CL2016002942A1 - Nuevos derivados de pirazolina pirimidina y su uso como inhibidores de malt1 - Google Patents
Nuevos derivados de pirazolina pirimidina y su uso como inhibidores de malt1Info
- Publication number
- CL2016002942A1 CL2016002942A1 CL2016002942A CL2016002942A CL2016002942A1 CL 2016002942 A1 CL2016002942 A1 CL 2016002942A1 CL 2016002942 A CL2016002942 A CL 2016002942A CL 2016002942 A CL2016002942 A CL 2016002942A CL 2016002942 A1 CL2016002942 A1 CL 2016002942A1
- Authority
- CL
- Chile
- Prior art keywords
- rent
- replaced
- optionally replaced
- alcoxyl
- independently
- Prior art date
Links
Classifications
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- 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
<p>LA PRESENTE INVENCIÓN DESCRIBE NUEVOS DERIVADOS DE LA PIRAZOLO-PIRIMIDINA DE IA FORMULA (I) O UNA SAL FARMACÉUTICAMENTE ACEPTABLE DEL MISMO; (I) EN LA QUE, R1 ES HALÓGENO, CIANO, O ALQUILO C1-C3 OPCIONALMENTE SUSTITUIDO POR HALÓGENO; R2 ES ALQUILO C1 - C6 OPCIONALMENTE SUSTITUIDO UNA O MÁS VECES POR ALQUILO C1-C6, ALQUENILO C2-C 6, HIDROXILO, N,N-DI-AIQUILAMINO C1 -C6, N-MONO-ALQUILAMINO C1-C6, O-RG, RG, FENILO , O POR ALCOXILO C1-C6 EN DONDE DICHO ALCOXILO DE NUEVO PUEDE SER OPCIONALMENTE SUSTITUIDO POR ALCOXILO C1-C6, N, N-DI-ALQUILAMINO C1-C6, RG O ALQUILO; CICLOALQUILO C3-C6 OPCIONALMENTE SUSTITUIDO POR ALQUILO C1 –C6 , N,N-DI-ALQUILAMINO C1-C6 O ALCOXILO C1-C6-ALQUILO C1-C6, Y/O DOS DE DICHOS SUSTITUYENTES OPCIONALES JUNTO CON LOS ÁTOMOS A LOS QUE ESTÁN UNIDOS PUEDEN FORMAR UN ANILLO HETEROCÍCLICO SATURADO ANULADO O ESPIROCÍCLICO DE 4-6 MIEMBROS QUE COMPRENDE 1 - 20 ÁTOMOS; FENILO OPCIONALMENTE SUSTITUIDO POR ALCOXILO C1-C6; UN ANILLO HETEROARILO DE 5 - 6 MIEMBROS QUE TIENE 1 A 3 HETEROÁTOMOS SELECCIONADOS DE N Y O, DICHO ANILLO ES OPCIONALMENTE SUSTITUIDO POR ALQUILO C1-C6 QUE PUEDE ESTAR OPCIONALMENTE SUSTITUIDO POR AMINO O HIDROXILO; RG; O N,N-DI-ALQUILAMINO CARBONILO C1 –C6; Y R ES FENILO SUSTITUIDO INDEPENDIENTEMENTE DOS O MÁS VECES POR RA, 2-PIRIDILO SUSTITUIDO INDEPENDIENTEMENTE UNA O MÁS VECES POR RB, 3-PIRIDILO SUSTITUIDO INDEPENDIENTEMENTE UNA O MÁS VECES POR RC, O 4-PIRIDILO INDEPENDIENTEMENTE SUSTITUIDO UNA O MÁS VECES POR RD; QUE GENERALMENTE ESTÁN INTERACTUANDO CON ACTIVIDAD PROTEOLÍTICA Y/O AUTOPROTEOLÍTICA DE MALT1, Y EN PARTICULAR QUE PUEDEN INHIBIR DICHA ACTIVIDAD. LA PRESENTE INVENCIÓN DESCRIBE ADEMÁS LA SÍNTESIS DE ESTOS NUEVOS DERIVADOS DE LA PIRAZOLO-PIRIMIDINA, SU USO COMO UN MEDICAMENTO, ESPECIALMENTE MEDIANTE LA INTERACCIÓN CON ACTIVIDAD PROTEOLÍTICA Y/O AUTOPROTEOLÍTICA DE MALT1.</p>
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14170408 | 2014-05-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2016002942A1 true CL2016002942A1 (es) | 2017-07-14 |
Family
ID=50828759
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2016002942A CL2016002942A1 (es) | 2014-05-28 | 2016-11-18 | Nuevos derivados de pirazolina pirimidina y su uso como inhibidores de malt1 |
Country Status (36)
| Country | Link |
|---|---|
| US (2) | US9815842B2 (es) |
| EP (1) | EP3149001B1 (es) |
| JP (1) | JP6545197B2 (es) |
| KR (1) | KR20170007311A (es) |
| CN (1) | CN106170489B (es) |
| AP (1) | AP2016009487A0 (es) |
| AR (1) | AR100645A1 (es) |
| AU (1) | AU2015265478B2 (es) |
| BR (1) | BR112016024545A2 (es) |
| CA (1) | CA2945077A1 (es) |
| CL (1) | CL2016002942A1 (es) |
| CR (1) | CR20160548A (es) |
| CU (1) | CU24393B1 (es) |
| CY (1) | CY1121946T1 (es) |
| DK (1) | DK3149001T3 (es) |
| EA (1) | EA032050B1 (es) |
| ES (1) | ES2738695T3 (es) |
| GT (1) | GT201600249A (es) |
| HR (1) | HRP20191261T1 (es) |
| HU (1) | HUE044351T2 (es) |
| IL (1) | IL247949A0 (es) |
| LT (1) | LT3149001T (es) |
| MX (1) | MX2016015544A (es) |
| MY (1) | MY182487A (es) |
| PE (1) | PE20170189A1 (es) |
| PH (1) | PH12016501862B1 (es) |
| PL (1) | PL3149001T3 (es) |
| PT (1) | PT3149001T (es) |
| RS (1) | RS59039B1 (es) |
| SG (1) | SG11201607895PA (es) |
| SI (1) | SI3149001T1 (es) |
| SV (1) | SV2016005328A (es) |
| TR (1) | TR201910730T4 (es) |
| TW (1) | TWI709561B (es) |
| UY (1) | UY36143A (es) |
| WO (1) | WO2015181747A1 (es) |
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| JP6575950B2 (ja) | 2012-07-24 | 2019-09-18 | ファーマサイクリックス エルエルシー | Ｂｒｕｔｏｎ型チロシンキナーゼ（Ｂｔｋ）阻害剤に対する耐性を伴う変異 |
| EP3341007B1 (en) | 2015-08-28 | 2020-12-23 | Cornell University | Malt1 inhibitors and uses thereof |
| CA3003820A1 (en) * | 2015-11-13 | 2017-05-18 | 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 |
| US20190275012A9 (en) | 2016-07-29 | 2019-09-12 | Lupin Limited | Substituted thiazolo-pyridine compounds as malt1 inhibitors |
| US10662156B2 (en) | 2016-07-29 | 2020-05-26 | Toray Industries, Inc. | Guanidine derivative and medical use thereof |
| EP3490995A1 (en) | 2016-07-29 | 2019-06-05 | Lupin Limited | Substituted thiazolo-pyridine compounds as malt1 inhibitors |
| EP3535254A4 (en) | 2016-11-01 | 2020-06-24 | Cornell University Cornell Center For Technology, Enterprise & Commercialization ("CCTEC") | COMPOUNDS FOR THE DEGRADATION OF MALT1 |
| 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 |
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| CN109415334B (zh) | 2016-12-27 | 2023-12-08 | 花王株式会社 | 1,3-二噁烷-5-酮类的制造方法 |
| US10822329B2 (en) | 2016-12-27 | 2020-11-03 | Kao Corporation | Method for producing glyceric acid ester |
| WO2018141749A1 (en) | 2017-02-01 | 2018-08-09 | Medivir Ab | Therapeutic applications of malt1 inhibitors |
| JPWO2018159650A1 (ja) * | 2017-02-28 | 2019-12-19 | 東レ株式会社 | グアニジン誘導体及びその医薬用途 |
| JP7142022B2 (ja) * | 2017-03-08 | 2022-09-26 | コーネル・ユニバーシティー | Ｍａｌｔ１の阻害剤およびそれらの使用 |
| WO2018226150A1 (en) * | 2017-06-05 | 2018-12-13 | Medivir Aktiebolag | Pyrazolopyrimidine as malt-1 inhibitors |
| JP7157738B2 (ja) * | 2017-06-08 | 2022-10-20 | 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 |
| CN112585128B (zh) | 2018-06-18 | 2023-02-21 | 詹森药业有限公司 | 作为malt1抑制剂的吡唑衍生物 |
| KR20210024002A (ko) * | 2018-06-18 | 2021-03-04 | 얀센 파마슈티카 엔.브이. | Malt1 억제제로서의 피라졸 유도체 |
| TWI784213B (zh) | 2018-11-28 | 2022-11-21 | 日商武田藥品工業股份有限公司 | 雜環化合物 |
| 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 |
| WO2021000855A1 (en) * | 2019-07-01 | 2021-01-07 | Qilu Regor Therapeutics Inc. | Malt1 inhibitors and uses thereof |
| 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 |
| WO2021262969A1 (en) | 2020-06-24 | 2021-12-30 | The General Hospital Corporation | Materials and methods of treating cancer |
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| 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 |
| GB202018412D0 (en) | 2020-11-23 | 2021-01-06 | Exscientia Ltd | Malt-1 modulators ii |
| WO2023139479A1 (en) * | 2022-01-18 | 2023-07-27 | Aurigene Oncology Limited | Substituted bicyclic heterocycles as malt-1 inhibitors |
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2015
- 2015-05-27 DK DK15733899.7T patent/DK3149001T3/da active
- 2015-05-27 US US15/312,321 patent/US9815842B2/en active Active
- 2015-05-27 CU CU2016000181A patent/CU24393B1/es unknown
- 2015-05-27 ES ES15733899T patent/ES2738695T3/es active Active
- 2015-05-27 JP JP2016569068A patent/JP6545197B2/ja not_active Expired - Fee Related
- 2015-05-27 EP EP15733899.7A patent/EP3149001B1/en active Active
- 2015-05-27 PL PL15733899T patent/PL3149001T3/pl unknown
- 2015-05-27 AU AU2015265478A patent/AU2015265478B2/en not_active Ceased
- 2015-05-27 RS RS20190905A patent/RS59039B1/sr unknown
- 2015-05-27 MX MX2016015544A patent/MX2016015544A/es active IP Right Grant
- 2015-05-27 SG SG11201607895PA patent/SG11201607895PA/en unknown
- 2015-05-27 AP AP2016009487A patent/AP2016009487A0/en unknown
- 2015-05-27 WO PCT/IB2015/053975 patent/WO2015181747A1/en active Application Filing
- 2015-05-27 PT PT15733899T patent/PT3149001T/pt unknown
- 2015-05-27 CA CA2945077A patent/CA2945077A1/en not_active Abandoned
- 2015-05-27 TW TW104117061A patent/TWI709561B/zh not_active IP Right Cessation
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- 2015-05-27 BR BR112016024545A patent/BR112016024545A2/pt active Search and Examination
- 2015-05-27 PE PE2016002391A patent/PE20170189A1/es unknown
- 2015-05-27 EA EA201692105A patent/EA032050B1/ru not_active IP Right Cessation
- 2015-05-27 KR KR1020167032664A patent/KR20170007311A/ko not_active Application Discontinuation
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- 2015-05-27 CN CN201580020935.9A patent/CN106170489B/zh not_active Expired - Fee Related
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2016
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2017
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2019
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