PE20120506A1 - Derivados de pirazolopiridina como inhibidores de quinasas - Google Patents
Derivados de pirazolopiridina como inhibidores de quinasasInfo
- Publication number
- PE20120506A1 PE20120506A1 PE2011001662A PE2011001662A PE20120506A1 PE 20120506 A1 PE20120506 A1 PE 20120506A1 PE 2011001662 A PE2011001662 A PE 2011001662A PE 2011001662 A PE2011001662 A PE 2011001662A PE 20120506 A1 PE20120506 A1 PE 20120506A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- pyridin
- amine
- cycloalkyl
- kinase inhibitors
- Prior art date
Links
- 150000005229 pyrazolopyridines Chemical class 0.000 title abstract 2
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- XKVUYEYANWFIJX-UHFFFAOYSA-N 5-methyl-1h-pyrazole Chemical compound CC1=CC=NN1 XKVUYEYANWFIJX-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- CIEWGZJDEDBECJ-UHFFFAOYSA-N 1-chloro-4-methylbenzene Chemical class [CH2]C1=CC=C(Cl)C=C1 CIEWGZJDEDBECJ-UHFFFAOYSA-N 0.000 abstract 1
- 101100294106 Caenorhabditis elegans nhr-3 gene Proteins 0.000 abstract 1
- 102000009784 Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Human genes 0.000 abstract 1
- 108010020246 Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 108060006633 protein kinase Proteins 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65611—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system (X = CH2, O, S, NH) optionally with an additional double bond and/or substituents, e.g. penicillins and analogs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Epidemiology (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 (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0904746A GB0904746D0 (en) | 2009-03-19 | 2009-03-19 | Compounds |
| US16202409P | 2009-03-20 | 2009-03-20 | |
| GB0912238A GB0912238D0 (en) | 2009-07-14 | 2009-07-14 | Compounds |
| GBGB1001418.1A GB201001418D0 (en) | 2010-01-28 | 2010-01-28 | Compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20120506A1 true PE20120506A1 (es) | 2012-05-14 |
Family
ID=42226628
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011001662A PE20120506A1 (es) | 2009-03-19 | 2010-03-19 | Derivados de pirazolopiridina como inhibidores de quinasas |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US20100317646A1 (https=) |
| EP (1) | EP2408772B1 (https=) |
| JP (1) | JP5732036B2 (https=) |
| KR (1) | KR101700229B1 (https=) |
| CN (1) | CN102428084B (https=) |
| AU (1) | AU2010224693B2 (https=) |
| CA (1) | CA2754605C (https=) |
| CL (1) | CL2011002267A1 (https=) |
| IL (1) | IL215147A0 (https=) |
| MX (1) | MX2011009807A (https=) |
| PE (1) | PE20120506A1 (https=) |
| RU (1) | RU2011142182A (https=) |
| WO (1) | WO2010106333A1 (https=) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2658984C (en) * | 2006-08-16 | 2014-12-02 | Joshua Kennedy-Smith | Non-nucleoside reverse transcriptase inhibitors |
| GB201008134D0 (en) * | 2010-05-14 | 2010-06-30 | Medical Res Council Technology | Compounds |
| GB201015949D0 (en) * | 2010-09-22 | 2010-11-03 | Medical Res Council Technology | Compounds |
| US9233977B2 (en) * | 2010-10-29 | 2016-01-12 | Merck Sharp & Dohme Corp. | Leucine-rich repeat kinase enzyme activity |
| WO2012118679A1 (en) | 2011-02-28 | 2012-09-07 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| WO2012135631A1 (en) | 2011-03-30 | 2012-10-04 | Arrien Pharmaeuticals Llc | Substituted 5-(pyrazin-2-yl)-1h-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors |
| EP2699572B1 (en) * | 2011-04-21 | 2016-08-10 | Origenis GmbH | Heterocyclic compounds as kinase inhibitors |
| AU2012258977A1 (en) | 2011-05-23 | 2014-01-16 | Imago Pharmaceuticals, Inc. | Inhibitors of LRRK2 kinase activity |
| CN102558174B (zh) * | 2011-08-23 | 2014-03-19 | 天津市斯芬克司药物研发有限公司 | 一种全新吡唑并[4,3-c]吡啶化合物的发明及其合成方法 |
| BR112014007654A8 (pt) * | 2011-09-30 | 2018-06-12 | Ipsen Pharma | Inibidores de lrrk2 quinase macrocíclicos. |
| GB201204985D0 (en) | 2012-03-21 | 2012-05-02 | Genentech Inc | Compounds |
| WO2013182612A1 (en) | 2012-06-07 | 2013-12-12 | Bayer Pharma Aktiengesellschaft | Glucose transport inhibitors |
| WO2014001973A1 (en) * | 2012-06-29 | 2014-01-03 | Pfizer Inc. | NOVEL 4-(SUBSTITUTED-AMINO)-7H-PYRROLO[2,3-d]PYRIMIDINES AS LRRK2 INHIBITORS |
| WO2014026330A1 (en) * | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| US10000482B2 (en) | 2012-10-19 | 2018-06-19 | Origenis Gmbh | Kinase inhibitors |
| EP2914597B1 (en) * | 2012-10-31 | 2017-12-06 | RaQualia Pharma Inc | Pyrazolopyridine derivatives as ttx-s blockers |
| MD20150037A2 (ro) * | 2012-11-08 | 2015-11-30 | Pfizer Inc. | Compuşi heteroaromatici şi utilizarea lor ca liganzi de dopamină D1 |
| EP2968995B1 (en) * | 2013-03-15 | 2018-05-09 | Elan Pharmaceuticals LLC | Inhibitors of lrrk2 kinase activity |
| US9045477B2 (en) * | 2013-03-15 | 2015-06-02 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| TW201533043A (zh) * | 2013-04-18 | 2015-09-01 | Lundbeck & Co As H | 作爲lrrk2抑制劑的芳基吡咯并吡啶衍生化合物 |
| TW201534597A (zh) | 2013-06-20 | 2015-09-16 | Ab Science | 作為選擇性蛋白質激酶抑制劑之苯并咪唑衍生物 |
| WO2015026683A1 (en) * | 2013-08-22 | 2015-02-26 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| JP6487921B2 (ja) | 2013-12-17 | 2019-03-20 | ファイザー・インク | LRRK2阻害薬としての新規の3,4−二置換−1H−ピロロ[2,3−b]ピリジンおよび4,5−二置換−7H−ピロロ[2,3−c]ピリダジン |
| EP3134405B1 (en) | 2014-04-25 | 2019-08-28 | Pfizer Inc | Heteroaromatic compounds and their use as dopamine d1 ligands |
| CR20160525A (es) * | 2014-05-14 | 2016-12-20 | Pfizer | Pirazolopiridinas y pirazolopirimidinas |
| WO2016036586A1 (en) * | 2014-09-03 | 2016-03-10 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| KR102161364B1 (ko) | 2015-09-14 | 2020-09-29 | 화이자 인코포레이티드 | LRRK2 억제제로서 이미다조[4,5-c]퀴놀린 및 이미다조[4,5-c][1,5]나프티리딘 유도체 |
| WO2017215600A1 (en) | 2016-06-15 | 2017-12-21 | Suzhou Yabao Pharmaceutical R&D Co., Ltd. | Substituted tricyclic herteocyclic compounds and use thereof |
| KR101923852B1 (ko) | 2017-02-24 | 2018-11-29 | 재단법인 대구경북첨단의료산업진흥재단 | 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물 |
| WO2019134985A1 (en) | 2018-01-08 | 2019-07-11 | F. Hoffmann-La Roche Ag | Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors |
| KR101990738B1 (ko) * | 2018-07-24 | 2019-06-19 | 재단법인 대구경북첨단의료산업진흥재단 | 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물 |
| AU2020395783A1 (en) * | 2019-12-04 | 2022-06-09 | Arcus Biosciences, Inc. | Inhibitors of HIF-2alpha |
| CR20220644A (es) | 2020-06-22 | 2023-02-17 | Hoffmann La Roche | Derivados de sulfona |
| MX2023002224A (es) * | 2020-09-03 | 2023-03-15 | Hoffmann La Roche | Compuestos heterociclicos. |
| AU2023225858B2 (en) * | 2022-02-25 | 2026-03-19 | Suzhou Yabao Pharmaceutical R & D Co., Ltd. | Substituted fused ring compound, pharmaceutical composition thereof, preparation method therefor and uses thereof |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3835144A (en) * | 1972-06-16 | 1974-09-10 | Squibb & Sons Inc | Amino derivatives of (4,3-c pyrazolopyridine cabroxylic acids and esters |
| NZ207394A (en) | 1983-03-08 | 1987-03-06 | Commw Serum Lab Commission | Detecting or determining sequence of amino acids |
| US5478830A (en) * | 1992-05-29 | 1995-12-26 | The Du Pont Merck Pharmaceutical Company | Fused-ring heterocycles for the treatment of atherosclerosis |
| US5300478A (en) * | 1993-01-28 | 1994-04-05 | Zeneca Limited | Substituted fused pyrazolo compounds |
| CA2482838A1 (en) * | 2002-05-31 | 2003-12-11 | Eisai Co., Ltd. | Pyrazole compounds and pharmaceutical compositions containing the compound |
| EP1545515A1 (en) * | 2002-08-12 | 2005-06-29 | Sugen, Inc. | 3-pyrrolyl-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors |
| US7348338B2 (en) * | 2003-07-17 | 2008-03-25 | Plexxikon, Inc. | PPAR active compounds |
| EP1653946A4 (en) * | 2003-08-06 | 2007-04-04 | Sugen Inc | 3-CYCLOPENTYLIDENE-1,3-DIHYDROINDOL-2-ONES GEOMETRICALLY LIMITED AS POWERFUL INHIBITORS OF PROTEIN KINASES |
| WO2005121094A1 (en) * | 2004-06-09 | 2005-12-22 | Pfizer Limited | Piperazine and piperidine derivatives as anti-hiv-agents |
| WO2006009245A1 (ja) * | 2004-07-23 | 2006-01-26 | Tanabe Seiyaku Co., Ltd. | 含窒素縮合二環式化合物 |
| PE20061119A1 (es) * | 2005-01-19 | 2006-11-27 | Aventis Pharma Sa | PIRAZOLO PIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE CINASAS FAK, KDR Y Tie |
| US7553639B2 (en) * | 2006-01-31 | 2009-06-30 | Elan Pharma International Limited | Alpha-synuclein kinase |
| CA2647543A1 (en) * | 2006-03-29 | 2007-11-08 | Foldrx Pharmaceuticals, Inc. | Inhibition of alpha-synuclein toxicity |
| EP2346868B1 (en) * | 2008-09-26 | 2016-01-27 | Boehringer Ingelheim International Gmbh | Azaindazole compounds as ccr1 receptor antagonists |
| GB201015949D0 (en) * | 2010-09-22 | 2010-11-03 | Medical Res Council Technology | Compounds |
-
2010
- 2010-03-19 MX MX2011009807A patent/MX2011009807A/es not_active Application Discontinuation
- 2010-03-19 US US12/727,754 patent/US20100317646A1/en not_active Abandoned
- 2010-03-19 CN CN201080021866.0A patent/CN102428084B/zh active Active
- 2010-03-19 PE PE2011001662A patent/PE20120506A1/es not_active Application Discontinuation
- 2010-03-19 WO PCT/GB2010/000498 patent/WO2010106333A1/en not_active Ceased
- 2010-03-19 CA CA2754605A patent/CA2754605C/en not_active Expired - Fee Related
- 2010-03-19 EP EP10711443.1A patent/EP2408772B1/en not_active Not-in-force
- 2010-03-19 JP JP2012500308A patent/JP5732036B2/ja not_active Expired - Fee Related
- 2010-03-19 AU AU2010224693A patent/AU2010224693B2/en not_active Ceased
- 2010-03-19 RU RU2011142182/04A patent/RU2011142182A/ru unknown
- 2010-03-19 KR KR1020117024068A patent/KR101700229B1/ko not_active Expired - Fee Related
-
2011
- 2011-09-13 CL CL2011002267A patent/CL2011002267A1/es unknown
- 2011-09-14 IL IL215147A patent/IL215147A0/en unknown
-
2017
- 2017-04-03 US US15/478,141 patent/US20170320870A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2010106333A1 (en) | 2010-09-23 |
| IL215147A0 (en) | 2011-12-29 |
| EP2408772B1 (en) | 2015-07-01 |
| CN102428084A (zh) | 2012-04-25 |
| KR101700229B1 (ko) | 2017-01-26 |
| CA2754605A1 (en) | 2010-09-23 |
| AU2010224693A1 (en) | 2011-09-15 |
| JP2012520861A (ja) | 2012-09-10 |
| JP5732036B2 (ja) | 2015-06-10 |
| RU2011142182A (ru) | 2013-04-27 |
| CA2754605C (en) | 2018-04-17 |
| CL2011002267A1 (es) | 2012-05-11 |
| EP2408772A1 (en) | 2012-01-25 |
| KR20110128925A (ko) | 2011-11-30 |
| AU2010224693B2 (en) | 2016-07-28 |
| US20170320870A1 (en) | 2017-11-09 |
| MX2011009807A (es) | 2011-09-29 |
| CN102428084B (zh) | 2016-05-18 |
| US20100317646A1 (en) | 2010-12-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |