AR081823A1 - DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd - Google Patents

DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd

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AR081823A1
AR081823A1 ARP110101269A ARP110101269A AR081823A1 AR 081823 A1 AR081823 A1 AR 081823A1 AR P110101269 A ARP110101269 A AR P110101269A AR P110101269 A ARP110101269 A AR P110101269A AR 081823 A1 AR081823 A1 AR 081823A1
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Argentina
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alkyl
nrc5rd5
alkynyl
alkenyl
independently selected
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ARP110101269A
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Andrew P Combs
Richard B Sparks
Eddy W Yue
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Incyte Corp
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Abstract

La presente provee derivados fusionados que modulan la actividad de fosfoinositida 3-quinasas (PI3Ks) y son de utilidad en el tratamiento de enfermedades relacionadas con la actividad de PI3K que incluyen, por ejemplo, trastornos inflamatorios, trastornos con inmunobase, cáncer y otras enfermedades.Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales farmacéuticamente aceptables; en donde V es CR2 o N; X es CR3 o N; Y es CR4 o N; siempre que al menos dos de V, X e Y sean distintos de N; W es CH o N; Z es un enlace, O, S o NRA; siempre que, cuando Z es un enlace, entonces Ar sea un grupo azaheteroarilo bicíclico, que está unido a Z un átomo de nitrógeno, en donde dicho grupo azaheteroarilo bicíclico está sustituido con n grupos RD seleccionados de modo independiente; L es un enlace, alquileno C1-4, NRB, O ó S; Q es alquilo C1-6, alquenilo C2-6, alquinilo C2-6 o Cy; en donde dicho alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están cada uno opcionalmente sustituidos con 1, 2, 3, 4 ó 5 grupos RC seleccionados de modo independiente; Cy es cicloalquilo, heterocicloalquilo, arilo o heteroarilo, cada uno opcionalmente sustituido con 1, 2, 3, 4 ó 5 grupos RC seleccionados de modo independiente; cada RC está seleccionado, de modo independiente, de halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb y S(O)2NRcRd; en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo están cada uno opcionalmente sustituidos con 1, 2, 3, 4 ó 5 sustituyentes seleccionados, de modo independiente, de halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2 y S(O)2NRc2Rd2; R1 está seleccionado, de modo independiente, de H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6 y alquinilo C2-6; en donde dicho alquilo C1-6, haloalquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 sustituyentes seleccionados, de modo independiente, de halo, OH, CN, NR11R12, alcoxi C1-6, haloalcoxi C1-6, tio, alquil C1-6-tio, alquil C1-6-sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6)aminocarbonilamino; cada R11 y R12 está seleccionado, de modo independiente, de H y alquilo C1-6; o cualquier R11 y R12 junto con el átomo de N al que están unidos forman un grupo heterocicloalquilo de 3, 4, 5, 6 ó 7 miembros, que está opcionalmente sustituido con 1, 2, 3 ó 4 sustituyentes seleccionados, de modo independiente, de alquilo C1-6; R2, R3, R4 o R5 están seleccionados cada uno, de modo independiente, de H, OH, NO2, CN, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, amino, alquil C1-6-amino, di(alquil C1-6)amino, tio, alquil C1-6-tio, alquil C1-6-sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6)aminocarbonilamino; Ar es heteroarilo, sustituido con n grupos RD seleccionados de modo independiente; cada RD está seleccionado, de modo independiente, de -(alquil C1-4)r-Cy1, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1 y S(O)2NRc1Rd1; RA está seleccionado de H, alquilo C1-6, alquenilo C2-6 y alquinilo C2-6; RB está seleccionado de H, alquilo C1-6, alquenilo C2-6 y alquinilo C2-6; en donde dicho alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 sustituyentes seleccionados, de modo independiente, de halo, OH, CN, NR11R12, alcoxi C1-6, haloalcoxi C1-6, tio, alquil C1-6-tio, alquil C1-6-sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6)aminocarbonilamino; cada Cy1 es, de modo independiente, arilo, heteroarilo, cicloalquilo o heterocicloalquilo, cada uno opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes seleccionados, de modo independiente, de OH, NO2, CN, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, amino, alquil C1-6-amino, di(alquil C1-6)amino, tio, alquil C1-6-tio, alquil C1-6-sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6)aminocarbonilamino; cada Ra, Rc y Rd está seleccionado, de modo independiente, de H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo, en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes seleccionados, de modo independiente, de alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5 y S(O)2NRc5Rd5; cada Rb está seleccionado, de modo independiente, de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo, en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes seleccionados, de modo independiente, de alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRC5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5 y S(O)2NRc5Rd5; o cualquier Rc y Rd junto con el átomo de N al que están unidos forman un grupo heterocicloalquilo de 3, 4, 5, 6 ó 7 miembros o un grupo heteroarilo, cada uno opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados, de modo independiente, de alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5 y S(O)2NRc5Rd5; cada Re, Rf y Rg está seleccionado, de modo independiente, de H, alquilo C1-6, CN, ORa5, SRb5, S(O)2Rb5, C(O)Rb5, S(O)2NRc5Rd5 y C(O)NRc5Rd5; cada Ra1, Rc1 y Rd1 está seleccionado, de modo independiente, de H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo, en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes seleccionados, de modo independiente, de OH, NO2, CN, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, amino, alquil C1-6-amino, di(alquil C1-6)amino, tio, alquil C1-6-tio, alquil C1-6-sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6)-aminocarbonil
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Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR077280A1 (es) 2009-06-29 2011-08-17 Incyte Corp Pirimidinonas como inhibidores de pi3k, y composiciones farmaceuticas que los comprenden
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
AR079529A1 (es) 2009-12-18 2012-02-01 Incyte Corp Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
ES2764848T3 (es) 2010-12-20 2020-06-04 Incyte Holdings Corp N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
PE20181272A1 (es) 2011-09-02 2018-08-03 Incyte Holdings Corp Heterociclilaminas como inhibidores de pi3k
US20150011569A1 (en) * 2011-12-15 2015-01-08 Philadelphia Health & Education Corporation D/B/A Drexel University College Of Medicine NOVEL P13K p110 INHIBITORS AND METHODS OF USE THEREOF
EA029473B1 (ru) 2011-12-15 2018-03-30 Новартис Аг Применение ингибиторов pi3k для лечения острой и церебральной малярии
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
WO2014015523A1 (en) 2012-07-27 2014-01-30 Hutchison Medipharma Limited Novel heteroaryl and heterocycle compounds, compositions and methods
EP2916868B1 (en) 2012-11-08 2022-05-11 Rhizen Pharmaceuticals S.A. Pharmaceutical compositions containing a pde4 inhibitor and a pi3 delta or dual pi3 delta-gamma kinase inhibitor
US9278950B2 (en) 2013-01-14 2016-03-08 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
PE20191245A1 (es) 2013-01-15 2019-09-18 Incyte Holdings Corp Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim
TWI736135B (zh) 2013-03-01 2021-08-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
SG11201601259YA (en) 2013-08-23 2016-03-30 Incyte Corp Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
MX2016009226A (es) * 2014-01-15 2016-10-05 Novartis Ag Combinaciones farmaceuticas.
HUE051625T2 (hu) 2014-04-08 2021-03-29 Incyte Corp B-sejtes rosszindulatú daganatok kezelése JAK és PI3K inhibitorok kombinációjával
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
EA201692557A1 (ru) 2014-07-04 2017-05-31 Люпин Лимитед Хинолизиноновые производные в качестве ингибиторов pi3k
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
CR20210055A (es) 2015-02-27 2021-04-27 Incyte Corp SALES DE IHNIBIDOR DE PI3K Y PROCESOS DE PREPARACIÓN (Divisional 2017-0389)
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
GB201511790D0 (en) 2015-07-06 2015-08-19 Iomet Pharma Ltd Pharmaceutical compound
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
TWI744256B (zh) 2015-11-06 2021-11-01 美商英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物
US20170190689A1 (en) 2016-01-05 2017-07-06 Incyte Corporation Pyridine and pyridimine compounds as pi3k-gamma inhibitors
US10138248B2 (en) 2016-06-24 2018-11-27 Incyte Corporation Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors
SI3621960T1 (sl) 2017-05-11 2021-11-30 Bristol-Myers Squibb Company Tienopiridini in benzotiofeni uporabni kot irak4 inhibitorji
BR112020007593A2 (pt) 2017-10-18 2020-09-24 Incyte Corporation derivados de imidazol condensados substituídos por grupos hidróxi terciários como inibidores de pi3k-gama
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
KR20210091121A (ko) 2018-09-05 2021-07-21 인사이트 코포레이션 포스포이노시티드 3-키나아제 (pi3k) 억제제의 결정질 형태
WO2020102150A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
US11078204B2 (en) 2018-11-13 2021-08-03 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
CN111170932A (zh) * 2020-01-13 2020-05-19 大连九信精细化工有限公司 一种2-氨甲基-5-三氟甲基吡啶盐的制备方法
WO2021246781A1 (en) * 2020-06-03 2021-12-09 Kainos Medicine, Inc. Pyridine derivatives as immunomodulators

Family Cites Families (249)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3169967A (en) 1957-11-14 1965-02-16 Ciba Geigy Corp Methyl o-lower alkanoyl-reserpates
US3037980A (en) 1955-08-18 1962-06-05 Burroughs Wellcome Co Pyrrolopyrimidine vasodilators and method of making them
DE1770420U (de) 1958-02-27 1958-07-17 Tara Union G M B H Blumentopf aus kunststoff.
US3506643A (en) 1966-12-09 1970-04-14 Max Thiel N**6-aralkyl-adenosine derivatives
DE2139107A1 (de) 1971-08-04 1973-02-15 Merck Patent Gmbh Heterocyclisch substituierte adenosinverbindungen
US3814251A (en) 1972-08-09 1974-06-04 Sperry Rand Corp Power transmission
US3962443A (en) 1972-08-14 1976-06-08 Dainippon Pharmaceutical Co., Ltd. Antibacterial pharmaceutical compositions and processes for preparation thereof
DE2248232A1 (de) 1972-10-02 1974-04-11 Basf Ag 4-thiopyrimido eckige klammer auf 4,5-d eckige klammer zu pyrimidine
US3862189A (en) 1973-08-14 1975-01-21 Warner Lambert Co Aralkyl-substituted purines and pyrimidines as antianginal bronchodilator agents
US3936454A (en) 1973-08-14 1976-02-03 Warner-Lambert Company 5-Amino-4-chloro-6-(substituted amino)-pyrimidines
DK3375A (es) 1974-01-25 1975-09-15 Ciba Geigy Ag
JPS50111080U (es) 1974-02-21 1975-09-10
JPS5625234Y2 (es) 1976-01-17 1981-06-15
JPS5359663U (es) 1976-10-25 1978-05-20
JPS56123981U (es) 1980-02-20 1981-09-21
JPS5883698U (ja) 1981-11-27 1983-06-06 石川島播磨重工業株式会社 熱交換器
JPS58162949A (ja) 1982-03-20 1983-09-27 Konishiroku Photo Ind Co Ltd ハロゲン化銀カラ−写真感光材料
JPS6190153A (ja) 1984-10-09 1986-05-08 Fuji Photo Film Co Ltd ハロゲン化銀写真感光材料の処理方法
JPS62103640U (es) 1985-12-18 1987-07-02
JPH07119970B2 (ja) 1986-04-18 1995-12-20 富士写真フイルム株式会社 画像形成方法
JPS6310746A (ja) 1986-07-01 1988-01-18 Tanabe Seiyaku Co Ltd ナフタレン誘導体
CA1324609C (en) 1986-07-30 1993-11-23 Eastman Kodak Company Photographic element and process
US4861701A (en) 1987-10-05 1989-08-29 Eastman Kodak Company Photographic element and process comprising a compound which comprises two timing groups in sequence
AT388372B (de) 1987-10-08 1989-06-12 Tanabe Seiyaku Co Neue naphthalinderivate und sie enthaltende pharmazeutika
US5124331A (en) 1988-03-02 1992-06-23 Yoshitomi Pharmaceutical Industries, Ltd. 3,4-dihydrothieno[2,3-d]pyrimidine compounds and their pharmaceutical use
US5208250A (en) 1988-05-25 1993-05-04 Warner-Lambert Company Known and selected novel arylmethylenyl derivatives of thiazolidinones, imidazolidinones and oxazolidinones useful as antiallergy agents and anti-inflammatory agents
UA27031A1 (uk) 1990-04-25 2000-02-28 Ніссан Кемікал Індастріз Лтд Похідhі 3(2h)піридазиhоhу або їх фармацевтичhо прийhятhі солі, що мають протитромботичhу, позитивhу іhотропhу, судиhорозширювальhу дію й аhтиалергічhу активhість та фармацевтичhа композиція hа їх осhові
SU1712359A1 (ru) 1990-05-07 1992-02-15 Уфимский Нефтяной Институт Гидрохлорид 8 @ -гидроксихинолинового эфира 8-гидроксихинолин-7-карбоновой кислоты, в качестве бактерицида дл подавлени сульфатвосстанавливающих бактерий и культур РSеUDомоNаS и АRтнRовастеR
DE69129389T2 (de) 1990-06-28 1998-10-08 Fuji Photo Film Co Ltd Photographische Silberhalogenidmaterialien
EP0481614A1 (en) 1990-10-01 1992-04-22 Merck & Co. Inc. Substituted pyridopyrimidinones and related heterocycles as angiotensin II antagonists
US5480883A (en) 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
AU1625192A (en) 1991-05-31 1992-12-03 Zeneca Limited Heterocyclic derivatives
JP3108483B2 (ja) 1991-09-30 2000-11-13 日清製粉株式会社 インドール誘導体およびこれを有効成分とする抗潰瘍薬
HUT64064A (en) 1992-02-13 1993-11-29 Chinoin Gyogyszer Es Vegyeszet Process for producing puyrido/1,2-a/pyrimidine derivatives and pharmaceutical compositions comprising same as active ingredient
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
AU3933493A (en) 1992-04-24 1993-11-29 E.I. Du Pont De Nemours And Company Arthropodicidal and fungicidal aminopyrimidines
TW229140B (es) 1992-06-05 1994-09-01 Shell Internat Res Schappej B V
FR2714907B1 (fr) 1994-01-07 1996-03-29 Union Pharma Scient Appl Nouveaux dérivés de l'Adénosine, leurs procédés de préparation, compositions pharmaceutiques les contenant.
US6342501B1 (en) 1994-02-25 2002-01-29 The Regents Of The University Of Michigan Pyrrolo[2,3-d] pyrimidines as antiviral agents
JPH09176162A (ja) 1995-12-22 1997-07-08 Toubishi Yakuhin Kogyo Kk チアゾリジンジオン誘導体及びその製造法並びにそれを含む医薬組成物
JPH1025294A (ja) 1996-03-26 1998-01-27 Akira Matsuda 縮合ヘテロ環誘導体、その製造法及びそれを含有する悪性腫瘍治療剤
EP0934307B1 (en) 1996-06-19 2011-04-27 Aventis Pharma Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
US6028076A (en) 1996-07-03 2000-02-22 Japan Energy Corporation Purine derivative
US5866702A (en) 1996-08-02 1999-02-02 Cv Therapeutics, Incorporation Purine inhibitors of cyclin dependent kinase 2
US6630496B1 (en) 1996-08-26 2003-10-07 Genetics Institute Llc Inhibitors of phospholipase enzymes
JPH10231297A (ja) 1997-02-20 1998-09-02 Japan Energy Corp 新規なアデニン−１−ｎ−オキシド誘導体およびその医薬用途
CA2309350C (en) 1997-11-12 2007-04-03 Mitsubishi Chemical Corporation Purine derivatives and medicaments comprising the same as active ingredient
TW572758B (en) 1997-12-22 2004-01-21 Sumitomo Pharma Type 2 helper T cell-selective immune response inhibitors comprising purine derivatives
CA2322161A1 (en) 1998-02-25 1999-09-02 Yibin Xiang Inhibitors of phospholipase enzymes
SK12782000A3 (sk) 1998-02-25 2001-04-09 Genetics Institute, Inc. Inhibítory fosfolipázových enzýmov, farmaceutický prostriedok s ich obsahom a ich použitie
US6828344B1 (en) 1998-02-25 2004-12-07 Genetics Institute, Llc Inhibitors of phospholipase enzymes
US6479487B1 (en) 1998-02-26 2002-11-12 Aventis Pharmaceuticals Inc. 6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines
CA2330756C (en) 1998-05-04 2007-10-02 Asta Medica Aktiengesellschaft Indole derivatives and their use for the treatment of malignant and other diseases based on pathological cell proliferation
EP1086950B1 (en) 1998-05-26 2010-09-29 Chugai Seiyaku Kabushiki Kaisha Heterocyclic indole derivatives and mono- or diazaindole derivatives
JP3997651B2 (ja) 1998-06-24 2007-10-24 コニカミノルタホールディングス株式会社 新規色素及び画像記録材料及び感熱転写材料及びインクジェット記録液
DE69942097D1 (de) 1998-08-11 2010-04-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
AU4963999A (en) 1998-08-25 2000-03-14 Uab Research Foundation, The Inhibitors of bacterial nad synthetase
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
RU2001124352A (ru) 1999-02-01 2004-02-20 Си Ви Терапьютикс, Инк. (Us) Пуриновые ингибиторы циклин-зависимой киназы 2 и Ikb-альфа
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
JP2000281654A (ja) 1999-03-26 2000-10-10 Tanabe Seiyaku Co Ltd イソキノリン誘導体
DE19932571A1 (de) 1999-07-13 2001-01-18 Clariant Gmbh Verfahren zur Herstellung von Biarylen unter Palladophosphacyclobutan-Katalyse
JP2001151771A (ja) 1999-09-10 2001-06-05 Kyowa Hakko Kogyo Co Ltd 含窒素芳香族複素環誘導体
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US6436965B1 (en) 2000-03-02 2002-08-20 Merck Frosst Canada & Co. PDE IV inhibiting amides, compositions and methods of treatment
EP1138328A1 (en) 2000-03-29 2001-10-04 Eli Lilly And Company Limited Naphthalene derivatives as CNS drugs
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
NZ522783A (en) 2000-06-28 2004-07-30 Smithkline Beecham P Wet milling process for pharmaceuticals with agitator or chamber having nylon with internal lubricant
CN1331340A (zh) 2000-06-30 2002-01-16 上海博德基因开发有限公司 一种新的多肽——人拓扑异构酶12.1和编码这种多肽的多核苷酸
CN1186326C (zh) 2000-07-05 2005-01-26 山之内制药株式会社 丙－1,3－二酮衍生物
FR2814073B1 (fr) 2000-09-21 2005-06-24 Yang Ji Chemical Company Ltd Composition pharmaceutique antifongique et/ou antiparasitaire et nouveaux derives de l'indole a titre de principes actifs d'une telle composition
DOP2002000334A (es) 2001-02-14 2002-08-30 Warner Lambert Co Pirimidinas biciclicas como inhibidores de metaloproteinasas de matriz
SE0100568D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
US7148237B2 (en) 2001-03-01 2006-12-12 Shionogi & Co., Ltd. Nitrogen-containing heteroaryl compounds having HIV integrase inhibitory activity
UA76977C2 (en) 2001-03-02 2006-10-16 Icos Corp Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers
US20050107400A1 (en) 2001-03-30 2005-05-19 Boyd Leslie F. Use of pyrazolopyridines as therapeutic compounds
JP4237497B2 (ja) 2001-03-30 2009-03-11 スミスクライン ビーチャム コーポレーション ピラゾロピリジン類、その調製方法及びその治療用化合物としての使用
DE60204452T2 (de) 2001-04-27 2005-12-15 Smithkline Beecham Corp. Pyrazolo[1,5a]Pyridinderivate
CZ294535B6 (cs) 2001-08-02 2005-01-12 Ústav Experimentální Botaniky Avčr Heterocyklické sloučeniny na bázi N6-substituovaného adeninu, způsoby jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující
GB0121033D0 (en) 2001-08-30 2001-10-24 Novartis Ag Organic compounds
US8124625B2 (en) 2001-09-14 2012-02-28 Shionogi & Co., Ltd. Method of enhancing the expression of apolipoprotein AI using olefin derivatives
DE60230890D1 (de) 2001-09-19 2009-03-05 Aventis Pharma Sa Indolizine als kinaseproteinhemmer
EP1432710A1 (en) 2001-09-26 2004-06-30 Bayer Pharmaceuticals Corporation 1, 8-naphthyridine derivatives as antidiabetics
ES2309206T3 (es) 2001-10-02 2008-12-16 Smithkline Beecham Corporation Compuestos quimicos.
ATE335490T1 (de) 2001-10-30 2006-09-15 Novartis Pharma Gmbh Staurosporin-derivate als hemmer der flt3- rezeptor-tyrosinkinase-wirkung
JP4663233B2 (ja) 2001-11-09 2011-04-06 エンゾン，インコーポレーテッド ベンジル脱離系を利用する高分子チオール結合プロドラッグ
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
AU2002357043B2 (en) 2001-12-06 2008-04-24 Merck Sharp & Dohme Corp. Mitotic kinesin inhibitors
JP4597519B2 (ja) 2001-12-06 2010-12-15 メルク・シャープ・エンド・ドーム・コーポレイション 有糸***キネシン阻害薬
TW200301135A (en) 2001-12-27 2003-07-01 Otsuka Maryland Res Inst Inc Pharmaceutical compositions comprising a multifunctional phosphodiesterase inhibitor and an adenosine uptake inhibitor
EP1484320A1 (en) 2002-02-13 2004-12-08 Takeda Chemical Industries, Ltd. Jnk inhibitor
AU2003225668A1 (en) 2002-03-01 2003-09-16 Pintex Pharmaceutical, Inc. Pin1-modulating compounds and methods of use thereof
AU2003222106A1 (en) 2002-04-03 2003-10-20 Bristol-Myers Squibb Company Thiopene-based tricyclic compounds and pharmaceutical compositions comprising same
MXPA04010983A (es) 2002-05-06 2005-02-14 Genelabs Tech Inc Derivados de nucleosidos para tratar infecciones por el virus de la hepatitis c.
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
AU2003257822A1 (en) 2002-08-13 2004-04-30 Shionogi And Co., Ltd. Heterocyclic compound having hiv integrase inhibitory activity
JP4190232B2 (ja) 2002-08-26 2008-12-03 富士通株式会社 機械研磨を行う方法
BR0314761A (pt) 2002-09-27 2005-07-26 Sumitomo Pharma Composto de adenina e seu uso
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
AU2003295776B2 (en) 2002-11-21 2011-05-12 Novartis Vaccines And Diagnostics, Inc. 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer
EP1568688B1 (en) 2002-11-25 2011-08-31 Mochida Pharmaceutical Co., Ltd. Therapeutic agent for respiratory disease containing 4-hydroxypiperidine derivative as active ingredient
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
CA2512000C (en) 2002-12-26 2011-08-09 Eisai Co., Ltd. Selective estrogen receptor modulator
CZ294538B6 (cs) 2002-12-30 2005-01-12 Ústav Experimentální Botaniky Akademie Vědčeské Re Substituční deriváty N6-benzyladenosinu, způsob jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující
RU2233842C1 (ru) 2003-01-13 2004-08-10 Петров Владимир Иванович Производные пурина, обладающие противовирусной активностью
AR043692A1 (es) 2003-02-06 2005-08-10 Novartis Ag 2-cianopirrolopirimidinas y sus usos farmaceuticos
GB0304640D0 (en) 2003-02-28 2003-04-02 Novartis Ag Organic compounds
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
SE0300908D0 (sv) 2003-03-31 2003-03-31 Astrazeneca Ab Azaindole derivatives, preparations thereof, uses thereof and compositions containing them
US7129264B2 (en) 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
EP1619948A4 (en) 2003-05-05 2007-02-14 Neurogen Corp SUBSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS
US7326711B2 (en) 2003-06-20 2008-02-05 Chiron Corporation Pyridino[1,2-a]pyrimidin-4-one compounds as anticancer agents
WO2005000309A2 (en) 2003-06-27 2005-01-06 Ionix Pharmaceuticals Limited Chemical compounds
JP4570015B2 (ja) 2003-07-14 2010-10-27 クミアイ化学工業株式会社 ２−イソオキサゾリン誘導体及びそれを有効成分として含有する除草剤
AU2004264419B2 (en) 2003-08-15 2009-01-15 Irm Llc 6-substituted anilino purines as RTK inhibitors
WO2005028434A2 (en) 2003-09-18 2005-03-31 Conforma Therapeutics Corporation Novel heterocyclic compounds as hsp90-inhibitors
CA2539853C (en) 2003-09-23 2011-04-19 Merck & Co., Inc. Isoquinolinone potassium channel inhibitors
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
WO2005074603A2 (en) 2004-02-03 2005-08-18 Abbott Laboratories Aminobenzoxazoles as therapeutic agents
EP1717238A4 (en) 2004-02-16 2008-03-05 Daiichi Seiyaku Co FUNGICIDES HETEROCYCLIC COMPOUNDS
CN1560035A (zh) 2004-03-12 2005-01-05 沈阳药科大学 5－羟基吲哚－3－羧酸脂类衍生物
WO2005091857A2 (en) 2004-03-12 2005-10-06 Bayer Pharmaceuticals Corporation 1,6-naphthyridine and 1,8-naphthyridine derivatives and their use to treat diabetes and related disorders
WO2005092892A1 (ja) 2004-03-26 2005-10-06 Dainippon Sumitomo Pharma Co., Ltd. ８−オキソアデニン化合物
CN1972945A (zh) 2004-04-02 2007-05-30 腺苷治疗有限责任公司 A2a腺苷受体的选择性拮抗剂
CN101031569B (zh) 2004-05-13 2011-06-22 艾科斯有限公司 作为人磷脂酰肌醇3-激酶δ抑制剂的喹唑啉酮
US20060074102A1 (en) 2004-05-14 2006-04-06 Kevin Cusack Kinase inhibitors as therapeutic agents
UA84954C2 (ru) 2004-07-22 2008-12-10 Astrazeneca Ab Конденсированные пиримидоны, пригодные для лечения и профилактики злокачественного новообразования
DE102004044221A1 (de) * 2004-09-14 2006-03-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 3-Methyl-7-butinyl-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
CN101233115A (zh) 2004-10-19 2008-07-30 诺华疫苗和诊断公司 吲哚和苯并咪唑衍生物
EP1807417A2 (en) 2004-11-04 2007-07-18 Neurogen Corporation Pyrazolylmethyl heteroaryl derivatives
JP2008520744A (ja) 2004-11-19 2008-06-19 ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 抗炎症性ピラゾロピリミジン
JP2008520612A (ja) 2004-11-24 2008-06-19 ノバルティス アクチエンゲゼルシャフト ＪＡＫ阻害剤およびＢｃｒ−Ａｂｌ、Ｆｌｔ−３、ＦＡＫまたはＲＡＦキナーゼ阻害剤のうち少なくとも１個の組合せ
AU2006214190A1 (en) 2005-02-17 2006-08-24 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
ATE474829T1 (de) 2005-06-27 2010-08-15 Amgen Inc Entzündungshemmende arylnitrilverbindungen
FR2889192A1 (fr) 2005-07-27 2007-02-02 Cytomics Systems Sa Composes antifongiques, compositions contenant ces composes et leurs utilisations
JP2009504769A (ja) 2005-08-16 2009-02-05 ジェンザイム・コーポレーション ケモカイン受容体結合化合物
US7642270B2 (en) 2005-09-14 2010-01-05 Janssen Pharmaceutica N.V. 5-oxo-5,8-dihydro-pyrido-pyrimidine as inhibitors of c-fms kinase
EP1939202A4 (en) 2005-09-22 2010-06-16 Dainippon Sumitomo Pharma Co NEW COMPOUND OF ADENINE
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
CA2628283C (en) 2005-11-01 2017-06-27 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
EP1783114A1 (en) 2005-11-03 2007-05-09 Novartis AG N-(hetero)aryl indole derivatives as pesticides
WO2007059108A2 (en) 2005-11-10 2007-05-24 Chemocentryx, Inc. Substituted quinolones and methods of use
US7989461B2 (en) 2005-12-23 2011-08-02 Amgen Inc. Substituted quinazolinamine compounds for the treatment of cancer
US20100227880A1 (en) 2006-01-25 2010-09-09 Kristjan Gudmundsson Chemical compounds
PE20071025A1 (es) 2006-01-31 2007-10-17 Mitsubishi Tanabe Pharma Corp Compuesto amina trisustituido
PE20070978A1 (es) * 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
US20090069304A1 (en) 2006-03-03 2009-03-12 Shionogi & Co., Ltd. Mmp-13 selective inhibitor
BRPI0709699A2 (pt) 2006-03-29 2011-07-26 Foldrx Pharmaceuticals Inc inibiÇço da toxidez da alfa-sinucleina
US8933130B2 (en) 2006-06-23 2015-01-13 Radius Health, Inc. Treatment of vasomotor symptoms with selective estrogen receptor modulators
US20080004253A1 (en) 2006-06-30 2008-01-03 Bryan James Branstetter Thiazolopyrimidine modulators of TRPV1
US20080009508A1 (en) 2006-07-10 2008-01-10 Lucie Szucova 6,9-Disubstituted Purine Derivatives And Their Use For Treating Skin
EP2046788A1 (en) 2006-07-12 2009-04-15 Syngeta Participations AG Triazolopyridine derivatives as herbicides
JP5336375B2 (ja) * 2006-08-30 2013-11-06 セルゾーム リミテッド キナーゼ阻害剤としてのトリアゾール誘導体
WO2008032033A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
EP1972631A1 (en) 2007-03-23 2008-09-24 Novartis AG Imidazopyridazines as PI3K lipid kinase inhibitors
WO2008055013A2 (en) 2006-10-31 2008-05-08 Janssen Pharmaceutica N.V. 5-oxo-5,8 - dihydro - pyrido - pyrimidines as inhibitors of c-fms kinase
AU2007323836B2 (en) 2006-11-13 2013-04-18 Icos Corporation Thienopyrimidinones for treatment of inflammatory disorders and cancers
MY188338A (en) 2006-11-22 2021-11-30 Incyte Holdings Corp Imidazotriazines and imidazopyrimidines as kinase inhibitors
CA2672960A1 (en) 2006-12-20 2008-07-10 Schering Corporation Novel jnk inhibitors
DE602007010359D1 (de) 2006-12-29 2010-12-16 Hoffmann La Roche Azaspiroderivate
CL2008000369A1 (es) 2007-02-05 2008-04-18 Xenon Pharmaceuticals Inc Compuestos derivados de piridopirimidinonas; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar dolor, depresion, enfermedades cardiovasculares, enfermedades respiratorias y enfermedades psiquiatricas.
US20090047246A1 (en) 2007-02-12 2009-02-19 Intermune, Inc. Novel inhibitors of hepatitis c virus replication
TW200902018A (en) 2007-03-20 2009-01-16 Dainippon Sumitomo Pharma Co Novel adenine compound
US20080233127A1 (en) 2007-03-21 2008-09-25 Wyeth Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
PT2137186E (pt) 2007-03-23 2016-03-30 Amgen Inc Compostos heterocíclicos e suas utilizações
AU2008231384B2 (en) 2007-03-23 2011-09-15 Amgen Inc. Heterocyclic compounds and their use
US8039505B2 (en) 2007-04-11 2011-10-18 University Of Utah Research Foundation Compounds for modulating T-cells
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
EP2167058B1 (en) 2007-06-18 2015-08-12 University Of Louisville Research Foundation, Inc. Family of pfkfb3 inhibitors with anti-neoplastic activities
KR101561710B1 (ko) 2007-06-29 2015-10-19 길리애드 사이언시즈, 인코포레이티드 퓨린 유도체 및 그것의 톨 유사 수용체 7의 조절 인자로서 용도
US20090053192A1 (en) 2007-08-10 2009-02-26 Burnham Institute For Medical Research Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof
JP2009076865A (ja) 2007-08-29 2009-04-09 Fujifilm Corp 有機電界発光素子
WO2009034386A1 (en) 2007-09-13 2009-03-19 Astrazeneca Ab Derivatives of adenine and 8-aza-adenine and uses thereof-796
JP2009080233A (ja) 2007-09-26 2009-04-16 Kyocera Mita Corp 電子写真感光体
CZ300774B6 (cs) 2007-10-05 2009-08-05 Univerzita Palackého Substituované 6-(alkylbenzylamino)purinové deriváty pro použití jako antagonisté cytokininových receptoru a prípravky obsahující tyto slouceniny
EP2217239A2 (en) 2007-11-07 2010-08-18 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
WO2009063235A1 (en) 2007-11-13 2009-05-22 Astrazeneca Ab Derivatives of 1,9-dihydro-6h-purin-6-one and uses thereof-018
JP2009120686A (ja) 2007-11-14 2009-06-04 Toyo Ink Mfg Co Ltd 光重合開始剤、重合性組成物、および重合物の製造方法。
CL2008003798A1 (es) * 2007-12-19 2009-10-09 Amgen Inc Compuestos derivados de heterobiciclos aromaticos sustituidos, inhibidores de pi3 quinasa; composicion farmaceutica; utiles en el tratamiento de cancer, melanomas, glioblastomas, entre otras enfermedades.
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
EP2231641B1 (en) 2007-12-21 2016-06-01 UCB Biopharma SPRL Quinoxaline and quinoline derivatives as kinase inhibitors
JP2011507900A (ja) 2007-12-21 2011-03-10 ワイス・エルエルシー イミダゾ［１，２−ａ］ピリジン化合物
US7960397B2 (en) 2007-12-28 2011-06-14 Institute Of Experimental Botany, Academy Of Sciences Of The Czech Republic 6,9-disubstituted purine derivatives and their use as cosmetics and cosmetic compositions
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
EA201070841A1 (ru) 2008-01-11 2011-02-28 Натко Фарма Лимитед НОВЫЕ ПИРАЗОЛО[3,4-d]ПИРИМИДИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ПРОТИВОРАКОВЫХ ЛЕКАРСТВЕННЫХ СРЕДСТВ
US9089572B2 (en) 2008-01-17 2015-07-28 California Institute Of Technology Inhibitors of p97
WO2009097446A1 (en) 2008-01-30 2009-08-06 Genentech, Inc. Pyrazolopyrimidine pi3k inhibitor compounds and methods of use
EP2444403A1 (en) 2008-04-18 2012-04-25 Shionogi Co., Ltd. Heterocyclic compound having inhibitory activity on PI3K
US8119647B2 (en) 2008-04-23 2012-02-21 Glenmark Pharmaceuticals S.A. Fused pyrimidineone compounds as TRPV3 modulators
WO2009140215A2 (en) 2008-05-11 2009-11-19 Geraghty, Erin Method for treating drug-resistant bacterial and other infections with clioquinol, phanquinone, and related compounds
US10301265B2 (en) 2008-05-28 2019-05-28 Virginia I. Roxas-Duncan Small molecule inhibitors of botulinum neurotoxins
US20110294836A1 (en) 2008-06-20 2011-12-01 Metabolex, Inc. Aryl gpr119 agonists and uses thereof
US8026271B2 (en) 2008-07-11 2011-09-27 National Health Research Institutes Formulations of indol-3-yl-2-oxoacetamide compounds
WO2010018458A2 (en) 2008-08-12 2010-02-18 Crystalgenomics, Inc. Phenol derivatives and methods of use thereof
JP5731978B2 (ja) 2008-09-26 2015-06-10 インテリカイン， エルエルシー 複素環キナーゼ阻害剤
KR20160091440A (ko) 2008-11-13 2016-08-02 길리아드 칼리스토가 엘엘씨 혈액 종양에 대한 요법
WO2010075068A1 (en) 2008-12-16 2010-07-01 Schering Corporation Pyridopyrimidine derivatives and methods of use thereof
AR075111A1 (es) 2008-12-24 2011-03-09 Bial Portela & Ca Sa Derivados heterociclicos de diazoles y triazoles, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de trastornos del metabolismo y del sistema nervioso, entre otros.
WO2010083444A1 (en) 2009-01-15 2010-07-22 Anvyl, Llc Alpha7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof
US8513284B2 (en) 2009-02-13 2013-08-20 Ucb Pharma, S.A. Fused pyridine and pyrazine derivatives as kinase inhibitors
TW201100428A (en) 2009-03-31 2011-01-01 Arqule Inc Substituted indolo-piperidine compounds
WO2010118367A2 (en) 2009-04-10 2010-10-14 Progenics Pharmaceuticals, Inc. Antiviral pyrimidines
KR20120005523A (ko) 2009-04-20 2012-01-16 길리아드 칼리스토가 엘엘씨 고형 종양의 치료 방법
WO2010127208A1 (en) 2009-04-30 2010-11-04 Forest Laboratories Holdings Limited Inhibitors of acetyl-coa carboxylase
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
WO2010151735A2 (en) 2009-06-25 2010-12-29 Amgen Inc. Heterocyclic compounds and their uses
MX2011013510A (es) 2009-06-25 2012-03-07 Amgen Inc Compuestos heterociclicos y sus usos.
AR077280A1 (es) 2009-06-29 2011-08-17 Incyte Corp Pirimidinonas como inhibidores de pi3k, y composiciones farmaceuticas que los comprenden
FR2947269B1 (fr) 2009-06-29 2013-01-18 Sanofi Aventis Nouveaux composes anticancereux
AR077252A1 (es) 2009-06-29 2011-08-10 Xenon Pharmaceuticals Inc Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos
KR101712035B1 (ko) 2009-06-29 2017-03-03 아지오스 파마슈티컬스 아이엔씨. 치료용 화합물 및 조성물
CN102647987A (zh) 2009-07-21 2012-08-22 吉里德卡利斯托加公司 使用pi3k抑制剂治疗肝脏障碍
PL2470546T3 (pl) 2009-08-28 2013-12-31 Takeda Pharmaceuticals Co Związki heksahydrooksazynopterydynowe do zastosowania jako inhibitory MTOR
US9242987B2 (en) 2009-10-20 2016-01-26 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as JAK inhibitors
IN2012DN02984A (es) 2009-10-22 2015-07-31 Gilead Sciences Inc
EA036876B1 (ru) 2009-11-05 2020-12-30 Ризен Фармасьютикалз С.А. Ингибиторы pi3k киназы
CU24077B1 (es) 2009-11-10 2015-03-30 Pfizer DERIVADOS DE N1-PIRAZOLOESPIROCETONA ÚTILES COMO INHIBIDORES DE ACETIL-CoA CARBOXILASA
WO2011058111A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Aminopurine derivatives as kinase inhibitors
US8957090B2 (en) 2009-11-12 2015-02-17 Ucb Pharma S.A. Fused bicyclic pyridine and pyrazine derivatives as kinase inhibitors
EP2511283A4 (en) 2009-12-10 2013-07-03 Inst Materia Medica Cams N6-SUBSTITUTED ADENOSINE DERIVATIVES, N6-SUBSTITUTED ADENINE DERIVATIVES AND THEIR USE
AR079529A1 (es) 2009-12-18 2012-02-01 Incyte Corp Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
AU2010330875B2 (en) 2009-12-18 2013-08-01 Amgen Inc. Heterocyclic compounds and their uses
JP2011136925A (ja) 2009-12-28 2011-07-14 Dainippon Sumitomo Pharma Co Ltd 含窒素二環性化合物
UY33199A (es) 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.
CA2789900A1 (en) 2010-03-22 2011-09-29 Glenmark Pharmaceuticals S.A. Pharmaceutical composition comprising a pyrimidineone derivative
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
CA2799579A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
AU2011265258A1 (en) 2010-06-11 2013-01-10 Calistoga Pharmaceuticals, Inc. Methods of treating hematological disorders with quinazolinone compounds in selected patients
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
AU2011272853A1 (en) 2010-07-01 2013-01-10 Amgen Inc. Heterocyclic compounds and their use as inhibitors of PI3K activity
WO2012003262A1 (en) 2010-07-01 2012-01-05 Amgen Inc. Heterocyclic compounds and their use as inhibitors of pi3k activity
WO2012003271A1 (en) 2010-07-02 2012-01-05 Amgen Inc. Heterocyclic compounds and their use as inhibitors of pi3k activity
CA2812467A1 (en) 2010-09-24 2012-03-29 Gilead Calistoga Llc Atropisomers of pi3k-inhibiting compounds
MX2013005005A (es) 2010-11-04 2013-10-25 Amgen Inc Derivados de ciano-4,6-diaminopirimidina o 6-aminopurina como inhibidores de pi3k-delta.
JP2013545749A (ja) 2010-11-10 2013-12-26 インフィニティー ファーマシューティカルズ， インコーポレイテッド 複素環化合物及びその使用
MX2013005567A (es) 2010-11-17 2013-10-30 Amgen Inc Derivados de quinolina como inhibidores de pik3.
US20140018540A1 (en) 2010-12-14 2014-01-16 Electrophoretics Limited Casein kinase 1delta (ck 1delta) inhibitors
ES2764848T3 (es) 2010-12-20 2020-06-04 Incyte Holdings Corp N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K
JP2014501261A (ja) 2010-12-23 2014-01-20 アムジエン・インコーポレーテツド 複素環化合物およびそれらの使用
SG10201600179RA (en) 2011-01-10 2016-02-26 Infinity Pharmaceuticals Inc Processes for preparing isoquinolinones and solid forms of isoquinolinones
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
US8969363B2 (en) 2011-07-19 2015-03-03 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PE20181272A1 (es) 2011-09-02 2018-08-03 Incyte Holdings Corp Heterociclilaminas como inhibidores de pi3k
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k

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