JP4758609B2 - γ−セクレターゼ阻害剤 - Google Patents

γ−セクレターゼ阻害剤 Download PDF

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Publication number
JP4758609B2
JP4758609B2 JP2003565966A JP2003565966A JP4758609B2 JP 4758609 B2 JP4758609 B2 JP 4758609B2 JP 2003565966 A JP2003565966 A JP 2003565966A JP 2003565966 A JP2003565966 A JP 2003565966A JP 4758609 B2 JP4758609 B2 JP 4758609B2
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JP
Japan
Prior art keywords
mmol
alkyl
compound
dcm
give
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2003565966A
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English (en)
Japanese (ja)
Other versions
JP2005522437A5 (https=
JP2005522437A (ja
Inventor
ドミトリ エイ． ピサニートスキー，
ヒューバート ビー． ジョシエン，
エリザベス エム． スミス，
ジョン ダブリュ． クレダー，
セオドロス アスベロム，
タオ グオ，
ダグラス ダブリュ． ホッブス，
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
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 Schering Corp filed Critical Schering Corp
Publication of JP2005522437A publication Critical patent/JP2005522437A/ja
Publication of JP2005522437A5 publication Critical patent/JP2005522437A5/ja
Application granted granted Critical
Publication of JP4758609B2 publication Critical patent/JP4758609B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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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)
  • Neurosurgery (AREA)
  • Biomedical Technology (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)
JP2003565966A 2002-02-06 2003-02-05 γ−セクレターゼ阻害剤 Expired - Fee Related JP4758609B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US35561802P 2002-02-06 2002-02-06
US60/355,618 2002-02-06
PCT/US2003/003471 WO2003066592A1 (en) 2002-02-06 2003-02-05 Gamma secretase inhibitors

Publications (3)

Publication Number Publication Date
JP2005522437A JP2005522437A (ja) 2005-07-28
JP2005522437A5 JP2005522437A5 (https=) 2006-04-06
JP4758609B2 true JP4758609B2 (ja) 2011-08-31

Family

ID=27734543

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2003565966A Expired - Fee Related JP4758609B2 (ja) 2002-02-06 2003-02-05 γ−セクレターゼ阻害剤

Country Status (21)

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

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100562516C (zh) 2001-12-27 2009-11-25 第一制药株式会社 β-淀粉样蛋白产生和分泌的抑制剂
US20040171614A1 (en) * 2002-02-06 2004-09-02 Schering-Plough Corporation Novel gamma secretase inhibitors
US7256186B2 (en) 2002-02-06 2007-08-14 Schering Corporation Gamma secretase inhibitors
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
WO2004080966A1 (ja) 2003-03-14 2004-09-23 Ono Pharmaceutical Co., Ltd. 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
CA2526487A1 (en) 2003-06-30 2005-01-06 Daiichi Pharmaceutical Co., Ltd. Heterocyclic methyl sulfone derivative
MXPA06001558A (es) 2003-08-08 2006-05-15 Schering Corp Inhibidores de amina ciclica bace-1 que poseen un sustituyente heterociclico.
ES2323068T3 (es) 2003-08-08 2009-07-06 Schering Corporation Inhibidores de bace-1 de aminas ciclicas con un sustituyente de benzamida.
RU2364587C2 (ru) * 2003-10-29 2009-08-20 Элан Фармасьютикалз, Инк. N-замещенные бензолсульфонамиды
TWI300410B (en) * 2004-04-05 2008-09-01 Schering Corp Novel gamma secretase inhibitors
CA2567343A1 (en) * 2004-05-20 2005-12-01 Elan Pharmaceuticals, Inc. N-cyclic sulfonamido inhibitors of gamma secretase
PE20060481A1 (es) * 2004-06-30 2006-06-19 Schering Corp N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasas
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
EP1790637B1 (en) 2004-09-13 2014-01-29 Ono Pharmaceutical Co., Ltd. Derivatives of N-4-piperidyl urea and medicaments containing them as active ingredient
GB0423356D0 (en) * 2004-10-21 2004-11-24 Merck Sharp & Dohme Therapeutic agents
BRPI0614944A2 (pt) * 2005-08-19 2011-04-26 Elan Pharm Inc inibidores sulfonamido n-bicìclicos ponte de gama-secretase
KR20090008217A (ko) 2006-03-10 2009-01-21 오노 야꾸힝 고교 가부시키가이샤 질소 함유 복소환 유도체 및 이들을 유효 성분으로 하는 약제
ATE509956T1 (de) * 2006-06-08 2011-06-15 Helmholtz Zentrum Muenchen Spezifische proteaseinhibitoren und ihre verwendung in der krebstherapie
EP2383267A1 (de) * 2006-09-29 2011-11-02 Grünenthal GmbH Substituierte Sulfonamid-Derivate
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
CA2669917A1 (en) * 2006-11-17 2008-05-22 Dawn M. George Aminopyrrolidines as chemokine receptor antagonists
US9126987B2 (en) 2006-11-30 2015-09-08 Probiodrug Ag Inhibitors of glutaminyl cyclase
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
JP5667440B2 (ja) 2007-04-18 2015-02-12 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体
JP2010528036A (ja) * 2007-05-25 2010-08-19 エラン ファーマシューティカルズ，インコーポレイテッド γセクレターゼの阻害剤としてのピラゾロピロリジン
JP2011523655A (ja) * 2008-06-03 2011-08-18 フレセニウス メディカル ケア ドイッチュランド ゲーエムベーハー ガンマセクレターゼモジュレータを含む医薬組成物
JP5934645B2 (ja) 2009-09-11 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
JP5688745B2 (ja) 2010-03-10 2015-03-25 プロビオドルグ エージー グルタミニルシクラーゼ（ｑｃ、ｅｃ２．３．２．５）の複素環阻害剤
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
WO2014122474A1 (en) 2013-02-07 2014-08-14 Takeda Pharmaceutical Company 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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999036398A1 (en) * 1998-01-14 1999-07-22 Eli Lilly And Company Limited Aminosulphonylbenzamide derivatives as modulators of the activity of neuronal calcium channels
WO1999045006A1 (en) * 1998-03-02 1999-09-10 Pfizer Inc. Heterocyclic compounds as inhibitors of rotamase enzymes
WO2000058285A1 (en) * 1999-03-25 2000-10-05 F. Hoffmann-La Roche Ag 1-arenesulfonyl-2-aryl-pyrrolidine and piperidine derivatives for the treatment of cns disorders
WO2002002554A1 (en) * 2000-06-30 2002-01-10 F. Hoffmann-La Roche Ag Sulfonyl-pyrrolidine derivatives useful for the treatment of neurological disorders

Family Cites Families (2)

* 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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999036398A1 (en) * 1998-01-14 1999-07-22 Eli Lilly And Company Limited Aminosulphonylbenzamide derivatives as modulators of the activity of neuronal calcium channels
WO1999045006A1 (en) * 1998-03-02 1999-09-10 Pfizer Inc. Heterocyclic compounds as inhibitors of rotamase enzymes
WO2000058285A1 (en) * 1999-03-25 2000-10-05 F. Hoffmann-La Roche Ag 1-arenesulfonyl-2-aryl-pyrrolidine and piperidine derivatives for the treatment of cns disorders
WO2002002554A1 (en) * 2000-06-30 2002-01-10 F. Hoffmann-La Roche Ag Sulfonyl-pyrrolidine derivatives useful for the treatment of neurological disorders

Also Published As

Publication number Publication date
MY141504A (en) 2010-05-14
AR038482A1 (es) 2005-01-19
RU2004126864A (ru) 2005-07-10
KR20040081489A (ko) 2004-09-21
BR0307492A (pt) 2004-11-23
ZA200406237B (en) 2005-09-22
PE20030977A1 (es) 2003-12-04
AU2003210865B2 (en) 2008-01-31
TW200302717A (en) 2003-08-16
US20040048848A1 (en) 2004-03-11
MXPA04007659A (es) 2005-06-08
CO5611195A2 (es) 2006-02-28
PL371735A1 (en) 2005-06-27
WO2003066592A1 (en) 2003-08-14
CN1628100A (zh) 2005-06-15
NZ534223A (en) 2007-05-31
EP1472223A1 (en) 2004-11-03
US20060100427A1 (en) 2006-05-11
JP2005522437A (ja) 2005-07-28
ECSP045218A (es) 2004-09-28
US7208602B2 (en) 2007-04-24
NO20043696L (no) 2004-11-05
CA2478423A1 (en) 2003-08-14
AU2003210865A1 (en) 2003-09-02
NO329067B1 (no) 2010-08-16

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