CN1628100A - γ-分泌酶抑制剂 - Google Patents

γ-分泌酶抑制剂 Download PDF

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Publication number
CN1628100A
CN1628100A CNA038032686A CN03803268A CN1628100A CN 1628100 A CN1628100 A CN 1628100A CN A038032686 A CNA038032686 A CN A038032686A CN 03803268 A CN03803268 A CN 03803268A CN 1628100 A CN1628100 A CN 1628100A
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CN
China
Prior art keywords
alkyl
substituted
aryl
alkylene
unsubstituted
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.)
Pending
Application number
CNA038032686A
Other languages
English (en)
Chinese (zh)
Inventor
D·A·皮沙尼斯基
H·B·乔西恩
E·M·史密斯
J·W·克拉德
T·艾斯贝罗姆
郭涛
D·W·霍布斯
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.)
Pharmacopeia Drug Discovery Inc
Merck Sharp and Dohme LLC
Original Assignee
Pharmacopeia Inc
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 Inc, Schering Corp filed Critical Pharmacopeia Inc
Publication of CN1628100A publication Critical patent/CN1628100A/zh
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96Sulfur atom
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-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)
CNA038032686A 2002-02-06 2003-02-05 γ-分泌酶抑制剂 Pending CN1628100A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US35561802P 2002-02-06 2002-02-06
US60/355,618 2002-02-06

Publications (1)

Publication Number Publication Date
CN1628100A true CN1628100A (zh) 2005-06-15

Family

ID=27734543

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA038032686A Pending CN1628100A (zh) 2002-02-06 2003-02-05 γ-分泌酶抑制剂

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=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101035765B (zh) * 2004-07-13 2010-10-13 弗·哈夫曼-拉罗切有限公司 磺酰胺衍生物

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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
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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
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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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101035765B (zh) * 2004-07-13 2010-10-13 弗·哈夫曼-拉罗切有限公司 磺酰胺衍生物

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
JP4758609B2 (ja) 2011-08-31
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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Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
ASS Succession or assignment of patent right

Owner name: PHARMECPIA DRUG R & D CO., LTD.

Free format text: FORMER OWNER: PHARMACOPEIA INC.

Effective date: 20050610

C41 Transfer of patent application or patent right or utility model
TA01 Transfer of patent application right

Effective date of registration: 20050610

Address after: Kenilworth in New Jersey in the United States

Applicant after: SCHERING CORP (US)

Co-applicant after: Pharmacopeia Drug Discovery

Address before: Kenilworth in New Jersey in the United States

Applicant before: SCHERING CORP (US)

Co-applicant before: Pharmacopeia Inc.

C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Open date: 20050615