EA201070495A1 - МОДУЛЯТОРЫ АКТИВНОСТИ γ-СЕКРЕТАЗЫ ИЗ ГРУППЫ ПИПЕРИДИНИЛА И ПИПЕРАЗИНИЛА - Google Patents

МОДУЛЯТОРЫ АКТИВНОСТИ γ-СЕКРЕТАЗЫ ИЗ ГРУППЫ ПИПЕРИДИНИЛА И ПИПЕРАЗИНИЛА

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Publication number
EA201070495A1
EA201070495A1 EA201070495A EA201070495A EA201070495A1 EA 201070495 A1 EA201070495 A1 EA 201070495A1 EA 201070495 A EA201070495 A EA 201070495A EA 201070495 A EA201070495 A EA 201070495A EA 201070495 A1 EA201070495 A1 EA 201070495A1
Authority
EA
Eurasian Patent Office
Prior art keywords
piperasininil
piperidinyl
group
secretase activity
activity modulators
Prior art date
Application number
EA201070495A
Other languages
English (en)
Other versions
EA017119B1 (ru
Inventor
Чих Юнг Хо
Original Assignee
Янссен Фармацевтика, Н.В.
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 Янссен Фармацевтика, Н.В. filed Critical Янссен Фармацевтика, Н.В.
Publication of EA201070495A1 publication Critical patent/EA201070495A1/ru
Publication of EA017119B1 publication Critical patent/EA017119B1/ru

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/38—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

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

Abstract

Настоящее изобретение относится к соединениям с общей формулой I, приведенной ниже, природа групп Het, R, R, R, R, R, R, R, Rи Rв которой объясняется в спецификации. Соединения формулы I могут применяться для лечения заболеваний, связанных с активностью γ-секретазы, включая болезнь Альцгеймера.
EA201070495A 2007-10-19 2008-10-15 МОДУЛЯТОРЫ АКТИВНОСТИ γ-СЕКРЕТАЗЫ ИЗ ГРУППЫ ПИПЕРИДИНИЛА И ПИПЕРАЗИНИЛА EA017119B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US98118907P 2007-10-19 2007-10-19
PCT/US2008/079905 WO2009052126A1 (en) 2007-10-19 2008-10-15 PIPERIDINYL AND PIPERAZINYL MODULATORS OF γ-SECRETASE

Publications (2)

Publication Number Publication Date
EA201070495A1 true EA201070495A1 (ru) 2010-10-29
EA017119B1 EA017119B1 (ru) 2012-09-28

Family

ID=40090456

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201070495A EA017119B1 (ru) 2007-10-19 2008-10-15 МОДУЛЯТОРЫ АКТИВНОСТИ γ-СЕКРЕТАЗЫ ИЗ ГРУППЫ ПИПЕРИДИНИЛА И ПИПЕРАЗИНИЛА

Country Status (19)

Country Link
US (1) US8252935B2 (ru)
EP (1) EP2212287B1 (ru)
JP (1) JP5439381B2 (ru)
KR (1) KR101569391B1 (ru)
CN (1) CN101903347B (ru)
AT (1) ATE543799T1 (ru)
AU (1) AU2008312612B2 (ru)
BR (1) BRPI0817433A2 (ru)
CA (1) CA2702837A1 (ru)
CO (1) CO6270359A2 (ru)
CR (1) CR11447A (ru)
EA (1) EA017119B1 (ru)
ES (1) ES2378594T3 (ru)
IL (1) IL205045A (ru)
MX (1) MX2010004309A (ru)
NI (1) NI201000064A (ru)
NZ (1) NZ584716A (ru)
WO (1) WO2009052126A1 (ru)
ZA (1) ZA201003519B (ru)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008312371B2 (en) * 2007-10-19 2013-06-20 Janssen Pharmaceutica, N.V. Amine linked modulators of gamma-secretase
JP5439381B2 (ja) 2007-10-19 2014-03-12 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ γ−セクレターゼのピペリジニル及びピペラジニル調節物質
WO2009052334A1 (en) * 2007-10-19 2009-04-23 Janssen Pharmaceutica, N.V. Carbon linked modulators of y-secretase
US20120129189A1 (en) * 2009-07-17 2012-05-24 Chulan Kwon Methods of Controlling Cell Proliferation
US20120135997A1 (en) 2009-07-17 2012-05-31 Shionogi & Co., Ltd. Pharmaceutical composition comprising a lactam or benzenesulfonamide compound
JP5883794B2 (ja) * 2009-11-05 2016-03-15 フィブロスタチン ソシエダ リミターダＦｉｂｒｏｓｔａｔｉｎ，Ｓｏｃｉｅｄａｄ Ｌｉｍｉｔａｄａ 擬似ｑ２ペプチドを用いるｇｐｂｐ抑制
RS64950B1 (sr) 2018-09-03 2024-01-31 Hoffmann La Roche Derivati bicikličnog heteroarila

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BE790287A (fr) * 1971-10-28 1973-04-19 Delalande Sa Acides pyrimidin-6yl acethydroxamiques, leur procede de preparation et leur application en therapeutique
BE826017R (fr) 1974-03-19 1975-08-26 Acides pyrimidin-6yl acethydroxamiques, leur procede de preparation et leur application en therapeutique
US4252951A (en) 1979-10-09 1981-02-24 Eli Lilly And Company Isolation of syn-7-(2-amino-4-thiazolyl)-(methoxyimino)acetamido-3-acetoxymethyl-3-cephem-4-carboxylic acid
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DE10131899A1 (de) 2001-07-04 2003-02-27 Boehringer Ingelheim Pharma In vitro-Screening-Assay für gamma-Secretase
WO2005097768A2 (en) * 2004-04-05 2005-10-20 Schering Corporation Novel gamma secretase inhibitors
WO2005110963A1 (en) * 2004-05-19 2005-11-24 Cellzome Ag (biphenyl-3-yl)-carboxylic acids and derivatives thereof and their use in therapy
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WO2009052334A1 (en) 2007-10-19 2009-04-23 Janssen Pharmaceutica, N.V. Carbon linked modulators of y-secretase
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Also Published As

Publication number Publication date
CR11447A (es) 2011-01-14
MX2010004309A (es) 2010-05-03
CN101903347A (zh) 2010-12-01
IL205045A (en) 2015-08-31
KR101569391B1 (ko) 2015-11-16
US8252935B2 (en) 2012-08-28
WO2009052126A1 (en) 2009-04-23
EA017119B1 (ru) 2012-09-28
JP2011500700A (ja) 2011-01-06
AU2008312612A1 (en) 2009-04-23
ES2378594T8 (es) 2013-02-27
ZA201003519B (en) 2012-07-25
EP2212287B1 (en) 2012-02-01
ES2378594T3 (es) 2012-04-16
US20090105275A1 (en) 2009-04-23
CN101903347B (zh) 2013-03-27
BRPI0817433A2 (pt) 2015-06-16
CO6270359A2 (es) 2011-04-20
NI201000064A (es) 2010-09-13
ATE543799T1 (de) 2012-02-15
NZ584716A (en) 2011-12-22
CA2702837A1 (en) 2009-04-23
EP2212287A1 (en) 2010-08-04
AU2008312612B2 (en) 2013-11-28
KR20100083829A (ko) 2010-07-22
AU2008312612A2 (en) 2010-07-22
AU2008312612A8 (en) 2010-05-27
JP5439381B2 (ja) 2014-03-12
IL205045A0 (en) 2010-11-30

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU