JP2010521446A5 - - Google Patents
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- JP2010521446A5 JP2010521446A5 JP2009553222A JP2009553222A JP2010521446A5 JP 2010521446 A5 JP2010521446 A5 JP 2010521446A5 JP 2009553222 A JP2009553222 A JP 2009553222A JP 2009553222 A JP2009553222 A JP 2009553222A JP 2010521446 A5 JP2010521446 A5 JP 2010521446A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- cancer
- composition
- phenyl
- formula
- 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.)
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- 239000000203 mixture Substances 0.000 claims description 64
- 150000001875 compounds Chemical class 0.000 claims description 63
- 238000000034 method Methods 0.000 claims description 34
- 208000024891 symptom Diseases 0.000 claims description 21
- 150000003839 salts Chemical class 0.000 claims description 12
- -1 alkyl sulfonic acid Chemical compound 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 9
- IIRWNGPLJQXWFJ-KRWDZBQOSA-N (1s)-2-amino-1-(4-chlorophenyl)-1-[4-(1h-pyrazol-4-yl)phenyl]ethanol Chemical compound C1([C@](O)(CN)C=2C=CC(=CC=2)C2=CNN=C2)=CC=C(Cl)C=C1 IIRWNGPLJQXWFJ-KRWDZBQOSA-N 0.000 claims description 8
- 238000004519 manufacturing process Methods 0.000 claims description 8
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 7
- 239000002253 acid Substances 0.000 claims description 7
- IIRWNGPLJQXWFJ-UHFFFAOYSA-N 2-amino-1-(4-chlorophenyl)-1-[4-(1h-pyrazol-4-yl)phenyl]ethanol Chemical compound C=1C=C(C2=CNN=C2)C=CC=1C(O)(CN)C1=CC=C(Cl)C=C1 IIRWNGPLJQXWFJ-UHFFFAOYSA-N 0.000 claims description 6
- 230000002265 prevention Effects 0.000 claims description 6
- 239000012453 solvate Substances 0.000 claims description 6
- 229910052783 alkali metal Inorganic materials 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 4
- 150000001204 N-oxides Chemical class 0.000 claims description 4
- PXIPVTKHYLBLMZ-UHFFFAOYSA-N Sodium azide Chemical compound [Na+].[N-]=[N+]=[N-] PXIPVTKHYLBLMZ-UHFFFAOYSA-N 0.000 claims description 4
- 239000012458 free base Substances 0.000 claims description 4
- XYFCBTPGUUZFHI-UHFFFAOYSA-N phosphine group Chemical group P XYFCBTPGUUZFHI-UHFFFAOYSA-N 0.000 claims description 4
- RIOQSEWOXXDEQQ-UHFFFAOYSA-N triphenylphosphine Chemical compound C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 RIOQSEWOXXDEQQ-UHFFFAOYSA-N 0.000 claims description 4
- IIRWNGPLJQXWFJ-QGZVFWFLSA-N (1r)-2-amino-1-(4-chlorophenyl)-1-[4-(1h-pyrazol-4-yl)phenyl]ethanol Chemical compound C1([C@@](O)(CN)C=2C=CC(=CC=2)C2=CNN=C2)=CC=C(Cl)C=C1 IIRWNGPLJQXWFJ-QGZVFWFLSA-N 0.000 claims description 3
- 150000001540 azides Chemical class 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- MIOPJNTWMNEORI-GMSGAONNSA-N (S)-camphorsulfonic acid Chemical compound C1C[C@@]2(CS(O)(=O)=O)C(=O)C[C@@H]1C2(C)C MIOPJNTWMNEORI-GMSGAONNSA-N 0.000 claims description 2
- LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 claims description 2
- 230000002378 acidificating effect Effects 0.000 claims description 2
- 239000007864 aqueous solution Substances 0.000 claims description 2
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims description 2
- 229940092714 benzenesulfonic acid Drugs 0.000 claims description 2
- 238000003821 enantio-separation Methods 0.000 claims description 2
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims description 2
- 229940098779 methanesulfonic acid Drugs 0.000 claims description 2
- 229910000073 phosphorus hydride Inorganic materials 0.000 claims description 2
- 239000003880 polar aprotic solvent Substances 0.000 claims description 2
- 239000002798 polar solvent Substances 0.000 claims description 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 claims description 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims description 2
- SEDZOYHHAIAQIW-UHFFFAOYSA-N trimethylsilyl azide Chemical compound C[Si](C)(C)N=[N+]=[N-] SEDZOYHHAIAQIW-UHFFFAOYSA-N 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000019691 hematopoietic and lymphoid cell neoplasm Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010048768 Dermatosis Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 206010043276 Teratoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 210000002615 epidermis Anatomy 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000008806 mesenchymal cell neoplasm Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 201000005528 peripheral nervous system neoplasm Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 description 24
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 24
- 102000008130 Cyclic AMP-Dependent Protein Kinases Human genes 0.000 description 19
- 108010049894 Cyclic AMP-Dependent Protein Kinases Proteins 0.000 description 19
- 102000005765 Proto-Oncogene Proteins c-akt Human genes 0.000 description 18
- 230000002159 abnormal effect Effects 0.000 description 15
- 230000000694 effects Effects 0.000 description 12
- 108091008611 Protein Kinase B Proteins 0.000 description 11
- 230000002401 inhibitory effect Effects 0.000 description 11
- 241000124008 Mammalia Species 0.000 description 10
- 230000001404 mediated effect Effects 0.000 description 8
- 101000600752 Rattus norvegicus 3-phosphoinositide-dependent protein kinase 1 Proteins 0.000 description 7
- 230000004663 cell proliferation Effects 0.000 description 7
- 230000030833 cell death Effects 0.000 description 6
- 230000032823 cell division Effects 0.000 description 4
- 230000033077 cellular process Effects 0.000 description 4
- 239000012535 impurity Substances 0.000 description 4
- 230000004048 modification Effects 0.000 description 3
- 238000012986 modification Methods 0.000 description 3
- 230000000069 prophylactic effect Effects 0.000 description 3
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 230000010261 cell growth Effects 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 230000001575 pathological effect Effects 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- RGRZYAZKXWNCEF-UHFFFAOYSA-N 1-(4-chlorophenyl)-1-[4-(1H-pyrazol-4-yl)phenyl]ethanol Chemical compound CC(O)(c1ccc(Cl)cc1)c1ccc(cc1)-c1cn[nH]c1 RGRZYAZKXWNCEF-UHFFFAOYSA-N 0.000 description 1
- 239000003929 acidic solution Substances 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 229940043274 prophylactic drug Drugs 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US89475207P | 2007-03-14 | 2007-03-14 | |
| GBGB0704932.3A GB0704932D0 (en) | 2007-03-14 | 2007-03-14 | Pharmaceutical compounds |
| PCT/GB2008/050180 WO2008110846A2 (en) | 2007-03-14 | 2008-03-14 | Compositions comprising (s)-2-amino-1-(4-chlorophenyl)-1-[4-(1h-pyrazol-4-yl)-phenyl]-ethanol as modulator of protein kinases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014170885A Division JP2015028033A (ja) | 2007-03-14 | 2014-08-25 | 医薬化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010521446A JP2010521446A (ja) | 2010-06-24 |
| JP2010521446A5 true JP2010521446A5 (https=) | 2012-05-10 |
Family
ID=38008428
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009553222A Pending JP2010521446A (ja) | 2007-03-14 | 2008-03-14 | 医薬化合物 |
| JP2014170885A Pending JP2015028033A (ja) | 2007-03-14 | 2014-08-25 | 医薬化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014170885A Pending JP2015028033A (ja) | 2007-03-14 | 2014-08-25 | 医薬化合物 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US20100113551A1 (https=) |
| EP (2) | EP2134339B1 (https=) |
| JP (2) | JP2010521446A (https=) |
| KR (1) | KR20100014720A (https=) |
| CN (1) | CN101686965B (https=) |
| AU (1) | AU2008224657B2 (https=) |
| BR (1) | BRPI0808802A2 (https=) |
| CA (1) | CA2679878A1 (https=) |
| CY (1) | CY1115877T1 (https=) |
| DK (1) | DK2134339T3 (https=) |
| ES (1) | ES2511817T3 (https=) |
| GB (1) | GB0704932D0 (https=) |
| HR (1) | HRP20141034T1 (https=) |
| IL (1) | IL200822A (https=) |
| MX (1) | MX2009009874A (https=) |
| NZ (1) | NZ579341A (https=) |
| PL (1) | PL2134339T3 (https=) |
| PT (1) | PT2134339E (https=) |
| RS (1) | RS53580B1 (https=) |
| RU (1) | RU2527151C2 (https=) |
| SI (1) | SI2134339T1 (https=) |
| WO (1) | WO2008110846A2 (https=) |
| ZA (1) | ZA200906303B (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0418078A8 (pt) | 2003-12-23 | 2018-01-02 | Astex Therapeutics Ltd | composto ou um seu sal, solvato, tautômero ou n-óxido, uso de um composto, métodos para a profilaxia ou tratamento de um estado ou condição doentia mediada pela proteína quinase b e mediada pela proteína quinase a, para tratar uma doença ou condição, para inibir uma proteína quinase b e uma proteína quinase a, para modular um processo celular, para tratar um distúrbio imune em um mamífero e para induzir apoptose em uma célula cancerosa, composição farmacêutica, e, processo para a preparação de um composto |
| EP1902032A1 (en) | 2005-06-22 | 2008-03-26 | Astex Therapeutics Limited | Pharmaceutical compounds |
| JP5345842B2 (ja) | 2005-06-23 | 2013-11-20 | アステックス・セラピューティクス・リミテッド | プロテインキナーゼモジュレーターとしてのピラゾール誘導体を含む医薬組み合わせ |
| GB0704932D0 (en) | 2007-03-14 | 2007-04-25 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| CA3121743A1 (en) | 2009-01-15 | 2010-07-22 | Incyte Holdings Corporation | Processes for preparing jak inhibitors and related intermediate compounds |
| WO2015134837A2 (en) * | 2014-03-06 | 2015-09-11 | University Of Southern California | Use of short term starvation regimen in combination with kinase inhibitors to enhance traditional chemo-drug efficacy and feasibility and reverse side effects of kinases in normal cells and tissues |
| RU2657832C1 (ru) * | 2017-06-07 | 2018-06-15 | федеральное государственное автономное образовательное учреждение высшего образования "Южный федеральный университет" | Антидиабетическое средство |
| EP3424533A1 (en) * | 2017-07-05 | 2019-01-09 | Nh Theraguix | Methods for treating tumors |
| US10696638B2 (en) | 2017-12-26 | 2020-06-30 | Industrial Technology Research Institute | Compounds for inhibiting AGC kinase and pharmaceutical compositions comprising the same |
| EP4125910B1 (en) * | 2020-03-25 | 2025-11-12 | Woolsey Pharmaceuticals, Inc. | Rho kinase inhibitors for treating frontotemporal dementia |
| CN111707830B (zh) * | 2020-07-16 | 2023-08-15 | 首都医科大学附属北京朝阳医院 | Rock激酶活性在辅助诊断肺损害中的应用 |
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| WO2025017499A1 (en) | 2023-07-17 | 2025-01-23 | Graviton Bioscience Bv | Formulations and uses of rock2 inhibitors for als |
| WO2025069008A1 (en) | 2023-09-28 | 2025-04-03 | Graviton Bioscience Bv | Therapy for treating type 1 diabetes using rock2 and dyrk1 inhibitors |
| WO2025069009A1 (en) | 2023-09-29 | 2025-04-03 | Graviton Bioscience Bv | Rock2 inhibitors in the treatment of obesity |
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| RU2419612C2 (ru) * | 2003-12-23 | 2011-05-27 | Астекс Терапьютикс Лимитед | Производные пиразола в качестве модуляторов протеинкиназы |
| BRPI0418078A8 (pt) | 2003-12-23 | 2018-01-02 | Astex Therapeutics Ltd | composto ou um seu sal, solvato, tautômero ou n-óxido, uso de um composto, métodos para a profilaxia ou tratamento de um estado ou condição doentia mediada pela proteína quinase b e mediada pela proteína quinase a, para tratar uma doença ou condição, para inibir uma proteína quinase b e uma proteína quinase a, para modular um processo celular, para tratar um distúrbio imune em um mamífero e para induzir apoptose em uma célula cancerosa, composição farmacêutica, e, processo para a preparação de um composto |
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-
2007
- 2007-03-14 GB GBGB0704932.3A patent/GB0704932D0/en not_active Ceased
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2008
- 2008-03-14 WO PCT/GB2008/050180 patent/WO2008110846A2/en not_active Ceased
- 2008-03-14 SI SI200831312T patent/SI2134339T1/sl unknown
- 2008-03-14 BR BRPI0808802A patent/BRPI0808802A2/pt not_active IP Right Cessation
- 2008-03-14 JP JP2009553222A patent/JP2010521446A/ja active Pending
- 2008-03-14 PL PL08719025T patent/PL2134339T3/pl unknown
- 2008-03-14 RS RSP20140587 patent/RS53580B1/sr unknown
- 2008-03-14 ES ES08719025.2T patent/ES2511817T3/es active Active
- 2008-03-14 PT PT87190252T patent/PT2134339E/pt unknown
- 2008-03-14 CA CA002679878A patent/CA2679878A1/en not_active Abandoned
- 2008-03-14 EP EP08719025.2A patent/EP2134339B1/en active Active
- 2008-03-14 NZ NZ579341A patent/NZ579341A/xx not_active IP Right Cessation
- 2008-03-14 MX MX2009009874A patent/MX2009009874A/es active IP Right Grant
- 2008-03-14 DK DK08719025.2T patent/DK2134339T3/da active
- 2008-03-14 US US12/531,013 patent/US20100113551A1/en not_active Abandoned
- 2008-03-14 CN CN200880015813.0A patent/CN101686965B/zh not_active Expired - Fee Related
- 2008-03-14 RU RU2009137779/04A patent/RU2527151C2/ru not_active IP Right Cessation
- 2008-03-14 KR KR1020097020516A patent/KR20100014720A/ko not_active Ceased
- 2008-03-14 HR HRP20141034AT patent/HRP20141034T1/hr unknown
- 2008-03-14 AU AU2008224657A patent/AU2008224657B2/en not_active Ceased
- 2008-03-14 EP EP11194939A patent/EP2433632A1/en not_active Withdrawn
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- 2014-11-12 CY CY20141100938T patent/CY1115877T1/el unknown
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