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 (cg-RX-API-DMAC7.html) | 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)
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| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
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| US20100048914A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal Cyp17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
| AU2009323766B2 (en) | 2008-12-02 | 2016-10-06 | Wave Life Sciences Ltd. | Method for the synthesis of phosphorus atom modified nucleic acids |
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| 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 |
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| RU2639876C2 (ru) | 2010-03-30 | 2017-12-25 | Версеон Корпорейшн | Мультизамещенные ароматические соединения в качестве ингибиторов тромбина |
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| WO2011150044A1 (en) * | 2010-05-26 | 2011-12-01 | Glaxosmithkline Llc | Combination |
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| WO2012021611A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
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| EP2620428B1 (en) | 2010-09-24 | 2019-05-22 | Wave Life Sciences Ltd. | Asymmetric auxiliary group |
| EP2627181A4 (en) | 2010-10-13 | 2014-03-19 | Millennium Pharm Inc | HETEROARYLE AND USES THEREOF |
| 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 |
| BR112013017722A2 (pt) | 2011-01-11 | 2016-07-12 | Glaxosmithkline Llc | combinação |
| US20120184542A1 (en) | 2011-01-19 | 2012-07-19 | Kevin Anderson | Pyrido pyrimidines |
| US20120184562A1 (en) | 2011-01-19 | 2012-07-19 | Kin-Chun Luk | 1,6- and 1,8-naphthyridines |
| 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 |
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| WO2012177925A1 (en) | 2011-06-21 | 2012-12-27 | The Board Institute, Inc. | Akt inhibitors for treating cancer expressing a magi3 - akt3 fusion gene |
| US9605019B2 (en) | 2011-07-19 | 2017-03-28 | Wave Life Sciences Ltd. | Methods for the synthesis of functionalized nucleic acids |
| EP2793879A4 (en) * | 2011-12-23 | 2015-07-01 | Millennium Pharm Inc | HETEROARYLE AND USES THEREOF |
| WO2013160222A1 (en) * | 2012-04-24 | 2013-10-31 | Glaxosmithkline Intellectual Property (No. 2) Limited | Treatment method for steroid responsive dermatoses |
| JP6246121B2 (ja) | 2012-07-13 | 2017-12-13 | 株式会社新日本科学 | キラル核酸アジュバント |
| JP6268157B2 (ja) | 2012-07-13 | 2018-01-24 | 株式会社Ｗａｖｅ Ｌｉｆｅ Ｓｃｉｅｎｃｅｓ Ｊａｐａｎ | 不斉補助基 |
| SG10201912895PA (en) | 2012-07-13 | 2020-02-27 | Wave Life Sciences Ltd | Chiral control |
| WO2014049488A1 (en) | 2012-09-28 | 2014-04-03 | Pfizer Inc. | Benzamide and heterobenzamide compounds |
| ES2628365T3 (es) | 2012-10-16 | 2017-08-02 | Janssen Pharmaceutica N.V. | Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T |
| BR112015008515A2 (pt) | 2012-10-16 | 2017-07-04 | Janssen Pharmaceutica Nv | moduladores de ror t de quinolinila ligada à heteroarila |
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| KR20150103735A (ko) | 2013-01-09 | 2015-09-11 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | 조합물 |
| 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 |
| SG11201507093WA (en) | 2013-03-14 | 2015-10-29 | Univ Maryland Baltimore Office Of Technology Transfer | Androgen receptor down-regulating agents and uses thereof |
| BR112015022340A2 (pt) | 2013-03-15 | 2017-07-18 | Verseon Corp | método para tratamento ou prevenção de uma doença ou distúrbio relacionado à calicreína em um sujeito, composto, e, composição farmacêutica |
| JP6479749B2 (ja) * | 2013-03-15 | 2019-03-06 | ヴァーセオン コーポレイション | トロンビン阻害剤としてのハロゲノピラゾール |
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| KR101797415B1 (ko) * | 2013-10-01 | 2017-11-13 | 노파르티스 아게 | 암의 치료를 위한 아푸레세르팁과 조합된 엔잘루타미드 |
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| US9221804B2 (en) | 2013-10-15 | 2015-12-29 | Janssen Pharmaceutica Nv | Secondary alcohol quinolinyl modulators of RORγt |
| CA2926313A1 (en) | 2013-10-15 | 2015-04-23 | Kristi A. Leonard | Secondary alcohol quinolinyl modulators of roryt |
| US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
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| US9328095B2 (en) | 2013-10-15 | 2016-05-03 | Janssen Pharmaceutica Nv | Heteroaryl linked quinolinyl modulators of RORgammat |
| WO2015057626A1 (en) | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | QUINOLINYL MODULATORS OF RORyT |
| 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 |
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| EA032469B1 (ru) | 2013-12-24 | 2019-05-31 | Бристол-Маерс Сквибб Компани | Новые трициклические соединения в качестве противораковых средств |
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