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AR054522A1 - Moduladores lxr basados en pirazol - Google Patents

Moduladores lxr basados en pirazol

Info

Publication number
AR054522A1
AR054522A1 ARP060102762A ARP060102762A AR054522A1 AR 054522 A1 AR054522 A1 AR 054522A1 AR P060102762 A ARP060102762 A AR P060102762A AR P060102762 A ARP060102762 A AR P060102762A AR 054522 A1 AR054522 A1 AR 054522A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
cycloalkyl
heteroaryl
independently
Prior art date
Application number
ARP060102762A
Other languages
English (en)
Original Assignee
Exelixis Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37309323&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR054522(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Exelixis Inc filed Critical Exelixis Inc
Publication of AR054522A1 publication Critical patent/AR054522A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D231/20—One oxygen atom attached in position 3 or 5
    • C07D231/22—One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
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    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
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    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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Abstract

Se describen composiciones farmacéuticas que contienen los compuestos, así como los métodos de utilizacion de dichos compuestos. Reivindicacion 1: Un compuesto de acuerdo con una de las formulas (1) a (4), o una sal, isomero o profármaco farmacéuticamente aceptable del mismo, en donde, A) R1 representa -L1-R5, en donde: L1 es un union, L5, L6, -L5-L6-L5-, o -L6-L5-L6-, en donde: cada L5 es independientemente -[C(R15)2]m-, donde, cada R15 es independientemente hidrogeno, halogeno, alquilo C1-6, o haloalquilo C1-6; cada L6 es independientemente -C(R11)2-, -C(R11)2C(R11)2-, -C(R11)=C(R11)-, -C(R11)2O-, -C(R11)2NR11-, -C:::C-, -O-, -S-, -NR11-, -N(R10)CO-, - N(R10)CO2-, -CON(R10)-, -CO-, -CS-, -CO2-, -OC(=O)-, -OC(=O)N(R10)-, - CONR11N(R11)2-, -CONR11-, -OCONR11-, -SO2-, -N(R10)SO2-, - SO2N(R10), -NR10CONR10-, -NR10CSNR10-, -C(=NR11)-, -C(=NOR11)-, -C(=NN(R1)2)-, arilo-, cicloalquilo C3-8, ciclo-haloalquiloC3-8, heteroarilo, heterociclilo, donde el arilo, cicloalquilo, ciclo-haloalquiloC3-8, heteroarilo, o heterociclilo son opcionalmente sustituidos con uno o más radicales de R14; o L1 representa una cadena de alidiilo C2-6 donde la cadena de alidiilo es opcionalmente interrumpida por -C(R11)2-, - C(R11)2C(R11)2-, - C(R11)=C(R11)-, -C(R11)2O-, -C(R11)2NR11-, -C:::C-, -O-, -S-, -N(R10)CO-, -N(R10)CO2-, -CON(R10)-, -CO-, -CO2-, - OC(=O)-, -OC(=O)N(R10)-, -SO2-, -N(R10)SO2-, o -SO2N(R10)-; R5 representa arilo, heterociclilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, cicloalquiloC3-8-alquiloC1-6-, cicloalqueniloC3-8-alquiloC1-6-, cicloalquiloC3-8-alqueniloC2-6, cicloalquilo C3-8, -C, -B-C, -A-B-C, donde, a representa -O-; B representa -[C(R15)2]m- o cicloalquilo C3-8; C representa alquilo C1-6, haloalquilo C1-6, -SO2R11, -SR11, -SO2N(R11)2, - SO2NR11COR11, -C:::N, C(O)OR11, CON(R11)2 o N(R11)2, donde R5 es opcionalmente sustituido con uno o más R5a, en donde cada R5a es independientemente alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquiniloC3-8-alquiloC1-6-, cicloalqueniloC3-8- alquiloC1-6-, cicloalquiloC3-8-alqueniloC2-6-, halogeno, nitro, heterocicli-oxi, arilo, ariloxi, arilalquilo, ariloxiarilo, aril-alcoxiC1-6, -C', -B-C', o - A'-B'-C' en donde A' es -O-; B representa -[C(R15)2]m- o cicloalquilo C3-8-; C' es -H, halogeno, -SO2R11, -OR11, -SR11, -N3, -COR11, - SO2N(R11)2, -SO2NR11COR11, -C:::N, -C(O)OR11, -OC(=O)R11, -CON(R11)2, -CON(R11)OR11, -OCON(R11)2, -NR11COR11, -NR11CON(R11) 2, -NR11COOR11, -N(R11)2, arilo, heteroarilo, o heterociclilo; en donde cada R5 se sustituye de manera opcional con uno o más grupos que son independientemente alquenilo C2-6, alquinilo C2-6, cicloalquiloC3-8-alquiloC1-6-, cicloalqueniloC3-8-alquiloC1-6-, cicloalquiloC3-8- alqueniloC2-6-, alcoxiarilo C0-6, alquilo C1-6, cicloalquilo C3-8, arilohalogeno, -C:::N, -COR11, -COOR11, -CON(R11)2, -SO2R11, -OR11, -SR11, -SO2R11, -SO2N(R11)2, -SO2NR11COR11, -OCON(R11)2; -NR11COR11, -NR11CON(R11)2, -NR11COOR11, o -N(R11)2; 2 y R21 son -L3-R7, en donde: cada L3 es independientemente un enlace o -V1-(CH2)n-V1-, -(CH2)m-V1-(CH2)n- en donde, n es 0-6; y cada V1 es independientemente -C(R11)2-, -C(R11)2C(R11)2-, -C(R11)=C(R11)-, -C(R11)2O-, -C(R11)2NR11-, -C:::C-, -O-, -S-, - NR7-, -N(R10)CO-, - N(R10)CO2-, -OCO-, -CO-, -CS-, -CONR10-, -C(=N-R11)-, -C(=N-OR11)-, -C[=N-N(R11)2], -CO2-, -OC(=O)-, -OC(=O)N(R10)-, -SO2-, -N(R10) SO2-, -SO2N(R10)-, -NR10CONR10-, -NR10CSNR10-, cicloalquilo C3-8, o ciclohaloalquilo C3-8; o cada L3 es independientemente una cadena alidiilo C2-6, en donde la cadena de alidiilo es opcionalmente interrumpida por -C(R11)2-, -C(R11)2C(R11)2-, -C(R11)=C(R11)-, -C(R11)2O-, - C(R11)2NR11-, -C:::C-, -O-, -S-, -N(R10)CO-, -N(R10)CO2-, -CON(R10)-, -CO- , -CO2-, -OC(=O)-, -OC(=O)N(R10)-, -SO2-, -N(R10)SO2-, o - SO2N(R10)-; y cada R7 es independientemente un hidrogeno, halogeno, nitro, arilo, heteroarilo, heterociclilo, -alquiloC1-6-heterociclilo, - alquiloC1-6-heteroarilo, -alquiloC1-6-arilo, -Z, -Y- Z, o -X-Y-Z, en donde, X es -O-; Y es -[C(R15)2]m-, -alqueniloC2-6, -cicloalquiloC3-8; Z es - H, -CN, halogeno, -OR11, -C(=O)R11, -C(=O)OR11, -C(=O)N(R11)2, -N(R11)2, -CN, -N3, -SO2R11, -S(=O)2N(R11)2, -C(=O)N(R11)N(R11)2, - C(=O)N(R11)(OR11), -OC(=O)- R11, -OC(=O)-N(R11)2, o -N(R11)COOR11, en donde R7 se sustituye de manera opcional con uno o más R7a, en donde, R7a es un halogeno, alquenilo C2-6, -alquiloC1-6-heterociclilo, -alquiloC1-6-heteroarilo, -alquiloC1-6-arilo, alcoxiheteroarilo C0-6, alcoxiheterociclilo C0-6, haloarilo, ariloxi, aralquil-oxi, ariloxialquilo, alcoxiarilo C1-6, ariloC0-6-alquilocarboxi, C(R11)=C(R11)-COOOR11, alcoxiheteroarilo C0-6, alcoxiheterociclilo C0-6, arilo, heteroarilo, heterociclilo, cicloalquilo C3-8, heteroarilo-oxi, -Z', -Y'-Z', o-X'-Y'-Z', en donde , X' es -O-; Y' es -[C(R15)2]m- o cicloalquilo C3-8; Z' es -alquiloC1-6, -haloalquiloC1-6, -OR11, -SR11, -S(=O)2R11, -C(=O)R11, -C(=O)OR11, - C(=O)N(R11)2, -N(R11)2, -N(R11)C(=O)R11, - S(=O)2N(R11)C(=O)R11, -CN, -S(=O)2N(R11)2, -C(=O)N(R11)N(R11)2, -C(=O)N(R11)(OR11), - OC(=O)-R11, -OC(=O)-OR11, -N(R11)C(=O)-R11, -N(R11)S(O=)2R11; en donde cada R7a se sustituye de manera opcional con uno o más R8, en donde cada R8 es independientemente un halogeno, nitro, ciano, heteroarilo, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6, haloalquiloC1- C6(OR11), alquilC0-C6OR11, alquiloC0-C6CON(R11)2, alquiloC0-6COR11, alquiloC0-C6COOR11, o alquiloC0-C6SO2R1, y en donde si dos R7a se presentan en el mismo carbono, se pueden combinar para formar un grupo heterociclilo o cicloalquilo; siempre que R2 y R21 no sean de manera simultánea -H; R3 es -L-R6, en donde, L es un enlace, -X3-(CH2)n-X3-, -(CH2)m-X3-(CH2)n- o -(CH2)1+w-Y3- (CH2)w-, en donde, n es 0-6; cada w es independientemente 0-5; y cada X3 es independientemente un enlace, -C(R11)2-, -C(R11)2C(R11)2-, -C(R11)=C(R11)-, -C:::C-, -CO-, -CS-, -CONR10-, -C(=N)(R11)-, -C(=N-OR11)-, -C[=N-N(R11)2], -CO2-, -SO2-, o - SO2N(R10)-; y Y3 es -O-, -S-, -NR7-, -N(R10)CO-, - N(R10)CO2-, -OCO-, -OC(=O)N(R10)-, -NR10CONR10-, -N(R10)SO2-, o -NR10CSNR10-; o L es una cadena de alidiilo C2-6 en donde la cadena de alidiilo se interrumpe de manera opcional por -C(R11)2-, - C(R11)2C(R11)2, -C(R11)=C(R11)-, -C(R11)2O-, -C(R11)2NR11-, -C:::C-, -O-, - S-, -N(R10)CO-, -N(R10)CO2-, -CON(R10)-, -CO-, -CO2-, -OC(=O)-, -OC(=O)N(R10)-, -SO2-, -N(R10)SO2-, o -SO2N(R10); y R6 es alquilo C1-6, haloalquilo C1-6, arilo, cicloalquilo C3-8, heteroarilo, heterociclilo, -CN, -C(=O)R11, -C(=O)OR11, -C(=O)N(R11)2, -N(R11)2, -SO2R11, -S(=O) 2N(R11)2, -C(=O)N(R11)N(R11)2, -C(=O)N(R11)(OR11), en donde el arilo, heteroarilo, cicloalquilo, o heterociclilo se sustituyen de manera opcional con uno o más R6a, en donde cada R6a es independientemente -Z'',-Y''-Z'', o -X''-Y''-Z'', en donde: X'' es -O-; Y'' es -[C(R15)2]m-, - alqueniloC2-6, cicloalquilo C3-8, heterociclilo, arilo, o heteroarilo, en donde el arilo, heteroarilo, cicloalquilo, o heterociclilo se sustituye de manera opcional con al menos un grupo independiente de Z''; Z'' es -H, -CN, halogeno, -OR11, -C(=O)R11, -C(=O)OR11, -C(O)N(R11)2, - N(R11)2, -N3, -SO2R11, -S(=O)2N(R11)2, -C(=O)N(R11)N(R11)2, - N(R11)C(=O)N(R11)2, -OC(=O)-R11, -C(=O)N(R11)(OR11), -OC(=O)-R11, - OC(=O)-N(R11)2, o -N(R11)COOR11; cada R10 es independientemente -R11, -C(=O)R11, -CO2R11, o -SO2R11; cada R11 es independientemente -hidrogeno, alqueniloC2-6, alquinilo C2-6, cicloalqueniloC3-8-alquiloC1-6-, cicloalquiloC3-8-alqueniloC2-6, N(R12)2, alquilo C1-6, -haloalquiloC1-6, -cicloalquiloC3-8, -alquiloC1-6-cicloalquiloC3-8, arilo, -alquiloC1-6-arilo, heteroarilo, -alquiloC1-6-heteroarilo, heterociclilo, o -alquiloC1- 6-heterociclilo; en donde cualquiera de los R11 se los sustituye de manera opcional con uno o más radicales R12; cada R12 es independientemente un halogeno, haloalquilo C1-6, alquilo C1-6, alcoxi C1-6, (alquiloC0-6)C=O(OR13); alquiloC0-6OR13, alquiloC0-6COR13, alquiloC0-6SO2R13, alquiloC0-6CN, alquiloC0-6CON(R13)2, alquiloC0-6CONR13OR13, alquiloC0-C6SO2N(R13)2, alquiloC0-6SR13, haloalquilC0-6OR13, ariloxi, aralquil-oxi, ariloxialquilo, alcoxiarilo C0-6, arilo-alquilcarbonC0-6-oxi, alquiloC0-6NR13SOR13, - alquiloC0-C6N(R13)2, o -OalquiloC0-6COOR13; cada R13 es independientemente un hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquiloC3-8-alquiloC1-6-, cicloalqueniloC3-8-alquiloC1-6-, o cicloalquiloC3-8- alqueniloC2-6-; cada R14 es independientemente alquilo C1-6, alcoxi C1-6, halogeno, haloalquilo C1-6, alquiloC0-6CON(R11)2, alquiloC0-6CONR11OR11, alquiloC0-6OR11, o alquiloC0-6COOR11; G es un grupo de la formula (5), en donde: J es arilo, heteroarilo, o se encuentra ausente; K es arilo, heteroarilo, o se encuentra ausente; cada R4 es independientemente un halogeno, nitro, alquenilo C2-6, cicloalquilo C3-8, -alquiloC1-6-heterociclilo, -alquiloC1-6-heteroarilo, -alquiloC1-6-arilo, - heterociclil-arilo, -heterociclil-heteroarilo, CR11=CR11COOR11, ariloxi, -S-arilo, aralquiloxi, ariloxialquilo, alcoxiarilo C1-6, arilo- alquilcarboxiC0-6, alcoxiheteroarilo C0-6, alcoxiheterociclilo C0-6, arilo, heteroarilo, heterociclilo, -M, -E-M, o -D-E-M, en donde: D es -O-; E es -[C(R15)2]m- o -cicloalquiloC3-8; M es -alquiloC1-6, haloalquilo C1-6, -COR11, -COOR11, -OC(=O)R11, -CON(R11)2, -C:::N, -OR11, - OCON(R11)2, -OCO2-R11, -N3, -NR11COR11, -NR11SO2R11, -N(R11)2, -NR11COOR11, -SOR11, - SO2R11, -SO2NR11COR11, -SO2N(R11)2, o - SR11; en donde cada R4 se sustituye de manera opcional con uno o más R4a, en donde cada R4a es independientemente halogeno, ariloxi, aralquiloxi, ariloxialquilo, alcoxiarilo C1-6, aril-alquilcarbonoC0-C6-oxi, - M', -E'-M', o -D'-E'-M', en donde D' es -O-; E' es -[C(R15)2]m- o cicloalquilC3-C8; M' es -alquiloC1-6, haloalquilo C1-6, -COR11, -CON(R11)2, -N(R11)COOR11, -N(R11)2, COOR11, C:::N, OR11, NR11COR11, NR11SO2R11, SO2R11, SO2N(R11)2, o SR11; cada R41 es independientemente un halogeno, nitro, alquiloC1-6-heterociclilo, -alquiloC1-6- heteroarilo, -alquiloC1-6-arilo, -M'', -E''-M'',
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Families Citing this family (124)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0412263B1 (pt) 2003-07-22 2019-10-15 Arena Pharmaceuticals, Inc. Derivados de diaril e aril heteroaril uréia, uso e composição farmacêutica contendo os mesmos, bem como processo para preparação da dita composição
SA05260357B1 (ar) 2004-11-19 2008-09-08 ارينا فارماسيتو تيكالز ، أنك مشتقات 3_فينيل_بيرازول كمعدلات لمستقبل سيروتينين 5_ht2a مفيدة في علاج الاضطرابات المتعلقه به
EP1910307A1 (en) 2005-06-27 2008-04-16 Exelixis, Inc. Pyrazole based lxr modulators
AU2007221020B9 (en) * 2006-02-28 2013-04-04 Dart Neuroscience (Cayman) Ltd. Therapeutic compounds
AU2013200480B2 (en) * 2006-02-28 2016-06-09 Dart Neuroscience (Cayman) Ltd. Therapeutic compounds
US7829713B2 (en) 2006-02-28 2010-11-09 Helicon Therapeutics, Inc. Therapeutic piperazines
EP2027119A2 (en) 2006-05-18 2009-02-25 Arena Pharmaceuticals, Inc. Ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
CN102827081A (zh) 2006-05-18 2012-12-19 艾尼纳制药公司 用作5-ht2a 血清素受体调节剂的苯基-吡唑的晶型和其制备方法
EP2018371B1 (en) 2006-05-18 2015-03-04 Arena Pharmaceuticals, Inc. Primary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
EP3231442B1 (en) 2006-06-23 2019-12-25 ADC Therapeutics SA Polynucleotides and polypeptide sequences involved in cancer
TWI408136B (zh) * 2006-10-02 2013-09-11 Nat Health Research Institutes 噻吩化合物及其醫藥組成物
TWI415845B (zh) 2006-10-03 2013-11-21 Arena Pharm Inc 用於治療與５-ｈｔ2ａ血清素受體相關聯病症之作為５-ｈｔ2ａ血清素受體之調節劑的吡唑衍生物
US8193225B2 (en) * 2006-10-13 2012-06-05 The Board Of Regents Of The University Of Texas System Isoxazole amides, derivatives and methods of chemical induction of neurogenesis
AU2007333194A1 (en) 2006-12-08 2008-06-19 Exelixis, Inc. LXR and FXR modulators
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
CN103087043A (zh) * 2007-03-16 2013-05-08 中国人民解放军军事医学科学院放射与辐射医学研究所 具有抗增殖活性的苯甲酰胺类衍生物及其药用制剂
KR20100016617A (ko) * 2007-05-18 2010-02-12 바이엘 쉐링 파마 악티엔게젤샤프트 과증식성 장애 및 혈관형성 관련 질환의 치료에 유용한 저산소증 유도성 인자 （ｈｉｆ）의 억제제
AU2008257559B2 (en) * 2007-05-25 2013-10-10 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds as positive modulators of metabotropic glutamate receptor 2 (MGLU2 receptor)
US20100197767A1 (en) * 2007-07-11 2010-08-05 Lior Nissim Nucleic acid construct systems capable of daignosing or treating a cell state
AU2008299781B2 (en) 2007-08-03 2013-11-14 Romark Laboratories L.C. Alkylsulfonyl-substituted thiazolide compounds
EP2190844B3 (en) 2007-08-15 2013-07-17 Arena Pharmaceuticals, Inc. Imidazo[1,2-a]pyridine derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
EP2182809B1 (en) 2007-08-27 2018-01-17 Dart Neuroscience (Cayman) Ltd Therapeutic isoxazole compounds
BRPI0816382A2 (pt) * 2007-09-06 2015-02-24 Merck Sharp & Dohme Composto, composição, e, métodos para ativar a guanilato ciclase solúvel e para tratar ou previnir doenças
WO2009094224A1 (en) 2008-01-25 2009-07-30 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
DE102008015032A1 (de) 2008-03-17 2009-09-24 Aicuris Gmbh & Co. Kg Substituierte Pyrazolamide und ihre Verwendung
DE102008015033A1 (de) 2008-03-17 2009-09-24 Aicuris Gmbh & Co. Kg Substituierte (Pyrazolyl-carbonyl)imidazolidinone und ihre Verwendung
WO2009123714A2 (en) 2008-04-02 2009-10-08 Arena Pharmaceuticals, Inc. Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor
EP2116539A1 (en) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof
US8063088B2 (en) * 2008-06-11 2011-11-22 Hoffmann-La Roche Inc. Imidazolidine derivatives
CA2741731A1 (en) 2008-10-28 2010-06-03 Arena Pharmaceuticals, Inc. Compositions of a 5-ht2a serotonin receptor modulator useful for the treatment of disorders related thereto
US9126946B2 (en) 2008-10-28 2015-09-08 Arena Pharmaceuticals, Inc. Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto
WO2010060186A1 (en) 2008-11-03 2010-06-03 Alethia Biotherapeutics Inc. Antibodies that specifically block the biological activity of a tumor antigen
DE102008057343A1 (de) 2008-11-14 2010-05-20 Bayer Schering Pharma Aktiengesellschaft Heterocyclisch substituierte Aryl-Verbindungen und ihre Verwendung
DE102008057344A1 (de) 2008-11-14 2010-05-20 Bayer Schering Pharma Aktiengesellschaft Aminoalkyl-substituierte Aryl-Verbindungen und ihre Verwendung
DE102008057364A1 (de) 2008-11-14 2010-05-20 Bayer Schering Pharma Aktiengesellschaft Substituierte Aryl-Verbindungen und ihre Verwendung
DE102009041242A1 (de) 2009-09-11 2011-12-15 Bayer Schering Pharma Aktiengesellschaft Heterocyclisch substituierte Aryl-Verbindungen und ihre Verwendung
DE102009041241A1 (de) 2009-09-11 2011-08-04 Bayer Schering Pharma Aktiengesellschaft, 13353 Substituierte Aryl-Verbindungen und ihre Verwendung
DE102008062878A1 (de) 2008-12-17 2010-06-24 Aicuris Gmbh & Co. Kg Substituierte Furancarboxamide und ihre Verwendung
DE102008062863A1 (de) 2008-12-17 2010-06-24 Aicuris Gmbh & Co. Kg Substituierte (Thiophenyl-carbonyl)imidazolidinone und ihre Verwendung
US9139589B2 (en) 2009-01-30 2015-09-22 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
UA106740C2 (uk) 2009-01-30 2014-10-10 Глаксосмітклайн Ллс Кристалічний гідрохлорид n-{(1s)-2-аміно-1-[(3-фторфеніл)метил]етил}-5-хлор-4-(4-хлор-1-метил-1h-піразол-5-іл)-2-тіофенкарбоксаміду
AU2010218224B2 (en) * 2009-02-26 2013-06-27 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
JP5730190B2 (ja) 2009-03-31 2015-06-03 株式会社レナサイエンス プラスミノーゲンアクチベーターインヒビター−１阻害剤
KR101760956B1 (ko) * 2009-05-12 2017-07-24 로마크 레버러토리즈, 엘.씨. 할로알킬 헤테로아릴 벤즈아미드 화합물
SI2435410T1 (sl) * 2009-05-28 2017-06-30 Bristol-Myers Squibb Company Lxr modulatorji
KR20180032689A (ko) 2009-06-26 2018-03-30 로마크 레버러토리즈, 엘.씨. 인플루엔자를 치료하기 위한 화합물 및 방법
DE102009036604A1 (de) 2009-07-30 2011-02-03 Aicuris Gmbh & Co. Kg Substituierte Bis-Arylpyrazolamide mit terminaler primärer Amidfunktionalisierung und ihre Verwendung
JP2011057661A (ja) * 2009-08-14 2011-03-24 Bayer Cropscience Ag 殺虫性カルボキサミド類
WO2011075596A1 (en) 2009-12-18 2011-06-23 Arena Pharmaceuticals, Inc. Crystalline forms of certain 3-phenyl-pyrazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
EP2353591A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
EP2353598A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for use in the prevention and/or treatment of postoperative pain
CA2797533A1 (en) * 2010-04-27 2011-11-10 Calcimedica, Inc. Compounds that modulate intracellular calcium
EP2388005A1 (en) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
EP2395003A1 (en) * 2010-05-27 2011-12-14 Laboratorios Del. Dr. Esteve, S.A. Pyrazole compounds as sigma receptor inhibitors
EA023254B1 (ru) 2010-05-27 2016-05-31 Мерк Шарп Энд Домэ Корп. Активаторы растворимой гуанилатциклазы
CN103313976B (zh) 2010-06-30 2016-11-23 铁木医药有限公司 sGC刺激物
WO2012008528A1 (ja) 2010-07-15 2012-01-19 大日本住友製薬株式会社 ピラゾール化合物
EP2415471A1 (en) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
TW201217365A (en) 2010-08-11 2012-05-01 Millennium Pharm Inc Heteroaryls and uses thereof
EP2603216A4 (en) 2010-08-11 2013-12-18 Millennium Pharm Inc HETEROARYLE AND USES THEREOF
US20130274212A1 (en) 2010-09-07 2013-10-17 Snu R&Db Foundation Sesterterpene Compounds and Use Thereof
UY33671A (es) 2010-10-13 2012-04-30 Millenium Pharmaceuticals Inc Heteroarilos y sus usos
EP2637659B1 (en) 2010-11-09 2016-05-18 Ironwood Pharmaceuticals, Inc. Sgc stimulators
ES2624131T3 (es) * 2011-03-08 2017-07-13 3-V Biosciences, Inc. Moduladores heterocíclicos de la síntesis de lípidos
TW201242953A (en) * 2011-03-25 2012-11-01 Bristol Myers Squibb Co Imidazole prodrug LXR modulators
PL3173427T3 (pl) 2011-03-31 2019-11-29 Adc Therapeutics Sa Przeciwciała przeciwko antygenowi związanemu z nerkami 1 i ich fragmenty wiążące antygen
EP2524694A1 (en) 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
EP2723717A2 (en) 2011-06-24 2014-04-30 Amgen Inc. Trpm8 antagonists and their use in treatments
WO2012177896A1 (en) 2011-06-24 2012-12-27 Amgen Inc. Trpm8 antagonists and their use in treatments
DE102011055815A1 (de) 2011-11-29 2013-05-29 Aicuris Gmbh & Co. Kg Carboxamid-substituierte Heteroaryl-Pyrazole und ihre Verwendung
EP2797915B1 (en) 2011-12-27 2016-07-13 Ironwood Pharmaceuticals, Inc. 2-benzyl-3-(oxazole/thiazole)-5-(pyrimidin-2-yl)-1(H)-pyrazole derivatives as stimulators of the soluble guanylate cyclase (sGC) for the treatment of e.g. hypertension or heart failure
AU2013209234B2 (en) 2012-01-09 2017-11-09 Adc Therapeutics Sa Method for treating breast cancer
PT2820013T (pt) * 2012-03-02 2018-10-25 Ralexar Therapeutics Inc Moduladores do recetor x do fígado (lxr) para o tratamento de doenças dérmicas, distúrbiose condições
WO2013138753A1 (en) 2012-03-16 2013-09-19 Fox Chase Chemical Diversity Center, Inc. Prodrugs of riluzole and their method of use
US8859781B2 (en) * 2012-07-12 2014-10-14 Euclises Pharmaceuticals, Inc. No-releasing nonoate(nitrogen-bound)sulfonamide-linked-coxib anti-cancer agents
JP6212827B2 (ja) * 2012-07-24 2017-10-18 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 Ｎ−シクロプロピル−ｎ−ピペリジニル−アミド誘導体、およびｇｐｒ１１９モジュレーターとしてのそれらの使用
US8952009B2 (en) 2012-08-06 2015-02-10 Amgen Inc. Chroman derivatives as TRPM8 inhibitors
JO3215B1 (ar) 2012-08-09 2018-03-08 Phenex Pharmaceuticals Ag حلقات غير متجانسة بها 5 ذرات تحتوي على النيتروجين بها استبدال بكربوكساميد أو سلفوناميد كمعدلات لمستقبل نووي غير محمي RORy
CA3211094A1 (en) 2012-08-13 2014-02-20 The Rockefeller University Treatment and diagnosis of melanoma
DE102012016908A1 (de) 2012-08-17 2014-02-20 Aicuris Gmbh & Co. Kg Tris-(Hetero)Aryl-Pyrazole und ihre Verwendung
JP6263789B2 (ja) * 2012-09-10 2018-01-24 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 Ｎ−シクロプロピル−ｎ−ピペリジニル−アミド、これらを含有する医薬組成物およびその使用
CN102924347A (zh) * 2012-11-21 2013-02-13 徐州宇家化工科技有限公司 苯基甲基砜衍生物的制备方法
EA201500736A1 (ru) 2013-01-10 2016-04-29 Грюненталь Гмбх Пиразолилкарбоксамиды i в качестве ингибиторов crac каналов
HK1216301A1 (zh) 2013-01-10 2016-11-04 Grünenthal GmbH 作为crac通道抑制剂的基於吡唑基的甲醯胺ii
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
US9828345B2 (en) 2013-02-28 2017-11-28 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors
CN105188380B (zh) * 2013-03-15 2017-08-15 百时美施贵宝公司 Lxr调节剂
US9834542B2 (en) 2013-03-15 2017-12-05 Bristo-Myers Squibb Company LXR modulators
CN105142635B (zh) 2013-03-15 2021-07-27 艾匹根生物技术有限公司 有用于治疗疾病的杂环化合物
US10092537B2 (en) 2013-04-15 2018-10-09 Renascience Co., Ltd. Use for PAI-1 inhibitor
WO2014199164A1 (en) * 2013-06-12 2014-12-18 Ampla Pharmaceuticals, Inc. Diaryl substituted heteroaromatic compounds
SG11201601644RA (en) * 2013-09-04 2016-04-28 Alexar Therapeutics Inc Liver x receptor (lxr) modulators
DK3041835T3 (da) 2013-09-04 2020-07-13 Ellora Therapeutics Inc Modulatorer af lever-X-receptorer (LXR)
CN103588758A (zh) * 2013-11-04 2014-02-19 南京大学 一类含1,4-苯并二噁烷骨架的硝基咪唑衍生物的合成、制备及其在抗癌药物中的应用
US9231217B2 (en) * 2013-11-28 2016-01-05 Semiconductor Energy Laboratory Co., Ltd. Synthesis method of organometallic complex, synthesis method of pyrazine derivative, 5,6-diaryl-2-pyrazyl triflate, light-emitting element, light-emitting device, electronic device, and lighting device
CA2933511A1 (en) 2013-12-17 2015-06-25 Laboratorios Del Dr. Esteve, S.A. Serotonin-norepinephrine reuptake inhibitors (snris) and sigma receptor ligands combinations
AU2014374043B2 (en) 2014-01-06 2019-06-27 Algomedix, Inc. TRPA1 modulators
US10669296B2 (en) 2014-01-10 2020-06-02 Rgenix, Inc. LXR agonists and uses thereof
AR101816A1 (es) 2014-04-02 2017-01-18 Bayer Cropscience Ag Derivados de 3-[(pirazol-5-il)-heteroaril]-benzamidas como agentes pesticidas
CA2950952C (en) 2014-06-10 2023-01-10 Sanford-Burnham Medical Research Institute Metabotropic glutamate receptor negative allosteric modulators (nams) and uses thereof
WO2015197187A1 (en) 2014-06-24 2015-12-30 Grünenthal GmbH Pyrazolyl-based carboxamides v
JP6633618B2 (ja) 2014-08-21 2020-01-22 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 強力なｒｏｃｋ阻害剤としてのタイドバックのベンズアミド誘導体
EP4119141A1 (en) 2015-06-12 2023-01-18 Axovant Sciences GmbH Nelotanserin for the prophylaxis and treatment of rem sleep behavior disorder
EP3322415A4 (en) 2015-07-15 2019-03-13 Axovant Sciences GmbH DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR FOR PROPHYLAXIS AND TREATMENT OF HALLUCINATIONS RELATED TO A NEUROGENERATIVE DISEASE
PL3395801T3 (pl) * 2015-12-16 2021-10-18 Nippon Soda Co., Ltd. Związek aryloazolowy i środek do zwalczania szkodników
CN109069461A (zh) 2016-01-11 2018-12-21 洛克菲勒大学 与髓源性抑制细胞相关的病症的治疗方法
EP3419612B1 (en) 2016-02-26 2024-11-06 The Regents of the University of California Heterocyclic small molecule inhibitors of pendrin ion exchange and pharmaceutical compositions
BR112019001459A2 (pt) 2016-07-27 2019-05-07 Hartis-Pharma Sa combinação, composição farmacêutica, e, método de prevenção e/ou de tratamento de uma doença ou de um distúrbio.
JOP20190086A1 (ar) 2016-10-21 2019-04-18 Novartis Ag مشتقات نافثيريدينون جديدة واستخدامها في معالجة عدم انتظام ضربات القلب
WO2019036024A1 (en) 2017-08-17 2019-02-21 Bristol-Myers Squibb Company 2- (1,1'-BIPHENYL) -1H-BENZO [D] IMIDAZOLE DERIVATIVES AND RELATED COMPOUNDS AS AGONISTS OF APELIN AND APJ FOR THE TREATMENT OF CARDIOVASCULAR DISEASES
EP3713575A4 (en) 2017-11-21 2021-08-25 Rgenix, Inc. POLYMORPHS AND THEIR USES
CN112243374A (zh) 2018-01-29 2021-01-19 卡普勒斯疗法有限责任公司 包括6元中心环的srebp抑制剂
WO2019165158A1 (en) * 2018-02-22 2019-08-29 University Of Florida Research Foundation, Incorporated Il-6 inhibitors and methods of treatment
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CA3127828A1 (en) * 2019-01-28 2020-08-06 Capulus Therapeutics, Llc Srebp inhibitors comprising a thiophene central ring
HUE067466T2 (hu) 2019-12-13 2024-10-28 Inspirna Inc Fémsók és alkalmazásuk
WO2021120890A1 (en) * 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
AU2020417293A1 (en) 2020-01-03 2022-09-01 Berg Llc Polycyclic amides as UBE2K modulators for treating cancer
EP4114467A4 (en) * 2020-03-02 2024-04-17 Trustees Of Tufts College Imidazole-based synthetic lipidoids for in vivo mrna delivery into immune cells
WO2023004280A1 (en) * 2021-07-19 2023-01-26 The Board Of Trustees Of The Leland Stanford Junior University Selective pyrazole lrrk2 inhibitors and methods for use thereof
WO2025104079A1 (en) * 2023-11-17 2025-05-22 Helmholtz-Zentrum für Infektionsforschung GmbH Salicylic acid and picolinic acid derivatives as inhibitors of energy coupling factor (ecf) transporters for the treatment of bacterial infections

Family Cites Families (114)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US655563A (en) * 1900-03-03 1900-08-07 Hewitt Lindstrom Motor Company Electric carriage.
GB1510107A (en) * 1974-05-23 1978-05-10 Sandoz Products Ltd Benzimidazolyl-furan derivatives and use thereof as optical brighteners
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
JPS5726653A (en) * 1980-05-09 1982-02-12 Ciba Geigy Ag Substituted phenyl ether
MX7065E (es) 1980-06-06 1987-04-10 Sankyo Co Un procedimiento microbiologico para preparar derivados de ml-236b
AU570021B2 (en) 1982-11-22 1988-03-03 Novartis Ag Analogs of mevalolactone
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
US4559394A (en) * 1983-06-03 1985-12-17 Phillips Petroleum Company Olefin polymerization using activated chromium catalyst treated with tertiary alcohol
US5583024A (en) 1985-12-02 1996-12-10 The Regents Of The University Of California Recombinant expression of Coleoptera luciferase
US4895867A (en) * 1986-06-26 1990-01-23 Norwich Eaton Pharmaceuticals, Inc. 2-(5-phenyl-2-furanyl)imidazoles useful as cardiotonic agents
IL82856A0 (en) * 1986-06-26 1987-12-20 Norwich Eaton Pharma Pharmaceutical compositions containing 2-(5-phenyl-2-furanyl)imidazoles and certain such novel compounds
US5221623A (en) 1986-07-22 1993-06-22 Boyce Thompson Institute For Plant Research, Inc. Use of bacterial luciferase structural genes for cloning and monitoring gene expression in microorganisms and for tagging and identification of genetically engineered organisms
US5071773A (en) 1986-10-24 1991-12-10 The Salk Institute For Biological Studies Hormone receptor-related bioassays
US5070012A (en) 1988-03-30 1991-12-03 The Board Of Trustees Of The Leland Stanford Junior University Monitoring of cells and trans-activating transcription elements
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
US5683888A (en) 1989-07-22 1997-11-04 University Of Wales College Of Medicine Modified bioluminescent proteins and their use
PH27357A (en) * 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
US5283173A (en) 1990-01-24 1994-02-01 The Research Foundation Of State University Of New York System to detect protein-protein interactions
US5283179A (en) 1990-09-10 1994-02-01 Promega Corporation Luciferase assay method
DE69232537T2 (de) 1991-09-17 2002-10-24 The Salk Institute For Biological Studies, La Jolla Rezeptoren der steroid/thyroid superfamilie von rezeptoren
US6492411B1 (en) * 1993-11-30 2002-12-10 G. D. Searle & Co. Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation
US5466823A (en) * 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
RO118291B1 (ro) * 1993-11-30 2003-04-30 Searle & Co Derivati de pirazol 1,3,4,5 - tetrasubstituiti si compozitie farmaceutica care ii contine
EP0743520A3 (en) 1993-12-30 1999-11-10 The Salk Institute For Biological Studies Novel uses for GAL4-receptor constructs
JP3466765B2 (ja) 1994-07-27 2003-11-17 キッコーマン株式会社 ビオチン化ホタルルシフェラーゼ、ビオチン化ホタルルシフェラーゼ遺伝子、新規な組み換え体ｄｎａ、ビオチン化ホタルルシフェラーゼの製造法及び生物発光分析法
JPH10509140A (ja) * 1994-11-08 1998-09-08 エーザイ株式会社 ピラゾール誘導体
US6005086A (en) 1995-01-13 1999-12-21 The Salk Institute For Biological Studies Farnesoid activated receptor polypeptides, and nucleic acid encoding the same
US5747661A (en) 1995-01-13 1998-05-05 Howard Hughes Medical Institute Retinoid-inducible response elements
US5741657A (en) 1995-03-20 1998-04-21 The Regents Of The University Of California Fluorogenic substrates for β-lactamase and methods of use
JP3964478B2 (ja) * 1995-06-30 2007-08-22 エーザイ・アール・アンド・ディー・マネジメント株式会社 ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬
US5955604A (en) 1996-10-15 1999-09-21 The Regents Of The University Of California Substrates for β-lactamase and uses thereof
PT839810E (pt) * 1996-11-04 2003-01-31 Bayer Cropscience Sa 1-poliarilpirazois como pesticidas
CN1248916A (zh) 1997-01-24 2000-03-29 加利福尼亚大学董事会 FXR、PPARα和LXRα激活剂恢复屏障功能、促进表皮分化和抑制增生的用途
US20020035156A1 (en) * 1997-04-18 2002-03-21 Barbara Roniker Combination therapy in the prevention of cardiovascular disorders
US6506747B1 (en) * 1998-06-05 2003-01-14 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted 1-(4-aminophenyl)pyrazoles and their use as anti-inflammatory agents
US6294558B1 (en) * 1999-05-31 2001-09-25 Pfizer Inc. Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
WO2000017334A2 (en) 1998-09-23 2000-03-30 Ludmila Solomin Analysis of ligand activated nuclear receptors i(in vivo)
GB9824310D0 (en) * 1998-11-05 1998-12-30 Univ London Activators of soluble guanylate cyclase
ES2326850T3 (es) 1998-12-23 2009-10-20 Glaxo Group Limited Ensayos para ligandos de receptores nucleares.
US6534261B1 (en) 1999-01-12 2003-03-18 Sangamo Biosciences, Inc. Regulation of endogenous gene expression in cells using zinc finger proteins
JP4221129B2 (ja) * 1999-02-15 2009-02-12 富士フイルム株式会社 含窒素ヘテロ環化合物、有機発光素子材料、有機発光素子
US6071955A (en) * 1999-02-25 2000-06-06 The Regents Of The University Of California FXR, PPARA and LXRA activators to treat acne/acneiform conditions
US6316503B1 (en) 1999-03-15 2001-11-13 Tularik Inc. LXR modulators
DE60013417T2 (de) 1999-03-26 2005-09-15 City Of Hope, Duarte Verfahren zum screenen von fxr-rezeptormodulatoren
RU2267484C2 (ru) * 1999-04-28 2006-01-10 Авентис Фарма Дойчланд Гмбх Производные диариловой кислоты и фармацевтическая композиция на их основе
CA2375781A1 (en) 1999-06-18 2000-12-28 Cv Therapeutics, Inc. Compositions and methods for increasing cholesterol efflux and raising hdl using atp binding cassette transporter protein abci
CA2377999A1 (en) 1999-07-08 2001-01-18 Tularik Inc Compositions and methods for raising hdl cholesterol levels
DE60023936T2 (de) 1999-12-06 2006-05-24 Sangamo Biosciences Inc., Richmond Methoden zur verwendung von randomisierten zinkfingerprotein-bibliotheken zur identifizierung von genfunktionen
US6602872B1 (en) 1999-12-13 2003-08-05 Merck & Co., Inc. Substituted pyridazines having cytokine inhibitory activity
WO2001060818A1 (en) 2000-02-14 2001-08-23 Tularik Inc. Lxr modulators
US6627647B1 (en) * 2000-03-23 2003-09-30 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted 1-(4-aminophenyl)imidazoles and their use as anti-inflammatory agents
US20020048572A1 (en) 2000-05-03 2002-04-25 Bei Shan Treatment of hypertriglyceridemia and other conditions using LXR modulators
PT1285908E (pt) 2000-05-29 2008-12-04 Kyorin Seiyaku Kk Derivados do ácido fenilpropiónico substituídos
ATE402164T1 (de) * 2001-04-26 2008-08-15 Eisai R&D Man Co Ltd Stickstoffhaltige verbindung mit kondensiertem ring und pyrazolylgruppe als substituent und medizinische zusammensetzung davon
CN1522251A (zh) * 2001-05-09 2004-08-18 ס������ũҩ��ʽ���� 唑化合物及其制备方法和应用
MXPA03011558A (es) * 2001-06-12 2004-03-26 Wellstat Therapeutics Corp Compuestos para el tratamiento de desordenes metabolicos.
HN2002000266A (es) 2001-09-24 2003-11-16 Bayer Corp Preparacion y uso de derivados de imidazol para el tratamiento de la obesidad.
ATE372114T1 (de) * 2001-09-27 2007-09-15 Applied Research Systems Verfahren zur erhöhung des testosteronspiegels
US6924311B2 (en) 2001-10-17 2005-08-02 X-Ceptor Therapeutics, Inc. Methods for affecting various diseases utilizing LXR compounds
US6555563B1 (en) * 2001-11-16 2003-04-29 Medinox, Inc. Heteroaryl substituted amidinyl and imidazolyl compounds and methods employing same for the treatment of inflammation
AU2003209388A1 (en) * 2002-01-29 2003-09-02 Merck And Co., Inc. Substituted imidazoles as cannabinoid receptor modulators
WO2003075921A2 (en) * 2002-03-05 2003-09-18 Transtech Pharma, Inc. Mono- and bicyclic azole derivatives that inhibit the interaction of ligands with rage
AU2003238667B2 (en) * 2002-04-05 2006-07-20 Cadila Healthcare Limited 4-(heterocyclyl)-benzenesulfoximine compounds for the treatment of inflammation
WO2003086287A2 (en) 2002-04-08 2003-10-23 The Ohio State University Research Foundation Compounds and methods for inducing apoptosis in proliferating cells
EP1494667A1 (en) * 2002-04-12 2005-01-12 Pfizer Japan Inc. Imidazole compounds as anti-inflammatory and analgesic agents
WO2004011446A1 (en) 2002-07-26 2004-02-05 Bayer Pharmaceuticals Corporation Indane, dihydrobenzofuran, and tetrahydronaphthalene carboxylic acid derivatives and their use as antidiabetics
AR040726A1 (es) 2002-07-31 2005-04-20 Smithkline Beecham Corp Compuesto de 2- fenilpiridin-4-il-heterociclico, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento
TWI324596B (en) * 2002-08-26 2010-05-11 Nat Health Research Institutes Imidazolamino compounds
EP1398029A1 (en) 2002-09-10 2004-03-17 LION Bioscience AG NR3B1 nuclear receptor binding 3-substituted pyrazole derivatives
AU2003270446A1 (en) * 2002-09-25 2004-04-19 The Board Of Trustees Of The University Of Illinois Method and composition for treating alzheimer's disease and dementias of vascular origin
JP2004137270A (ja) * 2002-09-26 2004-05-13 Nippon Nohyaku Co Ltd 新規除草剤、その使用方法、新規置換チエノピリミジン誘導体及びその中間体並びにそれらの製造方法
JP4631259B2 (ja) 2002-10-03 2011-02-16 コニカミノルタホールディングス株式会社 有機エレクトロルミネッセンス素子及び表示装置
WO2004033432A1 (ja) 2002-10-09 2004-04-22 Ssp Co., Ltd. 抗真菌活性を有する新規ピラゾール化合物
AU2003287965A1 (en) * 2002-10-24 2004-05-13 Carex Sa Modulation of peroxisome proliferator activated receptors activity
WO2004056740A1 (en) 2002-12-20 2004-07-08 Novo Nordisk A/S Dicarboxylic acid derivatives as ppar-agonists
ZA200504898B (en) * 2002-12-20 2006-11-29 Pharmacia Corp Acyclic pyrazole compounds
ATE444292T1 (de) * 2002-12-23 2009-10-15 Sanofi Aventis Deutschland Pyrazolderivate als faktor-xa-inhibitoren
AU2003296404A1 (en) * 2003-01-06 2004-08-10 Eli Lilly And Company Heterocyclic ppar modulators
EP1590336B1 (en) 2003-01-27 2010-12-01 Merck Sharp & Dohme Corp. Substituted pyrazoles, compositions containing such compounds and methods of use
CN1747936A (zh) * 2003-02-12 2006-03-15 特兰斯泰克制药公司 作为治疗试剂的取代吡咯衍生物
JP4590825B2 (ja) * 2003-02-21 2010-12-01 コニカミノルタホールディングス株式会社 白色発光有機エレクトロルミネッセンス素子
CA2512886A1 (en) * 2003-02-28 2004-09-10 Galderma Research & Development, S.N.C. Ligands that modulate lxr-type receptors
WO2004080972A1 (en) 2003-03-12 2004-09-23 Vertex Pharmaceuticals Incorporated Pirazole modulators of atp-binding cassette transporters
WO2004089303A2 (en) 2003-04-03 2004-10-21 Merck & Co., Inc. Di-aryl substituted pyrazole modulators of metabotropic glutamate receptor-5
DE10315571A1 (de) 2003-04-05 2004-10-14 Merck Patent Gmbh Pyrazolverbindungen
DE10315573A1 (de) 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazole
DE10315569A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazolverbindungen
US7226930B2 (en) * 2003-04-18 2007-06-05 Memory Pharmaceutical Corporation Phosphodiesterase 4 inhibitors
WO2005000295A1 (en) * 2003-05-20 2005-01-06 Transtech Pharma, Inc. Rage antagonists as agents to reverse amyloidosis and diseases associated therewith
EA010392B1 (ru) * 2003-05-27 2008-08-29 Сосьете Де Консей Де Решерш Э Д`Аппликасьон Сьентифик (С.К.Р.А.С.) Производные имидазолов, способ их получения и их применение в качестве лекарственного средства
JP2006528617A (ja) 2003-07-24 2006-12-21 ファーマジーン ラボラトリーズ リミテッド ５−ｈｔ２ｂ受容体アンタゴニスト
BRPI0412820A (pt) * 2003-07-25 2006-09-26 Pfizer compostos de aminopirazol e utilização como inibidores de chk1
JP4745971B2 (ja) * 2003-10-03 2011-08-10 ザ オハイオ ステート ユニバーシティー リサーチ ファウンデーション ＰＤＫ−１／Ａｋｔシグナル伝達インヒビター
WO2005037199A2 (en) * 2003-10-10 2005-04-28 Bristol-Myers Squibb Company Pyrazole derivatives as cannabinoid receptor modulators
WO2005037763A1 (en) 2003-10-14 2005-04-28 Eli Lilly And Company Phenoxyether derivatives as ppar modulators
EP1675585A2 (en) 2003-10-17 2006-07-05 Tanabe Seiyaku Co., Ltd. Large conductance calcium-activated k channel opener
JP2007509104A (ja) * 2003-10-24 2007-04-12 グラクソ　グループ　リミテッド 複素環式化合物
DK1692113T3 (en) * 2003-11-14 2018-01-08 Lorus Therapeutics Inc ARYLIMIDAZOLES AND USE THEREOF AS ANTICANCES
TW200526588A (en) 2003-11-17 2005-08-16 Smithkline Beecham Corp Chemical compounds
WO2005054176A1 (en) 2003-11-25 2005-06-16 Eli Lilly And Company Peroxisome proliferator activated receptor modulators
WO2005066137A1 (en) * 2003-12-19 2005-07-21 Neurogen Corporation 2,5-diaryl-1h-imidazole-4-carboxamides as neurokinin-3 receptor modulators for the treatment of central nervous system and peripheral diseases
WO2005102389A2 (en) * 2004-04-20 2005-11-03 Pfizer Products Inc. Combinations comprising alpha-2-delta ligands and ep4 receptor antagonists
ITMI20041032A1 (it) * 2004-05-24 2004-08-24 Neuroscienze S C A R L Compositi farmaceutici
KR20070048771A (ko) * 2004-08-06 2007-05-09 다이이찌 세이야꾸 가부시기가이샤 피라졸 유도체
US20070275968A1 (en) * 2004-09-07 2007-11-29 Hitoshi Kurata Substituted Biphenyl Derivative
JP2006104191A (ja) * 2004-09-07 2006-04-20 Sankyo Co Ltd 置換ビフェニル誘導体
EP1799673A1 (en) 2004-10-15 2007-06-27 Memory Pharmaceuticals Corporation Pyrazole derivatives as phosphodiesterase 4 inhibitors
AU2006205220B2 (en) * 2005-01-10 2012-09-13 Exelixis, Inc. Heterocyclic carboxamide compounds as steroid nuclear receptors ligands
US8084451B2 (en) * 2005-01-10 2011-12-27 University Of Connecticut Heteropyrrole analogs acting on cannabinoid receptors
EP1884513A4 (en) 2005-05-23 2010-04-28 Japan Tobacco Inc PYRAZOLE COMPOUND AND THERAPEUTIC AGENT FOR DIABETES COMPRISING THE SAME
EP1910307A1 (en) 2005-06-27 2008-04-16 Exelixis, Inc. Pyrazole based lxr modulators
US20080090834A1 (en) * 2006-07-06 2008-04-17 Pfizer Inc Selective azole pde10a inhibitor compounds
AU2007333194A1 (en) * 2006-12-08 2008-06-19 Exelixis, Inc. LXR and FXR modulators

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