CY1115420T1 - Δικυκλικες ενωσεις και οι χρησεις τους ως διπλοι αναστολεις c-src/jak - Google Patents
Δικυκλικες ενωσεις και οι χρησεις τους ως διπλοι αναστολεις c-src/jakInfo
- Publication number
- CY1115420T1 CY1115420T1 CY20141100393T CY141100393T CY1115420T1 CY 1115420 T1 CY1115420 T1 CY 1115420T1 CY 20141100393 T CY20141100393 T CY 20141100393T CY 141100393 T CY141100393 T CY 141100393T CY 1115420 T1 CY1115420 T1 CY 1115420T1
- Authority
- CY
- Cyprus
- Prior art keywords
- jak
- src
- compounds
- present
- kinase inhibitors
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—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
- 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
- C07D471/04—Ortho-condensed systems
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Transplantation (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Η παρούσα εφεύρεση αναφέρεται σε υποκατασταθείσες αρωματικές δικυκλικές ενώσεις περιέχουσες δακτυλίους πυριμιδίνης και πυριδίνης έχουσες τη δομή τύπου (I) καθώς επίσης και σε φαρμακευτικά αποδεκτά άλατα αυτών. Οι ενώσεις της παρούσας εφευρέσεως είναι χρήσιμες ως αναστολείς κινάσης της τυροσίνης, κατά προτίμηση αναστολείς των κινασών της οικογένειας SRC (SFK), συγκεκριμένα ως πολλαπλοί αναστολείς κινασών SFK/JAK και ακόμη προτιμότερα ως διπλοί αναστολείς κινασών c-SRC/JAK, αναστέλλοντας τοιουτοτρόπως την ενεργοποίηση του STAT3 και κατά συνέπεια την αφύσικη ανάπτυξη συγκεκριμένων κυτταρικών τύπων. Αξιοσημείωτα, οι ενώσεις της παρούσας εφευρέσεως είναι χρήσιμες για την αγωγή ή αναστολή ορισμένων νόσων που είναι το αποτέλεσμα της απορυθμίσεως του STAT3.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN415CH2010 | 2010-02-17 | ||
EP11709484.7A EP2536722B1 (en) | 2010-02-17 | 2011-02-17 | Bicyclic compounds and their uses as dual c-src / jak inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
CY1115420T1 true CY1115420T1 (el) | 2017-01-04 |
Family
ID=43903941
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CY20141100393T CY1115420T1 (el) | 2010-02-17 | 2014-06-03 | Δικυκλικες ενωσεις και οι χρησεις τους ως διπλοι αναστολεις c-src/jak |
Country Status (28)
Country | Link |
---|---|
US (2) | US8440679B2 (el) |
EP (1) | EP2536722B1 (el) |
JP (1) | JP2013519725A (el) |
KR (1) | KR20120130294A (el) |
CN (1) | CN102858770A (el) |
AR (1) | AR089641A1 (el) |
AU (1) | AU2011216895B2 (el) |
BR (1) | BR112012020639A2 (el) |
CA (1) | CA2789655A1 (el) |
CU (1) | CU20120118A7 (el) |
CY (1) | CY1115420T1 (el) |
DK (1) | DK2536722T3 (el) |
EA (1) | EA201290757A1 (el) |
ES (1) | ES2470190T3 (el) |
HK (1) | HK1178897A1 (el) |
HR (1) | HRP20140437T1 (el) |
IL (1) | IL221487A (el) |
MX (1) | MX2012009482A (el) |
NZ (1) | NZ602271A (el) |
PL (1) | PL2536722T3 (el) |
PT (1) | PT2536722E (el) |
RS (1) | RS53458B (el) |
SA (1) | SA111320200B1 (el) |
SG (1) | SG183329A1 (el) |
SI (1) | SI2536722T1 (el) |
SM (1) | SMT201400090B (el) |
TW (1) | TW201130838A (el) |
WO (1) | WO2011101806A1 (el) |
Families Citing this family (66)
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CN103214483B (zh) | 2005-12-13 | 2014-12-17 | 因塞特公司 | 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶 |
EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
DK2432472T3 (da) | 2009-05-22 | 2019-11-18 | Incyte Holdings Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- eller heptan-nitril som jak-inhibitorer |
SA111320200B1 (ar) | 2010-02-17 | 2014-02-16 | ديبيوفارم اس ايه | مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة |
KR102283091B1 (ko) | 2010-03-10 | 2021-07-30 | 인사이트 홀딩스 코포레이션 | Jak1 저해제로서의 피페리딘4일 아제티딘 유도체 |
EP2574168B9 (en) | 2010-05-21 | 2016-10-05 | Incyte Holdings Corporation | Topical formulation for a jak inhibitor |
UA112517C2 (uk) | 2010-07-06 | 2016-09-26 | Новартіс Аг | Тетрагідропіридопіримідинові похідні |
AR083933A1 (es) | 2010-11-19 | 2013-04-10 | Incyte Corp | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
CN103797010B (zh) | 2011-06-20 | 2016-02-24 | 因塞特控股公司 | 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物 |
UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
US8889870B2 (en) | 2012-03-12 | 2014-11-18 | Allergan, Inc. | Kinase inhibitors |
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EP2951590A1 (en) | 2013-02-04 | 2015-12-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for assaying jak2 activity in red blood cells and uses thereof |
RS62867B1 (sr) | 2013-03-06 | 2022-02-28 | Incyte Holdings Corp | Postupci i intermedijeri za dobijanje inhibitora jak |
EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
AU2014275643B2 (en) * | 2013-06-05 | 2018-08-09 | C&C Research Laboratories | Heterocyclic derivatives and use thereof |
EP3030227B1 (en) | 2013-08-07 | 2020-04-08 | Incyte Corporation | Sustained release dosage forms for a jak1 inhibitor |
PT3636649T (pt) | 2014-01-24 | 2024-04-09 | Turning Point Therapeutics Inc | Diaril macrociclos como moduladores das proteínas quinases |
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2011
- 2011-02-16 SA SA111320200A patent/SA111320200B1/ar unknown
- 2011-02-17 RS RS20140277A patent/RS53458B/en unknown
- 2011-02-17 AR ARP110100492A patent/AR089641A1/es unknown
- 2011-02-17 EP EP11709484.7A patent/EP2536722B1/en not_active Not-in-force
- 2011-02-17 CA CA2789655A patent/CA2789655A1/en not_active Abandoned
- 2011-02-17 EA EA201290757A patent/EA201290757A1/ru unknown
- 2011-02-17 BR BR112012020639A patent/BR112012020639A2/pt not_active IP Right Cessation
- 2011-02-17 MX MX2012009482A patent/MX2012009482A/es active IP Right Grant
- 2011-02-17 TW TW100105192A patent/TW201130838A/zh unknown
- 2011-02-17 ES ES11709484.7T patent/ES2470190T3/es active Active
- 2011-02-17 SI SI201130155T patent/SI2536722T1/sl unknown
- 2011-02-17 NZ NZ602271A patent/NZ602271A/xx not_active IP Right Cessation
- 2011-02-17 PL PL11709484T patent/PL2536722T3/pl unknown
- 2011-02-17 PT PT117094847T patent/PT2536722E/pt unknown
- 2011-02-17 WO PCT/IB2011/050669 patent/WO2011101806A1/en active Application Filing
- 2011-02-17 JP JP2012553436A patent/JP2013519725A/ja not_active Ceased
- 2011-02-17 CN CN2011800165418A patent/CN102858770A/zh active Pending
- 2011-02-17 SG SG2012060489A patent/SG183329A1/en unknown
- 2011-02-17 KR KR1020127023889A patent/KR20120130294A/ko not_active Application Discontinuation
- 2011-02-17 US US13/578,656 patent/US8440679B2/en not_active Expired - Fee Related
- 2011-02-17 AU AU2011216895A patent/AU2011216895B2/en not_active Expired - Fee Related
- 2011-02-17 DK DK11709484.7T patent/DK2536722T3/da active
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2012
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2013
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2014
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- 2014-06-03 CY CY20141100393T patent/CY1115420T1/el unknown
- 2014-07-10 SM SM201400090T patent/SMT201400090B/xx unknown
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PT2536722E (pt) | 2014-05-26 |
WO2011101806A1 (en) | 2011-08-25 |
US8440679B2 (en) | 2013-05-14 |
US8962637B2 (en) | 2015-02-24 |
JP2013519725A (ja) | 2013-05-30 |
US20130143895A1 (en) | 2013-06-06 |
DK2536722T3 (da) | 2014-05-26 |
RS53458B (en) | 2014-12-31 |
IL221487A (en) | 2014-11-30 |
NZ602271A (en) | 2013-09-27 |
AU2011216895A1 (en) | 2012-09-27 |
SMT201400090B (it) | 2014-09-08 |
ES2470190T3 (es) | 2014-06-23 |
AU2011216895B2 (en) | 2015-11-05 |
EA201290757A1 (ru) | 2013-04-30 |
SI2536722T1 (sl) | 2014-10-30 |
CA2789655A1 (en) | 2011-08-25 |
MX2012009482A (es) | 2012-11-29 |
SG183329A1 (en) | 2012-09-27 |
HRP20140437T1 (hr) | 2014-08-29 |
KR20120130294A (ko) | 2012-11-30 |
BR112012020639A2 (pt) | 2017-08-08 |
CU20120118A7 (es) | 2012-10-15 |
PL2536722T3 (pl) | 2014-11-28 |
US20130012518A1 (en) | 2013-01-10 |
EP2536722A1 (en) | 2012-12-26 |
SA111320200B1 (ar) | 2014-02-16 |
AR089641A1 (es) | 2014-09-10 |
CN102858770A (zh) | 2013-01-02 |
TW201130838A (en) | 2011-09-16 |
EP2536722B1 (en) | 2014-04-16 |
HK1178897A1 (en) | 2013-09-19 |
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