AR072622A1 - Derivados de imidazo[2,1-b][1,3,4]tiadiazol, composiciones farmaceuticas que los comprenden, metodo para prepararlos, y uso de los mismos para el tratamiento de tumores y otras enfermedades inducidas por quinasas - Google Patents
Derivados de imidazo[2,1-b][1,3,4]tiadiazol, composiciones farmaceuticas que los comprenden, metodo para prepararlos, y uso de los mismos para el tratamiento de tumores y otras enfermedades inducidas por quinasasInfo
- Publication number
- AR072622A1 AR072622A1 ARP090102879A ARP090102879A AR072622A1 AR 072622 A1 AR072622 A1 AR 072622A1 AR P090102879 A ARP090102879 A AR P090102879A AR P090102879 A ARP090102879 A AR P090102879A AR 072622 A1 AR072622 A1 AR 072622A1
- Authority
- AR
- Argentina
- Prior art keywords
- atoms
- independently
- denotes
- cyc
- tumors
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000005488 carboaryl group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- MZAGXDHQGXUDDX-JSRXJHBZSA-N (e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/C(N)=O MZAGXDHQGXUDDX-JSRXJHBZSA-N 0.000 abstract 1
- 108091005682 Receptor kinases Proteins 0.000 abstract 1
- 102000004887 Transforming Growth Factor beta Human genes 0.000 abstract 1
- 108090001012 Transforming Growth Factor beta Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- UVNXNSUKKOLFBM-UHFFFAOYSA-N imidazo[2,1-b][1,3,4]thiadiazole Chemical class N1=CSC2=NC=CN21 UVNXNSUKKOLFBM-UHFFFAOYSA-N 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Biomedical Technology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Communicable Diseases (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- AIDS & HIV (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Derivados de imidazo[2,1-b][1,3,4]tiadiazol de la formula (1) en donde R1 es carboarilo mono- o bicíclico no sustituido o heteroarilo mono- o bicíclico no sustituido que tiene 1 a 4 átomos de N, O y/o S, cada uno de los cuales puede estar sustituido con al menos un sustituyente seleccionado del grupo de A, Hal, -CN, -(CH2)nOR3, -CO-R3, -CO-NR3R3, -CO-N(R3)2, -(CH2)nNR3R3, -(CH2)nN(R3)2 y -SO2N(R3)2; R2 es A' o Cyc; R3 denota, de modo independiente entre sí, en R1, A' y Cyc: H, A, -OH, -OA, acilo o carboarilo opcionalmente sustituido; A denota, de modo independiente entre sí, en R1 y R3: alquilo no ramificado o ramificado que tiene 1-10 átomos de C, en donde uno o dos grupos CH2 no adyacentes pueden estar reemplazados por N y/o NH, y/o además, 1-7 átomos de H pueden estar reemplazados por Hal, -OH, morfolina y/o amino; y A' denota alquilo no ramificado o ramificado que tiene 1-10 átomos de C, en donde 1-7 átomos de H pueden estar reemplazados por Cyc, -OR3, -NR3R3, -N(R3)2, Het1 y carboarilo opcionalmente sustituido; Het1 denota, de modo independiente entre sí, en R1 y A': heterociclo mono- o bicíclico saturado, insaturado o aomático que tiene 1 a 4 átomos de N, O y/o S, opcionalmente sustituido con =O; Cyc denota, de modo independiente entre sí, en R2, R3 y A': cicloalquilo que tiene 3-7 átomos de C, que puede estar sustituido con -OR3, -NR3R3 o -N(R3)2; Hal denota, de modo independiente entre sí, en R1 y A: F, Cl, Br o I; y n es 0, 1, 2, 3 o 4; y /o sus sales fisiologicamente aceptables. Son inhibidores de la quinasa del receptor I TGF-beta y se pueden emplear, inter alia, para el tratamiento de tumores.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08013574 | 2008-07-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR072622A1 true AR072622A1 (es) | 2010-09-08 |
Family
ID=41009860
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090102879A AR072622A1 (es) | 2008-07-29 | 2009-07-29 | Derivados de imidazo[2,1-b][1,3,4]tiadiazol, composiciones farmaceuticas que los comprenden, metodo para prepararlos, y uso de los mismos para el tratamiento de tumores y otras enfermedades inducidas por quinasas |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8389554B2 (es) |
| EP (1) | EP2307425B1 (es) |
| JP (1) | JP2011529456A (es) |
| AR (1) | AR072622A1 (es) |
| AU (1) | AU2009275544B2 (es) |
| CA (1) | CA2732186A1 (es) |
| ES (1) | ES2470681T3 (es) |
| IL (1) | IL210869A (es) |
| WO (1) | WO2010012345A1 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE025976T2 (en) | 2007-09-27 | 2016-05-30 | Fund Centro Nac De Investig Oncologicas Carlos Iii | Imidazolothiadiazoles for use as protein kinase inhibitors |
| SG175001A1 (en) | 2009-04-02 | 2011-11-28 | Ct Nac Investigaciones Oncologicas Cnio | Imidazo [2, 1-b] [ 1, 3, 4 ] thiadiazole derivatives |
| WO2012020217A1 (en) | 2010-08-09 | 2012-02-16 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Amino- imidazolothiadiazoles for use as protein or lipid kinase inhibitors |
| WO2012020215A1 (en) | 2010-08-09 | 2012-02-16 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Amino- imidazolothiadiazoles for use as protein or lipid kinase inhibitors |
| EP2671885A1 (en) * | 2012-06-05 | 2013-12-11 | Ares Trading S.A. | Imidazo-oxadiazole and Imidazo-thiadiazole derivatives |
| EP3515916B1 (en) | 2016-09-22 | 2023-06-07 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| TW202500565A (zh) | 2016-10-24 | 2025-01-01 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
| WO2018218133A1 (en) | 2017-05-26 | 2018-11-29 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| EP3687997A1 (en) | 2017-09-29 | 2020-08-05 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| EP3755699A1 (en) * | 2018-02-21 | 2020-12-30 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| EP3768680A1 (en) | 2018-03-21 | 2021-01-27 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof |
| EP3768668B1 (en) | 2018-03-21 | 2024-08-28 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| MY200452A (en) | 2018-08-21 | 2023-12-27 | Kyorin Seiyaku Kk | Bicyclic heteroaromatic ring derivative |
| KR20220066923A (ko) | 2019-09-24 | 2022-05-24 | 릴레이 테라퓨틱스, 인크. | Shp2 포스파테이스 억제제 및 이의 제조 및 사용 방법 |
| EP4048678A4 (en) * | 2019-10-21 | 2023-10-18 | Novartis AG | COMPOUNDS AND COMPOSITIONS FOR TREATING PARASITIC DISEASES |
| JP2023541262A (ja) * | 2020-09-14 | 2023-09-29 | ザ ユニバーシティー オブ サセックス | Ｌｅｍｕｒチロシンキナーゼ３の小分子阻害剤 |
| CN114195736B (zh) * | 2021-12-30 | 2023-08-04 | 浙江闰土染料有限公司 | 2-氨基-5-溴-1,3,4-噻二唑的制备方法 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005509616A (ja) * | 2001-10-16 | 2005-04-14 | センジェント・セラピューティクス・インク | チロシンホスファターゼに対する有機硫黄阻害剤 |
| PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
| DE102005061840A1 (de) | 2005-12-23 | 2007-06-28 | Merck Patent Gmbh | Triazolderivate |
| WO2007118318A1 (en) | 2006-04-13 | 2007-10-25 | Aegera Therapeutics Inc. | USE OF IMIDAZO[2,1-b)]-1,3,4-THIADIAZOLE-2-SULFONAMIDE COMPOUNDS TO TREAT NEUROPATHIC PAIN |
| HUE025976T2 (en) * | 2007-09-27 | 2016-05-30 | Fund Centro Nac De Investig Oncologicas Carlos Iii | Imidazolothiadiazoles for use as protein kinase inhibitors |
-
2009
- 2009-07-01 EP EP09776906.1A patent/EP2307425B1/en not_active Not-in-force
- 2009-07-01 US US13/056,331 patent/US8389554B2/en not_active Expired - Fee Related
- 2009-07-01 AU AU2009275544A patent/AU2009275544B2/en not_active Ceased
- 2009-07-01 ES ES09776906.1T patent/ES2470681T3/es active Active
- 2009-07-01 JP JP2011520340A patent/JP2011529456A/ja active Pending
- 2009-07-01 CA CA2732186A patent/CA2732186A1/en not_active Abandoned
- 2009-07-01 WO PCT/EP2009/004753 patent/WO2010012345A1/en not_active Ceased
- 2009-07-29 AR ARP090102879A patent/AR072622A1/es unknown
-
2011
- 2011-01-25 IL IL210869A patent/IL210869A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| EP2307425B1 (en) | 2014-03-26 |
| WO2010012345A1 (en) | 2010-02-04 |
| AU2009275544A1 (en) | 2010-02-04 |
| IL210869A (en) | 2014-01-30 |
| JP2011529456A (ja) | 2011-12-08 |
| AU2009275544B2 (en) | 2013-09-12 |
| EP2307425A1 (en) | 2011-04-13 |
| US20110130396A1 (en) | 2011-06-02 |
| US8389554B2 (en) | 2013-03-05 |
| IL210869A0 (en) | 2011-04-28 |
| CA2732186A1 (en) | 2010-02-04 |
| ES2470681T3 (es) | 2014-06-24 |
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