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PE20030977A1 - Derivados de sulfonil-piperidin como inhibidores de la gamma secretasa - Google Patents

Derivados de sulfonil-piperidin como inhibidores de la gamma secretasa

Info

Publication number
PE20030977A1
PE20030977A1 PE2003000130A PE2003000130A PE20030977A1 PE 20030977 A1 PE20030977 A1 PE 20030977A1 PE 2003000130 A PE2003000130 A PE 2003000130A PE 2003000130 A PE2003000130 A PE 2003000130A PE 20030977 A1 PE20030977 A1 PE 20030977A1
Authority
PE
Peru
Prior art keywords
alkyl
aryl
sulfonil
gamma secretase
cycloalkyl
Prior art date
Application number
PE2003000130A
Other languages
English (en)
Inventor
John W Clader
Theodros Asberon
Hubert B Josien
Tao Guo
Elizabeth M Smith
Dmitri Pissarnitski
Douglas W Hobbs
Original Assignee
Pharmacopeia Drug Discovery
Schering Corp
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 Pharmacopeia Drug Discovery, Schering Corp filed Critical Pharmacopeia Drug Discovery
Publication of PE20030977A1 publication Critical patent/PE20030977A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I DONDE R1 ES ARILO, HETEROARILO CON R5; R2 ES ALQUILO, -X(CO)Y, -ALQUILENO C1-C6-X(CO)Y, ARILO, HETEROARILO, ENTRE OTROS; R3 ES H, ALQUILO; R3A Y R3B SON H, ALQUILO; R5 ES HALO, CF3, OH, O-ALQUILO, OCF3, CON, NH2, ENTRE OTROS; R11 ES ARILO, HETEROARILO, ALQUILO, CICLOALQUILO, ARILAQUILO, ARILCICLOALQUILO, ENTRE OTROS; X ES O, NH, NALQUILO; O-ALQUILENO; Y ES -NR6R7, ARILO, HETEROARILO, ALQUILO, CICLOALQUILO, ENTRE OTROS; R6 Y R7 SON H, ALQUILO, CICLOALQUILO, ARILAQUILO, HETEROARILALQUILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS EL GRUPO a, GRUPO b, ENTRE OTROS. LOS COMPUESTOS SON INHIBIDORES DE LA GAMMA SECRETASA Y SON UTILES PARA EL TRATAMIENTO DE ALZHEIMER
PE2003000130A 2002-02-06 2003-02-04 Derivados de sulfonil-piperidin como inhibidores de la gamma secretasa PE20030977A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US35561802P 2002-02-06 2002-02-06

Publications (1)

Publication Number Publication Date
PE20030977A1 true PE20030977A1 (es) 2003-12-04

Family

ID=27734543

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003000130A PE20030977A1 (es) 2002-02-06 2003-02-04 Derivados de sulfonil-piperidin como inhibidores de la gamma secretasa

Country Status (21)

Country Link
US (2) US7208602B2 (es)
EP (1) EP1472223A1 (es)
JP (1) JP4758609B2 (es)
KR (1) KR20040081489A (es)
CN (1) CN1628100A (es)
AR (1) AR038482A1 (es)
AU (1) AU2003210865B2 (es)
BR (1) BR0307492A (es)
CA (1) CA2478423A1 (es)
CO (1) CO5611195A2 (es)
EC (1) ECSP045218A (es)
MX (1) MXPA04007659A (es)
MY (1) MY141504A (es)
NO (1) NO329067B1 (es)
NZ (1) NZ534223A (es)
PE (1) PE20030977A1 (es)
PL (1) PL371735A1 (es)
RU (1) RU2004126864A (es)
TW (1) TW200302717A (es)
WO (1) WO2003066592A1 (es)
ZA (1) ZA200406237B (es)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2304140C2 (ru) 2001-12-27 2007-08-10 Дайити Фармасьютикал Ко., Лтд. ИНГИБИТОРЫ ПРОДУЦИРОВАНИЯ / СЕКРЕЦИИ β-АМИЛОИДНОГО БЕЛКА
US7256186B2 (en) 2002-02-06 2007-08-14 Schering Corporation Gamma secretase inhibitors
US20040171614A1 (en) * 2002-02-06 2004-09-02 Schering-Plough Corporation Novel gamma secretase inhibitors
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
NZ542304A (en) 2003-03-14 2009-07-31 Ono Pharmaceutical Co Nitrogen-containing heterocyclic derivatives and drugs containing the same as the active ingredient
CA2526487A1 (en) 2003-06-30 2005-01-06 Daiichi Pharmaceutical Co., Ltd. Heterocyclic methyl sulfone derivative
ATE424383T1 (de) 2003-08-08 2009-03-15 Schering Corp Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren
AR045219A1 (es) 2003-08-08 2005-10-19 Pharmacopeia Inc Aminas ciclicas inhibidoras de base - 1 que poseen un sustiuyente heterociclico
EP1680406A1 (en) * 2003-10-29 2006-07-19 Elan Pharmaceuticals, Inc. N-substituted benzene sulfonamides
EP1740570A2 (en) * 2004-04-05 2007-01-10 Schering Corporation Novel gamma secretase inhibitors
EP1758884A2 (en) * 2004-05-20 2007-03-07 Elan Pharmaceuticals, Inc. N-cyclic sulfonamido inhibitors of gamma secretase
US7763613B2 (en) * 2004-06-30 2010-07-27 Schering Corporation Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors
JP4845883B2 (ja) * 2004-07-13 2011-12-28 エフ．ホフマン−ラ ロシュ アーゲー スルホンアミド誘導体
AR049726A1 (es) 2004-07-22 2006-08-30 Schering Corp Amidas sustituidas inhibidoras de beta secretasa
ES2457041T3 (es) 2004-09-13 2014-04-24 Ono Pharmaceutical Co., Ltd. Derivados de N-4-piperidilurea y medicamentos que los contienen como principio activo
GB0423356D0 (en) * 2004-10-21 2004-11-24 Merck Sharp & Dohme Therapeutic agents
EP1916985A4 (en) * 2005-08-19 2010-06-09 Elan Pharm Inc BRIDGED N-CYCLIC SULPHONAMIDE INHIBITORS OF THE GAMMED CRYSTETRY
BRPI0708731A2 (pt) 2006-03-10 2011-06-07 Ono Pharmaceutical Co derivado heterocìclico nitrogenado, e agente farmacêutico compreendendo o derivado como ingrediente ativo
US20100226922A1 (en) * 2006-06-08 2010-09-09 Dorothea Maetzel Specific protease inhibitors and their use in cancer therapy
CN101553481A (zh) * 2006-09-29 2009-10-07 格吕伦塔尔有限公司 取代的磺酰胺衍生物
JP5379692B2 (ja) 2006-11-09 2013-12-25 プロビオドルグ エージー 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての３−ヒドロキシ−１，５−ジヒドロ−ピロール−２−オン誘導体
JP2010510224A (ja) * 2006-11-17 2010-04-02 アボット・ラボラトリーズ ケモカイン受容体拮抗薬としてのアミノピロリジン類
DK2091948T3 (da) 2006-11-30 2012-07-23 Probiodrug Ag Nye inhibitorer af glutaminylcyclase
US8080549B2 (en) * 2007-01-12 2011-12-20 Concert Pharmaceuticals, Inc. Endothelin receptor antagonists
AU2008220785B2 (en) 2007-03-01 2013-02-21 Vivoryon Therapeutics N.V. New use of glutaminyl cyclase inhibitors
US9656991B2 (en) 2007-04-18 2017-05-23 Probiodrug Ag Inhibitors of glutaminyl cyclase
WO2008147800A1 (en) * 2007-05-25 2008-12-04 Elan Pharmaceuticals, Inc. Pyrazolopyrrolidines as inhibitors of gamma secretase
US20110251220A1 (en) * 2008-06-03 2011-10-13 Acikgoez Oezlem Pharmaceutical compositions comprising gamma secretase modulators
EP2475428B1 (en) 2009-09-11 2015-07-01 Probiodrug AG Heterocylcic derivatives as inhibitors of glutaminyl cyclase
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
EA022420B1 (ru) 2010-03-10 2015-12-30 Пробиодруг Аг Гетероциклические ингибиторы глутаминилциклазы (qc, ec 2.3.2.5)
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
EP2953940B1 (en) 2013-02-07 2018-08-22 Heptares Therapeutics Limited Piperidin-1-yl and azepin-1-yl carboxylates as muscarinic m4 receptor agonists
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2687146B1 (fr) * 1992-02-12 1994-04-01 Adir Cie Nouveaux derives de pyrrolidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
US6166037A (en) * 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
GB9800750D0 (en) * 1998-01-14 1998-03-11 Lilly Co Eli Pharmaceutical compound
GB9804426D0 (en) 1998-03-02 1998-04-29 Pfizer Ltd Heterocycles
TW575561B (en) * 1999-03-25 2004-02-11 Hoffmann La Roche 1-arenesulfonyl-2-aryl-pyrrolidine and piperidine derivatives
US6589978B2 (en) * 2000-06-30 2003-07-08 Hoffman-La Roche Inc. 1-sulfonyl pyrrolidine derivatives

Also Published As

Publication number Publication date
NO329067B1 (no) 2010-08-16
US20040048848A1 (en) 2004-03-11
ECSP045218A (es) 2004-09-28
JP4758609B2 (ja) 2011-08-31
RU2004126864A (ru) 2005-07-10
AU2003210865B2 (en) 2008-01-31
BR0307492A (pt) 2004-11-23
MY141504A (en) 2010-05-14
TW200302717A (en) 2003-08-16
US7208602B2 (en) 2007-04-24
US20060100427A1 (en) 2006-05-11
AR038482A1 (es) 2005-01-19
MXPA04007659A (es) 2005-06-08
JP2005522437A (ja) 2005-07-28
NZ534223A (en) 2007-05-31
CA2478423A1 (en) 2003-08-14
ZA200406237B (en) 2005-09-22
KR20040081489A (ko) 2004-09-21
NO20043696L (no) 2004-11-05
CN1628100A (zh) 2005-06-15
WO2003066592A1 (en) 2003-08-14
EP1472223A1 (en) 2004-11-03
CO5611195A2 (es) 2006-02-28
PL371735A1 (en) 2005-06-27
AU2003210865A1 (en) 2003-09-02

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