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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 GB0304641A external-priority patent/GB0304641D0/en
Priority claimed from GB0304642A external-priority patent/GB0304642D0/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)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (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
GB0304641A GB0304641D0 (en) 2003-02-28 2003-02-28 Organic compounds
GB0304642A GB0304642D0 (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 (16)

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)
MX (1) MXPA05008348A (es)
PE (1) PE20050068A1 (es)
PL (1) PL378135A1 (es)
PT (1) PT1592426E (es)
TW (1) TW200420566A (es)
WO (1) WO2004069256A1 (es)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0201980D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
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
CN1980934B (zh) * 2004-05-03 2011-10-26 詹森药业有限公司 作为选择性雄激素受体调节剂（sarms）的新的吲哚衍生物
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
CA2766100C (en) 2009-06-29 2018-05-22 Incyte Corporation Pyrimidinones as pi3k inhibitors
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
WO2011130342A1 (en) 2010-04-14 2011-10-20 Incyte Corporation FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS
WO2011163195A1 (en) 2010-06-21 2011-12-29 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
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
KR102131612B1 (ko) 2011-09-02 2020-07-08 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
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
MX355055B (es) * 2012-04-17 2018-04-03 Astellas Pharma Inc Compuesto heterociclico aromatico biciclico nitrogenado.
JP6259451B2 (ja) 2012-06-15 2018-01-10 ヤンセン・サイエンシズ・アイルランド・ユーシー Ｒｓウイルス抗ウイルス薬としての、複素環によって置換された新規１，３−ジヒドロ−２ｈ−ベンゾイミダゾル−２−オン誘導体
NZ705759A (en) 2012-10-16 2019-01-25 Janssen Sciences Ireland Uc Rsv antiviral compounds
US9475806B2 (en) 2013-03-14 2016-10-25 Novartis Ag Complement factor B inhibitors and uses there of
EP3089963A1 (en) 2013-10-30 2016-11-09 Novartis AG 2-benzyl-benzimidazole complement factor b inhibitors and uses thereof
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
JP6632607B2 (ja) 2014-05-02 2020-01-22 クー バイオロジックス インク．Ｑｕ Ｂｉｏｌｏｇｉｃｓ Ｉｎｃ． 抗微生物免疫修飾
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
SI3831833T1 (sl) 2015-02-27 2023-03-31 Incyte Holdings Corporation Postopki za pripravo inhibitorja PI3K
WO2016179157A1 (en) 2015-05-05 2016-11-10 Carafe Drug Innovation, Llc Substituted 5-hydroxyoxindoles and their use as analgesics and fever reducers
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
MX2020003575A (es) * 2017-10-27 2020-07-22 Esteve Pharmaceuticals Sa Nuevos derivados de alcoxiamino para tratar dolor y estados relacionados con dolor.
IL278889B2 (en) 2018-06-01 2025-11-01 Incyte Corp Dosing regimen for the treatment of pi3k related disorders
AR116020A1 (es) 2018-09-03 2021-03-25 Bayer Ag COMPUESTOS DE 3,9-DIAZAESPIRO[5.5]UNDECANO COMO INHIBIDORES DE GGTasa I Y SU USO PARA EL TRATAMIENTO DE ENFERMEDADES HIPERPROLIFERATIVAS
EP4165034A1 (en) 2020-06-11 2023-04-19 Janssen Sciences Ireland Unlimited Company Hemi (l)-tartrate forms of 3-({5-chloro-1-[3-(methylsulfonyl)propyl]-1h-indol-2 yl} methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2h-imidazo[4,5-c]pyridin-2-one and pharmaceutical compositions comprising the same
CN116396202A (zh) * 2023-04-17 2023-07-07 南京优氟医药科技有限公司 一种（2s，4s）-4-氟代吡咯烷-2-羧酸的制备方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997034895A1 (de) * 1996-03-15 1997-09-25 Novartis Ag NEUE N-7 HETEROCYCLYL-PYRROLO[2,3-d]PYRIMIDINE UND IHRE VERWENDUNG
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
GB0100622D0 (en) * 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
GB0121033D0 (en) * 2001-08-30 2001-10-24 Novartis Ag Organic compounds
US20030144234A1 (en) * 2001-08-30 2003-07-31 Buxton Francis Paul Methods for the treatment of chronic pain and compositions therefor

Also Published As

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

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