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
KR100927304B1 (ko) 2001-12-27 2009-11-18 다이이찌 세이야꾸 가부시기가이샤 β-아밀로이드 단백 생산·분비 저해제
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
CA2517888C (en) 2003-03-14 2012-05-01 Ono Pharmaceutical Co., Ltd. Nitrogen-containing heterocyclic derivatives and drugs containing the same as the active ingredient
PL379466A1 (pl) 2003-06-30 2006-09-18 Daiichi Sankyo Company , Limited Heterocykliczne pochodne metylosulfonu
CA2534950A1 (en) 2003-08-08 2005-02-24 Schering Corporation Cyclic amine bace-1 inhibitors having a benzamide substituent
DE602004015476D1 (de) 2003-08-08 2008-09-11 Schering Corp Cyclische amine mit einem heterocyclischen substituenten als bace-1-inhibitoren
US7208488B2 (en) 2003-10-29 2007-04-24 Elan Pharmaceuticals, Inc. N-substituted benzene sulfonamides
AR049377A1 (es) * 2004-04-05 2006-07-26 Schering Corp Inhibidores de secretasa gamma
JP2007538106A (ja) * 2004-05-20 2007-12-27 イーラン ファーマスーティカルズ、インコーポレイテッド γセクレターゼのＮ−環式スルホンアミド阻害剤
AR050994A1 (es) 2004-06-30 2006-12-13 Schering Corp N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasas, y composicion farmaceutica en base al compuesto
KR100880972B1 (ko) * 2004-07-13 2009-02-03 에프. 호프만-라 로슈 아게 설폰아마이드 유도체
EP1781625B1 (en) 2004-07-22 2010-12-15 Schering Corporation Substituted amide beta secretase inhibitors
RU2409565C2 (ru) 2004-09-13 2011-01-20 Оно Фармасьютикал Ко., Лтд. Азотистые гетероциклические производные и лекарственные средства, содержащие их в качестве активного ингредиента
GB0423356D0 (en) * 2004-10-21 2004-11-24 Merck Sharp & Dohme Therapeutic agents
WO2007022502A2 (en) * 2005-08-19 2007-02-22 Elan Pharmaceuticals, Inc. Bridged n-cyclic sulfonamido inhibitors of gamma secretase
JPWO2007105637A1 (ja) 2006-03-10 2009-07-30 小野薬品工業株式会社 含窒素複素環誘導体およびそれらを有効成分とする薬剤
US20100226922A1 (en) * 2006-06-08 2010-09-09 Dorothea Maetzel Specific protease inhibitors and their use in cancer therapy
KR20090079914A (ko) * 2006-09-29 2009-07-22 그뤼넨탈 게엠베하 치환된 설폰아미드 유도체
EP2089383B1 (en) 2006-11-09 2015-09-16 Probiodrug AG 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US8754107B2 (en) * 2006-11-17 2014-06-17 Abbvie Inc. Aminopyrrolidines as chemokine receptor antagonists
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
US8080549B2 (en) * 2007-01-12 2011-12-20 Concert Pharmaceuticals, Inc. Endothelin receptor antagonists
CA2679446C (en) 2007-03-01 2016-05-17 Probiodrug Ag New use of glutaminyl cyclase inhibitors
EP2142514B1 (en) 2007-04-18 2014-12-24 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
NZ582039A (en) * 2007-05-25 2012-02-24 Elan Pharm Inc Pyrazolopyrrolidines as inhibitors of gamma secretase
WO2009146875A1 (en) * 2008-06-03 2009-12-10 Fresenius Medical Care Deutschland Gmbh Pharmaceutical compositions comprising gamma secretase modulators
CA2772488C (en) 2009-09-11 2018-04-17 Probiodrug Ag Heterocyclic derivatives as inhibitors of glutaminyl cyclase
ES2586231T3 (es) 2010-03-03 2016-10-13 Probiodrug Ag Inhibidores de glutaminil ciclasa
EP2545047B9 (en) 2010-03-10 2015-06-10 Probiodrug AG Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
US8541596B2 (en) 2010-04-21 2013-09-24 Probiodrug Ag Inhibitors
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
US9593106B2 (en) 2013-02-07 2017-03-14 Heptares Therapeutics Limited Piperidin-1-yl and azepin-1-yl carboxylates as muscarinic M4 receptor agonists
EP3461819B1 (en) 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase

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

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Legal Events

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FG Grant, registration
FD Application declared void or lapsed