ES2661380T3 - Compuestos heteroaromáticos como moduladores de PI3 quinasas y métodos de uso - Google Patents
Compuestos heteroaromáticos como moduladores de PI3 quinasas y métodos de uso Download PDFInfo
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- ES2661380T3 ES2661380T3 ES13855522.2T ES13855522T ES2661380T3 ES 2661380 T3 ES2661380 T3 ES 2661380T3 ES 13855522 T ES13855522 T ES 13855522T ES 2661380 T3 ES2661380 T3 ES 2661380T3
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- alkyl
- mmol
- compound
- cancer
- cycloalkyl
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- 238000000034 method Methods 0.000 title description 53
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- 125000001424 substituent group Chemical group 0.000 claims abstract description 41
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 37
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract description 36
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 27
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- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 23
- 229910052805 deuterium Inorganic materials 0.000 claims abstract description 23
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- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims abstract description 16
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Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
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- 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
- A61K31/435—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
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
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- General Health & Medical Sciences (AREA)
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- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| US201261726139P | 2012-11-14 | 2012-11-14 | |
| US201261726139P | 2012-11-14 | ||
| PCT/US2013/069366 WO2014078211A1 (en) | 2012-11-14 | 2013-11-10 | Heteroaromatic compounds as pi3 kinase modulators and methods of use |
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| ES2661380T3 true ES2661380T3 (es) | 2018-03-28 |
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| MY (1) | MY180641A (enExample) |
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| WO (1) | WO2014078211A1 (enExample) |
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| CN104496995A (zh) * | 2014-01-06 | 2015-04-08 | 广东东阳光药业有限公司 | 制备3-乙炔基咪唑并[1,2-b]哒嗪的方法 |
| EP3159342B1 (en) * | 2014-06-17 | 2020-08-05 | Cisen Pharmaceutical Co., Ltd. | Pyridino[1,2-a]pyrimidone analogue used as mtor/pi3k inhibitor |
| CN105503877A (zh) | 2014-09-24 | 2016-04-20 | 和记黄埔医药（上海）有限公司 | 咪唑并哒嗪类化合物及其用途 |
| SI3233839T1 (sl) * | 2014-12-19 | 2019-12-31 | Janssen Pharmaceutica Nv | Heterociklil vezani derivati imidazopiridazina kot inhibitorji PI3Kbeta |
| JP6568588B2 (ja) * | 2014-12-19 | 2019-08-28 | ヤンセン ファーマシューティカ エヌ．ベー． | ＰＩ３Ｋβ阻害剤としてのイミダゾピリダジン誘導体 |
| JP7149854B2 (ja) * | 2016-06-16 | 2022-10-07 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｐｉ３ｋ ｂｅｔａ阻害薬としての二環式ピリジン、ピラジンおよびピリミジン誘導体 |
| WO2018017633A1 (en) | 2016-07-21 | 2018-01-25 | Bristol-Myers Squibb Company | TGF Beta RECEPTOR ANTAGONISTS |
| JP2019534266A (ja) | 2016-10-14 | 2019-11-28 | 江蘇恒瑞医薬股▲ふん▼有限公司 | ５員ヘテロアリール環の架橋した環誘導体、その製造方法およびその医学的使用 |
| US11629146B2 (en) * | 2016-11-28 | 2023-04-18 | Praxis Precision Medicines, Inc. | Substituted [1,2,4]triazolo[4,3-a]pyrazines as modulators of sodium channel activity |
| CN108164525B (zh) * | 2016-12-08 | 2020-09-08 | 沈阳药科大学 | 一种抗肿瘤化合物的制备方法和用途 |
| AU2018209164B2 (en) | 2017-01-17 | 2021-11-04 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| FR3064364A1 (fr) * | 2017-03-27 | 2018-09-28 | S.P.C.M. Sa | Methode de dosage de polymeres cationiques |
| PH12022500017A1 (en) | 2020-04-29 | 2023-08-14 | De Shaw Res Llc | PI3K-a INHIBITORS AND METHODS OF USE THEREOF |
| WO2023039532A1 (en) * | 2021-09-10 | 2023-03-16 | Relay Therapeutics, Inc. | Pi3k-alpha inhibitors and methods of use thereof |
| WO2023220131A2 (en) * | 2022-05-10 | 2023-11-16 | Relay Therapeutics, Inc. | PI3Kα INHIBITORS AND METHODS OF USE THEREOF |
| CN120737113B (zh) * | 2025-09-03 | 2025-11-21 | 湖北师范大学 | 一种三唑并哒嗪类化合物区域选择性c3-h炔基化的方法 |
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| RU2036924C1 (ru) * | 1989-01-31 | 1995-06-09 | Такеда Кемикал Индастриз ЛТД | Способ получения производных имидазо (1,2-b)пиридазина или их солей и производные имидазо (1,2-b)пиридазина или их соли |
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| US5994341A (en) | 1993-07-19 | 1999-11-30 | Angiogenesis Technologies, Inc. | Anti-angiogenic Compositions and methods for the treatment of arthritis |
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| US5578716A (en) | 1993-12-01 | 1996-11-26 | Mcgill University | DNA methyltransferase antisense oligonucleotides |
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| US6268137B1 (en) | 1996-05-22 | 2001-07-31 | Methylgene, Inc. | Specific inhibitors of DNA methyl transferase |
| WO1998054313A2 (en) | 1997-05-30 | 1998-12-03 | Mcgill University | Dna methyltransferase genomic sequences and antisense oligonucleotides |
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| AU2001264595A1 (en) * | 2000-05-19 | 2001-12-03 | Guilford Pharmaceuticals Inc. | Sulfonamide and carbamide derivatives of 6(5h)phenanthridinones and their uses |
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| RU2009107705A (ru) * | 2006-08-04 | 2010-09-10 | Такеда Фармасьютикал Компани Лимитед (Jp) | Конденсированное гетероциклическое соединение и его применение |
| WO2009039140A1 (en) * | 2007-09-17 | 2009-03-26 | Smithkline Beecham Corporation | Pyridopyrimidine derivatives as pi3 kinase inhibitors |
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| AR071523A1 (es) * | 2008-04-30 | 2010-06-23 | Merck Serono Sa | Compuestos biciclicos fusionados, un proceso para su preparacion, el compuesto para ser utilizado como medicamento en el tratamiento y profilaxis de enfermedades, una composicion farmaceutica y un conjunto que comprende paquetes separados del compuesto y de un ingrediente activo del medicamento |
| UA111579C2 (uk) | 2009-08-17 | 2016-05-25 | Інтеллікіне Ллк | ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ |
| JP5951600B2 (ja) * | 2010-05-21 | 2016-07-13 | インフィニティー ファーマシューティカルズ， インコーポレイテッド | キナーゼ調節のための、化合物、組成物および方法 |
| UY33597A (es) | 2010-09-09 | 2012-04-30 | Irm Llc | Compuestos y composiciones como inhibidores de la trk |
| US9284334B2 (en) | 2011-05-19 | 2016-03-15 | Fundación Centro Nacional De Investigaciones Oncologicas Carlos Iii | Macrocyclic compounds as protein kinase inhibitors |
| 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 |
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2013
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- 2013-11-10 MY MYPI2015701411A patent/MY180641A/en unknown
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- 2013-11-10 SG SG11201502725TA patent/SG11201502725TA/en unknown
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- 2013-11-10 BR BR112015006726-3A patent/BR112015006726B1/pt not_active IP Right Cessation
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- 2013-11-10 CN CN201380054625.XA patent/CN104755085B/zh active Active
- 2013-11-10 WO PCT/US2013/069366 patent/WO2014078211A1/en not_active Ceased
- 2013-11-10 AU AU2013345107A patent/AU2013345107B2/en active Active
- 2013-11-10 RU RU2015116102A patent/RU2665036C9/ru active
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2015
- 2015-04-16 ZA ZA2015/02575A patent/ZA201502575B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2015116102A (ru) | 2017-01-10 |
| RU2665036C9 (ru) | 2018-11-12 |
| RU2665036C2 (ru) | 2018-08-27 |
| ZA201502575B (en) | 2016-11-30 |
| EP2919784A1 (en) | 2015-09-23 |
| MY180641A (en) | 2020-12-04 |
| BR112015006726B1 (pt) | 2021-11-23 |
| AU2013345107A1 (en) | 2015-04-30 |
| TW201422615A (zh) | 2014-06-16 |
| JP6268183B2 (ja) | 2018-01-24 |
| BR112015006726A2 (pt) | 2017-08-22 |
| EP3299019B1 (en) | 2019-10-09 |
| CA2889346C (en) | 2018-09-25 |
| AU2013345107B2 (en) | 2016-02-25 |
| SG11201502725TA (en) | 2015-05-28 |
| TWI574962B (zh) | 2017-03-21 |
| HK1210956A1 (en) | 2016-05-13 |
| EP2919784A4 (en) | 2016-07-06 |
| KR20150083833A (ko) | 2015-07-20 |
| EP3299019A1 (en) | 2018-03-28 |
| CN104755085A (zh) | 2015-07-01 |
| JP2015536994A (ja) | 2015-12-24 |
| US9926324B2 (en) | 2018-03-27 |
| CN104755085B (zh) | 2018-05-01 |
| WO2014078211A1 (en) | 2014-05-22 |
| KR102148679B1 (ko) | 2020-08-27 |
| CA2889346A1 (en) | 2014-05-22 |
| US20140134133A1 (en) | 2014-05-15 |
| EP2919784B1 (en) | 2017-12-20 |
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