AR089641A1 - COMPUESTOS BICICLICOS Y SUS USOS COMO INHIBIDORES DUALES DE c-SRC/JAK - Google Patents
COMPUESTOS BICICLICOS Y SUS USOS COMO INHIBIDORES DUALES DE c-SRC/JAKInfo
- Publication number
- AR089641A1 AR089641A1 ARP110100492A ARP110100492A AR089641A1 AR 089641 A1 AR089641 A1 AR 089641A1 AR P110100492 A ARP110100492 A AR P110100492A AR P110100492 A ARP110100492 A AR P110100492A AR 089641 A1 AR089641 A1 AR 089641A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- heteroaryl
- inhibitors
- aryl
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuestos bicíclicos aromáticos sustituidos que contienen anillos de pirimidina y piridina así como también sales aceptables para uso farmacéuticos de los mismos. Estos compuestos son útiles como inhibidores de la tirosina quinasa, con preferencia inhibidores de la familia SRC de las quinasas (SKF), en particular como inhibidores de las SFK/JAK quinasas e incluso, con preferencia, como inhibidores duales de las c-SRC/JAK quinasas, inhibiendo así la activación de STAT3 y, por lo tanto, el crecimiento anormal de los tipos celulares particulares. Estos compuestos son útiles para el tratamiento o inhibición de ciertas enfermedades que son el resultado de la desregulación de STAT3. Reivindicación 1: Un compuesto de la fórmula (1) donde R¹ es H, arilo, arilo sustituido, alquilo, alquilo sustituido, heteroarilo, heteroarilo sustituido, heterociclilo, heterociclilo sustituido, heterociclilalquilo o heterociclilalquilo sustituido; X es CH₂ o C=O; R² es H, alquilo C₁₋₆, halógeno, CF₃, u O-alquilo C₁₋₆; Y es -NHCO-, -CONH-, -NHSO₂, -NH-, -NCH₃-CO-, -NHCH₂-, O, -NHCONH- o -NHCOCH₂; R³ es alquilo, alquilo sustituido, arilo, o arilo sustituido, heteroarilo, heteroarilo sustituido, cicloalquilo, cicloalquilo sustituido o heterocicloalquilo; o una sal aceptable para uso farmacéutico del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN415CH2010 | 2010-02-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR089641A1 true AR089641A1 (es) | 2014-09-10 |
Family
ID=43903941
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110100492A AR089641A1 (es) | 2010-02-17 | 2011-02-17 | COMPUESTOS BICICLICOS Y SUS USOS COMO INHIBIDORES DUALES DE c-SRC/JAK |
Country Status (28)
Country | Link |
---|---|
US (2) | US8440679B2 (es) |
EP (1) | EP2536722B1 (es) |
JP (1) | JP2013519725A (es) |
KR (1) | KR20120130294A (es) |
CN (1) | CN102858770A (es) |
AR (1) | AR089641A1 (es) |
AU (1) | AU2011216895B2 (es) |
BR (1) | BR112012020639A2 (es) |
CA (1) | CA2789655A1 (es) |
CU (1) | CU20120118A7 (es) |
CY (1) | CY1115420T1 (es) |
DK (1) | DK2536722T3 (es) |
EA (1) | EA201290757A1 (es) |
ES (1) | ES2470190T3 (es) |
HK (1) | HK1178897A1 (es) |
HR (1) | HRP20140437T1 (es) |
IL (1) | IL221487A (es) |
MX (1) | MX2012009482A (es) |
NZ (1) | NZ602271A (es) |
PL (1) | PL2536722T3 (es) |
PT (1) | PT2536722E (es) |
RS (1) | RS53458B (es) |
SA (1) | SA111320200B1 (es) |
SG (1) | SG183329A1 (es) |
SI (1) | SI2536722T1 (es) |
SM (1) | SMT201400090B (es) |
TW (1) | TW201130838A (es) |
WO (1) | WO2011101806A1 (es) |
Families Citing this family (65)
Publication number | Priority date | Publication date | Assignee | Title |
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MY162590A (en) | 2005-12-13 | 2017-06-30 | Incyte Holdings Corp | Heteroaryl substituted pyrrolo[2,3-b] pyridines and pyrrolo[2,3-b] pyrimidines as janus kinase inhibitors |
EP3495369B1 (en) | 2007-06-13 | 2021-10-27 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
MX2011012262A (es) | 2009-05-22 | 2012-01-25 | Incyte Corp | 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il] octano-o heptano-nitrilo como inhibidores de cinasas janus (jak). |
SA111320200B1 (ar) | 2010-02-17 | 2014-02-16 | ديبيوفارم اس ايه | مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة |
SI3354652T1 (sl) | 2010-03-10 | 2020-08-31 | Incyte Holdings Corporation | Derivati piperidin-4-il azetidina kot inhibitorji JAK1 |
SG10201910912TA (en) | 2010-05-21 | 2020-01-30 | Incyte Corp | Topical Formulation for a JAK Inhibitor |
UA112517C2 (uk) | 2010-07-06 | 2016-09-26 | Новартіс Аг | Тетрагідропіридопіримідинові похідні |
BR112013012502A2 (pt) | 2010-11-19 | 2019-03-06 | Incyte Corporation | pirrolopiridina ciclobutil substituída e derivados de pirrolopirimidina derivativos como inibidores de jak |
WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
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 |
WO2013138393A1 (en) * | 2012-03-12 | 2013-09-19 | Allergan, Inc. | Method of treating ophthalmic conditions with kinase inhibitors |
PT3176170T (pt) | 2012-06-13 | 2019-02-05 | Incyte Holdings Corp | Compostos tricíclicos substituídos como inibidores de fgfr |
US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
SG11201503695XA (en) | 2012-11-15 | 2015-06-29 | Incyte Corp | Sustained-release dosage forms of ruxolitinib |
US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
US20160123982A1 (en) | 2013-02-04 | 2016-05-05 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for assaying jak2 activity in red blood cells and uses thereof |
EA030705B1 (ru) | 2013-03-06 | 2018-09-28 | Инсайт Холдингс Корпорейшн | Способы и промежуточные соединения при получении ингибитора jak |
PE20152033A1 (es) | 2013-04-19 | 2016-01-21 | Incyte Holdings Corp | Heterociclos bicicliclos como inhibidores de fgfr |
AU2014275643B2 (en) * | 2013-06-05 | 2018-08-09 | C&C Research Laboratories | Heterocyclic derivatives and use thereof |
ES2792549T3 (es) * | 2013-08-07 | 2020-11-11 | Incyte Corp | Formas de dosificación de liberación sostenida para un inhibidor de JAK1 |
US9714258B2 (en) | 2014-01-24 | 2017-07-25 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
AU2015240465B2 (en) | 2014-04-04 | 2020-02-27 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
US9321766B1 (en) | 2014-10-06 | 2016-04-26 | Allergan, Inc. | Kinase inhibitors |
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US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
EP3617205B1 (en) | 2015-02-20 | 2021-08-04 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
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TW201940182A (zh) | 2018-01-22 | 2019-10-16 | 美商安德賽特公司 | Car t 細胞之使用方法 |
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US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
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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 CA CA2789655A patent/CA2789655A1/en not_active Abandoned
- 2011-02-17 NZ NZ602271A patent/NZ602271A/xx not_active IP Right Cessation
- 2011-02-17 AR ARP110100492A patent/AR089641A1/es unknown
- 2011-02-17 US US13/578,656 patent/US8440679B2/en not_active Expired - Fee Related
- 2011-02-17 ES ES11709484.7T patent/ES2470190T3/es active Active
- 2011-02-17 CN CN2011800165418A patent/CN102858770A/zh active Pending
- 2011-02-17 MX MX2012009482A patent/MX2012009482A/es active IP Right Grant
- 2011-02-17 SG SG2012060489A patent/SG183329A1/en unknown
- 2011-02-17 EA EA201290757A patent/EA201290757A1/ru unknown
- 2011-02-17 PL PL11709484T patent/PL2536722T3/pl unknown
- 2011-02-17 PT PT117094847T patent/PT2536722E/pt unknown
- 2011-02-17 DK DK11709484.7T patent/DK2536722T3/da active
- 2011-02-17 KR KR1020127023889A patent/KR20120130294A/ko not_active Application Discontinuation
- 2011-02-17 JP JP2012553436A patent/JP2013519725A/ja not_active Ceased
- 2011-02-17 TW TW100105192A patent/TW201130838A/zh unknown
- 2011-02-17 BR BR112012020639A patent/BR112012020639A2/pt not_active IP Right Cessation
- 2011-02-17 EP EP11709484.7A patent/EP2536722B1/en not_active Not-in-force
- 2011-02-17 AU AU2011216895A patent/AU2011216895B2/en not_active Expired - Fee Related
- 2011-02-17 WO PCT/IB2011/050669 patent/WO2011101806A1/en active Application Filing
- 2011-02-17 SI SI201130155T patent/SI2536722T1/sl unknown
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2012
- 2012-08-15 IL IL221487A patent/IL221487A/en not_active IP Right Cessation
- 2012-08-15 CU CU2012000118A patent/CU20120118A7/es unknown
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2013
- 2013-01-14 US US13/741,019 patent/US8962637B2/en not_active Expired - Fee Related
- 2013-05-16 HK HK13105802.2A patent/HK1178897A1/xx not_active IP Right Cessation
-
2014
- 2014-05-15 HR HRP20140437AT patent/HRP20140437T1/hr unknown
- 2014-06-03 CY CY20141100393T patent/CY1115420T1/el unknown
- 2014-07-10 SM SM201400090T patent/SMT201400090B/xx unknown
Also Published As
Publication number | Publication date |
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CN102858770A (zh) | 2013-01-02 |
EA201290757A1 (ru) | 2013-04-30 |
MX2012009482A (es) | 2012-11-29 |
TW201130838A (en) | 2011-09-16 |
RS53458B (en) | 2014-12-31 |
US20130012518A1 (en) | 2013-01-10 |
CY1115420T1 (el) | 2017-01-04 |
SA111320200B1 (ar) | 2014-02-16 |
CA2789655A1 (en) | 2011-08-25 |
WO2011101806A1 (en) | 2011-08-25 |
SMT201400090B (it) | 2014-09-08 |
US8962637B2 (en) | 2015-02-24 |
AU2011216895B2 (en) | 2015-11-05 |
EP2536722B1 (en) | 2014-04-16 |
SI2536722T1 (sl) | 2014-10-30 |
EP2536722A1 (en) | 2012-12-26 |
SG183329A1 (en) | 2012-09-27 |
PL2536722T3 (pl) | 2014-11-28 |
AU2011216895A1 (en) | 2012-09-27 |
HRP20140437T1 (hr) | 2014-08-29 |
KR20120130294A (ko) | 2012-11-30 |
PT2536722E (pt) | 2014-05-26 |
HK1178897A1 (en) | 2013-09-19 |
US8440679B2 (en) | 2013-05-14 |
US20130143895A1 (en) | 2013-06-06 |
NZ602271A (en) | 2013-09-27 |
IL221487A (en) | 2014-11-30 |
DK2536722T3 (da) | 2014-05-26 |
ES2470190T3 (es) | 2014-06-23 |
JP2013519725A (ja) | 2013-05-30 |
BR112012020639A2 (pt) | 2017-08-08 |
CU20120118A7 (es) | 2012-10-15 |
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