JP2018529633A5 - - Google Patents
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- JP2018529633A5 JP2018529633A5 JP2018500582A JP2018500582A JP2018529633A5 JP 2018529633 A5 JP2018529633 A5 JP 2018529633A5 JP 2018500582 A JP2018500582 A JP 2018500582A JP 2018500582 A JP2018500582 A JP 2018500582A JP 2018529633 A5 JP2018529633 A5 JP 2018529633A5
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- 150000001875 compounds Chemical class 0.000 claims 53
- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 claims 27
- 125000000649 benzylidene group Chemical group [H]C(=[*])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 27
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 claims 27
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 27
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 27
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 238000000634 powder X-ray diffraction Methods 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 239000003153 chemical reaction reagent Substances 0.000 claims 6
- 239000013078 crystal Substances 0.000 claims 5
- 238000004519 manufacturing process Methods 0.000 claims 5
- XYFCBTPGUUZFHI-UHFFFAOYSA-N Phosphine Chemical compound P XYFCBTPGUUZFHI-UHFFFAOYSA-N 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 239000002585 base Substances 0.000 claims 3
- 239000003638 chemical reducing agent Substances 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 150000007529 inorganic bases Chemical class 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- USVVENVKYJZFMW-ONEGZZNKSA-N (e)-carboxyiminocarbamic acid Chemical compound OC(=O)\N=N\C(O)=O USVVENVKYJZFMW-ONEGZZNKSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 229910000073 phosphorus hydride Inorganic materials 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- CESUXLKAADQNTB-SSDOTTSWSA-N 2-methylpropane-2-sulfinamide Chemical compound CC(C)(C)[S@](N)=O CESUXLKAADQNTB-SSDOTTSWSA-N 0.000 claims 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- 206010000830 Acute leukaemia Diseases 0.000 claims 1
- 206010061424 Anal cancer Diseases 0.000 claims 1
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims 1
- 208000007860 Anus Neoplasms Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 206010006143 Brain stem glioma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010007953 Central nervous system lymphoma Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 201000001342 Fallopian tube cancer Diseases 0.000 claims 1
- 208000013452 Fallopian tube neoplasm Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010061252 Intraocular melanoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000032271 Malignant tumor of penis Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000000821 Parathyroid Neoplasms Diseases 0.000 claims 1
- 206010061336 Pelvic neoplasm Diseases 0.000 claims 1
- 208000002471 Penile Neoplasms Diseases 0.000 claims 1
- 206010034299 Penile cancer Diseases 0.000 claims 1
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 1
- 201000005746 Pituitary adenoma Diseases 0.000 claims 1
- 206010061538 Pituitary tumour benign Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000023915 Ureteral Neoplasms Diseases 0.000 claims 1
- 206010046392 Ureteric cancer Diseases 0.000 claims 1
- 206010046431 Urethral cancer Diseases 0.000 claims 1
- 206010046458 Urethral neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 201000005969 Uveal melanoma Diseases 0.000 claims 1
- 206010047741 Vulval cancer Diseases 0.000 claims 1
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 201000005188 adrenal gland cancer Diseases 0.000 claims 1
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 1
- 201000011165 anus cancer Diseases 0.000 claims 1
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000024207 chronic leukemia Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000030381 cutaneous melanoma Diseases 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000029559 malignant endocrine neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 208000026045 malignant tumor of parathyroid gland Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 210000000651 myofibroblast Anatomy 0.000 claims 1
- 201000002575 ocular melanoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical compound [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 claims 1
- 208000021310 pituitary gland adenoma Diseases 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 208000016800 primary central nervous system lymphoma Diseases 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000003708 skin melanoma Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 206010046885 vaginal cancer Diseases 0.000 claims 1
- 208000013139 vaginal neoplasm Diseases 0.000 claims 1
- 201000005102 vulva cancer Diseases 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021069649A JP7212713B2 (ja) | 2015-07-06 | 2021-04-16 | ジアリール大環状多形 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562188846P | 2015-07-06 | 2015-07-06 | |
| US62/188,846 | 2015-07-06 | ||
| US201562218672P | 2015-09-15 | 2015-09-15 | |
| US62/218,672 | 2015-09-15 | ||
| PCT/US2016/040972 WO2017007759A1 (en) | 2015-07-06 | 2016-07-05 | Diaryl macrocycle polymorph |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021069649A Division JP7212713B2 (ja) | 2015-07-06 | 2021-04-16 | ジアリール大環状多形 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018529633A JP2018529633A (ja) | 2018-10-11 |
| JP2018529633A5 true JP2018529633A5 (enExample) | 2019-08-15 |
| JP6917974B2 JP6917974B2 (ja) | 2021-08-11 |
Family
ID=57685592
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018500582A Active JP6917974B2 (ja) | 2015-07-06 | 2016-07-05 | ジアリール大環状多形 |
| JP2021069649A Active JP7212713B2 (ja) | 2015-07-06 | 2021-04-16 | ジアリール大環状多形 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021069649A Active JP7212713B2 (ja) | 2015-07-06 | 2021-04-16 | ジアリール大環状多形 |
Country Status (24)
| Country | Link |
|---|---|
| US (5) | US10294242B2 (enExample) |
| EP (2) | EP3319969B1 (enExample) |
| JP (2) | JP6917974B2 (enExample) |
| KR (1) | KR102623734B1 (enExample) |
| CN (2) | CN113354653B (enExample) |
| AU (1) | AU2016289454B2 (enExample) |
| BR (1) | BR112018000297A2 (enExample) |
| CA (1) | CA2990020C (enExample) |
| DK (1) | DK3319969T3 (enExample) |
| ES (1) | ES2979111T3 (enExample) |
| FI (1) | FI3319969T3 (enExample) |
| HR (1) | HRP20240780T1 (enExample) |
| HU (1) | HUE067352T2 (enExample) |
| IL (2) | IL256443B (enExample) |
| LT (1) | LT3319969T (enExample) |
| MX (2) | MX386680B (enExample) |
| PL (1) | PL3319969T3 (enExample) |
| PT (1) | PT3319969T (enExample) |
| RS (1) | RS65593B1 (enExample) |
| RU (1) | RU2765181C2 (enExample) |
| SI (1) | SI3319969T1 (enExample) |
| SM (1) | SMT202400213T1 (enExample) |
| WO (1) | WO2017007759A1 (enExample) |
| ZA (1) | ZA201708436B (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015112806A2 (en) | 2014-01-24 | 2015-07-30 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| RU2732405C2 (ru) | 2015-07-02 | 2020-09-16 | Тёрнинг Поинт Терапьютикс, Инк. | Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ |
| BR112018000297A2 (pt) | 2015-07-06 | 2018-09-04 | Tp Therapeutics Inc | polimorfo de macrociclo de diarila |
| WO2017015367A1 (en) * | 2015-07-21 | 2017-01-26 | Tp Therapeutics, Inc. | Chiral diaryl macrocycles and uses thereof |
| AU2017302019A1 (en) | 2016-07-28 | 2019-02-07 | Turning Point Therapeutics, Inc. | Macrocycle kinase inhibitors |
| TWI808958B (zh) * | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| CN107586796B (zh) * | 2017-07-20 | 2021-08-06 | 暨明医药科技（苏州）有限公司 | (r)-2-(1-氨基乙基)-4-氟苯酚的合成方法 |
| PT3658148T (pt) | 2017-07-28 | 2024-08-26 | Turning Point Therapeutics Inc | Compostos macrocíclicos e utilizações dos mesmos |
| RS63787B1 (sr) | 2017-12-19 | 2022-12-30 | Turning Point Therapeutics Inc | Makrociklična jedinjenja za lečenje bolesti |
| CN110386944B (zh) * | 2018-04-16 | 2021-10-29 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白激酶活性的二(杂)芳基大环化合物 |
| RS66346B1 (sr) | 2018-10-22 | 2025-01-31 | Alumis Inc | Inhibitori tyk2 i njihova upotreba |
| US12410191B2 (en) | 2019-05-21 | 2025-09-09 | Zhejiang Hisun Pharmaceutical Co., Ltd. | Macrolide derivatives, preparation method and application thereof |
| WO2020257169A1 (en) * | 2019-06-19 | 2020-12-24 | Turning Point Therapeutics, Inc. | Polymorphs of a macrocyclic kinase inhibitor |
| KR20220134522A (ko) * | 2019-11-27 | 2022-10-05 | 터닝 포인트 테라퓨틱스, 인크. | 디아릴 매크로시클릭 화합물을 수반하는 병용 요법 |
| WO2021108682A1 (en) | 2019-11-27 | 2021-06-03 | Turning Point Therapeutics, Inc. | Combination therapy involving diaryl macrocyclic compounds |
| US20250262216A1 (en) * | 2020-03-02 | 2025-08-21 | Turning Point Therapeutics, Inc. | Therapeutic uses of macrocyclic compounds |
| CN113620974B (zh) * | 2020-05-08 | 2023-01-31 | 山东轩竹医药科技有限公司 | 大环类酪氨酸激酶抑制剂的晶型及其制备方法 |
| CN112174982A (zh) * | 2020-09-10 | 2021-01-05 | 上海希迈医药科技有限公司 | 一种洛普替尼晶型及其制备方法 |
| IL301385A (en) | 2020-09-16 | 2023-05-01 | Alumis Inc | TYK2 inhibitors and their use |
| WO2025217347A2 (en) | 2024-04-11 | 2025-10-16 | Bristol-Myers Squibb Company | Process of preparing repotrectinib |
Family Cites Families (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4838925A (en) | 1986-04-25 | 1989-06-13 | E. I. Du Pont De Nemours And Company | Heterocyclic acyl sulfonamides |
| ES2021105B3 (es) | 1987-03-07 | 1991-10-16 | Bayer Ag | Procedimiento para la obtencion de 5-amino-4,6-dihalogeno piridinas. |
| ES2149869T3 (es) | 1993-03-25 | 2000-11-16 | Upjohn Co | Derivados de indol sustituidos por formil o ciano con actividad dopominergica. |
| KR100340159B1 (ko) | 1993-12-07 | 2002-11-23 | 일라이 릴리 앤드 캄파니 | 단백질키나제c억제제 |
| GB9403639D0 (en) * | 1994-02-25 | 1994-04-13 | Boots Co Plc | Therapeutic agents |
| FR2746309B1 (fr) | 1996-03-22 | 1998-04-17 | Oreal | Composition de teinture des fibres keratiniques contenant des pyrazolopyrimidineoxo ; leur utilisation pour la teinture comme coupleurs, procedes de teinture |
| RS49779B (sr) | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
| FR2793791B1 (fr) | 1999-05-19 | 2002-01-25 | Univ Paris 7 Denis Diderot | Nouveaux composes inhibiteurs specifiques de phospholipases a2 |
| WO2002010169A1 (en) | 2000-07-31 | 2002-02-07 | F. Hoffmann-La Roche Ag | Piperazine derivatives |
| RU2275373C2 (ru) | 2000-12-08 | 2006-04-27 | Орто-Макнейл Фармасьютикал, Инк. | Макрогетероциклические соединения |
| JP2004532834A (ja) | 2001-03-23 | 2004-10-28 | イーライ・リリー・アンド・カンパニー | ヒスタミンｈ３受容体アンタゴニストである非イミダゾール系アリールアルキルアミン化合物、その製造および治療的使用 |
| AU2002322802A1 (en) * | 2001-07-27 | 2003-02-17 | Merck And Co., Inc. | Thrombin inhibitors |
| EP1402888A1 (en) | 2002-09-18 | 2004-03-31 | Jerini AG | The use of substituted carbocyclic compounds as rotamases inhibitors |
| US8005919B2 (en) | 2002-11-18 | 2011-08-23 | Aol Inc. | Host-based intelligent results related to a character stream |
| US7550470B2 (en) | 2002-12-11 | 2009-06-23 | Merck & Co. Inc. | Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors |
| CN101332303B (zh) * | 2005-01-10 | 2012-09-26 | 艾尼纳制药公司 | 用于治疗糖尿病和其相关病状以及用于治疗通过增加血液glp-1水平而改善的病状的组合疗法 |
| US8960547B2 (en) | 2007-09-19 | 2015-02-24 | E-Seek, Inc. | Document scanner with instant retrieval process |
| US8270176B2 (en) | 2008-08-08 | 2012-09-18 | Stats Chippac Ltd. | Exposed interconnect for a package on package system |
| TWM352384U (en) | 2008-08-22 | 2009-03-11 | Luff Technology Co Ltd | Wireless detection device for club and system thereof |
| ES2668834T3 (es) * | 2008-09-08 | 2018-05-22 | Merck Serono Sa | Pirimidinas macrociclicas como inhibidores de proteína quinasas |
| SI2350075T1 (sl) | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| CN102264736B (zh) | 2008-10-22 | 2013-08-14 | 阵列生物制药公司 | 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物 |
| BRPI0914404A2 (pt) | 2008-10-31 | 2019-03-06 | Genentech Inc | "compostos, composição farmacêutica e método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak quinase em um paciente" |
| WO2010063487A1 (en) | 2008-12-05 | 2010-06-10 | Merz Pharma Gmbh & Co. Kgaa | Pyrazolopyrimidines, a process for their preparation and their use as medicine |
| WO2010086040A1 (en) | 2009-01-29 | 2010-08-05 | Biomarin Iga, Ltd. | Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| WO2011045330A1 (en) | 2009-10-13 | 2011-04-21 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| WO2011071725A1 (en) | 2009-12-07 | 2011-06-16 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core |
| US9150577B2 (en) | 2009-12-07 | 2015-10-06 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds containing an indole core |
| SA111320200B1 (ar) | 2010-02-17 | 2014-02-16 | ديبيوفارم اس ايه | مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة |
| BR122019024201B1 (pt) * | 2010-05-20 | 2021-08-03 | Array Biopharma Inc | Composto macrocíclico como inibidores de trk quinase, seu uso, e composição farmacêutica |
| GB2482674B (en) | 2010-08-09 | 2012-08-22 | Rolls Royce Plc | An aerofoil, an aerofoil sub-assembly and a method of making the same |
| UY33597A (es) | 2010-09-09 | 2012-04-30 | Irm Llc | Compuestos y composiciones como inhibidores de la trk |
| WO2012034095A1 (en) | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
| WO2012075393A2 (en) | 2010-12-02 | 2012-06-07 | President And Fellows Of Harvard College | Activators of proteasomal degradation and uses thereof |
| EP2508607A1 (en) | 2011-04-07 | 2012-10-10 | Helmholtz-Zentrum für Infektionsforschung GmbH | Medicament for liver regeneration and for treatment of liver failure |
| EP2541470B1 (en) | 2011-06-29 | 2017-10-04 | Denso Wave Incorporated | Information code and information code reader |
| WO2013001310A1 (en) | 2011-06-30 | 2013-01-03 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Macrocyclic compounds and their use as cdk8 inhibitors |
| MX2014001945A (es) * | 2011-08-19 | 2014-03-27 | Merck Sharp & Dohme | Procedimiento e intermedios para la preparacion de macrolactamas. |
| WO2013045702A2 (en) | 2011-09-29 | 2013-04-04 | L'oreal | Dye composition comprising a non-glycosyl iridoid compound and a specific nucleophile or an amino or thio polymer, dyeing process, and device therefor |
| WO2013045701A2 (en) | 2011-09-29 | 2013-04-04 | L'oreal | Dyeing process using a composition comprising a glycosyl iridoid compound and a nucleophile or an amino or thio polymer, composition and devices therefor |
| MX347765B (es) | 2011-09-30 | 2017-05-12 | Oncodesign Sa | Inhibidores macrociclicos de la quinasa flt3. |
| KR20140077963A (ko) | 2011-10-20 | 2014-06-24 | 글락소스미스클라인 엘엘씨 | 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체 |
| CA2863892C (en) | 2012-03-06 | 2016-08-30 | Pfizer Inc. | Macrocyclic derivatives for the treatment of proliferative diseases |
| DK2834243T3 (en) | 2012-03-09 | 2018-07-23 | Lexicon Pharmaceuticals Inc | Pyrazole [1,5-a] pyrimidine-based compounds, compositions comprising them and methods for their use |
| RU2014140739A (ru) | 2012-03-09 | 2016-04-27 | Лексикон Фармасьютикалз, Инк. | Соединения на основе имидазо[1, 2-b]пиридазина, композиции таких соединений и способы их применения |
| GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| EP2951174B1 (en) | 2013-01-30 | 2017-04-26 | Bayer Pharma Aktiengesellschaft | Amino-substituted isothiazoles |
| CN105358534A (zh) | 2013-04-23 | 2016-02-24 | 斯洛文尼亚莱柯制药股份有限公司 | 8-氯-1-甲基-苯并[d]吖庚因的新合成方法、新的中间体及其生产方法 |
| JPWO2015012328A1 (ja) | 2013-07-24 | 2017-03-02 | 武田薬品工業株式会社 | 複素環化合物 |
| US20150112816A1 (en) * | 2013-10-21 | 2015-04-23 | Disney Enterprises, Inc. | Systems and methods for providing a graphical user interface for providing brand integration within online content, managing brand integration within online content, and/or managing compensation associated with online content |
| WO2015073267A1 (en) | 2013-11-15 | 2015-05-21 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| WO2015112806A2 (en) | 2014-01-24 | 2015-07-30 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| BR202014004079U2 (pt) | 2014-02-21 | 2015-10-27 | Mix For You Ltda | higienizador íntimo |
| WO2016070241A1 (en) | 2014-11-03 | 2016-05-12 | Ctxt Pty Ltd | Triazine compounds, compositions and synthesis |
| HUE067779T2 (hu) | 2014-12-15 | 2024-11-28 | Cmg Pharmaceutical Co Ltd | Kondenzált gyûrûs heteroaril vegyületek és azok felhasználása TRK inhibitorokként |
| EP3259264B1 (en) | 2015-02-20 | 2022-07-27 | Rigel Pharmaceuticals, Inc. | Gdf-8 inhibitors |
| JP6575516B2 (ja) | 2015-03-09 | 2019-09-18 | 住友ゴム工業株式会社 | タイヤ |
| US10155765B2 (en) | 2015-03-12 | 2018-12-18 | Merck Sharp & Dohme Corp. | Carboxamide inhibitors of IRAK4 activity |
| US10329294B2 (en) | 2015-03-12 | 2019-06-25 | Merck Sharp & Dohme Corp. | Pyrazolopyrimidine inhibitors of IRAK4 activity |
| JP2018520992A (ja) | 2015-05-05 | 2018-08-02 | バイエル ファーマ アクチエンゲゼルシャフト | アミドで置換されているシクロヘキサン誘導体 |
| RU2732405C2 (ru) | 2015-07-02 | 2020-09-16 | Тёрнинг Поинт Терапьютикс, Инк. | Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ |
| US9524416B1 (en) | 2015-07-03 | 2016-12-20 | Fingerprint Cards Ab | Fingerprint sensing device comprising three-dimensional pattern |
| BR112018000297A2 (pt) | 2015-07-06 | 2018-09-04 | Tp Therapeutics Inc | polimorfo de macrociclo de diarila |
| US10239565B2 (en) | 2015-07-17 | 2019-03-26 | John Michael Baker | Pickup truck tailgate lifting apparatus |
| WO2017015367A1 (en) | 2015-07-21 | 2017-01-26 | Tp Therapeutics, Inc. | Chiral diaryl macrocycles and uses thereof |
| EP3368039A1 (en) | 2015-10-26 | 2018-09-05 | The Regents of The University of Colorado, A Body Corporate | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| JP6580495B2 (ja) | 2016-02-02 | 2019-09-25 | 三菱重工業株式会社 | 保持治具 |
| JP7086395B2 (ja) | 2016-03-04 | 2022-06-20 | ヴァンダービルト ユニバーシティー | 置換インドールＭｃｌ－１阻害剤 |
| US10632076B2 (en) | 2016-11-18 | 2020-04-28 | Fertin Pharma A/S | Tablet comprising separate binder and erythritol |
| WO2018112027A1 (en) | 2016-12-14 | 2018-06-21 | Development Center For Biotechnology | Antibody-drug conjugates and uses thereof |
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