BR112016021982B1 - Derivados de pirimidina macrocíclicos, seu uso e composição farmacêutica que os compreende - Google Patents
Derivados de pirimidina macrocíclicos, seu uso e composição farmacêutica que os compreende Download PDFInfo
- Publication number
- BR112016021982B1 BR112016021982B1 BR112016021982-1A BR112016021982A BR112016021982B1 BR 112016021982 B1 BR112016021982 B1 BR 112016021982B1 BR 112016021982 A BR112016021982 A BR 112016021982A BR 112016021982 B1 BR112016021982 B1 BR 112016021982B1
- Authority
- BR
- Brazil
- Prior art keywords
- 4alkyl
- optionally substituted
- int
- haloc1
- hydroxyl
- Prior art date
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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
- C07D471/22—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 systems contains four or more hetero rings
-
- 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
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- A61P25/24—Antidepressants
-
- 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
- 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
- C07D498/22—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 four or more hetero rings
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/582—Recycling of unreacted starting or intermediate materials
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14163443.6 | 2014-04-03 | ||
| EP14163443 | 2014-04-03 | ||
| EP14183747 | 2014-09-05 | ||
| EP14183747.6 | 2014-09-05 | ||
| PCT/EP2015/057399 WO2015150555A1 (en) | 2014-04-03 | 2015-04-02 | Macrocylic pyrimidine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112016021982A2 BR112016021982A2 (https=) | 2017-08-15 |
| BR112016021982B1 true BR112016021982B1 (pt) | 2022-07-26 |
Family
ID=52781117
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112016021982-1A BR112016021982B1 (pt) | 2014-04-03 | 2015-04-02 | Derivados de pirimidina macrocíclicos, seu uso e composição farmacêutica que os compreende |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US10017509B2 (https=) |
| EP (1) | EP3126364B1 (https=) |
| JP (1) | JP6529513B2 (https=) |
| KR (1) | KR102390276B1 (https=) |
| CN (2) | CN114213415A (https=) |
| AU (1) | AU2015239098B2 (https=) |
| BR (1) | BR112016021982B1 (https=) |
| CA (1) | CA2942636C (https=) |
| CL (1) | CL2016002461A1 (https=) |
| EA (1) | EA031246B1 (https=) |
| ES (1) | ES2667723T3 (https=) |
| IL (1) | IL248005B (https=) |
| MA (1) | MA39822A (https=) |
| MX (1) | MX369798B (https=) |
| MY (1) | MY185491A (https=) |
| NZ (1) | NZ725399A (https=) |
| PE (1) | PE20161362A1 (https=) |
| PH (1) | PH12016501963A1 (https=) |
| SG (1) | SG11201608240RA (https=) |
| UA (1) | UA118219C2 (https=) |
| WO (1) | WO2015150555A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI721104B (zh) | 2016-02-19 | 2021-03-11 | 瑞典商斯普林特生物科技公司 | 6‐芳基或6‐雜芳基‐4‐嗎啉‐4‐芳基‐吡啶‐2‐酮化合物 |
| ES2821400T3 (es) | 2016-02-19 | 2021-04-26 | Sprint Bioscience Ab | Compuestos de 6-heterociclil-4-morfolin-4-ilpiridin-2-ona útiles para el tratamiento del cáncer y la diabetes |
| EP3601236A1 (en) | 2017-03-28 | 2020-02-05 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| ES2900199T3 (es) | 2017-03-28 | 2022-03-16 | Bayer Ag | Novedosos compuestos macrocíclicos inhibidores de PTEFB |
| SI3672962T1 (sl) | 2017-08-23 | 2022-06-30 | Sprint Bioscience Ab | Morfolinilpiridonske spojine |
| SI3672967T1 (sl) | 2017-08-23 | 2022-04-29 | Sprint Bioscience Ab | Spojine azaindolilpiridona in diazaindolilpiridona |
| TW202325302A (zh) | 2017-08-23 | 2023-07-01 | 瑞典商斯普林特生物科技公司 | 吡啶胺-吡啶酮及嘧啶胺-吡啶酮化合物 |
| JP7199737B2 (ja) | 2017-08-23 | 2023-01-06 | スプリント バイオサイエンス アクティエボラーグ | ピリジルピリドン化合物 |
| US20230148005A1 (en) * | 2020-02-18 | 2023-05-11 | Theseus Pharmaceuticals, Inc. | Macrocyclic compounds and uses thereof |
| KR20230007369A (ko) * | 2020-04-07 | 2023-01-12 | 아이테오스 벨지움 에스에이 | 암의 치료를 위한 ent 저해제로서의 거대환식 다이아민 유도체 및 이와 아데노신 수용체 길항제와의 조합물 |
| CN113735879B (zh) * | 2020-05-27 | 2022-05-17 | 百极弘烨（广东）医药科技有限公司 | 一种大环jak抑制剂及其应用 |
| CN113735856A (zh) * | 2020-05-29 | 2021-12-03 | 百极弘烨(南通)医药科技有限公司 | 大环jak抑制剂及其应用 |
| WO2022020651A1 (en) * | 2020-07-22 | 2022-01-27 | Fog Pharmaceuticals, Inc. | Amino acids |
| CN118139846A (zh) * | 2021-09-23 | 2024-06-04 | 河南晟翔医药科技有限公司 | 一种egfr小分子抑制剂、含其的药物组合物及其用途 |
| KR102613509B1 (ko) * | 2021-12-15 | 2023-12-13 | 환인제약 주식회사 | 마크로사이클릭 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신경 퇴행성 질환의 예방 또는 치료용 약학적 조성물 |
| WO2024078263A1 (zh) * | 2022-10-09 | 2024-04-18 | 药雅科技(上海)有限公司 | 大环杂环类化合物作为egfr抑制剂的制备及其应用 |
| CN117229300A (zh) * | 2023-03-12 | 2023-12-15 | 药雅科技(上海)有限公司 | Egfr抑制剂的制备及其应用 |
| WO2024094171A1 (zh) * | 2022-11-04 | 2024-05-10 | 江苏恒瑞医药股份有限公司 | 取代的氨基嘧啶类化合物、其制备方法及其在医药上的应用 |
| CN116478076A (zh) * | 2023-04-26 | 2023-07-25 | 南京优氟医药科技有限公司 | 一种(2s,4s)-1-叔丁氧羰基-2-(二氟甲基)-4-羟基吡咯烷的制备方法 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004078682A2 (en) * | 2003-03-05 | 2004-09-16 | Irm Llc | Cyclic compounds and compositions as protein kinase inhibitors |
| AU2004224807A1 (en) | 2003-03-24 | 2004-10-07 | Axikin Pharmaceuticals, Inc. | 2-phenoxy- and 2-phenylsulfomamide derivatives with CCR3 antagonistic activity for the treatment of asthma and other inflammatory or immunological disorders |
| JO2785B1 (en) | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| MXPA06007018A (es) | 2003-12-18 | 2006-08-31 | Janssen Pharmaceutica Nv | Derivados de 3-ciano-quinolino con actividad anti-proliferativa. |
| MXPA06007017A (es) | 2003-12-18 | 2006-08-31 | Janssen Pharmaceutica Nv | Derivados de pirido y pirimidopirimidina como agentes antiproliferativos. |
| JO3088B1 (ar) | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
| MY169441A (en) | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| US8778919B2 (en) | 2005-06-30 | 2014-07-15 | Janssen Pharmaceutica Nv | Cyclic anilino—pyridinotriazines |
| WO2007058627A1 (en) | 2005-11-16 | 2007-05-24 | S*Bio Pte Ltd | Oxygen linked pyrimidine derivatives |
| WO2007059628A1 (en) | 2005-11-24 | 2007-05-31 | Oz Communications Inc. | Method for securely associating data with http and https sessions |
| CA2687909C (en) | 2007-06-21 | 2015-09-15 | Janssen Pharmaceutica Nv | Indolin-2-ones and aza-indolin-2-ones |
| AU2008281849B2 (en) | 2007-07-27 | 2013-11-28 | Janssen Pharmaceutica Nv | Pyrrolopyrimidines |
| US20090264431A1 (en) | 2007-08-20 | 2009-10-22 | Palovich Michael R | Novel cathepsin c inhibitors and their use |
| US8318929B2 (en) | 2008-03-10 | 2012-11-27 | Janssen Pharmaceutica Nv | 4-aryl-2-anilino-pyrimidines |
| JP2011522865A (ja) | 2008-06-13 | 2011-08-04 | ノバルティス アーゲー | Ｉａ心不全および癌の治療に有用なプロテインキナーゼｄ阻害剤としての２，４’−ビピリジニル化合物 |
| AU2010254056A1 (en) | 2009-05-28 | 2011-12-15 | Tetralogic Pharmaceuticals Corp. | IAP inhibitors |
| CN102548987B (zh) | 2009-07-14 | 2014-04-16 | 江苏迈度药物研发有限公司 | 作为激酶抑制剂的氟取代化合物及其使用方法 |
| TWI513695B (zh) | 2009-10-27 | 2015-12-21 | Merck Sharp & Dohme | （１，１，１，３，３，３－六氟－２－羥基丙－２－基）苯基衍生物 |
-
2015
- 2015-04-01 MA MA039822A patent/MA39822A/fr unknown
- 2015-04-02 CN CN202111600011.XA patent/CN114213415A/zh active Pending
- 2015-04-02 US US15/300,956 patent/US10017509B2/en active Active
- 2015-04-02 CN CN201580018080.6A patent/CN106164075B/zh active Active
- 2015-04-02 EA EA201692003A patent/EA031246B1/ru not_active IP Right Cessation
- 2015-04-02 JP JP2016560825A patent/JP6529513B2/ja active Active
- 2015-04-02 AU AU2015239098A patent/AU2015239098B2/en not_active Ceased
- 2015-04-02 UA UAA201611005A patent/UA118219C2/uk unknown
- 2015-04-02 WO PCT/EP2015/057399 patent/WO2015150555A1/en not_active Ceased
- 2015-04-02 MX MX2016012992A patent/MX369798B/es active IP Right Grant
- 2015-04-02 PE PE2016001882A patent/PE20161362A1/es unknown
- 2015-04-02 CA CA2942636A patent/CA2942636C/en active Active
- 2015-04-02 NZ NZ725399A patent/NZ725399A/en unknown
- 2015-04-02 EP EP15713522.9A patent/EP3126364B1/en active Active
- 2015-04-02 MY MYPI2016001777A patent/MY185491A/en unknown
- 2015-04-02 ES ES15713522.9T patent/ES2667723T3/es active Active
- 2015-04-02 KR KR1020167028764A patent/KR102390276B1/ko not_active Expired - Fee Related
- 2015-04-02 BR BR112016021982-1A patent/BR112016021982B1/pt not_active IP Right Cessation
- 2015-04-02 SG SG11201608240RA patent/SG11201608240RA/en unknown
-
2016
- 2016-09-25 IL IL248005A patent/IL248005B/en active IP Right Grant
- 2016-09-29 CL CL2016002461A patent/CL2016002461A1/es unknown
- 2016-10-03 PH PH12016501963A patent/PH12016501963A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20170022202A1 (en) | 2017-01-26 |
| SG11201608240RA (en) | 2016-10-28 |
| PE20161362A1 (es) | 2016-12-17 |
| ES2667723T3 (es) | 2018-05-14 |
| UA118219C2 (uk) | 2018-12-10 |
| EP3126364A1 (en) | 2017-02-08 |
| EA201692003A1 (ru) | 2017-06-30 |
| AU2015239098B2 (en) | 2019-08-01 |
| AU2015239098A1 (en) | 2016-09-29 |
| EP3126364B1 (en) | 2018-02-07 |
| BR112016021982A2 (https=) | 2017-08-15 |
| CA2942636C (en) | 2023-03-21 |
| MA39822A (fr) | 2018-02-06 |
| IL248005B (en) | 2018-12-31 |
| KR20160142316A (ko) | 2016-12-12 |
| PH12016501963B1 (en) | 2017-01-09 |
| WO2015150555A1 (en) | 2015-10-08 |
| US10017509B2 (en) | 2018-07-10 |
| CL2016002461A1 (es) | 2017-06-23 |
| PH12016501963A1 (en) | 2017-01-09 |
| CN106164075A (zh) | 2016-11-23 |
| MY185491A (en) | 2021-05-19 |
| CA2942636A1 (en) | 2015-10-08 |
| NZ725399A (en) | 2023-01-27 |
| JP2017509687A (ja) | 2017-04-06 |
| CN106164075B (zh) | 2021-11-26 |
| CN114213415A (zh) | 2022-03-22 |
| MX2016012992A (es) | 2016-12-07 |
| EA031246B1 (ru) | 2018-12-28 |
| MX369798B (es) | 2019-11-21 |
| KR102390276B1 (ko) | 2022-04-22 |
| JP6529513B2 (ja) | 2019-06-12 |
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Legal Events
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| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] |
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| 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] | ||
| B350 | Update of information on the portal [chapter 15.35 patent gazette] | ||
| B350 | Update of information on the portal [chapter 15.35 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: 20 (VINTE) ANOS CONTADOS A PARTIR DE 02/04/2015, OBSERVADAS AS CONDICOES LEGAIS |
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| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
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