JP2010518110A5 - - Google Patents
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- JP2010518110A5 JP2010518110A5 JP2009549232A JP2009549232A JP2010518110A5 JP 2010518110 A5 JP2010518110 A5 JP 2010518110A5 JP 2009549232 A JP2009549232 A JP 2009549232A JP 2009549232 A JP2009549232 A JP 2009549232A JP 2010518110 A5 JP2010518110 A5 JP 2010518110A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- leukemia
- pharmaceutical composition
- lymphoma
- compound
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 11
- -1 4-chloro-1-methyl-1H-pyrazol-5-yl Chemical group 0.000 claims description 3
- 238000000034 method Methods 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 208000032839 leukemia Diseases 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 5
- 241000124008 Mammalia Species 0.000 claims 5
- 206010038389 Renal cancer Diseases 0.000 claims 5
- 201000010982 kidney cancer Diseases 0.000 claims 5
- 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
- 210000004027 cell Anatomy 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
- 208000003174 Brain Neoplasms Diseases 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 208000032612 Glial tumor Diseases 0.000 claims 3
- 206010018338 Glioma Diseases 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 3
- 208000029742 colonic neoplasm Diseases 0.000 claims 3
- 208000005017 glioblastoma Diseases 0.000 claims 3
- 201000010536 head and neck cancer Diseases 0.000 claims 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims 3
- 201000007270 liver cancer Diseases 0.000 claims 3
- 208000014018 liver neoplasm Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 201000002510 thyroid cancer Diseases 0.000 claims 3
- 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
- 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
- 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
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000035490 Megakaryoblastic Acute Leukemia Diseases 0.000 claims 2
- 206010027406 Mesothelioma 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
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 208000007452 Plasmacytoma Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma 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
- 208000006593 Urologic 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
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 201000000053 blastoma Diseases 0.000 claims 2
- 201000011143 bone giant cell tumor Diseases 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
- 201000008184 embryoma Diseases 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 201000003444 follicular lymphoma Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 201000009277 hairy cell leukemia Diseases 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
- 239000003112 inhibitor Substances 0.000 claims 2
- 208000022013 kidney Wilms tumor Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 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
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 201000003120 testicular cancer Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 201000005102 vulva cancer Diseases 0.000 claims 2
- VEEGZPWAAPPXRB-BJMVGYQFSA-N (3e)-3-(1h-imidazol-5-ylmethylidene)-1h-indol-2-one Chemical compound O=C1NC2=CC=CC=C2\C1=C/C1=CN=CN1 VEEGZPWAAPPXRB-BJMVGYQFSA-N 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- 229940123780 DNA topoisomerase I inhibitor Drugs 0.000 claims 1
- 229940124087 DNA topoisomerase II inhibitor Drugs 0.000 claims 1
- AFJRDFWMXUECEW-LBPRGKRZSA-N N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methyl-3-pyrazolyl)-2-thiophenecarboxamide Chemical compound CN1N=CC(Cl)=C1C1=C(Cl)SC(C(=O)N[C@H](CN)CC=2C=C(F)C=CC=2)=C1 AFJRDFWMXUECEW-LBPRGKRZSA-N 0.000 claims 1
- 239000000365 Topoisomerase I Inhibitor Substances 0.000 claims 1
- 239000000317 Topoisomerase II Inhibitor Substances 0.000 claims 1
- 229940100198 alkylating agent Drugs 0.000 claims 1
- 239000002168 alkylating agent Substances 0.000 claims 1
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 1
- 229940121369 angiogenesis inhibitor Drugs 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 230000000340 anti-metabolite Effects 0.000 claims 1
- 229940044684 anti-microtubule agent Drugs 0.000 claims 1
- 229940100197 antimetabolite Drugs 0.000 claims 1
- 239000002256 antimetabolite Substances 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 230000022131 cell cycle Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000003668 hormone analog Substances 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 102000037979 non-receptor tyrosine kinases Human genes 0.000 claims 1
- 108091008046 non-receptor tyrosine kinases Proteins 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 229910052697 platinum Inorganic materials 0.000 claims 1
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Substances [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims 1
- 230000000861 pro-apoptotic effect Effects 0.000 claims 1
- 201000002025 prostate sarcoma Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000019491 signal transduction Effects 0.000 claims 1
- 230000011664 signaling Effects 0.000 claims 1
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- HLXOVAMYQUFLPE-UHFFFAOYSA-N 1-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazole Chemical compound CN1N=CC=C1B1OC(C)(C)C(C)(C)O1 HLXOVAMYQUFLPE-UHFFFAOYSA-N 0.000 description 1
- UTMKWFBCXAJEFO-UHFFFAOYSA-N BrC=1C=C(SC1Br)C(=O)O.BrC=1C=C(OC1Br)C(=O)O Chemical compound BrC=1C=C(SC1Br)C(=O)O.BrC=1C=C(OC1Br)C(=O)O UTMKWFBCXAJEFO-UHFFFAOYSA-N 0.000 description 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 1
- IAZDPXIOMUYVGZ-WFGJKAKNSA-N Dimethyl sulfoxide Chemical compound [2H]C([2H])([2H])S(=O)C([2H])([2H])[2H] IAZDPXIOMUYVGZ-WFGJKAKNSA-N 0.000 description 1
- IEGSHZJZJKDMBQ-UHFFFAOYSA-N n-(2-amino-1-phenylethyl)-4-bromo-5-(2-methylpyrazol-3-yl)thiophene-2-carboxamide Chemical compound CN1N=CC=C1C1=C(Br)C=C(C(=O)NC(CN)C=2C=CC=CC=2)S1 IEGSHZJZJKDMBQ-UHFFFAOYSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- CLUUDOMFHPDBIR-UHFFFAOYSA-N tert-butyl n-(2-amino-2-phenylethyl)carbamate Chemical compound CC(C)(C)OC(=O)NCC(N)C1=CC=CC=C1 CLUUDOMFHPDBIR-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US88858607P | 2007-02-07 | 2007-02-07 | |
| US60/888,586 | 2007-02-07 | ||
| PCT/US2008/053269 WO2008098104A1 (en) | 2007-02-07 | 2008-02-07 | Inhibitors of akt activity |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011024171A Division JP5010038B2 (ja) | 2007-02-07 | 2011-02-07 | Ａｋｔ活性阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010518110A JP2010518110A (ja) | 2010-05-27 |
| JP2010518110A5 true JP2010518110A5 (enExample) | 2011-04-07 |
| JP4723677B2 JP4723677B2 (ja) | 2011-07-13 |
Family
ID=39682107
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009549232A Active JP4723677B2 (ja) | 2007-02-07 | 2008-02-07 | Ａｋｔ活性阻害剤 |
| JP2011024171A Active JP5010038B2 (ja) | 2007-02-07 | 2011-02-07 | Ａｋｔ活性阻害剤 |
| JP2012089471A Active JP5511879B2 (ja) | 2007-02-07 | 2012-04-10 | Ａｋｔ活性阻害剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011024171A Active JP5010038B2 (ja) | 2007-02-07 | 2011-02-07 | Ａｋｔ活性阻害剤 |
| JP2012089471A Active JP5511879B2 (ja) | 2007-02-07 | 2012-04-10 | Ａｋｔ活性阻害剤 |
Country Status (34)
Families Citing this family (112)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7625890B2 (en) | 2005-11-10 | 2009-12-01 | Smithkline Beecham Corp. | Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| WO2009094224A1 (en) | 2008-01-25 | 2009-07-30 | Millennium Pharmaceuticals, Inc. | Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
| US20100048913A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
| SG171914A1 (en) | 2008-12-02 | 2011-07-28 | Chiralgen Ltd | Method for the synthesis of phosphorus atom modified nucleic acids |
| CA2750935A1 (en) | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| MA32998B1 (fr) * | 2009-01-30 | 2012-01-02 | Glaxosmithkline Llc | Chlorhydrate de n-{(1-s)-2-amino-1-[(3-fluorophényl) méthyl]éthyl}-5-chloro-4-(4-chloro-1-methyl-1h-pyrazol-5-yl)-2-thiophènecarboxamide cristallin |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| WO2010091306A1 (en) | 2009-02-05 | 2010-08-12 | Tokai Pharmaceuticals | Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens |
| US9744183B2 (en) | 2009-07-06 | 2017-08-29 | Wave Life Sciences Ltd. | Nucleic acid prodrugs and methods of use thereof |
| BR112012006485A2 (pt) * | 2009-09-23 | 2015-09-08 | Glaxosmithkline Llc | combinação |
| KR20120099219A (ko) * | 2009-09-23 | 2012-09-07 | 글락소스미스클라인 엘엘씨 | 조합물 |
| BR112012008271A2 (pt) * | 2009-10-08 | 2015-09-22 | Glaxosmithkline Llc | combinação |
| AU2010303364B2 (en) | 2009-10-08 | 2013-09-19 | Novartis Ag | Combination |
| WO2011060380A1 (en) * | 2009-11-14 | 2011-05-19 | The Regents Of The University Of California | Pik3ca mutation status and sash1 expression predicts synergy between lapatinib and an akt inhibitor in her2 positive breast cancer |
| US8598156B2 (en) | 2010-03-25 | 2013-12-03 | Glaxosmithkline Llc | Chemical compounds |
| CA2829790C (en) | 2010-03-30 | 2018-06-05 | Verseon Corporation | Multisubstituted aromatic compounds as inhibitors of thrombin |
| EP2572199B1 (en) | 2010-05-21 | 2017-03-08 | Novartis AG | Combination |
| JP2013526613A (ja) * | 2010-05-26 | 2013-06-24 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | 組合せ |
| EP2603216A4 (en) | 2010-08-11 | 2013-12-18 | Millennium Pharm Inc | HETEROARYLE AND USES THEREOF |
| US9062038B2 (en) | 2010-08-11 | 2015-06-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| EP2603214A4 (en) | 2010-08-11 | 2013-12-18 | Millennium Pharm Inc | HETEROARYLE AND USES THEREOF |
| DK2620428T3 (da) | 2010-09-24 | 2019-07-01 | Wave Life Sciences Ltd | Asymmetrisk hjælpegruppe |
| MX2013004003A (es) | 2010-10-13 | 2013-10-01 | Millenium Pharmaceuticals Inc | Heteroarilos y usos de los mismos. |
| TWI505828B (zh) | 2010-12-20 | 2015-11-01 | 葛蘭素史克智慧財產（第二）有限公司 | 新穎醫藥組成物 |
| CN103298345B (zh) | 2011-01-11 | 2016-12-14 | 诺瓦蒂斯公司 | 组合 |
| US20120184542A1 (en) | 2011-01-19 | 2012-07-19 | Kevin Anderson | Pyrido pyrimidines |
| US20120184548A1 (en) | 2011-01-19 | 2012-07-19 | Romyr Dominique | Carboxylic acid aryl amides |
| US8362023B2 (en) | 2011-01-19 | 2013-01-29 | Hoffmann-La Roche Inc. | Pyrazolo pyrimidines |
| US20120184562A1 (en) | 2011-01-19 | 2012-07-19 | Kin-Chun Luk | 1,6- and 1,8-naphthyridines |
| US8673905B2 (en) | 2011-03-17 | 2014-03-18 | Hoffmann-La Roche Inc. | Imidazo pyrazines |
| WO2012177925A1 (en) | 2011-06-21 | 2012-12-27 | The Board Institute, Inc. | Akt inhibitors for treating cancer expressing a magi3 - akt3 fusion gene |
| RU2014105311A (ru) | 2011-07-19 | 2015-08-27 | Уэйв Лайф Сайенсес Пте. Лтд. | Способы синтеза функционализованных нуклеиновых кислот |
| JP2015503504A (ja) * | 2011-12-23 | 2015-02-02 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | ヘテロアリールおよびその使用 |
| JP2015514792A (ja) | 2012-04-24 | 2015-05-21 | グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｎｏ．２ Ｌｉｍｉｔｅｄ | ステロイド反応性皮膚病の治療方法 |
| KR102712879B1 (ko) | 2012-07-13 | 2024-10-04 | 웨이브 라이프 사이언시스 리미티드 | 키랄 제어 |
| PT2872485T (pt) | 2012-07-13 | 2021-03-05 | Wave Life Sciences Ltd | Grupo auxiliar assimétrico |
| BR112015000723A2 (pt) | 2012-07-13 | 2017-06-27 | Shin Nippon Biomedical Laboratories Ltd | adjuvante de ácido nucléico quiral |
| JP6254169B2 (ja) | 2012-09-28 | 2017-12-27 | ファイザー・インク | ベンズアミドおよびヘテロベンズアミド化合物 |
| EA201590750A1 (ru) | 2012-10-16 | 2015-09-30 | Янссен Фармацевтика Нв | СВЯЗАННЫЕ С ФЕНИЛОМ ХИНОЛИНИЛОВЫЕ МОДУЛЯТОРЫ RORγT |
| ES2619610T3 (es) | 2012-10-16 | 2017-06-26 | Janssen Pharmaceutica Nv | Moduladores de ROR-gamma-t de quinolinilo enlazado con heteroarilo |
| SG11201502369XA (en) | 2012-10-16 | 2015-05-28 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of ror-gamma-t |
| CA2889051A1 (en) * | 2012-10-22 | 2014-05-01 | Glaxosmithkline Llc | Combination |
| SG11201503688SA (en) | 2012-11-30 | 2015-06-29 | Glaxosmithkline Llc | Novel pharmaceutical composition |
| WO2014108837A1 (en) | 2013-01-09 | 2014-07-17 | Glaxosmithkline Intellectual Property (No.2) Limited | Combination |
| CN105189488B (zh) | 2013-02-27 | 2018-07-24 | 百时美施贵宝公司 | 用作溴区结构域抑制剂的咔唑化合物 |
| BR112015023098A2 (pt) | 2013-03-14 | 2017-07-18 | Univ Jefferson | agentes de infrarregulação do receptor de andrógeno e usos dos mesmos |
| ES2853483T3 (es) | 2013-03-15 | 2021-09-16 | Verseon Int Corporation | Compuestos aromáticos multisustituidos como inhibidores de la serina proteasa |
| ES2791749T3 (es) * | 2013-03-15 | 2020-11-05 | Verseon Corp | Halogenopirazoles como inhibidores de la trombina |
| CN105764501A (zh) | 2013-07-26 | 2016-07-13 | 现代化制药公司 | 改善比生群治疗效益的组合物 |
| KR20160058774A (ko) | 2013-08-12 | 2016-05-25 | 토카이 파마슈티컬, 아이엔씨. | 안드로겐-표적 치료제를 이용하는 종양 질환 치료를 위한 바이오마커 |
| CN109674801A (zh) | 2013-10-01 | 2019-04-26 | 诺华股份有限公司 | 组合 |
| US20160235714A1 (en) * | 2013-10-01 | 2016-08-18 | Novartis Ag | Enzalutamide in combination with afuresertib for the treatment of cancer |
| US9328095B2 (en) | 2013-10-15 | 2016-05-03 | Janssen Pharmaceutica Nv | Heteroaryl linked quinolinyl modulators of RORgammat |
| EP3057949B1 (en) | 2013-10-15 | 2019-06-05 | Janssen Pharmaceutica NV | Secondary alcohol quinolinyl modulators of ror gamma t |
| US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
| US9346782B2 (en) | 2013-10-15 | 2016-05-24 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
| US9221804B2 (en) | 2013-10-15 | 2015-12-29 | Janssen Pharmaceutica Nv | Secondary alcohol quinolinyl modulators of RORγt |
| CA2927182A1 (en) | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | Quinolinyl modulators of ror.gamma.t |
| US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
| US9284308B2 (en) | 2013-10-15 | 2016-03-15 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of RORγt |
| WO2015056180A1 (en) | 2013-10-15 | 2015-04-23 | Glaxosmithkline Intellectual Property (No.2) Limited | Indoline derivatives as inhibitors of perk |
| SI3466949T1 (sl) | 2013-12-24 | 2021-03-31 | Bristol-Myers Squibb Company | Triciklična spojina kot sredstvo proti raku |
| JPWO2015108048A1 (ja) | 2014-01-15 | 2017-03-23 | 株式会社新日本科学 | 抗腫瘍作用を有するキラル核酸アジュバンド及び抗腫瘍剤 |
| JPWO2015108046A1 (ja) | 2014-01-15 | 2017-03-23 | 株式会社新日本科学 | 抗アレルギー作用を有するキラル核酸アジュバンド及び抗アレルギー剤 |
| JPWO2015108047A1 (ja) | 2014-01-15 | 2017-03-23 | 株式会社新日本科学 | 免疫誘導活性を有するキラル核酸アジュバンド及び免疫誘導活性剤 |
| PT3094728T (pt) | 2014-01-16 | 2022-05-19 | Wave Life Sciences Ltd | Desenho quiral |
| MX2016011674A (es) * | 2014-03-12 | 2017-04-27 | Novartis Ag | Combinacion que comprende un inhibidor de btk y un inhibidor de akt. |
| CN104926801B (zh) * | 2014-03-22 | 2019-06-04 | 浙江大学 | 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用 |
| KR102359214B1 (ko) | 2014-04-04 | 2022-02-07 | 델 마 파마슈티컬스 | 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체 |
| WO2015188073A1 (en) | 2014-06-06 | 2015-12-10 | Research Triangle Institute | Apelin receptor (apj) agonists and uses thereof |
| SG11201701940UA (en) | 2014-09-17 | 2017-04-27 | Verseon Corp | Pyrazolyl-substituted pyridone compounds as serine protease inhibitors |
| WO2016059602A2 (en) | 2014-10-16 | 2016-04-21 | Glaxo Group Limited | Methods of treating cancer and related compositions |
| TW201630907A (zh) | 2014-12-22 | 2016-09-01 | 必治妥美雅史谷比公司 | ＴＧＦβＲ拮抗劑 |
| HK1246164A1 (zh) | 2015-02-27 | 2018-09-07 | Verseon Corporation | 作为丝氨酸蛋白酶抑制剂的被取代的吡唑化合物 |
| EP3380097A2 (en) | 2015-08-28 | 2018-10-03 | Novartis AG | Pharmaceutical combination comprising (a) the alpha-isoform specific pi3k inhibitor alpelisib (byl719) and (b) an akt inhibitor, preferably mk-2206, afuresertib or uprosertib, and the use thereof in the treatment/prevention of cancer |
| WO2017098421A1 (en) | 2015-12-08 | 2017-06-15 | Glaxosmithkline Intellectual Property Development Limited | Benzothiadiazine compounds |
| HK1255452A1 (zh) | 2015-12-09 | 2019-08-16 | Research Triangle Institute | 改进的爱帕琳肽受体(apj)激动剂及其用途 |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| WO2017153952A1 (en) | 2016-03-10 | 2017-09-14 | Glaxosmithkline Intellectual Property Development Limited | 5-sulfamoyl-2-hydroxybenzamide derivatives |
| EP3473628B1 (en) * | 2016-06-16 | 2019-12-11 | Harbin Zhenbao Pharmaceutical Co., Ltd. | Dihydropyrazole azepine compound serving as akt inhibitor |
| US11926612B2 (en) * | 2016-10-12 | 2024-03-12 | Research Triangle Institute | Heterocyclic apelin receptor (APJ) agonists and uses thereof |
| WO2018100536A1 (en) | 2016-12-01 | 2018-06-07 | Glaxosmithkline Intellectual Property Development Limited | Methods of treating cancer |
| JP2020506904A (ja) | 2017-01-27 | 2020-03-05 | シグナルアールエックス ファーマシューティカルズ，インコーポレイテッド | キナーゼ、ブロモドメイン及びチェックポイント阻害剤としてのチエノピラノン及びフラノピラノン |
| CN107011377B (zh) * | 2017-05-03 | 2019-02-26 | 南通书创药业科技有限公司 | 一种β-羰基磷酸酯的制备方法 |
| WO2019008487A1 (en) | 2017-07-05 | 2019-01-10 | Novartis Ag | NEW PHARMACEUTICAL COMPOSITION |
| TW201922721A (zh) | 2017-09-07 | 2019-06-16 | 英商葛蘭素史克智慧財產發展有限公司 | 化學化合物 |
| WO2019053617A1 (en) | 2017-09-12 | 2019-03-21 | Glaxosmithkline Intellectual Property Development Limited | CHEMICAL COMPOUNDS |
| PT3725791T (pt) * | 2017-12-13 | 2023-04-04 | Harbin Zhenbao Pharmaceutical Co Ltd | Sal que serve como inibidor de akt e seu cristal |
| WO2020023340A1 (en) | 2018-07-23 | 2020-01-30 | Signalrx Pharmaceuticals, Inc. | Single molecule compounds providing multi-target inhibition of btk and other proteins and methods of use thereof |
| EP3866807A1 (en) | 2018-10-16 | 2021-08-25 | F. Hoffmann-La Roche AG | Use of akt inhibitors in ophthalmology |
| JP2022506508A (ja) | 2018-11-05 | 2022-01-17 | アイオバンス バイオセラピューティクス，インコーポレイテッド | Ａｋｔ経路阻害剤を利用したｔｉｌの拡大培養 |
| BR112021010353A2 (pt) | 2018-11-30 | 2021-08-31 | Glaxosmithkline Intellectual Property Development Limited | Compostos úteis em terapia hiv |
| AU2019407426A1 (en) | 2018-12-21 | 2021-07-22 | Daiichi Sankyo Company, Limited | Combination of antibody-drug conjugate and kinase inhibitor |
| CN110031626A (zh) * | 2019-04-02 | 2019-07-19 | 浙江理工大学 | 一种用于胃肠道间质肿瘤迁移的标志物ack1及其应用 |
| WO2021018941A1 (en) | 2019-07-31 | 2021-02-04 | Glaxosmithkline Intellectual Property Development Limited | Methods of treating cancer |
| BR112022001508A2 (pt) | 2019-08-08 | 2022-07-12 | Laekna Ltd | Método de tratamento de câncer |
| JP7656589B2 (ja) | 2019-08-26 | 2025-04-03 | アルビナス・オペレーションズ・インコーポレイテッド | エストロゲン受容体分解物質としてのテトラヒドロナフタレン誘導体を用いて乳癌を治療する方法 |
| CN118767143A (zh) | 2019-12-12 | 2024-10-15 | 听治疗有限责任公司 | 用于预防和治疗听力损失的组合物和方法 |
| US12014835B2 (en) | 2020-02-19 | 2024-06-18 | Vanderbilt University | Methods for evaluating therapeutic benefit of combination therapies |
| JP2023519882A (ja) | 2020-03-27 | 2023-05-15 | ソム、イノベーション、バイオテック、ソシエダッド、アノニマ | シヌクレイノパチーの治療に有用な化合物 |
| CN111592531B (zh) * | 2020-06-23 | 2023-08-15 | 上海鲲博玖瑞医药科技发展有限公司 | 福瑞塞替的制备方法 |
| CN111620860B (zh) * | 2020-06-23 | 2023-02-03 | 济南健丰化工有限公司 | 一种福瑞塞替的制备方法 |
| WO2022069554A1 (de) | 2020-10-01 | 2022-04-07 | Bayer Aktiengesellschaft | Verfahren zur herstellung von 4-bromfuran-2-carboxylaten |
| WO2023174210A1 (en) | 2022-03-14 | 2023-09-21 | Laekna Limited | Combination treatment for cancer |
| AU2023246862A1 (en) | 2022-03-31 | 2024-10-31 | Astrazeneca Ab | Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer |
| AR129423A1 (es) | 2022-05-27 | 2024-08-21 | Viiv Healthcare Co | Compuestos útiles en la terapia contra el hiv |
| EP4604957A1 (en) | 2022-10-17 | 2025-08-27 | Astrazeneca AB | Combinations of a serd for the treatment of cancer |
| JP2025539034A (ja) | 2022-11-11 | 2025-12-03 | アストラゼネカ・アクチエボラーグ | 癌の治療のための併用療法 |
| WO2024249875A1 (en) | 2023-06-02 | 2024-12-05 | Arvinas Operations, Inc. | Combinations of estrogen receptor degraders and akt inhibitors |
| CN117486856A (zh) * | 2023-11-02 | 2024-02-02 | 上海毕得医药科技股份有限公司 | 一种4-溴-5-(三氟甲基)噻吩-2-羧酸甲酯的合成方法 |
Family Cites Families (178)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1030415A (zh) | 1987-02-20 | 1989-01-18 | 山之内制药株式会社 | 饱和的杂环碳酰胺衍生物和它的制备方法 |
| ES2005163A6 (es) | 1987-04-14 | 1989-03-01 | Lilly S A E | Un procedimiento para la produccion de derivados de tiofen-2-carboxamida. |
| US4999359A (en) | 1988-03-16 | 1991-03-12 | Dr. Lo Zambeletti S.P.A. | Heterocyclic ethylene diamine compounds and their pharmaceutical compositions and methods |
| DE3810848A1 (de) | 1988-03-30 | 1989-10-19 | Boehringer Ingelheim Kg | Neue 2,3,4-substituierte imidazole und 3,4,5-substituierte 1,2,4-triazole, ihre herstellung und verwendung |
| DE3927483A1 (de) | 1989-08-19 | 1991-02-21 | Boehringer Ingelheim Kg | Neue substituierte heterocyclische fuenfringe, ihre herstellung und verwendung |
| US5258357A (en) | 1989-10-07 | 1993-11-02 | Basf Aktiengesellschaft | Carboxamides, their preparation and their use as herbicides |
| DE3933573A1 (de) | 1989-10-07 | 1991-04-18 | Basf Ag | Carbonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als herbizide |
| US6645969B1 (en) | 1991-05-10 | 2003-11-11 | Aventis Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase |
| US5559235A (en) | 1991-10-29 | 1996-09-24 | Glaxo Wellcome Inc. | Water soluble camptothecin derivatives |
| GB9201755D0 (en) | 1992-01-28 | 1992-03-11 | British Bio Technology | Compounds |
| US5595872A (en) | 1992-03-06 | 1997-01-21 | Bristol-Myers Squibb Company | Nucleic acids encoding microsomal trigyceride transfer protein |
| US5342947A (en) | 1992-10-09 | 1994-08-30 | Glaxo Inc. | Preparation of water soluble camptothecin derivatives |
| US5786373A (en) | 1992-10-14 | 1998-07-28 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| ES2133416T3 (es) | 1992-10-23 | 1999-09-16 | Merck Sharp & Dohme | Ligandos de subtipos de receptores de dopamina. |
| FR2707295A1 (fr) | 1993-06-07 | 1995-01-13 | Rhone Poulenc Agrochimie | Fongicides pyrazoles substitués en position 3 par un hétérocycle. |
| EP0712397B1 (en) * | 1993-08-06 | 1999-04-21 | Smithkline Beecham Plc | Amide derivatives as 5ht1d receptor antagonists |
| US5739135A (en) | 1993-09-03 | 1998-04-14 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| US5681835A (en) | 1994-04-25 | 1997-10-28 | Glaxo Wellcome Inc. | Non-steroidal ligands for the estrogen receptor |
| US5491237A (en) | 1994-05-03 | 1996-02-13 | Glaxo Wellcome Inc. | Intermediates in pharmaceutical camptothecin preparation |
| US5668148A (en) * | 1995-04-20 | 1997-09-16 | Merck & Co., Inc. | Alpha1a adrenergic receptor antagonists |
| JP3964478B2 (ja) | 1995-06-30 | 2007-08-22 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬 |
| US5846990A (en) * | 1995-07-24 | 1998-12-08 | Bristol-Myers Squibb Co. | Substituted biphenyl isoxazole sulfonamides |
| CA2201477C (en) * | 1995-08-02 | 2005-05-03 | Javier Bartroli | New pyrimidone derivatives with antifungal activity |
| EP0783502A1 (en) | 1995-08-02 | 1997-07-16 | J. URIACH & CIA. S.A. | New carboxamides with antifungal activity |
| US6174887B1 (en) | 1995-08-22 | 2001-01-16 | Japan Tobacco Inc. | Amide compounds and use of the same |
| US5972980A (en) | 1995-10-05 | 1999-10-26 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| AU6966696A (en) | 1995-10-05 | 1997-04-28 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| US6001866A (en) | 1995-10-05 | 1999-12-14 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| US5942544A (en) | 1996-02-22 | 1999-08-24 | Dupont Pharmaceuticals Company | α-branched anilines, toluenes, and analogs thereof as factor Xa inhibitors |
| WO1997036890A1 (en) | 1996-04-03 | 1997-10-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| CA2249645A1 (en) | 1996-04-03 | 1997-10-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| EP0891357A1 (en) | 1996-04-03 | 1999-01-20 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| WO1997036875A1 (en) | 1996-04-03 | 1997-10-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| JP2000509371A (ja) | 1996-04-03 | 2000-07-25 | メルク エンド カンパニー インコーポレーテッド | ファルネシル―タンパク質トランスフェラーゼ阻害剤 |
| CA2249607A1 (en) | 1996-04-03 | 1997-10-09 | Neville J. Anthony | Inhibitors of farnesyl-protein transferase |
| WO1997036896A1 (en) | 1996-04-03 | 1997-10-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| EP0891356A1 (en) | 1996-04-03 | 1999-01-20 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| WO1997036585A1 (en) | 1996-04-03 | 1997-10-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| AUPO163896A0 (en) | 1996-08-14 | 1996-09-05 | Resmed Limited | Determination of respiratory airflow |
| WO1998037068A1 (en) | 1997-02-21 | 1998-08-27 | Bristol-Myers Squibb Company | Benzoic acid derivatives and related compounds as antiarrhythmic agents |
| US5998336A (en) | 1997-02-26 | 1999-12-07 | The Board Of Trustees Of The Leland Stanford Junior University | Ceramic/metal and A15/metal superconducting composite materials exploiting the superconducting proximity effect and method of making the same |
| EP0986551B1 (en) | 1997-05-30 | 2006-08-02 | Takeda Pharmaceutical Company Limited | Sulfonamide derivatives, their production and use |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| DE19744026A1 (de) | 1997-10-06 | 1999-04-08 | Hoechst Marion Roussel De Gmbh | Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln |
| AU751139B2 (en) | 1997-10-13 | 2002-08-08 | Astellas Pharma Inc. | Amide derivative |
| CN1294590A (zh) | 1997-12-12 | 2001-05-09 | 欧罗赛铁克股份有限公司 | 通过2－硫代黄嘌呤制备3－取代腺嘌呤的方法 |
| US6232320B1 (en) | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
| AUPP433398A0 (en) | 1998-06-25 | 1998-07-16 | Australian National University, The | Compounds and processes |
| US6192967B1 (en) | 1998-10-19 | 2001-02-27 | Sunny En Liung Huang | Collapsible auto shade |
| US6130333A (en) | 1998-11-27 | 2000-10-10 | Monsanto Company | Bicyclic imidazolyl derivatives as phosphodiesterase inhibitors, pharmaceutical compositions and method of use |
| GB9827882D0 (en) | 1998-12-17 | 1999-02-10 | Smithkline Beecham Plc | Novel compounds |
| DE19904397A1 (de) | 1999-02-04 | 2000-08-10 | Bayer Ag | Verwendung von Pyrazol-Carbonsäureamiden |
| DE19904396A1 (de) | 1999-02-04 | 2000-08-10 | Bayer Ag | Substituierte Pyrazolbenzylamin-Derivate |
| JP2000256358A (ja) | 1999-03-10 | 2000-09-19 | Yamanouchi Pharmaceut Co Ltd | ピラゾール誘導体 |
| WO2000061551A2 (de) | 1999-04-13 | 2000-10-19 | Basf Aktiengesellschaft | Pyrimidin-2-on derivate als integrinrezeptorliganden |
| WO2000071510A2 (en) | 1999-05-24 | 2000-11-30 | Cor Therapeutics, Inc. | INHIBITORS OF FACTOR Xa |
| AU5283900A (en) | 1999-05-24 | 2000-12-12 | Cor Therapeutics, Inc. | Inhibitors of factor xa |
| JP2001247569A (ja) | 1999-08-12 | 2001-09-11 | Japan Tobacco Inc | ピロリジン誘導体又はピペリジン誘導体及びその医薬用途 |
| US6632815B2 (en) * | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| EP1235807A1 (en) | 1999-11-24 | 2002-09-04 | Millennium Pharmaceuticals, Inc. | B-amino acid-, aspartic acid- and diaminopropionic-based inhibitors of factor xa |
| US6770666B2 (en) | 1999-12-27 | 2004-08-03 | Japan Tobacco Inc. | Fused-ring compounds and use thereof as drugs |
| IL145071A0 (en) | 1999-12-27 | 2002-06-30 | Japan Tobacco Inc | Fused ring compounds and pharmaceutical compositions containing the same |
| KR20010111298A (ko) * | 2000-02-05 | 2001-12-17 | 버텍스 파마슈티칼스 인코포레이티드 | Ｅｒｋ의 억제제로서 유용한 피라졸 조성물 |
| EP1196390A2 (en) | 2000-02-05 | 2002-04-17 | Vertex Pharmaceuticals Incorporated | Pyrazole compositions useful as inhibitors of erk |
| WO2001056557A2 (en) | 2000-02-05 | 2001-08-09 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of erk |
| WO2001064642A2 (en) | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| GB0011098D0 (en) | 2000-05-08 | 2000-06-28 | Black James Foundation | Pharmaceutical compositions comprising protpn pump inhibitors and gastrin/cholecystokinin receptor ligands |
| US6914069B2 (en) * | 2000-05-19 | 2005-07-05 | Applied Research Systems Ars Holding N.V. | Pharmaceutically active compounds and methods of use |
| US6589195B1 (en) * | 2000-05-26 | 2003-07-08 | Orthomerica Products, Inc. | Modular adjustable prophylactic hip orthosis and adduction/abduction joint |
| EP1296977A1 (en) | 2000-06-23 | 2003-04-02 | Bristol-Myers Squibb Pharma Company | Heteroaryl-phenyl substituted factor xa inhibitors |
| WO2002007823A2 (en) | 2000-07-24 | 2002-01-31 | Davide Riccardo Grassetti | Inhibition of mutagenic effects of carcinogens |
| GB0018758D0 (en) | 2000-07-31 | 2000-09-20 | Smithkline Beecham Plc | Novel use and compunds |
| JO2654B1 (en) * | 2000-09-04 | 2012-06-17 | شركة جانسين فارماسوتيكا ان. في | Multiple aryl caroxa amides are useful as lipid - lowering agents |
| ES2274005T3 (es) | 2001-01-26 | 2007-05-16 | Chugai Seiyaku Kabushiki Kaisha | Inhibidores de malonyl-coa decarboxilasa usados como moduladores metabolicos. |
| WO2002088097A1 (en) * | 2001-04-27 | 2002-11-07 | Vertex Pharmaceuticals Incorporated | Triazole-derived kinase inhibitors and uses thereof |
| DE10223912A1 (de) * | 2001-06-28 | 2003-01-16 | Merck Patent Gmbh | TN- und STN-Flüssigkristallanzeigen |
| US20030015823A1 (en) * | 2001-07-18 | 2003-01-23 | Hydranautics | Method for forming a thick section, thermoset, solid casting |
| CA2456192A1 (en) | 2001-08-03 | 2003-02-13 | Qing Tang | Pyrazole-derived kinase inhibitors and uses thereof |
| ATE491701T1 (de) | 2001-08-03 | 2011-01-15 | Vertex Pharma | Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung |
| WO2003018585A1 (en) | 2001-08-24 | 2003-03-06 | Pharmacia & Upjohn Company | Substituted-heteroaryl-7-aza[2.2.1]bicycloheptanes for the treatment of disease |
| WO2003026649A1 (en) | 2001-09-27 | 2003-04-03 | Applied Research Systems Ars Holding N.V. | Methods of increasing endogenous testosterone levels |
| US6794252B2 (en) * | 2001-09-28 | 2004-09-21 | Texas Instruments Incorporated | Method and system for forming dual work function gate electrodes in a semiconductor device |
| WO2003035619A1 (en) | 2001-10-25 | 2003-05-01 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| US6897208B2 (en) | 2001-10-26 | 2005-05-24 | Aventis Pharmaceuticals Inc. | Benzimidazoles |
| WO2003039529A1 (en) | 2001-11-07 | 2003-05-15 | 4Sc A.G. | Selective antibacterial agents |
| TW200306819A (en) | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
| ES2437391T3 (es) | 2002-02-06 | 2014-01-10 | Vertex Pharmaceuticals, Inc. | Compuestos de heteroarilo útiles como inhibidores de GSK-3 |
| US7335779B2 (en) | 2002-03-08 | 2008-02-26 | Quonova, Llc | Modulation of pathogenicity |
| GB0206860D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Compounds |
| GB0206861D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Medicaments |
| CA2480856A1 (en) | 2002-04-05 | 2003-10-23 | Merck & Co., Inc. | Substituted aryl amides |
| CA2483500A1 (en) | 2002-04-26 | 2003-11-06 | Pfizer Products Inc. | Pyrimidine-2, 4, 6-trione metallo-proteinase inhibitors |
| AU2003240546A1 (en) | 2002-06-05 | 2003-12-22 | Pharmacia And Upjohn Company | Methods for identifying ligands using competitive binding 1h nmr experiments |
| GB0216224D0 (en) | 2002-07-12 | 2002-08-21 | Glaxo Group Ltd | Compounds |
| CA2494114A1 (en) | 2002-08-02 | 2004-02-12 | Argenta Discovery Limited | Substituted thienyl-hydroxamic acids as histone deacetylase inhibitors |
| AU2003268064A1 (en) | 2002-08-09 | 2004-02-25 | Astrazeneca Ab | Oxadiazoles as modulators of metabotropic glutamate receptor-5 |
| US6649638B1 (en) | 2002-08-14 | 2003-11-18 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| AU2003265395A1 (en) | 2002-08-14 | 2004-03-03 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| AU2003268184A1 (en) | 2002-08-23 | 2004-03-11 | Chiron Corporation | Pyrrole based inhibitors of glycogen synthase kinase 3 |
| DE10239443A1 (de) | 2002-08-28 | 2004-03-11 | Boehringer Ingelheim International Gmbh | Blockiervorrichtung für ein Sperrspannwerk mit federbetätigtem Abtrieb |
| EP1398029A1 (en) | 2002-09-10 | 2004-03-17 | LION Bioscience AG | NR3B1 nuclear receptor binding 3-substituted pyrazole derivatives |
| US20060084682A1 (en) | 2002-12-13 | 2006-04-20 | Heerding Dirk A | Thrombopoietin mimetics |
| BR0317430A (pt) | 2002-12-20 | 2005-10-25 | Pharmacia Corp | Compostos inibidores de quinase-2 de proteìna ativada por quinase de proteìna ativada por mitógeno |
| CA2515235A1 (en) | 2003-02-10 | 2004-08-19 | Bayer Healthcare Ag | Bis(hetero)aryl carboxamide derivatives for use as pgi2 antagonists |
| WO2004072018A1 (ja) | 2003-02-12 | 2004-08-26 | Takeda Pharmaceutical Company Limited | アミン誘導体 |
| US7223788B2 (en) | 2003-02-14 | 2007-05-29 | Sanofi-Aventis Deutschland Gmbh | Substituted N-aryl heterocycles, process for their preparation and their use as medicaments |
| EP1599447A1 (en) | 2003-02-28 | 2005-11-30 | Galderma Research & Development, S.N.C. | Ligands that modulate lxr-type receptors |
| US7517887B2 (en) | 2003-04-09 | 2009-04-14 | General Atomics | Reversible inhibitors of S-adenosyl-L-homocysteine hydrolase and uses thereof |
| JP2006524255A (ja) | 2003-04-21 | 2006-10-26 | イーラン ファーマスーティカルズ、インコーポレイテッド | ベンズアミド２−ヒドロキシ−３−ジアミノアルカン |
| ATE482933T1 (de) | 2003-05-26 | 2010-10-15 | Takeda Pharmaceutical | Sulfopyrrolderivate |
| EP1638964B1 (en) | 2003-06-20 | 2011-07-27 | Galderma Research & Development | Novel compounds that modulate ppar-gamma type receptors, and use thereof in cosmetic or pharmaceutical compositions |
| DE10331305A1 (de) | 2003-07-10 | 2005-02-17 | Siemens Ag | Kommunikationssystem, Peer-to-Peer-Nachrichten-Filter-Rechner und Verfahren zum Verarbeiten einer Peer-to-Peer-Nachricht |
| FR2857666B1 (fr) | 2003-07-15 | 2005-08-26 | Oreal | Composition tinctoriale comprenant a titre de coupleur un derive du furane et nouveaux derives du furane |
| BRPI0412257A (pt) | 2003-07-23 | 2006-10-03 | Synta Pharmaceuticals Corp | compostos para inflamação e usos imuno-relacionados |
| WO2005019200A2 (en) | 2003-08-14 | 2005-03-03 | Icos Corporation | Aryl piperidine derivatives as vla-1 integrin antagonists and uses thereof |
| DE602004012578T2 (de) | 2003-08-15 | 2008-12-11 | Vertex Pharmaceuticals Inc., Cambridge | Als inhibitoren von c-met geeignete pyrrolzusammensetzungen |
| WO2005019182A1 (en) | 2003-08-20 | 2005-03-03 | Bayer Healthcare Ag | Pyrazolylmethylbenzamide derivatives as p2xt-receptor antagonists |
| US20070004771A1 (en) | 2003-10-06 | 2007-01-04 | Glaxo Group Limited | Preparation of 1,6,7-trisubstituted azabenzimidazoles as kinase inhibitors |
| JP2007507547A (ja) | 2003-10-06 | 2007-03-29 | グラクソ グループ リミテッド | キナーゼ阻害剤としての１，７−二置換アザベンゾイミダゾールの調製 |
| US20050171171A1 (en) | 2003-11-13 | 2005-08-04 | Ambit Biosciences Corporation | Amide derivatives as FLT-3 modulators |
| BRPI0416852A (pt) | 2003-11-21 | 2007-02-27 | Array Biopharma Inc | inibidores da quinase akt |
| US8652089B2 (en) | 2004-01-19 | 2014-02-18 | Arthrex, Inc. | System for distending body tissue cavities by continuous flow irrigation |
| EP1708697A4 (en) | 2004-01-30 | 2007-11-28 | Smithkline Beecham Corp | CHEMICAL COMPOUNDS |
| WO2005077373A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| WO2005077345A1 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Compounds for the treatment of gastro-esophageal reflux disease |
| US7521473B2 (en) | 2004-02-25 | 2009-04-21 | Wyeth | Inhibitors of protein tyrosine phosphatase 1B |
| JP2007531354A (ja) * | 2004-03-30 | 2007-11-01 | 松下電器産業株式会社 | コンテンツ中継サーバ、コンテンツ中継システム、コンテンツ中継方法及びそのプログラム |
| CA2561977A1 (en) * | 2004-03-30 | 2005-10-13 | Chiron Corporation | Substituted thiophene derivatives as anti-cancer agents |
| US7973061B2 (en) | 2004-03-31 | 2011-07-05 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
| JP2005336172A (ja) | 2004-04-26 | 2005-12-08 | Japan Tobacco Inc | 腎虚血再灌流障害治療又は予防薬 |
| TW200600492A (en) * | 2004-05-18 | 2006-01-01 | Achillion Pharmaceuticals Inc | Substituted aryl acylthioureas and related compounds; inhibitors of viral replication |
| CA2568742A1 (en) | 2004-05-29 | 2005-12-08 | 7Tm Pharma A/S | Substituted thiazoleacetic as crth2 ligands |
| WO2006009876A2 (en) | 2004-06-17 | 2006-01-26 | Cengent Therapeutics, Inc. | Trisubstituted nitrogen modulators of tyrosine phosphatases |
| AU2005260689B2 (en) * | 2004-06-30 | 2012-05-10 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of protein kinases |
| US7671077B2 (en) * | 2004-07-19 | 2010-03-02 | Leu-Fen Hou Lin | Neuroprotective small organic molecules, compositions and uses related thereto |
| US20060019967A1 (en) | 2004-07-21 | 2006-01-26 | Su-Ying Wu | SARS CoV main protease inhibitors |
| US20060019968A1 (en) * | 2004-07-24 | 2006-01-26 | Laboratorios Dr. Esteve S.A. | Use of compounds active on the sigma receptor for the treatment of neuropathic pain |
| US7269099B2 (en) | 2004-07-30 | 2007-09-11 | Bolt Technology Corporation | Air gun |
| JP2006066488A (ja) * | 2004-08-25 | 2006-03-09 | Mitsubishi Electric Corp | 半導体受光素子およびその製造方法 |
| US7365385B2 (en) * | 2004-08-30 | 2008-04-29 | Micron Technology, Inc. | DRAM layout with vertical FETs and method of formation |
| US20060043513A1 (en) * | 2004-09-02 | 2006-03-02 | Deok-Hoon Kim | Method of making camera module in wafer level |
| TW200616969A (en) | 2004-09-17 | 2006-06-01 | Tanabe Seiyaku Co | Imidazole compound |
| US20060062453A1 (en) * | 2004-09-23 | 2006-03-23 | Sharp Laboratories Of America, Inc. | Color highlighting document image processing |
| WO2006043518A1 (ja) | 2004-10-18 | 2006-04-27 | Santen Pharmaceutical Co., Ltd. | 神経疾患治療剤 |
| JP2006120339A (ja) | 2004-10-19 | 2006-05-11 | Matsushita Electric Ind Co Ltd | 高周波加熱電源装置 |
| TW200619843A (en) | 2004-10-20 | 2006-06-16 | Sumitomo Bakelite Co | Semiconductor wafer and semiconductor device |
| DE102004051277A1 (de) | 2004-10-21 | 2006-04-27 | Merck Patent Gmbh | Heterocyclische Carbonylverbindungen |
| DE102004054666A1 (de) | 2004-11-12 | 2006-05-18 | Bayer Cropscience Gmbh | Substituierte Pyrazol-3-carboxamide, Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| CN101048383A (zh) * | 2004-11-23 | 2007-10-03 | 惠氏公司 | 促性腺激素释放激素受体拮抗剂 |
| MX2007003331A (es) | 2004-11-30 | 2007-06-05 | Neurosearch As | Nuevos derivados de arilo diazabiciclico. |
| SE527990C2 (sv) | 2004-12-06 | 2006-08-01 | Mora Of Sweden Ab | Isborr |
| EP1843763A2 (en) | 2005-02-03 | 2007-10-17 | Irm, Llc | Compounds and compositions as ppar modulators |
| JP2006232707A (ja) | 2005-02-23 | 2006-09-07 | Japan Tobacco Inc | 癌転移抑制剤 |
| US20080207760A1 (en) | 2005-04-11 | 2008-08-28 | Achillion Pharmaceuticals, Inc. | Pharmaceutical Compositions For and Methods of Inhibiting Hcv |
| US20060252807A1 (en) | 2005-04-22 | 2006-11-09 | Kalypsys, Inc. | Novel ortho-terphenyl inhibitors of p38 kinase and methods of treating inflammatory disorders |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| JP2008543919A (ja) | 2005-06-21 | 2008-12-04 | アステックス・セラピューティクス・リミテッド | 医薬化合物 |
| US20060288588A1 (en) | 2005-06-22 | 2006-12-28 | Frank Morabito | Garden tool |
| US8541461B2 (en) * | 2005-06-23 | 2013-09-24 | Astex Therapeutics Limited | Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators |
| MX2007016144A (es) | 2005-06-24 | 2008-03-06 | Genelabs Tech Inc | Derivados de heteroaril para tratar virus. |
| WO2006136637A2 (es) * | 2005-06-24 | 2006-12-28 | Eloy Antonio Martinez Albal | Implante dental de corona rotatoria |
| JP5244589B2 (ja) | 2005-06-27 | 2013-07-24 | エグゼリクシス パテント カンパニー エルエルシー | イミダゾールに基づくｌｘｒモジュレーター |
| CN100494167C (zh) | 2005-08-02 | 2009-06-03 | 天津大学 | 抗乙肝病毒的叔胺氧化物及制备方法和制备药物的应用 |
| GB0518237D0 (en) | 2005-09-07 | 2005-10-19 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| WO2007052843A1 (ja) | 2005-11-04 | 2007-05-10 | Takeda Pharmaceutical Company Limited | 複素環アミド化合物およびその用途 |
| US7838676B2 (en) | 2005-11-21 | 2010-11-23 | Amgen Inc. | Beta-secretase modulators and methods of use |
| KR20080080173A (ko) | 2005-12-14 | 2008-09-02 | 브리스톨-마이어스 스큅 컴퍼니 | 세린 프로테아제 억제제로서 유용한 6-원 헤테로사이클 |
| WO2007076423A2 (en) | 2005-12-22 | 2007-07-05 | Smithkline Beecham Corporation | INHIBITORS OF Akt ACTIVITY |
| ES2408318T3 (es) | 2005-12-23 | 2013-06-20 | Glaxosmithkline Llc | Inhibidores de azaindol de las cinasas Aurora |
| AR056882A1 (es) | 2006-02-01 | 2007-10-31 | Bayer Cropscience Sa | Derivados del fungicida n- cicloalquil- bencil- amida |
| NZ570847A (en) | 2006-02-28 | 2011-10-28 | Helicon Therapeutics Inc | Therapeutic compounds |
| JP2007277230A (ja) | 2006-03-15 | 2007-10-25 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| EP2099770B1 (en) | 2006-12-21 | 2015-06-10 | Sloan-Kettering Institute for Cancer Research | Pyridazinones and furan-containing compounds |
| KR20090086115A (ko) | 2006-12-22 | 2009-08-10 | 엔싸이시브 파마슈티칼즈 인코퍼레이티드 | Ｃ３ａ 수용체의 조정제 및 이의 사용 방법 |
| US8420690B2 (en) | 2007-02-07 | 2013-04-16 | Glaxosmithkline Llc | Inhibitors of Akt activity |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| WO2008121685A1 (en) | 2007-03-28 | 2008-10-09 | Smithkline Beecham Corporation | Methods of use for inhibitors of akt activity |
| US8338434B2 (en) | 2007-03-29 | 2012-12-25 | Glaxosmithkline Llc | Inhibitors of Akt activity |
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