HRP20150530T1 - Spojevi korisni za inhibiranje chk1 - Google Patents

Spojevi korisni za inhibiranje chk1 Download PDF

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Publication number
HRP20150530T1
HRP20150530T1 HRP20150530TT HRP20150530T HRP20150530T1 HR P20150530 T1 HRP20150530 T1 HR P20150530T1 HR P20150530T T HRP20150530T T HR P20150530TT HR P20150530 T HRP20150530 T HR P20150530T HR P20150530 T1 HRP20150530 T1 HR P20150530T1
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HR
Croatia
Prior art keywords
cancer
salt
compound
methylpyridin
pyrazin
Prior art date
Application number
HRP20150530TT
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English (en)
Inventor
Sajan Joseph
Susanta Samajdar
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Eli Lilly And Company
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.)
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Publication date
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Publication of HRP20150530T1 publication Critical patent/HRP20150530T1/hr

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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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/08Acetic acid
    • C07C53/10Salts thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/06Oxalic acid
    • C07C55/07Salts thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/10Succinic acid

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (13)

1. Spoj, naznačen time što je (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amin, ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amin.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je sol (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amina s metansulfonskom kiselinom.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je sol (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amina s octenom kiselinom.
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je hemioksalatna sol (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amina.
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je hemisukcinatna sol (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amina.
7. Farmaceutski pripravak, naznačen time što sadrži spoj ili sol u skladu bilo kojim od patentnih zahtjeva 1-6, kao i farmaceutski prihvatljivu podlogu, razrjeđivač ili pomoćnu tvar.
8. Spoj ili sol u skladu bilo kojim od patentnih zahtjeva 1-6, naznačeni time što su namijenjeni upotrebi u terapiji.
9. Spoj ili sol u skladu bilo kojim od patentnih zahtjeva 1-6, naznačeni time što su namijenjeni upotrebi u liječenju raka.
10. Spoj ili sol u skladu bilo kojim od patentnih zahtjeva 1-6, naznačeni time što su namijenjeni upotrebi u istodobnoj, odvojenoj ili uzastopnoj kombinaciji s ionizirajućim zračenjem u liječenju raka.
11. Spoj ili sol u skladu bilo kojim od patentnih zahtjeva 1-6, naznačeni time što su namijenjeni upotrebi u istodobnoj, odvojenoj ili uzastopnoj kombinaciji s jednim ili više kemoterapijskih sredstava u liječenju raka.
12. Spoj ili sol namijenjeni upotrebi u skladu s patentnim zahtjevom 11, naznačeni time što se jedno ili više kemoterapijskih sredstava bira iz skupine koju čine 5-fluoruracil, hidroksiurea, gemcitabin, metotreksat, pemetreksed, doksorubicin, etopozid, cisplatin i taksol.
13. Spoj ili sol namijenjeni upotrebi u skladu bilo kojim od patentnih zahtjeva 9-12, naznačeni time što se rak bira iz skupine koju čine rak mokraćnog mjehura, rak debelog crijeva, rak želuca, rak jetre, rak pluća, rak dojke, melanom, rak jajnika, rak gušterače, mezoteliom, rak bubrega i rak maternice.
HRP20150530TT 2010-11-08 2015-05-18 Spojevi korisni za inhibiranje chk1 HRP20150530T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41113710P 2010-11-08 2010-11-08
EP11788263.9A EP2638033B1 (en) 2010-11-08 2011-11-01 Compounds useful for inhibiting chk1
PCT/US2011/058692 WO2012064548A1 (en) 2010-11-08 2011-11-01 Compounds useful for inhibiting chk1

Publications (1)

Publication Number Publication Date
HRP20150530T1 true HRP20150530T1 (hr) 2015-06-19

Family

ID=45044707

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20150530TT HRP20150530T1 (hr) 2010-11-08 2015-05-18 Spojevi korisni za inhibiranje chk1

Country Status (22)

Country Link
US (1) US9067920B2 (hr)
EP (1) EP2638033B1 (hr)
JP (1) JP5792316B2 (hr)
KR (1) KR101533166B1 (hr)
CN (1) CN103180311B (hr)
AR (1) AR083575A1 (hr)
AU (1) AU2011326230B2 (hr)
BR (1) BR112013010009B1 (hr)
CA (1) CA2816944C (hr)
DK (1) DK2638033T3 (hr)
EA (1) EA022096B1 (hr)
ES (1) ES2541414T3 (hr)
HR (1) HRP20150530T1 (hr)
JO (1) JO3145B1 (hr)
ME (1) ME02119B (hr)
MX (1) MX2013005181A (hr)
PL (1) PL2638033T3 (hr)
PT (1) PT2638033E (hr)
RS (1) RS54012B1 (hr)
SI (1) SI2638033T1 (hr)
TW (1) TWI501956B (hr)
WO (1) WO2012064548A1 (hr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201402277D0 (en) 2014-02-10 2014-03-26 Sentinel Oncology Ltd Pharmaceutical compounds
ES2906785T3 (es) 2016-02-04 2022-04-20 Pharmaengine Inc Pirazoles 3,5-disustituidos útiles como inhibidores de la quinasa de punto de control 1 (CHK1), y sus preparaciones y aplicaciones
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
US11564920B2 (en) 2020-11-30 2023-01-31 Sumitomo Pharma Co., Ltd. 5-heteroaryl-1H-pyrazol-3-amine derivative
AU2021389190A1 (en) 2020-11-30 2023-06-29 Sumitomo Pharma Co., Ltd. 5-heteroaryl-1h-pyrazol-3-amine derivative
TW202333680A (zh) * 2021-12-24 2023-09-01 日商住友製藥股份有限公司 具有二環性骨架之1h-吡唑-3-胺衍生物
WO2023229032A1 (ja) * 2022-05-27 2023-11-30 住友ファーマ株式会社 免疫チェックポイント阻害剤に対して治療抵抗性を示すがんの治療薬

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA06000933A (es) * 2003-07-25 2006-03-30 Pfizer Compuestos de aminopirazol y uso como inhibidores de chk1.
CN100584840C (zh) * 2004-01-05 2010-01-27 阿斯利康(瑞典)有限公司 取代杂环化合物及其应用
WO2005121121A2 (en) * 2004-06-04 2005-12-22 Arena Pharmaceuticals, Inc. Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
CN101218229A (zh) * 2005-05-05 2008-07-09 阿斯利康(瑞典)有限公司 吡唑基-氨基取代的嘧啶及其在癌症治疗中的应用
US20090233896A1 (en) * 2005-06-09 2009-09-17 Arrington Kenneth L Inhibitors of checkpoint kinases
WO2008117050A1 (en) * 2007-03-27 2008-10-02 Astrazeneca Ab Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer
PA8850801A1 (es) * 2008-12-17 2010-07-27 Lilly Co Eli Compuestos útiles para inhibir chk1

Also Published As

Publication number Publication date
BR112013010009B1 (pt) 2021-10-19
JP5792316B2 (ja) 2015-10-07
MX2013005181A (es) 2013-10-17
AR083575A1 (es) 2013-03-06
CA2816944C (en) 2015-12-22
WO2012064548A1 (en) 2012-05-18
BR112013010009A2 (pt) 2020-09-29
KR20130099146A (ko) 2013-09-05
PT2638033E (pt) 2015-06-01
CA2816944A1 (en) 2012-05-18
EP2638033B1 (en) 2015-04-08
US9067920B2 (en) 2015-06-30
TWI501956B (zh) 2015-10-01
EA022096B1 (ru) 2015-10-30
EP2638033A1 (en) 2013-09-18
AU2011326230A1 (en) 2013-05-09
US20130190262A1 (en) 2013-07-25
ES2541414T3 (es) 2015-07-20
EA201390499A1 (ru) 2013-08-30
JO3145B1 (ar) 2017-09-20
ME02119B (me) 2015-10-20
CN103180311A (zh) 2013-06-26
JP2013541586A (ja) 2013-11-14
RS54012B1 (en) 2015-10-30
KR101533166B1 (ko) 2015-07-01
CN103180311B (zh) 2014-08-20
SI2638033T1 (sl) 2015-05-29
AU2011326230B2 (en) 2015-02-19
PL2638033T3 (pl) 2015-09-30
TW201305138A (zh) 2013-02-01
DK2638033T3 (en) 2015-04-27

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