AR089175A1 - Inhibidores de pak para el tratamiento de trastornos de proliferacion celular - Google Patents
Inhibidores de pak para el tratamiento de trastornos de proliferacion celularInfo
- Publication number
- AR089175A1 AR089175A1 ARP120104155A ARP120104155A AR089175A1 AR 089175 A1 AR089175 A1 AR 089175A1 AR P120104155 A ARP120104155 A AR P120104155A AR P120104155 A ARP120104155 A AR P120104155A AR 089175 A1 AR089175 A1 AR 089175A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- unsubstituted
- heteroaryl
- heterocycloalkyl
- alkyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 230000004663 cell proliferation Effects 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- -1 alkylsulfone Chemical group 0.000 abstract 3
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 2
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000005360 alkyl sulfoxide group Chemical group 0.000 abstract 1
- 125000003368 amide group Chemical group 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000005362 aryl sulfone group Chemical group 0.000 abstract 1
- 125000005361 aryl sulfoxide group Chemical group 0.000 abstract 1
- 125000005110 aryl thio group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 208000035269 cancer or benign tumor Diseases 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
Inhibidores de PAK y métodos para usarlos en el tratamiento de trastornos de proliferación celular y/o trastornos del sistema nervioso central. Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de la fórmula (1), fórmula (2), o fórmula (3), o una sal farmacéuticamente aceptable o N-óxido del mismo, donde: el anillo T es un anillo arilo o heteroarilo; R¹ es H, o alquilo sustituido o no sustituido; R² es alquilo no sustituido o alquilo sustituido con amino sustituido o no sustituido, amido, nitro, ariltio, alquilsulfóxido, arilsulfóxido, alquilsulfona, arilsulfona, ariloxi, alcoloxo, amida, éster, alcoilo, ciano, arilo, o heteroarilo; alcoxi sustituido o no sustituido; aralcoxi sustituido o no sustituido; heteroalquilo sustituido o no sustituido; cicloalquilo sustituido o no sustituido; cicloalquilalquilo sustituido o no sustituido; heterocicloalquilo sustituido o no sustituido; heterocicloalquilalquilo sustituido o no sustituido; espiro-cicloalquil-heterocicloalquilo; -alquilen-S(=O)R⁹; -alquilen-S(=O)₂R⁹; o -S(=O)₂R⁹; R³ es H, alquilo sustituido o no sustituido, alcoxi sustituido o no sustituido, amino sustituido o no sustituido, heteroalquilo sustituido o no sustituido, heterocicloalquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, heterocicloalquilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, aralquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, o heteroarilalquilo sustituido o no sustituido; R⁴ es heteroarilo sustituido o no sustituido unido al anillo T o el anillo fenilo a través de un átomo de carbono de R⁴, o heterocicloalquilo sustituido o no sustituido unido al anillo T o el anillo fenilo a través de un átomo de carbono de R⁴; cada R⁵ es en forma independiente halógeno, -CN, -NO₂, -OH, -OCF₃, -OCH₂F, -OCF₂H, -CF₃, -SR⁸, -NR¹⁰S(=O)₂R⁹, -S(=O)₂N(R¹⁰)₂, -S(=O)R⁹, -S(=O)₂R⁹, -C(=O)R⁹, -OC(=O)R⁹, -CO₂R¹⁰, -N(R¹⁰)₂, -C(=O)N(R¹⁰)₂, -NR¹⁰C(=O)R¹⁰, -NR¹⁰C(=O)OR¹⁰, NR¹⁰C(=O)N(R¹⁰)₂, alquilo sustituido o no sustituido, alcoxi sustituido o no sustituido, heteroalquilo sustituido o no sustituido, o heterocicloalquilo sustituido o no sustituido; o cicloalquilo sustituido o no sustituido; o arilo sustituido o no sustituido; o heteroarilo sustituido o no sustituido; cada R⁸ es en forma independiente H o R⁹; cada R⁹ es en forma independiente alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, heterocicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido, o heteroarilo sustituido o no sustituido; cada R¹⁰ es en forma independiente H, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, heterocicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido, o heteroarilo sustituido o no sustituido; o dos R¹⁰, junto con los átomos a los cuales están unidos forman un heterociclo; y s es 0 - 4.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161555902P | 2011-11-04 | 2011-11-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR089175A1 true AR089175A1 (es) | 2014-08-06 |
Family
ID=48192852
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120104155A AR089175A1 (es) | 2011-11-04 | 2012-11-05 | Inhibidores de pak para el tratamiento de trastornos de proliferacion celular |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US20150031693A1 (es) |
| EP (2) | EP2773642A1 (es) |
| JP (2) | JP2014532724A (es) |
| KR (2) | KR20140105451A (es) |
| CN (2) | CN104039786A (es) |
| AR (1) | AR089175A1 (es) |
| AU (2) | AU2012327187A1 (es) |
| BR (2) | BR112014010420A2 (es) |
| CA (2) | CA2854471A1 (es) |
| CL (2) | CL2014001131A1 (es) |
| CO (1) | CO7030960A2 (es) |
| CR (2) | CR20140250A (es) |
| EA (2) | EA201490927A1 (es) |
| IL (2) | IL232154A0 (es) |
| MA (2) | MA35660B1 (es) |
| MX (2) | MX2014005292A (es) |
| PH (2) | PH12014500956A1 (es) |
| SG (2) | SG11201401914WA (es) |
| TW (1) | TW201326169A (es) |
| WO (2) | WO2013067423A1 (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011156780A2 (en) * | 2010-06-10 | 2011-12-15 | Afraxis, Inc. | 8-(sulfonylbenzyl)pyrido[2,3-d]pyrimidin-7(8h)-ones for the treatment of cns disorders |
| MX343893B (es) | 2011-11-04 | 2016-11-28 | Hoffmann La Roche | Nuevos derivados de aril-quinolina. |
| US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| AU2014228746B2 (en) | 2013-03-15 | 2018-08-30 | Celgene Car Llc | Heteroaryl compounds and uses thereof |
| ES2892423T3 (es) | 2013-03-15 | 2022-02-04 | Celgene Car Llc | Compuestos de heteroarilo y usos de los mismos |
| WO2015011252A1 (en) * | 2013-07-26 | 2015-01-29 | F. Hoffmann-La Roche Ag | Pyrimidine-pyridinone serine/threonine kinase inhibitors |
| PT3102577T (pt) * | 2014-02-07 | 2018-10-23 | Principia Biopharma Inc | Derivados de quinolona como inibidores do recetor do fator de crescimento de fibroblastos |
| JP6631616B2 (ja) | 2014-07-26 | 2020-01-15 | ノース・アンド・サウス・ブラザー・ファーマシー・インベストメント・カンパニー・リミテッド | ＣＤＫ阻害剤としての２−アミノ−ピリド［２，３−ｄ］ピリミジン−７（８Ｈ）−オン誘導体及びその使用 |
| EP3288556A4 (en) | 2015-04-29 | 2018-09-19 | Dexcel Pharma Technologies Ltd. | Orally disintegrating compositions |
| CA3013959C (en) * | 2016-02-17 | 2024-05-28 | Nuralogix Corporation | System and method for detecting physiological state |
| US10076494B2 (en) | 2016-06-16 | 2018-09-18 | Dexcel Pharma Technologies Ltd. | Stable orally disintegrating pharmaceutical compositions |
| WO2017220516A1 (en) * | 2016-06-23 | 2017-12-28 | F. Hoffmann-La Roche Ag | Novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives |
| WO2018013466A2 (en) * | 2016-07-15 | 2018-01-18 | Dana-Farber Cancer Institute, Inc. | Biomarkers predictive of endocrine resistance in breast cancer |
| CN106818805A (zh) * | 2016-12-27 | 2017-06-13 | 东莞市联洲知识产权运营管理有限公司 | 一种天然乙酰胆碱酯酶抑制剂及其杀虫应用 |
| CN107083428B (zh) * | 2017-04-10 | 2020-09-25 | 徐州医科大学 | Pak5在癌症诊断预后治疗及药物筛选中的应用 |
| TWI831829B (zh) | 2018-09-12 | 2024-02-11 | 美商建南德克公司 | 苯氧基-吡啶基-嘧啶化合物及使用方法 |
| WO2020086882A1 (en) * | 2018-10-24 | 2020-04-30 | Northwestern University | Tumor cell aggregation inhibitors' for treating cancer |
| CN113508115A (zh) * | 2019-01-03 | 2021-10-15 | 基因泰克公司 | 吡啶并嘧啶酮和蝶啶酮化合物作为需要酶i(ire i α)的内切核糖核酸酶肌醇的抑制剂用于治疗癌症疾病 |
| CN112213400B (zh) * | 2019-07-09 | 2022-06-07 | 四川弘合生物科技有限公司 | 一种β-榄香烯及其有关物质的检测方法 |
| CN110496128B (zh) * | 2019-09-23 | 2022-09-30 | 吉林大学 | 利培酮或帕潘立酮在制备治疗弥漫性大b细胞淋巴瘤的药物中的应用 |
| AU2021381949A1 (en) | 2020-11-18 | 2023-06-15 | Deciphera Pharmaceuticals, Llc | Gcn2 and perk kinase inhibitors and methods of use thereof |
| WO2022152259A1 (zh) * | 2021-01-15 | 2022-07-21 | 江苏先声药业有限公司 | Cdk2/4/6抑制剂及其制备方法和应用 |
| CN113046323A (zh) * | 2021-04-02 | 2021-06-29 | 四川农业大学 | 一种基于miR-532-5p及其靶基因调控卵巢颗粒细胞的方法 |
| WO2025257301A1 (en) * | 2024-06-13 | 2025-12-18 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | Treatment of neurofibromatosis type 2 by inhibitors of g6pd, acsl3 and/or oxsm |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1201765A3 (en) * | 2000-10-16 | 2003-08-27 | Axxima Pharmaceuticals Aktiengesellschaft | Cellular kinases involved in cytomegalovirus infection and their inhibition |
| WO2008055842A1 (en) * | 2006-11-09 | 2008-05-15 | F. Hoffmann-La Roche Ag | Substituted 6-phenyl-pyrido [2,3-d] pyrimidin-7-one derivatives as kinase inhibitors and methods for using the same |
| EP2112150B1 (en) * | 2008-04-22 | 2013-10-16 | Forma Therapeutics, Inc. | Improved raf inhibitors |
| US8674095B2 (en) * | 2008-12-19 | 2014-03-18 | Afraxis Holdings, Inc. | Compounds for treating neuropsychiatric conditions |
| MX2012004157A (es) * | 2009-10-09 | 2012-08-03 | Afraxis Inc | 8-etil-6-(aril)pirido[2.3-d]pirimidin-7(8h)-onas para el tratamiento de trastornos del snc. |
| US8912203B2 (en) * | 2010-06-09 | 2014-12-16 | Afraxis Holdings, Inc. | 6-(sulfonylaryl)pyrido[2,3-D]pyrimidin-7(8H)-ones for the treatment of CNS disorders |
| WO2011156780A2 (en) * | 2010-06-10 | 2011-12-15 | Afraxis, Inc. | 8-(sulfonylbenzyl)pyrido[2,3-d]pyrimidin-7(8h)-ones for the treatment of cns disorders |
-
2012
- 2012-11-02 MX MX2014005292A patent/MX2014005292A/es not_active Application Discontinuation
- 2012-11-02 CN CN201280066130.4A patent/CN104039786A/zh active Pending
- 2012-11-02 BR BR112014010420A patent/BR112014010420A2/pt not_active Application Discontinuation
- 2012-11-02 WO PCT/US2012/063413 patent/WO2013067423A1/en not_active Ceased
- 2012-11-02 WO PCT/US2012/063426 patent/WO2013067434A1/en not_active Ceased
- 2012-11-02 KR KR1020147014685A patent/KR20140105451A/ko not_active Withdrawn
- 2012-11-02 AU AU2012327187A patent/AU2012327187A1/en not_active Abandoned
- 2012-11-02 CN CN201280066127.2A patent/CN104093717A/zh active Pending
- 2012-11-02 US US14/356,118 patent/US20150031693A1/en not_active Abandoned
- 2012-11-02 PH PH1/2014/500956A patent/PH12014500956A1/en unknown
- 2012-11-02 SG SG11201401914WA patent/SG11201401914WA/en unknown
- 2012-11-02 CA CA2854471A patent/CA2854471A1/en not_active Abandoned
- 2012-11-02 KR KR1020147014683A patent/KR20140096098A/ko not_active Withdrawn
- 2012-11-02 MX MX2014005296A patent/MX2014005296A/es not_active Application Discontinuation
- 2012-11-02 AU AU2012327183A patent/AU2012327183A1/en not_active Abandoned
- 2012-11-02 EP EP12844804.0A patent/EP2773642A1/en not_active Ceased
- 2012-11-02 EA EA201490927A patent/EA201490927A1/ru unknown
- 2012-11-02 SG SG11201401996TA patent/SG11201401996TA/en unknown
- 2012-11-02 US US13/668,079 patent/US20130116263A1/en not_active Abandoned
- 2012-11-02 CA CA2854462A patent/CA2854462A1/en not_active Abandoned
- 2012-11-02 JP JP2014540152A patent/JP2014532724A/ja active Pending
- 2012-11-02 JP JP2014540157A patent/JP2015501786A/ja active Pending
- 2012-11-02 EP EP12845870.0A patent/EP2773643A4/en not_active Withdrawn
- 2012-11-02 BR BR112014010631A patent/BR112014010631A2/pt not_active Application Discontinuation
- 2012-11-02 EA EA201490925A patent/EA201490925A1/ru unknown
- 2012-11-05 TW TW101141080A patent/TW201326169A/zh unknown
- 2012-11-05 AR ARP120104155A patent/AR089175A1/es unknown
-
2014
- 2014-04-22 IL IL232154A patent/IL232154A0/en unknown
- 2014-04-24 IL IL232215A patent/IL232215A0/en unknown
- 2014-04-30 CL CL2014001131A patent/CL2014001131A1/es unknown
- 2014-04-30 CL CL2014001132A patent/CL2014001132A1/es unknown
- 2014-05-02 PH PH12014500995A patent/PH12014500995A1/en unknown
- 2014-05-26 CR CR20140250A patent/CR20140250A/es unknown
- 2014-05-26 CR CR20140251A patent/CR20140251A/es unknown
- 2014-05-26 MA MA37064A patent/MA35660B1/fr unknown
- 2014-05-26 MA MA37065A patent/MA35661B1/fr unknown
- 2014-06-04 CO CO14119704A patent/CO7030960A2/es unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |