BR112016024545A2 - derivados de pirazolo pirimidina e seu uso como inibidores de malt1 - Google Patents
derivados de pirazolo pirimidina e seu uso como inibidores de malt1Info
- Publication number
- BR112016024545A2 BR112016024545A2 BR112016024545A BR112016024545A BR112016024545A2 BR 112016024545 A2 BR112016024545 A2 BR 112016024545A2 BR 112016024545 A BR112016024545 A BR 112016024545A BR 112016024545 A BR112016024545 A BR 112016024545A BR 112016024545 A2 BR112016024545 A2 BR 112016024545A2
- Authority
- BR
- Brazil
- Prior art keywords
- pyrimidine derivatives
- malt1
- present
- pyrazole pyrimidine
- malt1 inhibitors
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Abstract
a presente invenção descreve novos derivados de pirazolo pirimidina de fórmula (i) ou um sal farmaceuticamente aceitável dos mesmos, em que r1, r2 e r são como definidos no presente pedido de patente. a presente invenção descreve adicionalmente a síntese dos ditos novos derivados pirazolo-pirimidina, seu uso como um medicamento, especialmente pela interação com a atividade proteolítica e/ou autoproteolítica de malt1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14170408 | 2014-05-28 | ||
| PCT/IB2015/053975 WO2015181747A1 (en) | 2014-05-28 | 2015-05-27 | Novel pyrazolo pyrimidine derivatives and their use as malt1 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112016024545A2 true BR112016024545A2 (pt) | 2017-08-15 |
Family
ID=50828759
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112016024545A BR112016024545A2 (pt) | 2014-05-28 | 2015-05-27 | derivados de pirazolo pirimidina e seu uso como inibidores de malt1 |
Country Status (36)
| Country | Link |
|---|---|
| US (2) | US9815842B2 (pt) |
| EP (1) | EP3149001B1 (pt) |
| JP (1) | JP6545197B2 (pt) |
| KR (1) | KR20170007311A (pt) |
| CN (1) | CN106170489B (pt) |
| AP (1) | AP2016009487A0 (pt) |
| AR (1) | AR100645A1 (pt) |
| AU (1) | AU2015265478B2 (pt) |
| BR (1) | BR112016024545A2 (pt) |
| CA (1) | CA2945077A1 (pt) |
| CL (1) | CL2016002942A1 (pt) |
| CR (1) | CR20160548A (pt) |
| CU (1) | CU24393B1 (pt) |
| CY (1) | CY1121946T1 (pt) |
| DK (1) | DK3149001T3 (pt) |
| EA (1) | EA032050B1 (pt) |
| ES (1) | ES2738695T3 (pt) |
| GT (1) | GT201600249A (pt) |
| HR (1) | HRP20191261T1 (pt) |
| HU (1) | HUE044351T2 (pt) |
| IL (1) | IL247949A0 (pt) |
| LT (1) | LT3149001T (pt) |
| MX (1) | MX2016015544A (pt) |
| MY (1) | MY182487A (pt) |
| PE (1) | PE20170189A1 (pt) |
| PH (1) | PH12016501862A1 (pt) |
| PL (1) | PL3149001T3 (pt) |
| PT (1) | PT3149001T (pt) |
| RS (1) | RS59039B1 (pt) |
| SG (1) | SG11201607895PA (pt) |
| SI (1) | SI3149001T1 (pt) |
| SV (1) | SV2016005328A (pt) |
| TR (1) | TR201910730T4 (pt) |
| TW (1) | TWI709561B (pt) |
| UY (1) | UY36143A (pt) |
| WO (1) | WO2015181747A1 (pt) |
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| MX342405B (es) | 2010-06-03 | 2016-09-28 | Pharmacyclics Inc | El uso de inhibidores de la tirosina quinasa de bruton (btk). |
| AU2013293087B2 (en) | 2012-07-24 | 2017-08-31 | Pharmacyclics Llc | Mutations associated with resistance to inhibitors of Bruton's tyrosine kinase (BTK) |
| WO2017040304A1 (en) | 2015-08-28 | 2017-03-09 | Cornell University | Malt1 inhibitors and uses thereof |
| SG11201803480WA (en) * | 2015-11-13 | 2018-05-30 | Novartis Ag | Novel pyrazolo pyrimidine derivatives |
| TWI726969B (zh) | 2016-01-11 | 2021-05-11 | 比利時商健生藥品公司 | 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物 |
| CN107296807B (zh) * | 2016-04-15 | 2020-03-20 | 中国科学院上海生命科学研究院 | Malt1靶向抑制物在制备malt1依赖性肿瘤治疗药物中的应用 |
| WO2018019721A1 (en) | 2016-07-26 | 2018-02-01 | Basf Se | Herbicidal pyridine compounds |
| WO2018019755A1 (en) | 2016-07-26 | 2018-02-01 | Basf Se | Herbicidal pyridine compounds |
| CN109476599A (zh) | 2016-07-29 | 2019-03-15 | 东丽株式会社 | 胍衍生物和其医药用途 |
| BR112019001824A2 (pt) | 2016-07-29 | 2019-05-07 | Lupin Limited | compostos de tiazol-piridina substituídos como inibidores de malt1 |
| SG11201900745VA (en) * | 2016-07-29 | 2019-02-27 | Lupin Ltd | Substituted thiazolo-pyridine compounds as malt1 inhibitors |
| JP7097880B2 (ja) * | 2016-11-01 | 2022-07-08 | コーネル ユニバーシティー | Ｍａｌｔ１分解のための化合物 |
| TWI795381B (zh) * | 2016-12-21 | 2023-03-11 | 比利時商健生藥品公司 | 作為ｍａｌｔ１抑制劑之吡唑衍生物 |
| US10829482B2 (en) | 2016-12-27 | 2020-11-10 | Kao Corporation | Method for producing glyceric acid ester |
| US10870643B2 (en) | 2016-12-27 | 2020-12-22 | Kao Corporation | Method for manufacturing 1,3-dioxane-5-one |
| US10822329B2 (en) | 2016-12-27 | 2020-11-03 | Kao Corporation | Method for producing glyceric acid ester |
| US20200009135A1 (en) | 2017-02-01 | 2020-01-09 | Medivir Ab | Therapeutic applications of malt1 inhibitors |
| WO2018159650A1 (ja) * | 2017-02-28 | 2018-09-07 | 東レ株式会社 | グアニジン誘導体及びその医薬用途 |
| US11248007B2 (en) | 2017-03-08 | 2022-02-15 | Cornell University | Inhibitors of MALT1 and uses thereof |
| WO2018226150A1 (en) * | 2017-06-05 | 2018-12-13 | Medivir Aktiebolag | Pyrazolopyrimidine as malt-1 inhibitors |
| WO2018225829A1 (ja) * | 2017-06-08 | 2018-12-13 | 三井化学アグロ株式会社 | ピリドン化合物およびそれを有効成分とする農園芸用殺菌剤 |
| JP7271540B2 (ja) * | 2017-11-17 | 2023-05-11 | へパジーン セラピューティクス （エイチケイ） リミテッド | Ａｓｋ１阻害剤としての尿素誘導体 |
| KR20210024548A (ko) | 2018-06-18 | 2021-03-05 | 얀센 파마슈티카 엔.브이. | Malt1 억제제로서의 피라졸 유도체 |
| KR20210024002A (ko) | 2018-06-18 | 2021-03-04 | 얀센 파마슈티카 엔.브이. | Malt1 억제제로서의 피라졸 유도체 |
| WO2020111087A1 (ja) * | 2018-11-28 | 2020-06-04 | 武田薬品工業株式会社 | 複素環化合物 |
| CN109503473B (zh) * | 2019-01-07 | 2020-07-07 | 上海慧川生物医药科技有限公司 | 2-甲氧基-3-氨基-5-吡啶硼酸频哪醇酯及其中间体的合成方法 |
| CA3131856A1 (en) | 2019-04-11 | 2020-10-15 | Janssen Pharmaceutica N.V. | Pyridine rings containing derivatives as malt1 inhibitors |
| TW202115077A (zh) * | 2019-07-01 | 2021-04-16 | 大陸商上海齊魯銳格醫藥研發有限公司 | Ｍａｌｔ１抑制劑及其用途 |
| CN111138437B (zh) * | 2019-12-04 | 2021-03-05 | 杭州华东医药集团新药研究院有限公司 | 取代的吡唑并[1,5-a]嘧啶氨基酸衍生物及其用途 |
| EP4163280A1 (en) | 2020-05-27 | 2023-04-12 | Takeda Pharmaceutical Company Limited | Method for producing heterocyclic compound |
| US20230235077A1 (en) | 2020-06-24 | 2023-07-27 | The General Hospital Corporation | Materials and methods of treating cancer |
| TW202220992A (zh) * | 2020-08-05 | 2022-06-01 | 匈牙利商羅特格登公司 | 具藥理活性之經雜環取代的吡唑并〔１，５－ａ〕嘧啶衍生物 |
| JP2023549835A (ja) * | 2020-11-12 | 2023-11-29 | モノプテロス セラピューティクス，インコーポレーテッド | がんを治療する材料及び方法 |
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| WO2023139479A1 (en) * | 2022-01-18 | 2023-07-27 | Aurigene Oncology Limited | Substituted bicyclic heterocycles as malt-1 inhibitors |
| WO2023143249A1 (zh) * | 2022-01-28 | 2023-08-03 | 上海齐鲁制药研究中心有限公司 | 靶向malt1的蛋白降解化合物 |
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| US7517880B2 (en) | 1997-12-22 | 2009-04-14 | Bayer Pharmaceuticals Corporation | Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas |
| US20020065296A1 (en) | 1999-01-13 | 2002-05-30 | Bayer Corporation | Heteroaryl ureas containing nitrogen hetero-atoms as p38 kinase inhibitors |
| EP2324825A1 (en) | 2002-02-11 | 2011-05-25 | Bayer Healthcare LLC | Aryl ureas with angiogenesis inhibiting activity |
| WO2004078163A2 (en) | 2003-02-28 | 2004-09-16 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
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| EP2465928A1 (en) | 2010-12-16 | 2012-06-20 | Academisch Medisch Centrum bij de Universiteit van Amsterdam | Treatment of Th17-mediated diseases |
| US9096605B2 (en) * | 2011-08-24 | 2015-08-04 | Glaxosmithkline Llc | Pyrazolopyrimidine derivatives as PI3 kinase inhibitors |
| CN103570723B (zh) * | 2012-07-27 | 2016-07-13 | 广西梧州制药（集团）股份有限公司 | 吡唑并嘧啶衍生物及其制备方法和在药物制备中的用途 |
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| NZ711896A (en) | 2012-12-21 | 2018-04-27 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| WO2014181287A1 (en) | 2013-05-09 | 2014-11-13 | Piramal Enterprises Limited | Heterocyclyl compounds and uses thereof |
| CN103739550B (zh) * | 2014-01-02 | 2016-06-01 | 中国药科大学 | 2,3-二甲基-6-脲-2h-吲唑类化合物及其制备方法与应用 |
-
2015
- 2015-05-27 CR CR20160548A patent/CR20160548A/es unknown
- 2015-05-27 PE PE2016002391A patent/PE20170189A1/es unknown
- 2015-05-27 CN CN201580020935.9A patent/CN106170489B/zh not_active Expired - Fee Related
- 2015-05-27 AU AU2015265478A patent/AU2015265478B2/en not_active Ceased
- 2015-05-27 SG SG11201607895PA patent/SG11201607895PA/en unknown
- 2015-05-27 MX MX2016015544A patent/MX2016015544A/es active IP Right Grant
- 2015-05-27 TW TW104117061A patent/TWI709561B/zh not_active IP Right Cessation
- 2015-05-27 MY MYPI2016703450A patent/MY182487A/en unknown
- 2015-05-27 AP AP2016009487A patent/AP2016009487A0/en unknown
- 2015-05-27 US US15/312,321 patent/US9815842B2/en active Active
- 2015-05-27 HU HUE15733899 patent/HUE044351T2/hu unknown
- 2015-05-27 KR KR1020167032664A patent/KR20170007311A/ko not_active Application Discontinuation
- 2015-05-27 CU CU2016000181A patent/CU24393B1/es unknown
- 2015-05-27 WO PCT/IB2015/053975 patent/WO2015181747A1/en active Application Filing
- 2015-05-27 LT LTEP15733899.7T patent/LT3149001T/lt unknown
- 2015-05-27 CA CA2945077A patent/CA2945077A1/en not_active Abandoned
- 2015-05-27 PL PL15733899T patent/PL3149001T3/pl unknown
- 2015-05-27 ES ES15733899T patent/ES2738695T3/es active Active
- 2015-05-27 EA EA201692105A patent/EA032050B1/ru not_active IP Right Cessation
- 2015-05-27 RS RS20190905A patent/RS59039B1/sr unknown
- 2015-05-27 TR TR2019/10730T patent/TR201910730T4/tr unknown
- 2015-05-27 JP JP2016569068A patent/JP6545197B2/ja not_active Expired - Fee Related
- 2015-05-27 SI SI201530825T patent/SI3149001T1/sl unknown
- 2015-05-27 PT PT15733899T patent/PT3149001T/pt unknown
- 2015-05-27 BR BR112016024545A patent/BR112016024545A2/pt active Search and Examination
- 2015-05-27 EP EP15733899.7A patent/EP3149001B1/en active Active
- 2015-05-27 DK DK15733899.7T patent/DK3149001T3/da active
- 2015-05-28 AR ARP150101686A patent/AR100645A1/es unknown
- 2015-05-28 UY UY0001036143A patent/UY36143A/es not_active Application Discontinuation
-
2016
- 2016-09-21 IL IL247949A patent/IL247949A0/en unknown
- 2016-09-22 PH PH12016501862A patent/PH12016501862A1/en unknown
- 2016-11-18 CL CL2016002942A patent/CL2016002942A1/es unknown
- 2016-11-28 SV SV2016005328A patent/SV2016005328A/es unknown
- 2016-11-28 GT GT201600249A patent/GT201600249A/es unknown
-
2017
- 2017-10-11 US US15/729,979 patent/US10442808B2/en not_active Expired - Fee Related
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2019
- 2019-07-12 HR HRP20191261TT patent/HRP20191261T1/hr unknown
- 2019-07-24 CY CY20191100786T patent/CY1121946T1/el unknown
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