AR041206A1 - Imidazolpiridinas y metodos para preparar y usarlas - Google Patents
Imidazolpiridinas y metodos para preparar y usarlasInfo
- Publication number
- AR041206A1 AR041206A1 ARP030103249A ARP030103249A AR041206A1 AR 041206 A1 AR041206 A1 AR 041206A1 AR P030103249 A ARP030103249 A AR P030103249A AR P030103249 A ARP030103249 A AR P030103249A AR 041206 A1 AR041206 A1 AR 041206A1
- Authority
- AR
- Argentina
- Prior art keywords
- heterocycloalkyl
- cycloalkyl
- alkyl
- heteroaryl
- alkoxy
- Prior art date
Links
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 17
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 15
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000001072 heteroaryl group Chemical group 0.000 abstract 9
- -1 hydroxy, amino Chemical group 0.000 abstract 9
- 125000003545 alkoxy group Chemical group 0.000 abstract 8
- 125000004414 alkyl thio group Chemical group 0.000 abstract 7
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 abstract 6
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 abstract 6
- 125000002252 acyl group Chemical group 0.000 abstract 5
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 5
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 abstract 4
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 abstract 3
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 abstract 3
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000003435 aroyl group Chemical group 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000005163 aryl sulfanyl group Chemical group 0.000 abstract 3
- 125000004104 aryloxy group Chemical group 0.000 abstract 3
- 239000004202 carbamide Substances 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 3
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 abstract 3
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- NVBFHJWHLNUMCV-UHFFFAOYSA-N sulfamide Chemical compound NS(N)(=O)=O NVBFHJWHLNUMCV-UHFFFAOYSA-N 0.000 abstract 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000005126 aryl alkyl carbonyl amino group Chemical group 0.000 abstract 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 2
- 125000004658 aryl carbonyl amino group Chemical group 0.000 abstract 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 125000005169 cycloalkylcarbonylamino group Chemical group 0.000 abstract 2
- 125000005171 cycloalkylsulfanyl group Chemical group 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 2
- 125000005224 heteroarylcarbonylamino group Chemical group 0.000 abstract 2
- 101150101604 ACVR1B gene Proteins 0.000 abstract 1
- RYVZYACBVYKUHD-UHFFFAOYSA-N Alk5 Natural products CC#CC#CCCCCC=CC(=O)NCC(C)C RYVZYACBVYKUHD-UHFFFAOYSA-N 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 125000005018 aryl alkenyl group Chemical group 0.000 abstract 1
- 125000005099 aryl alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000005015 aryl alkynyl group Chemical group 0.000 abstract 1
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 abstract 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000005419 heteroarylsulfonylamino group Chemical group 0.000 abstract 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Gastroenterology & Hepatology (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Ophthalmology & Optometry (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se presentan compuestos que poseen una alta afinidad por Alk5 y/o Alk4, y pueden ser útiles como antagonistas de los mismos para la prevención y/o tratamiento de numerosas enfermedades, incluyendo desórdenes fibróticos. Reivindicación 1: Uncompuesto de la siguiente fórmula (1) en donde cada uno de X1, X2, X3, y X4 es independientemente seleccionado de entre CRx o N; siempre que sólo dos de entre X1, X2, X3 y X4 puedan ser N de manera simultánea; cada de Y1 e Y2, es independientementeseleccionado de entre CRy o N; siempre que al menos uno de entre Y1 e Y2 sea N; cada R1 es independientemente seleccionado de entre alquilo, alquenilo, alquinilo, alcoxi, acilo, halo, hidroxi, amino, nitro, ciano, guanadino, amidino, carboxi, sulfo,mercapto, alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, aminocarbonilo, alquilcarbonilamino, alquilsulfonilamino, alcoxicarbonilo, alquilcarboniloxi, urea, tiourea, sulfamoilo, sulfamida, carbamoilo, cicloalquilo, cicloalquiloxi,cicloalquilsulfanilo, heterocicloalquilo, heterocicloalquiloxi, heterocicloalquilsulfanilo, arilo, ariloxi, arilsulfanilo, aroil, heteroarilo, heteroariloxi, heteroarilsulfanilo, o heteroaroilo; cada R2 es independientemente seleccionado de entrealquilo, alquenilo, alquinilo, acilo, halo, hidroxi, -NH2, -NH(alquil), -N(alquil)2, -NH(cicloalquil), -N(alquil)(cicloalquil), -NH(heterocicloalquil), -NH(heteroaril), -NH-alquil-heterocicloalquilo, -NH-alquil-heteroarilo, -NH(aralquil),cicloalquilo, (cicloalquil)alquilo, arilo, aralquilo, aroilo, heterocicloalquilo, (heterocicloalquil)alquilo, heteroarilo, heteroaralquilo, heteroaroilo, nitro, ciano, guanadino, amidino, carboxi, sulfo, mercapto, alcoxi, cicloalquiloxi,(cicloalquil)alcoxi, ariloxi, arilalcoxi, heterocicloalquiloxi, (heterocicloalquil)alcoxi, heteroariloxi, heteroarilalcoxi, alquilsulfanilo, cicloalquilsulfanilo, (cicloalquil)alquilsulfanilo, arilsulfanilo, aralquilsulfanilo,heterocicloalquilsulfanilo, (heterocicloalquil)alquilsulfanilo, heteroarilsulfanilo, heteroarilalquilsulfanilo, alquilsulfinilo, alquilsulfonilo, aminocarbonilo, aminosulfonilo, alquilcarbonilamino, cicloalquilcarbonilamino,(cicloalquil)alquilcarbonilamino, arilcarbonilamino, aralquilcarbonilamino, (heterocicloalquil)carbonilamino, (heterocicloalquil)alquilcarbonilamino, heteroarilcarbonilamino, heteroaralquilcarbonilamino, alcoxicarbonilaminoalquilamino,(heteroaril)arilcarbonilaminoalquilamino, heteroaralquilcarbonilaminoalquilamino, (heteroaril)arilsulfonilaminoalquilcarbonilaminoalquilamino, arilsulfonilaminoalquilamino, alcoxicarbonilo, alquilcarboniloxi, urea, tiourea, sulfamoilo, sulfamida, ocarbamoilo; m es seleccionado de entre 0, 1, 2, 3, o 4; siempre que cuando m l 2, dos grupos R1 adyacentes pueden unirse entre sí para formar una porción cíclica opcionalmente sustituida de 4 a 8 miembros; n es seleccionado de entre 0, 1, 2, o 3;siempre que, cuando n l 2, dos grupos R2 adyacentes puedan unirse entre sí para formar una porción cíclica opcionalmente sustituida de 4 a 8 miembros; cada uno de Rx y Ry es independientemente seleccionado de entre H, alquilo, alquenilo, alquinilo,alcoxi, acilo, halo, hidroxi, amino, nitro, ciano, guanadino, amidino, carboxi, sulfo, mercapto, alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, cicloalquilcarbonilo, (cicloalquil)alquilcarbonilo, aroilo, aralquilcarbonilo,heterocicloalquilcarbonilo, (heterocicloalquil)acilo, heteroaroilo, (heteroaril)acilo, aminocarbonilo, alquilcarbonilamino, (amino)aminocarbonilo, alquilsulfonilaminocarbonilo, alquilsulfonilamino, cicloalquilcarbonilamino, cicloalquilsulfonilamino,(cicloalquil)alquilcarbonilamino, (cicloalquil)alquilsulfonilamino, arilcarbonilamino, arilsulfonilamino, aralquilcarbonilamino, aralquilsulfonilamino, (heterocicloalquil)carbonilamino, (heterocicloalquil)sulfonilamino,(heterocicloalquil)alquilcarbonilamino, (heterocicloalquil)alquilsulfonilamino. heteroarilcarbonilamino, heteroarilsulfonilamino, heteroaralquilcarbonilamino, heteroaralquilsulfonilamino, alcoxicarbonilo, alquilcarboniloxi, urea, tiourea,sulfamoilo, sulfamida, carbamoilo, cicloalquilo, cicloalquiloxi, cicloalquilsulfanilo, (cicloalquil)alquilo, (cicloalquil)alcoxi, (cicloalquil)alquilsulfanilo, heterocicloalquilo, heterocicloalquiloxi, heterocicloalquilsulfanilo,(heterocicloalquil)alquilo, (heterocicloalquil)alcoxi, (heterocicloalquil)alquilsulfanilo, arilo, ariloxi, arilsulfanilo, aralquilo, aralquiloxi, aralquilsulfanilo, arilalquenilo, arilalquinilo, heteroarilo, heteroariloxi, heteroarilsulfanilo,heteroaralquilo, (heteroaril)alcoxi, o (heteroaril)alquilsulfanilo; o una sal farmacéuticamente aceptable o un N-óxido de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40881202P | 2002-09-06 | 2002-09-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR041206A1 true AR041206A1 (es) | 2005-05-11 |
Family
ID=31978685
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030103249A AR041206A1 (es) | 2002-09-06 | 2003-09-08 | Imidazolpiridinas y metodos para preparar y usarlas |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20060135517A1 (es) |
| EP (1) | EP1546112A4 (es) |
| JP (1) | JP2006502164A (es) |
| KR (1) | KR20050035296A (es) |
| CN (1) | CN1694871B (es) |
| AR (1) | AR041206A1 (es) |
| AU (1) | AU2003270318B2 (es) |
| BR (1) | BR0314052A (es) |
| CA (1) | CA2497968A1 (es) |
| EA (1) | EA010426B1 (es) |
| GE (1) | GEP20074165B (es) |
| MX (1) | MXPA05002442A (es) |
| MY (1) | MY139566A (es) |
| NO (1) | NO20051493L (es) |
| NZ (1) | NZ539068A (es) |
| PL (1) | PL375691A1 (es) |
| RS (1) | RS20050199A (es) |
| UA (1) | UA80296C2 (es) |
| WO (1) | WO2004021989A2 (es) |
| ZA (1) | ZA200501853B (es) |
Families Citing this family (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
| JP4931589B2 (ja) * | 2004-07-02 | 2012-05-16 | 正明 松岡 | TGFβ2を標的としたアルツハイマー病治療薬のスクリーニング法 |
| AU2005278292B2 (en) * | 2004-08-31 | 2011-09-08 | Msd K.K. | Novel substituted imidazole derivatives |
| CA2578630A1 (en) * | 2004-08-31 | 2006-03-09 | Wen-Cherng Lee | Pyrimidinylimidazoles as tgf-beta inhibitors |
| AU2005295734A1 (en) * | 2004-10-15 | 2006-04-27 | Biogen Idec Ma Inc. | Methods of treating vascular injuries |
| JPWO2006070943A1 (ja) * | 2004-12-28 | 2008-06-12 | 武田薬品工業株式会社 | 縮合イミダゾール化合物およびその用途 |
| JP5206405B2 (ja) * | 2005-03-21 | 2013-06-12 | エムイーアイ・ファーマ・インコーポレイテッド | イミダゾ[1,2−a]ピリジン誘導体:製造および医薬用途 |
| US7666880B2 (en) | 2005-03-21 | 2010-02-23 | S*Bio Pte Ltd. | Imidazo[1,2-A]pyridine derivatives: preparation and pharmaceutical applications |
| US20070155738A1 (en) | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
| US7709468B2 (en) | 2005-09-02 | 2010-05-04 | Abbott Laboratories | Imidazo based heterocycles |
| US20100166819A1 (en) * | 2005-12-22 | 2010-07-01 | Biogen Idec Ma Inc. A Corporation | Transforming Growth Factor Modulators |
| DE102005061840A1 (de) * | 2005-12-23 | 2007-06-28 | Merck Patent Gmbh | Triazolderivate |
| WO2008027812A2 (en) | 2006-08-28 | 2008-03-06 | Forest Laboratories Holdings Limited | Imidazopyridine and imidazopyrimidine derivatives |
| MX2009003518A (es) | 2006-10-03 | 2009-08-25 | Genzyme Corp | Uso de antagonistas de tgf-beta para tratar a los infantes en riesgo de desarrollar displasia brocopulmonar. |
| US7977336B2 (en) | 2006-12-28 | 2011-07-12 | Banyu Pharmaceutical Co. Ltd | Aminopyrimidine derivatives as PLK1 inhibitors |
| WO2008116064A2 (en) | 2007-03-21 | 2008-09-25 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful for the treatment of proliferative, allergic, autoimmune or inflammatory diseases |
| WO2008133192A1 (ja) * | 2007-04-19 | 2008-11-06 | Takeda Pharmaceutical Company Limited | 縮合イミダゾール化合物およびその用途 |
| NZ590320A (en) | 2008-07-14 | 2012-12-21 | Gilead Sciences Inc | Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases |
| US8134000B2 (en) | 2008-07-14 | 2012-03-13 | Gilead Sciences, Inc. | Imidazolyl pyrimidine inhibitor compounds |
| WO2010009166A1 (en) | 2008-07-14 | 2010-01-21 | Gilead Colorado, Inc. | Oxindolyl inhibitor compounds |
| JP2011529073A (ja) | 2008-07-24 | 2011-12-01 | ブリストル−マイヤーズ スクイブ カンパニー | キナーゼ調節因子として有用な縮合ヘテロ環化合物 |
| CA2731323A1 (en) | 2008-07-28 | 2010-02-04 | Gilead Sciences, Inc. | Cycloalkylidene and heterocycloalkylidene histone deacetylase inhibitor compounds |
| US8759356B2 (en) * | 2009-05-19 | 2014-06-24 | Dow Agrosciences, Llc. | Compounds and methods for controlling fungi |
| JP2012528174A (ja) * | 2009-05-27 | 2012-11-12 | アボット・ラボラトリーズ | キナーゼ活性のピリミジン阻害剤 |
| AU2010259042A1 (en) | 2009-06-08 | 2011-12-15 | Gilead Sciences, Inc. | Cycloalkylcarbamate benzamide aniline HDAC inhibitor compounds |
| WO2010144371A1 (en) | 2009-06-08 | 2010-12-16 | Gilead Colorado, Inc. | Alkanoylamino benzamide aniline hdac inihibitor compounds |
| KR101774035B1 (ko) | 2009-10-30 | 2017-09-01 | 얀센 파마슈티카 엔.브이. | 이미다조[1,2―b]피리다진 유도체 및 PDE10 저해제로서의 그의 용도 |
| TWI450894B (zh) * | 2009-12-18 | 2014-09-01 | Mitsubishi Tanabe Pharma Corp | 新穎抗血小板藥 |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| JP5959330B2 (ja) * | 2011-06-17 | 2016-08-02 | 田辺三菱製薬株式会社 | 新規抗血小板薬 |
| US10604523B2 (en) | 2011-06-27 | 2020-03-31 | Janssen Pharmaceutica Nv | 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivatives |
| EP2737083A1 (en) | 2011-07-27 | 2014-06-04 | INSERM (Institut National de la Santé et de la Recherche Scientifique) | Methods for diagnosing and treating myhre syndrome |
| BR112014009789A2 (pt) | 2011-10-26 | 2017-04-25 | Seattle Children's Res Inst | cisteamina no tratamento da doença fibrótica |
| JP6426603B2 (ja) | 2012-06-26 | 2018-11-21 | ヤンセン ファーマシューティカ エヌ.ベー. | 神経障害または代謝障害の治療に使用するための、1−アリール−4−メチル−[1,2,4]トリアゾロ[4,3−a]−キノキサリン化合物などのPDE2阻害剤とPDE10阻害剤との組合せ |
| EP2869822B1 (en) | 2012-07-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | Inhibitors of phosphodiesterase 10 enzyme |
| EA039595B1 (ru) | 2012-10-05 | 2022-02-15 | Кадмон Корпорейшн, Ллк | Нуклеиновые кислоты, кодирующие человеческие анти-vegfr-2/kdr-антитела |
| CN104918919A (zh) | 2012-11-21 | 2015-09-16 | Ptc医疗公司 | 取代的反向嘧啶Bmi-1抑制剂 |
| RS60371B1 (sr) | 2013-03-14 | 2020-07-31 | Brigham & Womens Hospital Inc | Sastavi i postupci za ekspanziju i kultivisanje epitelnih matičnih ćelija |
| ES2625744T3 (es) * | 2013-06-04 | 2017-07-20 | Bayer Pharma Aktiengesellschaft | Imidazo[1,2-a]piridinas sustituidas con 3-arilo y su uso |
| US10370371B2 (en) | 2013-08-30 | 2019-08-06 | Ptc Therapeutics, Inc. | Substituted pyrimidine Bmi-1 inhibitors |
| WO2015076800A1 (en) | 2013-11-21 | 2015-05-28 | Ptc Therapeutics, Inc. | Substituted pyridine and pyrazine bmi-1 inhibitors |
| TW201613860A (en) | 2014-02-13 | 2016-04-16 | Incyte Corp | Cyclopropylamines as LSD1 inhibitors |
| CN106488915B (zh) | 2014-02-13 | 2020-10-02 | 因赛特公司 | 作为lsd1抑制剂的环丙胺 |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| SG10201806849WA (en) | 2014-02-13 | 2018-09-27 | Incyte Corp | Cyclopropylamines as lsd1 inhibitors |
| JP2017507140A (ja) | 2014-02-19 | 2017-03-16 | バイエル・ファルマ・アクティエンゲゼルシャフト | 3−(ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors |
| US9695168B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| CN107073042A (zh) | 2014-09-03 | 2017-08-18 | 布里格海姆妇女医院公司 | 用于产生内耳毛细胞来治疗听力损失的组合物、系统和方法 |
| CN107001361A (zh) | 2014-12-02 | 2017-08-01 | 拜耳医药股份有限公司 | 杂芳基取代的咪唑并[1,2‑a]吡啶及其用途 |
| EP3234120B1 (en) | 2014-12-15 | 2025-09-03 | The Regents of the University of California | Cytotoxic molecules responsive to intracellular ligands for selective t cell mediated killing |
| PL3240805T3 (pl) | 2014-12-15 | 2025-05-05 | The Regents Of The University Of California | Dwuswoisty chimeryczny receptor antygenu z bramką alternatywy, reaktywny wobec cd19 oraz cd20 |
| US9944647B2 (en) | 2015-04-03 | 2018-04-17 | Incyte Corporation | Heterocyclic compounds as LSD1 inhibitors |
| UA126277C2 (uk) | 2015-08-12 | 2022-09-14 | Інсайт Корпорейшн | Солі інгібітору lsd1 |
| US11014980B2 (en) | 2015-10-30 | 2021-05-25 | The Regents Of The University Of California | Transforming growth factor-beta-responsive polypeptides and their methods for use |
| CA3010610A1 (en) | 2016-01-08 | 2017-07-13 | The Brigham And Women's Hospital, Inc. | Production of differentiated enteroendocrine cells and insulin producing cells |
| US11583593B2 (en) | 2016-01-14 | 2023-02-21 | Synthis Therapeutics, Inc. | Antibody-ALK5 inhibitor conjugates and their uses |
| US11260130B2 (en) | 2016-03-02 | 2022-03-01 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV |
| US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
| US10201540B2 (en) | 2016-03-02 | 2019-02-12 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I |
| BR112018071585B1 (pt) | 2016-04-22 | 2024-01-02 | Incyte Corporation | Formulações de um inibidor de lsd1, seus usos e método de preparação das mesmas |
| US11701384B2 (en) | 2016-09-02 | 2023-07-18 | The Regents Of The University Of California | Methods and compositions involving interleukin-6 receptor alpha-binding single chain variable fragments |
| US11066419B2 (en) | 2016-12-30 | 2021-07-20 | Frequency Therapeutics, Inc. | 1H-pyrrole-2,5-dione compounds and methods of using same |
| EP3577116B1 (en) * | 2017-02-01 | 2025-04-23 | Changzhou Qianhong Bio-Pharma Co., Ltd | Derivatives of n-cycloalkyl/heterocycloalkyl-4-(imidazo[1,2-a]pyridine)pyrimidin-2-amine as therapeutic agents |
| CA3076476A1 (en) * | 2017-10-18 | 2019-04-25 | Jubilant Epipad LLC | Imidazo-pyridine compounds as pad inhibitors |
| CN111655260A (zh) * | 2017-10-26 | 2020-09-11 | 南方研究院 | 作为TGF-β抑制剂的噁二唑和噻二唑 |
| MX2020007797A (es) * | 2018-01-29 | 2020-09-18 | Merck Patent Gmbh | Inhibidores de la cinasa 2 de control general no desrepresible (gcn2) y usos de los mismos. |
| EP3768267B1 (en) | 2018-03-20 | 2025-05-14 | Icahn School of Medicine at Mount Sinai | Beta-carboline derivatives as dyrk1a inhibitors for the treatment of e.g. diabetes |
| EP3820467A4 (en) * | 2018-07-09 | 2022-05-04 | Synthis Therapeutics, Inc. | ANTIBODY-ALK5 INHIBITOR CONJUGATES AND THEIR USES |
| WO2020019108A1 (en) | 2018-07-23 | 2020-01-30 | Guangzhou Othrotx Co., Ltd. | Bisphosphonate drug conjugates |
| EP3837351A1 (en) | 2018-08-17 | 2021-06-23 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating foxo |
| CA3109386A1 (en) | 2018-08-17 | 2020-03-19 | Ptc Therapeutics, Inc. | Use of 5-fluoro-2-(6-fluoro-2-methyl-1h-benzo(d)imidazol-1-yl)-n4-(4-(trifluoromethyl)phenyl)pyrimidine-4,6-diamine in the treatment of pancreatic cancer |
| CA3109647A1 (en) | 2018-08-17 | 2020-02-20 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by upregulating jag-1 |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| WO2020142485A1 (en) | 2018-12-31 | 2020-07-09 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| JP2022527972A (ja) | 2019-04-02 | 2022-06-07 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 前悪性病変を有する患者において癌を予測及び予防する方法 |
| WO2020256721A1 (en) * | 2019-06-19 | 2020-12-24 | Synthis, Llc | Antib0dy-alk5 inhibitor conjugates and their uses |
| WO2023125541A1 (zh) * | 2021-12-27 | 2023-07-06 | 浙江光昊光电科技有限公司 | 一种有机电子器件 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3940486A (en) * | 1971-05-10 | 1976-02-24 | Ciba-Geigy Corporation | Imidazole derivatives in the treatment of pain |
| US4302464A (en) * | 1980-10-16 | 1981-11-24 | Pfizer Inc. | Imidazolylpyridine therapeutic agents |
| US4686231A (en) * | 1985-12-12 | 1987-08-11 | Smithkline Beckman Corporation | Inhibition of 5-lipoxygenase products |
| US5656644A (en) * | 1994-07-20 | 1997-08-12 | Smithkline Beecham Corporation | Pyridyl imidazoles |
| US5670527A (en) * | 1993-07-16 | 1997-09-23 | Smithkline Beecham Corporation | Pyridyl imidazole compounds and compositions |
| US5593992A (en) * | 1993-07-16 | 1997-01-14 | Smithkline Beecham Corporation | Compounds |
| US5593991A (en) * | 1993-07-16 | 1997-01-14 | Adams; Jerry L. | Imidazole compounds, use and process of making |
| GB9423460D0 (en) * | 1994-11-21 | 1995-01-11 | Merck Sharp & Dohme | Therapeutic agents |
| US5514505A (en) * | 1995-05-15 | 1996-05-07 | Xerox Corporation | Method for obtaining improved image contrast in migration imaging members |
| US5658903A (en) * | 1995-06-07 | 1997-08-19 | Smithkline Beecham Corporation | Imidazole compounds, compositions and use |
| US5739143A (en) * | 1995-06-07 | 1998-04-14 | Smithkline Beecham Corporation | Imidazole compounds and compositions |
| US5792778A (en) * | 1995-08-10 | 1998-08-11 | Merck & Co., Inc. | 2-substituted aryl pyrroles, compositions containing such compounds and methods of use |
| US5837719A (en) * | 1995-08-10 | 1998-11-17 | Merck & Co., Inc. | 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use |
| US5717100A (en) * | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
| TR199801361T2 (xx) * | 1996-01-11 | 1998-10-21 | Smithkline Beecham Corporation | Yeni ikameli imidazol bile�imleri. |
| ZA97175B (en) * | 1996-01-11 | 1997-11-04 | Smithkline Beecham Corp | Novel substituted imidazole compounds. |
| JP3420751B2 (ja) * | 1998-11-03 | 2003-06-30 | グラクソ グループ リミテッド | 選択的cox‐2インヒビターとしてのピラゾロピリジン誘導体 |
| CO5271680A1 (es) * | 2000-02-21 | 2003-04-30 | Smithkline Beecham Corp | Compuestos |
| JP4290858B2 (ja) * | 2000-06-12 | 2009-07-08 | 富士フイルム株式会社 | 有機電界発光素子 |
| WO2002040468A1 (en) * | 2000-11-16 | 2002-05-23 | Smithkline Beecham Corporation | Compounds |
| GB0217783D0 (en) * | 2002-07-31 | 2002-09-11 | Glaxo Group Ltd | Compounds |
| TW200417547A (en) * | 2002-07-31 | 2004-09-16 | Smithkline Beecham Corp | Compounds |
| PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
-
2003
- 2003-05-09 UA UAA200503149A patent/UA80296C2/uk unknown
- 2003-09-05 RS YUP-2005/0199A patent/RS20050199A/sr unknown
- 2003-09-05 CN CN038248662A patent/CN1694871B/zh not_active Expired - Fee Related
- 2003-09-05 AU AU2003270318A patent/AU2003270318B2/en not_active Ceased
- 2003-09-05 BR BR0314052-0A patent/BR0314052A/pt not_active IP Right Cessation
- 2003-09-05 PL PL03375691A patent/PL375691A1/xx not_active Application Discontinuation
- 2003-09-05 KR KR1020057003871A patent/KR20050035296A/ko not_active Withdrawn
- 2003-09-05 EP EP03752004A patent/EP1546112A4/en not_active Withdrawn
- 2003-09-05 GE GEAP20038732A patent/GEP20074165B/en unknown
- 2003-09-05 MX MXPA05002442A patent/MXPA05002442A/es active IP Right Grant
- 2003-09-05 CA CA002497968A patent/CA2497968A1/en not_active Abandoned
- 2003-09-05 WO PCT/US2003/027721 patent/WO2004021989A2/en not_active Ceased
- 2003-09-05 EA EA200500453A patent/EA010426B1/ru not_active IP Right Cessation
- 2003-09-05 NZ NZ539068A patent/NZ539068A/en unknown
- 2003-09-05 US US10/526,653 patent/US20060135517A1/en not_active Abandoned
- 2003-09-05 JP JP2004534570A patent/JP2006502164A/ja active Pending
- 2003-09-08 MY MYPI20033385A patent/MY139566A/en unknown
- 2003-09-08 AR ARP030103249A patent/AR041206A1/es not_active Application Discontinuation
-
2005
- 2005-03-03 ZA ZA200501853A patent/ZA200501853B/en unknown
- 2005-03-21 NO NO20051493A patent/NO20051493L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| MY139566A (en) | 2009-10-30 |
| ZA200501853B (en) | 2005-11-30 |
| AU2003270318B2 (en) | 2010-01-14 |
| WO2004021989A3 (en) | 2004-09-23 |
| US20060135517A1 (en) | 2006-06-22 |
| NO20051493D0 (no) | 2005-03-21 |
| JP2006502164A (ja) | 2006-01-19 |
| RS20050199A (sr) | 2007-08-03 |
| NO20051493L (no) | 2005-03-21 |
| CA2497968A1 (en) | 2004-03-18 |
| PL375691A1 (en) | 2005-12-12 |
| CN1694871A (zh) | 2005-11-09 |
| WO2004021989A2 (en) | 2004-03-18 |
| GEP20074165B (en) | 2007-07-25 |
| UA80296C2 (en) | 2007-09-10 |
| KR20050035296A (ko) | 2005-04-15 |
| EP1546112A2 (en) | 2005-06-29 |
| EA200500453A1 (ru) | 2005-10-27 |
| BR0314052A (pt) | 2005-07-05 |
| MXPA05002442A (es) | 2005-09-30 |
| EA010426B1 (ru) | 2008-08-29 |
| EP1546112A4 (en) | 2006-06-07 |
| AU2003270318A1 (en) | 2004-03-29 |
| CN1694871B (zh) | 2010-06-16 |
| NZ539068A (en) | 2006-10-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR041206A1 (es) | Imidazolpiridinas y metodos para preparar y usarlas | |
| AR041207A1 (es) | Pirazolo piridinas | |
| AR062196A1 (es) | Imidazo[4,5-b]pirazinas e imidazo[4,5-b]quinoxalinas, composiciones y metodos | |
| GR3032151T3 (en) | Sulphonamide derivatives as aspartyl protease inhibitors | |
| AR042659A1 (es) | Derivados de 4-5 diariltiazoles como ligandos de cb-1 | |
| AR051587A1 (es) | Metodos para tratar lesiones vascularesy dispositivo implantable | |
| CO5370678A1 (es) | 1,2,3,4-tetrahidroquinolinas 2-sustituidas 4-carboxiamino sustituidas | |
| AR036492A1 (es) | Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos inhibidores para la elaboracion de un medicamento para el tratamiento de enfermedades androgeno dependientes | |
| NZ595000A (en) | Imidazo[4,5-c]pyridine derivative for treating viral infections | |
| CA2250840A1 (en) | Antivirally active heterocyclic azahexane derivatives | |
| PE20050015A1 (es) | Derivados (3-oxo-morfolin-4-il)-fenilamida como inhibidores de factores de coagulacion y compuestos intermediarios en su preparacion | |
| ATE522528T1 (de) | Virale inhibitoren | |
| BRPI0519759A2 (pt) | composiÇÕes farmacÊuticas | |
| BRPI0307351B8 (pt) | composto, composição farmacêutica, uso de um composto, e, processo para preparar um composto | |
| WO2004002940A8 (en) | Inhibitors of hcv ns5b polymerase | |
| AR014868A1 (es) | UN COMPUESTO DERIVADO DE N,N ( SUSTITUIDO) FENIL (ARILO O HETEROARILO) PROPANAMINA, UNA COMPOSICIoN FARMACÉUTICA, USO DE DICHO COMPUESTO Y UN MÉTODO PARA PREPARARLO. | |
| WO2004050645A8 (en) | Substituted (thiazol-2-yl) -amide or sulfonamide as glycokinase activators useful in the treatment of type 2 diabetes | |
| BR0002518A (pt) | Derivados de 4-arilpiperidina para o tratamento de prurido | |
| AR047671A1 (es) | Compuestos de arilnitrona 2-sustituidos y 4-sustituidos | |
| EA200800932A1 (ru) | Модифицированные 4`-нуклеозиды в качестве противовирусных агентов | |
| AR019427A1 (es) | Compuestos heterociclicos como inhibidores de enzimas de rotamasa, procedimiento para su preparacion, su uso para la preparacion de medicamentos, composiciones farmaceuticas y compuestos intermediarios utiles para su preparacion | |
| CO5640098A2 (es) | Acidos biariloximetilaren-carboxilicos | |
| AR055563A1 (es) | Compuestos de piridil acido acetico, agente farmaceutico y utilizacion del compuesto para preparar dicho agente | |
| AR070791A1 (es) | Derivados de imidazo[4, 5 - d]piridazina, una composicion farmaceutica que los comprende y su uso en el tratamiento de una infeccion viral mediada por el virus de la hepatitis c. | |
| EA200600227A1 (ru) | Замещённые арилтиомочевины, применимые в качестве ингибиторов репликации вирусов |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal | ||
| FB | Suspension of granting procedure |