AR077598A1 - Compuestos heterociclicos fusionados como modulares de canales ionicos - Google Patents
Compuestos heterociclicos fusionados como modulares de canales ionicosInfo
- Publication number
- AR077598A1 AR077598A1 ARP100102716A ARP100102716A AR077598A1 AR 077598 A1 AR077598 A1 AR 077598A1 AR P100102716 A ARP100102716 A AR P100102716A AR P100102716 A ARP100102716 A AR P100102716A AR 077598 A1 AR077598 A1 AR 077598A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- heteroaryl
- cycloalkyl
- aryl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 102000004310 Ion Channels Human genes 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 19
- 125000001072 heteroaryl group Chemical group 0.000 abstract 17
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 15
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 15
- 125000003118 aryl group Chemical group 0.000 abstract 14
- 125000005843 halogen group Chemical group 0.000 abstract 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 12
- 125000000623 heterocyclic group Chemical group 0.000 abstract 11
- 125000001424 substituent group Chemical group 0.000 abstract 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 9
- -1 -O-CF2 Chemical group 0.000 abstract 8
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 150000002431 hydrogen Chemical group 0.000 abstract 7
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 6
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 5
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000002993 cycloalkylene group Chemical group 0.000 abstract 3
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000004419 alkynylene group Chemical group 0.000 abstract 2
- 125000000732 arylene group Chemical group 0.000 abstract 2
- 125000005549 heteroarylene group Chemical group 0.000 abstract 2
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 108010052164 Sodium Channels Proteins 0.000 abstract 1
- 102000018674 Sodium Channels Human genes 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000005415 substituted alkoxy group Chemical group 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Crystals, And After-Treatments Of Crystals (AREA)
- Pyridine Compounds (AREA)
- Optical Modulation, Optical Deflection, Nonlinear Optics, Optical Demodulation, Optical Logic Elements (AREA)
Abstract
Compuestos que son inhibidores del canal de sodio y a su uso en el tratamiento de diversos estados patologicos, incluyendo enfermedades cardiovasculares y diabetes. Uso de los compuestos y a composiciones farmacéuticas que los contienen. Reivindicacion 1: Un compuesto de la formula (1) en donde R1 es arilo o heteroarilo, en donde dicho arilo o heteroarilo están opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados, de modo independiente, del grupo que consiste en hidroxilo, halo, -NO2, CN, -SF5, -Si(CH3)3-O-CF3, -O-R20, -S-R20, -C(O)-R20, C(O)OH, -N(R20)(R22), -C(O)-N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-S(=O)2-R26, -S(=O)2- R20, -S(=O)2-N(R20)(R22), alcoxi C1-3, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo, heteroarilo y heterociclilo; en donde dicho alcoxi, alquilo, alquenilo, alquinilo, heteroarilo, cicloalquilo o heterociclilo están opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, -NO2, -O-CF3, -O-CF2, fenilo, heterociclilo, heteroarilo, cicloalquilo, -N(R20)(R22), -C(O)-R20, -C(O)-O-R20, -C(O)-N(R20)(R22), -CN y -O-R20, W1 es N o CR2 en donde R2 está seleccionado, de modo independiente, del grupo que consiste en hidrogeno, alquilo opcionalmente sustituido, amino, alcoxi opcionalmente sustituido, -CF3, -O-CF3, -CN y -N(R20)C(O)-R22; W2 es N o CR3 en donde R3 está seleccionado, de modo independiente, del grupo que consiste en hidrogeno, alquilo opcionalmente sustituido, -CF3, -halo y -O-R24; W3 es N o CR4, en donde R4 está seleccionado, de modo independiente, del grupo que consiste en hidrogeno, hidroxilo, halo, alquilo C1-4, alcoxi C1-3, -R25-N(R20)(R22), -R25-O-R20, -R25-C(O)-O-R20, -R25-C(O)-N(R20)(R22), -R25-C(O)-O-N(R20)(R22), -R25-N(R20)-C(O)-R22 y -R25-O-C(O)-N(R20)(R22), en donde dicho alquilo está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, Q está seleccionado de un enlace covalente o alquinileno C2-4; X1 es N o CRa, en donde Ra es hidrogeno, alquilo C1-15, alcoxi C1-4, -C(O)-O-R26, -C(O)-N(R26)(R28), -N(R20)-S(=O)2-R20, cicloalquilo, arilo, heteroarilo, heterociclilo, en donde dicho alquilo está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, -NO2, -O-CF3, -O-CHF2, cicloalquilo, -CN y alcoxi C1-4; y dicho alcoxi, cicloalquilo, arilo, heterociclilo o heteroarilo están opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, -NO2, -O-CF3, -O-CHF2, fenilo, heterociclilo, heteroarilo, cicloalquilo, -N(R20)(R22), -C(O)-R20, -C(O)-O-R20, -C(O)-N(R20)(R22), -CN y -O-R20;o Ra es -Y-Z-R25-R23-R20, en donde, Y es un enlace covalente o está seleccionado de alquileno C1-3 opcionalmente sustituido con uno o dos grupos alquilo C1-3 o fluor; Z es alquinileno C2-4, -O-, -S-, -NRö, -NR5'-C(O)-, -NRö-C(O)-NR5'- o -C(O)-NR3-, en donde cada Rö y R5' es, de modo independiente, hidrogeno o alquilo inferior C1-6; y en donde también dicho alquilo está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, -NO2, -O-CF3, -O-CF2, fenilo, heterociclilo, heteroarilo, cicloalquilo, -N(R20)(R22), -C(O)-R20, -C(O)-O-R20, -C(O)-N(R20)(R22), -CN y -O-R20, X2 es N o CRb; Rb está seleccionado del grupo que consiste en hidrogeno, alquilo sustituido, -CF3, -O-CF3, -O-R20, -S-R20, -N(R20)(R22), -N(R20)-C(O)-R22, -CF2-R20, -CF2-C(O)-O-R20 , -CF2-C(O)-N(R20)-S(=O)2-R26, -CF2-tetrazolilo, -C(O)-N(R20)-S(=O)2-R26, -N(R20)-C(O)-N(R20)(R22), -C(O)-R20, -C(O)-O-R20, -C(O)-N(R20)( R22) y -N(R20)-S(=O)2-R26, -R25-heteroarilo opcionalmente sustituido, -R25-arilo opcionalmente sustituido; R20 y R22 están seleccionados en cada instancia, de modo independiente, del grupo que consiste en hidrogeno, alquilo C1-15, alquenilo C2-15, alquinilo C2-15, cicloalquilo, heterociclilo, arilo y heteroarilo, en donde el alquilo, alquenilo, alquinilo, heterociclilo, arilo y heteroarilo están opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, alquilo, mono- o dialquilamino, alquilo o arilo o heteroarilamida, -NO2, -SO2R26, -CN, alcoxi C1-3, -CF3, -OCF3, arilo, cicloalquilo y heteroarilo; o cuando R20 y R22 están unidos a un átomo de nitrogeno comun R20 y R22 se pueden reunir para formar un anillo heterocíclico que entonces está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, alquilo, mono- o dialquilamino, alquilo o arilo o heteroarilamida, -NO2, -SO2R26, -CN, alcoxi C1-3, -CF3 y -OCF3, arilo, cicloalquilo; R23 es un enlace covalente o está seleccionado del grupo que consiste en cicloalquileno, heterociclileno, arileno y heteroarileno, en donde el cicloalquileno, heterociclileno, arileno y heteroarileno están opcionalmente sustituidos con uno a tres sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, alquilo, mono- o dialquilamino, alquilo o arilo o heteroarilamida, -NO2, -SO2R26, -CN, alcoxi C1-3, -CF3, -OCF3, arilo, cicloalquilo y heteroarilo; R24 está seleccionado en cada instancia, de modo independiente, de alquilo o arilo cualquiera de los cuales puede estar opcionalmente sustituido con 1, 2 o 3 grupos seleccionados, de modo independiente, de hidroxilo, -OCF3, halo, alcoxi C1-3, -O-R20 o alquil opcionalmente sustituido con halo, -NO2, -CF3, -O-CF3, -N(R20)(R22), -C(O)-R20, -C(O)-O-R20, -C(O)-N(R20)(R22), -CN o -O-R20; R25 es en cada instancia, de modo independiente, un enlace covalente o está seleccionado de alquileno C1-3 opcionalmente sustituido con uno o dos grupos alquilo C1-3; y R26 y R28 están seleccionados cada uno, de modo independiente, de hidrogeno, alquilo o cicloalquilo, en donde el alquilo, fenilo y cicloalquilo pueden estar sustituidos también con 1 a 3 sustituyentes seleccionados, de modo independiente, de hidroxilo, halo, alcoxi C1-4, -CF3 y -OCF3; o una de sus sales, ésteres, profármacos o solvatos farmacéuticamente aceptables, siempre que a) cuando X1 es CRa, Ra es -Y-Z-R25-R23-R20, Y no es un enlace covalente y Z es -O-, -S-, -SO2-, -C(O)-NR3-, -NR5'-C(O)- o NRö-, entonces R25 no pueda ser un enlace; b) cuando X1 es CRa, Ra es -Y-Z-R25-R23-R20,Y es enlace covalente y Z es -O-, -S-, -SO2- o NRö-, entonces R25 sea un enlace covalente y R23 no sea cicloalquileno; c) cuando Z es -NR5'-C(O)-, entonces Y no sea un enlace covalente; d) R23 y R25 no puedan ser enlaces covalentes; e) cuando X1 es CRa, Q es un enlace, R1 es heteroarilo y W1, W2 y W3 son todos CH, entonces el heteroarilo R1 pueda luego no estar sustituido con fenilo; f) cuando W1, W2 y W3 no son N, R2 es alquilo sustituido, X1 es CRa y X2 es N, entonces Ra no sea alquilo, cicloalquilo o heterociclilo; y g) cuando Q es un enlace covalente, R1 es fenilo, W1, W2 y W3 son CH, X1 es CRa y X2 es N, entonces Ra no sea alquilo C1-3 no sustituido; h) cuando Q es un enlace covalente, W1 y W2 son CH, W3 es NH, X1 es CRa y X2 es N, entonces R1 no sea heterarilo sustituido con arilo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22886409P | 2009-07-27 | 2009-07-27 | |
| US36003710P | 2010-06-30 | 2010-06-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR077598A1 true AR077598A1 (es) | 2011-09-07 |
Family
ID=42751632
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100102716A AR077598A1 (es) | 2009-07-27 | 2010-07-27 | Compuestos heterociclicos fusionados como modulares de canales ionicos |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US8952034B2 (es) |
| EP (1) | EP2464645B1 (es) |
| CN (1) | CN102725290B (es) |
| AR (1) | AR077598A1 (es) |
| AU (1) | AU2010276537B2 (es) |
| CA (1) | CA2774715C (es) |
| CY (1) | CY1119584T1 (es) |
| DK (1) | DK2464645T3 (es) |
| EA (1) | EA025824B1 (es) |
| ES (1) | ES2642586T3 (es) |
| HR (1) | HRP20171454T8 (es) |
| HU (1) | HUE034911T2 (es) |
| LT (1) | LT2464645T (es) |
| ME (1) | ME02847B (es) |
| NZ (1) | NZ598942A (es) |
| PL (1) | PL2464645T3 (es) |
| PT (1) | PT2464645T (es) |
| RS (1) | RS56410B1 (es) |
| SI (1) | SI2464645T1 (es) |
| SM (1) | SMT201700456T1 (es) |
| TW (2) | TWI490217B (es) |
| UY (1) | UY32805A (es) |
| WO (1) | WO2011014462A1 (es) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2464645T3 (en) | 2009-07-27 | 2017-10-23 | Gilead Sciences Inc | CONDENSED, HETEROCYCLIC COMPOUNDS AS IRON CHANNEL MODULATORS |
| US8703759B2 (en) | 2010-07-02 | 2014-04-22 | Gilead Sciences, Inc. | Fused heterocyclic compounds as ion channel modulators |
| WO2012065297A1 (en) | 2010-11-16 | 2012-05-24 | Impact Therapeutics, Inc. | 3-ARYL-6-ARYL-[1,2,4]TRIAZOLO[4,3-a]PYRIDINES AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF |
| PL2707361T3 (pl) | 2011-05-10 | 2018-01-31 | Gilead Sciences Inc | Skondensowane związki heterocykliczne stosowane jako modulatory kanału sodowego |
| TWI622583B (zh) | 2011-07-01 | 2018-05-01 | 基利科學股份有限公司 | 作為離子通道調節劑之稠合雜環化合物 |
| NO3175985T3 (es) | 2011-07-01 | 2018-04-28 | ||
| UY34329A (es) | 2011-09-15 | 2013-04-30 | Novartis Ag | Compuestos de triazolopiridina |
| AU2012312266A1 (en) * | 2011-09-21 | 2013-05-02 | Gilead Sciences, Inc. | Sodium channel blockers reduce glucagon secretion |
| BR112014006924B1 (pt) | 2011-09-27 | 2020-10-06 | Genfit | Derivados de triazolopiridazinas 6-substituídas como agonistas de rev-erb |
| CN104093716B (zh) | 2011-10-31 | 2017-06-23 | 克赛农制药股份有限公司 | 联芳醚磺酰胺化合物及其作为治疗剂的用途 |
| CN104024251B (zh) | 2011-10-31 | 2017-08-11 | 克赛农制药股份有限公司 | 苯磺酰胺化合物及其作为治疗剂的用途 |
| WO2013112932A1 (en) | 2012-01-27 | 2013-08-01 | Gilead Sciences, Inc. | Combination therapies using late sodium ion channel blockers and potassium ion channel blockers |
| AR091112A1 (es) | 2012-05-22 | 2015-01-14 | Genentech Inc | Benzamidas n-sustituidas como inhibidores de los canales de sodio nav1.7 |
| BR112015000187A2 (pt) | 2012-07-06 | 2017-06-27 | Genentech Inc | benzamidas substituídas com n e métodos de uso das mesmas |
| CN105263490B (zh) * | 2013-03-14 | 2018-05-22 | 基因泰克公司 | 取代的三唑并吡啶及其使用方法 |
| MX2015010775A (es) | 2013-03-15 | 2016-04-25 | Genentech Inc | Benzoxazoles sustituidos y metodos para usarlos. |
| EP2818471A1 (en) * | 2013-06-27 | 2014-12-31 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Nitrogen bicyclic compounds as inhibitors for Scyl1 and Grk5 |
| JO3367B1 (ar) * | 2013-09-06 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2 |
| EA201691085A1 (ru) | 2013-11-27 | 2017-02-28 | Дженентек, Инк. | Замещенные бензамиды и способы их применения |
| GB201321742D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201321745D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| PT3092234T (pt) * | 2013-12-20 | 2018-06-12 | Gilead Sciences Inc | Compostos heterocíclicos fundidos como moduladores de canal iónico |
| EA033889B1 (ru) | 2014-01-21 | 2019-12-05 | Янссен Фармацевтика Нв | Комбинация на основе лиганда sv2a и положительного аллостерического модулятора метаботропного глутаматергического рецептора 2 подтипа |
| LT3431106T (lt) | 2014-01-21 | 2021-02-10 | Janssen Pharmaceutica Nv | Deriniai, apimantys 2 potipio metabotropinio glutamaterginio receptoriaus teigiamus alosterinius moduliatorius arba ortosterinius agonistus, ir jų panaudojimas |
| TW201613908A (en) * | 2014-02-13 | 2016-04-16 | Gilead Sciences Inc | Solid forms of an ion channel modulator |
| WO2016007534A1 (en) | 2014-07-07 | 2016-01-14 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| JP2018520107A (ja) | 2015-05-22 | 2018-07-26 | ジェネンテック, インコーポレイテッド | 置換ベンズアミド及びその使用方法 |
| GB201511790D0 (en) | 2015-07-06 | 2015-08-19 | Iomet Pharma Ltd | Pharmaceutical compound |
| JP2018526371A (ja) | 2015-08-27 | 2018-09-13 | ジェネンテック, インコーポレイテッド | 治療化合物及びその使用方法 |
| SG10202007787RA (en) | 2015-09-28 | 2020-09-29 | Genentech Inc | Therapeutic compounds and methods of use thereof |
| US10899732B2 (en) | 2015-11-25 | 2021-01-26 | Genentech, Inc. | Substituted benzamides useful as sodium channel blockers |
| EP3436432B1 (en) | 2016-03-30 | 2021-01-27 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| US11352328B2 (en) | 2016-07-12 | 2022-06-07 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus |
| CN110072855A (zh) | 2016-10-17 | 2019-07-30 | 基因泰克公司 | 治疗性化合物及其使用方法 |
| PT3548033T (pt) * | 2016-11-28 | 2024-08-09 | Praxis Prec Medicines Inc | Compostos e respectivos métodos de utilização |
| US11261188B2 (en) | 2016-11-28 | 2022-03-01 | Praxis Precision Medicines, Inc. | Fused heteroaryl compounds, and methods thereof for treating diseases, disorders, and conditions relating to aberrant function of a sodium channel |
| US11492345B2 (en) | 2017-02-13 | 2022-11-08 | Praxis Precision Medicines, Inc. | Compounds and their methods of use |
| EP3601273B1 (en) | 2017-03-24 | 2021-12-01 | Genentech, Inc. | 4-piperidin-n-(pyrimidin-4-yl)chroman-7-sulfonamide derivatives as sodium channel inhibitors |
| WO2018187480A1 (en) | 2017-04-04 | 2018-10-11 | Praxis Precision Medicines, Inc. | Compounds and their methods of use |
| US11278535B2 (en) | 2017-08-15 | 2022-03-22 | Praxis Precision Medicines, Inc. | Compounds and their methods of use |
| US11028075B2 (en) | 2018-02-26 | 2021-06-08 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| CN111936494A (zh) | 2018-03-30 | 2020-11-13 | 豪夫迈·罗氏有限公司 | 作为钠通道抑制剂的取代的氢-吡啶并-吖嗪 |
| TW202003490A (zh) | 2018-05-22 | 2020-01-16 | 瑞士商赫孚孟拉羅股份公司 | 治療性化合物及其使用方法 |
| CN112423760A (zh) * | 2018-05-30 | 2021-02-26 | 普拉克西斯精密药物股份有限公司 | 离子通道调节剂 |
| EA202092908A1 (ru) * | 2018-09-28 | 2021-05-14 | Праксис Пресижн Медсинз, Инк. | Модуляторы ионных каналов |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
| US11773099B2 (en) | 2019-05-28 | 2023-10-03 | Praxis Precision Medicines, Inc. | Compounds and their methods of use |
| US11279700B2 (en) | 2019-05-31 | 2022-03-22 | Praxis Precision Medicines, Inc. | Ion channel modulators |
| US11505554B2 (en) | 2019-05-31 | 2022-11-22 | Praxis Precision Medicines, Inc. | Substituted pyridines as ion channel modulators |
| CN114980899A (zh) * | 2019-11-26 | 2022-08-30 | 普拉西斯精密医药公司 | 离子通道调节剂 |
| US11767325B2 (en) | 2019-11-26 | 2023-09-26 | Praxis Precision Medicines, Inc. | Substituted [1,2,4]triazolo[4,3-a]pyrazines as ion channel modulators |
| WO2021108625A1 (en) * | 2019-11-27 | 2021-06-03 | Praxis Precision Medicines, Inc. | Formulations of ion channel modulators and methods of preparation and use of ion channel modulators |
| US20230056497A1 (en) * | 2019-12-19 | 2023-02-23 | The United States Of America, As Represented By The Secretary, Dept. Of Health And Human Services | CD206 Modulators Their Use and Methods for Preparation |
| KR20250005348A (ko) * | 2022-04-26 | 2025-01-09 | 프락시스 프리시젼 메디신즈, 인크. | 신경 장애의 치료 |
Family Cites Families (165)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL128591C (es) * | 1965-07-02 | |||
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4230705A (en) * | 1976-09-22 | 1980-10-28 | American Cyanamid Company | 6-Phenyl-1,2,4-triazolo[4,3-b]pyridazines and their uses in treating anxiety |
| US4242515A (en) * | 1979-03-28 | 1980-12-30 | American Cyanamid Company | Substituted 3-alkyl-6-phenyl-1,2,4-triazolo-[4,3-a]pyridines |
| US4244953A (en) * | 1979-10-24 | 1981-01-13 | American Cyanamid Company | Substituted 6-phenyl-5,6,7,8-tetrahydro-1,2,4-triazolo-[4,3-a]pyridines |
| US4326525A (en) * | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US4812565A (en) * | 1982-09-30 | 1989-03-14 | A. H. Robins Company, Incorporated | Fused aromatic oxazepinones, thiazepinones, diazepinones and sulfur analogs thereof |
| US5364620A (en) * | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US4654343A (en) * | 1985-10-31 | 1987-03-31 | American Cyanamid Company | N-substituted-N[3-(1,2,4-triazolo[4,3-b]pyridazin-6-yl)phenyl]alkanamides, carbamates and ureas |
| US5023252A (en) * | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US4746655A (en) * | 1987-06-10 | 1988-05-24 | A. H. Robins Company, Incorporated | Fused aromatic-spiropiperidine oxazepinones(and thiones) |
| US5001139A (en) * | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| US4902514A (en) * | 1988-07-21 | 1990-02-20 | Alza Corporation | Dosage form for administering nilvadipine for treating cardiovascular symptoms |
| DE4010488A1 (de) | 1990-03-31 | 1991-10-02 | Hoechst Ag | Benzoxazinderivate, verfahren zu ihrer herstellung und ihre verwendung zum behandeln oder zur prophylaxe von krankheiten |
| CA2044564A1 (en) * | 1990-06-28 | 1991-12-29 | Quirico Branca | Amino acid derivatives |
| CN1060467A (zh) | 1990-09-25 | 1992-04-22 | 武田药品工业株式会社 | 1,3-苯并嗪衍生物、其生产方法和用途 |
| JPH04209692A (ja) | 1990-12-03 | 1992-07-31 | Asahi Glass Co Ltd | フォトクロミック材料 |
| EP0612729B1 (en) | 1991-05-10 | 1997-04-23 | Takeda Chemical Industries, Ltd. | Pyridine derivatives, their production and use |
| CA2112360A1 (en) | 1991-06-28 | 1993-12-23 | William Edward Bondinell | Bicyclic fibrinogen antagonists |
| US5939412A (en) * | 1992-06-26 | 1999-08-17 | Smithkline Beecham Corporation | Bicyclic fibrinogen antagonists |
| US5663166A (en) * | 1991-10-18 | 1997-09-02 | Genentech, Inc. | Nonpeptidyl integrin inhibitors having specificity for the GPIIb IIIa receptor |
| US5250679A (en) | 1991-10-18 | 1993-10-05 | Genentech, Inc. | Nonpeptidyl platelet aggregation inhibitors having specificity for the GPIIb III.sub. receptor |
| US5272158A (en) | 1991-10-29 | 1993-12-21 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| JPH06107647A (ja) | 1992-08-12 | 1994-04-19 | Takeda Chem Ind Ltd | 1,3−ベンゾオキサジン誘導体の製造法 |
| US5442055A (en) | 1992-11-13 | 1995-08-15 | Tanabe Seiyaku Co., Ltd. | Azetidinone compound and process for preparation thereof |
| US6011150A (en) * | 1992-11-13 | 2000-01-04 | Tanabe Seiyaku Co., Ltd. | Azetidinone compound and process for preparation thereof |
| GB9225860D0 (en) | 1992-12-11 | 1993-02-03 | Smithkline Beecham Plc | Novel treatment |
| GB9226302D0 (en) | 1992-12-17 | 1993-02-10 | Smithkline Beecham Plc | Pharmaceuticals |
| US5550229A (en) | 1993-06-23 | 1996-08-27 | Tanabe Seiyaku Co., Ltd. | Alkylation process for preparing azetidinone compound and starting compound therefor |
| DE19526173A1 (de) | 1995-07-18 | 1997-01-30 | Hoechst Ag | Polyfullerenaddukte, Verfahren zu ihrer regioselektiven Herstellung und deren Verwendung |
| JPH09157262A (ja) | 1995-12-08 | 1997-06-17 | Tanabe Seiyaku Co Ltd | アゼチジノン誘導体及びその合成中間体の製法 |
| GB9619492D0 (en) | 1996-09-18 | 1996-10-30 | Smithkline Beecham Plc | Novel treatment |
| JP2001526643A (ja) | 1997-04-18 | 2001-12-18 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | 5ht1a、5ht1bおよび5ht1d受容体アンタゴニスト活性を合わせ持つ化合物を含む二環式アリールまたは二環式複素環 |
| JP3964053B2 (ja) | 1997-07-10 | 2007-08-22 | 三井化学株式会社 | 遷移金属化合物からなるオレフィン重合用触媒ならびに重合方法 |
| WO1999013038A1 (en) | 1997-09-08 | 1999-03-18 | Unilever N.V. | Method for enhancing the activity of an enzyme |
| GEP20032868B (en) * | 1998-01-21 | 2003-01-27 | Merck Sharp & Dohme | Triazolo-Pyridazine Derivatives as Ligands for Gaba Receptors, Methods for Their Production, Pharmaceutical Compositions Containing the Same for Treatment and/or Prevention of disorders of Central Nervous System |
| AU2594799A (en) | 1998-02-11 | 1999-08-30 | Du Pont Pharmaceuticals Company | Novel cyclic sulfonamide derivatives as metalloproteinase inhibitors |
| HUP0101280A3 (en) | 1998-02-18 | 2003-02-28 | Neurosearch As | Positive ampa receptor modulator compounds and their use |
| CA2334836A1 (en) * | 1998-06-16 | 1999-12-23 | Merck Sharp & Dohme Limited | Triazolo-pyridine derivatives as ligands for gaba receptors |
| EP1123297A1 (en) | 1998-10-21 | 2001-08-16 | Novo Nordisk A/S | New compounds, their preparation and use |
| US6627651B1 (en) | 1999-05-07 | 2003-09-30 | Takeda Chemical Industries, Ltd. | Cyclic compounds and uses thereof |
| BR0013610A (pt) | 1999-08-27 | 2002-07-16 | Procter & Gamble | Componentes de formulções de ação rápida,composições e métodos para lavar roupa empregando os mesmos |
| CA2381903A1 (en) | 1999-08-27 | 2001-03-08 | The Procter & Gamble Company | Color safe laundry methods employing cationic formulation components |
| MXPA02002124A (es) | 1999-08-27 | 2002-09-18 | Procter & Gamble | Componentes de formulacion de incremento de estabilidad y composiciones y metodos de lavanderia que emplean los mismos. |
| MXPA02002125A (es) | 1999-08-27 | 2002-09-18 | Procter & Gamble | Componentes aumentadores del blanqueado, composiciones y metodos de lavanderia. |
| CZ2002687A3 (cs) | 1999-08-27 | 2002-09-11 | The Procter & Gamble Company | Barvu zachovávající prací způsoby používající formulační složky s obojetnými ionty |
| BR0013608A (pt) | 1999-08-27 | 2002-05-21 | Procter & Gamble | Disponibilidade controlada de componentes de formulações, composições e métodos para lavar roupa empregando os mesmos |
| CN1384868A (zh) | 1999-08-27 | 2002-12-11 | 宝洁公司 | 稳定的配制组分、使用该组分的组合物和洗衣方法 |
| US6469020B2 (en) | 2000-05-15 | 2002-10-22 | Darwin Discovery, Ltd. | Hydroxamic and carboxylic acid derivatives |
| CN1466577A (zh) | 2000-08-01 | 2004-01-07 | СҰҩƷ��ҵ��ʽ���� | 3,4-二氢异喹啉衍生物化合物以及将该化合物作为有效成分的药剂 |
| US20040058915A1 (en) | 2000-08-29 | 2004-03-25 | Khanna Ish Kumar | Compounds containing a bicyclic ring system useful as alpha v beta 3 antagonists |
| JP2002205992A (ja) * | 2000-11-08 | 2002-07-23 | Takeda Chem Ind Ltd | 二環式トリアゾロン誘導体およびそれを含有する除草剤 |
| EP1695716A2 (en) | 2000-12-26 | 2006-08-30 | Sankyo Company, Limited | Medicinal compositions containing diuretics and insulin sensitizers |
| AP2002002463A0 (en) | 2001-03-09 | 2002-06-30 | Pfizer Prod Inc | Novel triazolo-pyrimides anti-inflammatory compounds. |
| US6998408B2 (en) * | 2001-03-23 | 2006-02-14 | Bristol-Myers Squibb Pharma Company | 6-5, 6-6, or 6-7 Heterobicycles as factor Xa inhibitors |
| US20030114448A1 (en) | 2001-05-31 | 2003-06-19 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| JP2005089298A (ja) | 2001-09-18 | 2005-04-07 | Japan Tobacco Inc | ナフタレン化合物及びその医薬用途 |
| US7196108B2 (en) | 2002-03-08 | 2007-03-27 | Incyte San Diego Inc. | Bicyclic heterocycles for the treatment of diabetes and other diseases |
| JP2003277384A (ja) | 2002-03-26 | 2003-10-02 | Kyorin Pharmaceut Co Ltd | 縮合ニ環式ピリジン誘導体 |
| JP2003321461A (ja) | 2002-04-25 | 2003-11-11 | Kyorin Pharmaceut Co Ltd | 縮合ビフェニル誘導体 |
| CA2497658A1 (en) * | 2002-08-13 | 2004-02-19 | Warner-Lambert Company Llc | Chromone derivatives as matrix metalloproteinase inhibitors |
| US7005523B2 (en) * | 2002-08-30 | 2006-02-28 | Pfizer Inc. | Cycloalkyl-[4-(trifluorophenyl)-oxazol-5yl]-triazolo-pyridines |
| PA8579601A1 (es) * | 2002-08-30 | 2004-05-07 | Pfizer Prod Inc | Compuestos antiinflamatorios de di y trifloruro-triazolo-piridinas |
| JPWO2004026292A1 (ja) | 2002-09-20 | 2006-01-12 | 株式会社ツムラ | 鎮咳薬 |
| US20040204404A1 (en) * | 2002-09-30 | 2004-10-14 | Robert Zelle | Human N-type calcium channel blockers |
| WO2004037997A2 (en) | 2002-10-22 | 2004-05-06 | The Trustees Of The University Of Pennsylvania | Fragments and activity of rel protein in m. tuberculosis adn other uses thereof |
| DE60310991T2 (de) | 2002-11-07 | 2007-10-18 | Merck & Co, Inc. | Phenylalaninderivate als hemmer der dipeptidyl peptidase zur behandlung oder prävention von diabetes |
| JP2006516283A (ja) | 2003-01-13 | 2006-06-29 | コーテックス ファーマシューティカルズ, インコーポレイテッド | 睡眠不足とストレスに起因する知覚衰退の処置方法 |
| MY142651A (en) | 2003-03-18 | 2010-12-15 | Merck Sharp & Dohme | Biaryl substituted triazoles as sodium channel blockers |
| DE10317526A1 (de) | 2003-04-16 | 2004-11-04 | Degussa Ag | Verfahren zum Delignifizieren von ligninhaltigen Faserstoffen |
| CA2521625A1 (en) | 2003-04-17 | 2004-11-04 | Merck & Co., Inc. | Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity |
| WO2004096767A1 (en) | 2003-04-25 | 2004-11-11 | H. Lundbeck A/S | Sustituted indoline and indole derivatives |
| AU2004253543B2 (en) * | 2003-07-01 | 2009-02-19 | Merck & Co., Inc. | Ophthalmic compositions for treating ocular hypertension |
| KR20060118398A (ko) * | 2003-08-05 | 2006-11-23 | 버텍스 파마슈티칼스 인코포레이티드 | 전압 개폐 이온 채널 억제제로서의 축합 피라미딘 화합물 |
| US20050239767A1 (en) * | 2003-10-28 | 2005-10-27 | Chan Michael K | Intermolecular SNAr of the heterocycle-activated nitro and fluoro groups-application in the synthesis of polyazamacrocyclic ligands |
| AU2004305318A1 (en) | 2003-12-18 | 2005-07-07 | Pfizer Products Inc. | Methods of treating acute inflammation in animals with p38 MAP kinase inhibitors |
| US7306631B2 (en) | 2004-03-30 | 2007-12-11 | The Procter & Gamble Company | Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof |
| GB0412986D0 (en) * | 2004-06-10 | 2004-07-14 | Xention Discovery Ltd | Compounds |
| WO2006002470A1 (en) | 2004-06-30 | 2006-01-12 | Monash University | Chiral ligands for asymmetric catalysis |
| JP2006063064A (ja) | 2004-07-27 | 2006-03-09 | Takeda Chem Ind Ltd | 受容体作動剤 |
| JP2007297283A (ja) | 2004-07-28 | 2007-11-15 | Santen Pharmaceut Co Ltd | 新規桂皮酸関連化合物 |
| CA2577060A1 (en) | 2004-08-13 | 2006-02-23 | Amgen Inc. | Substituted benzofused heterocycles |
| US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
| JP2008510810A (ja) | 2004-08-23 | 2008-04-10 | メルク エンド カムパニー インコーポレーテッド | 糖尿病の治療または予防のためのジペプチジルペプチダーゼ−iv阻害剤としての縮合トリアゾール誘導体 |
| CA2579850A1 (en) | 2004-09-13 | 2006-03-23 | Merck & Co., Inc. | Tricyclic anilide spirohydantoin cgrp receptor antagonists |
| WO2006048727A1 (en) | 2004-11-02 | 2006-05-11 | Pfizer Products Inc. | Piperazinylphenalkyl lactam/amine ligands for the 5ht1b receptor |
| WO2006091897A2 (en) | 2005-02-25 | 2006-08-31 | Adenosine Therapeutics, Llc | Derivatives of 8-substituted xanthines |
| TW200643015A (en) | 2005-03-11 | 2006-12-16 | Akzo Nobel Nv | 2-(4-oxo-4H-quinazolin-3-yl)acetamide derivatives |
| AR056317A1 (es) | 2005-04-20 | 2007-10-03 | Xenon Pharmaceuticals Inc | Compuestos de oxindol y composicion farmaceutica |
| PT2444079T (pt) | 2005-05-17 | 2017-03-03 | Sarcode Bioscience Inc | Composições e métodos para tratamento de distúrbios dos olhos |
| TW200714597A (en) | 2005-05-27 | 2007-04-16 | Astrazeneca Ab | Chemical compounds |
| US7572807B2 (en) * | 2005-06-09 | 2009-08-11 | Bristol-Myers Squibb Company | Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors |
| US7632837B2 (en) | 2005-06-17 | 2009-12-15 | Bristol-Myers Squibb Company | Bicyclic heterocycles as cannabinoid-1 receptor modulators |
| US7572808B2 (en) | 2005-06-17 | 2009-08-11 | Bristol-Myers Squibb Company | Triazolopyridine cannabinoid receptor 1 antagonists |
| EP1893617A1 (en) | 2005-06-17 | 2008-03-05 | Wyeth a Corporation of the State of Delaware | Tricyclic compounds useful as serotonin inhibitors and 5-ht1a agonists and antagonists |
| WO2007004028A2 (en) | 2005-06-30 | 2007-01-11 | Ranbaxy Laboratories Limited | Processes for the preparation of penems and its intermediate |
| GB0516963D0 (en) * | 2005-08-18 | 2005-09-28 | Carbonite Corp | Liquid dispensers |
| US8932641B2 (en) | 2005-08-26 | 2015-01-13 | Amnos Co., Ltd. | Dried amnion and method for drying treatment of amnion |
| JP2009508963A (ja) * | 2005-09-21 | 2009-03-05 | インサイト・コーポレイション | アミド化合物および医薬組成物としてのその使用 |
| EP1940850A2 (en) | 2005-09-23 | 2008-07-09 | Schering Corporation | Fused tetracyclic mglur1 antagonists as therapeutic agents |
| US20090022694A1 (en) | 2005-10-18 | 2009-01-22 | Distefano Peter | Sirt1 inhibition |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| US7851464B2 (en) | 2005-11-18 | 2010-12-14 | Merck Sharp & Dohme Corp. | Spirolactam aryl CGRP receptor antagonists |
| JP2009515976A (ja) | 2005-11-18 | 2009-04-16 | メルク エンド カムパニー インコーポレーテッド | スピロラクタム二環式cgrp受容体アンタゴニスト |
| TW200734342A (en) | 2005-12-15 | 2007-09-16 | Astrazeneca Ab | New compounds for the treatment of cardiac arrhythmias |
| ZA200804496B (en) | 2005-12-16 | 2009-09-30 | Alcon Inc | Control of intraocular pressure using ALK5 modulation agents |
| US8013073B2 (en) | 2005-12-30 | 2011-09-06 | Chevron Oronite Company Llc | Method for preparing polyolefins containing vinylidine end groups using nonaromatic heterocyclic compounds |
| JP2009531390A (ja) * | 2006-03-31 | 2009-09-03 | ノバルティス アクチエンゲゼルシャフト | 有機化合物 |
| US8883781B2 (en) | 2006-06-12 | 2014-11-11 | Vertex Pharmaceuticals Incorporated | Thienopyrimidines useful as modulators of ion channels |
| WO2008005338A1 (en) | 2006-06-29 | 2008-01-10 | Arena Pharmaceuticals, Inc. | Modulators of the histamine h3-receptor useful for the treatment of disorders related thereto |
| CN101541783B (zh) | 2006-06-30 | 2014-10-01 | 苏尼西斯制药有限公司 | 吡啶酮基pdk1抑制剂 |
| WO2008007661A1 (en) | 2006-07-11 | 2008-01-17 | Takeda Pharmaceutical Company Limited | Tricyclic heterocyclic compound and use thereof |
| CA2656855A1 (en) | 2006-07-12 | 2008-01-17 | Christoph Luthy | Triazolopyridine derivatives as herbicides |
| PE20121506A1 (es) * | 2006-07-14 | 2012-11-26 | Amgen Inc | Compuestos triazolopiridinas como inhibidores de c-met |
| US8217177B2 (en) | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| JP2010505855A (ja) * | 2006-10-06 | 2010-02-25 | アボット・ラボラトリーズ | 新規なイミダゾチアゾール類およびイミダゾオキサゾール類 |
| WO2008118141A2 (en) | 2006-10-17 | 2008-10-02 | Acadia Pharmaceuticals Inc. | Use of cannabinoid modulating compounds in combination with other therapeutic compounds for adjunctive therapy |
| MX2009004426A (es) * | 2006-10-23 | 2009-08-12 | Cephalon Inc | Derivados biciclicos fusionados de 2,4-diaminopirimidina como inhibidores alk y c-met. |
| CL2007003108A1 (es) | 2006-10-28 | 2008-07-18 | Methylgene Inc Envivo Pharmace | Compuestos derivados de n-hidroxiamida sustituida con heterociclos, inhibidores de histona desacetilasa; composicion farmaceutica que comprende a dichos compuestos; y uso para tratar una enfermedad del grupo que consiste en enfermedad de huntington, |
| JPWO2008053913A1 (ja) * | 2006-11-02 | 2010-02-25 | 塩野義製薬株式会社 | Mmp−13を選択的に阻害するスルホニルウレア誘導体 |
| WO2008080012A1 (en) | 2006-12-21 | 2008-07-03 | Cv Therapeutics, Inc. | Reduction of cardiovascular symptoms |
| US8076350B2 (en) | 2006-12-22 | 2011-12-13 | Abbott Laboratories | Spirocyclic azaadamantane derivatives and methods of use |
| WO2008094909A2 (en) | 2007-01-29 | 2008-08-07 | Xenon Pharmaceuticals Inc. | Quinazolinone and fused pyrimidinone compounds and their use in treating sodium channel-mediated diseases or conditions |
| EP2131657A1 (en) * | 2007-02-28 | 2009-12-16 | Merck & Co., Inc. | Substituted benzodiazepinones, benzoxazepinones and benzothiazepinones as sodium channel blockers |
| JP5497429B2 (ja) | 2007-03-07 | 2014-05-21 | 武田薬品工業株式会社 | ベンゾオキサゼピン誘導体およびその用途 |
| GB0706072D0 (en) | 2007-03-28 | 2007-05-09 | Sterix Ltd | Compound |
| WO2008134553A1 (en) | 2007-04-26 | 2008-11-06 | Xenon Pharmaceuticals Inc. | Methods of using bicyclic compounds in treating sodium channel-mediated diseases |
| WO2008144483A2 (en) | 2007-05-18 | 2008-11-27 | Armgo Pharma, Inc. | Agents for treating disorders involving modulation of ryanodine receptors |
| US8188083B2 (en) * | 2007-06-28 | 2012-05-29 | Abbott Laboratories | Triazolopyridazines |
| US20110263569A1 (en) | 2007-08-22 | 2011-10-27 | President And Fellows Of Harvard College | Ryanodine channel binders and uses thereof |
| MX2010002760A (es) * | 2007-09-12 | 2010-04-01 | Wyeth Llc | Derivados de isoquinolinilo e isoindolinilo como antagonistas de la histamina-3. |
| US8119658B2 (en) | 2007-10-01 | 2012-02-21 | Bristol-Myers Squibb Company | Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| US8293763B2 (en) | 2007-12-19 | 2012-10-23 | Genentech, Inc. | 8-anilinoimidazopyridines and their use as anti-cancer and/or anti-inflammatory agents |
| EP2231669A1 (en) * | 2008-01-09 | 2010-09-29 | The U.S.A. As Represented By The Secretary, Department Of Health And Human Services | Phosphodiesterase inhibitors |
| KR20110013348A (ko) | 2008-02-06 | 2011-02-09 | 길리애드 사이언시즈, 인코포레이티드 | 통증 치료를 위한 라놀라진의 용도 |
| WO2009137499A1 (en) | 2008-05-05 | 2009-11-12 | Envivo Pharmaceuticals, Inc. | Inhibitors of histone deacetylase |
| US20110288070A1 (en) | 2008-05-05 | 2011-11-24 | ROGERS Kathryn | Methods for treating cognitive disorders using inhibitors of histone deacetylase |
| DE102008024182A1 (de) | 2008-05-19 | 2009-11-26 | Merck Patent Gmbh | Verbindungen für organische elektronische Vorrichtung |
| EA020807B1 (ru) | 2008-06-17 | 2015-01-30 | Астразенека Аб | Соединения пиридина |
| US8338477B2 (en) | 2008-07-11 | 2012-12-25 | Neumedics | Tetracycline derivatives with reduced antibiotic activity and neuroprotective benefits |
| WO2010018686A1 (ja) | 2008-08-12 | 2010-02-18 | 日本曹達株式会社 | 含窒素ヘテロ環誘導体および農園芸用殺菌剤 |
| WO2010022001A1 (en) | 2008-08-18 | 2010-02-25 | Im&T Research, Inc. | Methods for preparing fluoroalkyl arylsulfinyl compounds and fluorinated compounds thereto |
| JP2012502047A (ja) | 2008-09-04 | 2012-01-26 | ギリアード サイエンシーズ, インコーポレイテッド | 心房細動を治療する方法 |
| US20100113461A1 (en) * | 2008-10-29 | 2010-05-06 | Gilead Palo Alto, Inc. | Substituted heterocyclic compounds |
| WO2010056527A2 (en) * | 2008-10-30 | 2010-05-20 | Gilead Palo Alto, Inc. | Fused heterocyclic compounds as ion channel modulators |
| US20110319411A1 (en) | 2008-12-08 | 2011-12-29 | Sirtis Pharmaceuticals, Inc. | Isoindolinone and related analogs as sirtuin modulators |
| EP2376495A4 (en) | 2008-12-08 | 2012-10-31 | Vm Pharma Llc | COMPOSITIONS OF PROTEIN RECEPTOR TYROSINE KINASE INHIBITORS |
| FR2943342B1 (fr) * | 2009-03-20 | 2011-03-04 | Servier Lab | Nouveaux derives de benzothiadiazepines,leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| US9150554B2 (en) | 2009-03-27 | 2015-10-06 | Presidio Pharmaceuticals, Inc. | Fused ring inhibitors of hepatitis C |
| US20100305093A1 (en) | 2009-04-09 | 2010-12-02 | Exelixis, Inc. | Inhibitors of mTOR and Methods of Making and Using |
| DK2464645T3 (en) | 2009-07-27 | 2017-10-23 | Gilead Sciences Inc | CONDENSED, HETEROCYCLIC COMPOUNDS AS IRON CHANNEL MODULATORS |
| SI2483278T1 (sl) | 2009-09-28 | 2014-03-31 | F. Hoffmann-La Roche Ag | Inhibitorske spojine benzoksazepina pi3k in njihova uporaba pri zdravljenju raka |
| CN104530079B (zh) | 2009-12-18 | 2017-10-20 | 北京凯因科技股份有限公司 | C型肝炎病毒复制的新型抑制剂 |
| TWI508726B (zh) * | 2009-12-21 | 2015-11-21 | Gilead Sciences Inc | 治療心房纖維性顫動之方法 |
| US8703759B2 (en) * | 2010-07-02 | 2014-04-22 | Gilead Sciences, Inc. | Fused heterocyclic compounds as ion channel modulators |
| WO2012019071A1 (en) | 2010-08-06 | 2012-02-09 | The Trustees Of Columbia University In The City Of New York | Methods of preventing and treating sarcopenia |
| WO2012019076A1 (en) | 2010-08-06 | 2012-02-09 | The Trustees Of Columbia University In The City Of New York | Compositions and methods for preventing and treating cardiac ischemia/reperfusion injury |
| WO2012037105A1 (en) | 2010-09-14 | 2012-03-22 | The Trustees Of Columbia University In The City Of New York | Methods of treating, ameliorating or preventing stress-induced neuronal disorders and diseases |
| WO2012050918A2 (en) | 2010-09-29 | 2012-04-19 | Presidio Pharmaceutical, Inc. | Tricyclic fused ring inhibitors of hepatitis c |
| WO2012071509A2 (en) | 2010-11-24 | 2012-05-31 | Exelixis, Inc. | Benzoxazepines as inhibitors of p13k/mtor and methods of their use and manufacture |
| PL2707361T3 (pl) * | 2011-05-10 | 2018-01-31 | Gilead Sciences Inc | Skondensowane związki heterocykliczne stosowane jako modulatory kanału sodowego |
| NO3175985T3 (es) * | 2011-07-01 | 2018-04-28 | ||
| TWI622583B (zh) | 2011-07-01 | 2018-05-01 | 基利科學股份有限公司 | 作為離子通道調節劑之稠合雜環化合物 |
| WO2013112932A1 (en) | 2012-01-27 | 2013-08-01 | Gilead Sciences, Inc. | Combination therapies using late sodium ion channel blockers and potassium ion channel blockers |
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