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)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Gastroenterology & Hepatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Hematology (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 (78)
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 |
EP1786802A1 (en) * | 2004-08-31 | 2007-05-23 | Biogen Idec MA, Inc. | Pyrimidinylimidazoles as tgf-beta inhibitors |
WO2006025567A1 (ja) * | 2004-08-31 | 2006-03-09 | Banyu Pharmaceutical Co., Ltd. | 新規置換イミダゾール誘導体 |
CA2584248A1 (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 |
US7666880B2 (en) | 2005-03-21 | 2010-02-23 | S*Bio Pte Ltd. | Imidazo[1,2-A]pyridine derivatives: preparation and pharmaceutical applications |
TW200714600A (en) * | 2005-03-21 | 2007-04-16 | 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 |
WO2007076086A2 (en) * | 2005-12-22 | 2007-07-05 | Biogen Idec Ma Inc | Tricyclic spiro compounds useful as transforming growth factor modulators |
DE102005061840A1 (de) * | 2005-12-23 | 2007-06-28 | Merck Patent Gmbh | Triazolderivate |
US7563797B2 (en) | 2006-08-28 | 2009-07-21 | Forest Laboratories Holding Limited | Substituted imidazo(1,2-A)pyrimidines and imidazo(1,2-A) pyridines as cannabinoid receptor ligands |
DK2083863T3 (da) | 2006-10-03 | 2015-06-22 | Genzyme Corp | Antistoffer mod tgf-beta til anvendelse til behandling af spædbørn med risiko for udvikling af bronkopulmonal dysplasi |
US7977336B2 (en) * | 2006-12-28 | 2011-07-12 | Banyu Pharmaceutical Co. Ltd | Aminopyrimidine derivatives as PLK1 inhibitors |
JP2010522241A (ja) | 2007-03-21 | 2010-07-01 | ブリストル−マイヤーズ スクイブ カンパニー | 増殖性疾患、アレルギー性疾患、自己免疫疾患または炎症性疾患として有用な縮合ヘテロ環化合物 |
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 |
US8124764B2 (en) | 2008-07-14 | 2012-02-28 | Gilead Sciences, Inc. | Fused heterocyclyc inhibitor compounds |
EP2303841A1 (en) | 2008-07-14 | 2011-04-06 | Gilead Sciences, Inc. | Oxindolyl inhibitor compounds |
WO2010009139A2 (en) | 2008-07-14 | 2010-01-21 | Gilead Colorado, Inc. | Imidazolyl pyrimidine inhibitor compounds |
WO2010011837A1 (en) | 2008-07-24 | 2010-01-28 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
CA2731323A1 (en) | 2008-07-28 | 2010-02-04 | Gilead Sciences, Inc. | Cycloalkylidene and heterocycloalkylidene histone deacetylase inhibitor compounds |
BRPI1011058A2 (pt) * | 2009-05-19 | 2015-08-25 | Dow Agrosciences Llc | Compostos e metodos controlar fungos |
US8536180B2 (en) * | 2009-05-27 | 2013-09-17 | Abbvie Inc. | Pyrimidine inhibitors of kinase activity |
AU2010259042A1 (en) | 2009-06-08 | 2011-12-15 | Gilead Sciences, Inc. | Cycloalkylcarbamate benzamide aniline HDAC inhibitor compounds |
MX2011013165A (es) | 2009-06-08 | 2012-01-30 | Gilead Sciences Inc | Compuestos inhibidores de hdac de alcanoilamino-benzamida-anilina. |
CN102596961B (zh) | 2009-10-30 | 2015-12-02 | 詹森药业有限公司 | 咪唑并[1,2-b]哒嗪衍生物及其作为PDE10抑制剂的用途 |
KR101552760B1 (ko) | 2009-12-18 | 2015-09-11 | 미쓰비시 타나베 파마 코퍼레이션 | 신규 항혈소판약 |
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 |
US9468612B2 (en) | 2011-10-26 | 2016-10-18 | Seattle Children's Hospital | Cysteamine in the treatment of fibrotic disease |
RU2657540C2 (ru) | 2012-06-26 | 2018-06-14 | Янссен Фармацевтика Нв | Комбинации, содержащие ингибиторы pde 2, такие как 1-арил-4-метил-[1,2,4]триазоло[4,3-а]хиноксалиновые соединения, и ингибиторы pde 10, для применения в лечении неврологических или метаболических расстройств |
EP2869822B1 (en) | 2012-07-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | Inhibitors of phosphodiesterase 10 enzyme |
JP6449772B2 (ja) | 2012-10-05 | 2019-01-09 | カドモン コーポレイション,リミティド ライアビリティ カンパニー | ヒト抗vegfr2/kdr抗体 |
AU2013348009C1 (en) | 2012-11-21 | 2019-08-08 | Ptc Therapeutics, Inc. | Substituted reverse pyrimidine Bmi-1 inhibitors |
ES2786925T3 (es) | 2013-03-14 | 2020-10-14 | Brigham & Womens Hospital Inc | Composiciones y procedimientos para la expansión y el cultivo de células madre epiteliales |
CN105339368B (zh) * | 2013-06-04 | 2017-08-15 | 拜耳制药股份公司 | 3‑芳基‑取代的咪唑并[1,2‑a]吡啶及其用途 |
NZ748260A (en) * | 2013-08-30 | 2020-01-31 | 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 |
US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
LT3105218T (lt) | 2014-02-13 | 2019-12-10 | Incyte Corp | Ciklopropilaminai kaip lsd1 inhibitoriai |
TWI720451B (zh) | 2014-02-13 | 2021-03-01 | 美商英塞特控股公司 | 作為lsd1抑制劑之環丙胺 |
US9493442B2 (en) | 2014-02-13 | 2016-11-15 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
CN106459090A (zh) | 2014-02-19 | 2017-02-22 | 拜耳制药股份公司 | 3‑(嘧啶‑2‑基)咪唑并[1,2‑a]吡啶 |
WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
US9695180B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors |
TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪 |
WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | 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 |
WO2016087343A1 (de) | 2014-12-02 | 2016-06-09 | Bayer Pharma Aktiengesellschaft | Heteroaryl-substituierte imidazo[1,2-a]pyridine und ihre verwendung |
EP3234120A4 (en) | 2014-12-15 | 2018-05-16 | The Regents of the University of California | Cytotoxic molecules responsive to intracellular ligands for selective t cell mediated killing |
TWI714567B (zh) | 2015-04-03 | 2021-01-01 | 美商英塞特公司 | 作為lsd1抑制劑之雜環化合物 |
CR20180152A (es) | 2015-08-12 | 2018-08-09 | Incyte Corp | Sales de un inhibidor de lsd1 |
CN108884155B (zh) | 2015-10-30 | 2022-12-06 | 加利福尼亚大学董事会 | 转化生长因子-β应答多肽及其使用方法 |
CN108779437A (zh) | 2016-01-08 | 2018-11-09 | 麻省理工学院 | 分化的肠内分泌细胞和胰岛素产生细胞的制备 |
US11583593B2 (en) | 2016-01-14 | 2023-02-21 | Synthis Therapeutics, Inc. | Antibody-ALK5 inhibitor conjugates and their uses |
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 |
US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
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 |
SG11201809299QA (en) | 2016-04-22 | 2018-11-29 | Incyte Corp | Formulations of an lsd1 inhibitor |
CN109963590B (zh) | 2016-09-02 | 2024-03-15 | 加利福尼亚大学董事会 | 涉及白介素-6受体α结合单链可变片段的方法和组合物 |
CN110392686A (zh) | 2016-12-30 | 2019-10-29 | 频率治疗公司 | 1h-吡咯-2,5-二酮化合物以及使用它们来诱导干/祖支持细胞自我更新的方法 |
SG11201907095UA (en) * | 2017-02-01 | 2019-08-27 | Aucentra Therapeutics Pty Ltd | DERIVATIVES OF N-CYCLOALKYL/HETEROCYCLOALKYL-4-(IMIDAZO [1,2-a]PYRIDINE)PYRIMIDIN-2-AMINE AS THERAPEUTIC AGENTS |
BR112020007607A2 (pt) * | 2017-10-18 | 2020-09-29 | Jubilant Epipad LLC | compostos das fórmulas (i), (ii) e (iii); processos de preparação de compostos das fórmulas (i), (ii) e (iii); composição farmacêutica; compostos; método para a inibição de uma ou mais famílias de pad em uma célula; método de tratamento de uma afecção mediada por uma ou mais pad; composto da fórmula (i), fórmula (ii) e fórmula (iii); uso do composto; método para o tratamento e/ou prevenção de uma afecção; método para o tratamento de artrite reumatoide; e método de tratamento de câncer |
CA3080202C (en) * | 2017-10-26 | 2024-02-20 | Southern Research Institute | Oxadiazoles and thiadiazoles as tgf-beta inhibitors |
AU2019212969A1 (en) * | 2018-01-29 | 2020-08-13 | Merck Patent Gmbh | GCN2 inhibitors and uses thereof |
CA3093340A1 (en) | 2018-03-20 | 2019-09-26 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
JP7335957B2 (ja) * | 2018-07-09 | 2023-08-30 | シンシス セラピューティクス,インコーポレイテッド | 抗体-alk5阻害剤コンジュゲートおよびその使用 |
US20210309679A1 (en) | 2018-07-23 | 2021-10-07 | 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 |
EP3837352A1 (en) | 2018-08-17 | 2021-06-23 | 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 |
AU2019419414A1 (en) | 2018-12-31 | 2023-04-06 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
EP3947737A2 (en) | 2019-04-02 | 2022-02-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
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 |
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 |
US5670527A (en) * | 1993-07-16 | 1997-09-23 | Smithkline Beecham Corporation | Pyridyl imidazole compounds and compositions |
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 |
US5739143A (en) * | 1995-06-07 | 1998-04-14 | Smithkline Beecham Corporation | Imidazole compounds and compositions |
US5658903A (en) * | 1995-06-07 | 1997-08-19 | Smithkline Beecham Corporation | Imidazole compounds, compositions and 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 |
US5792778A (en) * | 1995-08-10 | 1998-08-11 | Merck & Co., Inc. | 2-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 |
NZ327044A (en) * | 1996-01-11 | 2000-01-28 | Smithkline Beecham Corp | Substituted imidazole compounds |
ZA97175B (en) * | 1996-01-11 | 1997-11-04 | Smithkline Beecham Corp | Novel substituted imidazole compounds. |
TR200101208T2 (tr) * | 1998-11-03 | 2001-10-22 | Glaxo Group Limited | Seçici COX-2 inhibitörleri olarak pirazolopiridin türevleri |
AR029803A1 (es) * | 2000-02-21 | 2003-07-16 | Smithkline Beecham Plc | Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden |
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 |
AU2003260345A1 (en) * | 2002-07-31 | 2004-02-23 | Smithkline Beecham Corporation | 2-phenylpyridin-4-yl derivatives as alk5 inhibitors |
GB0217783D0 (en) * | 2002-07-31 | 2002-09-11 | Glaxo Group Ltd | 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 KR KR1020057003871A patent/KR20050035296A/ko not_active Application Discontinuation
- 2003-09-05 RS YUP-2005/0199A patent/RS20050199A/sr unknown
- 2003-09-05 JP JP2004534570A patent/JP2006502164A/ja active Pending
- 2003-09-05 EP EP03752004A patent/EP1546112A4/en not_active Withdrawn
- 2003-09-05 MX MXPA05002442A patent/MXPA05002442A/es active IP Right Grant
- 2003-09-05 US US10/526,653 patent/US20060135517A1/en not_active Abandoned
- 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 GE GEAP20038732A patent/GEP20074165B/en unknown
- 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 AU AU2003270318A patent/AU2003270318B2/en not_active Ceased
- 2003-09-05 WO PCT/US2003/027721 patent/WO2004021989A2/en active Application Filing
- 2003-09-05 CA CA002497968A patent/CA2497968A1/en not_active Abandoned
- 2003-09-05 CN CN038248662A patent/CN1694871B/zh not_active Expired - Fee Related
- 2003-09-08 AR ARP030103249A patent/AR041206A1/es not_active Application Discontinuation
- 2003-09-08 MY MYPI20033385A patent/MY139566A/en unknown
-
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 |
---|---|
EA200500453A1 (ru) | 2005-10-27 |
WO2004021989A2 (en) | 2004-03-18 |
EA010426B1 (ru) | 2008-08-29 |
BR0314052A (pt) | 2005-07-05 |
NZ539068A (en) | 2006-10-27 |
KR20050035296A (ko) | 2005-04-15 |
EP1546112A4 (en) | 2006-06-07 |
JP2006502164A (ja) | 2006-01-19 |
AU2003270318A1 (en) | 2004-03-29 |
PL375691A1 (en) | 2005-12-12 |
WO2004021989A3 (en) | 2004-09-23 |
ZA200501853B (en) | 2005-11-30 |
MXPA05002442A (es) | 2005-09-30 |
GEP20074165B (en) | 2007-07-25 |
NO20051493D0 (no) | 2005-03-21 |
CN1694871B (zh) | 2010-06-16 |
CA2497968A1 (en) | 2004-03-18 |
CN1694871A (zh) | 2005-11-09 |
AU2003270318B2 (en) | 2010-01-14 |
NO20051493L (no) | 2005-03-21 |
US20060135517A1 (en) | 2006-06-22 |
UA80296C2 (en) | 2007-09-10 |
RS20050199A (en) | 2007-08-03 |
EP1546112A2 (en) | 2005-06-29 |
MY139566A (en) | 2009-10-30 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR041206A1 (es) | Imidazolpiridinas y metodos para preparar y usarlas | |
AR041207A1 (es) | Pirazolo piridinas | |
AR043184A1 (es) | Pirazoles y metodos de elaboracion y uso de estos | |
AR039241A1 (es) | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos | |
AR062196A1 (es) | Imidazo[4,5-b]pirazinas e imidazo[4,5-b]quinoxalinas, composiciones y metodos | |
HK1012622A1 (en) | Sulphonamide derivatives as aspartyl protease inhibitors | |
AR029887A1 (es) | Compuestos para el tratamiento de la isquemia, su uso en la fabricacion de medicamentos y composiciones que los contienen | |
AR042659A1 (es) | Derivados de 4-5 diariltiazoles como ligandos de cb-1 | |
AR046202A1 (es) | Compuestos nucleosidicos para el tratamiento de infecciones virales | |
WO2004043367A3 (en) | Fused heterocyclic compounds and use thereof | |
AR051587A1 (es) | Metodos para tratar lesiones vascularesy dispositivo implantable | |
BR0109115A (pt) | Inibidores de dipeptidil peptidase iv à base de pirrolidina de ciclopropil fundido e método | |
BR0305259A (pt) | Inibidores de hcv ns5b polimerase | |
CO5130004A1 (es) | 1-aril-3-arilmetil-1,8-naftiridin-4(1h)-onas | |
RS20050432A (en) | Novel aromatic fluoroglycoside derivatives,pharmaceutical products containing said compounds and the use thereof | |
WO2002100851A3 (en) | Thiophene derivatives as antiviral agents for flavivirus infection | |
CY1112042T1 (el) | Ιικοι αναστολεις | |
RU95122612A (ru) | 4-аминопиридины, способ их получения, содержащие эти соединения лекарственные средства | |
AR047671A1 (es) | Compuestos de arilnitrona 2-sustituidos y 4-sustituidos | |
AR006720A1 (es) | Un compuesto derivado de azahexano heterociclico, su uso para la preparacion de una composicion farmaceutica, procedimiento para prepararlo y una composicion farmaceutica que lo comprende | |
BRPI0519759A2 (pt) | composiÇÕes farmacÊuticas | |
CO5251454A1 (es) | Derivados aromaticos y heteroaromaticos de 1,5-benzodiazepin-2-onas | |
AR063690A1 (es) | Derivados de 1h-pirrol-2-il-carbonilo sustituidos, un metodo para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de un medicamento util en el tratamiento de infecciones bacterianas. | |
BR0002515A (pt) | Derivados de 4-arilpiperidina para o tratamento do prurido | |
BR9503468A (pt) | Composto composiçao farmacêutica processo para preparaçao do composto seu uso e processo para tratar um animal afetado por ou em risco de contrair uma doença viral ou relacionada |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA | Abandonment or withdrawal | ||
FB | Suspension of granting procedure |