AR040075A2 - 1h-pirimido[4,5-d]pirimidin-2-onas y sales, composiciones farmaceuticas y uso para la fabricacion de un medicamento - Google Patents
1h-pirimido[4,5-d]pirimidin-2-onas y sales, composiciones farmaceuticas y uso para la fabricacion de un medicamentoInfo
- Publication number
- AR040075A2 AR040075A2 ARP030101602A ARP030101602A AR040075A2 AR 040075 A2 AR040075 A2 AR 040075A2 AR P030101602 A ARP030101602 A AR P030101602A AR P030101602 A ARP030101602 A AR P030101602A AR 040075 A2 AR040075 A2 AR 040075A2
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- aryl
- ring
- heteroaryl
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 229940126601 medicinal product Drugs 0.000 title 1
- 239000001257 hydrogen Substances 0.000 abstract 16
- 229910052739 hydrogen Inorganic materials 0.000 abstract 16
- 150000002431 hydrogen Chemical class 0.000 abstract 15
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000001072 heteroaryl group Chemical group 0.000 abstract 9
- 125000000623 heterocyclic group Chemical group 0.000 abstract 9
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 8
- 125000003107 substituted aryl group Chemical group 0.000 abstract 8
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 7
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 6
- 229910052760 oxygen Inorganic materials 0.000 abstract 6
- 239000001301 oxygen Substances 0.000 abstract 6
- 239000011593 sulfur Chemical group 0.000 abstract 6
- 229910052717 sulfur Inorganic materials 0.000 abstract 6
- 150000003839 salts Chemical class 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- -1 aryl-C1-10 alkyl Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 3
- 102100023482 Mitogen-activated protein kinase 14 Human genes 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- JPOJBQLUJAIHHL-UHFFFAOYSA-N 1h-pyrimido[4,5-d]pyrimidin-2-one Chemical compound N1=CN=C2NC(=O)N=CC2=C1 JPOJBQLUJAIHHL-UHFFFAOYSA-N 0.000 abstract 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 abstract 1
- 208000017667 Chronic Disease Diseases 0.000 abstract 1
- 206010012689 Diabetic retinopathy Diseases 0.000 abstract 1
- 108010084680 Heterogeneous-Nuclear Ribonucleoprotein K Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 206010028289 Muscle atrophy Diseases 0.000 abstract 1
- 206010035664 Pneumonia Diseases 0.000 abstract 1
- 206010057190 Respiratory tract infections Diseases 0.000 abstract 1
- 241000700605 Viruses Species 0.000 abstract 1
- XOCUXOWLYLLJLV-UHFFFAOYSA-N [O].[S] Chemical compound [O].[S] XOCUXOWLYLLJLV-UHFFFAOYSA-N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 201000009240 nasopharyngitis Diseases 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 208000020029 respiratory tract infectious disease Diseases 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
- 241000712461 unidentified influenza virus Species 0.000 abstract 1
Classifications
-
- 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
-
- 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
- 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
-
- 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
- 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
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P17/06—Antipsoriatics
-
- 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
- A61P17/16—Emollients or protectives, e.g. against radiation
-
- 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
-
- 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
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- 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
-
- 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
- A61P31/04—Antibacterial agents
-
- 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
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Communicable Diseases (AREA)
- Neurosurgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Ophthalmology & Optometry (AREA)
- Endocrinology (AREA)
- Molecular Biology (AREA)
- Psychiatry (AREA)
Abstract
1H-pirimido[4,5-d]pirimidin-2-ona que tiene la siguientes fórmula (1); donde R1, X y R3 son seleccionados respectivamente de los grupos a) R11, X1, y R13; b) R31, X3 y R33; y c) R51, X5 y R53; a) donde: R11 es un anillo arilo o heteroarilo, cuyo anillo está opcionalmente sustituido; R12 es hidrógeno, alquilo C1-10, cicloalquilo C3-7, cicloalquil(C3-7)-alquilo(C1-10), arilo, aril-alquilo C1-10, heteroarilo, heteroaril-alquilo C1-10, heterocíclico, o un resto heterociclil-alquilo C1-10; y en el que cada uno de estos restos, excluyendo hidrógeno, está opcionalmente sustituido; R13 es un resto alquilo C1-10, cicloalquilo C3-7, cicloalquil(C3-7)-alquilo(C1-10), aril-alquilo C1-10, heteroaril-alquilo C1-10, o heterociclil-alquilo C1-10; y en el que cada uno de estos restos están opcionalmente sustituidos; X1 es R12, OR12, S(O)mR12 o (CH2)nNR14R15, o (CH2)nNR12R14; n es 0 o un número entero que tiene un valor de 1 a 10; m es 0 o un número entero que tiene un valor de 1 ó 2; R14 y R15 se seleccionan cada uno independientemente de hidrógeno, alquilo C1-4 opcionalmente sustituido, arilo opcionalmente sustituido, o un aril-alquilo C1-4 opcionalmente sustituido, o R14 y R15 junto con el nitrógeno al que están unidos forman un anillo heterocíclico de 5 a 7 miembros, cuyo anillo contiene opcionalmente un heteroátomo adicional seleccionado de oxígeno, azufre o NR19; R16 es hidrógeno, alquilo C1-10, cicloalquilo C3-7, heterociclilo, heterociclil-alquilo C1-10, arilo, aril-alquilo C1-10, heteroarilo o un resto heteroaril-alquilo C1-10; y en el que cada uno de estos restos, excluyendo hidrógeno, puede estar opcionalmente sustituido; R19 es hidrógeno, C(Z)R16, alquilo C1-10 opcionalmente sustituido, arilo opcionalmente sustituido, o aril-alquilo C1-4 opcionalmente sustituido, Z es oxígeno o azufre; o una de sus sales farmacéuticamente aceptables; b) donde: R31 es un arilo, o un anillo heteroarilo, cuyo anillo está opcionalmente sustituido; R32 es un anillo heterocíclico o heterocíclico-alquilo C1-10, cuyo anillo está opcionalmente sustituido; R32' es un anillo heterocíclico, heterocíclico-alquilo C1-10, arilo, o heteroarilo, cuyo anillo está opcionalmente sustituido; R33 es un anillo arilo o heteroarilo, cuyo anillo está opcionalmente sustituido; X3 es R32', OR32, S(O)mR32 o (CH2)nNR34R35, o (CH2)nNR32R34; con la condición de que, cuando X3 es (CH2)nNR34R35, entonces R34R35 debe formar el anillo ciclado opcionalmente sustituido que comprende opcionalmente un resto oxígeno, azufre o nitrógeno, n es 0 o un número entero que tiene un valor de 1 a 10; m es 0 o un número que tiene un valor de 1 ó 2; R34 y R35 se seleccionan independientemente de hidrógeno, alquilo C1-4 opcionalmente sustituido, arilo opcionalmente sustituido, o aril-alquilo C1-4 opcionalmente sustituido; o R34 y R35 junto con el nitrógeno al que están unidos un anillo heterocíclico de 5 a 7 miembros cuyo anillo contiene opcionalmente un heteroátomo adicional seleccionado de oxígeno, azufre o NR39, y cuyo anillo está opcionalmente sustituidos; R36 es hidrógeno, alquilo C1-10, cicloalquilo C3-7, heterocíclico, heterociclil-alquilo C1-10, arilo, aril-alquilo C1-10, heteroarilo o un resto heteroaril-alquilo C1-10; y en el que cada uno de estos restos, excluyendo hidrógeno, está opcionalmente sustituido; R39 es hidrógeno, C(Z)R36, alquilo C1-10 opcionalmente sustituido, arilo opcionalmente sustituido, o aril-alquilo C1-4 opcionalmente sustituido; Z es oxígeno o azufre; o una de sus sales farmacéuticamente aceptables; c) donde: X5 es R52, OR52, S(O)mR52 o (CH2)nNR54R55, o (CH2)nR52R54; n es 0 o un número entero que tiene un valor de 1 a 10; m es 0 o un número entero que tiene un valor de 1 ó 2; y R51 es un anillo arilo opcionalmente sustituido; R52 es hidrógeno, alquilo C1-10, cicloalquilo C3-7, cicloalquil(C3-7)-alquilo, arilo, aril-alquilo C1-10,. heteroarilo, heteroaril-alquilo C1-10, resto heterocíclico, o un resto heterociclil-alquilo C1-10; y en el que cada uno de estos restos, excluyendo hidrógeno está opcionalmente sustituido; R53 es un anillo arilo opcionalmente sustituido; R54 y R55 se seleccionan cada uno independientemente de hidrógeno, alquilo C1-4 opcionalmente sustituido, arilo opcionalmente sustituido, o aril-alquilo C1-4 opcionalmente sustituido, o R54 y R55 junto con el nitrógeno al que están unidos forman un anillo heterocíclico de 5 a 7 miembros cuyo anillo contiene opcionalmente un heteroátomo adicional seleccionado de oxígeno, azufre o NR59; R56 es hidrógeno, alquilo C1-10, cicloalquilo C3-7, heterociclilo, heteroaril-alquilo C1-10, arilo, aril-alquilo C1-10, heteroarilo o un resto heteroaril-alquilo C1-10; y en el que cada uno de estos restos, excluyendo hidrógeno, puede estar opcionalmente sustituido; R59 es hidrógeno, C(Z)R56, alquilo C1-10 opcionalmente sustituido, arilo opcionalmente sustituido o un aril-alquilo C1-4 opcionalmente sustituido; Z es oxígeno azufre o una de sus sales farmacéuticamente aceptables. Composiciones farmacéuticas que comprenden el compuesto o una sal farmacéuticamente aceptable del mismo. Uso del compuesto o de una sal farmacéuticamente aceptable del mismo, para la fabricación de un medicamento para el tratamiento, incluyendo la profilaxis, de una enfermedad mediada por CSBP / RK / p38 quinasa en un mamífero. Estas enfermedades incluyen afecciones crónicas como la retinopatía diabética y degeneración muscular; infecciones de las vías respiratorias causadas por virus; neumonía inducida por el virus de la influenza y resfriado común.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18641900P | 2000-03-02 | 2000-03-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR040075A2 true AR040075A2 (es) | 2005-03-16 |
Family
ID=22684876
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010100940A AR030053A1 (es) | 2000-03-02 | 2001-02-28 | 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas |
| ARP030101602A AR040075A2 (es) | 2000-03-02 | 2003-05-07 | 1h-pirimido[4,5-d]pirimidin-2-onas y sales, composiciones farmaceuticas y uso para la fabricacion de un medicamento |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010100940A AR030053A1 (es) | 2000-03-02 | 2001-02-28 | 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas |
Country Status (25)
| Country | Link |
|---|---|
| EP (1) | EP1265900B1 (es) |
| JP (1) | JP2003525295A (es) |
| KR (1) | KR100806978B1 (es) |
| CN (1) | CN100482664C (es) |
| AR (2) | AR030053A1 (es) |
| AT (1) | ATE362473T1 (es) |
| AU (2) | AU2001239992B2 (es) |
| BR (1) | BR0108715A (es) |
| CA (1) | CA2402092C (es) |
| CY (1) | CY1106816T1 (es) |
| CZ (1) | CZ20022933A3 (es) |
| DE (1) | DE60128457T2 (es) |
| DK (1) | DK1265900T3 (es) |
| ES (1) | ES2287107T3 (es) |
| HU (1) | HUP0204431A3 (es) |
| IL (3) | IL151426A0 (es) |
| MX (1) | MXPA02008588A (es) |
| MY (1) | MY141144A (es) |
| NO (1) | NO326409B1 (es) |
| NZ (1) | NZ520914A (es) |
| PL (1) | PL358280A1 (es) |
| PT (1) | PT1265900E (es) |
| TW (1) | TWI290926B (es) |
| WO (1) | WO2001064679A1 (es) |
| ZA (1) | ZA200207017B (es) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6858617B2 (en) | 1998-05-26 | 2005-02-22 | Smithkline Beecham Corporation | Substituted imidazole compounds |
| CN1138778C (zh) | 1998-05-26 | 2004-02-18 | 沃尼尔·朗伯公司 | 用作细胞增殖抑制剂的二环嘧啶及二环3,4-二氢嘧啶化合物及用途 |
| ES2230171T3 (es) | 1999-11-23 | 2005-05-01 | Smithkline Beecham Corporation | Compuestos 3,4-dihidro-(1h)quinazolin-2-ona como inhibidores de csbp/p38 quinasa. |
| JP2003514900A (ja) | 1999-11-23 | 2003-04-22 | スミスクライン・ビーチャム・コーポレイション | ＣＳＢＰ／ｐ３８キナーゼ阻害剤としての３，４−ジヒドロ−（１Ｈ）−キナゾリン−２−オン化合物 |
| EP1233950B1 (en) | 1999-11-23 | 2005-10-05 | Smithkline Beecham Corporation | 3,4-DIHYDRO-(1H)QUINAZOLIN-2-ONE COMPOUNDS AS CSBP/P39 kINASE INHIBITORS |
| US7235551B2 (en) | 2000-03-02 | 2007-06-26 | Smithkline Beecham Corporation | 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases |
| EP2404603A1 (en) * | 2000-10-23 | 2012-01-11 | Glaxosmithkline LLC | Novel trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds for the treatment of CSBP/p38 kinase mediated diseases |
| AU2002246677B2 (en) * | 2000-12-20 | 2006-11-16 | Merck Sharp & Dohme Corp. | (Halo-Benzo Carbonyl)Heterocyclo Fused Phenyl p38 Kinase Inhibiting Agents |
| GB0124848D0 (en) | 2001-10-16 | 2001-12-05 | Celltech R&D Ltd | Chemical compounds |
| ATE485275T1 (de) | 2002-02-12 | 2010-11-15 | Glaxosmithkline Llc | Nicotinamide und deren verwendung als p38 inhibitoren |
| KR100608414B1 (ko) | 2002-02-13 | 2006-08-02 | 에프. 호프만-라 로슈 아게 | 신규한 피리딘- 및 피리미딘-유도체 |
| PL373339A1 (en) * | 2002-04-19 | 2005-08-22 | Smithkline Beecham Corporation | Novel compounds |
| GB0214268D0 (en) * | 2002-06-20 | 2002-07-31 | Celltech R&D Ltd | Chemical compounds |
| PA8577501A1 (es) | 2002-07-25 | 2004-02-07 | Warner Lambert Co | Inhibidores de quinasas |
| GB0218800D0 (en) * | 2002-08-13 | 2002-09-18 | Celltech R&D Ltd | Chemical compounds |
| US7084270B2 (en) | 2002-08-14 | 2006-08-01 | Hoffman-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| US7268139B2 (en) | 2002-08-29 | 2007-09-11 | Scios, Inc. | Methods of promoting osteogenesis |
| US7129351B2 (en) | 2002-11-04 | 2006-10-31 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| WO2004043367A2 (en) | 2002-11-06 | 2004-05-27 | Bristol-Myers Squibb Company | Fused heterocyclic compounds and use thereof |
| US7098332B2 (en) | 2002-12-20 | 2006-08-29 | Hoffmann-La Roche Inc. | 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones |
| KR100864393B1 (ko) | 2003-04-10 | 2008-10-20 | 에프. 호프만-라 로슈 아게 | 피리미도 화합물 |
| US7244441B2 (en) | 2003-09-25 | 2007-07-17 | Scios, Inc. | Stents and intra-luminal prostheses containing map kinase inhibitors |
| DE602004025504D1 (de) * | 2003-12-23 | 2010-03-25 | Novartis Ag | Bicyclische heterocyclische p-38-kinase-inhibitoren |
| JP5111113B2 (ja) * | 2004-12-13 | 2012-12-26 | サネシス ファーマシューティカルズ， インコーポレイテッド | Ｒａｆキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン |
| EP1676574A3 (en) | 2004-12-30 | 2006-07-26 | Johnson & Johnson Vision Care, Inc. | Methods for promoting survival of transplanted tissues and cells |
| JP5201817B2 (ja) * | 2005-10-28 | 2013-06-05 | 大塚製薬株式会社 | 医薬組成物 |
| US20100069409A1 (en) * | 2006-06-16 | 2010-03-18 | Glaxo Group Limited | "novel compounds" |
| WO2007147109A2 (en) * | 2006-06-16 | 2007-12-21 | Glaxo Group Limited | Novel compounds |
| KR101040394B1 (ko) * | 2010-05-18 | 2011-06-09 | (주)이성산업 | 역화 방지 기능을 갖는 야외용 가스 히터 |
| CN102816162B (zh) * | 2011-06-10 | 2016-04-27 | 中国科学院广州生物医药与健康研究院 | 嘧啶并嘧啶酮类化合物及其药用组合物和应用 |
| TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
| CN111793068A (zh) | 2013-03-15 | 2020-10-20 | 西建卡尔有限责任公司 | 杂芳基化合物和其用途 |
| KR102350704B1 (ko) | 2013-03-15 | 2022-01-13 | 셀젠 카르 엘엘씨 | 헤테로아릴 화합물 및 이의 용도 |
| CN106831722B (zh) * | 2013-10-16 | 2019-08-30 | 上海璎黎药业有限公司 | 稠合杂环化合物、其制备方法、药物组合物和用途 |
| WO2017151409A1 (en) | 2016-02-29 | 2017-09-08 | University Of Florida Research Foundation, Incorporated | Chemotherapeutic methods |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| EP3692144A1 (en) | 2017-10-05 | 2020-08-12 | Fulcrum Therapeutics, Inc. | Use of p38 inhibitors to reduce expression of dux4 |
| US20250042890A1 (en) | 2021-10-20 | 2025-02-06 | Insilico Medicine Ip Limited | METHIONINE ADENOSYLTRANSFERASE 2a (MAT2A) INHIBITORS AND USES THEREOF |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS60226882A (ja) * | 1984-04-24 | 1985-11-12 | Nippon Zoki Pharmaceut Co Ltd | 新規ピリミドピリミジン誘導体 |
| SK14099A3 (en) * | 1996-08-06 | 2000-05-16 | Pfizer | Substituted pyrido- or pyrimido-containing 6,6- or 6,7-bicyclic derivatives |
| CN1138778C (zh) * | 1998-05-26 | 2004-02-18 | 沃尼尔·朗伯公司 | 用作细胞增殖抑制剂的二环嘧啶及二环3,4-二氢嘧啶化合物及用途 |
| EP1086085A1 (en) * | 1998-06-12 | 2001-03-28 | Vertex Pharmaceuticals Incorporated | INHIBITORS OF p38 |
| HRP20010274A2 (en) * | 1998-10-23 | 2002-06-30 | Hoffmann La Roche | Bicyclic nitrogen heterocycles |
-
2001
- 2001-02-28 AR ARP010100940A patent/AR030053A1/es unknown
- 2001-02-28 MY MYPI20010900A patent/MY141144A/en unknown
- 2001-03-02 DE DE60128457T patent/DE60128457T2/de not_active Expired - Lifetime
- 2001-03-02 PT PT01914625T patent/PT1265900E/pt unknown
- 2001-03-02 TW TW090104783A patent/TWI290926B/zh not_active IP Right Cessation
- 2001-03-02 ES ES01914625T patent/ES2287107T3/es not_active Expired - Lifetime
- 2001-03-02 AU AU2001239992A patent/AU2001239992B2/en not_active Ceased
- 2001-03-02 BR BR0108715-0A patent/BR0108715A/pt not_active Application Discontinuation
- 2001-03-02 NZ NZ520914A patent/NZ520914A/en not_active IP Right Cessation
- 2001-03-02 HU HU0204431A patent/HUP0204431A3/hu unknown
- 2001-03-02 CN CNB018076866A patent/CN100482664C/zh not_active Expired - Fee Related
- 2001-03-02 WO PCT/US2001/006688 patent/WO2001064679A1/en not_active Ceased
- 2001-03-02 CZ CZ20022933A patent/CZ20022933A3/cs unknown
- 2001-03-02 PL PL01358280A patent/PL358280A1/xx not_active Application Discontinuation
- 2001-03-02 AU AU3999201A patent/AU3999201A/xx active Pending
- 2001-03-02 KR KR1020027011408A patent/KR100806978B1/ko not_active Expired - Fee Related
- 2001-03-02 JP JP2001564176A patent/JP2003525295A/ja active Pending
- 2001-03-02 AT AT01914625T patent/ATE362473T1/de active
- 2001-03-02 EP EP01914625A patent/EP1265900B1/en not_active Expired - Lifetime
- 2001-03-02 CA CA2402092A patent/CA2402092C/en not_active Expired - Fee Related
- 2001-03-02 IL IL15142601A patent/IL151426A0/xx active IP Right Grant
- 2001-03-02 DK DK01914625T patent/DK1265900T3/da active
- 2001-03-02 MX MXPA02008588A patent/MXPA02008588A/es active IP Right Grant
-
2002
- 2002-08-22 IL IL151426A patent/IL151426A/en not_active IP Right Cessation
- 2002-08-30 NO NO20024134A patent/NO326409B1/no not_active IP Right Cessation
- 2002-09-02 ZA ZA200207017A patent/ZA200207017B/en unknown
-
2003
- 2003-05-07 AR ARP030101602A patent/AR040075A2/es unknown
-
2007
- 2007-08-13 CY CY20071101080T patent/CY1106816T1/el unknown
-
2008
- 2008-02-28 IL IL189865A patent/IL189865A0/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR040075A2 (es) | 1h-pirimido[4,5-d]pirimidin-2-onas y sales, composiciones farmaceuticas y uso para la fabricacion de un medicamento | |
| ES2657687T3 (es) | Derivados de pirrolopirimidina para uso en el tratamiento de infecciones virales | |
| ES2707885T3 (es) | Alquilpirimidinderivados para el tratamiento de infecciones víricas y otras enfermedades | |
| KR102488479B1 (ko) | 인플루엔자 바이러스 감염에 사용하기 위한 인돌 | |
| CO2022012884A2 (es) | Compuestos de amino pirimidina fusionados | |
| DK2314582T3 (da) | Heterocykliske forbindelser som antivirusmidler | |
| UY29825A1 (es) | Derivados sustituidos de 3h-imidazol-(4,5 b (beta))piridina-2-il benzoatos y benzamidas, composiciones farmacéuticas que los contienen y aplicaciones | |
| PA8547701A1 (es) | Nucleosidos 4 substituidos. | |
| UY28084A1 (es) | Derivados antivirales de nucleosidos | |
| AR035668A1 (es) | Imidazoquinolinas y 6,7,8,9-tetrahidroimidazoquinolinas, composiciones farmaceuticas que las comprenden, uso de dichos compuestos en la preparacion de medicamentos, e intermediarios utiles en la sintesis de dichos compuestos | |
| UY28578A1 (es) | Derivados de amida | |
| AR125401A1 (es) | Compuestos heterocíclicos novedosos | |
| NO20074781L (no) | 4-Oksokinazolin-3-ylbenzamidderivater for behandling av cytokinsykdommer | |
| BR112014000563A2 (pt) | composto, composição farmacêutica, e, uso do composto | |
| NO20062905L (no) | Nye hydroksaminsyreestere og farmasoytisk anvendelse derav | |
| EA200870302A1 (ru) | 1,3-диоксанкарбоновые кислоты | |
| MS Wassel et al. | Antiviral activity of adamantane-pyrazole derivatives against foot and mouth disease virus infection in vivo and in vitro with molecular docking study | |
| UY29301A1 (es) | Derivados amida | |
| MX2021014161A (es) | Metodos de tratamiento del sindrome de sjogren utilizando un inhibidor de la tirosina quinasa de bruton. | |
| ECSP088257A (es) | Derivados de amida | |
| BR112022019467A2 (pt) | Derivados de n-heteroarilalquil-2-(heterociclila e heterociclilmetil) acetamida como agonistas de sstr4 | |
| ES2597803T3 (es) | Derivados de naftiridinona y su uso en el tratamiento, mejora o prevención de una enfermedad viral | |
| CN104936959B (zh) | 2,6,9-三取代嘌呤衍生物及其制备方法与应用 | |
| DK0527081T3 (da) | Hidtil ukendte substituerede 3-piperazinylalkyl-2,3-dihydro-1,3-4H-benzoxazin-4-oner, deres fremstilling og terapeutiske anvendelse | |
| MX2023001725A (es) | Derivados de espiropiperidinilo sustituidos con heteroarilo y usos farmaceuticos de los mismos. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |