AR036374A1 - Pirrolo pirimidinas. - Google Patents
Pirrolo pirimidinas.Info
- Publication number
- AR036374A1 AR036374A1 ARP020103229A ARP020103229A AR036374A1 AR 036374 A1 AR036374 A1 AR 036374A1 AR P020103229 A ARP020103229 A AR P020103229A AR P020103229 A ARP020103229 A AR P020103229A AR 036374 A1 AR036374 A1 AR 036374A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- heterocyclyl
- aryl
- cycloalkyl
- optionally substituted
- Prior art date
Links
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 32
- 125000003118 aryl group Chemical group 0.000 abstract 13
- 125000005843 halogen group Chemical group 0.000 abstract 9
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 9
- 125000003545 alkoxy group Chemical group 0.000 abstract 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 8
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000004043 oxo group Chemical group O=* 0.000 abstract 5
- 125000003435 aroyl group Chemical group 0.000 abstract 4
- 125000004104 aryloxy group Chemical group 0.000 abstract 4
- 125000005842 heteroatom Chemical group 0.000 abstract 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 abstract 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 3
- 125000004391 aryl sulfonyl group Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 102000004171 Cathepsin K Human genes 0.000 abstract 2
- 108090000625 Cathepsin K Proteins 0.000 abstract 2
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 2
- 125000003368 amide group Chemical group 0.000 abstract 2
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- -1 for example Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical compound O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 abstract 1
- 125000005257 alkyl acyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000005251 aryl acyl group Chemical group 0.000 abstract 1
- 125000005018 aryl alkenyl group Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- WJRBRSLFGCUECM-UHFFFAOYSA-N hydantoin Chemical compound O=C1CNC(=O)N1 WJRBRSLFGCUECM-UHFFFAOYSA-N 0.000 abstract 1
- 229940091173 hydantoin Drugs 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 abstract 1
- CYJAWBVQRMVFEO-UHFFFAOYSA-N piperazine-2,6-dione Chemical compound O=C1CNCC(=O)N1 CYJAWBVQRMVFEO-UHFFFAOYSA-N 0.000 abstract 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000003003 spiro group Chemical group 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 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
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—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
- C07D473/00—Heterocyclic compounds containing purine ring systems
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Communicable Diseases (AREA)
- Transplantation (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Un compuesto de fĂłrmula (1), o una sal o Ă©ster farmacĂ©uticamente aceptable del mismo en donde: R es H, -R2, -OR2 Ăł NR1R2; en donde R1 es H, alquilo inferior o cicloalquilo C3-10; y R2 es alquilo inferior o cicloalquilo C3-10; y en donde R1 y R2 son independientemente, opcionalmente sustituidos por halo, hidroxi, alcoxi inferior, CN, NO2, u opcionalmente mono- o di-alquilo inferior amino sustituido; X es =N- Ăł =C(Z)-; en donde Z es H, -C(O)-NR3R4, -NH-C(O)-R3, -CH2-NH-C(O)-R3, -C(O)-R3, -S(O)-R3, -S(O)2-R3, -CH2-C(O)-R3, -CH2-NR3R4, -R4, -C=C-CH2-R5, N-heterociclilo, N-heterociclilo-carbonilo, o -C(P)=C(Q)-R4, en donde P y Q independientemente son H, alquilo inferior o arilo, R3 es arilo, arilo-alquilo inferior, cicloalquilo C3-10, cicloalquilo C3-10-alquilo inferior, heterociclilo o heterociclilo-alquilo inferior; R4 es H, arilo, arilo-alquilo inferior, arilo-alquenilo inferior, cicloalquilo C3-10, cicloalquilo C3-10-alquilo inferior, heterociclilo o heterociclilo-alquilo inferior, o en donde R3 y R4 junto con el ĂĄtomo de nitrĂłgeno al cual se unen para formar un grupo N-heterociclilo, en donde N-heterociclilo denota un nitrĂłgeno saturado, parcialmente insaturado o aromĂĄtico, que contiene un radical heterocĂclico colocado por medio de un ĂĄtomo de nitrĂłgeno del mismo, que tiene de 3 a 8 ĂĄtomos de anillo que contienen opcionalmente 1, 2 Ăł 3 heteroĂĄtomos adicionales seleccionados de N, NR6, O, S, S(O) Ăł S(O)2 en donde R6 es H u opcionalmente sustituido (alquilo inferior, carboxi, acilo (incluyendo alquilo inferior acilo, por ejemplo, formilo, acetilo o propionilo, o arilo acilo, por ejemplo, benzoĂlo), amido, arilo, S(O) Ăł S(O)2, y en donde el N-heterociclilo es opcionalmente fusionado en una estructura bicĂclica, por ejemplo, con un anillo de benceno o piridina, y en donde el N-heterociclilo es opcionalmente unido en una estructura espiro con un cicloalquilo de 3 a 8 miembros o anillo heterocĂclico en donde el anillo heterocĂclico tiene de 3 a 10 miembros de anillo y contiene de 1 a 3 heteroĂĄtomos seleccionados de N, NR6, O, S, S(O) Ăł S(O)2 en donde R6 es como se define arriba), y en donde heterociclilo denota un anillo que tiene de 3 a 10 miembros de anillo y contiene de 1 a 3 heteroĂĄtomos seleccionados de N, NR6, O, S, S(O) Ăł S(O)2 en donde R6 es como se definiĂł arriba), y en donde R3 y R4 son independientemente, opcionalmente sustituidos por uno o mĂĄs grupos, por ejemplo, 1-3 grupos, seleccionados de halo, hidroxi, oxo, alcoxi inferior, CN o NO2, u (opcionalmente mono- o di-alquilo inferior amino sustituido, arilo, arilo-alquilo inferior, N-heterociclilo o N-heterociclilo-alquilo inferior (en donde la sustituciĂłn opcional comprende de 1 a 3 sustituyentes seleccionados de halo, hidroxi, alcoxi inferior, CN, NO2, u opcionalmente mono- o di-alquilo inferior amino sustituido)), y en donde R5 es arilo, arilo-alquilo inferior, ariloxi, aroĂlo o N-heterociclilo como se definiĂł arriba, y en donde R5 es opcionalmente sustituido por R7 que representa de 1 a 5 sustituyentes seleccionados de halo, hidroxi, CN, NO2 u oxo, u opcionalmente sustituido (alcoxi inferior, alquilo inferior, arilo, ariloxi, aroĂlo, alquilsulfonilo inferior, arilsulfonilo, opcionalmente mono- o di-alquilo inferior amino sustituido, o N-heterociclilo, o N-heterociclilo-alquilo inferior (en donde N-heterociclilo es como se definiĂł arriba), y en donde R7 es opcionalmente sustituido por desde 1 a 3 sustituyentes seleccionados de halo, hidroxi, opcionalmente mono- o di-alquilo inferior amino sustituido, alquilo inferior carbonilo, alcoxi inferior o alquilamido inferior; R3 es alquilo inferior, cicloalquilo C3-10 Ăł cicloalquilo C3-10-alquilo inferior, todos los cuales son independientemente opcionalmente sustituidos por halo, hidroxi, CN, NO2 u opcionalmente mono- o di-alquilo inferior-amino sustituido; y R14 es H o opcionalmente sustituido (arilo, arilo-W-alquilo inferior-W-, cicloalquilo C3-10, cicloalquilo C3-10-W-, N-heterociclilo, o, N-heterociclilo-W- (en donde N-heterociclilo es como se definiĂł arriba), ftalimida, hidantoĂna, oxazolidinona, o, 2,6-dioxo-piperazina),en donde -W- es, -O-, -C(O)-, -NH(R6)-,-NH(R6)-C(O), -NH(R6)-C(O)-O-, (en donde R6 es como se definiĂł arriba), -S(O)-, S(O)2-Ăł -S-, en donde R14 es opcionalmente sustituido por R18 que representa de 1 a 10 sustituyentes seleccionados de halo, hidroxi, CN, NO2, oxo, amido, carbonilo, sulfonamido, alquildioximetileno, o (alcoxi inferior alquilo inferior, alquenilo inferior, alquinilo inferior, alcoxi carbonilo inferior, opcionalmente mono- o di-alquilo inferior amino sustituido, arilo, arilo-alquilo inferior, arilo-alquenilo inferior, ariloxi, aroĂlo, alquilsulfonilo inferior, arilsulfonilo, N-heterociclilo, N-heterociclilo-alquilo inferior (en donde N-heterociclilo es como se define arriba), heterociclilo o R14 que comprende arilo tiene el arilo fusionado con un anillo que contiene heteroĂĄtomo, y en donde R18 es opcionalmente sustituido por R19 que representa de 1 a 4 sustituyentes seleccionados de halo, hidroxi, CN, NO2, u oxo, u opcionalmente sustituido (alcoxi inferior, alquilo inferior, alcoxi inferior-alquilo inferior, cicloalquilo C3-10, alcoxicarbonilo inferior, haloalquilo inferior, opcionalmente mono- o di-alquilo inferior amino sustituido, arilo, ariloxi, aroĂlo, (por ejemplo benzoĂlo), acilo (por ejemplo alquilcarbonilo inferior), alquilsulfonilo inferior, arilsulfonilo o N-heterociclilo, o N-heterociclilo-alquilo inferior (en donde N-heterociclilo es como se definiĂł arriba)), en donde R19 es opcionalmente sustituido por desde 1 a 4 sustituyentes seleccionados de halo, hidroxi, CN, NO2, oxo, opcionalmente mono- o di-alquilo inferior amino sustituido, alquilo inferior o alcoxi inferior. Son inhibidores de la catepsina K y encuentran uso farmacĂ©uticamente para el tratamiento de enfermedades y condiciones mĂ©dicas en las cuales estĂĄ involucrada la catepsina K, por ejemplo varios trastornos que incluyen inflamaciĂłn, artritis reumatoide, osteoartritis, osteoporosis y tumores.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0121033.5A GB0121033D0 (en) | 2001-08-30 | 2001-08-30 | Organic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036374A1 true AR036374A1 (es) | 2004-09-01 |
Family
ID=9921234
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020103229A AR036374A1 (es) | 2001-08-30 | 2002-08-28 | Pirrolo pirimidinas. |
Country Status (29)
| Country | Link |
|---|---|
| US (2) | US7452886B2 (es) |
| EP (1) | EP1423391B8 (es) |
| JP (1) | JP4629334B2 (es) |
| KR (1) | KR100695845B1 (es) |
| CN (1) | CN100372849C (es) |
| AR (1) | AR036374A1 (es) |
| AT (1) | ATE326469T1 (es) |
| AU (1) | AU2002333760B2 (es) |
| BR (1) | BR0212226A (es) |
| CA (1) | CA2458684C (es) |
| CY (1) | CY1105573T1 (es) |
| DE (1) | DE60211530T2 (es) |
| DK (1) | DK1423391T3 (es) |
| EC (1) | ECSP044998A (es) |
| ES (1) | ES2262888T3 (es) |
| GB (1) | GB0121033D0 (es) |
| HU (1) | HUP0401301A3 (es) |
| IL (3) | IL160367A0 (es) |
| MX (1) | MXPA04001935A (es) |
| MY (1) | MY157368A (es) |
| NO (1) | NO328890B1 (es) |
| NZ (1) | NZ531343A (es) |
| PE (1) | PE20030418A1 (es) |
| PL (1) | PL368280A1 (es) |
| PT (1) | PT1423391E (es) |
| RU (1) | RU2331644C2 (es) |
| TW (1) | TWI297690B (es) |
| WO (1) | WO2003020721A1 (es) |
| ZA (1) | ZA200401042B (es) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030144234A1 (en) * | 2001-08-30 | 2003-07-31 | Buxton Francis Paul | Methods for the treatment of chronic pain and compositions therefor |
| SE0201980D0 (sv) * | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| GB0220187D0 (en) | 2002-08-30 | 2002-10-09 | Novartis Ag | Organic compounds |
| JP4509028B2 (ja) | 2002-09-24 | 2010-07-21 | ăăă«ăăŁăč ăąăŒăČăŒ | ææ©ććç© |
| PE20050068A1 (es) * | 2003-02-06 | 2005-03-11 | Novartis Ag | 2-cianopirrolopirimidinas como inhibidores de la catepsina s |
| GB0304640D0 (en) * | 2003-02-28 | 2003-04-02 | Novartis Ag | Organic compounds |
| EP1619193A4 (en) * | 2003-04-18 | 2010-08-11 | Ono Pharmaceutical Co | SPIROPIPERIDINE COMPOUND AND MEDICINAL USE THEREOF |
| AU2004233582B2 (en) * | 2003-04-28 | 2008-05-15 | Novartis Ag | Pharmaceutical compositon comprising a cathepsin S inhibitor and an opioid |
| EP1797883A3 (en) * | 2003-04-28 | 2007-08-01 | Novartis AG | Pharmaceutical composition comprising a cathepsin S inhibitor and an opioid |
| JP2006525335A (ja) * | 2003-04-30 | 2006-11-09 | ăšăăăšă ăă·ăŒăăłăŒăăŹăŒă·ă§ăł | æźșè«æ§ïŒăžăăăăăăă«ïŒăă§ăă«ăąă«ăă«çœźæăžăăăăăłăŸăă©ăłćăłăžăăăăăłăŸăă©ăłèȘć°äœ |
| WO2005011703A1 (en) * | 2003-08-04 | 2005-02-10 | Akzo Nobel N.V. | 2-cyano-1,3,5-triazine-4,6-diamine derivatives |
| EP1786816A4 (en) * | 2003-09-10 | 2009-11-04 | Virochem Pharma Inc | SPIROHYDANTOIN COMPOUNDS AND METHODS FOR MODULATING CHEMOKINE RECEPTOR ACTIVITY |
| CN1918137B (zh) | 2004-02-18 | 2012-08-01 | éżæŻć©ćș·(çć ž)æéć Źćž | ććććç©ćć ¶äœäžșä»Łè°ąćè°·æ°šé žćäœæźæćçćșçš |
| US20070197510A1 (en) * | 2004-03-10 | 2007-08-23 | Kazuyuki Ohmoto | Nitriles and medicinal compositions containing the same as the active ingredient |
| ES2251292B1 (es) * | 2004-04-20 | 2007-07-01 | Inke, S.A. | Procedimiento para la obtencion de un compuesto farmaceuticamente activo y de sus intermedios de sintesis. |
| CA2564953A1 (en) | 2004-05-03 | 2005-11-24 | Janssen Pharmaceutica N.V. | Novel indole derivatives as selective androgen receptor modulators (sarms) |
| TW200614993A (en) | 2004-06-11 | 2006-05-16 | Akzo Nobel Nv | 4-phenyl-pyrimidine-2-carbonitrile derivatives |
| WO2006022454A1 (ja) | 2004-08-27 | 2006-03-02 | Ono Pharmaceutical Co., Ltd | 楩ćșæ§ćșăć«æăăććç©ăăăłăăźçšé |
| KR100651849B1 (ko) * | 2005-02-01 | 2006-12-01 | ìì§ì ì ìŁŒìíìŹ | ìžíêž° |
| RU2424234C2 (ru) * | 2005-08-05 | 2011-07-20 | ĐбŃĐžĐ¶Đ”ĐœĐžĐșŃ ĐĄĐ° | ĐĐŸĐČŃĐ” ĐžĐœĐłĐžĐ±ĐžŃĐŸŃŃ ŃĐžŃŃĐ”ĐžĐœĐŸĐČŃŃ ĐżŃĐŸŃДаз Đž ĐžŃ ŃĐ”ŃапДĐČŃĐžŃĐ”ŃĐșĐŸĐ” ĐżŃĐžĐŒĐ”ĐœĐ”ĐœĐžĐ” |
| EP1933860A2 (en) | 2005-09-01 | 2008-06-25 | Ares Trading S.A. | Treatment of optic neuritis |
| US7326715B2 (en) | 2005-09-23 | 2008-02-05 | N.V. Organon | 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives |
| TW200745055A (en) * | 2005-09-23 | 2007-12-16 | Organon Nv | 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives |
| AR056720A1 (es) * | 2005-10-26 | 2007-10-17 | Smithkline Beecham Corp | Compuesto de tiazol substtuido composicion farmaceuticamente que lo comprende y su uso para preparar un medicamento |
| WO2007058322A1 (ja) | 2005-11-18 | 2007-05-24 | Ono Pharmaceutical Co., Ltd. | 楩ćșæ§ćșăć«æăăććç©ăăăłăăźçšé |
| TW200804382A (en) * | 2005-12-05 | 2008-01-16 | Incyte Corp | Lactam compounds and methods of using the same |
| US7687515B2 (en) | 2006-01-17 | 2010-03-30 | N.V. Organon | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| US8618122B2 (en) | 2006-05-16 | 2013-12-31 | Ono Pharmaceutical Co., Ltd. | Compound having acidic group which may be protected, and use thereof |
| EP2061775A2 (en) | 2006-09-13 | 2009-05-27 | Astra Zeneca AB | Spiro-oxazolidinone compounds and their use as metabotropic glutamate receptor potentiators |
| TW200911803A (en) * | 2007-07-16 | 2009-03-16 | Organon Nv | 6-phenyl-1H-imidazo [4,5-c] pyridine-4-carbonitrile derivatives |
| US7932251B2 (en) | 2007-07-16 | 2011-04-26 | N.V. Organon | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| MX2010004272A (es) | 2007-10-19 | 2010-04-30 | Astrazeneca Ab | Derivados de tetrazol como moduladores de receptores de glutamato metabotropicos (mglurs). |
| MX2010014223A (es) | 2008-06-20 | 2011-01-21 | Novartis Ag | Composiciones pediatricas para el tratamiento de esclerosis multiple. |
| US8026236B2 (en) | 2009-01-16 | 2011-09-27 | N.V. Organon | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| TW201035094A (en) | 2009-01-16 | 2010-10-01 | Organon Nv | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| CN104945420A (zh) | 2009-06-29 | 2015-09-30 | ć ćĄçčć Źćž | äœäžșpi3kæć¶ćçć§ć¶é źç±» |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| CA2785716A1 (en) | 2009-12-30 | 2011-07-07 | Arqule, Inc. | Substituted pyrrolo-aminopyrimidine compounds |
| US9115126B2 (en) | 2010-01-15 | 2015-08-25 | Merck Sharp & Dohme B.V. | 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derivatives |
| WO2011130342A1 (en) | 2010-04-14 | 2011-10-20 | Incyte Corporation | FUSED DERIVATIVES AS ÎĄI3ÎÎŽ INHIBITORS |
| US9062055B2 (en) | 2010-06-21 | 2015-06-23 | Incyte Corporation | Fused pyrrole derivatives as PI3K inhibitors |
| WO2012027495A1 (en) | 2010-08-27 | 2012-03-01 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| MX344315B (es) | 2010-10-06 | 2016-12-13 | InstituciĂł Catalana De Recerca I Estudis Avancats | Metodo para el diagnostico, pronostico y tratamiento de la metastasis de cancer de mama. |
| CA2822070C (en) | 2010-12-20 | 2019-09-17 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| US9108984B2 (en) | 2011-03-14 | 2015-08-18 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors |
| US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
| AR087760A1 (es) | 2011-09-02 | 2014-04-16 | Incyte Corp | Heterociclilaminas como inhibidores de pi3k |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| EP2650682A1 (en) | 2012-04-09 | 2013-10-16 | FundaciĂł Privada Institut de Recerca BiomĂšdica | Method for the prognosis and treatment of cancer metastasis |
| PL2840083T3 (pl) * | 2012-04-17 | 2018-01-31 | Astellas Pharma Inc | Bicykliczny aromatyczny zwiÄ zek heterocykliczny zawierajÄ cy azot |
| CN104603288B (zh) | 2012-06-06 | 2018-12-14 | çç©ć»ćŠç 究æșæćșéäŒ | çšäșèșçèœŹç§»çèŻæăéąććæČ»ççæčæł |
| EP3553186B1 (en) | 2012-10-12 | 2021-11-17 | Inbiomotion, S.L. | Method for the diagnosis, prognosis and treatment of prostate cancer metastasis |
| US10119171B2 (en) | 2012-10-12 | 2018-11-06 | Inbiomotion S.L. | Method for the diagnosis, prognosis and treatment of prostate cancer metastasis |
| US20160032399A1 (en) | 2013-03-15 | 2016-02-04 | Inbiomotion S.L. | Method for the Prognosis and Treatment of Renal Cell Carcinoma Metastasis |
| US20160032400A1 (en) | 2013-03-15 | 2016-02-04 | FundaciĂł Institut De Recerca BiomĂšdica (Irb Barcelona) | Method for the prognosis and treatment of cancer metastasis |
| ES2727904T3 (es) | 2013-10-09 | 2019-10-21 | Fundacio Inst De Recerca Biomedica Irb Barcelona | MĂ©todo para el pronĂłstico y tratamiento de cĂĄncer metastatizante del hueso que se origina a partir de cĂĄncer de mama |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| AU2015358868A1 (en) | 2014-12-11 | 2017-06-01 | Inbiomotion S.L. | Binding members for human C-Maf |
| PT3831833T (pt) | 2015-02-27 | 2023-02-06 | Incyte Corp | Processos para a preparação de um inibidor pi3k |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| WO2016183060A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| EP3458610B1 (en) | 2016-05-25 | 2021-05-05 | Inbiomotion S.L. | Therapeutic treatment of breast cancer based on c-maf status |
| AU2018372762B2 (en) | 2017-11-22 | 2025-08-21 | Inbiomotion S.L. | Therapeutic treatment of breast cancer based on c-maf status |
| KR102054910B1 (ko) * | 2017-12-19 | 2019-12-12 | í늌ì ìœ(ìŁŒ) | íŒëĄ€ëĄ[2,3-d]íŒëŠŹëŻžë ì ëìČŽ ëë ìŽì ìŒ ë° ìŽë„Œ íŹíšíë ìœí ìĄ°ì±ëŹŒ |
| EP3556760A1 (en) * | 2018-04-19 | 2019-10-23 | F. Hoffmann-La Roche AG | Spiro compounds |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| KR102884803B1 (ko) | 2018-06-01 | 2025-11-12 | ìžìŹìŽíž ìœíŹë ìŽì | Pi3k êŽë š ì„ì ì ìčëŁë„Œ ìí íŹìŹ ìëČ |
| AU2020250933A1 (en) | 2019-04-05 | 2021-10-28 | Centre Hospitalier RĂ©gional Et Universitaire De Brest | Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning |
| EP4326721A1 (en) * | 2021-04-22 | 2024-02-28 | Protego Biopharma, Inc. | Spirocyclic imidazolidinones and imidazolidinediones for treatment of light chain amyloidosis |
| CA3239086A1 (en) * | 2021-12-01 | 2023-06-08 | St Pharm Co., Ltd. | Method for preparing triazolopyrimidinone derivative |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL270922A (es) | 1960-11-02 | |||
| CH627919A5 (de) | 1977-04-14 | 1982-02-15 | Ciba Geigy Ag | Herbizide mittel. |
| US5958930A (en) * | 1991-04-08 | 1999-09-28 | Duquesne University Of The Holy Ghost | Pyrrolo pyrimidine and furo pyrimidine derivatives |
| EP0682027B1 (de) * | 1994-05-03 | 1997-10-15 | Novartis AG | Pyrrolopyrimidinderivate mit antiproliferativer Wirkung |
| US5683999A (en) * | 1995-03-17 | 1997-11-04 | The Dupont Merck Pharmaceutical Company | Cyclic urea HIV protease inhibitors |
| DK0831829T3 (da) * | 1995-06-07 | 2003-12-15 | Pfizer | Heterocykliske, ringkondenserede pyrimidinderivater |
| ID24653A (id) * | 1997-03-19 | 2000-07-27 | Basf Ag | Zat-zat terapi |
| ATE347362T1 (de) * | 1998-06-30 | 2006-12-15 | Lilly Co Eli | Bicyclische spla 2-inhibitoren |
| CA2344249A1 (en) * | 1998-09-18 | 2000-03-30 | Basf Aktiengesellschaft | Pyrrolopyrimidines as protein kinase inhibitors |
| ATE380031T1 (de) * | 1999-12-10 | 2007-12-15 | Pfizer Prod Inc | Pyrrolo 2,3-d pyrimidinderivate enthaltende zusammensetzungen |
| AU2001247589A1 (en) * | 2000-03-20 | 2001-10-03 | Axys Pharmaceuticals, Inc. | Non-amidine containing protease inhibitors |
| MXPA02010693A (es) | 2000-04-28 | 2003-03-10 | Tanabe Seiyaku Co | Compuestos ciclicos. |
-
2001
- 2001-08-30 GB GBGB0121033.5A patent/GB0121033D0/en not_active Ceased
-
2002
- 2002-08-27 MY MYPI20023181A patent/MY157368A/en unknown
- 2002-08-28 AR ARP020103229A patent/AR036374A1/es unknown
- 2002-08-28 TW TW091119570A patent/TWI297690B/zh not_active IP Right Cessation
- 2002-08-29 PL PL02368280A patent/PL368280A1/xx not_active Application Discontinuation
- 2002-08-29 CA CA002458684A patent/CA2458684C/en not_active Expired - Fee Related
- 2002-08-29 PE PE2002000833A patent/PE20030418A1/es not_active Application Discontinuation
- 2002-08-29 MX MXPA04001935A patent/MXPA04001935A/es active IP Right Grant
- 2002-08-29 PT PT02797553T patent/PT1423391E/pt unknown
- 2002-08-29 DK DK02797553T patent/DK1423391T3/da active
- 2002-08-29 IL IL16036702A patent/IL160367A0/xx unknown
- 2002-08-29 HU HU0401301A patent/HUP0401301A3/hu unknown
- 2002-08-29 JP JP2003524991A patent/JP4629334B2/ja not_active Expired - Fee Related
- 2002-08-29 DE DE60211530T patent/DE60211530T2/de not_active Expired - Lifetime
- 2002-08-29 NZ NZ531343A patent/NZ531343A/en not_active IP Right Cessation
- 2002-08-29 WO PCT/EP2002/009663 patent/WO2003020721A1/en not_active Ceased
- 2002-08-29 AT AT02797553T patent/ATE326469T1/de active
- 2002-08-29 AU AU2002333760A patent/AU2002333760B2/en not_active Ceased
- 2002-08-29 BR BR0212226-0A patent/BR0212226A/pt not_active Application Discontinuation
- 2002-08-29 US US10/487,760 patent/US7452886B2/en not_active Expired - Fee Related
- 2002-08-29 KR KR1020047003048A patent/KR100695845B1/ko not_active Expired - Fee Related
- 2002-08-29 RU RU2004109815/04A patent/RU2331644C2/ru not_active IP Right Cessation
- 2002-08-29 ES ES02797553T patent/ES2262888T3/es not_active Expired - Lifetime
- 2002-08-29 CN CNB028168402A patent/CN100372849C/zh not_active Expired - Fee Related
- 2002-08-29 EP EP02797553A patent/EP1423391B8/en not_active Expired - Lifetime
-
2004
- 2004-02-09 ZA ZA200401042A patent/ZA200401042B/en unknown
- 2004-02-12 IL IL160367A patent/IL160367A/en not_active IP Right Cessation
- 2004-03-01 EC EC2004004998A patent/ECSP044998A/es unknown
- 2004-03-19 NO NO20041180A patent/NO328890B1/no not_active IP Right Cessation
-
2006
- 2006-08-03 CY CY20061101095T patent/CY1105573T1/el unknown
-
2008
- 2008-09-25 US US12/237,896 patent/US20090054467A1/en not_active Abandoned
-
2009
- 2009-05-07 IL IL198643A patent/IL198643A/en not_active IP Right Cessation
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR036374A1 (es) | Pirrolo pirimidinas. | |
| AR036375A1 (es) | Compuestos pirrolo [2,3-d] pirimidina -2- carbonitrilo, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos compuestos para la preparacion de medicamentos | |
| PE20200834A1 (es) | Derivados acetamida de biciclo[1.1.1]pentano sustituidos como moduladores del factor de iniciacion eucariota 2b y composiciones farmaceuticas de las mismas | |
| AR127309A2 (es) | Derivados de piridazinona | |
| LV12211A (lv) | Homoeritromicina-a atvasinajumi | |
| AR044045A1 (es) | Compuesto de piperidincarbonilpiperazina, composicion farmaceutica que lo comprende, su uso para la elaboracion de un medicamento y procedimiento para su preparacion | |
| AR038240A1 (es) | Compuesto de piperidina, uso del mismo para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para su preparacion | |
| AR034858A1 (es) | Compuestos elevadores de abca-1,composicion farmaceutica y el uso de los mismos para la manufactura de un medicamento | |
| AR045529A1 (es) | Imidazoquinolinas sustituidas con grupos ariloxi o arilalquilenoxi | |
| AR063280A1 (es) | Uso de compuestos de espiro-oxindol como agentes terapeuticos | |
| CU23148A3 (es) | Compuestos azapoliciclicos condensados con arilo | |
| UY26143A1 (es) | Derivados heterocĂclicos Ăștiles como agentes anticancerosos | |
| AR037487A1 (es) | Compuestos derivados de pirimidina, proceso para prepararlos, composicion farmaceutica y el uso de los mismos en la fabricacion de medicamentos que producen un efecto inhibidor del ciclo celular (anti-proliferacion celular) | |
| AR040773A1 (es) | Pirazoles utiles como inhibidores de gsk-3 | |
| AR040595A1 (es) | Derivados de amina sustituida y metodos de uso | |
| AR040629A1 (es) | Derivados de hidrazono-malonitrilo, los medicamentos que los contienen, uso para la preparacion de un medicamento, un conjunto de elementos (kit) que los comprende, un procedimiento para la preparacion, los intermediarios utiles en dicho procedimiento, y las combinaciones de uno de dichos derivados | |
| WO2021171230A1 (en) | Novel substituted sulfonylurea and sulfoximineurea derivatives | |
| AR035685A1 (es) | Derivados de isoxazolina, sus prodrogas, composiciones farmaceuticas que comprenden dichos compuestos, procesos para preparar dichas composiciones, uso de dichos compuestos para la fabricacion de medicamentos, uso de dichas composiciones para la fabricacion de medicamentos, procesos para la preparac | |
| AR019867A1 (es) | Uso de un derivado de pirrolidina para la fabricacion de un repelente contra insectos, acaros y garrapatas, dicho compuesto, una composicion que locomprende, un proceso para la preparacion de dicha composicion, y un proceso para repeler insectos de lugares y materiales | |
| AR019871A1 (es) | Una composicion farmaceutica que comprende inhibidores del factor de transcripcion nf-kb y el uso de los mismos para la manufactura de un medicamento | |
| AR050956A1 (es) | Derivados de bencimidazol; sintesis de los mismos; composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por ligandos del receptor cb1. | |
| AR047730A1 (es) | Uso de los derivados de 3-aminocaprolactam como agentes anti-inflamatorios | |
| US20220313657A1 (en) | Novel substituted sulfoximine derivatives | |
| UY26147A1 (es) | Derivados de 1-trifluorometil-4-hidroxi-7-piperidinil-aminometilcromano. | |
| MX2024009874A (es) | Composiciones topicas y usos de estas. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |