PE20211247A1 - Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos - Google Patents
Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismosInfo
- Publication number
- PE20211247A1 PE20211247A1 PE2020000353A PE2020000353A PE20211247A1 PE 20211247 A1 PE20211247 A1 PE 20211247A1 PE 2020000353 A PE2020000353 A PE 2020000353A PE 2020000353 A PE2020000353 A PE 2020000353A PE 20211247 A1 PE20211247 A1 PE 20211247A1
- Authority
- PE
- Peru
- Prior art keywords
- ring
- cycloalkyl
- compound
- sulfoxides
- methods
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Referido a un compuesto de formula I, o una sal farmaceuticamente aceptable del mismo, en donde R1 es alquilo C1-6, cicloalquilo C3-C6, CH2(cicloalquilo C3-C6), entre otros; n es 0, 1 o 2; el anillo A y el anillo B se fusionan para formar un sistema anular policiclico; en donde A es un anillo heteroaromatico de 5 miembros, en el que se sustituye opcionalmente C con un sustituyente tal como F, Cl, metilo o trifluorometilo; y B es un anillo carbociclico de 4 a 8 miembros, o anillo heterociclico de 4 a 8 miembros, 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; RB1 es R3a o R3b, cada R3a y R3b, cuando estan presentes son independientemente halogeno, deuterio, hidroxilo, entre otros; y RB2 es R4 y R4 es alquilo C1-C6, haloalquilo C1-C6, cilcoalquilo C3-C6, entre otros. Un compuesto seleccionado es 2-(difluorometilsulfinil)-5-fenil-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol. Este compuesto son Sulfonas y sulfoxidos biciclicos que tienen actividad inhibitoria 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 |
---|---|---|---|
US201762579392P | 2017-10-31 | 2017-10-31 | |
PCT/EP2018/079772 WO2019086494A1 (en) | 2017-10-31 | 2018-10-30 | Bicyclic sulfones and sulfoxides and methods of use thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20211247A1 true PE20211247A1 (es) | 2021-07-13 |
Family
ID=64051580
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2020000353A PE20211247A1 (es) | 2017-10-31 | 2018-10-30 | Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos |
Country Status (21)
Country | Link |
---|---|
US (2) | US11072617B2 (es) |
EP (1) | EP3704097B1 (es) |
JP (1) | JP2021501183A (es) |
KR (1) | KR20200083515A (es) |
CN (1) | CN111278809B (es) |
AR (1) | AR113811A1 (es) |
AU (1) | AU2018360270A1 (es) |
BR (1) | BR112020008446A2 (es) |
CA (1) | CA3078688A1 (es) |
CL (1) | CL2020001062A1 (es) |
CO (1) | CO2020003475A2 (es) |
CR (1) | CR20200168A (es) |
IL (1) | IL273847A (es) |
MA (1) | MA50503A (es) |
MX (1) | MX2020003451A (es) |
PE (1) | PE20211247A1 (es) |
PH (1) | PH12020550537A1 (es) |
RU (1) | RU2020115915A (es) |
SG (1) | SG11202002877RA (es) |
TW (1) | TW201922748A (es) |
WO (1) | WO2019086494A1 (es) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP6890179B2 (ja) | 2016-12-02 | 2021-06-18 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 二環式アミド化合物及びその使用方法 |
SG11202000333UA (en) | 2017-07-14 | 2020-02-27 | Hoffmann La Roche | Bicyclic ketone compounds and methods of use thereof |
TW202214617A (zh) | 2020-06-02 | 2022-04-16 | 法商賽諾菲公司 | 作為ripk1抑制劑之異㗁唑啶及其用途 |
IL312739A (en) | 2021-11-11 | 2024-07-01 | Genzyme Corp | Isoxazolidines as RIPK1 inhibitors and their use |
Family Cites Families (46)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE1620508A1 (de) * | 1965-07-23 | 1969-09-18 | Thomae Gmbh Dr K | Verfahren zur Herstellung neuer 4,5,6,7-Tetrahydrothiazolo-[5,4-c]-pyridine |
US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
US3948903A (en) | 1972-12-15 | 1976-04-06 | Parke, Davis & Company | Substituted N-(1,2-dihydro-2-oxonicotinyl)-cephalexins and -cephaloglycins |
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 |
GB8610530D0 (en) * | 1986-04-30 | 1986-06-04 | Fbc Ltd | Herbicides |
US5004697A (en) | 1987-08-17 | 1991-04-02 | Univ. Of Ca | Cationized antibodies for delivery through the blood-brain barrier |
US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
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 |
ATE191853T1 (de) | 1992-07-27 | 2000-05-15 | Us Health | Zielgerichte liposome zur blut-hirne schranke |
US6080772A (en) | 1995-06-07 | 2000-06-27 | Sugen, Inc. | Thiazole compounds and methods of modulating signal transduction |
AU8071698A (en) * | 1997-06-13 | 1998-12-30 | Sugen, Inc. | Novel heteroaryl compounds for the modulation of protein tyrosine enzyme relatedcellular signal transduction |
EP1254115A2 (en) | 2000-02-11 | 2002-11-06 | Bristol-Myers Squibb Company | Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases |
US6514221B2 (en) | 2000-07-27 | 2003-02-04 | Brigham And Women's Hospital, Inc. | Blood-brain barrier opening |
US20020065259A1 (en) | 2000-08-30 | 2002-05-30 | Schatzberg Alan F. | 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 |
ATE445838T1 (de) | 2001-07-25 | 2009-10-15 | Raptor Pharmaceutical Inc | Zusammensetzungen und verfahren zur modulation des transports durch die blut-hirn-schranke |
US20030162695A1 (en) | 2002-02-27 | 2003-08-28 | Schatzberg Alan F. | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
NZ538223A (en) | 2002-08-26 | 2008-03-28 | Takeda Pharmaceutical | Calcium receptor modulating compound and use thereof |
EP1581186A2 (en) | 2002-12-03 | 2005-10-05 | Blanchette Rockefeller Neurosciences Institute | Artificial low-density lipoprotein carriers for transport of substances across the blood-brain barrier |
PE20050525A1 (es) | 2003-05-02 | 2005-09-08 | Elan Pharm Inc | Derivados de pirazol sustituido y compuestos relacionados como antagonistas del receptor de bradiquinina b1 |
WO2005025511A2 (en) | 2003-09-10 | 2005-03-24 | Cedars-Sinai Medical Center | Potassium channel mediated delivery of agents through the blood-brain barrier |
EP2083009A1 (de) | 2008-01-22 | 2009-07-29 | Grünenthal GmbH | Substituierte Tethrahydroimidazopyridin-Verbindungen und deren Verwendung in Arzneimitteln |
US8299077B2 (en) | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
RU2628616C2 (ru) | 2011-11-03 | 2017-08-21 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения пиперазина |
BR112014026176A2 (pt) | 2012-05-22 | 2017-06-27 | Hoffmann La Roche | dipiridilaminas substituídas e usos das mesmas |
MX2015009270A (es) | 2013-01-18 | 2015-10-30 | Hoffmann La Roche | Pirazoles sustituidos en posicion 3 y uso de los mismos como inhibidores de la cinasa cremallera de leucinas dual (dlk). |
TWI648274B (zh) | 2013-02-15 | 2019-01-21 | 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 (二) |
WO2014177524A1 (en) | 2013-05-01 | 2014-11-06 | F. Hoffmann-La Roche Ag | C-linked heterocycloalkyl substituted pyrimidines and their uses |
AR096151A1 (es) | 2013-05-01 | 2015-12-09 | Hoffmann La Roche | Compuestos de biheteroarilo y usos de los mismos |
ES2780699T3 (es) | 2013-07-10 | 2020-08-26 | Vertex Pharma | Amidas de piperidina fusionadas útiles como moduladores de canales iónicos |
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. |
MX2016010675A (es) | 2014-03-26 | 2016-11-10 | Hoffmann La Roche | Compuestos condensados de [1,4]diazepina como inhibidores de produccion de la autotaxina (atx) y acido lisofosfatidico (lpa). |
BR112017003546A2 (pt) | 2014-08-21 | 2017-12-05 | Glaxosmithkline Ip Dev Ltd | amidas heterocíclicas como inibidores de rip1 quinase como medicamentos |
CN107406462B (zh) | 2015-03-09 | 2020-11-10 | 豪夫迈·罗氏有限公司 | 三环dlk抑制剂及其用途 |
AU2016287581B2 (en) | 2015-07-02 | 2019-06-06 | F. Hoffmann-La Roche Ag | Bicyclic lactams and methods of use thereof |
US10709692B2 (en) * | 2015-12-04 | 2020-07-14 | Denali Therapeutics Inc. | Isoxazolidine derived inhibitors of receptor interacting protein kinase 1 (RIPK1) |
US10961258B2 (en) | 2015-12-21 | 2021-03-30 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides as kinase inhibitors |
SG10201913587WA (en) * | 2016-02-05 | 2020-02-27 | Denali Therapeutics Inc | Inhibitors of receptor-interacting protein kinase 1 |
JP6890179B2 (ja) | 2016-12-02 | 2021-06-18 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 二環式アミド化合物及びその使用方法 |
US11072607B2 (en) | 2016-12-16 | 2021-07-27 | Genentech, Inc. | Inhibitors of RIP1 kinase and methods of use thereof |
SG11202000333UA (en) | 2017-07-14 | 2020-02-27 | Hoffmann La Roche | Bicyclic ketone compounds and methods of use thereof |
SG11202003283TA (en) | 2017-10-11 | 2020-05-28 | Hoffmann La Roche | Bicyclic compounds for use as rip1 kinase inhibitors |
-
2018
- 2018-10-30 MX MX2020003451A patent/MX2020003451A/es unknown
- 2018-10-30 RU RU2020115915A patent/RU2020115915A/ru unknown
- 2018-10-30 SG SG11202002877RA patent/SG11202002877RA/en unknown
- 2018-10-30 MA MA050503A patent/MA50503A/fr unknown
- 2018-10-30 CR CR20200168A patent/CR20200168A/es unknown
- 2018-10-30 US US16/175,206 patent/US11072617B2/en active Active
- 2018-10-30 WO PCT/EP2018/079772 patent/WO2019086494A1/en active Application Filing
- 2018-10-30 PE PE2020000353A patent/PE20211247A1/es unknown
- 2018-10-30 CA CA3078688A patent/CA3078688A1/en active Pending
- 2018-10-30 TW TW107138469A patent/TW201922748A/zh unknown
- 2018-10-30 BR BR112020008446-8A patent/BR112020008446A2/pt not_active Application Discontinuation
- 2018-10-30 AU AU2018360270A patent/AU2018360270A1/en not_active Abandoned
- 2018-10-30 KR KR1020207015138A patent/KR20200083515A/ko not_active Application Discontinuation
- 2018-10-30 CN CN201880070578.0A patent/CN111278809B/zh active Active
- 2018-10-30 EP EP18796020.8A patent/EP3704097B1/en active Active
- 2018-10-30 AR ARP180103157A patent/AR113811A1/es unknown
- 2018-10-30 JP JP2020524177A patent/JP2021501183A/ja active Pending
-
2020
- 2020-03-25 CO CONC2020/0003475A patent/CO2020003475A2/es unknown
- 2020-04-06 IL IL273847A patent/IL273847A/en unknown
- 2020-04-20 CL CL2020001062A patent/CL2020001062A1/es unknown
- 2020-04-30 PH PH12020550537A patent/PH12020550537A1/en unknown
-
2021
- 2021-06-06 US US17/340,082 patent/US20230002391A1/en active Pending
Also Published As
Publication number | Publication date |
---|---|
US11072617B2 (en) | 2021-07-27 |
BR112020008446A2 (pt) | 2020-12-29 |
US20230002391A1 (en) | 2023-01-05 |
MX2020003451A (es) | 2020-08-03 |
CN111278809B (zh) | 2024-06-25 |
RU2020115915A3 (es) | 2022-05-06 |
MA50503A (fr) | 2020-09-09 |
CO2020003475A2 (es) | 2020-04-24 |
CR20200168A (es) | 2020-07-12 |
RU2020115915A (ru) | 2021-12-01 |
EP3704097B1 (en) | 2023-10-25 |
AR113811A1 (es) | 2020-06-10 |
WO2019086494A1 (en) | 2019-05-09 |
EP3704097A1 (en) | 2020-09-09 |
SG11202002877RA (en) | 2020-04-29 |
EP3704097C0 (en) | 2023-10-25 |
US20190127382A1 (en) | 2019-05-02 |
CN111278809A (zh) | 2020-06-12 |
PH12020550537A1 (en) | 2021-03-22 |
CL2020001062A1 (es) | 2020-08-21 |
AU2018360270A1 (en) | 2020-03-26 |
JP2021501183A (ja) | 2021-01-14 |
IL273847A (en) | 2020-05-31 |
TW201922748A (zh) | 2019-06-16 |
KR20200083515A (ko) | 2020-07-08 |
CA3078688A1 (en) | 2019-05-09 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
PE20211247A1 (es) | Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos | |
PE20211246A1 (es) | Compuestos biciclicos para su uso como inhibidores de rip1 quinasa | |
DOP2018000187A (es) | Derivados de pirazolo[1,5-a]pirazin-4-ilo | |
CL2020000427A1 (es) | Derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos. | |
CL2019000941A1 (es) | Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret. | |
CO2022006183A2 (es) | Agonista del receptor glp-1 y uso de este | |
PE20230249A1 (es) | Compuestos de heteroarilo biciclicos y usos de estos | |
UY36112A (es) | Compuestos de imidazo[4,5-c]quinolin-2-ona y su uso para tratar cáncer | |
PE20190656A1 (es) | Compuestos de tiazolo-piridina sustituida como inhibidores de malt1 | |
DOP2016000158A (es) | Análogos de cortistatina y síntesis y usos de los mismos. | |
CL2017002922A1 (es) | Agonistas de triazol del receptor apj | |
CL2019001626A1 (es) | Inhibidores de pequeñas moléculas de la familia jak de quinasas. | |
AR111693A1 (es) | Compuestos de 5-metil-1,3,4-oxadiazol-2-ilo con actividad inhibitoria de oga | |
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 | |
PE20190811A1 (es) | Derivados de pirazolopirimidinas como inhibidor de quinasa | |
CU20170154A7 (es) | Derivados de pirazol-3-il-amina sustituidos como inhibidores cdk | |
BR112017007662A2 (pt) | composto, composição farmacêutica, processo de elaboração de uma composição farmacêutica, método de tratamento de distúrbio ou doença relativa a er, kit de tratamento e uso de composto | |
AR106099A1 (es) | Compuestos bicíclicos como inhibidores duales de atx / ca | |
WO2015132799A3 (en) | Heterocyclic compounds | |
AR089641A1 (es) | COMPUESTOS BICICLICOS Y SUS USOS COMO INHIBIDORES DUALES DE c-SRC/JAK | |
CR20180307A (es) | Compuestos de imidazo[4,5-c] quinolin-2-ona y su uso en el tratamiento del cáncer | |
CL2016000495A1 (es) | Compuestos derivados de triazolo[4,5-d]pirimidina, agonistas de receptor cb2; proceso de preparación; composición que los comprende y el uso para el tratamiento o profilaxis del dolor, aterosclerosis, inflamación, diabetes mellitus, entre otras enfermedades. | |
AR107927A1 (es) | Compuestos de pirrolidina, sal farmacéuticamente aceptable del mismo, composición farmacéutica que lo comprende y su uso para la fabricación de un medicamento | |
AR072952A1 (es) | Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso | |
EA201890827A1 (ru) | Конденсированные производные пиразола в качестве ингибиторов киназы |