PE20211246A1 - Compuestos biciclicos para su uso como inhibidores de rip1 quinasa - Google Patents
Compuestos biciclicos para su uso como inhibidores de rip1 quinasaInfo
- Publication number
- PE20211246A1 PE20211246A1 PE2020000378A PE2020000378A PE20211246A1 PE 20211246 A1 PE20211246 A1 PE 20211246A1 PE 2020000378 A PE2020000378 A PE 2020000378A PE 2020000378 A PE2020000378 A PE 2020000378A PE 20211246 A1 PE20211246 A1 PE 20211246A1
- Authority
- PE
- Peru
- Prior art keywords
- ring
- deuterium
- alkyl
- compound
- hydroxyl
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Referido a un compuesto de formula I, o una sal farmaceuticamente aceptable del mismo, en el que R1 es H, deuterio, F, hidroxilo, entre otros; R2a y R2b son, H deuterio, F entre otros; cada R6 es H halogeno, alquilo C1-C6, entre otros, el anillo A y el anillo B se fusionan para formar un sistema de anillos policiclico; en el que A es un anillo heteroaromatico de 5 elementos en el que C se sustituye opcionalmente con F, Cl, metilo o trifluorometilo; y B es un anillo carbociclico de 4 a 8 elementos o anillo heterociclico de 4 a 8 elementos, entre otros, que tiene de 1 a 3 heteroatomos seleccionados entre N, O y S; p es 1 o 2 y q es 0 o 1; o p es 0 , y q es1; cada RB1 es halogeno, deuterio, hidroxilo, alquilo C1-C6, entre otros; RB2 es alquilo C1-C6, haloalquilo C1-C6, cicloalquilo C3-C6, entre otros. Un compuesto seleccionado es cis-7-fluoro-5-fenil-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-il]propan-1-ol. Este compuesto biciclico es inhibidor de la quinasa de la proteina 1 de interaccion con receptores (RIP1 quinasa); tambien se refiere a compuestos intermedios, metodos de preparacion de los mismos, y su uso en el tratamiento de enfermedades y trastornos asociados a inflamacion, muerte celular y otros.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762570892P | 2017-10-11 | 2017-10-11 | |
| PCT/EP2018/077656 WO2019072942A1 (en) | 2017-10-11 | 2018-10-10 | BICYCLIC COMPOUNDS FOR USE AS INHIBITORS OF KINASE RIP1 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211246A1 true PE20211246A1 (es) | 2021-07-13 |
Family
ID=63840848
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2020000378A PE20211246A1 (es) | 2017-10-11 | 2018-10-10 | Compuestos biciclicos para su uso como inhibidores de rip1 quinasa |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US11673892B2 (es) |
| EP (1) | EP3694858B1 (es) |
| JP (1) | JP7362600B2 (es) |
| KR (1) | KR20200070297A (es) |
| CN (1) | CN111201229B (es) |
| AU (1) | AU2018348930A1 (es) |
| BR (1) | BR112020007067A2 (es) |
| CA (1) | CA3078653A1 (es) |
| CL (1) | CL2020000944A1 (es) |
| CO (1) | CO2020004977A2 (es) |
| CR (1) | CR20200151A (es) |
| IL (1) | IL273443A (es) |
| MA (1) | MA50356A (es) |
| MX (1) | MX2020003439A (es) |
| PE (1) | PE20211246A1 (es) |
| PH (1) | PH12020550253A1 (es) |
| RU (1) | RU2020114670A (es) |
| SG (1) | SG11202003283TA (es) |
| WO (1) | WO2019072942A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018100070A1 (en) | 2016-12-02 | 2018-06-07 | F. Hoffmann-La Roche Ag | Bicyclic amide compounds and methods of use thereof |
| KR20240065201A (ko) | 2017-07-14 | 2024-05-14 | 에프. 호프만-라 로슈 아게 | 이환형 케톤 화합물 및 이의 사용 방법 |
| TW201922748A (zh) | 2017-10-31 | 2019-06-16 | 瑞士商赫孚孟拉羅股份公司 | 雙環碸及亞碸類以及其使用方法 |
| EP3908586B1 (en) * | 2019-01-11 | 2022-12-21 | F. Hoffmann-La Roche AG | Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof |
| CN114591333B (zh) * | 2020-12-04 | 2023-08-01 | 广州嘉越医药科技有限公司 | 一种吡咯并嘧啶类化合物的制备方法 |
| WO2023039795A1 (zh) * | 2021-09-16 | 2023-03-23 | 维泰瑞隆（北京）生物科技有限公司 | Rip1激酶抑制剂及其用途 |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| EP0102324A3 (de) | 1982-07-29 | 1984-11-07 | Ciba-Geigy Ag | Lipide und Tenside in wässriger Phase |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| HUT35524A (en) | 1983-08-02 | 1985-07-29 | Hoechst Ag | Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance |
| US5004697A (en) | 1987-08-17 | 1991-04-02 | Univ. Of Ca | Cationized antibodies for delivery through the blood-brain barrier |
| US5112596A (en) | 1990-04-23 | 1992-05-12 | Alkermes, Inc. | Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability |
| US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
| WO1992004343A1 (en) * | 1990-09-04 | 1992-03-19 | Yamanouchi Pharmaceutical Co., Ltd. | Novel tetrahydrobenzazole derivative |
| DE69328430T2 (de) | 1992-07-27 | 2001-01-25 | The Government Of The United States Of America As Represented By The Secretary Of National Institute Of Health, Office Of Technology Transfer | Zielgerichte liposome zur blut-hirne schranke |
| US6080772A (en) | 1995-06-07 | 2000-06-27 | Sugen, Inc. | Thiazole compounds and methods of modulating signal transduction |
| CA2293400A1 (en) | 1997-06-13 | 1998-12-17 | Gerald Mcmahon | Novel heteroaryl compounds for the modulation of protein tyrosine enzyme related cellular signal transduction |
| US6514221B2 (en) | 2000-07-27 | 2003-02-04 | Brigham And Women's Hospital, Inc. | Blood-brain barrier opening |
| PL213199B1 (pl) | 2000-08-10 | 2013-01-31 | Pharmacia Italia Spa | Zwiazek bicyklo-pirazolowy, sposób wytwarzania go, jego kompozycja farmaceutyczna, oraz kombinatoryczna biblioteka chemiczna |
| AU2001286930A1 (en) | 2000-08-30 | 2002-03-13 | The Board Of Trustees Of The Leland Stanford Junior University | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| US7034036B2 (en) | 2000-10-30 | 2006-04-25 | Pain Therapeutics, Inc. | Inhibitors of ABC drug transporters at the blood-brain barrier |
| DE10121982B4 (de) | 2001-05-05 | 2008-01-24 | Lts Lohmann Therapie-Systeme Ag | Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung |
| UA76461C2 (en) | 2001-05-24 | 2006-08-15 | Lilly Co Eli | Pyrrazole derivatives as pharmaceutical agents, use thereof, a pharmaceutical composition on their basis |
| EP1554572B1 (en) | 2001-07-25 | 2009-10-14 | Raptor Pharmaceutical Inc. | Compositions and methods for modulating blood-brain barrier transport |
| US20030162695A1 (en) | 2002-02-27 | 2003-08-28 | Schatzberg Alan F. | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| KR101186210B1 (ko) | 2002-12-03 | 2012-10-08 | 블랜체트 록펠러 뉴로사이언시즈 인스티튜트 | 혈뇌장벽을 통과하는 물질 수송용 인공 저밀도 지단백질 운반체 |
| JP2007505142A (ja) | 2003-09-10 | 2007-03-08 | セダーズ−シナイ メディカル センター | 血液脳関門を通過する薬剤のカリウムチャネル媒介性送達 |
| AU2008212625B2 (en) | 2007-02-07 | 2012-07-19 | Pfizer Inc. | 3-amino-pyrrolo[3,4-c] pyrazole- 5 (1H, 4H, 6H) carbaldehyde derivatives as PKC inhibitors |
| JP2012051806A (ja) | 2009-02-26 | 2012-03-15 | Eisai R & D Management Co Ltd | イミダゾリルピラジン誘導体 |
| AU2010272578B2 (en) | 2009-07-15 | 2015-03-05 | Cellzome Limited | Substituted triazole and imidazole derivatives as gamma secretase modulators |
| WO2013010904A1 (en) | 2011-07-15 | 2013-01-24 | Janssen Pharmaceuticals, Inc. | Novel substituted indole derivatives as gamma secretase modulators |
| EP2852584B1 (en) | 2012-05-22 | 2018-02-28 | F. Hoffmann-La Roche AG | Substituted dipyridylamines and uses thereof |
| RU2015131314A (ru) | 2013-01-18 | 2017-02-27 | Ф. Хоффманн-Ля Рош Аг | 3-замещенные пиразолы и их применение в качестве ингибиторов dlk |
| TWI638815B (zh) | 2013-02-15 | 2018-10-21 | 英商葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之雜環醯胺類（一） |
| PE20200447A1 (es) | 2013-05-01 | 2020-02-28 | Hoffmann La Roche | Compuestos de biheteroarilo y usos de los mismos |
| CN105164114B (zh) | 2013-05-01 | 2018-03-23 | 豪夫迈·罗氏有限公司 | C‑连接的杂环烷基取代的嘧啶类和它们的用途 |
| MX2016008110A (es) | 2013-12-20 | 2016-08-19 | Hoffmann La Roche | Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos. |
| KR20170042595A (ko) | 2014-08-21 | 2017-04-19 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | 의약으로서의 rip1 키나제 억제제로서의 헤테로시클릭 아미드 |
| EP3268373B1 (en) | 2015-03-09 | 2022-04-27 | F. Hoffmann-La Roche AG | Tricyclic dlk inhibitors and uses thereof |
| ES2930749T3 (es) * | 2015-07-02 | 2022-12-21 | Hoffmann La Roche | Lactamas bicíclicas como inhibidores de la proteína de interacción con el receptor 1 (RIP1) cinasa para tratar, por ejemplo, enfermedades inflamatorias |
| CR20180413A (es) * | 2016-02-05 | 2018-12-04 | Denali Therapeutics Inc | Inhibidores de la proteína quinasa 1 que interactua con el receptor |
| KR102613433B1 (ko) | 2017-10-11 | 2023-12-13 | 주식회사 대웅제약 | 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물 |
-
2018
- 2018-10-10 PE PE2020000378A patent/PE20211246A1/es unknown
- 2018-10-10 KR KR1020207013188A patent/KR20200070297A/ko not_active Application Discontinuation
- 2018-10-10 BR BR112020007067-0A patent/BR112020007067A2/pt not_active Application Discontinuation
- 2018-10-10 JP JP2020520532A patent/JP7362600B2/ja active Active
- 2018-10-10 CN CN201880066460.0A patent/CN111201229B/zh active Active
- 2018-10-10 WO PCT/EP2018/077656 patent/WO2019072942A1/en active Application Filing
- 2018-10-10 EP EP18785936.8A patent/EP3694858B1/en active Active
- 2018-10-10 AU AU2018348930A patent/AU2018348930A1/en not_active Abandoned
- 2018-10-10 MA MA050356A patent/MA50356A/fr unknown
- 2018-10-10 RU RU2020114670A patent/RU2020114670A/ru unknown
- 2018-10-10 CA CA3078653A patent/CA3078653A1/en active Pending
- 2018-10-10 SG SG11202003283TA patent/SG11202003283TA/en unknown
- 2018-10-10 CR CR20200151A patent/CR20200151A/es unknown
- 2018-10-10 MX MX2020003439A patent/MX2020003439A/es unknown
-
2020
- 2020-03-19 IL IL273443A patent/IL273443A/en unknown
- 2020-04-08 CL CL2020000944A patent/CL2020000944A1/es unknown
- 2020-04-09 US US16/844,952 patent/US11673892B2/en active Active
- 2020-04-09 PH PH12020550253A patent/PH12020550253A1/en unknown
- 2020-04-23 CO CONC2020/0004977A patent/CO2020004977A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2020114670A (ru) | 2021-11-12 |
| KR20200070297A (ko) | 2020-06-17 |
| WO2019072942A1 (en) | 2019-04-18 |
| CL2020000944A1 (es) | 2020-08-21 |
| IL273443A (en) | 2020-05-31 |
| MX2020003439A (es) | 2020-07-29 |
| EP3694858B1 (en) | 2023-01-11 |
| US20200283446A1 (en) | 2020-09-10 |
| PH12020550253A1 (en) | 2021-02-22 |
| CN111201229B (zh) | 2024-08-23 |
| BR112020007067A2 (pt) | 2020-10-06 |
| SG11202003283TA (en) | 2020-05-28 |
| JP2020536915A (ja) | 2020-12-17 |
| MA50356A (fr) | 2021-04-21 |
| CN111201229A (zh) | 2020-05-26 |
| CR20200151A (es) | 2020-05-23 |
| AU2018348930A1 (en) | 2020-03-26 |
| CO2020004977A2 (es) | 2020-05-05 |
| JP7362600B2 (ja) | 2023-10-17 |
| US11673892B2 (en) | 2023-06-13 |
| CA3078653A1 (en) | 2019-04-18 |
| EP3694858A1 (en) | 2020-08-19 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20211246A1 (es) | Compuestos biciclicos para su uso como inhibidores de rip1 quinasa | |
| PE20190656A1 (es) | Compuestos de tiazolo-piridina sustituida como inhibidores de malt1 | |
| AR119651A1 (es) | Compuestos heterocíclicos y de heteroarilo para tratar la enfermedad de huntington | |
| CL2019000941A1 (es) | Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret. | |
| CL2020000856A1 (es) | Isoquinolinas como inhibidores de hpk1. (divisional solicitud 201902734) | |
| UY37310A (es) | Compuestos de indol sustituidos con [1,2,4]triazolo[1,5-a]piridinilo | |
| PE20191613A1 (es) | Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret | |
| CY1124800T1 (el) | Παραγωγο πυριδο[3,4-d]πυριμιδινης και φαρμακευτικως αποδεκτο αλας αυτου | |
| DOP2018000187A (es) | Derivados de pirazolo[1,5-a]pirazin-4-ilo | |
| DOP2016000281A (es) | Compuestos de imidazo[4,5-c]quinolin-2-ona y su uso para tratar cáncer | |
| PE20221629A1 (es) | Analogos novedosos de nucleosidos sustituidos en el anillo aromatico biciclico 6-6 para su uso como inhibidores de prmt5 | |
| CO2017000912A2 (es) | Derivados de 2 -h indazol como inhibidores de kinasas dependientes de ciclinas (cdk) y usos terapeuticos de los mismos | |
| CL2016002148A1 (es) | Derivados de fenilen-1,5-diamina 2,4-disustituidos y aplicaciones de los mismos, y composiciones farmacéuticas y composiciones farmacéuticamente aceptables preparadas a partir de los mismos. | |
| DOP2018000065A (es) | Derivados de 8-[6-[3-(amino)propoxi]-3-piridil]1-isopropilimidazo[4,5-c]quinolin-2-ona como moduladores selectivos de la cinasa de la ataxia telangiectasia mutada (atm) para el tratamiento del cáncer | |
| PE20191245A1 (es) | Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim | |
| PE20170189A1 (es) | Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1 | |
| CO2018011408A2 (es) | Compuestos de pirimidina como inhibidores de la quinasa jak | |
| CL2017000270A1 (es) | Derivados de heterociclilo opcionalmente condensados de pirimidina útiles para el tratamiento de enfermedades inflamatorias, metabólicas, oncológicas y autoinmunitarias. | |
| PE20190339A1 (es) | 1h-pirazolo[4,3-b] piridinas como inhibidores de pde1 | |
| AR108461A1 (es) | Compuestos imidazo[4,5-c]quinolin-2-ona y su uso en el tratamiento del cáncer | |
| AR110753A1 (es) | Inhibidores selectivos de jak1 | |
| UY36003A (es) | Derivados de amida, procesos de preparación y composiciones, útiles en afecciones asociadas con el receptor sub-tipo 1 de orexina. | |
| CO2021016433A2 (es) | Derivados heterocíclicos condensados | |
| PE20211247A1 (es) | Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos | |
| PE20170683A1 (es) | Triazolo[4,5-d]pirimidinas como agonistas del receptor canabinoide 2 |