PE20050068A1 - 2-cianopirrolopirimidinas como inhibidores de la catepsina s - Google Patents

2-cianopirrolopirimidinas como inhibidores de la catepsina s

Info

Publication number
PE20050068A1
PE20050068A1 PE2004000127A PE2004000127A PE20050068A1 PE 20050068 A1 PE20050068 A1 PE 20050068A1 PE 2004000127 A PE2004000127 A PE 2004000127A PE 2004000127 A PE2004000127 A PE 2004000127A PE 20050068 A1 PE20050068 A1 PE 20050068A1
Authority
PE
Peru
Prior art keywords
pyridyl
phenyl
catepsin
inhibitors
dimethylethyl
Prior art date
Application number
PE2004000127A
Other languages
English (en)
Inventor
Francis Paul Buxton
Takeru Ehara
Pamposh Ganju
Allan Hallett
Osamu Irie
Atsuko Iwasaki
Takanori Kanazawa
Keiichi Masuya
Kazuhiko Nonomura
Junichi Sakaki
Christopher Robert Snell
Chuanzheng Song
Keiko Tanabe
Naoki Teno
Ichiro Umemura
Fumiaki Yokokawa
Original Assignee
Novartis Ag
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
Priority claimed from GB0302748A external-priority patent/GB0302748D0/en
Priority claimed from GB0304642A external-priority patent/GB0304642D0/en
Priority claimed from GB0304641A external-priority patent/GB0304641D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20050068A1 publication Critical patent/PE20050068A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

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

Abstract

SE REFIERE A DERIVADOS DE PIRROLO PIRIMIDINA DE FORMULA I, EN DONDE Y ES -(CH2)t-O o -(CH2)r-S-; p ES 1 o 2; r Y t SON 1,2 o 3; R1 ES FENILO, PIRIDILO, PIRIMIDILO, INDOLILO, ENTRE OTROS; R2 ES ALQUILO OPCIONALMENTE SUSTITUIDO POR CICLOALQUILO EL CUAL ESTA OPCIONALMENTE SUSTITUIDO POR HALOGENO O ES FENILO MONO O DI SUSTITUIDO POR HALOGENO; SIEMPRE QUE R2 NO REPRESENTE 1,1-DIMETILETILO SI Y ES O Y R1 SEA 3-PIRIDILO, 4-PIRIDILO, 5-CLORO-3-PIRIDILO, 6-CLORO-3-PIRIDILO, ENTRE OTROS; Y SIEMPRE QUE R2 NO SEA 1,1-DIMETILETILO SI Y ES S y R1 SEA 4-PIRIDILO. EN OTRAS OPCIONES Y ES -(CH2)- o -CH=CH-, Y p ES 1 O 2; O Y ES -(CH2)f-, f ES 1 O 2, p ES 1. SON COMPUESTOS PREFERIDOS: 6-BROMOMETIL-2-CIANO-7-(2-CICLOHEXIL-ETIL)-7H-PIRROLO[2.3-d]PIRIMIDINA; ESTER TER-BUTILICO DEL ACIDO 4-(4-HIDROXI-FENIL)-PIPERIDIN-1-CARBOXILICO; ESTER BUTILICOO DEL ACIDO 4-(4-HIDROXI-FENIL)-3,6-DIHIDRO-2H-PIRIDIN-1-CARBOXILICO, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y UNA COMPOSICION. ESTOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE LAS ENZIMAS DE CATEPSINA S Y SON UTILES PARA EL TRATAMIENTO Y PREVENCION DEL DOLOR NEUROPATICO
PE2004000127A 2003-02-06 2004-02-04 2-cianopirrolopirimidinas como inhibidores de la catepsina s PE20050068A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0302748A GB0302748D0 (en) 2003-02-06 2003-02-06 Organic compounds
GB0304642A GB0304642D0 (en) 2003-02-28 2003-02-28 Organic compounds
GB0304641A GB0304641D0 (en) 2003-02-28 2003-02-28 Organic compounds

Publications (1)

Publication Number Publication Date
PE20050068A1 true PE20050068A1 (es) 2005-03-11

Family

ID=32854008

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000127A PE20050068A1 (es) 2003-02-06 2004-02-04 2-cianopirrolopirimidinas como inhibidores de la catepsina s

Country Status (17)

Country Link
US (1) US20060247251A1 (es)
EP (1) EP1592426B1 (es)
JP (1) JP4499667B2 (es)
AR (1) AR043692A1 (es)
AT (1) ATE381335T1 (es)
AU (1) AU2004210422B2 (es)
BR (1) BRPI0407327A (es)
CA (1) CA2514287A1 (es)
DE (1) DE602004010785T2 (es)
ES (1) ES2297378T3 (es)
HK (1) HK1084883A1 (es)
MX (1) MXPA05008348A (es)
PE (1) PE20050068A1 (es)
PL (1) PL378135A1 (es)
PT (1) PT1592426E (es)
TW (1) TW200420566A (es)
WO (1) WO2004069256A1 (es)

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GB0304640D0 (en) * 2003-02-28 2003-04-02 Novartis Ag Organic compounds
EP1797883A3 (en) * 2003-04-28 2007-08-01 Novartis AG Pharmaceutical composition comprising a cathepsin S inhibitor and an opioid
CA2564953A1 (en) * 2004-05-03 2005-11-24 Janssen Pharmaceutica N.V. Novel indole derivatives as selective androgen receptor modulators (sarms)
US9107864B2 (en) 2004-06-07 2015-08-18 Qu Biologics Inc. Tissue targeted antigenic activation of the immune response to treat cancers
US8501198B2 (en) 2004-06-07 2013-08-06 Qu Biologics Inc. Tissue targeted antigenic activation of the immune response to treat cancers
SI2448938T1 (sl) 2009-06-29 2014-08-29 Incyte Corporation Experimental Station Pirimidinoni kot zaviralci pi3k
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
UY33304A (es) * 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
US9193721B2 (en) 2010-04-14 2015-11-24 Incyte Holdings Corporation Fused derivatives as PI3Kδ inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
KR102157718B1 (ko) 2010-07-26 2020-09-18 큐 바이올로직스 인코포레이티드 면역원성 소염 조성물
TWI501967B (zh) * 2010-12-16 2015-10-01 Janssen R&D Ireland 作為呼吸道融合病毒抗病毒劑之氮雜吲哚類
TWI527814B (zh) 2010-12-16 2016-04-01 健生科學愛爾蘭無限公司 作為呼吸道融合病毒抗病毒劑之氮雜苯并咪唑類
TWI515187B (zh) 2010-12-16 2016-01-01 健生科學愛爾蘭無限公司 作為呼吸道融合病毒抗病毒劑之吲哚類
ES2764848T3 (es) 2010-12-20 2020-06-04 Incyte Holdings Corp N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
HUE030869T2 (en) 2011-09-02 2017-06-28 Incyte Holdings Corp Heterocyclic amines as inhibitors of PI3K
CN103304525B (zh) * 2012-03-08 2015-08-05 深圳海王药业有限公司 一种制备达非那新中间体5-(卤代乙基)-2,3-二氢苯并呋喃的方法
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
EP2840083B1 (en) * 2012-04-17 2017-09-13 Astellas Pharma Inc. Nitrogenated bicyclic aromatic heterocyclic compound
ES2632914T3 (es) * 2012-06-15 2017-09-18 Janssen Sciences Ireland Uc Derivados de 1,3-dihidro-2H-bencimidazol-2-ona sustituidos con heterociclos como agentes antivirales para el virus respiratorio sincicial
CA2884491C (en) 2012-10-16 2021-08-31 Abdellah Tahri Rsv antiviral compounds
EP2970269B1 (en) * 2013-03-14 2017-04-19 Novartis AG 2-(1h-indol-4-ylmethyl)-3h-imidazo[4,5-b]pyridine-6-carbonitrile derivatives as complement factor b inhibitors useful for the treatment of ophthalmic diseases
JP2016535042A (ja) 2013-10-30 2016-11-10 ノバルティス アーゲー ２−ベンジル−ベンゾイミダゾール補体因子ｂ阻害剤およびその使用
TWI671299B (zh) 2014-04-14 2019-09-11 愛爾蘭商健生科學愛爾蘭無限公司 作為ｒｓｖ抗病毒化合物之螺脲化合物
US10251946B2 (en) 2014-05-02 2019-04-09 Qu Biologics Inc. Anti-microbial immunomodulation
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
TWI748941B (zh) 2015-02-27 2021-12-11 美商英塞特公司 Ｐｉ３ｋ抑制劑之鹽及製備方法
WO2016179157A1 (en) 2015-05-05 2016-11-10 Carafe Drug Innovation, Llc Substituted 5-hydroxyoxindoles and their use as analgesics and fever reducers
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
JP2021500416A (ja) * 2017-10-27 2021-01-07 エステベ ファーマスーティカルズ，ソシエダッド アノニマ 疼痛及び疼痛関連状態を治療するための新規アルコキシアミノ誘導体
WO2020048829A1 (en) 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 3,9-diazaspiro[5.5]undecane compounds

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JP2002519325A (ja) * 1998-06-30 2002-07-02 イーライ・リリー・アンド・カンパニー 二環性ｓＰＬＡ２インヒビター
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US20030144234A1 (en) * 2001-08-30 2003-07-31 Buxton Francis Paul Methods for the treatment of chronic pain and compositions therefor
GB0121033D0 (en) * 2001-08-30 2001-10-24 Novartis Ag Organic compounds

Also Published As

Publication number Publication date
US20060247251A1 (en) 2006-11-02
JP2006516554A (ja) 2006-07-06
WO2004069256A8 (en) 2004-10-14
TW200420566A (en) 2004-10-16
EP1592426B1 (en) 2007-12-19
ES2297378T3 (es) 2008-05-01
MXPA05008348A (es) 2005-11-04
AU2004210422A1 (en) 2004-08-19
DE602004010785D1 (de) 2008-01-31
CA2514287A1 (en) 2004-08-19
PL378135A1 (pl) 2006-03-06
BRPI0407327A (pt) 2006-01-10
ATE381335T1 (de) 2008-01-15
EP1592426A1 (en) 2005-11-09
DE602004010785T2 (de) 2008-12-04
JP4499667B2 (ja) 2010-07-07
HK1084883A1 (en) 2006-08-11
AU2004210422B2 (en) 2008-01-17
AR043692A1 (es) 2005-08-10
WO2004069256A1 (en) 2004-08-19
PT1592426E (pt) 2008-03-13

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