SA518400660B1 - مركبات بيرميدين-2-يل أمينو -1h- بيرازول في صورة مثبطات لاستخدامها في علاج الاضطرابات التنكسية العصبيةlrrk2 - Google Patents
مركبات بيرميدين-2-يل أمينو -1h- بيرازول في صورة مثبطات لاستخدامها في علاج الاضطرابات التنكسية العصبيةlrrk2Info
- Publication number
- SA518400660B1 SA518400660B1 SA518400660A SA518400660A SA518400660B1 SA 518400660 B1 SA518400660 B1 SA 518400660B1 SA 518400660 A SA518400660 A SA 518400660A SA 518400660 A SA518400660 A SA 518400660A SA 518400660 B1 SA518400660 B1 SA 518400660B1
- Authority
- SA
- Saudi Arabia
- Prior art keywords
- pyrazols
- ylamino
- pyrimidin
- treatment
- neurodegenerative disorders
- Prior art date
Links
- 229940124786 LRRK2 inhibitor Drugs 0.000 title abstract 2
- YZVIWEZBAJAZOB-UHFFFAOYSA-N N-pyrazol-1-ylpyrimidin-2-amine Chemical class N1=C(N=CC=C1)NN1N=CC=C1 YZVIWEZBAJAZOB-UHFFFAOYSA-N 0.000 title 1
- 208000015122 neurodegenerative disease Diseases 0.000 title 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- 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
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- 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
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- 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]
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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
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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
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
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- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/20—Spiro-condensed systems
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Abstract
يتعلق الاختراع الحالي بوجهٍ عام بمثبطات inhibitors LRRK2، أو ملح salt أو نظير معالج بالديوتيريوم deuterated analog أو عقار أولي prodrug أو مماثل كيميائي tautomer أو متجاسم stereoisomer أو خليط متجاسمات stereoisomers مقبول صيدليًا منها، وطرق تحضيرها واستخدامها. (الصيغة (I)) (I)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662350876P | 2016-06-16 | 2016-06-16 | |
| US201662417151P | 2016-11-03 | 2016-11-03 | |
| US201762476581P | 2017-03-24 | 2017-03-24 | |
| US201762510711P | 2017-05-24 | 2017-05-24 | |
| PCT/US2017/037782 WO2017218843A1 (en) | 2016-06-16 | 2017-06-15 | Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SA518400660B1 true SA518400660B1 (ar) | 2023-06-04 |
Family
ID=59216078
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SA521430638A SA521430638B1 (ar) | 2016-06-16 | 2018-12-13 | H مركبات بيرميدين-2-يل أمينو-1 lrrk2 بيرازول في صورة مثبطات لاستخدامها في علاج الاضطرابات التنكسية العصبية |
| SA518400660A SA518400660B1 (ar) | 2016-06-16 | 2018-12-13 | مركبات بيرميدين-2-يل أمينو -1h- بيرازول في صورة مثبطات لاستخدامها في علاج الاضطرابات التنكسية العصبيةlrrk2 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SA521430638A SA521430638B1 (ar) | 2016-06-16 | 2018-12-13 | H مركبات بيرميدين-2-يل أمينو-1 lrrk2 بيرازول في صورة مثبطات لاستخدامها في علاج الاضطرابات التنكسية العصبية |
Country Status (36)
| Country | Link |
|---|---|
| US (6) | US20170362206A1 (ar) |
| EP (2) | EP3472153B1 (ar) |
| JP (1) | JP7004459B2 (ar) |
| KR (2) | KR102553188B1 (ar) |
| CN (2) | CN114315819A (ar) |
| AU (2) | AU2017286653B2 (ar) |
| BR (1) | BR112018075569A2 (ar) |
| CA (1) | CA3025672A1 (ar) |
| CL (1) | CL2018003597A1 (ar) |
| CO (1) | CO2018013585A2 (ar) |
| CR (2) | CR20180592A (ar) |
| CU (1) | CU24605B1 (ar) |
| CY (1) | CY1124789T1 (ar) |
| DO (2) | DOP2018000285A (ar) |
| EC (1) | ECSP18092481A (ar) |
| ES (1) | ES2900368T3 (ar) |
| HR (1) | HRP20211923T1 (ar) |
| HU (1) | HUE056678T2 (ar) |
| IL (3) | IL299412A (ar) |
| JO (1) | JOP20180113B1 (ar) |
| LT (1) | LT3472153T (ar) |
| MD (1) | MD3472153T2 (ar) |
| MX (3) | MX2018015630A (ar) |
| PE (2) | PE20190395A1 (ar) |
| PH (1) | PH12018502427A1 (ar) |
| PL (1) | PL3472153T3 (ar) |
| PT (1) | PT3472153T (ar) |
| RS (1) | RS62868B1 (ar) |
| SA (2) | SA521430638B1 (ar) |
| SG (2) | SG11201810579YA (ar) |
| SI (1) | SI3472153T1 (ar) |
| TN (1) | TN2018000422A1 (ar) |
| TW (1) | TWI786049B (ar) |
| UA (1) | UA126231C2 (ar) |
| WO (1) | WO2017218843A1 (ar) |
| ZA (1) | ZA201900229B (ar) |
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| WO2017156493A1 (en) | 2016-03-11 | 2017-09-14 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
| US11214565B2 (en) | 2015-11-20 | 2022-01-04 | Denali Therapeutics Inc. | Compound, compositions, and methods |
| RS62868B1 (sr) | 2016-06-16 | 2022-02-28 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1h-pirazoli kao inhibitori lrrk2 za upotrebu u lečenju neurodegenerativnih poremećaja |
| MX2020005332A (es) | 2017-11-21 | 2021-01-08 | Denali Therapeutics Inc | Polimorfos y formas solidas de un compuesto de pirimidinilamino-pirazol y metodos de produccion. |
| BR112020012611A2 (pt) | 2017-12-20 | 2020-12-08 | Denali Therapeutics Inc. | Processo para a preparação de compostos pirimidinil-4-aminopirazol |
| KR20190131981A (ko) * | 2018-05-18 | 2019-11-27 | 재단법인 대구경북첨단의료산업진흥재단 | 외상성 뇌손상 또는 뇌졸중의 예방 또는 치료용 약학적 조성물 |
| AR118641A1 (es) * | 2019-04-11 | 2021-10-20 | Denali Therapeutics Inc | Compuestos, composiciones y métodos |
| MX2021014705A (es) * | 2019-05-31 | 2022-04-06 | Denali Therapeutics Inc | Formulacion de liberacion modificada de un compuesto de pirimidinilamino-pirazol y metodos de tratamiento. |
| EP3769768A1 (en) | 2019-07-23 | 2021-01-27 | Consejo Superior de Investigaciones Cientificas (CSIC) | Compounds useful for the treatment of parkinson s disease |
| WO2021086966A1 (en) * | 2019-10-29 | 2021-05-06 | Biogen Ma Inc. | Spirocyclic o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors |
| KR102342803B1 (ko) | 2020-03-23 | 2021-12-24 | 환인제약 주식회사 | 신규한 피리미딘 유도체 및 이를 포함하는 신경퇴행성 질환 및 암의 예방 또는 치료용 조성물 |
| CA3172750A1 (en) | 2020-03-23 | 2021-09-30 | Ge Hyeong Lee | Novel pyrimidine derivative, and composition for preventing or treating neurodegenerative diseases and cancer, comprising same |
| CN114426542B (zh) * | 2020-10-29 | 2023-06-30 | 苏州亚宝药物研发有限公司 | 取代的二芳基胺化合物及其药物组合物、制备方法和用途 |
| TW202308635A (zh) * | 2021-04-30 | 2023-03-01 | 美商戴納立製藥公司 | 治療與監測帕金森氏病之方法 |
| WO2023073013A1 (en) | 2021-10-27 | 2023-05-04 | H. Lundbeck A/S | Lrrk2 inhibitors |
| WO2024056775A1 (en) | 2022-09-15 | 2024-03-21 | H. Lundbeck A/S | Macrocyclic leucine-rich repeat kinase 2 (lrrk2) inhibitors |
| CN115894456A (zh) * | 2022-11-13 | 2023-04-04 | 药康众拓(江苏)医药科技有限公司 | 一种氘代吡唑氨基嘧啶类化合物、药物组合物和用途 |
| CN115819405A (zh) * | 2022-12-20 | 2023-03-21 | 沪渝人工智能研究院 | 嘧啶氨基吡唑衍生物及其作为富亮氨酸重复激酶2抑制剂的应用 |
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