ECSP109845A - Inhibidores tetrahidropiranocromeno de gamma secretasa - Google Patents
Inhibidores tetrahidropiranocromeno de gamma secretasaInfo
- Publication number
- ECSP109845A ECSP109845A EC2010009845A ECSP109845A ECSP109845A EC SP109845 A ECSP109845 A EC SP109845A EC 2010009845 A EC2010009845 A EC 2010009845A EC SP109845 A ECSP109845 A EC SP109845A EC SP109845 A ECSP109845 A EC SP109845A
- Authority
- EC
- Ecuador
- Prior art keywords
- tertiary amine
- gamma secretase
- basic tertiary
- heteroaryl
- basic
- Prior art date
Links
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003512 tertiary amines Chemical class 0.000 abstract 5
- 238000000034 method Methods 0.000 abstract 4
- 239000000203 mixture Substances 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 150000001299 aldehydes Chemical class 0.000 abstract 1
- 150000001336 alkenes Chemical class 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 239000005667 attractant Substances 0.000 abstract 1
- 230000031902 chemoattractant activity Effects 0.000 abstract 1
- 239000003540 gamma secretase inhibitor Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 150000002576 ketones Chemical class 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- -1 sulfonyl anhydride Chemical class 0.000 abstract 1
- 150000003461 sulfonyl halides Chemical class 0.000 abstract 1
- YBBRCQOCSYXUOC-UHFFFAOYSA-N sulfuryl dichloride Chemical compound ClS(Cl)(=O)=O YBBRCQOCSYXUOC-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—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
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/78—Ring systems having three or more relevant rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (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)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyrane Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
Se describen nuevos inhibidores de gamma secretasa de la fórmula: .También se describen métodos de inhibir la gamma-secretasa, métodos de tratar enfermedades neurodegenerativas, y métodos de tratar enfermedad de Alzheimer. También se describen procesos para preparar alquenos en un paso de reacción usando una mezcla de un aldehído (o cetona) y un alquilo sustituido con dos grupos atrayentes de electrones y la reacción de la mezcla con: (a) un haluro de sulfonilo (por ej., un cloruro de sulfonilo) y una amina terciaria básica, o, (b) un anhídrido de sulfonilo y una amina básica, o (c) un aril-C(O)-haluro y una amina terciaria básica, o (d) un aril-C(O)-O-C(O)-arilo y una amina terciaria básica, o (e) un heteroaril-C(O)-haluro y una amina terciaria básica, o (f) un heteroaril-C(O)-O-C(O)-heteroarilo y una amina terciaria básica.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94803307P | 2007-07-05 | 2007-07-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP109845A true ECSP109845A (es) | 2010-02-26 |
Family
ID=39830164
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2010009845A ECSP109845A (es) | 2007-07-05 | 2010-01-05 | Inhibidores tetrahidropiranocromeno de gamma secretasa |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8664411B2 (es) |
| EP (1) | EP2435416B1 (es) |
| JP (1) | JP5240871B2 (es) |
| KR (1) | KR20100044197A (es) |
| CN (1) | CN101754960A (es) |
| AR (1) | AR067445A1 (es) |
| AU (1) | AU2008275735B2 (es) |
| BR (1) | BRPI0814256A8 (es) |
| CA (1) | CA2691542A1 (es) |
| CL (1) | CL2008001960A1 (es) |
| CO (1) | CO6270309A2 (es) |
| EC (1) | ECSP109845A (es) |
| PE (1) | PE20090435A1 (es) |
| RU (1) | RU2483061C2 (es) |
| TW (1) | TW200908959A (es) |
| WO (1) | WO2009008980A2 (es) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR059075A1 (es) | 2006-01-20 | 2008-03-12 | Schering Corp | Bencesulfonil - cromano , tiocromano tetrahidronaftaleno e inhibidores de gamma secretasa relacionados |
| US8618123B2 (en) * | 2007-07-17 | 2013-12-31 | Merck Sharp & Dohme Corp. | Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors |
| PL2475428T3 (pl) | 2009-09-11 | 2015-12-31 | Probiodrug Ag | Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej |
| WO2012040444A2 (en) * | 2010-09-24 | 2012-03-29 | Bristol-Myers Squibb Company | Treatment of patients with incipient alzheimer's disease |
| WO2012138678A1 (en) * | 2011-04-04 | 2012-10-11 | Merck Sharp & Dohme Corp. | Gamma secretase inhibitors |
| US9226927B2 (en) * | 2011-09-09 | 2016-01-05 | Merck Sharp & Dohme Corp. | Gamma secretase inhibitors |
| EP2925313A4 (en) | 2012-11-29 | 2016-05-11 | Merck Sharp & Dohme | SPIROCYCLIC SULPHONES AS GAMMA SECRETASE INHIBITORS |
| WO2014096212A1 (en) | 2012-12-20 | 2014-06-26 | Janssen Pharmaceutica Nv | NOVEL TRICYCLIC 3,4-DIHYDRO-2H-PYRIDO[1,2-α]PYRAZINE-1,6-DIONE DERIVATIVES AS GAMMA SECRETASE MODULATORS |
| KR102171710B1 (ko) | 2013-01-17 | 2020-10-30 | 얀센 파마슈티카 엔.브이. | 감마 세크레타제 조절 인자로서의 신규 치환 피리도-피페라지논 유도체 |
| US10562897B2 (en) | 2014-01-16 | 2020-02-18 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
| MX2019005384A (es) * | 2016-11-09 | 2019-08-12 | Squibb Bristol Myers Co | Sulfonas triciclicas como moduladores del receptor huerfano relacionado con retinoide (ror) gamma. |
| WO2018226992A1 (en) | 2017-06-07 | 2018-12-13 | Adrx, Inc. | Tau aggregation inhibitors |
| CN111201030B (zh) | 2017-07-25 | 2024-11-01 | 真和制药有限公司 | 通过阻断tim-3和其配体的相互作用治疗癌症 |
| CA3073062A1 (en) | 2017-08-18 | 2019-02-21 | Adrx, Inc. | Tau aggregation peptide inhibitors |
| PL3461819T3 (pl) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitory cyklazy glutaminylowej |
| KR20210124308A (ko) | 2019-01-30 | 2021-10-14 | 트루바인딩 아이엔씨. | 항-gal3 항체 및 이의 용도 |
| MX2022014786A (es) | 2020-05-26 | 2023-01-16 | Truebinding Inc | Metodos para tratar enfermedades inflamatorias mediante el bloqueo de galectina-3. |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1348442A (zh) | 1999-02-26 | 2002-05-08 | 默克公司 | 新的磺胺化合物及其应用 |
| FR2827590B1 (fr) * | 2001-07-18 | 2003-10-24 | Atuser | Transbordeur de liquides alimentaires usages |
| GB0108591D0 (en) * | 2001-04-05 | 2001-05-23 | Merck Sharp & Dohme | Therapeutic agents |
| MXPA04001014A (es) | 2001-08-03 | 2004-05-27 | Schering Corp | Novedosos inhibidores de la gama secretasa. |
| RU2202370C1 (ru) * | 2001-12-26 | 2003-04-20 | Эпштейн Олег Ильич | Нейропсихотропное лекарственное средство |
| GB0222833D0 (en) | 2002-10-02 | 2002-11-06 | Syngenta Ltd | Chemical process |
| GB0223039D0 (en) | 2002-10-04 | 2002-11-13 | Merck Sharp & Dohme | Therapeutic compounds |
| KR20060013404A (ko) | 2003-05-16 | 2006-02-09 | 머크 샤프 앤드 돔 리미티드 | γ-세크레타제 억제용 사이클릭 설폰아미드 |
| GB0317491D0 (en) * | 2003-07-25 | 2003-08-27 | Novartis Ag | Organic compounds |
| DE102005062098A1 (de) * | 2005-12-22 | 2007-06-28 | Merck Patent Gmbh | Oxaphenanthren-Derivate |
| AR059075A1 (es) * | 2006-01-20 | 2008-03-12 | Schering Corp | Bencesulfonil - cromano , tiocromano tetrahidronaftaleno e inhibidores de gamma secretasa relacionados |
| TW200813054A (en) * | 2006-06-02 | 2008-03-16 | Elan Pharm Inc | Fused, tricyclic sulfonamide inhibitors of gamma secretase |
| JP5503663B2 (ja) | 2008-11-13 | 2014-05-28 | メルク・シャープ・アンド・ドーム・コーポレーション | ガンマセクレターゼモジュレータ |
-
2008
- 2008-07-01 EP EP08768856.0A patent/EP2435416B1/en active Active
- 2008-07-01 KR KR1020107002496A patent/KR20100044197A/ko not_active Withdrawn
- 2008-07-01 CN CN200880023464A patent/CN101754960A/zh active Pending
- 2008-07-01 RU RU2010103716/04A patent/RU2483061C2/ru not_active IP Right Cessation
- 2008-07-01 WO PCT/US2008/008192 patent/WO2009008980A2/en not_active Ceased
- 2008-07-01 JP JP2010514862A patent/JP5240871B2/ja not_active Expired - Fee Related
- 2008-07-01 BR BRPI0814256A patent/BRPI0814256A8/pt not_active IP Right Cessation
- 2008-07-01 AU AU2008275735A patent/AU2008275735B2/en not_active Ceased
- 2008-07-01 US US12/665,580 patent/US8664411B2/en active Active
- 2008-07-01 CA CA002691542A patent/CA2691542A1/en not_active Abandoned
- 2008-07-02 TW TW097124900A patent/TW200908959A/zh unknown
- 2008-07-02 AR ARP080102867A patent/AR067445A1/es not_active Application Discontinuation
- 2008-07-02 PE PE2008001121A patent/PE20090435A1/es not_active Application Discontinuation
- 2008-07-02 CL CL2008001960A patent/CL2008001960A1/es unknown
-
2009
- 2009-12-30 CO CO09149364A patent/CO6270309A2/es not_active Application Discontinuation
-
2010
- 2010-01-05 EC EC2010009845A patent/ECSP109845A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN101754960A (zh) | 2010-06-23 |
| JP2010532359A (ja) | 2010-10-07 |
| US8664411B2 (en) | 2014-03-04 |
| BRPI0814256A2 (pt) | 2015-02-03 |
| US20110236400A1 (en) | 2011-09-29 |
| CA2691542A1 (en) | 2009-01-15 |
| WO2009008980A2 (en) | 2009-01-15 |
| JP5240871B2 (ja) | 2013-07-17 |
| AU2008275735A2 (en) | 2010-02-11 |
| RU2010103716A (ru) | 2011-08-10 |
| WO2009008980A3 (en) | 2009-03-19 |
| EP2435416A2 (en) | 2012-04-04 |
| CO6270309A2 (es) | 2011-04-20 |
| PE20090435A1 (es) | 2009-04-18 |
| TW200908959A (en) | 2009-03-01 |
| BRPI0814256A8 (pt) | 2016-02-10 |
| AR067445A1 (es) | 2009-10-14 |
| RU2483061C2 (ru) | 2013-05-27 |
| CL2008001960A1 (es) | 2009-11-27 |
| KR20100044197A (ko) | 2010-04-29 |
| AU2008275735A1 (en) | 2009-01-15 |
| EP2435416B1 (en) | 2016-03-30 |
| AU2008275735B2 (en) | 2014-03-27 |
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