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DK2474545T3 - Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus-kinaseinhibitorer - Google Patents

Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus-kinaseinhibitorer Download PDF

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Publication number
DK2474545T3
DK2474545T3 DK11152714.9T DK11152714T DK2474545T3 DK 2474545 T3 DK2474545 T3 DK 2474545T3 DK 11152714 T DK11152714 T DK 11152714T DK 2474545 T3 DK2474545 T3 DK 2474545T3
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Prior art keywords
pyrrolo
mol
methyl
compound
pyrazol
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DK11152714.9T
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Inventor
James D Rodgers
Stacey Shepard
Thomas P Maduskuie
Haisheng Wang
Nikoo Falahatpisheh
Maria Rafalski
Argyrios G Arvanitis
Louis Storace
Ravi Kumar Jalluri
Jordan S Fridman
Krishna Vaddi
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Incyte Holdings Corp
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Publication of DK2474545T3 publication Critical patent/DK2474545T3/da

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    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
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    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • A—HUMAN NECESSITIES
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    • A61K9/0012—Galenical forms characterised by the site of application
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/04—Antipruritics
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • 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
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  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (20)

1. Forbindelse, som er 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]propannitril, eller et farmaceutisk acceptabelt salt deraf, til anvendelse i behandling afen cancer valgt fra akut lymfoblastisk leukæmi, cancer af hovedet og hals, gastrisk cancer, glioblastom, melanom, Sezary syndrom, og mycosis fungoides hos en patient.
2. Forbindelsen eller salt til anvendelse ifølge krav 1, hvor canceren er akut lymfoblastisk leukæmi.
3. Forbindelsen eller salt til anvendelse ifølge krav 1, hvor canceren er cancer af hovedet og hals.
4. Forbindelsen eller salt til anvendelse ifølge krav 1, hvor canceren er gastrisk cancer.
5. Forbindelsen eller salt til anvendelse ifølge krav 1, hvor canceren er glioblastom.
6. Forbindelsen eller salt til anvendelse ifølge krav 1, hvor canceren er melanom.
7. Forbindelsen eller salt til anvendelse ifølge krav 1, hvor canceren er Sezary syndrom.
8. Forbindelsen eller salt til anvendelse ifølge krav 1, hvor canceren er mycosis fungoides.
9. Forbindelsen ellersalt til anvendelse ifølge krav 1, hvor forbindelsen ellersaltet administreres i kombination med et yderligere farmaceutisk middel.
10. Forbindelsen eller salt til anvendelse ifølge krav 9, hvor det ene yderligere farmaceutiske middel er et kemoterapeutisk middel.
11. Forbindelsen eller salt til anvendelse ifølge krav 10, hvor det kemoterapeutiske middel er revlimid.
12. Forbindelsen eller salt til anvendelse ifølge krav 10, hvor det kemoterapeutiske middel er et DNA-skadende middel.
13. Forbindelsen eller salt til anvendelse ifølge krav 12, hvor det DNA-skadende middel er valgt fra melphalan, doxorubicin, cyclophosphamid, vineristin, etoposid, og carmustin.
14. Forbindelsen eller salt til anvendelse ifølge krav 9, hvor det yderligere farmaceutiske middel er valgt fra melphalan plus prednison, doxorubicin, dexamethason, og bortezomib.
15. Forbindelsen eller salt til anvendelse ifølge krav 9, hvor det yderligere farmaceutiske middel er et corticosteroid.
16. Forbindelsen eller salt til anvendelse ifølge krav 15, hvor corticosteroidet er dexamethason.
17. Forbindelsen eller salt til anvendelse ifølge krav 15, hvor corticosteroidet er prednison.
18. Forbindelsen eller salt til anvendelse ifølge krav 1, hvor ca. 5 til ca. 1000 mg af forbindelsen eller saltet administreres til patienten.
19. Forbindelsen eller salt til anvendelse ifølge krav 9, hvor forbindelsen eller saltet og det yderligere farmaceutiske middel administreres simultant til patienten.
20. Forbindelsen eller salt til anvendelse ifølge krav 9, hvor forbindelsen eller saltet og det yderligere farmaceutiske middel indgives sekventielt til patienten.
DK11152714.9T 2005-12-13 2006-12-12 Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus-kinaseinhibitorer DK2474545T3 (da)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US74990505P 2005-12-13 2005-12-13
US81023106P 2006-06-02 2006-06-02
US85062506P 2006-10-10 2006-10-10
US85687206P 2006-11-03 2006-11-03
US85940406P 2006-11-16 2006-11-16
EP06839328A EP1966202B1 (en) 2005-12-13 2006-12-12 Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors

Publications (1)

Publication Number Publication Date
DK2474545T3 true DK2474545T3 (da) 2017-01-23

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ID=37903501

Family Applications (7)

Application Number Title Priority Date Filing Date
DK11152714.9T DK2474545T3 (da) 2005-12-13 2006-12-12 Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus-kinaseinhibitorer
DK11152723.0T DK2426129T3 (da) 2005-12-13 2006-12-12 Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus kinase-inhibitorer
DK11152708.1T DK2348023T5 (da) 2005-12-13 2006-12-12 Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus-kinase-inhibitorer
DK11152730.5T DK2455382T3 (da) 2005-12-13 2006-12-12 Heteroaryl substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus kinase-inhibitorer
DK06839328.9T DK1966202T3 (da) 2005-12-13 2006-12-12 Heteroarylsubstituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-d]pyrimidiner som Januskinaseinhibitorer
DK16197502.4T DK3184526T3 (da) 2005-12-13 2006-12-12 Pyrrolo[2,3-d]pyrimidinderivativer som janus-kinase-inhibitor
DK11152677.8T DK2343299T3 (da) 2005-12-13 2006-12-12 Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus kinase-inhibitorer

Family Applications After (6)

Application Number Title Priority Date Filing Date
DK11152723.0T DK2426129T3 (da) 2005-12-13 2006-12-12 Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus kinase-inhibitorer
DK11152708.1T DK2348023T5 (da) 2005-12-13 2006-12-12 Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus-kinase-inhibitorer
DK11152730.5T DK2455382T3 (da) 2005-12-13 2006-12-12 Heteroaryl substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus kinase-inhibitorer
DK06839328.9T DK1966202T3 (da) 2005-12-13 2006-12-12 Heteroarylsubstituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-d]pyrimidiner som Januskinaseinhibitorer
DK16197502.4T DK3184526T3 (da) 2005-12-13 2006-12-12 Pyrrolo[2,3-d]pyrimidinderivativer som janus-kinase-inhibitor
DK11152677.8T DK2343299T3 (da) 2005-12-13 2006-12-12 Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus kinase-inhibitorer

Country Status (36)

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US (16) US7598257B2 (da)
EP (10) EP2343298B9 (da)
JP (4) JP5017278B2 (da)
KR (4) KR101391900B1 (da)
CN (4) CN103214484B (da)
AR (1) AR057995A1 (da)
AT (1) ATE525374T1 (da)
AU (1) AU2006326548B2 (da)
BR (1) BRPI0619817B8 (da)
CA (1) CA2632466C (da)
CR (2) CR10065A (da)
CY (8) CY1112762T1 (da)
DK (7) DK2474545T3 (da)
EA (3) EA035795B1 (da)
EC (2) ECSP088540A (da)
ES (10) ES2867505T3 (da)
FR (2) FR13C0007I2 (da)
HK (5) HK1124840A1 (da)
HR (7) HRP20110903T1 (da)
HU (7) HUE030235T2 (da)
IL (3) IL192019A (da)
LT (5) LT2426129T (da)
LU (1) LU92137I2 (da)
ME (1) ME01312B (da)
MX (1) MX346183B (da)
MY (2) MY159449A (da)
NZ (2) NZ778831A (da)
PL (7) PL2474545T3 (da)
PT (7) PT2426129T (da)
RS (7) RS55634B1 (da)
SG (3) SG10202003901UA (da)
SI (7) SI2426129T1 (da)
TW (6) TWI664182B (da)
UA (2) UA98449C2 (da)
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ZA (1) ZA200805165B (da)

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WO2009114552A1 (en) * 2008-03-10 2009-09-17 The Board Of Trustees Of The Leland Stanford Junior University Heteroaryl compounds, compositions, and methods of use in cancer treatment
KR20120108042A (ko) * 2008-03-11 2012-10-04 인사이트 코포레이션 Ｊａｋ 억제제로서의 아제티딘 및 시클로부탄 유도체
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