JP2011515397A5 - - Google Patents
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- Publication number
- JP2011515397A5 JP2011515397A5 JP2011500801A JP2011500801A JP2011515397A5 JP 2011515397 A5 JP2011515397 A5 JP 2011515397A5 JP 2011500801 A JP2011500801 A JP 2011500801A JP 2011500801 A JP2011500801 A JP 2011500801A JP 2011515397 A5 JP2011515397 A5 JP 2011515397A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- lower alkyl
- hydrogen
- optionally substituted
- alkyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- -1 heterocyclyloxyalkyl Chemical group 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 5
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000004404 heteroalkyl group Chemical group 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000000467 secondary amino group Chemical group [H]N([*:1])[*:2] 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000001302 tertiary amino group Chemical group 0.000 claims 2
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 208000010962 ALK-positive anaplastic large cell lymphoma Diseases 0.000 claims 1
- 208000028564 B-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000003803 Inflammatory myofibroblastic tumor Diseases 0.000 claims 1
- 206010067917 Inflammatory myofibroblastic tumour Diseases 0.000 claims 1
- SOWBFZRMHSNYGE-UHFFFAOYSA-N Monoamide-Oxalic acid Natural products NC(=O)C(O)=O SOWBFZRMHSNYGE-UHFFFAOYSA-N 0.000 claims 1
- ZWIJMWCYBYYPLU-UHFFFAOYSA-N NNC(=O)C(N)=N Chemical compound NNC(=O)C(N)=N ZWIJMWCYBYYPLU-UHFFFAOYSA-N 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000005124 aminocycloalkyl group Chemical group 0.000 claims 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 1
- 150000001540 azides Chemical class 0.000 claims 1
- 125000005335 azido alkyl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000004966 cyanoalkyl group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 0 C[C@@](C*)NC(C=CNC1O)=C1c1nc(C(*)C(C(CN2*)=C3*)C2=O)c3[n]1 Chemical compound C[C@@](C*)NC(C=CNC1O)=C1c1nc(C(*)C(C(CN2*)=C3*)C2=O)c3[n]1 0.000 description 3
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3803208P | 2008-03-19 | 2008-03-19 | |
| US61/038,032 | 2008-03-19 | ||
| PCT/US2009/001691 WO2009117097A1 (en) | 2008-03-19 | 2009-03-18 | Novel tyrosine kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013006922A Division JP2013082744A (ja) | 2008-03-19 | 2013-01-18 | 新規チロシンキナーゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011515397A JP2011515397A (ja) | 2011-05-19 |
| JP2011515397A5 true JP2011515397A5 (https=) | 2012-05-10 |
| JP5628145B2 JP5628145B2 (ja) | 2014-11-19 |
Family
ID=40814009
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011500801A Expired - Fee Related JP5628145B2 (ja) | 2008-03-19 | 2009-03-18 | 新規チロシンキナーゼ阻害剤 |
| JP2013006922A Pending JP2013082744A (ja) | 2008-03-19 | 2013-01-18 | 新規チロシンキナーゼ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013006922A Pending JP2013082744A (ja) | 2008-03-19 | 2013-01-18 | 新規チロシンキナーゼ阻害剤 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8815906B2 (https=) |
| EP (2) | EP2966076A1 (https=) |
| JP (2) | JP5628145B2 (https=) |
| CN (1) | CN102036990B (https=) |
| AU (1) | AU2009226153B2 (https=) |
| CA (1) | CA2718872C (https=) |
| DK (1) | DK2262807T3 (https=) |
| MX (1) | MX2010010272A (https=) |
| WO (1) | WO2009117097A1 (https=) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2010010272A (es) * | 2008-03-19 | 2011-05-25 | Chembridge Corp | Nuevos inhibidores de tirosina quinasa. |
| US9249147B2 (en) * | 2008-03-19 | 2016-02-02 | Chembridge Corporation | Tyrosine kinase inhibitors |
| WO2011049625A1 (en) | 2009-10-20 | 2011-04-28 | Mansour Samadpour | Method for aflatoxin screening of products |
| NZ599830A (en) | 2009-11-05 | 2014-08-29 | Rhizen Pharmaceuticals Sa | Novel kinase modulators |
| ME03376B (me) | 2010-05-20 | 2020-01-20 | Array Biopharma Inc | Makrociklička jedinjenja kао inhibiтori trk kinaze |
| WO2012037155A2 (en) | 2010-09-13 | 2012-03-22 | Gtx, Inc. | Tyrosine kinase inhibitors |
| PH12013502240B1 (en) | 2011-05-04 | 2018-06-27 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of protein kinase |
| EP2779833A4 (en) * | 2011-11-14 | 2015-03-18 | Tesaro Inc | MODULATION OF SPECIFIC TYROSINE KINASES |
| CA2871237A1 (en) | 2012-04-24 | 2013-10-31 | Chugai Seiyaku Kabushiki Kaisha | Benzamide derivative |
| AR090835A1 (es) | 2012-04-24 | 2014-12-10 | Chugai Pharmaceutical Co Ltd | Derivados de quinazolindiona |
| RS56494B1 (sr) | 2012-07-04 | 2018-01-31 | Rhizen Pharmaceuticals S A | Selektivni inhibitori pi3k delta |
| MX2015011428A (es) | 2013-03-06 | 2016-02-03 | Genentech Inc | Metodos para tratar y prevenir la resistencia a los farmacos para el cancer. |
| CN104109168B (zh) * | 2013-04-20 | 2017-02-15 | 山东轩竹医药科技有限公司 | 四并环激酶抑制剂 |
| WO2015054465A1 (en) | 2013-10-11 | 2015-04-16 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| US10005739B2 (en) | 2013-10-23 | 2018-06-26 | Chugai Seiyaku Kabushiki Kaisha | Quinazolinone and isoquinolinone derivative |
| US11045468B2 (en) * | 2014-02-04 | 2021-06-29 | Astellas Pharma Inc. | Pharmaceutical composition comprising diamino heterocyclic carboxamide compound as active ingredient |
| EP3131903A4 (en) * | 2014-04-17 | 2018-05-02 | Amgen Inc. | Polymorphic forms and co-crystals of a c-met inhibitor |
| CN107073121A (zh) | 2014-06-13 | 2017-08-18 | 基因泰克公司 | 治疗及预防癌症药物抗性的方法 |
| US20180044350A1 (en) * | 2015-03-10 | 2018-02-15 | Pottayil Govindan Nair Sasikumar | Therapeutic cyclic compounds as immunomodulators |
| US10087191B2 (en) | 2015-06-16 | 2018-10-02 | Jiangsu Hengrui Medicine Co., Ltd. | Piperidine derivative and preparation method and pharmaceutical use thereof |
| BR112018000808A2 (pt) | 2015-07-16 | 2018-09-04 | Array Biopharma Inc | compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase |
| MA43416A (fr) | 2015-12-11 | 2018-10-17 | Regeneron Pharma | Méthodes pour ralentir ou empêcher la croissance de tumeurs résistantes au blocage de l'egfr et/ou d'erbb3 |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| WO2018136661A1 (en) | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| US10513515B2 (en) | 2017-08-25 | 2019-12-24 | Biotheryx, Inc. | Ether compounds and uses thereof |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| JP7060694B2 (ja) | 2018-01-18 | 2022-04-26 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピロロ［２，３－ｄ］ピリミジン化合物 |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
| CA3106239A1 (en) | 2018-07-27 | 2020-01-30 | Biotheryx, Inc. | Bifunctional compounds as cdk modulators |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| EA202192575A1 (ru) | 2019-03-21 | 2022-01-14 | Онксео | Соединения dbait в сочетании с ингибиторами киназ для лечения рака |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| WO2021222150A2 (en) | 2020-04-28 | 2021-11-04 | Anwita Biosciences, Inc. | Interleukin-2 polypeptides and fusion proteins thereof, and their pharmaceutical compositions and therapeutic applications |
| TW202216676A (zh) | 2020-07-06 | 2022-05-01 | 美商塔朵根公司 | 用於心理疾病或心理強化的有益苯并噻吩組合物 |
| CN116209657A (zh) | 2020-08-06 | 2023-06-02 | 泰科根公司 | 用于精神障碍或增强的2-氨基茚满化合物 |
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| US3536809A (en) | 1969-02-17 | 1970-10-27 | Alza Corp | Medication method |
| US3598123A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US3916899A (en) | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
| US4008719A (en) | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
| IE58110B1 (en) | 1984-10-30 | 1993-07-14 | Elan Corp Plc | Controlled release powder and process for its preparation |
| US5073543A (en) | 1988-07-21 | 1991-12-17 | G. D. Searle & Co. | Controlled release formulations of trophic factors in ganglioside-lipsome vehicle |
| IT1229203B (it) | 1989-03-22 | 1991-07-25 | Bioresearch Spa | Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative. |
| US5120548A (en) | 1989-11-07 | 1992-06-09 | Merck & Co., Inc. | Swelling modulated polymeric drug delivery device |
| US5733566A (en) | 1990-05-15 | 1998-03-31 | Alkermes Controlled Therapeutics Inc. Ii | Controlled release of antiparasitic agents in animals |
| US5580578A (en) | 1992-01-27 | 1996-12-03 | Euro-Celtique, S.A. | Controlled release formulations coated with aqueous dispersions of acrylic polymers |
| EP0600830A1 (de) * | 1992-11-27 | 1994-06-08 | Ciba-Geigy Ag | Substituierte Derivate von Diaminophthalimid als Protein-Tyrosin-Kinase-Hemmer |
| US5591767A (en) | 1993-01-25 | 1997-01-07 | Pharmetrix Corporation | Liquid reservoir transdermal patch for the administration of ketorolac |
| IT1270594B (it) | 1994-07-07 | 1997-05-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida |
| US7189716B2 (en) | 2003-01-03 | 2007-03-13 | Bristol-Myers Squibb Company | Tyrosine kinase inhibitors |
| AU2004234087A1 (en) | 2003-04-28 | 2004-11-11 | Tibotec Pharmaceuticals Ltd. | HIV integrase inhibitors |
| EP1648455A4 (en) | 2003-07-23 | 2009-03-04 | Exelixis Inc | MODULATORS OF ALK PROTEIN (ANAPLASTIC LYMPHOMA KINASE) AND METHODS OF USE |
| DE602006002887D1 (de) * | 2005-04-14 | 2008-11-06 | Hoffmann La Roche | Tricyclische azolderivate, ihre herstellung und ihre verwendung als pharmazeutische mittel |
| CN101208093A (zh) * | 2005-04-27 | 2008-06-25 | 阿斯利康(瑞典)有限公司 | 吡唑-嘧啶衍生物在治疗疼痛中的用途 |
| US20080062003A1 (en) * | 2006-08-07 | 2008-03-13 | Christian Paetz | Wireless controllable power control device molded into a power cable |
| US8063225B2 (en) * | 2006-08-14 | 2011-11-22 | Chembridge Corporation | Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders |
| WO2008022747A1 (en) * | 2006-08-21 | 2008-02-28 | F. Hoffmann-La Roche Ag | Tricyclic lactam derivatives, their manufacture and use as pharmaceutical agents |
| MX2010010272A (es) * | 2008-03-19 | 2011-05-25 | Chembridge Corp | Nuevos inhibidores de tirosina quinasa. |
-
2009
- 2009-03-18 MX MX2010010272A patent/MX2010010272A/es active IP Right Grant
- 2009-03-18 WO PCT/US2009/001691 patent/WO2009117097A1/en not_active Ceased
- 2009-03-18 US US12/922,891 patent/US8815906B2/en not_active Expired - Fee Related
- 2009-03-18 JP JP2011500801A patent/JP5628145B2/ja not_active Expired - Fee Related
- 2009-03-18 DK DK09721981.0T patent/DK2262807T3/en active
- 2009-03-18 EP EP15177176.3A patent/EP2966076A1/en not_active Withdrawn
- 2009-03-18 CA CA2718872A patent/CA2718872C/en not_active Expired - Fee Related
- 2009-03-18 AU AU2009226153A patent/AU2009226153B2/en not_active Ceased
- 2009-03-18 EP EP09721981.0A patent/EP2262807B1/en not_active Not-in-force
- 2009-03-18 CN CN200980118256.XA patent/CN102036990B/zh not_active Expired - Fee Related
-
2013
- 2013-01-18 JP JP2013006922A patent/JP2013082744A/ja active Pending
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