AR036375A1 - 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 - Google Patents
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 medicamentosInfo
- Publication number
- AR036375A1 AR036375A1 ARP020103230A ARP020103230A AR036375A1 AR 036375 A1 AR036375 A1 AR 036375A1 AR P020103230 A ARP020103230 A AR P020103230A AR P020103230 A ARP020103230 A AR P020103230A AR 036375 A1 AR036375 A1 AR 036375A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- heterocyclyl
- aryl
- optionally
- cycloalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003814 drug Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- LELOWRISYMNNSU-UHFFFAOYSA-N Hydrocyanic acid Natural products N#C LELOWRISYMNNSU-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 20
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- -1 pyrrolo [2,3-d] pyrimidine-2-carbonitrile compound Chemical class 0.000 abstract 3
- 102000004171 Cathepsin K Human genes 0.000 abstract 2
- 108090000625 Cathepsin K Proteins 0.000 abstract 2
- 125000003282 alkyl amino group Chemical group 0.000 abstract 2
- 125000003277 amino group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 125000005330 8 membered heterocyclic group Chemical group 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 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
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000005257 alkyl acyl group Chemical group 0.000 abstract 1
- 125000003368 amide group Chemical group 0.000 abstract 1
- 125000005251 aryl acyl group Chemical group 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms 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
- 125000000592 heterocycloalkyl group Chemical group 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
- 125000002924 primary amino group Chemical group [H]N([H])* 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
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- 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
-
- 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
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- A61P33/00—Antiparasitic agents
-
- 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
- A61P33/00—Antiparasitic agents
- A61P33/10—Anthelmintics
- A61P33/12—Schistosomicides
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto pirrolo [2,3-d] pirimidina-2-carbonitrilo de la fórmula (1), o una sal o éster farmacéuticamente aceptable del mismo, donde: R es H, -R4, -OR4 o NR3R4; donde R3 es H, alquilo inferior o cicloalquilo C3-10; R4 es alquilo inferior o cicloalquilo C3-10; y donde R3 y R4 se sustituyen independientemente, opcionalmente por halo, hidroxi, alcoxi inferior, CN, NO2, u opcionalmente amino sustituidos con mono- o bi-alquilo inferior; R1 es -CO-NR5R6, -NH-CO-R5, -CH2-NH-C(O)-R5, -CO-R5, -S(O)R5, -S(O)2-R5, -CH2-CO-R5 ó -CH2-NR5R6, donde R5 es arilo, arilo-alquilo inferior, cicloalquilo C3-10, cicloalquilo C3-10-alquilo inferior, heterocicloalquilo o heterocicloalquilo-alquilo inferior; R6 es H, arilo, arilo-alquilo inferior, arilo-alquenilo inferior, cicloalquilo C3-10, cicloalquilo C3-10 -alquilo inferior, heterociclilo o heterociclilo-alquilo inferior; o donde R5 y R6 junto con el átomo de nitrógeno al cual se unen forman un grupo N-heterociclo, donde N-heterociclo denota un nitrógeno saturado, parcialmente no saturado o aromático que contiene una mitad heterocíclica unida a través de un átomo de nitrógeno de la misma que tiene de 3 a 8 átomos anulares que contienen opcionalmente 1, 2 ó 3 heteroátomos adicionales seleccionados de entre N, NR7, O, S, S(O) ó S(O)2 donde R7 es H u opcionalmente sustituido (alquilo inferior, carboxi, acilo (incluyendo tanto el acilo de alquilo inferior, por ejemplo, formilo, acetilo o propionilo, o acilo de arilo, por ejemplo, benzoílo), amido, aril S(O) ó S(O)2), y donde el N-heterociclilo se fusiona opcionalmente en una estructura bicíclica, por ejemplo, con un anillo de benceno o piridina, y donde el N-heterociclilo se enlaza opcionalmente en una estructura espiral con un anillo heterocíclico o de cicloalquilo integrado de 3 a 8 miembros en el que el anillo heterocíclico tiene de 3 a 10 miembros anulares y contiene de 1 a 3 heteroátomos seleccionados de entre N, NR6, O, S; S(O), ó S(O)2, donde R6 es como se definió con anterioridad), y donde heterociclilo denota un anillo que tiene de 3 a 10 miembros anulares y que contiene de 1 a 3 heteroátomos seleccionados de entre N, NR7, O, S, S(O) ó S(O)2 donde R7 es como se definió con anterioridad), y donde R5 y R6 se sustituyen independientemente, opcionalmente por uno o más grupos, por ejemplo, 1-3 grupos, seleccionados de entre halo, hidroxi, oxo, alcoxi inferior, CN o NO2, u opcionalmente sustituidos (opcionalmente amino sustituido con mono- o bi-alquilo inferior, alcoxi inferior, arilo, alquilo inferior con arilo, N-heterociclilo, o N-heterociclilo-alquilo inferior (donde la sustitución opcional comprende de 1 a 3 sustituyentes seleccionados entre halo, hidroxi, alcoxi inferior, alcoxi inferior-alquilo inferior, alcoxi inferior-carbonilo, CN, NO2, opcionalmente amino sustituido con mono- o bi-alquilo inferior, N-heterociclilo o N-heterociclilo-alquilo inferior, u opcionalmente amino sustituido con mono- o bi-alquilo inferior; R2 es H independientemente, u opcionalmente sustituido (alquilo inferior, arilo, arilo-alquilo inferior, cicloalquilo C3-10, cicloalquilo C3-10-alquilo inferior, heterociclilo, o heterociclilo-alquilo inferior), y donde R2 se sustituye opcionalmente por halo, hidroxi, oxo, alcoxi inferior, CN, NO2, u opcionalmente amino sustituido con mono- o bi-alquilo inferior, un proceso para su preparación, una composición farmacéutica y el uso de dichos compuestos para la preparación de medicamentos, los cuales son inhibidores de la catepsina K y encuentran uso farmacéutico para el tratamiento de enfermedades y condiciones médicas en las cuales se encuentra involucrada la catepsina K, por ejemplo, diversos padecimientos que incluyen inflamación, artritis reumatoide, osteoartritis, osteoporosis y tumores.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0121024A GB0121024D0 (en) | 2001-08-30 | 2001-08-30 | Organic compounds |
| GBGB0121026.9A GB0121026D0 (en) | 2001-08-30 | 2001-08-30 | Organic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036375A1 true AR036375A1 (es) | 2004-09-01 |
Family
ID=26246490
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020103230A AR036375A1 (es) | 2001-08-30 | 2002-08-28 | 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 |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US7112589B2 (es) |
| EP (1) | EP1423121B1 (es) |
| JP (1) | JP4131701B2 (es) |
| KR (1) | KR100629834B1 (es) |
| CN (1) | CN1549717B (es) |
| AR (1) | AR036375A1 (es) |
| AT (1) | ATE345136T1 (es) |
| AU (1) | AU2002333758B2 (es) |
| BR (1) | BR0212141A (es) |
| CA (1) | CA2456127C (es) |
| CO (1) | CO5560576A2 (es) |
| DE (1) | DE60216122T2 (es) |
| ES (1) | ES2275946T3 (es) |
| HU (1) | HUP0401431A3 (es) |
| IL (1) | IL160295A0 (es) |
| MX (1) | MXPA04001930A (es) |
| NZ (1) | NZ531287A (es) |
| PE (1) | PE20030772A1 (es) |
| PL (1) | PL208280B1 (es) |
| PT (1) | PT1423121E (es) |
| RU (1) | RU2326119C2 (es) |
| WO (1) | WO2003020278A1 (es) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR036375A1 (es) * | 2001-08-30 | 2004-09-01 | Novartis Ag | 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 |
| SE0201980D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| SE0201976D0 (sv) * | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| GB0220187D0 (en) | 2002-08-30 | 2002-10-09 | Novartis Ag | Organic compounds |
| US20060281714A1 (en) * | 2003-07-21 | 2006-12-14 | Johann Zimmermann | Combinations of a cathepsin k inhibitor and a bisphosphonate in the treatment of bone metastasis, tumor growth and tumor-induced bone loss |
| WO2005011703A1 (en) * | 2003-08-04 | 2005-02-10 | Akzo Nobel N.V. | 2-cyano-1,3,5-triazine-4,6-diamine derivatives |
| EP1667983A4 (en) * | 2003-09-23 | 2010-07-21 | Merck Sharp & Dohme | PYRAZOL MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS |
| WO2005049028A1 (en) * | 2003-11-19 | 2005-06-02 | Novartis Ag | Use of cathepsin k inhibitors in severe bone loss diseases |
| JPWO2005103012A1 (ja) * | 2004-04-21 | 2008-03-13 | 小野薬品工業株式会社 | ヒドラジノ複素環ニトリル化合物およびその用途 |
| TW200614993A (en) * | 2004-06-11 | 2006-05-16 | Akzo Nobel Nv | 4-phenyl-pyrimidine-2-carbonitrile derivatives |
| WO2006027211A1 (en) * | 2004-09-07 | 2006-03-16 | Glaxo Group Limited | 2,4-substituted pyrimidines as cysteine protease inhibitors |
| WO2006040300A1 (en) * | 2004-10-12 | 2006-04-20 | N.V. Organon | 4-cycloalkyl-pyrimidine-2-carbonitrile derivatives |
| IL164942A0 (en) * | 2004-10-31 | 2005-12-18 | Yeda Res & Dev | The use of a protease or a protease inhibitor for the manufacture of medicaments |
| GB0514684D0 (en) * | 2005-07-18 | 2005-08-24 | Novartis Ag | Organic compounds |
| RU2424234C2 (ru) * | 2005-08-05 | 2011-07-20 | Ибриженикс Са | Новые ингибиторы цистеиновых протеаз и их терапевтическое применение |
| WO2007025776A2 (en) * | 2005-09-02 | 2007-03-08 | Glaxo Group Limited | Cysteine protease inhibitors |
| TW200745055A (en) * | 2005-09-23 | 2007-12-16 | Organon Nv | 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives |
| US7326715B2 (en) | 2005-09-23 | 2008-02-05 | N.V. Organon | 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives |
| US7687515B2 (en) | 2006-01-17 | 2010-03-30 | N.V. Organon | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| EP2019688A2 (en) * | 2006-05-22 | 2009-02-04 | Velcura Therapeutics, Inc. | Use of cathepsin k antagonists in bone production |
| CN101479269A (zh) * | 2006-06-23 | 2009-07-08 | 阿斯利康(瑞典)有限公司 | 蝶啶衍生物及其作为组织蛋白酶抑制剂的用途 |
| EP1947091A1 (en) * | 2007-01-16 | 2008-07-23 | Glaxo Group Limited | Pyrimidyl nitrile derivatives as cysteine protease inhibitors |
| US7932251B2 (en) | 2007-07-16 | 2011-04-26 | N.V. Organon | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| ES2413504T3 (es) | 2007-12-21 | 2013-07-16 | Ligand Pharmaceuticals Inc. | Moduladores selectivos del receptor de andrógeno (SARM) y usos de los mismos |
| JP5587790B2 (ja) | 2008-01-09 | 2014-09-10 | アミュラ セラピューティクス リミティド | 化合物 |
| 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 |
| EP2316820A1 (en) * | 2009-10-28 | 2011-05-04 | Dompe S.p.A. | 2-aryl-propionamide derivatives useful as bradykinin receptor antagonists and pharmaceutical compositions containing them |
| 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 |
| MX344315B (es) | 2010-10-06 | 2016-12-13 | Institució Catalana De Recerca I Estudis Avancats | Metodo para el diagnostico, pronostico y tratamiento de la metastasis de cancer de mama. |
| US8524710B2 (en) * | 2010-11-05 | 2013-09-03 | Hoffmann-La Roche Inc. | Pyrrolidine derivatives |
| EP2650682A1 (en) | 2012-04-09 | 2013-10-16 | Fundació Privada Institut de Recerca Biomèdica | Method for the prognosis and treatment of cancer metastasis |
| CN104603288B (zh) | 2012-06-06 | 2018-12-14 | 生物医学研究机构基金会 | 用于肺癌转移的诊断、预后和治疗的方法 |
| 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 |
| US20160032400A1 (en) | 2013-03-15 | 2016-02-04 | Fundació Institut De Recerca Biomèdica (Irb Barcelona) | Method for the prognosis and treatment of cancer metastasis |
| US20160032399A1 (en) | 2013-03-15 | 2016-02-04 | Inbiomotion S.L. | Method for the Prognosis and Treatment of Renal Cell Carcinoma Metastasis |
| ES2727904T3 (es) | 2013-10-09 | 2019-10-21 | Fundacio Inst De Recerca Biomedica Irb Barcelona | Método para el pronóstico y tratamiento de cáncer metastatizante del hueso que se origina a partir de cáncer de mama |
| EP3094323A4 (en) | 2014-01-17 | 2017-10-11 | Ligand Pharmaceuticals Incorporated | Methods and compositions for modulating hormone levels |
| AU2015358868A1 (en) | 2014-12-11 | 2017-06-01 | Inbiomotion S.L. | Binding members for human C-Maf |
| EP3458610B1 (en) | 2016-05-25 | 2021-05-05 | Inbiomotion S.L. | Therapeutic treatment of breast cancer based on c-maf status |
| CA3050045A1 (en) * | 2017-01-27 | 2018-08-02 | Genfit | Rorgamma modulators and uses thereof |
| CN108586356B (zh) * | 2017-03-16 | 2021-02-19 | 杭州科巢生物科技有限公司 | 瑞博西尼新中间体及其制备瑞博西尼的合成方法 |
| AU2018372762B2 (en) | 2017-11-22 | 2025-08-21 | Inbiomotion S.L. | Therapeutic treatment of breast cancer based on c-maf status |
| CN109467536B (zh) * | 2018-12-23 | 2020-06-05 | 沧州普瑞东方科技有限公司 | 2-氯/羟基嘧啶-5-羧酸的合成方法 |
| AU2020250933A1 (en) | 2019-04-05 | 2021-10-28 | Centre Hospitalier Régional Et Universitaire De Brest | Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning |
| BR112021020864A2 (pt) | 2019-04-19 | 2021-12-14 | Ligand Pharm Inc | Formas cristalinas e métodos de produção de formas cristalinas de um composto |
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| NL270922A (es) | 1960-11-02 | |||
| NL295648A (es) * | 1962-07-26 | |||
| BR6915234D0 (pt) | 1969-05-22 | 1973-06-07 | American Cyanamid Co | Novos derivados de melamina e processo para sua preparaca |
| CH627919A5 (de) | 1977-04-14 | 1982-02-15 | Ciba Geigy Ag | Herbizide mittel. |
| JPH11512399A (ja) * | 1995-09-01 | 1999-10-26 | シグナル ファーマシューティカルズ，インコーポレイテッド | ピリミジンカルボキサミドおよび関連化合物ならびに炎症状態を処置するための方法 |
| EP0880501A1 (en) | 1996-02-02 | 1998-12-02 | Zeneca Limited | Heterocyclic compounds useful as pharmaceutical agents |
| DE19817459A1 (de) | 1998-04-20 | 1999-10-21 | Basf Ag | Neue heterozyklische substituierte Amide, Herstellung und Anwendung |
| PL364045A1 (en) * | 1999-09-13 | 2004-12-13 | Boehringer Ingelheim Pharmaceuticals, Inc. | Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases |
| CA2383466C (en) | 1999-09-16 | 2009-08-25 | Tanabe Seiyaku Co., Ltd. | Aromatic nitrogen-containing 6-membered cyclic compounds |
| MXPA02010693A (es) * | 2000-04-28 | 2003-03-10 | Tanabe Seiyaku Co | Compuestos ciclicos. |
| GB0013383D0 (en) | 2000-06-01 | 2000-07-26 | Glaxo Group Ltd | Therapeutic benzamide derivatives |
| AR036375A1 (es) * | 2001-08-30 | 2004-09-01 | Novartis Ag | 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 |
| SE0201980D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| SE0201976D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
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2002
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- 2002-08-29 PE PE2002000834A patent/PE20030772A1/es not_active Application Discontinuation
- 2002-08-29 CA CA002456127A patent/CA2456127C/en not_active Expired - Fee Related
- 2002-08-29 PL PL367821A patent/PL208280B1/pl not_active IP Right Cessation
- 2002-08-29 BR BR0212141-7A patent/BR0212141A/pt not_active IP Right Cessation
- 2002-08-29 AU AU2002333758A patent/AU2002333758B2/en not_active Ceased
- 2002-08-29 MX MXPA04001930A patent/MXPA04001930A/es active IP Right Grant
- 2002-08-29 IL IL16029502A patent/IL160295A0/xx unknown
- 2002-08-29 RU RU2004109812/04A patent/RU2326119C2/ru not_active IP Right Cessation
- 2002-08-29 KR KR1020047002973A patent/KR100629834B1/ko not_active Expired - Fee Related
- 2002-08-29 CN CN028169638A patent/CN1549717B/zh not_active Expired - Fee Related
- 2002-08-29 ES ES02797650T patent/ES2275946T3/es not_active Expired - Lifetime
- 2002-08-29 WO PCT/EP2002/009661 patent/WO2003020278A1/en not_active Ceased
- 2002-08-29 PT PT02797650T patent/PT1423121E/pt unknown
- 2002-08-29 JP JP2003524585A patent/JP4131701B2/ja not_active Expired - Fee Related
- 2002-08-29 US US10/487,741 patent/US7112589B2/en not_active Expired - Fee Related
- 2002-08-29 DE DE60216122T patent/DE60216122T2/de not_active Expired - Lifetime
- 2002-08-29 EP EP02797650A patent/EP1423121B1/en not_active Expired - Lifetime
- 2002-08-29 NZ NZ531287A patent/NZ531287A/en unknown
- 2002-08-29 HU HU0401431A patent/HUP0401431A3/hu unknown
- 2002-08-29 AT AT02797650T patent/ATE345136T1/de active
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2004
- 2004-02-25 CO CO04016657A patent/CO5560576A2/es not_active Application Discontinuation
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2005
- 2005-11-30 US US11/291,007 patent/US20060074092A1/en not_active Abandoned
Also Published As
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|---|---|
| IL160295A0 (en) | 2004-07-25 |
| US20060074092A1 (en) | 2006-04-06 |
| ES2275946T3 (es) | 2007-06-16 |
| AU2002333758B2 (en) | 2006-01-19 |
| JP2005505550A (ja) | 2005-02-24 |
| RU2004109812A (ru) | 2005-10-20 |
| DE60216122T2 (de) | 2007-09-06 |
| CN1549717A (zh) | 2004-11-24 |
| PE20030772A1 (es) | 2003-10-02 |
| DE60216122D1 (de) | 2006-12-28 |
| CO5560576A2 (es) | 2005-09-30 |
| MXPA04001930A (es) | 2004-06-15 |
| WO2003020278A1 (en) | 2003-03-13 |
| JP4131701B2 (ja) | 2008-08-13 |
| BR0212141A (pt) | 2004-08-24 |
| EP1423121B1 (en) | 2006-11-15 |
| HUP0401431A3 (en) | 2004-11-29 |
| US20040249153A1 (en) | 2004-12-09 |
| US7112589B2 (en) | 2006-09-26 |
| KR20040029101A (ko) | 2004-04-03 |
| KR100629834B1 (ko) | 2006-09-29 |
| PL208280B1 (pl) | 2011-04-29 |
| ATE345136T1 (de) | 2006-12-15 |
| CN1549717B (zh) | 2011-08-17 |
| RU2326119C2 (ru) | 2008-06-10 |
| EP1423121A1 (en) | 2004-06-02 |
| PT1423121E (pt) | 2007-02-28 |
| PL367821A1 (en) | 2005-03-07 |
| CA2456127A1 (en) | 2003-03-13 |
| CA2456127C (en) | 2009-10-20 |
| HUP0401431A2 (hu) | 2004-10-28 |
| NZ531287A (en) | 2005-12-23 |
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