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PE20211247A1 - Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos - Google Patents

Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos

Info

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
Application number
PE2020000353A
Other languages
English (en)
Inventor
Snahel Patel
Gregory Hamilton
Craig Stivala
Huifen Chen
Blake Daniels
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20211247A1 publication Critical patent/PE20211247A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16Heterocyclic 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)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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.
PE2020000353A 2017-10-31 2018-10-30 Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos PE20211247A1 (es)

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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3548484B1 (en) 2016-12-02 2025-04-30 F. Hoffmann-La Roche AG Bicyclic amide compounds and methods of use thereof
RS65308B1 (sr) 2017-07-14 2024-04-30 Hoffmann La Roche Biciklična ketonska jedinjenja i postupci za njihovu upotrebu
PE20211247A1 (es) 2017-10-31 2021-07-13 Hoffmann La Roche Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos
EP3908586B1 (en) 2019-01-11 2022-12-21 F. Hoffmann-La Roche AG Bicyclic pyrrolotriazolr 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
CA3237975A1 (en) 2021-11-11 2023-05-19 Elisabeth Defossa Isoxazolidines as ripk1 inhibitors and use thereof

Family Cites Families (51)

* Cited by examiner, † Cited by third party
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
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
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
WO1998056376A1 (en) 1997-06-13 1998-12-17 Sugen, Inc. Novel heteroaryl compounds for the modulation of protein tyrosine enzyme related cellular signal transduction
CA2399791A1 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in 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
AU2003302676A1 (en) 2002-12-03 2004-06-23 Blanchette Rockefeller Neurosciences Institute Artificial low-density lipoprotein carriers for transport of substances across the blood-brain barrier
EP1633348B1 (en) 2003-05-02 2008-10-08 Elan Pharmaceuticals, Inc. 4- BROMO - 5 - (2- CHLORO - BENZOYLAMINO) - 1H - PYRAZOLE - 3 - CARBOXYLIC ACID AMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ B sb 1 /sb RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES
US20050089473A1 (en) 2003-09-10 2005-04-28 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
CN101824036A (zh) 2009-03-05 2010-09-08 上海恒瑞医药有限公司 四氢咪唑并[1,5-a]吡嗪衍生物的盐,其制备方法及其在医药上的应用
ES2552514T3 (es) 2011-11-03 2015-11-30 Hoffmann-La Roche Ag Compuestos bicíclicos de piperazina
JP6267193B2 (ja) 2012-05-22 2018-01-24 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 置換ジピリジルアミン類及びそれらの使用
CN104918934B (zh) 2013-01-18 2017-12-22 霍夫曼-拉罗奇有限公司 3‑取代的吡唑及其作为dlk抑制剂的用途
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)
MX2015014861A (es) 2013-05-01 2016-03-09 Hoffmann La Roche Pirimidinas sustituidas con heterocicloalquilo c-enlazado y sus usos.
MY182082A (en) 2013-05-01 2021-01-18 Hoffmann La Roche Biheteroaryl compounds and uses thereof
SG11201600082VA (en) 2013-07-10 2016-02-26 Vertex Pharma Fused piperidine amides as modulators of ion channels
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.
EA032357B1 (ru) 2014-03-26 2019-05-31 Ф. Хоффманн-Ля Рош Аг Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
WO2016027253A1 (en) 2014-08-21 2016-02-25 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors as medicaments
EP3268373B1 (en) 2015-03-09 2022-04-27 F. Hoffmann-La Roche AG Tricyclic dlk inhibitors and uses thereof
UY36680A (es) 2015-05-19 2016-12-30 Glaxosmithkline Ip Dev Ltd Amidas heterocíclicas como inhibidores de quinasa
RU2716136C2 (ru) 2015-07-02 2020-03-06 Ф. Хоффманн-Ля Рош Аг Бициклические лактамы и способы их применения
US10751444B2 (en) 2015-08-07 2020-08-25 Victor Matthew Phillips Flowable hemostatic gel composition and its methods of use
WO2017096301A1 (en) * 2015-12-04 2017-06-08 Denali Therapeutics Inc. Isoxazolidine derived inhibitors of receptor interacting protein kinase 1 (ripk 1)
WO2017109724A1 (en) 2015-12-21 2017-06-29 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
JP6974331B2 (ja) 2016-02-05 2021-12-01 デナリ セラピューティクス インコーポレイテッドDenali Therapeutics Inc. 化合物、組成物及び方法
CA3042713A1 (en) 2016-11-08 2018-05-17 Cyclerion Therapeutics, Inc. Sgc stimulators
EP3548484B1 (en) 2016-12-02 2025-04-30 F. Hoffmann-La Roche AG Bicyclic amide compounds and methods of use thereof
US11072607B2 (en) 2016-12-16 2021-07-27 Genentech, Inc. Inhibitors of RIP1 kinase and methods of use thereof
RS65308B1 (sr) 2017-07-14 2024-04-30 Hoffmann La Roche Biciklična ketonska jedinjenja i postupci za njihovu upotrebu
MX2020003439A (es) 2017-10-11 2020-07-29 Hoffmann La Roche Compuestos biciclicos para usarse como inhibidores de cinasa de la proteina 1 de interaccion con receptores (rip1).
PE20211247A1 (es) 2017-10-31 2021-07-13 Hoffmann La Roche Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos

Also Published As

Publication number Publication date
RU2020115915A3 (es) 2022-05-06
CR20200168A (es) 2020-07-12
IL273847A (en) 2020-05-31
EP3704097B1 (en) 2023-10-25
US11072617B2 (en) 2021-07-27
CA3078688A1 (en) 2019-05-09
AU2018360270A1 (en) 2020-03-26
MX2020003451A (es) 2020-08-03
CN111278809B (zh) 2024-06-25
EP3704097C0 (en) 2023-10-25
JP2021501183A (ja) 2021-01-14
CL2020001062A1 (es) 2020-08-21
KR20200083515A (ko) 2020-07-08
EP3704097A1 (en) 2020-09-09
AR113811A1 (es) 2020-06-10
WO2019086494A1 (en) 2019-05-09
TW201922748A (zh) 2019-06-16
CN111278809A (zh) 2020-06-12
CO2020003475A2 (es) 2020-04-24
MA50503A (fr) 2020-09-09
RU2020115915A (ru) 2021-12-01
BR112020008446A2 (pt) 2020-12-29
US20230002391A1 (en) 2023-01-05
PH12020550537A1 (en) 2021-03-22
US12338241B2 (en) 2025-06-24
US20190127382A1 (en) 2019-05-02
SG11202002877RA (en) 2020-04-29

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