AR069637A1 - Derivados de pirazinas - Google Patents
Derivados de pirazinasInfo
- Publication number
- AR069637A1 AR069637A1 ARP080105334A AR069637A1 AR 069637 A1 AR069637 A1 AR 069637A1 AR P080105334 A ARP080105334 A AR P080105334A AR 069637 A1 AR069637 A1 AR 069637A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atoms
- groups
- optionally substituted
- alkyl
- heterocyclic group
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P11/08—Bronchodilators
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- C07D471/10—Spiro-condensed systems
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
-
- 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
-
- 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
- C07D487/10—Spiro-condensed systems
Abstract
Compuestos utiles para el tratamiento de enfermedades que respondan al bloqueo del canal de sodio epitelial. También se describen composiciones farmacéuticas que contienen los compuestos, y procesos para la preparacion de los compuestos. Reivindicacion 1: Un compuesto de la formula (1), o solvatos, hidratos o sales farmacéuticamente aceptables del mismo, en donde R1 es H, halogeno, alquilo de 1 a 8 átomos de carbono, halo-alquilo de 1 a 8 átomos de carbono, halo-alcoxilo de 1 a 8 átomos de carbono, grupo carbocíclico de 3 a 15 átomos de carbono, nitro, ciano, un grupo carbocíclico aromático de 6 a 15 miembros, o un alquilo de 1 a 8 átomos de carbono sustituido por un grupo carbocíclico aromático de 6 a 15 miembros; R2, R3, R4 y R5 se seleccionan cada uno independientemente a partir de H y alquilo de 1 a 6 átomos de carbono; R6, R7, R8, R9, R10 y R11 se seleccionan cada uno independientemente a partir de H; SO2R16; arilo opcionalmente sustituido por uno o más grupos Z; un grupo carbocíclico de 3 a 10 átomos de carbono opcionalmente sustituido por uno o más grupos Z; un grupo heterocíclico de 3 a 14 átomos de carbono opcionalmente sustituido por uno o más grupos Z; alquilo de 1 a 8 átomos de carbono opcionalmente sustituido por un grupo arilo que está opcionalmente sustituido por uno o más grupos Z, un grupo carbocíclico de 3 a 10 átomos de carbono opcionalmente sustituido por uno o más grupos Z, o un grupo heterocíclico de 3 a 14 átomos de carbono opcionalmente sustituido por uno o más grupos Z; o está representado por la formula (2): -(alquileno de 0 a 6 átomos de carbono)-A(alquileno de 0 a 6 átomos de carbono)-B-(X-R12)q-R22 (2); en donde los grupos alquileno están opcionalmente sustituidos por uno o más grupos Z; o R6 y R7, junto con los átomos con los que están unidos, forman un grupo heterocíclico de 3 a 10 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos adicionales seleccionados a partir de N, O y S, y estando el grupo heterocíclico opcionalmente sustituido por uno o más grupos Z; SO2R16 grupo carbocíclico aromático de 6 a 15 átomos de carbono opcionalmente sustituido por uno o más grupos Z; un grupo carbocíclico de 3 a 10 átomos de carbono; un grupo heterocíclico de 3 a 14 átomos de carbono opcionalmente sustituido por uno o más grupos Z; o un grupo representado por la formula (2); o R7 y R8, junto con el átomo de carbono con el que están unidos, forman un grupo carbocíclico o heterocíclico de 3 a 10 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos seleccionados a partir de N, O y S, y estando los grupos carbocíclico y heterocíclico opcionalmente sustituidos por uno o más grupos Z; SO2R16; grupo carbocíclico aromático de 6 a 15 átomos de carbono opcionalmente sustituido por uno o más grupos Z; un grupo carbocíclico de 3 a 10 átomos de carbono; un grupo heterocíclico de 3 a 14 átomos de carbono opcionalmente sustituido por uno o más grupos Z; o un grupo representado por la formula 2; o R9 y R10, junto con el átomo de carbono con el que están unidos, forman un grupo carbocíclico o heterocíclico de 3 a 10 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos seleccionados a partir de N, O y S, y estando los grupos carbocíclico y heterocíclico opcionalmente sustituidos por uno o más grupos Z; SO2R16; grupo carbocíclico aromático de 6 a 15 átomos de carbono opcionalmente sustituido por uno o más grupos Z; un grupo carbocíclico de 3 a 10 átomos de carbono; un grupo heterocíclico de 3 a 14 átomos de carbono opcionalmente sustituido por uno o más grupos Z; o un grupo representado por la formula 2; o R8 y R9, junto con los átomos de carbono con los que están unidos, forman un cicloalquilo de 3 a 10 miembros, o un grupo heterocíclico de 3 a 10 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos seleccionados a partir de N, O y S, y estando los grupos carbocíclico y heterocíclico opcionalmente sustituidos por uno o más grupos Z; SO2R16; grupo carbocíclico aromático de 6 a 15 átomos de carbono opcionalmente sustituido por uno o más grupos Z; un grupo carbocíclico de 3 a 10 átomos de carbono; un grupo heterocíclico de 3 a 14 átomos de carbono opcionalmente sustituido por uno o más grupos Z; o un grupo representado por la formula (2); o R10 y R11, junto con los átomos con los que están unidos, forman un grupo heterocíclico de 3 a 10 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos adicionales seleccionados a partir de N, O y S, y estando el grupo heterocíclico opcionalmente sustituido por uno o más grupos Z; SO2R16; grupo carbocíclico aromático de 6 a 15 átomos de carbono opcionalmente sustituido por uno o más grupos Z; un grupo carbocíclico de 3 a 10 átomos de carbono; un grupo heterocíclico de 3 a 14 átomos de carbono opcionalmente sustituido por uno o más grupos Z; o un grupo representado por la formula (2); A se selecciona a partir de un enlace, -NR13(SO2)-, -(SO2)NR13-, -(SO2)-, -NR13C(O)-, -C(O)NR13-, -NR13C(O)NR14-, -NR13C(O)O-, -NR13-, C(O)O, OC(O), C(O), O y S; B se selecciona a partir de un enlace, -(grupo alquenilo de 2 a 4 átomos de carbono)-, -(grupo alquinilo de 2 a 4 átomos de carbono)-, -NH-, arilo, O-arilo, NH-arilo, un grupo carbocíclico de 3 a 14 átomos de carbono, y un grupo heterocíclico de 3 a 14 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos seleccionados a partir de N, O y S, en donde los grupos arilo, carbocíclico y heterocíclico están cada uno opcionalmente sustituidos por uno o más grupos Z; X se selecciona a partir de un enlace, -NR15(SO2)-, -(SO2)NR15-, -(SO2)-, -NR15C(O)-, -C(O)NR15-, -NR15C(O)NR17-, -NR15C(O)O-, -NR15-, C(O)O, CO(O), C(O), O y S; R12 se selecciona a partir de alquileno de 1 a 8 átomos de carbono, alquenileno de 1 a 8 átomos de carbono, -cicloalquilo de 3 a 8 átomos de carbono-, -alquileno de 1 a 8 átomos de carbono, -cicloalquilo de 3 a 8 átomos de carbono-, y -arilo-, en donde los grupos alquileno, cicloalquilo y arilo están opcionalmente sustituidos por uno o más grupos Z; R13, R14, R15 y R17 se seleccionan cada uno independientemente a partir de H y alquilo de 1 a 6 átomos de carbono; R16 se selecciona a partir de alquilo de 1 a 8 átomos de carbono, arilo, y un grupo heterocíclico de 3 a 14 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos seleccionados a partir de N, O, y S; Z se selecciona independientemente a partir de OH, arilo, O-arilo, aralquilo de 7 a 14 átomos de carbono, O-aralquilo de 7 a 14 átomos de carbono, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, NR19(SO2)R21, (SO2)NR19R21, (SO2)R20, NR19C(O)R20, C(O)NR19R20. NR19C(O)NR20R18. NR19C(O)OR20, NR19R21, C(O)OR10, C(O)R19, SR19, OR19, oxo, CN, NO2, y halogeno, en donde los grupos alquilo. alcoxilo, aralquilo y arilo están cada uno opcionalmente sustituidos por uno o más sustituyentes seleccionados a partir de OH, halogeno, halo-alquilo de 1 a 4 átomos de carbono y alcoxilo de 1 a 4 átomos de carbono; R18 y R20 se seleccionan cada uno independientemente a partir de H y alquilo de 1 a 6 átomos de carbono; R19 y R21 se seleccionan cada uno independientemente a partir de H; alquilo de 1 a 8 átomos de carbono; cicloalquilo de 3 a 8 átomos de carbono; alcoxilo de 1 a 4 átomos de carbono-alquilo de 1 a 4 átomos de carbono; (alquilo de 0 a 4 átomos de carbono)-arilo opcionalmente sustituido por uno o más grupos seleccionados a partir de alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono y halogeno; (alquilo de 0 a 4 átomos de carbono)-grupo heterocíclico de 3 a 14 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos seleccionados a partir de N, O y S, opcionalmente sustituido por uno o más grupos seleccionados a partir de halogeno, oxo, alquilo de 1 a 6 átomos de carbono y C(O)alquilo de 1 a 6 átomos de carbono; (alquilo de 0 a 4 átomos de carbono)-O-arilo opcionalmente sustituido por uno o más grupos seleccionados a partir de alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono y halogeno; y (alquilo de 0 a 4 átomos de carbono)-O-grupo heterocíclico de 3 a 14 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos seleccionados a partir de N, O y S, opcionalmente sustituido por uno o más grupos seleccionados a partir de halogeno, alquilo de 1 a 6 átomos de carbono y C(O)-alquilo de 1 a 6 átomos de carbono; en donde los grupos alquilo y alcoxilo están opcionalmente sustituidos por uno o más átomos de halogeno, alcoxilo de 1 a 4 átomos de carbono, C(O)NH2, C(O)NH-alquilo de 1 a 6 átomos de carbono o C(O)N(alquilo de 1 a 6 átomos de carbono)2 ; o R19 y R20, junto con el átomo de nitrogeno con el que están unidos, forman un grupo heterocíclico de 5 a 10 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos adicionales seleccionados a partir de N, O y S, estando el grupo heterocíclico opcionalmente sustituido por uno o más sustituyentes seleccionados a partir de OH; halogeno; arilo; grupo heterocíclico de 5 a 10 miembros que incluye uno o más heteroátomos seleccionados a partir de N, O, y S; S(O)2-arilo; S(O)2-alquilo de 1 a 6 átomos de carbono; alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por uno o más átomos de halogeno; alcoxilo de 1 a 6 átomos de carbono opcionalmente sustituido por uno o más grupos OH, o alcoxilo de 1 a 4 átomos de carbono; y C(O)O-alquilo de 1 a 6 átomos de carbono, en donde los grupos sustituyentes de arilo y heterocíclicos están ellos mismos opcionalmente sustituidos por alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono o alcoxilo de 1 a 6 átomos de carbono; R22 se selecciona a partir de H, halogeno, alquilo de 1 a 8 átomos de carbono, alcoxilo de 1 a 8 átomos de carbono. arilo, O-arilo, S(O)2-arilo, S(O)2-alquilo de 1 a 6 átomos de carbono, S(O)2NR23R24, NHS(O)2NR23R24, un grupo carbocíclico de 3 a 14 átomos de carbono, un grupo heterocíclico de 3 a 14 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos selecciona
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP07122739 | 2007-12-10 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR069637A1 true AR069637A1 (es) | 2010-02-10 |
Family
ID=39322745
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP080105334 AR069637A1 (es) | 2007-12-10 | 2008-12-09 | Derivados de pirazinas |
Country Status (30)
Country | Link |
---|---|
US (5) | US8039472B2 (es) |
EP (3) | EP2520574A1 (es) |
JP (1) | JP5455922B2 (es) |
KR (1) | KR101578235B1 (es) |
CN (1) | CN101939054B (es) |
AR (1) | AR069637A1 (es) |
AU (1) | AU2008334629B2 (es) |
BR (1) | BRPI0820669A2 (es) |
CA (1) | CA2707857C (es) |
CL (1) | CL2008003651A1 (es) |
CO (1) | CO6310968A2 (es) |
CR (1) | CR11470A (es) |
CU (1) | CU23967B1 (es) |
EA (1) | EA017919B1 (es) |
EC (1) | ECSP10010242A (es) |
ES (2) | ES2654395T3 (es) |
HN (1) | HN2010001165A (es) |
IL (1) | IL206165A0 (es) |
MA (1) | MA31894B1 (es) |
MX (1) | MX2010006421A (es) |
MY (1) | MY152955A (es) |
NZ (1) | NZ585789A (es) |
PE (1) | PE20091096A1 (es) |
PL (1) | PL2444120T3 (es) |
PT (1) | PT2444120T (es) |
TN (1) | TN2010000256A1 (es) |
TW (1) | TWI439462B (es) |
UA (1) | UA104997C2 (es) |
WO (1) | WO2009074575A2 (es) |
ZA (1) | ZA201003837B (es) |
Families Citing this family (89)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6858615B2 (en) | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenyl guanidine sodium channel blockers |
US8354427B2 (en) | 2004-06-24 | 2013-01-15 | Vertex Pharmaceutical Incorporated | Modulators of ATP-binding cassette transporters |
EA017919B1 (ru) * | 2007-12-10 | 2013-04-30 | Новартис Аг | Производные пиразин-2-карбоксамида для лечения заболеваний, которые поддаются лечению путем блокирования эпителиальных натриевых каналов |
MX344703B (es) | 2008-02-26 | 2017-01-03 | Parion Sciences Inc | Bloqueadores de canal de sodio poliaromaticos. |
UA103198C2 (en) | 2008-08-04 | 2013-09-25 | Новартис Аг | Squaramide derivatives as cxcr2 antagonists |
WO2010039260A2 (en) * | 2008-10-02 | 2010-04-08 | The Johns Hopkins University | Spiperone derivatives and methods of treating disorders |
NZ592685A (en) | 2008-10-23 | 2013-04-26 | Vertex Pharma | Modulators of cystic fibrosis transmembrane conductance regulator |
EP2433940B9 (en) * | 2009-04-28 | 2015-10-28 | Chugai Seiyaku Kabushiki Kaisha | Spiroimidazolone derivative |
WO2010138794A2 (en) | 2009-05-29 | 2010-12-02 | The University Of North Carolina At Chapel Hill | Regulation of sodium channels by plunc proteins |
US20110098311A1 (en) * | 2009-10-22 | 2011-04-28 | Vertex Pharmaceuticals Incorported | Compositions for treatment of cystic fibrosis and other chronic diseases |
NZ600172A (en) | 2009-10-23 | 2014-07-25 | Vertex Pharma | Process for preparing modulators of cystic fibrosis transmembrane conductance regulator |
US8389727B2 (en) | 2009-10-23 | 2013-03-05 | Vertex Pharmaceuticals Incorporated | Solid forms of N-(4-(7-Azabicyclo[2.2.1]Heptan-7-yl)-2-Trifluoromethyl)Phenyl)-4-Oxo-5-(Trifluoromethyl)-1,4-Dihydroquinoline-3-Carboxamide |
WO2011146886A1 (en) | 2010-05-20 | 2011-11-24 | Vertex Pharmaceuticals Incorporated | Processes for producing modulators of cystic fibrosis transmembrane conductance regulator |
US9050339B2 (en) | 2010-09-17 | 2015-06-09 | Novartis Ag | Pyrazine derivatives as ENaC blockers |
US8372845B2 (en) * | 2010-09-17 | 2013-02-12 | Novartis Ag | Pyrazine derivatives as enac blockers |
AR086745A1 (es) | 2011-06-27 | 2014-01-22 | Parion Sciences Inc | 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil)carbamimidoil)pirazina-2-carboxamida |
KR102024955B1 (ko) | 2011-09-02 | 2019-09-24 | 노파르티스 아게 | 치환된 시클로부텐디온 항염 화합물의 콜린 염 |
JP6091513B2 (ja) | 2011-11-02 | 2017-03-08 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 複素環化合物、前記化合物を含む薬物、これらの使用及びこれらの調製方法 |
AU2012331275A1 (en) | 2011-11-02 | 2014-04-03 | Boehringer Ingelheim International Gmbh | Novel process for the preparation of acylguanidines and acylthioureas |
US8809340B2 (en) | 2012-03-19 | 2014-08-19 | Novartis Ag | Crystalline form |
WO2013155406A1 (en) * | 2012-04-12 | 2013-10-17 | The Chinese University Of Hong Kong | Contragestion and treating inflammation by modulating sodium channel activity in the epithelium |
EP2838882A1 (en) | 2012-04-20 | 2015-02-25 | Vertex Pharmaceuticals Incorporated | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
WO2014044849A1 (en) * | 2012-09-24 | 2014-03-27 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof |
HRP20181740T4 (hr) | 2012-11-02 | 2024-01-05 | Vertex Pharmaceuticals Incorporated | Farmaceutski pripravci za liječenje bolesti koje su posredovane s cftr |
NO2930176T3 (es) | 2012-12-10 | 2018-07-07 | ||
MX2015007797A (es) | 2012-12-17 | 2015-10-05 | Parion Sciences Inc | Compuestos de 3,5-diamino-6-cloro-n-(n-(4-fenilbutil) carbamimidoil) pirazin-2-carboxamida. |
ES2674665T3 (es) * | 2012-12-17 | 2018-07-03 | Parion Sciences, Inc. | Compuestos de 3,5-diamino-6-cloro-N-(N-(4-fenilbutilo)carbamimidoilo)-pirazina-2-carboxamida |
WO2014099676A1 (en) | 2012-12-17 | 2014-06-26 | Parion Sciences, Inc. | Chloro-pyrazine carboxamide derivatives useful for the treatment of diseases favoured by insufficient mucosal hydration |
CN105189478B (zh) | 2013-01-07 | 2019-10-22 | 南加州大学 | 脱氧尿苷三磷酸酶抑制剂 |
DE202013000888U1 (de) | 2013-01-29 | 2014-05-05 | WKW Erbslöh Automotive GmbH | Vorrichtung zur Abdeckung eines in Längsrichtung eines Kraftfahrzeuges verlaufenden Dachkanals |
EP2970468B1 (en) | 2013-03-13 | 2021-07-07 | Novartis AG | Notch2 binding molecules for treating respiratory diseases |
EP2991981B1 (en) * | 2013-04-30 | 2017-03-01 | Boehringer Ingelheim International GmbH | Diaminopyrazine compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof |
EP2815749A1 (en) | 2013-06-20 | 2014-12-24 | IP Gesellschaft für Management mbH | Solid form of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione having specified X-ray diffraction pattern |
EP3016944A4 (en) * | 2013-07-02 | 2016-11-16 | California Inst Biomedical Res | COMPOUNDS FOR THE TREATMENT OF CYSTIC FIBROSIS |
US9102633B2 (en) | 2013-12-13 | 2015-08-11 | Parion Sciences, Inc. | Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds |
CA2935717C (en) | 2014-01-03 | 2022-06-21 | University Of Southern California | Uracil isostere and pharmaceutical compositions thereof useful as deoxyuridine triphosphatase inhibitors |
UY36034A (es) | 2014-03-18 | 2015-09-30 | Astrazeneca Ab | Derivados de 3,5-diamino-6-cloro-pirazina-2-carboxamida y sales farmaceuticamente aceptables de estos |
EP2932966A1 (en) | 2014-04-16 | 2015-10-21 | Novartis AG | Gamma secretase inhibitors for treating respiratory diseases |
BR112016003511B8 (pt) | 2014-06-09 | 2023-10-03 | Chugai Pharmaceutical Co Ltd | Composição farmacêutica que contém derivados de hidantoína e uso dos mesmos |
SG11201702769QA (en) | 2014-10-08 | 2017-05-30 | Univ North Carolina | Improved peptide inhibitors of sodium channels |
CA2966023A1 (en) | 2014-10-31 | 2016-05-06 | Abbvie S.A.R.L. | Substituted tetrahydropyrans and method of use |
EP3245201B1 (en) * | 2015-01-12 | 2019-06-19 | Boehringer Ingelheim International GmbH | Substituted benzimidazolium compounds useful in the treatment of respiratory diseases |
US10155749B2 (en) * | 2015-01-12 | 2018-12-18 | Boehringer Ingelheim International Gmbh | Substituted benzimidazolium compounds useful in the treatment of respiratory diseases |
WO2016113169A1 (en) * | 2015-01-12 | 2016-07-21 | Boehringer Ingelheim International Gmbh | Tetra- and pentasubstituted benzimidazolium compounds useful in the treatment of respiratory diseases |
AU2016272702A1 (en) | 2015-06-02 | 2017-12-21 | Abbvie S.A.R.L. | Substituted pyridines and method of use |
FR3038605B1 (fr) * | 2015-07-06 | 2018-08-24 | Universite Amiens Picardie Jules Verne | Diamines primaires vicinales associees a des motifs chelateurs de metaux et/ou de radicaux libres, actives contre les stress carbonyle et oxydant et leur utilisation |
WO2017006271A1 (en) | 2015-07-08 | 2017-01-12 | University Of Southern California | Deoxyuridine triphosphatase inhibitors containing amino sulfonyl linkage |
US10544105B2 (en) | 2015-07-08 | 2020-01-28 | Cv6 Therapeutics (Ni) Limited | Deoxyuridine triphosphatase inhibitors containing cyclopropano linkage |
WO2017006282A1 (en) | 2015-07-08 | 2017-01-12 | Cv6 Therapeutics (Ni) Limited | Hydantoin containing deoxyuridine triphosphatase inhibitors |
WO2017006270A1 (en) | 2015-07-08 | 2017-01-12 | University Of Southern California | Deoxyuridine triphosphatase inhibitors |
US9840513B2 (en) | 2015-07-16 | 2017-12-12 | Abbvie S.Á.R.L. | Substituted tricyclics and method of use |
CA3001094A1 (en) | 2015-10-09 | 2017-04-13 | Abbvie S.A.R.L. | Substituted pyrazolo[3,4-b]pyridin-6-carboxylic acids and their use |
KR20180083323A (ko) | 2015-10-09 | 2018-07-20 | 애브비 에스.에이.알.엘. | N-설포닐화 피라졸로[3,4-b]피리딘-6-카복스아미드 및 사용 방법 |
US10130622B2 (en) | 2015-10-09 | 2018-11-20 | Abbvie S.Á.R.L. | Compounds for treatment of cystic fibrosis |
US10402062B2 (en) * | 2016-04-16 | 2019-09-03 | Apple Inc. | Organized timeline |
CN109219602A (zh) | 2016-04-26 | 2019-01-15 | 艾伯维公司 | 囊性纤维化跨膜传导调节物蛋白的调节剂 |
US10138227B2 (en) | 2016-06-03 | 2018-11-27 | Abbvie S.Á.R.L. | Heteroaryl substituted pyridines and methods of use |
GB201610854D0 (en) | 2016-06-21 | 2016-08-03 | Entpr Therapeutics Ltd | Compounds |
US10399940B2 (en) | 2016-10-07 | 2019-09-03 | Abbvie S.Á.R.L. | Substituted pyrrolidines and methods of use |
US9981910B2 (en) | 2016-10-07 | 2018-05-29 | Abbvie S.Á.R.L. | Substituted pyrrolidines and methods of use |
GB201619694D0 (en) | 2016-11-22 | 2017-01-04 | Entpr Therapeutics Ltd | Compounds |
US11168059B2 (en) | 2016-11-23 | 2021-11-09 | Cv6 Therapeutics (Ni) Limited | Amino sulfonyl compounds |
WO2018098208A1 (en) | 2016-11-23 | 2018-05-31 | Cv6 Therapeutics (Ni) Limited | Nitrogen ring linked deoxyuridine triphosphatase inhibitors |
WO2018098207A1 (en) | 2016-11-23 | 2018-05-31 | Cv6 Therapeutics (Ni) Limited | Hydantoin containing deoxyuridine triphosphatase inhibitors |
US11174271B2 (en) | 2016-11-23 | 2021-11-16 | Cv6 Therapeutics (Ni) Limited | 6-membered uracil isosteres |
US10858344B2 (en) | 2016-11-23 | 2020-12-08 | Cv6 Therapeutics (Ni) Limited | Hydantoin containing deoxyuridine triphosphatase inhibitors |
EP3558982A1 (en) | 2016-12-20 | 2019-10-30 | AbbVie S.À.R.L. | Deuterated cftr modulators and methods of use |
WO2018128720A1 (en) | 2017-01-05 | 2018-07-12 | Cv6 Therapeutics (Ni) Limited | Uracil containing compounds |
TW201831471A (zh) | 2017-02-24 | 2018-09-01 | 盧森堡商艾伯維公司 | 囊腫纖化症跨膜傳導調節蛋白的調節劑及其使用方法 |
EP3600440A1 (en) | 2017-03-20 | 2020-02-05 | Sienna Biopharmaceuticals, Inc. | Reduced exposure conjugates modulating therapeutic targets |
WO2018175302A1 (en) | 2017-03-20 | 2018-09-27 | Sienna Biopharmaceuticals, Inc. | Polymer conjugates targeting c-src with reduced exposure |
US10988454B2 (en) | 2017-09-14 | 2021-04-27 | Abbvie Overseas S.À.R.L. | Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
GB201717051D0 (en) | 2017-10-17 | 2017-11-29 | Enterprise Therapeutics Ltd | Compounds |
WO2019193062A1 (en) | 2018-04-03 | 2019-10-10 | Abbvie S.Á.R.L | Substituted pyrrolidines and their use |
GB201808093D0 (en) | 2018-05-18 | 2018-07-04 | Enterprise Therapeutics Ltd | Compounds |
EP3917516A4 (en) * | 2019-01-28 | 2022-10-12 | Flatley Discovery Lab, LLC | COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS |
US11345691B2 (en) | 2019-06-03 | 2022-05-31 | AbbVie Global Enterprises Ltd. | Prodrug modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
WO2021011327A1 (en) | 2019-07-12 | 2021-01-21 | Orphomed, Inc. | Compound for treating cystic fibrosis |
KR20220100625A (ko) | 2019-11-12 | 2022-07-15 | 젠자임 코포레이션 | 결핍된 cftr 활성에 의해 매개되는 질환 및 병태를 치료하기 위한 6원 헤테로아릴아미노설폰아미드 |
WO2021113806A1 (en) | 2019-12-05 | 2021-06-10 | Genzyme Corporation | Arylamides and methods of use thereof |
WO2021113809A1 (en) | 2019-12-05 | 2021-06-10 | Genzyme Corporation | Arylamides and methods of use thereof |
WO2022150174A1 (en) | 2021-01-06 | 2022-07-14 | AbbVie Global Enterprises Ltd. | Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
US20220213041A1 (en) | 2021-01-06 | 2022-07-07 | AbbVie Global Enterprises Ltd. | Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Protein and Methods of Use |
WO2023034946A1 (en) | 2021-09-03 | 2023-03-09 | Genzyme Corporation | Indole compounds and uses thereof in the treatement of cystic fibrosis |
CA3230259A1 (en) | 2021-09-03 | 2023-03-09 | Junkai Liao | Indole compounds and methods of use |
CN113880735A (zh) * | 2021-11-08 | 2022-01-04 | 湖北九宁化学科技有限公司 | 一种双氟磺酰二乙胺锂的制备方法 |
WO2024054851A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocyclic compounds, compositions and methods of using thereof |
WO2024054840A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocyclic compounds, compositions, and methods of using thereof |
WO2024054845A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocycic compounds, compositions, and methods of using thereof |
Family Cites Families (141)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3328404A (en) * | 1966-08-25 | 1967-06-27 | Merck & Co Inc | Derivatives of pyrazine |
US3432502A (en) * | 1966-08-25 | 1969-03-11 | Merck & Co Inc | Preparation of pyrazinoylguanidine and pyrazinamidoguanidine products |
NL6707564A (es) * | 1966-08-25 | 1968-02-26 | ||
IL27897A (en) * | 1966-08-25 | 1972-02-29 | Merck & Co Inc | Preparation of pyrazinoalguanides and pyrazinoamidoguanidines |
GB1219606A (en) | 1968-07-15 | 1971-01-20 | Rech S Et D Applic Scient Soge | Quinuclidinol derivatives and preparation thereof |
US3503972A (en) * | 1968-11-04 | 1970-03-31 | Merck & Co Inc | Alkyl n-amidino (or guanidino)-pyrazinimidates |
US3577418A (en) * | 1969-02-12 | 1971-05-04 | Merck & Co Inc | Pyrazinamide derivatives and processes for their preparation |
US3573306A (en) * | 1969-03-05 | 1971-03-30 | Merck & Co Inc | Process for preparation of n-substituted 3,5-diamino-6-halopyrazinamides |
US4085211A (en) * | 1975-12-15 | 1978-04-18 | Merck & Co., Inc. | Pyrazinecarboxamides and processes for preparing same |
US4246406A (en) | 1979-03-27 | 1981-01-20 | Merck & Co., Inc. | Heterocyclic substituted pyrazinoylguanidines |
US4272537A (en) * | 1980-07-02 | 1981-06-09 | Merck & Co., Inc. | 3-Amino-5-substituted-6-halo-N-(4,4-disubstituted-6-substituted-1,3,5-triazin-2-yl)-2-pyrazinecarboxamides |
US4277602A (en) * | 1980-07-02 | 1981-07-07 | Merck & Co., Inc. | 3-Amino-5-substituted-6-halo-N-(3,4-dihydro-6-substituted-1,3,5-truazin-2-yl)2-pyrazinecarboxamides |
JPS6235216A (ja) | 1985-08-09 | 1987-02-16 | Noritoshi Nakabachi | 不均質物質層の層厚非破壊測定方法および装置 |
EP0300431A3 (en) | 1987-07-22 | 1990-06-27 | Neorx Corporation | Method of radiolabeling chelating compounds comprising sulfur atoms with metal radionuclides |
GB8923590D0 (en) | 1989-10-19 | 1989-12-06 | Pfizer Ltd | Antimuscarinic bronchodilators |
PT100441A (pt) | 1991-05-02 | 1993-09-30 | Smithkline Beecham Corp | Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso |
WO1993018007A1 (en) | 1992-03-13 | 1993-09-16 | Tokyo Tanabe Company Limited | Novel carbostyril derivative |
WO1993019750A1 (en) | 1992-04-02 | 1993-10-14 | Smithkline Beecham Corporation | Compounds useful for treating allergic or inflammatory diseases |
CZ283425B6 (cs) | 1992-04-02 | 1998-04-15 | Smithkline Beecham Corporation | Fenylové deriváty a farmaceutické prostředky s jejich obsahem |
WO1993019751A1 (en) | 1992-04-02 | 1993-10-14 | Smithkline Beecham Corporation | Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor |
EP0620222A3 (en) | 1993-04-14 | 1995-04-12 | Lilly Co Eli | Tetrahydro-beta-carbolines. |
EP0702004A2 (de) | 1994-09-15 | 1996-03-20 | Ciba-Geigy Ag | 2,9-Diamino- und 2-amino-8-carbamoyl-4-hydroxy-alkansäureamid-derivative |
GB9622386D0 (en) | 1996-10-28 | 1997-01-08 | Sandoz Ltd | Organic compounds |
US6166037A (en) | 1997-08-28 | 2000-12-26 | Merck & Co., Inc. | Pyrrolidine and piperidine modulators of chemokine receptor activity |
AU9281298A (en) | 1997-10-01 | 1999-04-23 | Kyowa Hakko Kogyo Co. Ltd. | Benzodioxole derivatives |
US6541669B1 (en) | 1998-06-08 | 2003-04-01 | Theravance, Inc. | β2-adrenergic receptor agonists |
CA2335094C (en) | 1998-06-30 | 2008-12-23 | The Dow Chemical Company | Polymer polyols and a process for the production thereof |
GB9913083D0 (en) | 1999-06-04 | 1999-08-04 | Novartis Ag | Organic compounds |
ES2246233T3 (es) | 1999-05-04 | 2006-02-16 | Schering Corporation | Derivados de piperidina utiles como antagonistas de ccr5. |
ES2244437T3 (es) | 1999-05-04 | 2005-12-16 | Schering Corporation | Derivados de piperazina utiles como antagonistas de ccr5. |
US6683115B2 (en) | 1999-06-02 | 2004-01-27 | Theravance, Inc. | β2-adrenergic receptor agonists |
ES2165768B1 (es) | 1999-07-14 | 2003-04-01 | Almirall Prodesfarma Sa | Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen. |
PL200923B1 (pl) | 1999-08-21 | 2009-02-27 | Nycomed Gmbh | Lek zawierający inhibitor PDE w połączeniu z agonistą receptoraß₂ -adrenergicznego oraz zastosowanie połączenia roflumilastu i salmeterolu |
OA11558A (en) | 1999-12-08 | 2004-06-03 | Advanced Medicine Inc | Beta 2-adrenergic receptor agonists. |
AU5629301A (en) | 2000-04-27 | 2001-11-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Novel, slow-acting betamimetics, a method for their production and their use as medicaments |
US6916828B2 (en) | 2000-06-27 | 2005-07-12 | Laboratorios S.A.L.V.A.T., S.A. | Carbamates derivatived from arylakylamines |
GB0015876D0 (en) | 2000-06-28 | 2000-08-23 | Novartis Ag | Organic compounds |
DE10038639A1 (de) | 2000-07-28 | 2002-02-21 | Schering Ag | Nichtsteroidale Entzündungshemmer |
AU2001275760B2 (en) | 2000-08-05 | 2005-03-17 | Glaxo Group Limited | 6.alpha., 9.alpha.-difluoro-17.alpha.-'(2-furanylcarboxyl) oxy!-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4,-diene-17-carbothioic acid S-fluoromethyl ester as an anti-inflammatory agent |
DE10056400A1 (de) | 2000-11-14 | 2002-05-23 | Merck Patent Gmbh | Galenische Formulierung |
GB0028383D0 (en) | 2000-11-21 | 2001-01-03 | Novartis Ag | Organic compounds |
PL362989A1 (en) | 2000-12-22 | 2004-11-15 | Almirall Prodesfarma Ag | Quinuclidine carbamate derivatives and their use as m3 antagonists |
SK287414B6 (sk) | 2000-12-28 | 2010-09-07 | Laboratorios Almirall, S.A. | Chinuklidínové deriváty a kompozície s ich obsahom |
GB0103630D0 (en) | 2001-02-14 | 2001-03-28 | Glaxo Group Ltd | Chemical compounds |
EP1366025B1 (en) | 2001-03-08 | 2007-06-27 | Glaxo Group Limited | Agonists of beta-adrenoreceptors |
ATE381537T1 (de) | 2001-03-22 | 2008-01-15 | Glaxo Group Ltd | Formanilid-derivative als beta2-adrenorezeptor- agonisten |
HUP0400070A2 (hu) | 2001-04-30 | 2004-04-28 | Glaxo Group Limited | 17alfa-helyzetben ciklusos észtercsoportot tartalmazó androsztán-17béta-karbotiosav-észter-származékok mint gyulladásgátló szerek, eljárás a vegyületek előállítására és ezeket tartalmazó gyógyszerkészítmények |
JP2005500290A (ja) | 2001-06-12 | 2005-01-06 | グラクソ グループ リミテッド | 抗炎症性の、17β−カルボチオアートアンドロスタン誘導体である17α複素環エステル |
EP2327767B1 (en) | 2001-06-21 | 2015-04-29 | BASF Enzymes LLC | Nitrilases |
ATE417606T1 (de) | 2001-09-14 | 2009-01-15 | Glaxo Group Ltd | Phenethanolamin-derivate zur behandlung von erkrankungen der atemwege |
CZ2004501A3 (cs) | 2001-10-17 | 2004-09-15 | Ucb, S.A. | Chinuklidinové deriváty, způsoby jejich přípravy a jejich použití jako M2 a/nebo M3 inhibitoru muskarinového receptoru |
GB0125259D0 (en) | 2001-10-20 | 2001-12-12 | Glaxo Group Ltd | Novel compounds |
MY130622A (en) | 2001-11-05 | 2007-07-31 | Novartis Ag | Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (pde4) inhibitors |
TWI249515B (en) | 2001-11-13 | 2006-02-21 | Theravance Inc | Aryl aniline beta2 adrenergic receptor agonists |
WO2003042160A1 (en) | 2001-11-13 | 2003-05-22 | Theravance, Inc. | Aryl aniline beta-2 adrenergic receptor agonists |
WO2003048181A1 (en) | 2001-12-01 | 2003-06-12 | Glaxo Group Limited | 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents |
HUP0500107A3 (en) | 2001-12-20 | 2011-05-30 | Chiesi Farma Spa | 1-alkyl-1-azoniabicyclo[2.2.2.]octane carbamate derivatives, pharmaceutical compositions comprising thereof and their use as muscarinic receptor antagonists |
WO2003072592A1 (en) | 2002-01-15 | 2003-09-04 | Glaxo Group Limited | 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents |
AU2003201693A1 (en) | 2002-01-21 | 2003-09-02 | Glaxo Group Limited | Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents |
GB0202216D0 (en) | 2002-01-31 | 2002-03-20 | Glaxo Group Ltd | Novel compounds |
US6858615B2 (en) * | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenyl guanidine sodium channel blockers |
GB0204719D0 (en) | 2002-02-28 | 2002-04-17 | Glaxo Group Ltd | Medicinal compounds |
EP1490317A1 (en) | 2002-03-26 | 2004-12-29 | Boehringer Ingelheim Pharmaceuticals Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
EA008830B1 (ru) | 2002-03-26 | 2007-08-31 | Бёрингер Ингельхайм Фармасьютиклз, Инк. | Миметики глюкокортикоидов, способы их получения, фармацевтические композиции и их применение |
US7282591B2 (en) | 2002-04-11 | 2007-10-16 | Merck & Co., Inc. | 1h-benzo{f}indazol-5-yl derivatives as selective glucocorticoid receptor modulators |
ES2206021B1 (es) | 2002-04-16 | 2005-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de pirrolidinio. |
JP2005523920A (ja) | 2002-04-25 | 2005-08-11 | グラクソ グループ リミテッド | フェネタノールアミン誘導体 |
JP2005527618A (ja) | 2002-05-28 | 2005-09-15 | セラヴァンス インコーポレーテッド | アルコキシアリールβ2アドレナリン作動性レセプターアゴニスト |
ES2201907B1 (es) | 2002-05-29 | 2005-06-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos. |
US7186864B2 (en) | 2002-05-29 | 2007-03-06 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
DE10224888A1 (de) | 2002-06-05 | 2003-12-24 | Merck Patent Gmbh | Pyridazinderivate |
US7074806B2 (en) | 2002-06-06 | 2006-07-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
DE10225574A1 (de) | 2002-06-10 | 2003-12-18 | Merck Patent Gmbh | Aryloxime |
DE10227269A1 (de) | 2002-06-19 | 2004-01-08 | Merck Patent Gmbh | Thiazolderivate |
EP1517895B1 (en) | 2002-06-25 | 2007-03-14 | Merck Frosst Canada Ltd. | 8-(biaryl) quinoline pde4 inhibitors |
AU2003281219A1 (en) | 2002-07-02 | 2004-01-23 | Bernard Cote | Di-aryl-substituted-ethane pyridone pde4 inhibitors |
ES2204295B1 (es) | 2002-07-02 | 2005-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de quinuclidina-amida. |
ES2518940T3 (es) | 2002-07-08 | 2014-11-06 | Pfizer Products Inc. | Moduladores del receptor de glucocorticoides |
GB0217225D0 (en) | 2002-07-25 | 2002-09-04 | Glaxo Group Ltd | Medicinal compounds |
PE20050130A1 (es) | 2002-08-09 | 2005-03-29 | Novartis Ag | Compuestos organicos |
EP1556049A1 (en) | 2002-08-10 | 2005-07-27 | ALTANA Pharma AG | Piperidine-pyridazones and phthalazones as pde4 inhibitors |
PL373146A1 (en) | 2002-08-10 | 2005-08-22 | Altana Pharma Ag | Pyridazinone-derivatives as pde4 inhibitors |
WO2004018449A1 (en) | 2002-08-10 | 2004-03-04 | Altana Pharma Ag | Piperidine-derivatives as pde4 inhibitors |
PL373597A1 (en) | 2002-08-10 | 2005-09-05 | Altana Pharma Ag | Piperidine-n-oxide-derivatives |
CA2495603A1 (en) | 2002-08-17 | 2004-03-04 | Altana Pharma Ag | Benzonaphthyridines with pde 3/4 inhibiting activity |
RS20050116A (en) | 2002-08-17 | 2007-11-15 | Altana Pharma Ag., | Novel phenanthridines |
SE0202483D0 (sv) | 2002-08-21 | 2002-08-21 | Astrazeneca Ab | Chemical compounds |
CA2496175A1 (en) | 2002-08-21 | 2004-03-04 | Boehringer Ingelheim Pharmaceuticals, Inc. | Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
DE60231341D1 (de) | 2002-08-23 | 2009-04-09 | Ranbaxy Lab Ltd | Fluor- und sulfonylaminohaltige, 3,6-disubstituierptorantagonisten |
JP4587295B2 (ja) | 2002-08-29 | 2010-11-24 | ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング | Pde4インヒビターとしての3−ヒドロキシ−6−フェニルフェナントリジン |
DE60333371D1 (de) | 2002-08-29 | 2010-08-26 | Boehringer Ingelheim Pharma | 3-(sulfonamidoethyl)-indol-derivate zur verwendung als glucocorticoid-mimetika bei der behandlung von entzündlichen, allergischen und proliferativen erkrankungen |
CA2495827C (en) | 2002-08-29 | 2012-05-08 | Altana Pharma Ag | 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors |
GB0220730D0 (en) | 2002-09-06 | 2002-10-16 | Glaxo Group Ltd | Medicinal compounds |
JP2006096662A (ja) | 2002-09-18 | 2006-04-13 | Sumitomo Pharmaceut Co Ltd | 新規6−置換ウラシル誘導体及びアレルギー性疾患の治療剤 |
CA2497903A1 (en) | 2002-09-18 | 2004-04-01 | Ono Pharmaceutical Co., Ltd. | Triazaspiro[5.5]undecane derivatives and drugs comprising the same as the active ingredient |
JP4520309B2 (ja) | 2002-09-20 | 2010-08-04 | メルク・シャープ・エンド・ドーム・コーポレイション | 選択的糖質コルチコイド受容体調節剤としてのオクタヒドロ−2−H−ナフト[1,2−f]インドール−4−カルボキサミド誘導体 |
JP2004107299A (ja) | 2002-09-20 | 2004-04-08 | Japan Energy Corp | 新規1−置換ウラシル誘導体及びアレルギー性疾患の治療剤 |
DE10246374A1 (de) | 2002-10-04 | 2004-04-15 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
EP1440966A1 (en) | 2003-01-10 | 2004-07-28 | Pfizer Limited | Indole derivatives useful for the treatment of diseases |
AU2003269316A1 (en) | 2002-10-11 | 2004-05-04 | Pfizer Inc. | Indole derivatives as beta-2 agonists |
AU2003298094A1 (en) | 2002-10-22 | 2004-05-13 | Glaxo Group Limited | Medicinal arylethanolamine compounds |
AP2021A (en) | 2002-10-23 | 2009-08-03 | Glenmark Pharmaceuticals Ltd | Novel tricyclic compounds useful for the treatmentof inflammatory and allergic disorders: Process f or their preparation and pharmaceutical compositions containing them |
AR041724A1 (es) | 2002-10-28 | 2005-05-26 | Glaxo Group Ltd | Compuestos derivados de fenetanolamina y su utilizacion en composiciones farmaceuticas |
GB0225030D0 (en) | 2002-10-28 | 2002-12-04 | Glaxo Group Ltd | Medicinal compounds |
GB0225287D0 (en) | 2002-10-30 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
GB0225535D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
GB0225540D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
DE10253426B4 (de) | 2002-11-15 | 2005-09-22 | Elbion Ag | Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung |
DE10253220A1 (de) | 2002-11-15 | 2004-05-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
DE10253282A1 (de) | 2002-11-15 | 2004-05-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung |
DE10261874A1 (de) | 2002-12-20 | 2004-07-08 | Schering Ag | Nichtsteroidale Entzündungshemmer |
JP4606408B2 (ja) | 2003-01-21 | 2011-01-05 | メルク・シャープ・エンド・ドーム・コーポレイション | 選択的グルココルチコイド受容体調節物質としての17−カルバモイルオキシコルチゾル誘導体 |
PE20040950A1 (es) | 2003-02-14 | 2005-01-01 | Theravance Inc | DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS |
WO2004080972A1 (en) | 2003-03-12 | 2004-09-23 | Vertex Pharmaceuticals Incorporated | Pirazole modulators of atp-binding cassette transporters |
EP1460064A1 (en) | 2003-03-14 | 2004-09-22 | Pfizer Limited | Indole-2-carboxamide derivatives useful as beta-2 agonists |
US7696244B2 (en) | 2003-05-16 | 2010-04-13 | The Regents Of The University Of California | Compounds having activity in increasing ion transport by mutant-CFTR and uses thereof |
GB0312832D0 (en) | 2003-06-04 | 2003-07-09 | Pfizer Ltd | 2-amino-pyridine derivatives useful for the treatment of diseases |
WO2004111014A1 (en) | 2003-06-06 | 2004-12-23 | Vertex Pharmaceuticals Incorporated | Pyrimidine derivatives as modulators of atp-binding cassette transporters |
EP1636269A2 (en) | 2003-06-10 | 2006-03-22 | Ace Biosciences A/S | Extracellular aspergillus polypeptides |
ZA200602755B (en) | 2003-09-06 | 2007-06-27 | Vertex Pharma | Modulators of ATP-binding cassette transporters |
EP1664002A1 (en) | 2003-09-17 | 2006-06-07 | Novartis AG | Organic compounds |
AU2004279855A1 (en) | 2003-10-08 | 2005-04-21 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters containing cycloalkyl or pyranyl groups |
US7541466B2 (en) | 2003-12-23 | 2009-06-02 | Genzyme Corporation | Tetrahydroisoquinoline derivatives for treating protein trafficking diseases |
CA2554796A1 (en) | 2004-01-30 | 2005-08-18 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
WO2005120497A2 (en) | 2004-06-04 | 2005-12-22 | The Regents Of The University Of California | Compounds having activity in increasing ion transport by mutant-cftr and uses thereof |
US20060199828A1 (en) | 2005-03-04 | 2006-09-07 | Georg Jaeschke | Pyrazine-2-carboxyamide derivatives |
JP5385605B2 (ja) | 2005-03-11 | 2014-01-08 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atp結合カセットトランスポーターのモジュレーター |
WO2006101740A2 (en) | 2005-03-18 | 2006-09-28 | The Regents Of The University Of California | Compounds having activity in correcting mutant-cftr processing and uses thereof |
US8822451B2 (en) | 2005-05-24 | 2014-09-02 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
CA2618057A1 (en) | 2005-08-11 | 2007-02-22 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
NL2000284C2 (nl) | 2005-11-04 | 2007-09-28 | Pfizer Ltd | Pyrazine-derivaten. |
GB0526244D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
GB0526240D0 (en) * | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
CL2006003737A1 (es) | 2005-12-29 | 2008-02-08 | Janssen Pharmaceutica Nv | Uso de compuestos derivados de triazina o pirimidina sustituida, para tratar o prevenir enfermedades mediadas por los receptores de prokineticina 2 tales como trastornos gastrointestinales. |
SI2121636T1 (sl) | 2006-12-14 | 2017-06-30 | Janssen Pharmaceutica N.V. | Postopek za pripravo derivatov piperazinila in diazepanil benzamida |
US8450348B2 (en) | 2007-02-21 | 2013-05-28 | Forma Tm, Llc | Derivatives of squaric acid with anti-proliferative activity |
ES2436658T3 (es) | 2007-12-10 | 2014-01-03 | Synthon B.V. | Síntesis de paliperidona |
EA017919B1 (ru) | 2007-12-10 | 2013-04-30 | Новартис Аг | Производные пиразин-2-карбоксамида для лечения заболеваний, которые поддаются лечению путем блокирования эпителиальных натриевых каналов |
US20110172217A1 (en) | 2008-09-05 | 2011-07-14 | Shionogi & Co., Ltd. | Ring-fused morpholine derivative having pi3k-inhibiting activity |
US9556201B2 (en) | 2009-10-29 | 2017-01-31 | Glaxosmithkline Llc | Bicyclic pyridines and analogs as sirtuin modulators |
AU2014338549B2 (en) | 2013-10-25 | 2017-05-25 | Novartis Ag | Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors |
-
2008
- 2008-12-09 EA EA201000886A patent/EA017919B1/ru not_active IP Right Cessation
- 2008-12-09 CN CN200880126433.4A patent/CN101939054B/zh active Active
- 2008-12-09 BR BRPI0820669-4A patent/BRPI0820669A2/pt not_active IP Right Cessation
- 2008-12-09 CA CA2707857A patent/CA2707857C/en not_active Expired - Fee Related
- 2008-12-09 ES ES11184004.7T patent/ES2654395T3/es active Active
- 2008-12-09 PE PE2008002031A patent/PE20091096A1/es not_active Application Discontinuation
- 2008-12-09 EP EP20120173703 patent/EP2520574A1/en not_active Withdrawn
- 2008-12-09 NZ NZ585789A patent/NZ585789A/en not_active IP Right Cessation
- 2008-12-09 MY MYPI20102511 patent/MY152955A/en unknown
- 2008-12-09 ES ES08860731.2T patent/ES2602331T3/es active Active
- 2008-12-09 UA UAA201007106A patent/UA104997C2/uk unknown
- 2008-12-09 JP JP2010537419A patent/JP5455922B2/ja active Active
- 2008-12-09 AU AU2008334629A patent/AU2008334629B2/en not_active Ceased
- 2008-12-09 EP EP11184004.7A patent/EP2444120B1/en active Active
- 2008-12-09 PT PT111840047T patent/PT2444120T/pt unknown
- 2008-12-09 EP EP08860731.2A patent/EP2231280B1/en active Active
- 2008-12-09 AR ARP080105334 patent/AR069637A1/es unknown
- 2008-12-09 KR KR1020107015184A patent/KR101578235B1/ko not_active IP Right Cessation
- 2008-12-09 TW TW97147843A patent/TWI439462B/zh not_active IP Right Cessation
- 2008-12-09 CL CL2008003651A patent/CL2008003651A1/es unknown
- 2008-12-09 WO PCT/EP2008/067110 patent/WO2009074575A2/en active Application Filing
- 2008-12-09 MX MX2010006421A patent/MX2010006421A/es active IP Right Grant
- 2008-12-09 PL PL11184004T patent/PL2444120T3/pl unknown
- 2008-12-10 US US12/332,086 patent/US8039472B2/en active Active
-
2010
- 2010-05-28 ZA ZA2010/03837A patent/ZA201003837B/en unknown
- 2010-05-31 MA MA32874A patent/MA31894B1/fr unknown
- 2010-06-01 CR CR11470A patent/CR11470A/es unknown
- 2010-06-03 IL IL206165A patent/IL206165A0/en unknown
- 2010-06-04 TN TN2010000256A patent/TN2010000256A1/fr unknown
- 2010-06-10 EC ECSP10010242 patent/ECSP10010242A/es unknown
- 2010-06-10 CO CO10070372A patent/CO6310968A2/es active IP Right Grant
- 2010-06-10 HN HN2010001165A patent/HN2010001165A/es unknown
- 2010-06-10 CU CU20100118A patent/CU23967B1/es not_active IP Right Cessation
-
2011
- 2011-06-10 US US13/157,893 patent/US20110237572A1/en not_active Abandoned
-
2012
- 2012-09-13 US US13/613,495 patent/US8697687B2/en active Active
-
2014
- 2014-02-21 US US14/186,904 patent/US9139586B2/en active Active
-
2015
- 2015-09-08 US US14/847,262 patent/US9643983B2/en active Active
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR069637A1 (es) | Derivados de pirazinas | |
AR047585A1 (es) | Derivados de bisarilurea | |
PE20090276A1 (es) | Compuestos derivados de imidazoquinolina como moduladores de tlr7 | |
AR035548A1 (es) | Compuestos organicos | |
TW200643015A (en) | 2-(4-oxo-4H-quinazolin-3-yl)acetamide derivatives | |
BRPI0707491B8 (pt) | compostos úteis como agentes moduladores de receptores de mineralocorticóides, os referidos agentes compreendendo os mesmos e composições farmacêuticas | |
AR066120A1 (es) | Derivados de pirimidinona y sus metodos de uso | |
HRP20080113T3 (en) | Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto | |
AR052903A1 (es) | Compuestos de bis arilo y heteroarilo sustituidos como antagonistas selectivos de 5ht2a, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de trastornos del sueno. | |
AR059328A1 (es) | Derivados de antranilamida-2-amino-heteroareno-carboxamida, un proceso para su obtencion, composiciones farmaceuticas que los contienen y el uso de estos compuestos para la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por cetp | |
HRP20070510T3 (en) | Benzimidazole derivative and its use as a ii receptor antagonist | |
AR060658A1 (es) | Derivados de diceto-piperazina y piperidina como agentes antivirales | |
NO20075312L (no) | N-(N-sulfonylaminometyl)cyklopropankarboksamidderivater nyttige ved smertebehandling | |
RS52999B (en) | BIS (AMIDIDA TIO-HYDRAZIDE) Salts for Cancer Treatment | |
AR051469A1 (es) | Derivados de indol tetraciclicos como agentes antiviricos | |
NO20074763L (no) | (1,5-difenyl-1H-pyrazol-3-yl)oksadiazolderivater, fremgangsmate ved fremstilling derav og anvendelse av samme i terapi | |
AR037907A1 (es) | Derivados de azaindolilalquilamina como ligandos de 5-hidroxitriptamina-6 | |
PE20070212A1 (es) | Heterociclos de 1,4-dihidropiridina-condensados, procesos para preparar los mismos, uso y composiciones que los contienen | |
SI2310396T1 (en) | Macrocyclic derivatives of indole are useful as inhibitors of hepatitis C virus | |
NO20075617L (no) | 4-fenyl-5-okso-1,4,5,6,7,8-heksahydrokinolinderivater for behandling av infertilitet | |
ATE396183T1 (de) | Chromanderivate und ihre verwendung als liganden des 5-ht-rezeptors | |
HRP20080119T3 (en) | Benzothiadiazine derivatives, method for preparing same and pharmaceutical compositions containing same | |
CO6241117A2 (es) | Derivados de n-(fenil) -n-morfolin-4-il-piridin -2-il) - -pirimidina-2, 4-diamina como inhibidores del ephb4 quinasa para el tratamiento de condiciones proliferativas | |
AR053326A1 (es) | 4 - feniltetrahidroisoquinolinas sustituidas, su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la activacion de nhe y composicion farmaceutica que las comprende. | |
PE20081116A1 (es) | Derivados de diaril, dipiridinil y arilpiridinil como antagonistas del receptor opioide |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |