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
- PLGJELISCRTPQD-UHFFFAOYSA-N C1NNC=C1.C1=CN=CN=C1 Chemical class C1NNC=C1.C1=CN=CN=C1 PLGJELISCRTPQD-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 101150113681 MALT1 gene Proteins 0.000 abstract 2
- 102000057613 Mucosa-Associated Lymphoid Tissue Lymphoma Translocation 1 Human genes 0.000 abstract 2
- 108700026676 Mucosa-Associated Lymphoid Tissue Lymphoma Translocation 1 Proteins 0.000 abstract 2
- 230000000468 autoproteolytic effect Effects 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- TUJKJAMUKRIRHC-UHFFFAOYSA-N hydroxyl Chemical class [OH] TUJKJAMUKRIRHC-UHFFFAOYSA-N 0.000 abstract 2
- 230000002797 proteolythic effect Effects 0.000 abstract 2
- -1 AMINO Chemical class 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- XFXPMWWXUTWYJX-UHFFFAOYSA-N Cyanide Chemical group N#[C-] XFXPMWWXUTWYJX-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000003993 interaction Effects 0.000 abstract 1
- 229940126601 medicinal product Drugs 0.000 abstract 1
- SONNWYBIRXJNDC-VIFPVBQESA-N phenylephrine Chemical class CNC[C@H](O)C1=CC=CC(O)=C1 SONNWYBIRXJNDC-VIFPVBQESA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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) | MX373846B (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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| MX342405B (es) | 2010-06-03 | 2016-09-28 | Pharmacyclics Inc | El uso de inhibidores de la tirosina quinasa de bruton (btk). |
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| JP6989505B2 (ja) | 2015-08-28 | 2022-01-05 | コーネル ユニヴァーシティー | Ｍａｌｔ１阻害剤およびその使用 |
| 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 |
| WO2018019755A1 (en) | 2016-07-26 | 2018-02-01 | Basf Se | Herbicidal pyridine compounds |
| WO2018019721A1 (en) | 2016-07-26 | 2018-02-01 | Basf Se | Herbicidal pyridine compounds |
| CR20190110A (es) | 2016-07-29 | 2019-08-27 | Lupin Ltd | Compuestos de tiazolo-piridina sustituida como inhibidores de malt1 |
| KR20190033607A (ko) | 2016-07-29 | 2019-03-29 | 루핀 리미티드 | Malt1 저해제로서의 치환 티아졸로-피리딘 화합물 |
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| 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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| EP3710441A1 (en) * | 2017-11-17 | 2020-09-23 | Hepagene Therapeutics, Inc. | Urea derivatives as inhibitors of ask1 |
| WO2019133809A1 (en) | 2017-12-28 | 2019-07-04 | The General Hospital Corporation | Targeting the cbm signalosome complex induces regulatory t cells to inflame the tumor microenvironment |
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| US11040031B2 (en) * | 2018-06-18 | 2021-06-22 | Janssen Pharmaceutica Nv | Pyrazole derivatives as MALT1 inhibitors |
| AU2019390863B2 (en) * | 2018-11-28 | 2025-02-20 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
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| EP3953345B1 (en) * | 2019-04-11 | 2023-04-05 | Janssen Pharmaceutica NV | Pyridine rings containing derivatives as malt1 inhibitors |
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| 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 |
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| US20230235077A1 (en) | 2020-06-24 | 2023-07-27 | The General Hospital Corporation | Materials and methods of treating cancer |
| EP4192833B1 (en) * | 2020-08-05 | 2026-01-21 | Richter Gedeon Nyrt. | Pharmacologically active heterocyclic-substituted pyrazolo[1,5-a]pyrimidine derivatives |
| EP4228647A4 (en) * | 2020-10-16 | 2024-09-11 | Rarefied Biosciences, Inc. | MALT1 MODULATORS AND THEIR USES |
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| TW202340198A (zh) * | 2022-01-28 | 2023-10-16 | 大陸商上海齊魯製藥研究中心有限公司 | 靶向ｍａｌｔ１的蛋白降解化合物、包含其的醫藥組合物及其用途 |
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