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PE20141203A1 - Benzilindazoles sustituidos para uso como inhibidores de la quinasa bub1 en el tratamiento de enfermedades hiperproliferativas - Google Patents

Benzilindazoles sustituidos para uso como inhibidores de la quinasa bub1 en el tratamiento de enfermedades hiperproliferativas

Info

Publication number
PE20141203A1
PE20141203A1 PE2014000471A PE2014000471A PE20141203A1 PE 20141203 A1 PE20141203 A1 PE 20141203A1 PE 2014000471 A PE2014000471 A PE 2014000471A PE 2014000471 A PE2014000471 A PE 2014000471A PE 20141203 A1 PE20141203 A1 PE 20141203A1
Authority
PE
Peru
Prior art keywords
benzylindazoles
inhibitors
substituted
treatment
indazol
Prior art date
Application number
PE2014000471A
Other languages
English (en)
Inventor
Marion Hitchcock
Anne Mengel
Vera Putter
Gerhard Siemeister
Antje Margret Wengner
Hans Briem
Knut Eis
Volker Schulze
Amaury Ernesto Fernandez-Montalvan
Stefan Prechtl
Simon Holton
Jorg Fanghanel
Philip Lienau
Cornelia Preusse
Mark Jean Gnoth
Original Assignee
Bayer Ip Gmbh
Bayer Pharma 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
Application filed by Bayer Ip Gmbh, Bayer Pharma AG filed Critical Bayer Ip Gmbh
Publication of PE20141203A1 publication Critical patent/PE20141203A1/es

Links

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01H—NEW PLANTS OR NON-TRANSGENIC PROCESSES FOR OBTAINING THEM; PLANT REPRODUCTION BY TISSUE CULTURE TECHNIQUES
    • A01H6/00—Angiosperms, i.e. flowering plants, characterised by their botanic taxonomy
    • A01H6/36—Ericaceae, e.g. azalea, cranberry or blueberry
    • A01H6/368—Vaccinium, e.g. cranberry, blueberry
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Developmental Biology & Embryology (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Physiology (AREA)
  • Botany (AREA)
  • Environmental Sciences (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Extrusion Moulding Of Plastics Or The Like (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE BENZILINDAZOLES SUSTITUIDOS DE FORMULA (I) DONDE R1 ES H, HALOGENO O ALQUILO(C1-C3); R2 Y R3 SON CADA UNO H, HALOGENO, CIANO, HALOALQUILO(C1-C6), ENTRE OTROS; R4 ES H, HIDROXI, ALQUENILO(C2-C6), ENTRE OTROS; R6 ES H, CN, ALCOXI(C1-C6), ENTRE OTROS; R7 ES H, ALQUILO(C1-C6), HALOALQUILO(C1-C6), ENTRE OTROS; R8 ES H, HALOGENO, ALQUILO(C1-C6), ENTRE OTROS; n ES DE 0 A 3; m ES DE 0 A 4. SON COMPUESTOS PREFERIDOS: 2-[1-(6-CLORO-2-FLUORO-3-METILBENCIL)-1H-INDAZOL-3-IL]-5-METOXI-N-(PIRIDIN-4-IL)PIRIMIDIN-4-AMINA; 2-[1-(6-CLORO-2-FLUORO-3-METOXIBENCIL)-1H-INDAZOL-3-IL]-5-METOXI-N-(PIRIDIN-4-IL)PIRIMIDIN-4-AMINA; 5-METOXI-2-{1-[3-(5-METIL-1,2,4-OXADIAZOL-3-IL)BENCIL]-1H-INDAZOL-3-IL}-N-(PIRIDIN-4-IL)PIRIMIDIN-4-AMINA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO PARA SU OBTENCION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA QUINASA BUB1 SIENDO UTILES PARA EL TRATAMIENTO DE TUMORES CERVICOUTERINOS, DE MAMA, MELANOMA, METASTASIS
PE2014000471A 2011-10-06 2012-10-04 Benzilindazoles sustituidos para uso como inhibidores de la quinasa bub1 en el tratamiento de enfermedades hiperproliferativas PE20141203A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11184061 2011-10-06

Publications (1)

Publication Number Publication Date
PE20141203A1 true PE20141203A1 (es) 2014-10-01

Family

ID=46968229

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014000471A PE20141203A1 (es) 2011-10-06 2012-10-04 Benzilindazoles sustituidos para uso como inhibidores de la quinasa bub1 en el tratamiento de enfermedades hiperproliferativas

Country Status (38)

Country Link
US (3) US20140249133A1 (es)
EP (1) EP2763982B1 (es)
JP (1) JP6140170B2 (es)
KR (1) KR102007056B1 (es)
CN (1) CN103974948B (es)
AP (1) AP3847A (es)
AR (1) AR088449A1 (es)
AU (1) AU2012320582B2 (es)
BR (1) BR112014008045A2 (es)
CA (1) CA2851037A1 (es)
CO (1) CO6930363A2 (es)
CR (1) CR20140161A (es)
CU (1) CU20140043A7 (es)
CY (1) CY1120318T1 (es)
DK (1) DK2763982T3 (es)
DO (1) DOP2014000062A (es)
EA (1) EA201400412A1 (es)
EC (1) ECSP14013284A (es)
ES (1) ES2665036T3 (es)
GT (1) GT201400063A (es)
HR (1) HRP20180546T1 (es)
HU (1) HUE037154T2 (es)
IL (1) IL231591A (es)
LT (1) LT2763982T (es)
MX (1) MX361279B (es)
NO (1) NO2763982T3 (es)
PE (1) PE20141203A1 (es)
PH (1) PH12014500758A1 (es)
PL (1) PL2763982T3 (es)
PT (1) PT2763982T (es)
RS (1) RS57099B1 (es)
SG (1) SG11201400616YA (es)
SI (1) SI2763982T1 (es)
TN (1) TN2014000138A1 (es)
TW (1) TWI588141B (es)
UA (1) UA111754C2 (es)
UY (1) UY34374A (es)
WO (1) WO2013050438A1 (es)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA111754C2 (uk) 2011-10-06 2016-06-10 Байєр Фарма Акцієнгезелльшафт Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань
JP6141866B2 (ja) 2011-12-21 2017-06-07 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 置換ベンジルピラゾール類
HK1207861A1 (en) * 2012-05-11 2016-02-12 Bayer Pharma Aktiengesellschaft Substituted cycloalkenopyrazoles as bub1 inhibitors for the treatment of cancer
EP2976336A1 (en) 2013-03-21 2016-01-27 Bayer Pharma Aktiengesellschaft 3-heteroaryl substituted indazoles
CA2907730A1 (en) * 2013-03-21 2014-09-25 Bayer Pharma Aktiengesellschaft Diaminoheteroaryl substituted indazoles
WO2014147204A1 (en) * 2013-03-21 2014-09-25 Bayer Pharma Aktiengesellschaft Heteroaryl substituted indazoles
JP2016522231A (ja) * 2013-06-21 2016-07-28 バイエル ファーマ アクチエンゲゼルシャフト ジアミノヘテロアリール置換ピラゾール類
EP3010911A1 (en) * 2013-06-21 2016-04-27 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
JP2016525076A (ja) * 2013-06-21 2016-08-22 バイエル ファーマ アクチエンゲゼルシャフト 置換されたベンジルピラゾール類
EP3010901B1 (en) * 2013-06-21 2017-09-13 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
EP3010902A1 (en) * 2013-06-21 2016-04-27 Bayer Pharma Aktiengesellschaft Substituted benzylpyrazoles
WO2015063003A1 (en) 2013-10-30 2015-05-07 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
WO2015193339A1 (en) * 2014-06-17 2015-12-23 Bayer Pharma Aktiengesellschaft 3-amino-1,5,6,7-tetrahydro-4h-indol-4-ones
CN107074825A (zh) * 2014-09-19 2017-08-18 拜耳制药股份公司 作为bub1激酶抑制剂的苄基取代的吲唑类化合物
CA2961578A1 (en) * 2014-09-19 2016-03-24 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles as bub1 kinase inhibitors
WO2016041925A1 (en) * 2014-09-19 2016-03-24 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles
US10350206B2 (en) 2014-09-19 2019-07-16 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles as BUB1 inhibitors
GB201419264D0 (en) * 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
CN107406417B (zh) 2015-01-28 2020-06-09 拜耳制药股份公司 4H-吡咯并[3,2-c]吡啶-4-酮衍生物
PT3307734T (pt) * 2015-06-09 2020-02-25 Abbvie Inc Moduladores de recetores nucleares (ror) para o tratamento de doenças inflamatórias e autoimunes
CA2989469A1 (en) * 2015-06-17 2016-12-22 Bayer Pharma Aktiengesellschaft 3-amino-1,5,6,7-tetrahydro-4h-indol-4-ones
CA3008393A1 (en) * 2015-12-16 2017-06-22 Bayer Pharma Aktiengesellschaft Hetero-1,5,6,7-tetrahydro-4h-indol-4-ones
WO2017148995A1 (en) 2016-03-04 2017-09-08 Bayer Pharma Aktiengesellschaft 1-(pyrimidin-2-yl)-1h-indazoles having bub1 kinase inhibiting activity
WO2017157991A1 (en) 2016-03-18 2017-09-21 Bayer Pharma Aktiengesellschaft 1-alkyl-pyrazoles and -indazoles as bub1 inhibitors for the treatment of hyperproliferative diseases
WO2017157992A1 (en) 2016-03-18 2017-09-21 Bayer Pharma Aktiengesellschaft Annulated pyrazoles as bub1 kinase inhibitors for treating proliferative disorders
WO2018122168A1 (en) 2016-12-29 2018-07-05 Bayer Pharma Aktiengesellschaft Combinations of bub1 kinase and parp inhibitors
WO2018158175A1 (en) 2017-02-28 2018-09-07 Bayer Pharma Aktiengesellschaft Combination of bub1 inhibitors
WO2018206547A1 (en) 2017-05-12 2018-11-15 Bayer Pharma Aktiengesellschaft Combination of bub1 and atr inhibitors
WO2018215282A1 (en) 2017-05-26 2018-11-29 Bayer Pharma Aktiengesellschaft Combination of bub1 and pi3k inhibitors
KR102328682B1 (ko) 2018-08-27 2021-11-18 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
KR102048050B1 (ko) * 2019-08-29 2020-01-22 대한민국 Adb-푸비나카의 대사체 합성 방법
CN110684016A (zh) * 2019-09-27 2020-01-14 上海应用技术大学 一种含氟的azd9291衍生物及其制备方法和应用
EP4217070A1 (en) 2020-09-23 2023-08-02 Scorpion Therapeutics, Inc. Pyrrolo[3,2-c]pyridin-4-one derivatives useful in the treatment of cancer
WO2022072645A2 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Methods for treating cancer
TW202229282A (zh) 2020-09-30 2022-08-01 美商史考皮恩治療有限公司 治療癌症之方法
WO2022094271A1 (en) 2020-10-30 2022-05-05 Scorpion Therapeutics, Inc. Methods for treating cancer
WO2022098992A1 (en) 2020-11-05 2022-05-12 Scorpion Therapeutics, Inc. Use of macrocyclic compounds in methods of treating cancer
WO2022197913A1 (en) 2021-03-18 2022-09-22 Scorpion Therapeutics, Inc. Bicyclic derivatives which can be used to treat cancer
WO2023173083A1 (en) 2022-03-11 2023-09-14 Scorpion Therapeutics, Inc. Tetrahydroindole derivatives as egfr and/or her2 inhibtors useful for the treatment of cancer
JP2025510646A (ja) 2022-03-14 2025-04-15 スラップ ファーマシューティカルズ エルエルシー 多環式化合物
WO2024254298A1 (en) 2023-06-08 2024-12-12 Scorpion Therapeutics, Inc. A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer
WO2024254266A1 (en) 2023-06-08 2024-12-12 Scorpion Therapeutics, Inc. A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5011472A (en) 1988-09-06 1991-04-30 Brown University Research Foundation Implantable delivery system for biological factors
US5470862A (en) 1995-02-03 1995-11-28 Ohmeda Pharmaceutical Products Division Inc. Substituted pyrazolyl compounds and methods employing such compounds
ES2325045T3 (es) 1996-10-14 2009-08-24 Bayer Healthcare Ag Nuevos derivados de pirazol heterociclilmetil sustituidos y su uso en el tratamiento de enfermedades cardiovasculares.
DE19834047A1 (de) * 1998-07-29 2000-02-03 Bayer Ag Substituierte Pyrazolderivate
DE19846514A1 (de) * 1998-10-09 2000-04-20 Bayer Ag Neue Heterocyclyl-methyl-substituierte Pyrazole
JP4286146B2 (ja) 2001-12-18 2009-06-24 メルク エンド カムパニー インコーポレーテッド メタボトロピックグルタミン酸受容体−５のヘテロアリール置換ピラゾール系調節剤
US7166293B2 (en) 2002-03-29 2007-01-23 Carlsbad Technology, Inc. Angiogenesis inhibitors
AU2003272324A1 (en) 2002-09-10 2004-04-30 Scios Inc. INHIBITORS OF TFGBeta
DE10244810A1 (de) * 2002-09-26 2004-04-08 Bayer Ag Neue Morpholin-überbrückte Indazolderivate
US8748601B2 (en) 2003-04-11 2014-06-10 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
WO2005070900A1 (en) 2004-01-22 2005-08-04 Altana Pharma Ag N-4-(6- (heteo) aryl-pyrimidin-4-ylaminophenyl) -bezenesulfonamides as kinase inhibitors
WO2007065010A2 (en) * 2005-12-02 2007-06-07 Hif Bio, Inc. Anti-angiogenesis compounds
DE102006043443A1 (de) 2006-09-15 2008-03-27 Bayer Healthcare Ag Neue aza-bicyclische Verbindungen und ihre Verwendung
WO2008141731A2 (en) 2007-05-18 2008-11-27 Bayer Healthcare Ag Inhibitors of hypoxia inducible factor (hif) useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
JP2010111624A (ja) * 2008-11-06 2010-05-20 Shionogi & Co Ltd Ｔｔｋ阻害作用を有するインダゾール誘導体
EP2373626B1 (en) 2008-12-18 2016-08-24 Nerviano Medical Sciences S.r.l. Substituted indazole derivatives active as kinase inhibitors
EP2491033A4 (en) 2009-10-20 2013-03-13 Eiger Biopharmaceuticals Inc AZAINDAZOLES FOR THE TREATMENT OF FLAVIVIRIDAE VIRUS INFECTION
RS59908B1 (sr) 2009-11-27 2020-03-31 Adverio Pharma Gmbh Postupak za proizvodnju metil-{4,6-diamino-2-[1-(2-fluorobenzil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}metilkarbamata
WO2011115804A1 (en) 2010-03-17 2011-09-22 Ironwood Pharmaceuticals, Inc. Sgc stimulators
SG10201502484SA (en) 2010-03-30 2015-05-28 Verseon Corp Multisubstituted aromatic compounds as inhibitors of thrombin
JP5860459B2 (ja) 2010-06-30 2016-02-16 アイアンウッド ファーマシューティカルズ インコーポレイテッド ｓＧＣ刺激薬
UA111754C2 (uk) 2011-10-06 2016-06-10 Байєр Фарма Акцієнгезелльшафт Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань
JP6141866B2 (ja) 2011-12-21 2017-06-07 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 置換ベンジルピラゾール類
US9139564B2 (en) 2011-12-27 2015-09-22 Ironwood Pharmaceuticals, Inc. 2-benzyl, 3-(pyrimidin-2-yl) substituted pyrazoles useful as sGC stimulators
HK1207861A1 (en) 2012-05-11 2016-02-12 Bayer Pharma Aktiengesellschaft Substituted cycloalkenopyrazoles as bub1 inhibitors for the treatment of cancer
WO2014047111A1 (en) 2012-09-18 2014-03-27 Ironwood Pharmaceuticals, Inc. Sgc stimulators
EP2897953B8 (en) 2012-09-19 2019-06-26 Cyclerion Therapeutics, Inc. Sgc stimulators
US9738610B2 (en) 2012-09-24 2017-08-22 Whitehead Institute For Biomedical Research Indazole derivatives and uses thereof
CA2907730A1 (en) 2013-03-21 2014-09-25 Bayer Pharma Aktiengesellschaft Diaminoheteroaryl substituted indazoles
WO2014147204A1 (en) 2013-03-21 2014-09-25 Bayer Pharma Aktiengesellschaft Heteroaryl substituted indazoles
EP2976336A1 (en) 2013-03-21 2016-01-27 Bayer Pharma Aktiengesellschaft 3-heteroaryl substituted indazoles
EP3010911A1 (en) 2013-06-21 2016-04-27 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
JP2016522231A (ja) 2013-06-21 2016-07-28 バイエル ファーマ アクチエンゲゼルシャフト ジアミノヘテロアリール置換ピラゾール類
EP3010902A1 (en) 2013-06-21 2016-04-27 Bayer Pharma Aktiengesellschaft Substituted benzylpyrazoles
EP3010901B1 (en) 2013-06-21 2017-09-13 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
JP2016525076A (ja) 2013-06-21 2016-08-22 バイエル ファーマ アクチエンゲゼルシャフト 置換されたベンジルピラゾール類
WO2015063003A1 (en) 2013-10-30 2015-05-07 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
US10350206B2 (en) 2014-09-19 2019-07-16 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles as BUB1 inhibitors
WO2016041925A1 (en) 2014-09-19 2016-03-24 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles
CA2961578A1 (en) 2014-09-19 2016-03-24 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles as bub1 kinase inhibitors
CN107074825A (zh) 2014-09-19 2017-08-18 拜耳制药股份公司 作为bub1激酶抑制剂的苄基取代的吲唑类化合物
WO2017148995A1 (en) 2016-03-04 2017-09-08 Bayer Pharma Aktiengesellschaft 1-(pyrimidin-2-yl)-1h-indazoles having bub1 kinase inhibiting activity
WO2017157991A1 (en) 2016-03-18 2017-09-21 Bayer Pharma Aktiengesellschaft 1-alkyl-pyrazoles and -indazoles as bub1 inhibitors for the treatment of hyperproliferative diseases
WO2017157992A1 (en) 2016-03-18 2017-09-21 Bayer Pharma Aktiengesellschaft Annulated pyrazoles as bub1 kinase inhibitors for treating proliferative disorders
WO2018122168A1 (en) 2016-12-29 2018-07-05 Bayer Pharma Aktiengesellschaft Combinations of bub1 kinase and parp inhibitors
WO2018158175A1 (en) 2017-02-28 2018-09-07 Bayer Pharma Aktiengesellschaft Combination of bub1 inhibitors
WO2018206547A1 (en) 2017-05-12 2018-11-15 Bayer Pharma Aktiengesellschaft Combination of bub1 and atr inhibitors
WO2018215282A1 (en) 2017-05-26 2018-11-29 Bayer Pharma Aktiengesellschaft Combination of bub1 and pi3k inhibitors

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