AR098854A1 - 5-aril-1-imino-1-oxo-[1,2,4]tiadiazinas - Google Patents

5-aril-1-imino-1-oxo-[1,2,4]tiadiazinas

Info

Publication number
AR098854A1
AR098854A1 ARP140104787A ARP140104787A AR098854A1 AR 098854 A1 AR098854 A1 AR 098854A1 AR P140104787 A ARP140104787 A AR P140104787A AR P140104787 A ARP140104787 A AR P140104787A AR 098854 A1 AR098854 A1 AR 098854A1
Authority
AR
Argentina
Prior art keywords
halogen
alkyl
heteroaryl
group
cyano
Prior art date
Application number
ARP140104787A
Other languages
English (en)
Inventor
Guba Wolfgang
Haap Wolfgang
Peters Jens
Uwe - Obst Sander Ulrike
Kuglstatter Andreas
Schnider Christian
Woltering Thomas
Wermuth Roger
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 AR098854A1 publication Critical patent/AR098854A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/549Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente proporciona un compuesto que tiene actividad inhibidora de BACE1, su fabricación, composiciones farmacéuticas que los contienen y su uso como sustancias terapéuticamente activas. Los compuestos activos son útiles en el tratamiento terapéutico y/o profiláctico de, por ejemplo, la enfermedad de Alzheimer. BACE es una enzima escisora de APP en sitio b. Reivindicación 1: Un compuesto de fórmula (1), en la que R¹ se selecciona entre el grupo que consiste en i) alquilo C₁₋₆, y ii) halógeno-alquilo C₁₋₆; R² se selecciona entre el grupo que consiste en i) hidrógeno, ii) halógeno; iii) -NH-C(=O)-R⁴, iv) arilo, v) arilo sustituido por 1 - 3 sustituyentes seleccionados individualmente entre ciano, alquilo C₁₋₆, halógeno-alquilo C₁₋₆ y halógeno, vi) heteroarilo, vii) heteroarilo sustituido por 1 - 3 sustituyentes seleccionados individualmente entre R⁶, y viii) -CºC-R⁵; R³ es halógeno; R⁴ se selecciona entre el grupo que consiste en i) heteroarilo, y ii) heteroarilo opcionalmente sustituido por 1 - 3 sustituyentes seleccionados individualmente entre R⁶; R⁵ se selecciona entre el grupo que consiste en i) arilo, ii) arilo, heteroarilo sustituido por 1 - 3 sustituyentes seleccionados individualmente entre ciano, alquilo C₁₋₆, halógeno-alquilo C₁₋₆ y halógeno, iii) heteroarilo, y iv) heteroarilo, heteroarilo sustituido por 1 - 3 sustituyentes seleccionados individualmente entre ciano, alquilo C₁₋₆, halógeno-alquilo C₁₋₆ y halógeno; R⁶ se selecciona entre el grupo que consiste en i) ciano, ii) halógeno; iii) alquilo C₁₋₆, iv) halógeno-alquilo C₁₋₆, v) alquinilo C₂₋₆-O-, vi) heteroarilo, y vii) heteroarilo, heteroarilo sustituido por 1 - 3 sustituyentes seleccionados individualmente entre ciano, alquilo C₁₋₆, alcoxi C₁₋₆, halógeno-alquilo C₁₋₆, halógeno-alcoxi C₁₋₆ y halógeno; R⁷ se selecciona entre el grupo que consiste en i) halógeno, y ii) halógeno-alquilo C₁₋₆; m es 1 ó 2; n es 0 ó 1; y p es 0, 1 ó 2; o sales farmacéuticamente aceptable de los mismos.
ARP140104787A 2013-12-20 2014-12-19 5-aril-1-imino-1-oxo-[1,2,4]tiadiazinas AR098854A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13198700 2013-12-20

Publications (1)

Publication Number Publication Date
AR098854A1 true AR098854A1 (es) 2016-06-15

Family

ID=49876438

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140104787A AR098854A1 (es) 2013-12-20 2014-12-19 5-aril-1-imino-1-oxo-[1,2,4]tiadiazinas

Country Status (13)

Country Link
US (1) US9605006B2 (es)
EP (1) EP3083644B1 (es)
JP (1) JP6461162B2 (es)
KR (1) KR102285306B1 (es)
CN (2) CN105683199B (es)
AR (1) AR098854A1 (es)
BR (1) BR112016007430A2 (es)
CA (1) CA2924022A1 (es)
HK (1) HK1220204A1 (es)
MX (1) MX365292B (es)
RU (1) RU2016128365A (es)
TW (1) TW201609754A (es)
WO (1) WO2015091595A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2016016061A (es) * 2014-08-15 2017-03-10 Hoffmann La Roche 2,2,2-trifluoroetil-tiadiazinas.
JP6895424B2 (ja) * 2015-08-12 2021-06-30 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Bace1阻害剤
CN114644566A (zh) * 2020-12-21 2022-06-21 抚顺顺能化工有限公司 一种2-氨基-2-苯基丁酸的制备方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5766198B2 (ja) * 2010-10-29 2015-08-19 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
US8404680B2 (en) * 2011-02-08 2013-03-26 Hoffmann-La Roche Inc. N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors
US9067924B2 (en) * 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
US9221839B2 (en) * 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
EP2694521B1 (en) * 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
JP2014524472A (ja) * 2011-08-22 2014-09-22 メルク・シャープ・アンド・ドーム・コーポレーション Bace阻害剤としての2−スピロ置換イミノチアジンならびにそのモノオキシドおよびジオキシド、組成物、ならびにそれらの使用
US9493484B2 (en) * 2012-02-08 2016-11-15 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
US9428476B2 (en) * 2013-03-15 2016-08-30 Merck Sharp & Dohme Corp. S-imino-S-oxo-iminothiadiazine compounds as BACE inhibitors, compositions, and their use

Also Published As

Publication number Publication date
BR112016007430A2 (pt) 2017-08-01
EP3083644B1 (en) 2019-03-13
EP3083644A1 (en) 2016-10-26
MX365292B (es) 2019-05-29
MX2016006906A (es) 2016-08-17
CN105683199A (zh) 2016-06-15
KR102285306B1 (ko) 2021-08-04
JP6461162B2 (ja) 2019-01-30
CN108690052A (zh) 2018-10-23
TW201609754A (zh) 2016-03-16
CN105683199B (zh) 2018-06-26
US9605006B2 (en) 2017-03-28
HK1220204A1 (zh) 2017-04-28
US20160318952A1 (en) 2016-11-03
WO2015091595A1 (en) 2015-06-25
RU2016128365A (ru) 2018-01-25
JP2017500344A (ja) 2017-01-05
CA2924022A1 (en) 2015-06-25
KR20160098263A (ko) 2016-08-18

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