AR077033A1 - Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicas - Google Patents
Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicasInfo
- Publication number
- AR077033A1 AR077033A1 ARP100102023A ARP100102023A AR077033A1 AR 077033 A1 AR077033 A1 AR 077033A1 AR P100102023 A ARP100102023 A AR P100102023A AR P100102023 A ARP100102023 A AR P100102023A AR 077033 A1 AR077033 A1 AR 077033A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- optionally substituted
- link
- independently
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- 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
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
Una composicion farmacéutica que incluye un compuesto de la formula 1 y métodos para el uso del mismo. Reivindicacion 1: Un compuesto de la formula (1): los estereoisomeros o las sales farmacéuticamente aceptables del mismo, en la que: A es CR3 o N; B y D son con independencia CR15 o N, dichos B y D no pueden ser N al mismo tiempo; R1 es con independencia H, halogeno, alquilo C1-3, cicloalquilo C3-4, -CF3, -OR6, -SR6, -OCF3, -CN, -NO2, -NR6SO2R7, -NR6C(O)R7 o -NR6R7, en la que dos R1 no pueden ser H al mismo tiempo y dichos alquilo y cicloalquilo están opcionalmente sustituidos por halogeno, OR6, -NR6R7 o fenilo; R2 y R3 son con independencia H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halogeno, -(alquilo C0-3)CN, -(alquilo C0-3)OR8, -(alquilo C0-3)SR8, -(alquilo C0-3)NR8R9, -(alquilo C0-3)CF3, -O(alquilo C0-3)CF3, -(alquilo C0-3)NO2, -(alquilo C0-3)C(O)R8, -(alquilo C0-3)C(O)OR8, -(alquilo C0-3)C(O)NR8R9, -(alquilo C0-3)NR8C(O)R9, -(alquilo C0-3)S(O)1-2R8, -(alquilo C0-3)NR8S-(O)1-2R9, -(alquilo C0-3)S-(O)1-2NR8R9, -(alquilo C0-3)(cicloalquilo C3-6), -(alquilo C0-3) (heterociclilo de 3-6 eslabones), -(alquilo C0-3)-(heteroarilo de 5-6 eslabones) o -(alquilo C0-3)fenilo, en la que y R3 están opcionalmente sustituidos con independencia por R10; R4 es H, -NH2, -NH-, -OH, -SH, -NR6C(O)-, -NR6C(O)O-, -NR6C(O)NR7-, -NR6S(O)1-2- o -NR6S(O)1-2NR7-. R5 está ausente, es alquilo C1-6, cicloalquilo C3-6, fenilo, heterociclilo de 3-7 eslabones o heteroarilo de 5-6 eslabones, dicho R5 está opcionalmente sustituido por R10; R6 y R7 son en cada caso con independencia H o alquilo C1-3, opcionalmente sustituido por halogeno, oxo o -NR11R12; o R6 y R7 junto con el átomo al que están unidos forman con independencia un heterociclilo de 3-6 eslabones, opcionalmente sustituido por halogeno, oxo, -NR11R12 o alquilo C1-3; R8 y R9 son en cada caso con independencia H, alquilo C1-3, cicloalquilo C3-6, fenilo, heterociclilo de 3-6 eslabones o heteroarilo de 5-6 eslabones, opcionalmente sustituido por R10; o R8 y R9 junto con el átomo al que están unidos forman con independencia un heterociclilo de 3-6 eslabones, opcionalmente sustituido por halogeno, oxo, -NR11R12 o alquilo C1-3; R10 es con independencia H, oxo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halogeno, -(alquilo C0-3)CN, -(alquilo C0-3)OR11, -(alquilo C0-3)SR11, -(alquilo C0-3)NR11R12, -(alquilo C0-3)CF3, -(alquilo C0-3)NO2, -(alquilo C0-3)C(O)R11, -(alquilo C0-3)C(O)ORH, -(alquilo C0-3)-C(O)NR11R12, -(alquilo C0-3)NR11C(O)R12, -(alquilo C0-3)-S(O)1-2R11, -(alquilo C0-3)NR11S(O)1-2R12, -(alquilo C0-3)-S(O)1-2NR11R12, -(alquilo C0-3) (ciclo-alquilo C3-6) , -(alquilo C0-3)(heterociclilo de 3-6 eslabones), -(alquilo C0-3)C(O)-(heterociclilo de 3-6 eslabones), -(alquilo C0-3) (heteroarilo de 5-6 eslabones) o -(alquilo C0-3)fenilo, dicho R10 está opcionalmente sustituido con independencia por halogeno, alquilo C1-3, oxo, -CF3, -(alquilo C0-3)OR13, -(alquilo C0-3)NR13R14, -(alquilo C0-3)C(O)R13 o -(alquilo C0-3)S(O)1-2R13; R11 y R12 son con independencia H, alquilo C1-6, -(alquilo C0-3) (cicloalquilo C3-6) , -(alquilo C0-3) -(heterociclilo de 3-6 eslabones), -(alquilo C0-3) (heteroarilo de 5-6 eslabones) o -(alquilo C0-3)fenilo, opcionalmente sustituido por halogeno, oxo, -OR13, -SR13, -NR13R14, alquilo C1-3, -(alquilo C0-3) (cicloalquilo C3-6), -(alquilo C0-3)-fenilo, -(alquilo C0-3) (heterociclilo de 3-6 eslabones) o -(alquilo C0-3)(heteroarilo de 5-6 eslabones); o R11 y R12 junto con el átomo al que están unidos forman un heterociclilo de 3-6 eslabones, opcionalmente sustituido por halogeno, oxo, -NR13R14 o alquilo C1-3; R13 y R14 son con independencia H, alquilo C1-6, OH u OCH3, opcionalmente sustituido por halogeno, -NH2, -N(CH3)2, fenilo u oxo, dicho fenilo está opcionalmente sustituido por halogeno, alquilo C1-6, CF3, -NRaRb u ORa; o R13 y R14 junto al átomo al que están unidos forman un heterociclilo de 3-6 eslabones, opcionalmente sustituido por halogeno, oxo, -NH2, -N(CH3)2 o alquilo C1-3; R15 es con independencia H, halogeno, alquilo C1-3, alquenilo C1-3, alquinilo C1-3, cicloalquilo C3-4, -CF3, -ORa, -SRa, -CN, -NO2, -NRaSO2Rb, -NRaC(O)Rb o -NRaRb; Ra y Rb son con independencia H o alquilo C1-6 opcionalmente sustituido por halogeno u oxo; o Ra y Rb junto al átomo al que están unidos forman un heterociclilo de 3-6 eslabones, opcionalmente sustituido por halogeno, oxo o alquilo C1-3; con las condiciones siguientes: si R4 es -OH, R5 está ausente, y uno de B y D es N y el otro es CH, entonces la porcion de la formula 1 que tiene la estructura: (2), es diferente de (3) si la porcion de la formula 1 que tiene la estructura: (4) es (5), entonces la porcion de la formula 1 que tiene la estructura: (2) es diferente de las siguientes: (6); si la porcion de la formula 1 que tiene la estructura: (4) es (7), entonces la porcion de la formula 1 que tiene la estructura: (2) es diferente de las siguientes: (8), si A es CR3, B y D son CH, o B es CH y D es N, un R1 es -CH3 y el otro R1 es H, R2 es H, R4 es H o Cl; R5 está ausente; R3 es diferente de la estructura: (9); si A es CR3, B y D son CH, un R1 es F y el otro R1 es H, R2 es H, R4 es H o Cl; R5 está ausente; R3 es diferente de 3-cloro-piridin-2-ilo; si A es CR3, B es N; D es CH, un R1 es -CH3 y el otro R1 es H; R2 y son H; R5 está ausente; R4 es diferente de OH; y si A es CR3, B es CH, D es N, R1 es Cl, R2 y R3 son H, R4 es -NH-, R5 es diferente de la estructura: (10), en las que la línea ondulada representa el punto de union a la formula 1.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US18632209P | 2009-06-11 | 2009-06-11 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR077033A1 true AR077033A1 (es) | 2011-07-27 |
Family
ID=42313557
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100102023A AR077033A1 (es) | 2009-06-11 | 2010-06-09 | Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicas |
Country Status (14)
Country | Link |
---|---|
US (1) | US8486950B2 (es) |
EP (1) | EP2440529A1 (es) |
JP (1) | JP5763057B2 (es) |
KR (1) | KR101530117B1 (es) |
CN (1) | CN102459187B (es) |
AR (1) | AR077033A1 (es) |
AU (1) | AU2010258597B2 (es) |
BR (1) | BRPI1011129A2 (es) |
CA (1) | CA2764728A1 (es) |
IL (1) | IL216511A0 (es) |
MX (1) | MX2011012840A (es) |
SG (1) | SG176781A1 (es) |
TW (1) | TW201103904A (es) |
WO (1) | WO2010142752A1 (es) |
Families Citing this family (55)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2013505262A (ja) * | 2009-09-17 | 2013-02-14 | バンダービルト ユニバーシティー | mGluR5ネガティブアロステリックモジュレータとしての置換ヘテロアリールアミンカルボキサミド類似体、ならびに、その形成方法および使用方法 |
US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
EP3075730B1 (en) | 2010-06-04 | 2018-10-24 | Genentech, Inc. | Aminopyrimidine derivatives as lrrk2 modulators |
AU2011328139A1 (en) | 2010-11-10 | 2013-04-04 | F. Hoffmann-La Roche Ag | Pyrazole aminopyrimidine derivatives as LRRK2 modulators |
WO2012160464A1 (en) | 2011-05-26 | 2012-11-29 | Daiichi Sankyo Company, Limited | Heterocyclic compounds as protein kinase inhibitors |
WO2013018695A1 (ja) | 2011-07-29 | 2013-02-07 | 武田薬品工業株式会社 | 複素環化合物 |
JP6043290B2 (ja) | 2011-09-22 | 2016-12-14 | 武田薬品工業株式会社 | 縮合複素環化合物 |
EP2818473A4 (en) | 2012-02-20 | 2015-04-15 | Takeda Pharmaceutical | HETEROCYCLIC COMPOUND |
JPWO2013146963A1 (ja) | 2012-03-28 | 2015-12-14 | 武田薬品工業株式会社 | 複素環化合物 |
JP6267193B2 (ja) * | 2012-05-22 | 2018-01-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 置換ジピリジルアミン類及びそれらの使用 |
CN104507940B (zh) | 2012-06-01 | 2017-01-25 | 武田药品工业株式会社 | 杂环化合物 |
EP2914592B1 (en) * | 2012-11-03 | 2017-10-11 | Boehringer Ingelheim International GmbH | Inhibitors of cytomegalovirus |
NZ710270A (en) | 2013-01-31 | 2020-09-25 | Vertex Pharma | Pyridone amides as modulators of sodium channels |
TW201444798A (zh) * | 2013-02-28 | 2014-12-01 | 必治妥美雅史谷比公司 | 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物 |
CN105102448B (zh) | 2013-02-28 | 2018-03-06 | 百时美施贵宝公司 | 作为rock1和rock2抑制剂的苯基吡唑衍生物 |
EP2975031A4 (en) | 2013-03-14 | 2017-04-19 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
EA201591881A1 (ru) | 2013-03-28 | 2016-04-29 | Такеда Фармасьютикал Компани Лимитед | Гетероциклическое соединение |
WO2014177524A1 (en) * | 2013-05-01 | 2014-11-06 | F. Hoffmann-La Roche Ag | C-linked heterocycloalkyl substituted pyrimidines and their uses |
JP6411342B2 (ja) | 2013-07-03 | 2018-10-24 | 武田薬品工業株式会社 | アミド化合物 |
US10053468B2 (en) | 2013-07-03 | 2018-08-21 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
JPWO2015016206A1 (ja) | 2013-07-30 | 2017-03-02 | 武田薬品工業株式会社 | 複素環化合物 |
US20160168132A1 (en) * | 2013-07-31 | 2016-06-16 | Minoryx Therapeutics S.L. | Di(hetero)arylamides and sulfonamides, methods for their preparation and therapeutic uses thereof |
CA2925935A1 (en) | 2013-10-03 | 2015-04-09 | Millennium Pharmaceuticals, Inc. | Method for the prophylaxis or treatment of systemic lupus erythematosus and/or lupus nephritis |
TWI582077B (zh) * | 2013-11-07 | 2017-05-11 | 必治妥美雅史谷比公司 | 作爲IL-12、IL-23及/或IFNα反應調節劑之經烷基-醯胺取代之吡啶化合物 |
WO2015068856A1 (en) | 2013-11-08 | 2015-05-14 | Takeda Pharmaceutical Company Limited | Pyrazole for the treatment autoimmune disorders |
AU2014353150A1 (en) | 2013-11-19 | 2016-07-07 | Vanderbilt University | Substituted imidazopyridine and triazolopyridine compounds as negative allosteric modulators of mGluR5 |
TWI651329B (zh) | 2013-12-13 | 2019-02-21 | 美商維泰克斯製藥公司 | 作為鈉通道調節劑之吡啶酮醯胺之前藥 |
US9533982B2 (en) | 2014-03-20 | 2017-01-03 | Vanderbilt University | Substituted bicyclic heteroaryl carboxamide analogs as mGluR5 negative allosteric modulators |
CN104926801B (zh) * | 2014-03-22 | 2019-06-04 | 浙江大学 | 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用 |
US10179790B2 (en) * | 2014-06-04 | 2019-01-15 | Thomas Helledays Stiftelse For Medicinsk Forskning | MTH1 inhibitors for treatment of cancer |
WO2016028971A1 (en) * | 2014-08-21 | 2016-02-25 | Bristol-Myers Squibb Company | Tied-back benzamide derivatives as potent rock inhibitors |
EP3967312A1 (en) | 2014-09-12 | 2022-03-16 | UNION therapeutics A/S | Antibacterial use of halogenated salicylanilides |
US9550778B2 (en) | 2014-10-03 | 2017-01-24 | Vanderbilt University | Substituted 6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analogs as negative allosteric modulators of mGluR5 |
GB201509326D0 (en) | 2015-05-29 | 2015-07-15 | Antibio Tx Aps | Novel use |
WO2016199943A1 (en) | 2015-06-11 | 2016-12-15 | Takeda Pharmaceutical Company Limited | Heterocyclic compounds |
CN108026088B (zh) | 2015-07-17 | 2021-02-12 | 武田药品工业株式会社 | 用作hdac抑制剂的噁二唑衍生物 |
JP6689297B2 (ja) | 2015-07-23 | 2020-04-28 | 武田薬品工業株式会社 | 複素環化合物 |
WO2018030550A1 (en) | 2016-08-09 | 2018-02-15 | Takeda Pharmaceutical Company Limited | Heterocyclic compounds with an ror(gamma)t modulating activity |
CN110520412A (zh) | 2017-02-15 | 2019-11-29 | 南洋理工大学 | 用于治疗结核病的化合物 |
WO2018213426A1 (en) | 2017-05-16 | 2018-11-22 | Vertex Pharmaceuticals Incorporated | Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels |
JP2021512935A (ja) | 2018-02-12 | 2021-05-20 | 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Vertex Pharmaceuticals Incorporated | 疼痛を処置する方法 |
WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
EP3885347B1 (en) | 2018-11-14 | 2023-11-22 | UBE Corporation | Dihydropyrrolopyrazole derivative |
WO2020117877A1 (en) * | 2018-12-04 | 2020-06-11 | Aquinnah Pharmaceuticals, Inc. | Compounds, compositions and methods of use |
JP7407196B2 (ja) * | 2018-12-20 | 2023-12-28 | アムジエン・インコーポレーテツド | Kif18a阻害剤 |
US11419834B2 (en) | 2019-02-25 | 2022-08-23 | Rhode Island Hospital | Methods for treating diseases or infections caused by or associated with H. pylori using a halogenated salicylanilide |
WO2020188015A1 (en) | 2019-03-21 | 2020-09-24 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
WO2021018165A1 (zh) * | 2019-07-30 | 2021-02-04 | 江苏恒瑞医药股份有限公司 | 吡啶苯甲酰胺类衍生物、其制备方法及其在医药上的应用 |
AU2020378630A1 (en) | 2019-11-08 | 2022-05-26 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
JP2023504546A (ja) | 2019-12-06 | 2023-02-03 | 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 | ナトリウムチャネルの調節因子としての置換テトラヒドロフラン |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
WO2021209377A1 (en) * | 2020-04-16 | 2021-10-21 | Basf Se | A process for the preparation of 4-cyanobenzoyl chlorides |
EP3944859A1 (en) | 2020-07-30 | 2022-02-02 | Assistance Publique Hôpitaux de Paris | Method for treating immune toxicities induced by immune checkpoint inhibitors |
WO2022063140A1 (en) * | 2020-09-23 | 2022-03-31 | Shenzhen Ionova Life Science Co., Ltd. | Pyrimidine and pyridine derivatives as hpk1 modulator and methods using same |
AR126073A1 (es) | 2021-06-04 | 2023-09-06 | Vertex Pharma | N-(hidroxialquil(hetero)aril)tetrahidrofuran carboxamidas como moduladores de canales de sodio |
Family Cites Families (36)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3317534A (en) | 1963-10-30 | 1967-05-02 | Chugai Pharmaceutical Co Ltd | Benzamidopyrimidines |
JPS62158252A (ja) * | 1985-12-28 | 1987-07-14 | Kirin Brewery Co Ltd | 4−アミノピリジンベンズアミド誘導体 |
DE4127404A1 (de) * | 1991-08-19 | 1993-02-25 | Thomae Gmbh Dr K | Cyclische iminoderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
ES2176251T3 (es) * | 1993-07-28 | 2002-12-01 | Aventis Pharma Ltd | Compuestos utilizados como inhibidores de pde iv y del factor de necrosis tumoral(tnf). |
EP1195372A1 (en) * | 1994-04-18 | 2002-04-10 | Mitsubishi Pharma Corporation | N-heterocyclic substituted benzamide derivatives with antihypertensive activity |
US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
JP3122469B2 (ja) * | 1995-06-06 | 2001-01-09 | ヘキスト・マリオン・ルセル・インコーポレイテツド | 抗精神病剤としてのピリジンイミニル−1,2−ベイゾイソオキサゾール類及び−ベンゾイソチアゾール類 |
JPH111456A (ja) * | 1997-06-13 | 1999-01-06 | Otsuka Pharmaceut Co Ltd | アミド誘導体 |
US6562844B2 (en) * | 1998-01-23 | 2003-05-13 | Pharmacia & Upjohn Company | Oxazolidinone combinatorial libraries, compositions and methods of preparation |
DE10021246A1 (de) | 2000-04-25 | 2001-10-31 | Schering Ag | Substituierte Benzoesäureamide und deren Verwendung als Arzneimittel |
CA2407587A1 (en) * | 2000-04-28 | 2001-11-08 | Sankyo Company, Limited | Ppar.gamma. modulators |
US20040102324A1 (en) * | 2002-02-28 | 2004-05-27 | Annis Gary David | Heterocyclic diamide invertebrate pest control agents |
CN1460097A (zh) * | 2001-03-27 | 2003-12-03 | 第一三得利制药株式会社 | 以取代的苯甲酸衍生物为有效成分的NF-κB抑制剂 |
JP2003073357A (ja) * | 2001-09-03 | 2003-03-12 | Mitsubishi Pharma Corp | アミド化合物を含有するRhoキナーゼ阻害剤 |
CA2494061C (en) * | 2002-07-31 | 2011-06-14 | Wayne R. Danter | Protein tyrosine kinase inhibitors |
US7338950B2 (en) | 2003-10-07 | 2008-03-04 | Renovis, Inc. | Amide compounds as ion channel ligands and uses thereof |
GB0403635D0 (en) * | 2004-02-18 | 2004-03-24 | Devgen Nv | Pyridinocarboxamides with improved activity as kinase inhibitors |
US7102002B2 (en) * | 2004-06-16 | 2006-09-05 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
WO2006040645A1 (en) * | 2004-10-11 | 2006-04-20 | Ranbaxy Laboratories Limited | N-(3,5-dichloropyridin-4-yl)-2,4,5-alkoxy and 2,3,4-alkoxy benzamide derivatives as pde-iv (phophodiesterase type-iv) inhibitors for the treatment of inflammatory diseases such as asthma |
CN101080392B (zh) | 2004-12-16 | 2010-05-05 | 霍夫曼-拉罗奇有限公司 | 作为抗肥胖药剂的哌嗪基吡啶衍生物 |
DE602005013819D1 (de) | 2004-12-22 | 2009-05-20 | Astrazeneca Ab | Pyridincarbonsäureamidderivate zur verwendung als antikrebsmittel |
EP1863794A2 (en) | 2005-03-16 | 2007-12-12 | Targegen, Inc. | Pyrimidine compounds and methods of use |
DE102005060449A1 (de) | 2005-12-17 | 2007-06-21 | Bayer Cropscience Ag | Carboxamide |
EA200870217A1 (ru) | 2006-01-30 | 2009-02-27 | Экселиксис, Инк. | 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции |
MX2008016423A (es) * | 2006-06-29 | 2009-01-22 | Hoffmann La Roche | Arilamidas sustituidas con tetrazol. |
ES2428874T3 (es) | 2006-08-09 | 2013-11-12 | Basilea Pharmaceutica Ag | Nuevos macrólidos útiles contra las enfermedades inflamatorias y alérgicas |
WO2008044700A1 (fr) * | 2006-10-11 | 2008-04-17 | Takeda Pharmaceutical Company Limited | INHIBITEUR DE LA GSK-3β |
SI2343286T1 (sl) | 2006-10-28 | 2015-05-29 | Methylgene Inc. | Derivati dibenzo(b,f)(1,4) oksazepina kot inhibitorji histonske deacetilaze |
US8455513B2 (en) * | 2007-01-10 | 2013-06-04 | Aerie Pharmaceuticals, Inc. | 6-aminoisoquinoline compounds |
WO2008112695A2 (en) * | 2007-03-12 | 2008-09-18 | Irm Llc | Pyrazolo [3,4-d] pyrimidines and 1, 2, 5, 6-tetraaza- as- indacenes as protein kinase inhibitors for cancer treatment |
WO2008153974A1 (en) * | 2007-06-07 | 2008-12-18 | Intra-Cellular Therapies, Inc. | Novel heterocycle compounds and uses thereof |
NZ582772A (en) | 2007-07-17 | 2012-06-29 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
WO2009017838A2 (en) * | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
US7982036B2 (en) | 2007-10-19 | 2011-07-19 | Avila Therapeutics, Inc. | 4,6-disubstitued pyrimidines useful as kinase inhibitors |
JP2011507910A (ja) | 2007-12-21 | 2011-03-10 | ユニバーシティー オブ ロチェスター | 真核生物の寿命を変更するための方法 |
FR2926297B1 (fr) | 2008-01-10 | 2013-03-08 | Centre Nat Rech Scient | Molecules chimiques inhibitrices du mecanisme d'epissage pour traiter des maladies resultant d'anomalies d'epissage. |
-
2010
- 2010-06-09 TW TW099118786A patent/TW201103904A/zh unknown
- 2010-06-09 AR ARP100102023A patent/AR077033A1/es unknown
- 2010-06-10 MX MX2011012840A patent/MX2011012840A/es active IP Right Grant
- 2010-06-10 KR KR1020127000759A patent/KR101530117B1/ko not_active IP Right Cessation
- 2010-06-10 AU AU2010258597A patent/AU2010258597B2/en not_active Expired - Fee Related
- 2010-06-10 EP EP10721178A patent/EP2440529A1/en not_active Withdrawn
- 2010-06-10 WO PCT/EP2010/058128 patent/WO2010142752A1/en active Application Filing
- 2010-06-10 JP JP2012514472A patent/JP5763057B2/ja not_active Expired - Fee Related
- 2010-06-10 SG SG2011091451A patent/SG176781A1/en unknown
- 2010-06-10 CA CA2764728A patent/CA2764728A1/en not_active Abandoned
- 2010-06-10 BR BRPI1011129A patent/BRPI1011129A2/pt not_active IP Right Cessation
- 2010-06-10 CN CN201080025358.XA patent/CN102459187B/zh not_active Expired - Fee Related
- 2010-06-10 US US12/813,142 patent/US8486950B2/en not_active Expired - Fee Related
-
2011
- 2011-11-21 IL IL216511A patent/IL216511A0/en unknown
Also Published As
Publication number | Publication date |
---|---|
JP2012529470A (ja) | 2012-11-22 |
WO2010142752A1 (en) | 2010-12-16 |
AU2010258597A1 (en) | 2011-12-15 |
IL216511A0 (en) | 2012-02-29 |
TW201103904A (en) | 2011-02-01 |
CA2764728A1 (en) | 2010-12-16 |
EP2440529A1 (en) | 2012-04-18 |
CN102459187A (zh) | 2012-05-16 |
SG176781A1 (en) | 2012-01-30 |
US20100317643A1 (en) | 2010-12-16 |
KR20120034729A (ko) | 2012-04-12 |
MX2011012840A (es) | 2012-01-27 |
JP5763057B2 (ja) | 2015-08-12 |
CN102459187B (zh) | 2015-06-17 |
KR101530117B1 (ko) | 2015-06-18 |
US8486950B2 (en) | 2013-07-16 |
BRPI1011129A2 (pt) | 2016-11-01 |
AU2010258597B2 (en) | 2016-02-25 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR077033A1 (es) | Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicas | |
AR078408A1 (es) | Derivados de indol como moduladores de los crac | |
AR048315A1 (es) | Compuestos heterociclicos inhibidores de la produccion de citocinas; composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades inflamatorias y oncologicas. | |
PE20080841A1 (es) | Derivados de quinazolinona e isoquinolinona y su uso para el tratamiento o prevencion de trastornos relacionados con el estres o la depresion | |
AR050430A1 (es) | Analogos de dipeptidos inhibidores de la hepatitis c | |
CO2020006411A2 (es) | Inhibidores de endonucleasa cap-dependientes | |
AR082111A1 (es) | Furopiridinas o tienopiridinas condensadas, composiciones farmaceuticas que las contienen utiles para tratar trastornos psicoticos y del sistema nervioso central, y metodo de preparacion de las mismas | |
CO6220855A2 (es) | Compuesto a base de 54 -fenil-6-(2,2,2-trifluoro-1-feniletoxi)pirimidina y metodos para su empleo | |
AR063240A1 (es) | Derivados de n-aril pirazol,composiciones farmaceuticas que los contienen y usos para el tratamiento de la diabetes tipo2,y enfermedades relacionadas. | |
AR078163A1 (es) | Utilizacion de aminodihidrotiazinas para el tratamiento o prevencion de la diabetes | |
AR064010A1 (es) | Inhibidores de la actividad de la akt | |
AR051293A1 (es) | Inhibidores bace | |
AR044152A1 (es) | Derivados de alquilarilo, metodo de preparacion y uso para el tratamiento de la obesidad | |
AR053778A1 (es) | Compuestos de quinazolina para el tratamiento de desordenes mediados por la proteina quinasa | |
AR081577A1 (es) | Derivados de aminopirimidina como moduladores de la lrrk2 | |
AR051995A1 (es) | Derivados de tieno-piridina como intensificadores alostericos de gaba -b | |
AR057982A1 (es) | Compuestos de [hetero) arilo con actividad antagonista de mch y composicion farmaceutica que comprende estos compuestos | |
AR051195A1 (es) | Piridinas como inhibidores de plk | |
PE20091100A1 (es) | Nuevos compuestos 010 | |
AR069524A1 (es) | Derivados de isoxazolo - pirazina, un procedimiento para la preparacion del compuesto, medicamento en base al compuesto y uso del compuesto para preparar un medicamento | |
AR080328A1 (es) | Tienopirimidinas que contienen un grupo alquilo sustituido inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros | |
AR057980A1 (es) | Derivados de la 1- amino-ftalazina sustituida, su preparacion y composicion farmaceutica | |
AR079130A1 (es) | Compuestos inhibidores de la hepatitis c | |
AR059621A1 (es) | Acidos 4- fenil- tiazol-5- carboxilicos y amidas de acidos 4- fenil- tiazol5 carboxilicos como inhibidores de la plk1 | |
AR067058A1 (es) | Oxazolidinonas sustituidas y su uso para preparar medicamentos |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |