AR060545A1 - Compuestos de benzoaxol y benzotiazol 6-0- sustituidos y metodos de inhibicion de la senalizacion de csf-1r. composiciones farmaceuticas - Google Patents
Compuestos de benzoaxol y benzotiazol 6-0- sustituidos y metodos de inhibicion de la senalizacion de csf-1r. composiciones farmaceuticasInfo
- Publication number
- AR060545A1 AR060545A1 ARP070101682A ARP070101682A AR060545A1 AR 060545 A1 AR060545 A1 AR 060545A1 AR P070101682 A ARP070101682 A AR P070101682A AR P070101682 A ARP070101682 A AR P070101682A AR 060545 A1 AR060545 A1 AR 060545A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- heteroaryl
- alkyl
- alkynyl
- alkenyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 102100028198 Macrophage colony-stimulating factor 1 receptor Human genes 0.000 title 1
- 101710150918 Macrophage colony-stimulating factor 1 receptor Proteins 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 230000011664 signaling Effects 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 12
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 6
- 125000003342 alkenyl group Chemical group 0.000 abstract 5
- 125000000304 alkynyl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000005017 substituted alkenyl group Chemical group 0.000 abstract 5
- 125000004426 substituted alkynyl group Chemical group 0.000 abstract 5
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 3
- 125000003107 substituted aryl group Chemical group 0.000 abstract 3
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- -1 amino, substituted amino Chemical group 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 125000005415 substituted alkoxy group Chemical group 0.000 abstract 2
- 229940124597 therapeutic agent Drugs 0.000 abstract 2
- LELOWRISYMNNSU-UHFFFAOYSA-N Hydrocyanic acid Chemical group N#C LELOWRISYMNNSU-UHFFFAOYSA-N 0.000 abstract 1
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicinal Preparation (AREA)
Abstract
También se describen composiciones de los compuestos, ya sea solas o en combinacion con al menos un agente terapéutico adicional, con un portador farmacéuticamente aceptable, y usos de los compuestos, ya sea solos o en combinacion con al menos un agente terapéutico adicional. Reivindicacion 1: Un compuesto, estereoisomero, tautomero, solvato, oxido, éster o profármaco caracterizado porque tiene la formula (1) o una de sus sales farmacéuticamente aceptable en donde X es O, S o S(O); R1 y R2 están seleccionados, de modo independiente, del grupo que consiste en hidrogeno, alquilo, alquilo sustituido, acilo, cicloalquilo, cicloalquilo sustituido, cicloalquenilo, cicloalquenilo sustituido, arilo, arilo sustituido, heterociclilo, heterociclilo sustituido, heteroarilo y heteroarilo sustituido; o R1 y R2 se toman juntos para formar un grupo seleccionado de heterociclilo, heterociclilo sustituido, heteroarilo o heteroarilo sustituido; R3 está seleccionado del grupo que consiste en hidrogeno, halo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, carbonitrilo, arilo, arilo sustituido, cicloalquilo, cicloalquilo sustituido, cicloalquenilo, cicloalquenilo sustituido, heteroarilo, heteroarilo sustituido, heterociclilo, heterociclilo sustituido, amino, amino sustituido, acilo, acilamino, alcoxi, alcoxi sustituido, carboxilo, carboxiléster, sulfonilo sustituido, aminosulfonilo y aminocarbonilo; cada R6 es, de modo independiente, alquilo, alquilo sustituido! alcoxi, alcoxi sustituido, amino, amino sustituido o halo; n es 0, 1 o 2; y cuando X es O, R4 es hidrogeno, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo o alquinilo sustituido y R5 es hidrogeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, aminocarbonilo, halo, heteroarilo, heteroarilo sustituido, cicloalquilo o cicloalquilo sustituido o R4 y R5 se toman juntos para formar un grupo seleccionado de heterociclilo, heterociclilo sustituido, cicloalquilo, cicloalquilo sustituido, arilo, arilo sustituido, heteroarilo y heteroarilo sustituido; y cuando X es S o S(O), R4 es hidrogeno, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo o alquinilo sustituido y R5 es hidrogeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, aminocarbonilo, halo, heteroarilo, heteroarilo sustituido, cicloalquilo o cicloalquilo sustituido.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US79351706P | 2006-04-19 | 2006-04-19 | |
| US89385707P | 2007-03-08 | 2007-03-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR060545A1 true AR060545A1 (es) | 2008-06-25 |
Family
ID=38610468
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070101682A AR060545A1 (es) | 2006-04-19 | 2007-04-19 | Compuestos de benzoaxol y benzotiazol 6-0- sustituidos y metodos de inhibicion de la senalizacion de csf-1r. composiciones farmaceuticas |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US7553854B2 (es) |
| EP (1) | EP2010528B1 (es) |
| JP (1) | JP5328640B2 (es) |
| KR (1) | KR101464385B1 (es) |
| AR (1) | AR060545A1 (es) |
| AU (1) | AU2007237904B2 (es) |
| BR (1) | BRPI0710540B1 (es) |
| CA (1) | CA2649288C (es) |
| CR (1) | CR10365A (es) |
| CY (1) | CY1119679T1 (es) |
| DK (1) | DK2010528T3 (es) |
| EA (1) | EA018917B1 (es) |
| EC (1) | ECSP088830A (es) |
| ES (1) | ES2654847T3 (es) |
| HR (1) | HRP20171924T1 (es) |
| HU (1) | HUE035654T2 (es) |
| IL (1) | IL194662A0 (es) |
| LT (1) | LT2010528T (es) |
| MA (1) | MA30407B1 (es) |
| MX (1) | MX2008013427A (es) |
| NO (1) | NO20084800L (es) |
| PE (1) | PE20080359A1 (es) |
| PL (1) | PL2010528T3 (es) |
| PT (1) | PT2010528T (es) |
| RS (1) | RS56600B1 (es) |
| SI (1) | SI2010528T1 (es) |
| SM (1) | SMP200800063B (es) |
| TN (1) | TNSN08406A1 (es) |
| TW (1) | TW200813039A (es) |
| WO (1) | WO2007121484A2 (es) |
Families Citing this family (74)
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|---|---|---|---|---|
| ATE447404T1 (de) * | 2002-03-29 | 2009-11-15 | Novartis Vaccines & Diagnostic | Substituierte benzazole und ihre verwendung als raf-kinase-hemmer |
| MX2008013427A (es) * | 2006-04-19 | 2008-11-04 | Novartis Ag | Compuestos de benzoxazole y benzotiazole sustituidos-6-0 y metodos para inhibir la señalizacion csf-1r. |
| DK2120958T3 (da) * | 2006-12-06 | 2013-07-01 | Univ Central Florida Res Found | Stat3-inhibitor med anticancer-aktivitet og associerede fremgangsmåder |
| US8293769B2 (en) | 2007-05-21 | 2012-10-23 | Novartis Ag | CSF-1R inhibitors, compositions, and methods of use |
| CL2008001626A1 (es) | 2007-06-05 | 2009-06-05 | Takeda Pharmaceuticals Co | Compuestos derivados de heterociclos fusionados, agente farmaceutico que los comprende y su uso en la profilaxis y tratamiento del cancer. |
| JP5270553B2 (ja) * | 2007-08-23 | 2013-08-21 | 武田薬品工業株式会社 | 複素環化合物およびその用途 |
| JP2011500635A (ja) * | 2007-10-18 | 2011-01-06 | ノバルティス アーゲー | 癌および骨疾患の処置のためのcsf−1r阻害剤 |
| US20110009421A1 (en) * | 2008-02-27 | 2011-01-13 | Takeda Pharmaceutical Company Limited | Compound having 6-membered aromatic ring |
| WO2010064611A1 (ja) | 2008-12-01 | 2010-06-10 | 武田薬品工業株式会社 | 複素環化合物およびその用途 |
| JO3101B1 (ar) | 2008-12-02 | 2017-09-20 | Takeda Pharmaceuticals Co | مشتقات بنزوثيازول كعوامل مضادة للسرطان |
| WO2011133661A2 (en) * | 2010-04-21 | 2011-10-27 | Research Development Foundation | Methods and compositions related to dopaminergic neuronal cells |
| AR081626A1 (es) | 2010-04-23 | 2012-10-10 | Cytokinetics Inc | Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos |
| EP2560488B1 (en) | 2010-04-23 | 2015-10-28 | Cytokinetics, Inc. | Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use |
| AR081331A1 (es) | 2010-04-23 | 2012-08-08 | Cytokinetics Inc | Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos |
| US8937088B2 (en) | 2011-01-06 | 2015-01-20 | Astar Biotech Llc | Ureas for the treatment and prevention of cancer |
| US8759380B2 (en) * | 2011-04-22 | 2014-06-24 | Cytokinetics, Inc. | Certain heterocycles, compositions thereof, and methods for their use |
| BR112013028095B1 (pt) | 2011-05-05 | 2020-03-03 | Sloan-Kettering Institute For Cancer Research | Uso de inibidores de csf-1r para o tratamento de tumores cerebrais |
| WO2012151541A1 (en) * | 2011-05-05 | 2012-11-08 | Novartis Ag | Csf-1r inhibitors for treatment of brain tumors |
| MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
| CA2964367C (en) | 2014-10-14 | 2024-01-30 | Novartis Ag | Antibody molecules to pd-l1 and uses thereof |
| CN107206102A (zh) * | 2014-12-03 | 2017-09-26 | 豪夫迈·罗氏有限公司 | 抗金黄色葡萄球菌抗体利福霉素缀合物及其用途 |
| TW201630937A (zh) | 2014-12-22 | 2016-09-01 | 戊瑞治療有限公司 | 用於治療pvns之抗-csf1r抗體 |
| CN107683279B (zh) * | 2015-04-07 | 2020-11-03 | 广东众生睿创生物科技有限公司 | 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 |
| WO2016182988A1 (en) | 2015-05-08 | 2016-11-17 | Memorial Sloan Kettering Cancer Center | Compositions and methods for treatment of glioma |
| WO2017019896A1 (en) | 2015-07-29 | 2017-02-02 | Novartis Ag | Combination therapies comprising antibody molecules to pd-1 |
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| WO2017106656A1 (en) | 2015-12-17 | 2017-06-22 | Novartis Ag | Antibody molecules to pd-1 and uses thereof |
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| TWI753892B (zh) | 2016-03-28 | 2022-02-01 | 美商英塞特公司 | 作為tam抑制劑之吡咯并三嗪化合物 |
| EP3523285A4 (en) * | 2016-10-10 | 2020-04-22 | Development Center for Biotechnology | CHINOXALINE COMPOUNDS AS TYPE III RECEPTOR TYROSIN KINASE INHIBITORS |
| EP3526217B1 (en) * | 2016-10-14 | 2023-04-19 | Novartis AG | Crystalline forms of 4-(2-((1r,2r)-2-hydroxycyclohexylamino) benzothiazol-6-yloxy)-n-methylpicolinamide |
| CN109789209A (zh) | 2016-10-14 | 2019-05-21 | 诺华股份有限公司 | 使用csf-1r抑制剂治疗眼部疾病的方法 |
| WO2018083635A2 (en) | 2016-11-04 | 2018-05-11 | Auckland Uniservices Limited | Tricyclic heterocyclic derivatives and uses thereof |
| WO2018119387A1 (en) * | 2016-12-23 | 2018-06-28 | Tesaro, Inc. | Small molecule inhibitors of colony stimulating factor-1 receptor (csf-1r) and uses thereof |
| WO2018146641A1 (en) * | 2017-02-11 | 2018-08-16 | Invictus Oncology Pvt. Ltd. | Novel inhibitors of cellular signalling |
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| WO2019113469A1 (en) | 2017-12-07 | 2019-06-13 | The Regents Of The University Of Michigan | Nsd family inhibitors and methods of treatment therewith |
| TWI869346B (zh) | 2018-05-30 | 2025-01-11 | 瑞士商諾華公司 | Entpd2抗體、組合療法、及使用該等抗體和組合療法之方法 |
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| MD3813800T2 (ro) | 2018-06-29 | 2025-10-31 | Incyte Corp | Formulări de inhibitor al AXL/MER |
| AR116109A1 (es) | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
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| KR20210106437A (ko) | 2018-12-20 | 2021-08-30 | 노파르티스 아게 | 3-(1-옥소이소인돌린-2-일)피페리딘-2,6-디온 유도체를 포함하는 투약 요법 및 약학적 조합물 |
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