JP2017510643A5 - - Google Patents
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- Publication number
- JP2017510643A5 JP2017510643A5 JP2017502934A JP2017502934A JP2017510643A5 JP 2017510643 A5 JP2017510643 A5 JP 2017510643A5 JP 2017502934 A JP2017502934 A JP 2017502934A JP 2017502934 A JP2017502934 A JP 2017502934A JP 2017510643 A5 JP2017510643 A5 JP 2017510643A5
- Authority
- JP
- Japan
- Prior art keywords
- cycloalkyl
- membered
- independently
- alkyl
- membered heteroaryl
- 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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- 125000000623 heterocyclic group Chemical group 0.000 claims 24
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052799 carbon Inorganic materials 0.000 claims 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 201000010099 disease Diseases 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 230000001404 mediated effect Effects 0.000 claims 11
- 102000001253 Protein Kinase Human genes 0.000 claims 10
- 229910052757 nitrogen Inorganic materials 0.000 claims 10
- 108060006633 protein kinase Proteins 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 206010052779 Transplant rejections Diseases 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 7
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 6
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 4
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 4
- 102000042838 JAK family Human genes 0.000 claims 4
- -1 pyrazolopyridinyl Chemical group 0.000 claims 4
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 4
- 125000004641 (C1-C12) haloalkyl group Chemical group 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 3
- 208000026935 allergic disease Diseases 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 125000004642 (C1-C12) alkoxy group Chemical group 0.000 claims 2
- MSYGAHOHLUJIKV-UHFFFAOYSA-N 3,5-dimethyl-1-(3-nitrophenyl)-1h-pyrazole-4-carboxylic acid ethyl ester Chemical compound CC1=C(C(=O)OCC)C(C)=NN1C1=CC=CC([N+]([O-])=O)=C1 MSYGAHOHLUJIKV-UHFFFAOYSA-N 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- 208000004262 Food Hypersensitivity Diseases 0.000 claims 2
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 2
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 2
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 2
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 2
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 2
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 102000011017 Type 4 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 claims 2
- 108010037584 Type 4 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 claims 2
- 208000024780 Urticaria Diseases 0.000 claims 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 2
- 208000028004 allergic respiratory disease Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 239000005441 aurora Substances 0.000 claims 2
- 150000001602 bicycloalkyls Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 201000001981 dermatomyositis Diseases 0.000 claims 2
- 235000020932 food allergy Nutrition 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 206010028537 myelofibrosis Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 208000037244 polycythemia vera Diseases 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000009890 sinusitis Diseases 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000006707 (C3-C12) heterocycloalkyl group Chemical group 0.000 claims 1
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 102000003989 Aurora kinases Human genes 0.000 claims 1
- 108090000433 Aurora kinases Proteins 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 206010016946 Food allergy Diseases 0.000 claims 1
- 241000238631 Hexapoda Species 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000000048 adrenergic agonist Substances 0.000 claims 1
- 229940126157 adrenergic receptor agonist Drugs 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 229940125715 antihistaminic agent Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 208000004921 cutaneous lupus erythematosus Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 229940125721 immunosuppressive agent Drugs 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 239000002919 insect venom Substances 0.000 claims 1
- 210000000936 intestine Anatomy 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 231100000614 poison Toxicity 0.000 claims 1
- 239000002574 poison Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 231100000611 venom Toxicity 0.000 claims 1
- 208000034280 venom allergy Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461971552P | 2014-03-28 | 2014-03-28 | |
| US61/971,552 | 2014-03-28 | ||
| PCT/US2015/022863 WO2015148868A1 (en) | 2014-03-28 | 2015-03-27 | Substituted heteroaryl compounds and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017510643A JP2017510643A (ja) | 2017-04-13 |
| JP2017510643A5 true JP2017510643A5 (OSRAM) | 2018-03-22 |
| JP6538148B2 JP6538148B2 (ja) | 2019-07-03 |
Family
ID=54189377
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017502933A Active JP6517318B2 (ja) | 2014-03-28 | 2015-03-27 | 置換されたヘテロアリール化合物および使用方法 |
| JP2017502935A Active JP6517319B2 (ja) | 2014-03-28 | 2015-03-27 | 置換されたヘテロアリール化合物および使用方法 |
| JP2017502934A Active JP6538148B2 (ja) | 2014-03-28 | 2015-03-27 | 置換されたヘテロアリール化合物および使用方法 |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017502933A Active JP6517318B2 (ja) | 2014-03-28 | 2015-03-27 | 置換されたヘテロアリール化合物および使用方法 |
| JP2017502935A Active JP6517319B2 (ja) | 2014-03-28 | 2015-03-27 | 置換されたヘテロアリール化合物および使用方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US9399637B2 (OSRAM) |
| EP (5) | EP3122729A4 (OSRAM) |
| JP (3) | JP6517318B2 (OSRAM) |
| AU (1) | AU2015235880B2 (OSRAM) |
| CA (1) | CA2943979A1 (OSRAM) |
| MX (1) | MX2016012574A (OSRAM) |
| WO (3) | WO2015148868A1 (OSRAM) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017156493A1 (en) | 2016-03-11 | 2017-09-14 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
| WO2015148868A1 (en) * | 2014-03-28 | 2015-10-01 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| US11517026B2 (en) | 2014-09-11 | 2022-12-06 | Koninklijke Philips N.V. | Method for controlling a process of roasting coffee beans and device for use in a process for roasting coffee beans |
| CN106478651B (zh) * | 2015-08-31 | 2019-07-09 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| WO2017044434A1 (en) * | 2015-09-11 | 2017-03-16 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| JP2018527381A (ja) * | 2015-09-17 | 2018-09-20 | サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． | 置換されたヘテロアリール化合物および使用方法 |
| WO2017087905A1 (en) | 2015-11-20 | 2017-05-26 | Denali Therapeutics Inc. | Compound, compositions, and methods |
| JP6453794B2 (ja) * | 2016-03-07 | 2019-01-16 | Ckd株式会社 | 検査装置、ブリスタ包装機、ｐｔｐシートの製造方法および錠剤 |
| PE20190395A1 (es) | 2016-06-16 | 2019-03-13 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos |
| EP3552247B1 (en) | 2016-12-09 | 2020-04-29 | Koninklijke Philips N.V. | Actuator device and method |
| WO2018169700A1 (en) * | 2017-03-14 | 2018-09-20 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| EP3710006A4 (en) * | 2017-11-19 | 2021-09-01 | Sunshine Lake Pharma Co., Ltd. | SUBSTITUTED HETEROARYL COMPOUNDS AND THEIR METHODS OF USE |
| CN110833553A (zh) * | 2018-08-15 | 2020-02-25 | 广西梧州制药（集团）股份有限公司 | 吡唑并嘧啶衍生物在治疗Arthus反应的用途 |
| CN114302887B (zh) * | 2019-09-05 | 2025-04-15 | 伯尔尼大学 | 三环Janus激酶(JAK)抑制剂及其在治疗自身免疫性疾病中的用途 |
| CN110862376A (zh) * | 2019-10-24 | 2020-03-06 | 嘉兴特科罗生物科技有限公司 | 一种小分子化合物 |
| JP7659560B2 (ja) * | 2019-12-16 | 2025-04-09 | コリア リサーチ インスティチュート オブ ケミカル テクノロジー | 新規なピリミジン誘導体及びその用途 |
| TWI775313B (zh) | 2020-02-18 | 2022-08-21 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| AR121356A1 (es) | 2020-02-18 | 2022-05-11 | Gilead Sciences Inc | Compuestos antivirales |
| TWI794742B (zh) | 2020-02-18 | 2023-03-01 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| WO2022053000A1 (zh) * | 2020-09-10 | 2022-03-17 | 四川海思科制药有限公司 | 一种碳环酰胺衍生物及其在医药上的应用 |
| JP7621624B2 (ja) * | 2021-01-11 | 2025-01-27 | 広州力▲しん▼生物科技有限公司 | ２－アミノピリミジン系化合物、その医薬組成物、及び使用 |
| ES3028915T3 (en) | 2021-04-16 | 2025-06-20 | Gilead Sciences Inc | Methods of preparing carbanucleosides using amides |
| EP4387977A1 (en) | 2021-08-18 | 2024-06-26 | Gilead Sciences, Inc. | Phospholipid compounds and methods of making and using the same |
| CN117064888A (zh) * | 2023-09-26 | 2023-11-17 | 中国科学院水生生物研究所 | 氯喹或其药学上可接受的盐在制备预防生产非整倍体配子的药物中的应用 |
Family Cites Families (109)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1524747A (en) | 1976-05-11 | 1978-09-13 | Ici Ltd | Polypeptide |
| US4410545A (en) | 1981-02-13 | 1983-10-18 | Syntex (U.S.A.) Inc. | Carbonate diester solutions of PGE-type compounds |
| US4328245A (en) | 1981-02-13 | 1982-05-04 | Syntex (U.S.A.) Inc. | Carbonate diester solutions of PGE-type compounds |
| US4409239A (en) | 1982-01-21 | 1983-10-11 | Syntex (U.S.A.) Inc. | Propylene glycol diester solutions of PGE-type compounds |
| LU88769I2 (fr) | 1982-07-23 | 1996-11-05 | Zeneca Ltd | Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R)) |
| GB8327256D0 (en) | 1983-10-12 | 1983-11-16 | Ici Plc | Steroid derivatives |
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| US5010099A (en) | 1989-08-11 | 1991-04-23 | Harbor Branch Oceanographic Institution, Inc. | Discodermolide compounds, compositions containing same and method of preparation and use |
| NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
| GB9127376D0 (en) | 1991-12-24 | 1992-02-19 | Wellcome Found | Amidino derivatives |
| GB9300059D0 (en) | 1992-01-20 | 1993-03-03 | Zeneca Ltd | Quinazoline derivatives |
| MX9301943A (es) | 1992-04-02 | 1994-08-31 | Smithkline Beecham Corp | Compuestos. |
| TW225528B (OSRAM) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| GB9314893D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Quinazoline derivatives |
| EP0957087B1 (en) | 1994-06-15 | 2002-12-04 | The Wellcome Foundation Limited | Intermediates useful in the preparation of enzyme inhibitors |
| DE69536015D1 (de) | 1995-03-30 | 2009-12-10 | Pfizer Prod Inc | Chinazolinone Derivate |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| US5843901A (en) | 1995-06-07 | 1998-12-01 | Advanced Research & Technology Institute | LHRH antagonist peptides |
| DK0836605T3 (da) | 1995-07-06 | 2002-05-13 | Novartis Ag | Pyrrolopyrimidiner og fremgangsmåder til deres fremstilling |
| US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| SK284073B6 (sk) | 1996-04-12 | 2004-09-08 | Warner-Lambert Company | Polycyklické zlúčeniny, ich použitie a farmaceutické kompozície na ich báze |
| WO1997049688A1 (en) | 1996-06-24 | 1997-12-31 | Pfizer Inc. | Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases |
| NZ334821A (en) | 1996-08-30 | 2000-12-22 | Novartis Ag | Method for producing epothilones |
| DE69724269T2 (de) | 1996-09-06 | 2004-06-09 | Obducat Ab | Verfahren für das anisotrope ätzen von strukturen in leitende materialien |
| CA2265630A1 (en) | 1996-09-13 | 1998-03-19 | Gerald Mcmahon | Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders |
| EP0837063A1 (en) | 1996-10-17 | 1998-04-22 | Pfizer Inc. | 4-Aminoquinazoline derivatives |
| CN100344627C (zh) | 1996-11-18 | 2007-10-24 | 生物技术研究有限公司(Gbf) | 埃坡霉素c、其制备方法以及作为细胞抑制剂和植物保护剂的应用 |
| US6441186B1 (en) | 1996-12-13 | 2002-08-27 | The Scripps Research Institute | Epothilone analogs |
| MY117948A (en) | 1997-01-13 | 2004-08-30 | Glaxo Group Ltd | Nitride oxide synthase inhibitors. |
| DE19723722A1 (de) | 1997-05-30 | 1998-12-10 | Schering Ag | Nichtsteroidale Gestagene |
| CO4940418A1 (es) | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
| GB9721069D0 (en) | 1997-10-03 | 1997-12-03 | Pharmacia & Upjohn Spa | Polymeric derivatives of camptothecin |
| US6350458B1 (en) | 1998-02-10 | 2002-02-26 | Generex Pharmaceuticals Incorporated | Mixed micellar drug deliver system and method of preparation |
| US6506766B1 (en) | 1998-02-13 | 2003-01-14 | Abbott Laboratories | Glucocortiocoid-selective antinflammatory agents |
| US6194181B1 (en) | 1998-02-19 | 2001-02-27 | Novartis Ag | Fermentative preparation process for and crystal forms of cytostatics |
| ATE307123T1 (de) | 1998-02-25 | 2005-11-15 | Sloan Kettering Inst Cancer | Synthese von epothilonen, ihren zwischenprodukten und analogen verbindungen |
| GB9811599D0 (en) | 1998-05-30 | 1998-07-29 | Glaxo Group Ltd | Nitric oxide synthase inhibitors |
| EP1107964B8 (en) | 1998-08-11 | 2010-04-07 | Novartis AG | Isoquinoline derivatives with angiogenesis inhibiting activity |
| EP1135470A2 (en) | 1998-11-20 | 2001-09-26 | Kosan Biosciences, Inc. | Recombinant methods and materials for producing epothilone and epothilone derivatives |
| EP1175422A2 (en) | 1999-05-04 | 2002-01-30 | Ligand Pharmaceuticals Incorporated | Tetracyclic progesterone receptor modulator compounds and methods |
| ES2165768B1 (es) | 1999-07-14 | 2003-04-01 | Almirall Prodesfarma Sa | Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen. |
| CO5180649A1 (es) | 1999-09-01 | 2002-07-30 | Abbott Lab | Antagonistas de los receptores de los glucocorticoides para el tratamiento de la diabetes para el tratamiento de la diabetes |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| CA2423251A1 (en) | 2000-09-29 | 2002-04-04 | Glaxo Group Limited | Morpholin-acetamide derivatives for the treatment of inflammatory diseases |
| PE20020544A1 (es) | 2000-11-07 | 2002-07-30 | Novartis Ag | Derivados de indolilmaleimida |
| GB0031179D0 (en) | 2000-12-21 | 2001-01-31 | Glaxo Group Ltd | Nitric oxide synthase inhibitors |
| HUP0400639A3 (en) * | 2000-12-21 | 2010-03-29 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them |
| US6484903B2 (en) | 2001-01-09 | 2002-11-26 | Riverwood International Corporation | Carton with an improved dispensing feature in combination with a unique handle |
| AR035885A1 (es) | 2001-05-14 | 2004-07-21 | Novartis Ag | Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica |
| GB0119249D0 (en) | 2001-08-07 | 2001-10-03 | Novartis Ag | Organic compounds |
| WO2003030909A1 (en) * | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| ES2314106T3 (es) * | 2001-10-17 | 2009-03-16 | BOEHRINGER INGELHEIM PHARMA GMBH & CO.KG | Derivados de pirimidina, agentes farmaceuticos que contiene dichos compuestos, uso y metodo para su obtencion. |
| CA2472746A1 (en) | 2002-01-14 | 2003-07-24 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical formulations containing them and uses thereof |
| EP1467730A4 (en) | 2002-01-22 | 2010-03-10 | Univ California | Non-steroid ligands for the glucocorticoid receptor, compositions and uses thereof |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| JP2005521717A (ja) | 2002-03-26 | 2005-07-21 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | グルココルチコイドミメチックス、その製造方法、その医薬組成物、及び使用 |
| DE60318188T2 (de) | 2002-03-26 | 2008-12-11 | Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield | Glucocorticoid-mimetika, deren herstellung, pharmazeutische zusammensetzungen und verwendung |
| DE10215316C1 (de) | 2002-04-02 | 2003-12-18 | Schering Ag | Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer |
| AR039209A1 (es) | 2002-04-03 | 2005-02-09 | Novartis Ag | Derivados de indolilmaleimida |
| WO2003086294A2 (en) | 2002-04-11 | 2003-10-23 | Merck & Co., Inc. | 1h-benzo[f]indazol-5-yl derivatives as selective glucocorticoid receptor modulators |
| US7186864B2 (en) | 2002-05-29 | 2007-03-06 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| US7074806B2 (en) | 2002-06-06 | 2006-07-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| EP1521733B1 (en) | 2002-07-08 | 2014-08-20 | Pfizer Products Inc. | Modulators of the glucocorticoid receptor |
| JP2006508042A (ja) | 2002-07-18 | 2006-03-09 | ブリストル−マイヤーズ スクイブ カンパニー | グルココルチコイド受容体の修飾物質および方法 |
| WO2004018429A2 (en) | 2002-08-21 | 2004-03-04 | Boehringer Ingelheim Pharmaceuticals, Inc. | Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| CA2499150A1 (en) | 2002-09-20 | 2004-04-01 | Merck & Co., Inc. | Octahydro-2-h-naphtho[1,2-f] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators |
| GB0224084D0 (en) | 2002-10-16 | 2002-11-27 | Glaxo Group Ltd | Novel compounds |
| US20050014753A1 (en) | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
| US7122542B2 (en) | 2003-07-30 | 2006-10-17 | Rigel Pharmaceuticals, Inc. | Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds |
| JP4812763B2 (ja) | 2004-05-18 | 2011-11-09 | ライジェル ファーマシューティカルズ， インコーポレイテッド | シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途 |
| WO2006000398A1 (en) | 2004-06-28 | 2006-01-05 | Glaxo Group Limited | 2,3-benzoxazin derivatives as non-steroidal glucocorticoid receptor modulators |
| WO2006000401A1 (en) | 2004-06-28 | 2006-01-05 | Glaxo Group Limited | Substituted oxazines as glucocorticoid receptor modulators |
| GB0418045D0 (en) | 2004-08-12 | 2004-09-15 | Glaxo Group Ltd | Compounds |
| RU2391338C2 (ru) | 2004-10-19 | 2010-06-10 | Ф.Хоффманн-Ля Рош Аг | Производные хинолина |
| GB2420559B (en) | 2004-11-15 | 2008-08-06 | Rigel Pharmaceuticals Inc | Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses |
| WO2006067614A2 (en) | 2004-12-23 | 2006-06-29 | Pfizer Products Inc. | Heteroaromatic derivatives useful as anticancer agents |
| US8211929B2 (en) | 2004-12-30 | 2012-07-03 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| WO2008045978A1 (en) | 2006-10-10 | 2008-04-17 | Rigel Pharmaceuticals, Inc. | Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors |
| RS53588B1 (sr) | 2006-12-08 | 2015-02-27 | Irm Llc | Jedinjenja i kompozicije kao inhibitori protein kinaza |
| WO2008118822A1 (en) | 2007-03-23 | 2008-10-02 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| CA2693594A1 (en) | 2007-07-17 | 2009-01-22 | Rigel Pharmaceuticals, Inc. | Cyclic amine substituted pyrimidinediamines as pkc inhibitors |
| US20110028405A1 (en) * | 2007-12-20 | 2011-02-03 | Richard John Harrison | Sulfamides as zap-70 inhibitors |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| MY155639A (en) * | 2008-04-16 | 2015-11-13 | Portola Pharm Inc | 2, 6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors |
| PT2323993E (pt) | 2008-04-16 | 2015-10-12 | Portola Pharm Inc | 2,6-diamino-pirimidina-5-il-carboxamidas como inibidores de quinasses syk ou jak |
| US8258144B2 (en) | 2008-04-22 | 2012-09-04 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| EP2361248B1 (en) | 2008-06-27 | 2018-09-19 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| US8697694B2 (en) | 2008-08-20 | 2014-04-15 | Merck Sharp & Dohme Corp. | Substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
| ES2618889T3 (es) | 2009-01-14 | 2017-06-22 | Rigel Pharmaceuticals, Inc. | Compuestos de 2,4-pirimidindiamina para el tratamiento de trastornos inflamatorios |
| ES2635504T3 (es) | 2009-01-21 | 2017-10-04 | Rigel Pharmaceuticals, Inc. | Derivados de N2-(3-piridilo o fenil)-N4-(4-piperidil)-2,4-pirimidinadiamina útiles en el tratamiento de enfermedades inflamatorias, toimmunitarias o proliferativas |
| KR20110132607A (ko) | 2009-03-24 | 2011-12-08 | 엠에스디 가부시키가이샤 | 오로라 ａ 선택적 억제 작용을 갖는 신규한 아미노피리딘 유도체 |
| JP5918693B2 (ja) | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Ｅｇｆｒ阻害剤及び疾患の治療方法 |
| CA2764983A1 (en) | 2009-06-10 | 2010-12-16 | Abbott Laboratories | 2- ( lh-pyrazol-4 -ylamino ) -pyrimidine as kinase inhibitors |
| CA2780759A1 (en) | 2009-12-01 | 2011-06-09 | Rigel Pharmaceuticals, Inc. | Protein kinase c inhibitors and uses thereof |
| JP6035238B2 (ja) | 2010-07-21 | 2016-11-30 | ライジェル ファーマシューティカルズ， インコーポレイテッド | プロテインキナーゼｃ阻害剤およびその使用 |
| WO2012059932A1 (en) * | 2010-11-01 | 2012-05-10 | Aurigene Discovery Technologies Limited | 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors |
| ES2653967T3 (es) * | 2010-11-10 | 2018-02-09 | Genentech, Inc. | Derivados de pirazol aminopirimidina como moduladores de LRRK2 |
| AU2012357038B2 (en) | 2011-12-23 | 2016-05-12 | Cellzome Limited | Pyrimidine-2,4-diamine derivatives as kinase inhibitors |
| JP6141334B2 (ja) | 2012-02-17 | 2017-06-07 | アッヴィ・インコーポレイテッド | ヒト呼吸器多核体ウイルス（ｒｓｖ）の阻害剤として有用なジアミノピリミジン |
| EP2833889B1 (en) | 2012-04-04 | 2017-11-01 | Rigel Pharmaceuticals, Inc. | Protein kinase c inhibitors and uses thereof |
| RU2637948C2 (ru) * | 2012-05-03 | 2017-12-08 | Дженентек, Инк. | Производные пиразоламинопиримидина в качестве модуляторов обогащенной лейциновыми повторами киназы 2 (lrrk2) для применения при лечении болезни паркинсона |
| WO2014040555A1 (zh) | 2012-09-12 | 2014-03-20 | 山东亨利医药科技有限责任公司 | 作为酪氨酸激酶抑制剂的含氮杂芳环衍生物 |
| US9598440B2 (en) | 2012-10-08 | 2017-03-21 | Merck Sharp & Dohme Corp. | Inhibitors of IRAK4 activity |
| CN104955824B (zh) | 2012-11-20 | 2017-09-22 | 豪夫迈·罗氏有限公司 | 作为含t790m的egfr突变体的抑制剂的氨基嘧啶化合物 |
| EP2970275B1 (en) | 2013-03-14 | 2018-05-09 | Rigel Pharmaceuticals, Inc. | Protein kinase c inhibitors and uses thereof |
| WO2015039613A1 (zh) | 2013-09-18 | 2015-03-26 | 北京韩美药品有限公司 | 抑制btk和/或jak3激酶活性的化合物 |
| WO2015148868A1 (en) * | 2014-03-28 | 2015-10-01 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
-
2015
- 2015-03-27 WO PCT/US2015/022863 patent/WO2015148868A1/en not_active Ceased
- 2015-03-27 US US14/670,422 patent/US9399637B2/en active Active
- 2015-03-27 EP EP15769393.8A patent/EP3122729A4/en not_active Withdrawn
- 2015-03-27 US US14/670,421 patent/US9403801B2/en active Active
- 2015-03-27 AU AU2015235880A patent/AU2015235880B2/en active Active
- 2015-03-27 EP EP17202803.7A patent/EP3327006B1/en active Active
- 2015-03-27 JP JP2017502933A patent/JP6517318B2/ja active Active
- 2015-03-27 US US14/670,425 patent/US9394281B2/en active Active
- 2015-03-27 EP EP17202947.2A patent/EP3312164B1/en active Active
- 2015-03-27 EP EP15768584.3A patent/EP3122728A4/en not_active Ceased
- 2015-03-27 WO PCT/US2015/022862 patent/WO2015148867A1/en not_active Ceased
- 2015-03-27 JP JP2017502935A patent/JP6517319B2/ja active Active
- 2015-03-27 JP JP2017502934A patent/JP6538148B2/ja active Active
- 2015-03-27 MX MX2016012574A patent/MX2016012574A/es unknown
- 2015-03-27 WO PCT/US2015/022864 patent/WO2015148869A1/en not_active Ceased
- 2015-03-27 EP EP15769715.2A patent/EP3122730B1/en active Active
- 2015-03-27 CA CA2943979A patent/CA2943979A1/en not_active Abandoned
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