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AR079662A1 - Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa - Google Patents
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AR079662A1 - Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa - Google Patents

Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa

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Publication number
AR079662A1
AR079662A1 ARP100104818A ARP100104818A AR079662A1 AR 079662 A1 AR079662 A1 AR 079662A1 AR P100104818 A ARP100104818 A AR P100104818A AR P100104818 A ARP100104818 A AR P100104818A AR 079662 A1 AR079662 A1 AR 079662A1
Authority
AR
Argentina
Prior art keywords
inhibitors
alkyl
triptasa
bencilaminas
indolil
Prior art date
Application number
ARP100104818A
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English (en)
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Sanofi Aventis
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Filing date
Publication date
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR079662A1 publication Critical patent/AR079662A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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 three hetero rings
    • C07D498/14Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)

Abstract

La presente describe y reivindica una serie de indolil-piperidinil bencilaminas sustituidas de formula (1), en donde R1, R2 y R3 son como se describen en este documento. Más específicamente, los compuestos de la presente son inhibidores de b-triptasa y, por lo tanto, son utiles como agentes farmacéuticos. Además, la presente describe métodos de preparacion de indolil-piperidinil bencilaminas sustituidas. Reivindicacion 1: Un compuesto de la formula (1) en el que R1 es F, Cl, Br, OCH2CO2CH3, OCH2CONW1W2, CH2OH o alquilo, haloalquilo, alcoxi o haloalcoxi opcionalmente sustituido; en el que W1 y W2 son independientemente H o alquilo; R2 es H, F, Cl, Br, OH, CH2OH, alquilo o alcoxi; siempre que R1 y R2 no sean H simultáneamente; R3 es arilo o heteroarilo; o una sal del mismo o un enantiomero o diastereomero del mismo.
ARP100104818A 2009-12-23 2010-12-21 Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa AR079662A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US28965009P 2009-12-23 2009-12-23
FR1057580 2010-09-21

Publications (1)

Publication Number Publication Date
AR079662A1 true AR079662A1 (es) 2012-02-08

Family

ID=44246893

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104818A AR079662A1 (es) 2009-12-23 2010-12-21 Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa

Country Status (14)

Country Link
US (1) US20120245161A1 (es)
EP (1) EP2516419A1 (es)
JP (1) JP2013515733A (es)
KR (1) KR20120097410A (es)
CN (1) CN102770425A (es)
AR (1) AR079662A1 (es)
AU (1) AU2010333779A1 (es)
CA (1) CA2784894A1 (es)
MX (1) MX2012006805A (es)
RU (1) RU2012131341A (es)
SG (1) SG181504A1 (es)
TW (1) TW201132633A (es)
UY (1) UY33155A (es)
WO (1) WO2011079102A1 (es)

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CN105121411B (zh) 2013-04-15 2017-10-10 杜邦公司 杀真菌酰胺
AU2014353894A1 (en) * 2013-11-25 2016-06-02 Novogen ltd Functionalised and substituted indoles as anti-cancer agents
WO2015157005A1 (en) 2014-04-10 2015-10-15 E I Du Pont De Nemours And Company Substituted tolyl fungicide mixtures
EP3519816A4 (en) 2016-09-29 2020-05-06 The Regents of the University of California CONNECTIONS FOR INCREASING NEURONAL PLASTICITY
MA49014A (fr) * 2017-03-21 2020-02-05 Arbutus Biopharma Corp Dihydroindène-4-carboxamides substitués, leurs analogues et procédés d'utilisation correspondant
CN119405809A (zh) 2017-08-14 2025-02-11 Epizyme股份有限公司 通过抑制setd2治疗癌症的方法
CN112585119A (zh) * 2018-08-14 2021-03-30 Epizyme股份有限公司 经取代的吲哚及其使用方法
TWI846654B (zh) 2018-11-06 2024-06-21 美商富曼西公司 經取代之甲苯基殺真菌劑
CN109438214B (zh) * 2018-11-13 2021-06-11 大连奇凯医药科技有限公司 高纯度5-溴-2,4-二氟苯甲酸的制备方法
KR102946120B1 (ko) 2019-02-27 2026-03-30 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 뇌 장애를 치료하기 위한 아제피노-인돌 및 다른 헤테로사이클
MX2021010198A (es) * 2019-02-27 2021-09-21 Univ California Indoles n-sustituidos y otros heterociclos para el tratamiento de trastornos cerebrales.
PY2133975A (es) 2020-05-06 2022-01-19 Fmc Corp Fungicidas de tolilo sustituido y sus mezclas
CN113372223B (zh) * 2021-05-20 2022-10-28 宁波职业技术学院 一种2-氟-3-溴-苄胺的制备方法
CN115745864B (zh) 2021-09-03 2025-10-10 深圳零一生命科技有限责任公司 吲哚类化合物及其制备方法和应用
IL313455A (en) 2021-12-15 2024-08-01 Delix Therapeutics Inc Phenoxy and benzyloxy modified psychroplastogens and their uses

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Publication number Priority date Publication date Assignee Title
US6777433B2 (en) 1999-12-22 2004-08-17 Merck Frosst Canada & Co. Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates
OA12274A (en) * 2000-05-22 2006-05-09 Aventis Pharma Inc Arylmethylamine derivatives for use as tryptase inhibitors.
GB0012362D0 (en) * 2000-05-22 2000-07-12 Aventis Pharma Ltd Chemical compounds
EP1678146A1 (en) 2003-10-23 2006-07-12 Pharmacia Corporation Pyrimidine compounds for the treatment of inflammation
DOP2005000039A (es) * 2004-03-26 2005-10-31 Aventis Pharma Inc Hidrocloruro de [4-(5-aminometil-2-fluoro-fenil)- piperidin-1-il]-(4-bomo-3-metil-5-propoxi-tiofen-2-il)-metanona como un inhibidor de la triptasa de mastocitos
RS54413B1 (sr) * 2008-08-22 2016-04-28 Sanofi [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metoksi-etil)-4trifluorometoksi-1h-indol-3-il]metanon kao inhibitor triptaze iz mastocita
FR2955324A1 (fr) * 2010-01-15 2011-07-22 Sanofi Aventis [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees
RS53456B (sr) * 2009-12-23 2014-12-31 Sanofi Prolekovi [4[4-(5-aminometil-2-fluor-fenil)-piperidin-1-il]-(1h-pirolo-piridin-il)-metanona i njihova sinteza

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Publication number Publication date
EP2516419A1 (en) 2012-10-31
AU2010333779A1 (en) 2012-07-12
KR20120097410A (ko) 2012-09-03
SG181504A1 (en) 2012-07-30
RU2012131341A (ru) 2014-01-27
US20120245161A1 (en) 2012-09-27
WO2011079102A1 (en) 2011-06-30
CA2784894A1 (en) 2011-06-30
JP2013515733A (ja) 2013-05-09
UY33155A (es) 2011-07-29
MX2012006805A (es) 2012-07-10
TW201132633A (en) 2011-10-01
CN102770425A (zh) 2012-11-07

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