AR058285A1 - Compuestos derivados de tiadiazolidinonas y composicion farmaceutica - Google Patents
Compuestos derivados de tiadiazolidinonas y composicion farmaceuticaInfo
- Publication number
- AR058285A1 AR058285A1 ARP060105391A ARP060105391A AR058285A1 AR 058285 A1 AR058285 A1 AR 058285A1 AR P060105391 A ARP060105391 A AR P060105391A AR P060105391 A ARP060105391 A AR P060105391A AR 058285 A1 AR058285 A1 AR 058285A1
- Authority
- AR
- Argentina
- Prior art keywords
- amino
- alkoxy
- heterocyclyl
- cycloalkyl
- aryl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 7
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- -1 alkyloxy-alkoxy Chemical group 0.000 abstract 4
- 125000004104 aryloxy group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical group 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 102000002727 Protein Tyrosine Phosphatase Human genes 0.000 abstract 3
- 125000003282 alkyl amino group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 3
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 108020000494 protein-tyrosine phosphatase Proteins 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000001054 5 membered carbocyclic group Chemical group 0.000 abstract 2
- 125000003627 8 membered carbocyclic group Chemical group 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 2
- 125000004001 thioalkyl group Chemical group 0.000 abstract 2
- 125000005000 thioaryl group Chemical group 0.000 abstract 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 2
- ZMWAXVAETNTVAT-UHFFFAOYSA-N 7-n,8-n,5-triphenylphenazin-5-ium-2,3,7,8-tetramine;chloride Chemical compound [Cl-].C=1C=CC=CC=1NC=1C=C2[N+](C=3C=CC=CC=3)=C3C=C(N)C(N)=CC3=NC2=CC=1NC1=CC=CC=C1 ZMWAXVAETNTVAT-UHFFFAOYSA-N 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 201000009030 Carcinoma Diseases 0.000 abstract 1
- 208000035473 Communicable disease Diseases 0.000 abstract 1
- 208000032928 Dyslipidaemia Diseases 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 208000002705 Glucose Intolerance Diseases 0.000 abstract 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 abstract 1
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010022489 Insulin Resistance Diseases 0.000 abstract 1
- 208000017170 Lipid metabolism disease Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 206010033645 Pancreatitis Diseases 0.000 abstract 1
- 102000014400 SH2 domains Human genes 0.000 abstract 1
- 108050003452 SH2 domains Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 210000001789 adipocyte Anatomy 0.000 abstract 1
- 210000004204 blood vessel Anatomy 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 abstract 1
- 208000006575 hypertriglyceridemia Diseases 0.000 abstract 1
- 210000000987 immune system Anatomy 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 208000002551 irritable bowel syndrome Diseases 0.000 abstract 1
- 208000023589 ischemic disease Diseases 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 230000000626 neurodegenerative effect Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- DCWXELXMIBXGTH-UHFFFAOYSA-N phosphotyrosine Chemical compound OC(=O)C(N)CC1=CC=C(OP(O)(O)=O)C=C1 DCWXELXMIBXGTH-UHFFFAOYSA-N 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 abstract 1
- 150000003573 thiols Chemical group 0.000 abstract 1
- 230000002792 vascular Effects 0.000 abstract 1
Classifications
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- 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
- C07D417/10—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 carbon chain containing aromatic 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
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- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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-
- A—HUMAN NECESSITIES
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- 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]
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
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- A—HUMAN NECESSITIES
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- 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
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- 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
- A61P9/12—Antihypertensives
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- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
Abstract
Los compuestos de la Formula (1) son inhibidores de fosfatasas de proteína tirosina (PTPasas), y por lo tanto, se pueden emplear para el tratamiento de las condiciones mediadas por la actividad de la PTPasa. Los compuestos de la presente invencion también se pueden emplear como inhibidores de otras enzimas caracterizadas por una region de enlace de fosfotirosina, tal como el dominio SH2. De acuerdo con lo anterior, los compuestos de la Formula 1 se pueden emplear para la prevencion y/o el tratamiento de resistencia a la insulina asociada con obesidad, intolerancia a la glucosa, diabetes mellitus, hipertension y enfermedades isquémicas de los vasos sanguíneos grandes y pequenos, condiciones que acompanan a la diabetes tipo 2, incluyendo hiperlipidemia, hipertrigliceridemia, ateroesclerosis, restenosis vascular, síndrome de intestino irritable, pancreatitis, tumores de células adiposas y carcinomas, tales como liposaecoma, dislipidemia, y otros trastornos en donde se indique la resistencia a la indulina. En adicion, los compuestos de la presente invencion se pueden emplear para tratar y/o prevenir cáncer, osteoporosis, enfermedades neurodegenerativas e infecciosas, y enfermedades que involucren inflamacion y al sistema inmune. Composicion farmacéutica en base al compuesto y uso de este para prepararla. Reivindicacion 1: Un compuesto de la formula (1) en donde: R1 es hidrogeno, -C(O)R2, -C(O)NR3R4 o -C(O)OR5, en donde: R2 y R3 son, independientemente uno del otro, hidrogeno, cicloalquilo, arilo, heterociclilo, aralquilo, heteroaralquilo, o alquilo opcionalmente sustituido por uno a cuatro sustituyentes seleccionados a partir del grupo que consiste en halogeno, cicloalquilo, cicloalcoxilo, alcoxilo, alquiloxi-alcoxilo, amino, alquil-amino, dialquil-amino, arilo, ariloxilo, y heterociclílo; R4 y R5 son, independientemente uno del otro, cicloalquilo, arilo, heterociclílo, aralquilo, heteroaralquilo, o alquilo opcionalmente sustituido por uno a cuatro sustituyentes seleccionados a partir del grupo que consiste en halogeno, cicloalquilo, cicloalcoxilo, alcoxilo, alquiloxi-alcoxilo, amino, alquil-amino, dialquil-amino, arilo, ariloxilo, y heterociclílo; U, W y V son , independientemente, unos de otros, hidrogeno, hidroxilo, halogeno, ciano, nitro, alcoxilo, tioalquilo, tionoalquilo, sulfonilo, carboxilo libre o esterificado, carbamoílo, sulfamoílo, amino opcionalmente sustituido, cicloalquilo, arilo, ariloxilo, tioarilo, heterociclílo, heterociclíloxilo, alquenilo, alquinilo, o alquilo (de 1 a 8 átomos de carbono) opcionalmente sustituido por uno o cuatro sustituyentes seleccionados a partir del grupo que consiste en halogeno, hidroxilo, cicloalquilo, cicloalcoxilo, acilo, aciloxilo, alcoxilo, alquiloxi-alcoxilo, amino, alquil-amino, dialquil-amino, acil-amino, carbamoílo, tiol, tioalquilo, tionoalquilo, sulfonilo, sulfonamido, sulfamoílo, nitro, ciano, carboxilo libre o esterificado, arilo, ariloxilo, tioarilo, alquenilo, alquinilo, aralcoxilo, heteroaralcoxilo, heterociclilo, y heterocicliloxolo; o U y W, combinados junto con los átomos de carbono con los que están unidos, forman un anillo carbocíclico o heterocíclico de 5 a 8 miembros, aromático, o no aromático parcial o completamentesaturado, opcionalmente sustituido; o W y V, combinados junto con los átomos de carbono con los que están unidos, forman un anillo carbocíclico o heterocíclico de 5 a 8 miembros,aromático, o no aromático parcial o completamente saturado opcioanlmente sustituido; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US74849205P | 2005-12-08 | 2005-12-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR058285A1 true AR058285A1 (es) | 2008-01-30 |
Family
ID=37903424
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060105391A AR058285A1 (es) | 2005-12-08 | 2006-12-06 | Compuestos derivados de tiadiazolidinonas y composicion farmaceutica |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US8252820B2 (es) |
| EP (1) | EP1963293A1 (es) |
| JP (1) | JP2009518419A (es) |
| KR (1) | KR20080075218A (es) |
| CN (1) | CN101336235A (es) |
| AR (1) | AR058285A1 (es) |
| AU (1) | AU2006321902B2 (es) |
| BR (1) | BRPI0619567A2 (es) |
| CA (1) | CA2631007A1 (es) |
| CR (1) | CR10047A (es) |
| EC (1) | ECSP088509A (es) |
| GT (1) | GT200800093A (es) |
| IL (1) | IL191711A0 (es) |
| MA (1) | MA30018B1 (es) |
| NO (1) | NO20083030L (es) |
| NZ (1) | NZ568663A (es) |
| PE (2) | PE20100470A1 (es) |
| RU (1) | RU2008127262A (es) |
| TN (1) | TNSN08248A1 (es) |
| TW (1) | TW200800928A (es) |
| UA (1) | UA94921C2 (es) |
| WO (1) | WO2007067612A1 (es) |
| ZA (1) | ZA200804489B (es) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0619543A2 (pt) * | 2005-12-08 | 2011-10-04 | Novartis Ag | derivados de 1,2,5-tiazolidina, composições farmacêuticas contendo os mesmos e referidos usos |
| BRPI0619547A2 (pt) * | 2005-12-08 | 2011-10-04 | Novartis Ag | 1,1,3-trioxo-1,2,5-tiadiazolidinas, composição farmacêutica e uso das mesmas |
| WO2007115058A2 (en) * | 2006-03-31 | 2007-10-11 | Novartis Ag | Thiadiazolidinone inhibitors of ptpase |
| DE102007015169A1 (de) * | 2007-03-27 | 2008-10-02 | Universität des Saarlandes Campus Saarbrücken | 17Beta-Hydroxysteroid-Dehydrogenase-Typ1-Inhibitoren zur Behandlung hormonabhängiger Erkrankungen |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| CN103201244B (zh) * | 2010-08-26 | 2015-06-17 | 阿尔比马尔公司 | 用于制备1-溴代-2-(环丙基甲氧基)-5-氟代-4-甲氧基苯的方法 |
| AU2011313191A1 (en) | 2010-10-08 | 2013-05-02 | Mochida Pharmaceutical Co., Ltd. | Cyclic amide derivative |
| EP2683699B1 (de) | 2011-03-08 | 2015-06-24 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| WO2012120052A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2683700B1 (de) | 2011-03-08 | 2015-02-18 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683704B1 (de) | 2011-03-08 | 2014-12-17 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| WO2012120054A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| CA2834465A1 (en) | 2011-04-28 | 2012-11-01 | Mochida Pharmaceutical Co., Ltd. | Cyclic amide derivative |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2017078499A2 (ko) * | 2015-11-06 | 2017-05-11 | 경북대학교 산학협력단 | 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물 |
| PE20210372A1 (es) * | 2018-06-21 | 2021-02-26 | Abbvie Inc | Inhibidores de proteina tirosina fosfatasa y sus metodos de uso |
| KR20210060514A (ko) | 2018-09-18 | 2021-05-26 | 바스프 에스이 | 디아미노트리아진 화합물 |
| MX2021010544A (es) * | 2019-03-14 | 2021-10-01 | Calico Life Sciences Llc | Inhibidores de la proteina tirosina fosfatasa y metodos para usarlos. |
| JP2023507774A (ja) * | 2019-12-18 | 2023-02-27 | カリコ ライフ サイエンシーズ エルエルシー | タンパク質チロシンホスファターゼ阻害剤及びそれらの使用方法 |
| US20240383886A1 (en) * | 2019-12-20 | 2024-11-21 | Calico Life Sciences Llc | Protein Tyrosine Phosphatase Degraders and Methods of Use Thereof |
| JP2023542503A (ja) * | 2020-09-11 | 2023-10-10 | カリコ ライフ サイエンシーズ エルエルシー | タンパク質チロシンホスファターゼ阻害物質及びその使用方法 |
| KR20230137954A (ko) | 2021-01-27 | 2023-10-05 | 바스프 에스이 | 디아미노트리아진 화합물 |
| EP4305030A1 (en) * | 2021-03-11 | 2024-01-17 | Kumquat Biosciences Inc. | Heterocycles and uses thereof |
| MX2024005656A (es) * | 2021-11-11 | 2024-08-06 | Calico Life Sciences Llc | Inhibidores de proteina tirosina fosfatasa y metodos de uso de estos. |
| AU2022387106A1 (en) * | 2021-11-11 | 2024-05-23 | Abbvie Inc. | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| AR128379A1 (es) | 2022-01-31 | 2024-04-24 | Bristol Myers Squibb Co | Inhibidores de la proteína tirosina fosfatasa, composiciones y métodos de uso |
| EP4472958A1 (en) * | 2022-02-02 | 2024-12-11 | Nerio Therapeutics, Inc. | Protein tyrosine phosphatase inhibitors and uses thereof |
| CN119137117A (zh) * | 2022-02-02 | 2024-12-13 | 耐瑞欧医疗公司 | 蛋白酪氨酸磷酸酶抑制剂及其用途 |
| WO2023150150A1 (en) * | 2022-02-02 | 2023-08-10 | Nerio Therapeutics, Inc. | Protein tyrosine phosphatase inhibitors and uses thereof |
| WO2024059041A1 (en) * | 2022-09-13 | 2024-03-21 | Kumquat Biosciences, Inc. | Benzo-fused n-heterocycles and uses thereof |
| WO2024067802A1 (zh) * | 2022-09-30 | 2024-04-04 | 深圳众格生物科技有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其制备方法和医药用途 |
| TW202432118A (zh) * | 2022-11-09 | 2024-08-16 | 美商必治妥美雅史谷比公司 | 蛋白質酪胺酸磷酸酶抑制劑、其組合物及使用方法 |
| WO2024137727A1 (en) * | 2022-12-21 | 2024-06-27 | Bristol-Myers Squibb Company | 1,2,4-thiazolidin-3-one-1,1-dioxide inhibitors of protein tyrosine phosphatase, compositions, and methods of use |
| WO2024141015A1 (en) * | 2022-12-30 | 2024-07-04 | Insilico Medicine Ip Limited | Protein tyrosine phosphatase inhibitors and uses thereof |
| CN118852335A (zh) * | 2023-04-28 | 2024-10-29 | 中科中山药物创新研究院 | 噻二唑烷酮衍生物及其制备方法和应用 |
| WO2025011570A1 (zh) * | 2023-07-11 | 2025-01-16 | 深圳众格生物科技有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其组合物、医药用途 |
| WO2025016906A1 (en) * | 2023-07-14 | 2025-01-23 | Katholieke Universiteit Leuven | Novel compounds for the treatment of cancer and metabolic diseases |
| CN117343052B (zh) * | 2023-12-04 | 2024-02-06 | 英矽智能科技(上海)有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002076439A2 (en) * | 2001-03-23 | 2002-10-03 | The Board Of Trustees Of The University Of Illinois | Compounds capable of modulating the activity of multidrug transporters and therapeutic use of the same |
| PT1492780E (pt) * | 2002-04-03 | 2012-04-11 | Novartis Ag | Derivados 5-substituídos de 1,1-dioxo-1,2,5-tiazolidina-3- -ona como inibidores de ptpase 1b |
| GB0225986D0 (en) * | 2002-11-07 | 2002-12-11 | Astrazeneca Ab | Chemical compounds |
| GB0227813D0 (en) | 2002-11-29 | 2003-01-08 | Astrazeneca Ab | Chemical compounds |
| CA2511818A1 (en) * | 2002-12-30 | 2004-07-29 | Jeffrey O. Saunders | Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders |
| US7135575B2 (en) * | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| WO2005035551A2 (en) * | 2003-10-08 | 2005-04-21 | Incyte Corporation | Inhibitors of proteins that bind phosphorylated molecules |
| BRPI0619543A2 (pt) | 2005-12-08 | 2011-10-04 | Novartis Ag | derivados de 1,2,5-tiazolidina, composições farmacêuticas contendo os mesmos e referidos usos |
| BRPI0619547A2 (pt) | 2005-12-08 | 2011-10-04 | Novartis Ag | 1,1,3-trioxo-1,2,5-tiadiazolidinas, composição farmacêutica e uso das mesmas |
| UA94724C2 (en) | 2005-12-08 | 2011-06-10 | Новартис Аг | Thiadiazolidinone derivatives as antidiabetic agents |
| WO2007115058A2 (en) | 2006-03-31 | 2007-10-11 | Novartis Ag | Thiadiazolidinone inhibitors of ptpase |
-
2006
- 2006-06-12 UA UAA200807752A patent/UA94921C2/ru unknown
- 2006-12-06 AR ARP060105391A patent/AR058285A1/es not_active Application Discontinuation
- 2006-12-06 RU RU2008127262/04A patent/RU2008127262A/ru not_active Application Discontinuation
- 2006-12-06 CN CNA2006800524439A patent/CN101336235A/zh active Pending
- 2006-12-06 EP EP06844889A patent/EP1963293A1/en not_active Withdrawn
- 2006-12-06 WO PCT/US2006/046542 patent/WO2007067612A1/en active Application Filing
- 2006-12-06 CA CA002631007A patent/CA2631007A1/en not_active Abandoned
- 2006-12-06 BR BRPI0619567-9A patent/BRPI0619567A2/pt not_active IP Right Cessation
- 2006-12-06 KR KR1020087016433A patent/KR20080075218A/ko not_active Application Discontinuation
- 2006-12-06 NZ NZ568663A patent/NZ568663A/en not_active IP Right Cessation
- 2006-12-06 PE PE2010000301A patent/PE20100470A1/es not_active Application Discontinuation
- 2006-12-06 JP JP2008544464A patent/JP2009518419A/ja active Pending
- 2006-12-06 AU AU2006321902A patent/AU2006321902B2/en not_active Ceased
- 2006-12-06 PE PE2006001572A patent/PE20071094A1/es not_active Application Discontinuation
- 2006-12-06 US US12/096,432 patent/US8252820B2/en not_active Expired - Fee Related
- 2006-12-07 TW TW095145872A patent/TW200800928A/zh unknown
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2008
- 2008-05-26 IL IL191711A patent/IL191711A0/en unknown
- 2008-05-27 ZA ZA200804489A patent/ZA200804489B/xx unknown
- 2008-06-02 MA MA30986A patent/MA30018B1/fr unknown
- 2008-06-05 CR CR10047A patent/CR10047A/es not_active Application Discontinuation
- 2008-06-06 EC EC2008008509A patent/ECSP088509A/es unknown
- 2008-06-06 GT GT200800093A patent/GT200800093A/es unknown
- 2008-06-06 TN TNP2008000248A patent/TNSN08248A1/en unknown
- 2008-07-04 NO NO20083030A patent/NO20083030L/no not_active Application Discontinuation
Also Published As
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|---|---|
| CA2631007A1 (en) | 2007-06-14 |
| PE20071094A1 (es) | 2008-01-07 |
| US20100035942A1 (en) | 2010-02-11 |
| US8252820B2 (en) | 2012-08-28 |
| UA94921C2 (en) | 2011-06-25 |
| JP2009518419A (ja) | 2009-05-07 |
| IL191711A0 (en) | 2008-12-29 |
| AU2006321902A1 (en) | 2007-06-14 |
| ZA200804489B (en) | 2009-08-26 |
| RU2008127262A (ru) | 2010-01-20 |
| TW200800928A (en) | 2008-01-01 |
| KR20080075218A (ko) | 2008-08-14 |
| MA30018B1 (fr) | 2008-12-01 |
| ECSP088509A (es) | 2008-07-30 |
| GT200800093A (es) | 2010-07-09 |
| TNSN08248A1 (en) | 2009-10-30 |
| CN101336235A (zh) | 2008-12-31 |
| AU2006321902B2 (en) | 2011-11-10 |
| WO2007067612A1 (en) | 2007-06-14 |
| BRPI0619567A2 (pt) | 2011-10-04 |
| PE20100470A1 (es) | 2010-07-13 |
| NZ568663A (en) | 2011-07-29 |
| CR10047A (es) | 2008-10-16 |
| NO20083030L (no) | 2008-08-28 |
| EP1963293A1 (en) | 2008-09-03 |
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