BRPI0709773B8 - derivados de malonamida, processo de produção do mesmo, medicamento, e seus usos como inibidores de gama-secretase no tratamento do mal de alzheimer - Google Patents
derivados de malonamida, processo de produção do mesmo, medicamento, e seus usos como inibidores de gama-secretase no tratamento do mal de alzheimerInfo
- Publication number
- BRPI0709773B8 BRPI0709773B8 BRPI0709773A BRPI0709773A BRPI0709773B8 BR PI0709773 B8 BRPI0709773 B8 BR PI0709773B8 BR PI0709773 A BRPI0709773 A BR PI0709773A BR PI0709773 A BRPI0709773 A BR PI0709773A BR PI0709773 B8 BRPI0709773 B8 BR PI0709773B8
- Authority
- BR
- Brazil
- Prior art keywords
- alzheimer
- gamma
- disease
- treatment
- lower alkyl
- Prior art date
Links
- WRIRWRKPLXCTFD-UHFFFAOYSA-N malonamide Chemical class NC(=O)CC(N)=O WRIRWRKPLXCTFD-UHFFFAOYSA-N 0.000 title abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 title abstract 2
- 239000003540 gamma secretase inhibitor Substances 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D223/18—Dibenzazepines; Hydrogenated dibenzazepines
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- 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)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
derivados de malonamida como inibidores de gama-secretase. a presente invenção refere-se a derivados de malonamida de fórmula (i) i em que a1 é-chr- ou -c(o)-; a2 é -c(o)- e r2/r3 são independentemente um do outro hidrogênio, alquila inferior; r é hidrogênio ou alquila inferior substituída com halogênio; r1 é hidrogênio, alquila inferior ou -(ch2)n-arila, opcionalmente substiuído com halogênio; r4 é alquila inferior substituída com halogênio n é 0, 1 ou 2; e a sais de adição de ácido farmaceuticamente adequados, enantiômeros oticamente puros, racematos ou misturas diastereoméricas dos mesmos para o tratamento do mal de alzheimer.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06111771.9 | 2006-03-27 | ||
| EP06111771 | 2006-03-27 | ||
| PCT/EP2007/052557 WO2007110335A1 (en) | 2006-03-27 | 2007-03-19 | Malonamide derivatives as gamma secretase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0709773A2 BRPI0709773A2 (pt) | 2011-07-26 |
| BRPI0709773B1 BRPI0709773B1 (pt) | 2020-09-15 |
| BRPI0709773B8 true BRPI0709773B8 (pt) | 2021-05-25 |
Family
ID=36843221
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0709773A BRPI0709773B8 (pt) | 2006-03-27 | 2007-03-19 | derivados de malonamida, processo de produção do mesmo, medicamento, e seus usos como inibidores de gama-secretase no tratamento do mal de alzheimer |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7425551B2 (pt) |
| EP (1) | EP2018368B1 (pt) |
| JP (1) | JP5129231B2 (pt) |
| KR (1) | KR101169628B1 (pt) |
| CN (1) | CN101410378B (pt) |
| AR (1) | AR060125A1 (pt) |
| AU (1) | AU2007229550B2 (pt) |
| BR (1) | BRPI0709773B8 (pt) |
| CA (1) | CA2645756C (pt) |
| CL (1) | CL2007000789A1 (pt) |
| ES (1) | ES2398531T3 (pt) |
| IL (1) | IL194054A (pt) |
| MX (1) | MX2008012136A (pt) |
| NO (1) | NO20083917L (pt) |
| RU (1) | RU2440342C2 (pt) |
| TW (1) | TW200740760A (pt) |
| WO (1) | WO2007110335A1 (pt) |
| ZA (1) | ZA200808190B (pt) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010509235A (ja) * | 2006-11-03 | 2010-03-25 | ノースウェスタン ユニバーシティ | 多発性硬化症の治療 |
| KR101150574B1 (ko) * | 2007-02-02 | 2012-05-30 | 에프. 호프만-라 로슈 아게 | 6-옥소-6,7-다이하이드로-5ｈ-다이벤조［ｂ,ｄ］아제핀-7-일 유도체 |
| FR2913886B1 (fr) | 2007-03-22 | 2012-03-02 | Guerbet Sa | Utilisation de nanoparticules metalliques dans le diagnostique de la maladie d'alzheimer |
| US8309299B2 (en) * | 2010-05-19 | 2012-11-13 | Hoffmann-La Roche Inc. | Combination therapy and method for assessing resistance to treatment |
| TWI530489B (zh) | 2011-03-22 | 2016-04-21 | 必治妥美雅史谷比公司 | 雙（氟烷基）－１，４－苯二氮呯酮化合物 |
| AR087107A1 (es) | 2011-07-27 | 2014-02-12 | Lilly Co Eli | Compuesto inhibidor de la señalizacion de la trayectoria notch |
| JO3491B1 (ar) | 2015-07-07 | 2020-07-05 | Audion Therapeutics | مركبات مثبطة لإشارات مسار notch |
| WO2022020658A1 (en) * | 2020-07-23 | 2022-01-27 | Purdue Research Foundation | Notch signaling inhibitors for treating obesity and metabolic disorders |
| US20240400531A1 (en) * | 2021-08-31 | 2024-12-05 | Basf Se | Herbicidal malonamides containing a condensed ring system |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| 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 |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (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 |
| WO2026015801A1 (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 |
| WO2026015790A1 (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 |
| 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 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SU1404505A1 (ru) * | 1987-01-22 | 1988-06-23 | Томский политехнический институт им.С.М.Кирова | Способ получени 6,7-дигидро-5н-дибенз (с, @ )азепин-7-она |
| WO2001077086A1 (en) * | 2000-04-11 | 2001-10-18 | Dupont Pharmaceuticals Company | SUBSTITUTED LACTAMS AS INHIBITORS OF Aβ PROTEIN PRODUCTION |
| CN1386118A (zh) * | 2000-06-01 | 2002-12-18 | 布里斯托尔-迈尔斯斯奎布药品公司 | 作为Aβ蛋白产生抑制剂的被环状琥珀酸酯取代的内酰胺类化合物 |
| TW200502221A (en) * | 2002-10-03 | 2005-01-16 | Astrazeneca Ab | Novel lactams and uses thereof |
| EP1592684B1 (en) | 2003-02-04 | 2008-07-30 | F. Hoffmann-La Roche Ag | Malonamide derivatives as gamma-secretase inhibitors |
| KR100838852B1 (ko) * | 2003-09-09 | 2008-06-16 | 에프. 호프만-라 로슈 아게 | 감마-세크리테이즈의 활성을 차단하는 말론아미드 유도체 |
| SI1673347T1 (sl) * | 2003-10-06 | 2015-10-30 | F. Hoffmann - La Roche Ag | Substituirani derivati dibenzo-azepina in benzo-diazepina, ki so uporabni kot inhibitorji gama-sekretaze |
-
2007
- 2007-03-19 ES ES07727035T patent/ES2398531T3/es active Active
- 2007-03-19 CN CN2007800103966A patent/CN101410378B/zh active Active
- 2007-03-19 KR KR1020087023614A patent/KR101169628B1/ko active Active
- 2007-03-19 RU RU2008142361/04A patent/RU2440342C2/ru not_active IP Right Cessation
- 2007-03-19 CA CA2645756A patent/CA2645756C/en active Active
- 2007-03-19 WO PCT/EP2007/052557 patent/WO2007110335A1/en not_active Ceased
- 2007-03-19 AU AU2007229550A patent/AU2007229550B2/en active Active
- 2007-03-19 EP EP07727035A patent/EP2018368B1/en active Active
- 2007-03-19 BR BRPI0709773A patent/BRPI0709773B8/pt active IP Right Grant
- 2007-03-19 MX MX2008012136A patent/MX2008012136A/es active IP Right Grant
- 2007-03-19 JP JP2009502013A patent/JP5129231B2/ja active Active
- 2007-03-22 US US11/726,639 patent/US7425551B2/en active Active
- 2007-03-23 TW TW096110174A patent/TW200740760A/zh unknown
- 2007-03-26 CL CL2007000789A patent/CL2007000789A1/es unknown
- 2007-03-26 AR ARP070101236A patent/AR060125A1/es not_active Application Discontinuation
-
2008
- 2008-09-11 IL IL194054A patent/IL194054A/en active IP Right Grant
- 2008-09-15 NO NO20083917A patent/NO20083917L/no not_active Application Discontinuation
- 2008-09-23 ZA ZA200808190A patent/ZA200808190B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP2018368A1 (en) | 2009-01-28 |
| US20070225273A1 (en) | 2007-09-27 |
| US7425551B2 (en) | 2008-09-16 |
| WO2007110335A1 (en) | 2007-10-04 |
| JP2009531369A (ja) | 2009-09-03 |
| JP5129231B2 (ja) | 2013-01-30 |
| TW200740760A (en) | 2007-11-01 |
| IL194054A (en) | 2013-05-30 |
| RU2440342C2 (ru) | 2012-01-20 |
| KR101169628B1 (ko) | 2012-07-30 |
| BRPI0709773B1 (pt) | 2020-09-15 |
| CN101410378B (zh) | 2012-12-05 |
| BRPI0709773A2 (pt) | 2011-07-26 |
| AR060125A1 (es) | 2008-05-28 |
| CA2645756C (en) | 2013-12-31 |
| AU2007229550B2 (en) | 2012-03-08 |
| AU2007229550A1 (en) | 2007-10-04 |
| RU2008142361A (ru) | 2010-05-10 |
| KR20080098441A (ko) | 2008-11-07 |
| CN101410378A (zh) | 2009-04-15 |
| ES2398531T3 (es) | 2013-03-20 |
| ZA200808190B (en) | 2009-08-26 |
| EP2018368B1 (en) | 2012-12-05 |
| NO20083917L (no) | 2008-10-23 |
| CL2007000789A1 (es) | 2008-01-18 |
| CA2645756A1 (en) | 2007-10-04 |
| MX2008012136A (es) | 2008-10-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 15/09/2020, OBSERVADAS AS CONDICOES LEGAIS. |
|
| B16C | Correction of notification of the grant [chapter 16.3 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 19/03/2007 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF |