IL272988B - Imidazo-[1,5-a]pyrazine derivatives as pi3k-delta inhibitors - Google Patents
Imidazo-[1,5-a]pyrazine derivatives as pi3k-delta inhibitorsInfo
- Publication number
- IL272988B IL272988B IL272988A IL27298820A IL272988B IL 272988 B IL272988 B IL 272988B IL 272988 A IL272988 A IL 272988A IL 27298820 A IL27298820 A IL 27298820A IL 272988 B IL272988 B IL 272988B
- Authority
- IL
- Israel
- Prior art keywords
- compound
- 6alkyl
- optionally substituted
- heterocyclyl
- substituent
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- 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
- A61K31/4164—1,3-Diazoles
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-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
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- 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
- A61P7/06—Antianaemics
-
- 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
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2017101058 | 2017-09-08 | ||
| CN2017119373 | 2017-12-28 | ||
| CN2018086555 | 2018-05-11 | ||
| PCT/CN2018/104559 WO2019047915A1 (en) | 2017-09-08 | 2018-09-07 | IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3KDELTA INHIBITORS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL272988A IL272988A (en) | 2020-04-30 |
| IL272988B true IL272988B (en) | 2022-08-01 |
Family
ID=65633578
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL272988A IL272988B (en) | 2017-09-08 | 2018-09-07 | Imidazo-[1,5-a]pyrazine derivatives as pi3k-delta inhibitors |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US11220506B2 (https=) |
| EP (2) | EP3679042B1 (https=) |
| JP (1) | JP7128264B2 (https=) |
| KR (1) | KR20200052297A (https=) |
| CN (2) | CN111704615B (https=) |
| AU (2) | AU2018328569B2 (https=) |
| BR (1) | BR112020004500A2 (https=) |
| CA (1) | CA3072842A1 (https=) |
| DK (1) | DK3679042T3 (https=) |
| ES (1) | ES2944658T3 (https=) |
| FI (1) | FI3679042T3 (https=) |
| HU (1) | HUE061898T2 (https=) |
| IL (1) | IL272988B (https=) |
| MX (1) | MX2020002630A (https=) |
| NZ (1) | NZ761680A (https=) |
| PL (1) | PL3679042T3 (https=) |
| PT (1) | PT3679042T (https=) |
| SG (1) | SG11202001286SA (https=) |
| TW (2) | TWI817956B (https=) |
| WO (1) | WO2019047915A1 (https=) |
| ZA (1) | ZA202000875B (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3045959A1 (en) | 2016-12-07 | 2018-06-14 | Beigene, Ltd. | Imidazo [1,5-a] pyrazine derivatives as pi3kdelta inhibitors |
| BR112020004500A2 (pt) | 2017-09-08 | 2020-12-01 | Beigene, Ltd. | derivados de imidazo [1,5-a] pirazina como inibidores de pi3kdelta |
| US20230011916A1 (en) * | 2019-11-21 | 2023-01-12 | Beigene, Ltd. | Methods of cancer treatment using anti-ox40 antibodies in combination with pi3 kinase delta inhibitors |
| AU2022280905A1 (en) * | 2021-05-27 | 2024-01-18 | Beigene Switzerland Gmbh | SALTS OF A PI3Kdelta INHIBITOR, CRYSTALLINE FORMS, METHODS OF PREPARATION, AND USES THEREFORE |
| WO2023040810A1 (en) * | 2021-09-14 | 2023-03-23 | Beigene, Ltd. | Methods of cancer treatment using a combination of btk inhibitors and pi3 kinase inhibitors |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005089352A (ja) * | 2003-09-16 | 2005-04-07 | Kissei Pharmaceut Co Ltd | 新規なイミダゾ［１，５−ａ］ピラジン誘導体、それを含有する医薬組成物およびそれらの用途 |
| UA83509C2 (en) * | 2003-10-15 | 2008-07-25 | Оси Фармасьютикалз, Инк. | Imidazopyrazines as tyrosine kinase inhibitors |
| TW200738725A (en) * | 2006-01-25 | 2007-10-16 | Osi Pharm Inc | Unsaturated mTOR inhibitors |
| US20120077813A1 (en) * | 2009-04-15 | 2012-03-29 | Astrazeneca Ab | Imidazole Substituted Pyrimidines Useful in the Treatment of Glycogen Synthase Kinase-3 Related Disorders such as Alzheimer's Disease |
| BRPI1014572B8 (pt) | 2009-04-16 | 2022-07-19 | Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii | Imidazopirazinas para uso como inibidores de cinase |
| RU2013138835A (ru) * | 2011-02-09 | 2015-03-20 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения в качестве ингибиторов pi3 киназы |
| ES2588186T3 (es) | 2012-01-10 | 2016-10-31 | Bayer Intellectual Property Gmbh | Imidazopirazinas sustituidas como inhibidores de la quinasa Akt |
| AU2013337717B2 (en) | 2012-11-01 | 2018-10-25 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using PI3 kinase isoform modulators |
| TWI687220B (zh) * | 2013-03-01 | 2020-03-11 | 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 |
| CA2914284A1 (en) | 2013-05-30 | 2014-12-04 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| CA2922058A1 (en) * | 2013-10-18 | 2015-04-23 | Medivation Technologies, Inc. | Heterocyclic compounds and methods of use |
| PL3179991T3 (pl) * | 2014-08-11 | 2022-02-14 | Acerta Pharma B.V. | Kombinacje terapeutyczne inhibitora btk i inhibitora bcl-2 |
| AR102220A1 (es) * | 2015-10-08 | 2017-02-15 | Incyte Corp | Imidazopiridinas e imidazopirazinas como inhibidores de lsd1 |
| HRP20210508T1 (hr) * | 2016-06-16 | 2021-05-28 | Janssen Pharmaceutica Nv | Biciklički derivati piridina, pirazina i pirimidina kao inhibitori pi3k beta |
| CA3045959A1 (en) * | 2016-12-07 | 2018-06-14 | Beigene, Ltd. | Imidazo [1,5-a] pyrazine derivatives as pi3kdelta inhibitors |
| BR112020004500A2 (pt) | 2017-09-08 | 2020-12-01 | Beigene, Ltd. | derivados de imidazo [1,5-a] pirazina como inibidores de pi3kdelta |
-
2018
- 2018-09-07 BR BR112020004500-4A patent/BR112020004500A2/pt not_active Application Discontinuation
- 2018-09-07 KR KR1020207007386A patent/KR20200052297A/ko active Pending
- 2018-09-07 FI FIEP18853233.7T patent/FI3679042T3/fi active
- 2018-09-07 TW TW107131522A patent/TWI817956B/zh not_active IP Right Cessation
- 2018-09-07 DK DK18853233.7T patent/DK3679042T3/da active
- 2018-09-07 JP JP2020513700A patent/JP7128264B2/ja active Active
- 2018-09-07 SG SG11202001286SA patent/SG11202001286SA/en unknown
- 2018-09-07 AU AU2018328569A patent/AU2018328569B2/en not_active Ceased
- 2018-09-07 CN CN202010273331.8A patent/CN111704615B/zh active Active
- 2018-09-07 WO PCT/CN2018/104559 patent/WO2019047915A1/en not_active Ceased
- 2018-09-07 PL PL18853233.7T patent/PL3679042T3/pl unknown
- 2018-09-07 NZ NZ761680A patent/NZ761680A/en not_active IP Right Cessation
- 2018-09-07 ES ES18853233T patent/ES2944658T3/es active Active
- 2018-09-07 CA CA3072842A patent/CA3072842A1/en active Pending
- 2018-09-07 CN CN201880057835.7A patent/CN111051312A/zh active Pending
- 2018-09-07 MX MX2020002630A patent/MX2020002630A/es unknown
- 2018-09-07 PT PT188532337T patent/PT3679042T/pt unknown
- 2018-09-07 IL IL272988A patent/IL272988B/en unknown
- 2018-09-07 EP EP18853233.7A patent/EP3679042B1/en active Active
- 2018-09-07 HU HUE18853233A patent/HUE061898T2/hu unknown
- 2018-09-07 US US16/643,040 patent/US11220506B2/en active Active
- 2018-09-07 TW TW111147323A patent/TW202336010A/zh unknown
- 2018-09-07 EP EP23152036.2A patent/EP4219502A1/en not_active Withdrawn
-
2020
- 2020-02-11 ZA ZA2020/00875A patent/ZA202000875B/en unknown
-
2021
- 2021-11-23 US US17/533,442 patent/US11905294B2/en active Active
-
2023
- 2023-10-25 AU AU2023254925A patent/AU2023254925A1/en not_active Abandoned
-
2024
- 2024-01-11 US US18/410,925 patent/US20240150361A1/en not_active Abandoned
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