JP2012516344A5 - - Google Patents
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- JP2012516344A5 JP2012516344A5 JP2011548275A JP2011548275A JP2012516344A5 JP 2012516344 A5 JP2012516344 A5 JP 2012516344A5 JP 2011548275 A JP2011548275 A JP 2011548275A JP 2011548275 A JP2011548275 A JP 2011548275A JP 2012516344 A5 JP2012516344 A5 JP 2012516344A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- leukemia
- chloro
- methyl
- mammal
- 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.)
- Pending
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- 238000000034 method Methods 0.000 claims 17
- 241000124008 Mammalia Species 0.000 claims 13
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 208000032839 leukemia Diseases 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 6
- 210000004027 cell Anatomy 0.000 claims 6
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims 4
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 4
- 208000034578 Multiple myelomas Diseases 0.000 claims 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 4
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 4
- YFQJOPFTGMHYNV-YDALLXLXSA-N n-[(2s)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide;hydrochloride Chemical compound Cl.CN1N=CC(Cl)=C1C1=C(Cl)SC(C(=O)N[C@H](CN)CC=2C=C(F)C=CC=2)=C1 YFQJOPFTGMHYNV-YDALLXLXSA-N 0.000 claims 4
- -1 4-chloro-1-methyl-1H-pyrazol-5-yl Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000000843 powder Substances 0.000 claims 3
- 230000005855 radiation Effects 0.000 claims 3
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000012609 Cowden disease Diseases 0.000 claims 2
- 201000002847 Cowden syndrome Diseases 0.000 claims 2
- 206010014733 Endometrial cancer Diseases 0.000 claims 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 2
- 206010014967 Ependymoma Diseases 0.000 claims 2
- 208000031637 Erythroblastic Acute Leukemia Diseases 0.000 claims 2
- 208000036566 Erythroleukaemia Diseases 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 2
- 208000002966 Giant Cell Tumor of Bone Diseases 0.000 claims 2
- 208000032612 Glial tumor Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 208000005726 Inflammatory Breast Neoplasms Diseases 0.000 claims 2
- 206010021980 Inflammatory carcinoma of the breast Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000000172 Medulloblastoma Diseases 0.000 claims 2
- 208000035490 Megakaryoblastic Acute Leukemia Diseases 0.000 claims 2
- 206010027406 Mesothelioma Diseases 0.000 claims 2
- 208000008770 Multiple Hamartoma Syndrome Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 claims 2
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000004337 Salivary Gland Neoplasms Diseases 0.000 claims 2
- 206010061934 Salivary gland cancer Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 208000000389 T-cell leukemia Diseases 0.000 claims 2
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 2
- 206010057644 Testis cancer Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 206010047741 Vulval cancer Diseases 0.000 claims 2
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 2
- 208000008383 Wilms tumor Diseases 0.000 claims 2
- 208000021841 acute erythroid leukemia Diseases 0.000 claims 2
- 208000037833 acute lymphoblastic T-cell leukemia Diseases 0.000 claims 2
- 208000013593 acute megakaryoblastic leukemia Diseases 0.000 claims 2
- 208000020700 acute megakaryocytic leukemia Diseases 0.000 claims 2
- 201000011143 bone giant cell tumor Diseases 0.000 claims 2
- 210000004556 brain Anatomy 0.000 claims 2
- 210000000481 breast Anatomy 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 2
- 210000001072 colon Anatomy 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 201000003444 follicular lymphoma Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 201000009277 hairy cell leukemia Diseases 0.000 claims 2
- 210000003128 head Anatomy 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 201000004653 inflammatory breast carcinoma Diseases 0.000 claims 2
- 210000003734 kidney Anatomy 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 210000003739 neck Anatomy 0.000 claims 2
- 201000008026 nephroblastoma Diseases 0.000 claims 2
- 210000000440 neutrophil Anatomy 0.000 claims 2
- 201000008968 osteosarcoma Diseases 0.000 claims 2
- 210000001672 ovary Anatomy 0.000 claims 2
- 210000000496 pancreas Anatomy 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 210000002307 prostate Anatomy 0.000 claims 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 201000003120 testicular cancer Diseases 0.000 claims 2
- 210000001685 thyroid gland Anatomy 0.000 claims 2
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 201000005102 vulva cancer Diseases 0.000 claims 2
- GCNXUMCDUZBULH-HNCPQSOCSA-N Cl.NC[C@@H](CC1=CC(=CC=C1)F)C1=C(SC(=C1C1=C(C=NN1C)Cl)Cl)C(=O)N Chemical compound Cl.NC[C@@H](CC1=CC(=CC=C1)F)C1=C(SC(=C1C1=C(C=NN1C)Cl)Cl)C(=O)N GCNXUMCDUZBULH-HNCPQSOCSA-N 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 229940034982 antineoplastic agent Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14849009P | 2009-01-30 | 2009-01-30 | |
| US61/148,490 | 2009-01-30 | ||
| PCT/US2010/022323 WO2010088331A1 (en) | 2009-01-30 | 2010-01-28 | Crystalline n-{(1-s)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1h-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015114505A Division JP6328590B2 (ja) | 2009-01-30 | 2015-06-05 | 結晶質n−{(1s)−2−アミノ−1−[(3−フルオロフェニル)メチル]エチル}−5−クロロ−4−(4−クロロ−1−メチル−1h−ピラゾール−5−イル)−2−チオフェンカルボキサミド塩酸塩 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012516344A JP2012516344A (ja) | 2012-07-19 |
| JP2012516344A5 true JP2012516344A5 (https=) | 2012-10-11 |
Family
ID=42395995
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011548275A Pending JP2012516344A (ja) | 2009-01-30 | 2010-01-28 | 結晶質n−{(1s)−2−アミノ−1−[(3−フルオロフェニル)メチル]エチル}−5−クロロ−4−(4−クロロ−1−メチル−1h−ピラゾール−5−イル)−2−チオフェンカルボキサミド塩酸塩 |
| JP2015114505A Active JP6328590B2 (ja) | 2009-01-30 | 2015-06-05 | 結晶質n−{(1s)−2−アミノ−1−[(3−フルオロフェニル)メチル]エチル}−5−クロロ−4−(4−クロロ−1−メチル−1h−ピラゾール−5−イル)−2−チオフェンカルボキサミド塩酸塩 |
| JP2016235681A Withdrawn JP2017061559A (ja) | 2009-01-30 | 2016-12-05 | 結晶質n−{(1s)−2−アミノ−1−[(3−フルオロフェニル)メチル]エチル}−5−クロロ−4−(4−クロロ−1−メチル−1h−ピラゾール−5−イル)−2−チオフェンカルボキサミド塩酸塩 |
| JP2019057789A Active JP6924794B2 (ja) | 2009-01-30 | 2019-03-26 | 結晶質n−{(1s)−2−アミノ−1−[(3−フルオロフェニル)メチル]エチル}−5−クロロ−4−(4−クロロ−1−メチル−1h−ピラゾール−5−イル)−2−チオフェンカルボキサミド塩酸塩 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015114505A Active JP6328590B2 (ja) | 2009-01-30 | 2015-06-05 | 結晶質n−{(1s)−2−アミノ−1−[(3−フルオロフェニル)メチル]エチル}−5−クロロ−4−(4−クロロ−1−メチル−1h−ピラゾール−5−イル)−2−チオフェンカルボキサミド塩酸塩 |
| JP2016235681A Withdrawn JP2017061559A (ja) | 2009-01-30 | 2016-12-05 | 結晶質n−{(1s)−2−アミノ−1−[(3−フルオロフェニル)メチル]エチル}−5−クロロ−4−(4−クロロ−1−メチル−1h−ピラゾール−5−イル)−2−チオフェンカルボキサミド塩酸塩 |
| JP2019057789A Active JP6924794B2 (ja) | 2009-01-30 | 2019-03-26 | 結晶質n−{(1s)−2−アミノ−1−[(3−フルオロフェニル)メチル]エチル}−5−クロロ−4−(4−クロロ−1−メチル−1h−ピラゾール−5−イル)−2−チオフェンカルボキサミド塩酸塩 |
Country Status (25)
| Country | Link |
|---|---|
| US (5) | US20110288142A1 (https=) |
| EP (2) | EP4242206A1 (https=) |
| JP (4) | JP2012516344A (https=) |
| KR (1) | KR101420484B1 (https=) |
| CN (1) | CN102405047B (https=) |
| AR (1) | AR075153A1 (https=) |
| AU (1) | AU2010208265B2 (https=) |
| BR (1) | BRPI1006896B1 (https=) |
| CA (1) | CA2750565C (https=) |
| CL (1) | CL2011001830A1 (https=) |
| CO (1) | CO6400189A2 (https=) |
| CR (1) | CR20110422A (https=) |
| EA (1) | EA018907B1 (https=) |
| IL (1) | IL214023A (https=) |
| MA (1) | MA32998B1 (https=) |
| MX (1) | MX2011008073A (https=) |
| MY (1) | MY161598A (https=) |
| NZ (1) | NZ594064A (https=) |
| PE (1) | PE20120003A1 (https=) |
| SG (1) | SG172926A1 (https=) |
| TW (1) | TWI503317B (https=) |
| UA (1) | UA106740C2 (https=) |
| UY (1) | UY32407A (https=) |
| WO (1) | WO2010088331A1 (https=) |
| ZA (1) | ZA201105033B (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102405047B (zh) | 2009-01-30 | 2014-07-09 | 葛兰素史密斯克莱有限责任公司 | 结晶型的n-{(1s)-2-氨基-1-[(3-氟苯基)甲基]乙基}-5-氯-4-(4-氯-1-甲基-1h-吡唑-5-基)-2-噻吩甲酰胺盐酸盐 |
| WO2011146710A1 (en) | 2010-05-21 | 2011-11-24 | Glaxosmithkline Llc | Combination |
| US20130237554A1 (en) * | 2010-05-26 | 2013-09-12 | Rakesh Kumar | Combination |
| SG10201600077RA (en) * | 2011-01-11 | 2016-02-26 | Glaxosmithkline Llc | Combination |
| US20150087683A1 (en) | 2012-04-24 | 2015-03-26 | Glaxosmithkline Intellectual Property (No.2) Limited | Treatment method for steroid responsive dermatoses |
| EP2986287A2 (en) * | 2013-04-18 | 2016-02-24 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods and pharmaceutical compositions (ctps 1 inhibitors, e.g. norleucine) for inhibiting t cell proliferation in a subject in need thereof |
| CN109806266A (zh) * | 2013-10-01 | 2019-05-28 | 诺华股份有限公司 | 用于癌症治疗的组合及其应用 |
| MX2016004265A (es) * | 2013-10-01 | 2016-07-08 | Novartis Ag | Combinacion. |
| AU2015228475B9 (en) * | 2014-03-12 | 2017-09-21 | Novartis Ag | Combination comprising a BTK inhibitor and an AKT inhibitor |
| ES2909576T3 (es) | 2016-10-11 | 2022-05-09 | Univ Duke | Tratamiento con lasofoxifeno del cáncer de mama ER+ |
| JP6515944B2 (ja) | 2016-12-20 | 2019-05-22 | 株式会社デンソー | 半導体装置およびその製造方法 |
| US11497730B2 (en) | 2018-04-10 | 2022-11-15 | Duke University | Lasofoxifene treatment of breast cancer |
| TWI857119B (zh) | 2019-08-08 | 2024-10-01 | 香港商來凱有限公司 | 治療癌症之方法 |
| US11915283B1 (en) | 2019-08-13 | 2024-02-27 | Splitcart Llc | Cost sharing platform and system |
| US12067592B2 (en) | 2019-08-13 | 2024-08-20 | Splitcart Llc | Co-purchasing system and method |
| GB202116903D0 (en) * | 2021-11-18 | 2022-01-05 | Sermonix Pharmaceuticals Inc | Lasofoxifene treatment of aromatase-resistant er+ cancer |
| EP4493189A1 (en) | 2022-03-14 | 2025-01-22 | Laekna Limited | Combination treatment for cancer |
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