru) |
| AR (1) | AR114564A1 (ru) |
| AU (1) | AU2019207666B2 (ru) |
| BR (1) | BR112020013788A2 (ru) |
| CA (1) | CA3086310C (ru) |
| CL (1) | CL2020001817A1 (ru) |
| DK (1) | DK3737684T3 (ru) |
| EA (1) | EA202091641A1 (ru) |
| ES (1) | ES2933820T3 (ru) |
| HR (1) | HRP20221449T1 (ru) |
| HU (1) | HUE060515T2 (ru) |
| IL (1) | IL275868B2 (ru) |
| LT (1) | LT3737684T (ru) |
| MA (1) | MA51558B1 (ru) |
| MX (1) | MX2020007443A (ru) |
| PH (1) | PH12020500583A1 (ru) |
| PL (1) | PL3737684T3 (ru) |
| PT (1) | PT3737684T (ru) |
| RS (1) | RS63806B1 (ru) |
| SG (1) | SG11202006490YA (ru) |
| SI (1) | SI3737684T1 (ru) |
| TW (1) | TWI774905B (ru) |
| UA (1) | UA124694C2 (ru) |
| WO (1) | WO2019137927A1 (ru) |
| ZA (1) | ZA202004910B (ru) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2020007443A (es) * | 2018-01-10 | 2020-09-14 | Idorsia Pharmaceuticals Ltd | Derivados de 2,4,6,7-tetrahidro-pirazolo[4,3-d]pirimidin-5-ona y compuestos relacionados como moduladores del receptor c5a para el tratamiento de vasculitis y enfermedades inflamatorias. |
| EP3740477A1 (en) | 2018-01-19 | 2020-11-25 | Idorsia Pharmaceuticals Ltd | C5a receptor modulators |
| EP3740476A1 (en) * | 2018-01-19 | 2020-11-25 | Idorsia Pharmaceuticals Ltd | C5a receptor modulators |
| US20220265658A1 (en) * | 2019-07-09 | 2022-08-25 | Idorsia Pharmaceuticals Ltd. | Pharmaceutical composition comprising a tetrahydropyrazolopyrimidinone compound |
| US11193891B2 (en) * | 2019-12-20 | 2021-12-07 | Robert Bosch Gmbh | Receptors and spacers for a fluorescence-based lead ion chemosensor |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003218374A1 (en) * | 2002-03-28 | 2003-10-13 | Neurogen Corporation | Substituted tetrahydroisoquinolines as c5a receptor modulators |
| WO2004033455A2 (en) * | 2002-10-08 | 2004-04-22 | Novo Nordisk A/S | Hemisuccinate salts of heterocyclic dpp-iv inhibitors |
| US7906528B2 (en) * | 2004-10-05 | 2011-03-15 | Novartis International Pharmaceutical Ltd. | Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds |
| ES2632975T3 (es) * | 2010-06-24 | 2017-09-18 | Chemocentryx, Inc. | Antagonistas de C5aR |
| US8846656B2 (en) * | 2011-07-22 | 2014-09-30 | Novartis Ag | Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators |
| TWI736135B (zh) * | 2013-03-01 | 2021-08-11 | 美商英塞特控股公司 | 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途 |
| CN105705489B (zh) | 2013-09-04 | 2019-04-26 | 百时美施贵宝公司 | 用作免疫调节剂的化合物 |
| AU2014316682B2 (en) | 2013-09-06 | 2018-11-22 | Aurigene Discovery Technologies Limited | 1,2,4-oxadiazole derivatives as immunomodulators |
| WO2015044900A1 (en) | 2013-09-27 | 2015-04-02 | Aurigene Discovery Technologies Limited | Therapeutic immunomodulating compounds |
| US9738646B2 (en) * | 2014-09-16 | 2017-08-22 | Gilead Sciences, Inc. | Solid forms of a toll-like receptor modulator |
| US9682940B2 (en) * | 2015-08-25 | 2017-06-20 | Janssen Pharmaceutica Nv | Indazole derivatives useful as CB-1 inverse agonists |
| MX2020007443A (es) * | 2018-01-10 | 2020-09-14 | Idorsia Pharmaceuticals Ltd | Derivados de 2,4,6,7-tetrahidro-pirazolo[4,3-d]pirimidin-5-ona y compuestos relacionados como moduladores del receptor c5a para el tratamiento de vasculitis y enfermedades inflamatorias. |
| EP3740476A1 (en) | 2018-01-19 | 2020-11-25 | Idorsia Pharmaceuticals Ltd | C5a receptor modulators |
| EP3740477A1 (en) | 2018-01-19 | 2020-11-25 | Idorsia Pharmaceuticals Ltd | C5a receptor modulators |
| US20220265658A1 (en) | 2019-07-09 | 2022-08-25 | Idorsia Pharmaceuticals Ltd. | Pharmaceutical composition comprising a tetrahydropyrazolopyrimidinone compound |
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2019
- 2019-01-09 MX MX2020007443A patent/MX2020007443A/es unknown
- 2019-01-09 HR HRP20221449TT patent/HRP20221449T1/hr unknown
- 2019-01-09 TW TW108100804A patent/TWI774905B/zh active
- 2019-01-09 JP JP2020538035A patent/JP7014914B2/ja active Active
- 2019-01-09 CA CA3086310A patent/CA3086310C/en active Active
- 2019-01-09 BR BR112020013788-0A patent/BR112020013788A2/pt unknown
- 2019-01-09 SI SI201930400T patent/SI3737684T1/sl unknown
- 2019-01-09 CN CN201980007596.9A patent/CN111566109B/zh active Active
- 2019-01-09 ES ES19700269T patent/ES2933820T3/es active Active
- 2019-01-09 DK DK19700269.4T patent/DK3737684T3/da active
- 2019-01-09 UA UAA202004963A patent/UA124694C2/uk unknown
- 2019-01-09 KR KR1020207022343A patent/KR102574564B1/ko active IP Right Grant
- 2019-01-09 WO PCT/EP2019/050372 patent/WO2019137927A1/en unknown
- 2019-01-09 MA MA51558A patent/MA51558B1/fr unknown
- 2019-01-09 LT LTEPPCT/EP2019/050372T patent/LT3737684T/lt unknown
- 2019-01-09 PL PL19700269.4T patent/PL3737684T3/pl unknown
- 2019-01-09 US US16/961,600 patent/US11608341B2/en active Active
- 2019-01-09 RS RS20221138A patent/RS63806B1/sr unknown
- 2019-01-09 PT PT197002694T patent/PT3737684T/pt unknown
- 2019-01-09 EA EA202091641A patent/EA202091641A1/ru unknown
- 2019-01-09 SG SG11202006490YA patent/SG11202006490YA/en unknown
- 2019-01-09 AU AU2019207666A patent/AU2019207666B2/en active Active
- 2019-01-09 HU HUE19700269A patent/HUE060515T2/hu unknown
- 2019-01-09 AR ARP190100043A patent/AR114564A1/es unknown
- 2019-01-09 EP EP19700269.4A patent/EP3737684B1/en active Active
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2020
- 2020-07-06 IL IL275868A patent/IL275868B2/en unknown
- 2020-07-07 PH PH12020500583A patent/PH12020500583A1/en unknown
- 2020-07-08 CL CL2020001817A patent/CL2020001817A1/es unknown
- 2020-08-07 ZA ZA2020/04910A patent/ZA202004910B/en unknown
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2022
- 2022-12-20 US US18/084,911 patent/US20230192708A1/en active Pending
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