CA2898294C - Heteroaromatic compounds as pi3 kinase modulators - Google Patents
Heteroaromatic compounds as pi3 kinase modulators Download PDFInfo
- Publication number
- CA2898294C CA2898294C CA2898294A CA2898294A CA2898294C CA 2898294 C CA2898294 C CA 2898294C CA 2898294 A CA2898294 A CA 2898294A CA 2898294 A CA2898294 A CA 2898294A CA 2898294 C CA2898294 C CA 2898294C
- Authority
- CA
- Canada
- Prior art keywords
- cancer
- alkylene
- cycloalkyl
- alkyl
- compound
- Prior art date
- Legal status (The legal status 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 status listed.)
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Classifications
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- 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
- 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
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361767721P | 2013-02-21 | 2013-02-21 | |
| US61/767,721 | 2013-02-21 | ||
| PCT/US2014/016643 WO2014130375A1 (en) | 2013-02-21 | 2014-02-15 | Heteroaromatic compounds as pi3 kinase modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2898294A1 CA2898294A1 (en) | 2014-08-28 |
| CA2898294C true CA2898294C (en) | 2020-06-09 |
Family
ID=51351332
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2898294A Active CA2898294C (en) | 2013-02-21 | 2014-02-15 | Heteroaromatic compounds as pi3 kinase modulators |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9573953B2 (enExample) |
| EP (1) | EP2958564B1 (enExample) |
| JP (1) | JP6389829B2 (enExample) |
| KR (1) | KR102148681B1 (enExample) |
| AU (1) | AU2014219256B2 (enExample) |
| BR (1) | BR112015018318A2 (enExample) |
| CA (1) | CA2898294C (enExample) |
| ES (1) | ES2674705T3 (enExample) |
| MX (1) | MX2015010700A (enExample) |
| MY (1) | MY182036A (enExample) |
| RU (1) | RU2672910C9 (enExample) |
| SG (1) | SG11201505493QA (enExample) |
| TW (1) | TWI620749B (enExample) |
| WO (1) | WO2014130375A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112018003588A2 (pt) | 2015-08-26 | 2018-09-25 | Blueprint Medicines Corp | compostos e composições úteis para tratamento de distúrbios relacionados ao ntrk |
| RU2018122089A (ru) * | 2015-11-19 | 2019-12-25 | Блюпринт Медсинс Корпорейшн | Соединения и композиции, подходящие для лечения расстройств, связанных с ntrk |
| WO2018136202A2 (en) * | 2016-12-23 | 2018-07-26 | Plexxikon Inc. | Compounds and methods for cdk8 modulation and indications therefor |
| MX393780B (es) | 2017-01-17 | 2025-03-24 | Heparegenix Gmbh | Inhibidores de proteina cinasa para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocitos |
| WO2018169700A1 (en) * | 2017-03-14 | 2018-09-20 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| CN109867671B (zh) * | 2017-12-02 | 2020-07-07 | 广东东阳光药业有限公司 | 一种吡唑[1,5-a]吡啶化合物的晶型及其药物组合物和用途 |
| CN109867668B (zh) * | 2017-12-02 | 2021-03-26 | 广东东阳光药业有限公司 | 一种吡唑[1,5-a]吡啶化合物的晶型及其药物组合物和用途 |
| CN109867669B (zh) * | 2017-12-02 | 2021-02-26 | 广东东阳光药业有限公司 | 一种吡唑[1,5-a]吡啶化合物的晶型及其药物组合物和用途 |
| CN109867672B (zh) * | 2017-12-02 | 2020-07-07 | 广东东阳光药业有限公司 | 吡唑[1,5-a]吡啶衍生物的盐及其用途 |
| CN109867670B (zh) * | 2017-12-02 | 2020-07-07 | 广东东阳光药业有限公司 | 一种吡唑[1,5-a]吡啶化合物的单钠盐及其医药用途 |
| US11179376B2 (en) * | 2017-12-20 | 2021-11-23 | Sunshine Lake Pharma Co., Ltd. | Salts of pyrazolo[1,5-a]pyridine derivative and use thereof |
| CN112770757B (zh) * | 2018-10-19 | 2024-01-16 | 广东东阳光药业股份有限公司 | 一种治疗纤维化疾病的药物组合或药物组合物 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5886026A (en) | 1993-07-19 | 1999-03-23 | Angiotech Pharmaceuticals Inc. | Anti-angiogenic compositions and methods of use |
| KR100392057B1 (ko) | 1993-11-30 | 2003-10-30 | 맥길 유니버시티 | 세포의 CpG 디뉴클레오티드 내의 시토신의 메틸화를 감소하는 방법 |
| US5578716A (en) | 1993-12-01 | 1996-11-26 | Mcgill University | DNA methyltransferase antisense oligonucleotides |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| US6268137B1 (en) | 1996-05-22 | 2001-07-31 | Methylgene, Inc. | Specific inhibitors of DNA methyl transferase |
| US6020318A (en) | 1997-05-30 | 2000-02-01 | Methylgene, Inc. | DNA methyltransferase genomic sequences and antisense oligonucleotides |
| AU8125098A (en) | 1997-05-30 | 1998-12-30 | Mcgill University | Dna methyltransferase genomic sequences and antisense oligonucleotides |
| US6066625A (en) | 1998-02-03 | 2000-05-23 | Methylgene, Inc. | Optimized antisense oligonucleotides complementary to DNA methyltransferase sequences |
| US6953783B1 (en) | 1998-10-19 | 2005-10-11 | Methylgene, Inc. | Modulation of gene expression by combination therapy |
| JP2003500052A (ja) | 1999-05-03 | 2003-01-07 | メチルジーン インコーポレイテッド | ヒストン脱アセチル酵素の抑制 |
| EP1233958B1 (en) | 1999-11-23 | 2011-06-29 | MethylGene Inc. | Inhibitors of histone deacetylase |
| CA2408385A1 (en) | 2000-03-24 | 2001-09-24 | Methylgene, Inc. | Inhibition of specific histone deacetylase isoforms |
| EP1280764B1 (en) | 2000-03-24 | 2010-11-24 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| RU2308457C2 (ru) * | 2001-04-27 | 2007-10-20 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Пиразоло [1, 5-а] пиридины и содержащие их лекарственные средства |
| JP3795044B2 (ja) | 2001-09-14 | 2006-07-12 | メシルジーン、インコーポレイテッド | ヒストンデアセチラーゼの阻害剤 |
| US7868204B2 (en) | 2001-09-14 | 2011-01-11 | Methylgene Inc. | Inhibitors of histone deacetylase |
| US6897220B2 (en) | 2001-09-14 | 2005-05-24 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| US7196078B2 (en) | 2002-09-04 | 2007-03-27 | Schering Corpoartion | Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| KR20050074487A (ko) | 2002-10-17 | 2005-07-18 | 메틸진, 인크. | 히스톤 데아세틸라아제의 억제제 |
| WO2004052315A2 (en) * | 2002-12-11 | 2004-06-24 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| ES2222813B1 (es) * | 2003-07-24 | 2005-12-16 | Ferrer Internacional, S.A. | N-(3-(3-sustituidas-pirazolo(1,5-a)pirimidin-7-il)-fenil)-sulfonamidas y composiciones y metodos relacionados. |
| WO2005030704A1 (en) | 2003-09-24 | 2005-04-07 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| US7329662B2 (en) | 2003-10-03 | 2008-02-12 | Hoffmann-La Roche Inc. | Pyrazolo-pyridine |
| WO2005092899A1 (en) | 2004-03-26 | 2005-10-06 | Methylgene Inc. | Inhibitors of histone deacetylase |
| ES2438017T3 (es) | 2004-07-30 | 2014-01-15 | Methylgene Inc. | Inhibidores de la señalización del receptor del VEGF y del receptor del HGF |
| ATE460417T1 (de) | 2005-03-23 | 2010-03-15 | Hoffmann La Roche | Acetylenylpyrazolopyrimidinderivate als mglur2- antagonsten |
| EP2211615A4 (en) * | 2007-10-22 | 2010-10-13 | Glaxosmithkline Llc | PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS |
| CL2008003798A1 (es) * | 2007-12-19 | 2009-10-09 | Amgen Inc | Compuestos derivados de heterobiciclos aromaticos sustituidos, inhibidores de pi3 quinasa; composicion farmaceutica; utiles en el tratamiento de cancer, melanomas, glioblastomas, entre otras enfermedades. |
| WO2010118207A1 (en) * | 2009-04-09 | 2010-10-14 | Schering Corporation | Pyrazolo [1, 5-a] pyrimidine derivatives as mtor inhibitors |
| GEP201706639B (en) | 2009-08-17 | 2017-03-27 | Intellikine Llc | Heterocyclic compounds and uses thereof |
| US8883801B2 (en) | 2010-08-23 | 2014-11-11 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors |
| CN102675286B (zh) | 2011-03-07 | 2015-08-19 | 中国科学院上海药物研究所 | 一类吲唑类化合物及其制备方法、用途和药物组合物 |
| KR101953210B1 (ko) * | 2011-05-19 | 2019-02-28 | 푼다시온 센트로 나시오날 드 인베스티가시오네스 온콜로기카스 카를로스Ⅲ | 단백질 키나아제 억제제로서의 대환식 화합물 |
| WO2012174312A2 (en) | 2011-06-15 | 2012-12-20 | Glaxosmithkline Llc | Benzimidazole derivatives as antiviral agents |
| KR101274986B1 (ko) | 2011-07-27 | 2013-06-17 | 한국과학기술원 | 이미다조피리딘 유도체, 이를 포함하는 ＰＩ3Ｋ 및/또는 ｍＴＯＲ 저해제용 약학 조성물 및 ＰＩ3Ｋ 및/또는 ｍＴＯＲ과 연관된 질환 치료용 약학 조성물 |
| GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| CN102924450A (zh) | 2012-11-01 | 2013-02-13 | 西安交通大学 | 6-(5-吡啶基)-1,2,4-三唑并吡啶类化合物及其制备方法和用途 |
-
2014
- 2014-02-15 BR BR112015018318A patent/BR112015018318A2/pt not_active Application Discontinuation
- 2014-02-15 SG SG11201505493QA patent/SG11201505493QA/en unknown
- 2014-02-15 RU RU2015131467A patent/RU2672910C9/ru active
- 2014-02-15 MX MX2015010700A patent/MX2015010700A/es unknown
- 2014-02-15 CA CA2898294A patent/CA2898294C/en active Active
- 2014-02-15 WO PCT/US2014/016643 patent/WO2014130375A1/en not_active Ceased
- 2014-02-15 ES ES14754663.4T patent/ES2674705T3/es active Active
- 2014-02-15 US US14/181,670 patent/US9573953B2/en active Active
- 2014-02-15 MY MYPI2015702491A patent/MY182036A/en unknown
- 2014-02-15 KR KR1020157019069A patent/KR102148681B1/ko active Active
- 2014-02-15 AU AU2014219256A patent/AU2014219256B2/en active Active
- 2014-02-15 EP EP14754663.4A patent/EP2958564B1/en active Active
- 2014-02-15 JP JP2015558892A patent/JP6389829B2/ja active Active
- 2014-02-18 TW TW103105349A patent/TWI620749B/zh active
Also Published As
| Publication number | Publication date |
|---|---|
| TWI620749B (zh) | 2018-04-11 |
| AU2014219256A1 (en) | 2015-07-30 |
| ES2674705T3 (es) | 2018-07-03 |
| CA2898294A1 (en) | 2014-08-28 |
| US20140234254A1 (en) | 2014-08-21 |
| KR102148681B1 (ko) | 2020-08-27 |
| JP2016509056A (ja) | 2016-03-24 |
| EP2958564A4 (en) | 2016-10-26 |
| RU2672910C2 (ru) | 2018-11-21 |
| RU2672910C9 (ru) | 2019-06-04 |
| BR112015018318A2 (pt) | 2017-08-22 |
| HK1218385A1 (en) | 2017-02-17 |
| EP2958564B1 (en) | 2018-05-09 |
| SG11201505493QA (en) | 2015-08-28 |
| WO2014130375A1 (en) | 2014-08-28 |
| AU2014219256B2 (en) | 2017-02-16 |
| TW201443049A (zh) | 2014-11-16 |
| EP2958564A1 (en) | 2015-12-30 |
| KR20150118102A (ko) | 2015-10-21 |
| MY182036A (en) | 2021-01-18 |
| JP6389829B2 (ja) | 2018-09-12 |
| MX2015010700A (es) | 2017-01-23 |
| RU2015131467A (ru) | 2017-03-24 |
| US9573953B2 (en) | 2017-02-21 |
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