AR095079A1 - Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo - Google Patents

Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo

Info

Publication number
AR095079A1
AR095079A1 ARP140100780A ARP140100780A AR095079A1 AR 095079 A1 AR095079 A1 AR 095079A1 AR P140100780 A ARP140100780 A AR P140100780A AR P140100780 A ARP140100780 A AR P140100780A AR 095079 A1 AR095079 A1 AR 095079A1
Authority
AR
Argentina
Prior art keywords
substituted
alkoxy
alkyl
cycloalkyl
pyridinyl
Prior art date
Application number
ARP140100780A
Other languages
English (en)
Inventor
Mattei Patrizio
Mauser Harald
Tang Guozhi
Wang Lisha
Hert Jrme
Hunziker Daniel
Original Assignee
Hoffmann La Roche
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR095079A1 publication Critical patent/AR095079A1/es

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Abstract

Reivindicación 1: Compuestos de la fórmula (1) en la que: R¹ es cicloalquilo sustituido, cicloalquilalquilo sustituido, fenilo sustituido, fenilalquilo sustituido, fenoxialquilo sustituido, fenilcicloalquilo sustituido, fenilalquenilo sustituido, fenilalquinilo sustituido, naftilo sustituido, naftilalquilo sustituido, naftiloxialquilo sustituido, naftilalquenilo sustituido, piridinilo sustituido, piridinil-alquilo sustituido, piridinilalquenilo sustituido, piridinil-alquinilo sustituido, tiofenilo sustituido, tiofenilalquilo sustituido, tiofenilalquenilo sustituido, tiofenilalquinilo sustituido, indolilo sustituido, quinolilo sustituido, iso-quinolilo sustituido, 2,3-dihidro-1H-isoindol-2-ilo sustituido, 1H-indol-2-ilo sustituido o benzofuran-2-ilo sustituido, dichos cicloalquilo sustituido, cicloalquil-alquilo sustituido, fenilo sustituido, fenilalquilo sustituido, fenoxialquilo sustituido, fenilcicloalquilo sustituido, fenilalquenilo sustituido, fenilalquinilo sustituido, naftilo sustituido, naftilalquilo sustituido, naftiloxialquilo sustituido, naftilalquenilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridinilalquenilo sustituido, piridinilalquinilo sustituido, tiofenilo sustituido, tiofenilalquilo sustituido, tiofenil-alquenilo sustituido, tiofenilalquinilo sustituido, indolilo sustituido, quinolilo sustituido, isoquinolilo sustituido, 2,3-dihidro-1H-isoindol-2-ilo sustituido, 1H-indol-2-ilo sustituido y benzofuran-2-ilo sustituido están sustituidos por R⁷, R⁸ y R⁹; R² es fenilo sustituido, piridinilo sustituido, pirrolilo sustituido, oxodihidropiridinilo o tiofenilo sustituido, dichos fenilo sustituido, piridinilo sustituido, pirrolilo sustituido y tiofenilo sustituido están sustituidos por R¹⁰, R¹¹ y R¹²; Y es -OC(O)-, -NR⁵C(O)-, -C(O)-, -S(O)₂-, un resto de fórmula (2) ó un resto de fórmula (3); A es -N- o CH-; W es -O-, -S-, -NR⁶-, -C(O)-, -S(O)₂-, o -CR³R⁴-; R³ y R⁴ se eligen con independencia entre H, halógeno, alquilo y cicloalquilo; R⁵ y R⁶ se eligen con independencia entre H, alquilo y cicloalquilo; R⁷, R⁸ y R⁹ se eligen con independencia entre H, alquilo, hidroxialquilo, haloalquilo, hidroxihaloalquilo, cicloalquilo, cicloalquilalquilo, cicloalquilalcoxi, cicloalcoxi, cicloalcoxialquilo, cicloalquilalcoxialquilo, alcoxi, alcoxi-alquilo, haloalcoxi, alcoxihaloalquilo, alcoxialcoxi, alcoxi-alcoxialquilo, fenilo, fenilo sustituido, piridinilo, piridinilo sustituido, halógeno, hidroxi, ciano, alquil-sulfanilo, haloalquilsulfanilo, cicloalquilsulfanilo, alquilsulfinilo, haloalquilsulfinilo, cicloalquilsulfinilo, alquilsulfonilo, haloalquilsulfonilo, cicloalquilsulfonilo, aminosulfonilo sustituido, amino sustituido y aminoalquilo sustituido, dichos aminosulfonilo sustituido, amino sustituido y aminoalquilo sustituido están sustituidos en el átomo de nitrógeno por uno o dos sustituyentes elegidos con independencia entre H, alquilo, cicloalquilo, cicloalquil-alquilo, hidroxialquilo, alcoxialquilo, alquilcarbonilo y cicloalquilcarbonilo, y dichos fenilo sustituido y piridinilo sustituido están opcionalmente sustituidos de una a tres veces por sustituyentes elegidos con independencia entre alquilo, halógeno, haloalquilo, alcoxi y haloalcoxi, y por lo menos uno de R⁷, R⁸ y R⁹ no es H; R¹⁰ es aminosulfonilo sustituido, alcoxicarbonilo, alquil-carbonilamino, alquilsulfonilamino, amino sustituido, carboxi, ciano, hidroxi o tetrazolilo, dicho amino sustituido está sustituido en el átomo de nitrógeno por uno o dos sustituyentes elegidos con independencia entre H, alquilo, cicloalquilo, cicloalquilalquilo, hidroxialquilo y alcoxialquilo; R¹¹ y R¹² se eligen con independencia entre H, alquilo, cicloalquilo, alcoxi, halógeno y haloalquilo; m, n, p y q se eligen con independencia entre 1 y 2; o las sales farmacéuticamente aceptables.
ARP140100780A 2013-03-12 2014-03-10 Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo AR095079A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13158724 2013-03-12

Publications (1)

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AR095079A1 true AR095079A1 (es) 2015-09-16

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Family Applications (1)

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ARP140100780A AR095079A1 (es) 2013-03-12 2014-03-10 Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo

Country Status (33)

Country Link
US (2) US20150376194A1 (es)
EP (1) EP2970256B1 (es)
JP (2) JP6483034B2 (es)
KR (1) KR20150126036A (es)
CN (1) CN105073748B (es)
AR (1) AR095079A1 (es)
AU (1) AU2014230943B8 (es)
BR (1) BR112015022804A2 (es)
CA (1) CA2901047A1 (es)
CL (1) CL2015002386A1 (es)
CR (1) CR20150436A (es)
DK (1) DK2970256T3 (es)
EA (1) EA035015B1 (es)
ES (1) ES2763417T3 (es)
HK (1) HK1211935A1 (es)
HR (1) HRP20192274T1 (es)
HU (1) HUE046776T2 (es)
IL (1) IL240796B (es)
LT (1) LT2970256T (es)
MA (1) MA38432B1 (es)
MX (1) MX2015011311A (es)
MY (1) MY177574A (es)
PE (1) PE20151605A1 (es)
PH (1) PH12015501934A1 (es)
PL (1) PL2970256T3 (es)
PT (1) PT2970256T (es)
RS (1) RS59682B1 (es)
SG (1) SG11201507396YA (es)
SI (1) SI2970256T1 (es)
TW (1) TWI678368B (es)
UA (1) UA115354C2 (es)
WO (1) WO2014139978A1 (es)
ZA (1) ZA201505944B (es)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6258928B2 (ja) 2012-06-13 2018-01-10 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 新規ジアザスピロシクロアルカンおよびアザスピロシクロアルカン
PT2900669T (pt) 2012-09-25 2019-10-29 Hoffmann La Roche Derivados de hexahidropirrolo[3,4−c]pirrol e compostos relacionados enquanto inibidores da autotaxina (atx) e enquanto inibidores da produção de ácido lisofosfatídico (lpa) para o tratamento de, por exemplo, doenças renais
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
JP6546596B2 (ja) * 2013-09-26 2019-07-17 カデント セラピューティクス,インコーポレーテッド Nr2bの選択的オクタヒドロ−シクロペンタ[c]ピロール負調節因子
WO2015078803A1 (en) 2013-11-26 2015-06-04 F. Hoffmann-La Roche Ag NEW OCTAHYDRO-CYCLOBUTA [1,2-c;3,4-c']DIPYRROL-2-YL
CN106029667B (zh) 2014-03-26 2019-08-23 豪夫迈·罗氏有限公司 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的稠合[1,4]二氮杂*化合物
SI3122750T1 (sl) * 2014-03-26 2019-12-31 F. Hoffmann-La Roche Ag Biciklične spojine kot zaviralci proizvodnje avtotaksina (ATX) in lizofosfatidne kisline (LPA)
KR20160133004A (ko) 2014-04-04 2016-11-21 엑스-알엑스, 인크. 오토탁신의 치환된 스피로시클릭 억제제
JO3579B1 (ar) 2014-09-26 2020-07-05 Luc Therapeutics Inc مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول
GB201501870D0 (en) 2015-02-04 2015-03-18 Cancer Rec Tech Ltd Autotaxin inhibitors
GB201502020D0 (en) 2015-02-06 2015-03-25 Cancer Rec Tech Ltd Autotaxin inhibitory compounds
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
WO2016197009A1 (en) 2015-06-05 2016-12-08 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
WO2017012502A1 (en) 2015-07-17 2017-01-26 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
UA123362C2 (uk) 2015-09-04 2021-03-24 Ф. Хоффманн-Ля Рош Аг Феноксиметильні похідні
CN107922415B (zh) 2015-09-24 2022-04-15 豪夫迈·罗氏有限公司 新的作为双重atx/ca抑制剂的二环化合物
MA42918A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
JP6876685B2 (ja) 2015-09-24 2021-05-26 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Atx阻害剤としての二環式化合物
MX2017015034A (es) * 2015-09-24 2018-04-13 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca).
US20180289702A1 (en) * 2015-10-30 2018-10-11 Robert Nitsch Lpa level reduction for treating central nervous system disorders
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
CN108456208B (zh) * 2017-02-22 2021-04-16 广州市恒诺康医药科技有限公司 氮杂螺环类化合物及其制备方法和应用
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
CA3053329A1 (en) * 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag Heterocyclic compounds useful as dual atx/ca inhibitors
BR112018075312A2 (pt) 2017-03-20 2019-10-01 Forma Therapeutics Inc composições de pirrolopirrol como ativadores da piruvato quinase (pkr)
JP2021506921A (ja) 2017-12-21 2021-02-22 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 放射性標識化合物
EP3852791A4 (en) 2018-09-19 2022-06-15 Forma Therapeutics, Inc. ACTIVATION OF PYRUVATE KINASE R
US20200129485A1 (en) 2018-09-19 2020-04-30 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
WO2020119896A1 (en) * 2018-12-11 2020-06-18 F. Hoffmann-La Roche Ag Heterocyclic inhibitors of atx
CN113412113A (zh) * 2018-12-11 2021-09-17 豪夫迈·罗氏有限公司 氨基嗪酰胺
CN113549063B (zh) * 2020-04-23 2024-04-05 南京药石科技股份有限公司 一种光学异构的八氢-2H-吡咯并[3,4-c]吡啶-2-羧酸叔丁酯的制备方法
TW202211918A (zh) * 2020-06-30 2022-04-01 印度商卡地拉保健有限公司 新穎奧特他新(autotaxin)抑制劑
CA3195597A1 (en) * 2020-10-16 2022-04-21 Jonnie R. Williams Metalloenzyme inhibitors for treating cancers, alzheimer's disease, hemochromatosis, and other disorders

Family Cites Families (138)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1252898B (de) 1965-06-12 1967-10-26 Bayer Ag Verfahren zur Herstellung von Copolymerisaten des Trioxans
US5240928A (en) 1989-07-03 1993-08-31 Merck & Co., Inc. Substituted quinazolinones as angiotensin II antagonists
DE3930262A1 (de) 1989-09-11 1991-03-21 Thomae Gmbh Dr K Kondensierte diazepinone, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
KR910009330B1 (ko) 1989-10-23 1991-11-11 재단법인 한국화학연구소 항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법
CA2037630C (en) 1990-03-07 2001-07-03 Akira Morimoto Nitrogen-containing heterocylic compounds, their production and use
US5470975A (en) 1990-10-16 1995-11-28 E.R. Squibb & Sons, Inc. Dihydropyrimidine derivatives
US5290780A (en) 1991-01-30 1994-03-01 American Cyanamid Co. Angiotensin II receptor blocking 2,3,6 substituted quinazolinones
US5238942A (en) 1991-05-10 1993-08-24 Merck & Co., Inc. Substituted quinazolinones bearing acidic functional groups as angiotensin ii antagonists
DE4121214A1 (de) 1991-06-27 1993-01-14 Bayer Ag 7-azaisoindolinyl-chinolon- und -naphthyridoncarbonsaeure-derivate
US5202322A (en) 1991-09-25 1993-04-13 Merck & Co., Inc. Quinazolinone and pyridopyrimidine a-II antagonists
US5532243A (en) * 1992-02-14 1996-07-02 The Dupont Merck Pharmaceutical Company Antipsychotic nitrogen-containing bicyclic compounds
US5358951A (en) 1993-04-23 1994-10-25 American Cyanamid Company Angiotensin II receptor blocking 2, 3, 6 substituted quinazolinones
DE4407047A1 (de) 1994-03-03 1995-09-07 Merck Patent Gmbh Acetamide
US20010016657A1 (en) 1997-03-18 2001-08-23 Smithkline Beecham P.L.C. Substituted isoquinoline derivatives and their use as anticonvulsants
CN1290251A (zh) 1998-02-04 2001-04-04 万有制药株式会社 N-酰基环胺衍生物
JP2001039950A (ja) 1999-07-30 2001-02-13 Banyu Pharmaceut Co Ltd N−アシル環状アミン誘導体
ATE250604T1 (de) 1999-10-27 2003-10-15 Millennium Pharm Inc Pyridyl enthaltende spirocyclische verbindungen als inhibitoren der fibrinogen-abhängigen blutplättchen aggregation
MXPA03008109A (es) * 2001-03-07 2003-12-12 Pfizer Prod Inc Moduladores de la actividad de receptores de quimiocinas.
AU2003223510B2 (en) 2002-04-12 2008-05-08 Merck Sharp & Dohme Corp. Bicyclic amides
GB0303852D0 (en) 2003-02-19 2003-03-26 Pfizer Ltd Triazole compounds useful in therapy
WO2005023762A1 (en) 2003-09-04 2005-03-17 Abbott Laboratories Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
SE0302811D0 (sv) 2003-10-23 2003-10-23 Astrazeneca Ab Novel compounds
GB0324790D0 (en) 2003-10-24 2003-11-26 Astrazeneca Ab Amide derivatives
US7226951B2 (en) 2003-12-17 2007-06-05 Allergan, Inc. Compounds having selective cytochrome P450RAI-1 or selective cytochrome P450RAI-2 inhibitory activity and methods of obtaining the same
KR100610731B1 (ko) 2004-02-24 2006-08-09 한국과학기술연구원 T-형 칼슘 채널 차단제로서 유용한 3,4-디히드로퀴나졸린유도체 및 그의 제조 방법
JP4845873B2 (ja) 2004-03-03 2011-12-28 ケモセントリックス インコーポレーティッド 二環式および架橋した窒素複素環
CN101001860A (zh) 2004-06-09 2007-07-18 霍夫曼-拉罗奇有限公司 杂环抗病毒化合物
CN101035773B (zh) 2004-08-10 2012-06-06 詹森药业有限公司 抑制hiv的1,2,4-三嗪-6-酮衍生物
US7410949B2 (en) 2005-01-18 2008-08-12 Hoffmann-La Roche Inc. Neuropeptide-2 receptor (Y-2R) agonists and uses thereof
GB0504019D0 (en) 2005-02-26 2005-04-06 Astrazeneca Ab Amide derivatives
BRPI0610433A2 (pt) 2005-04-28 2010-11-23 Wyeth Corp forma polimórfica ii de tanaproget, processos para preparar a mesma, e para preparar forma micronizada de um composto, composição farmacêutica, método de preparação de uma composição farmacêutica, e, uso da forma polimórfica ii de tanaproget ou da forma micronizada
US7737279B2 (en) 2005-05-10 2010-06-15 Bristol-Myers Squibb Company 1,6-dihydro-1,3,5,6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same
TW200800999A (en) 2005-09-06 2008-01-01 Astrazeneca Ab Novel compounds
EP1942108B1 (en) 2005-10-28 2013-09-04 Ono Pharmaceutical Co., Ltd. Compound containing basic group and use thereof
DK1961744T3 (da) 2005-11-18 2013-07-15 Ono Pharmaceutical Co Forbindelse indeholdende basiske grupper samt anvendelse deraf
JP2007176809A (ja) 2005-12-27 2007-07-12 Hideaki Natsukari 複素環置換アミド化合物、その製造法および医薬組成物
WO2007103719A2 (en) 2006-03-03 2007-09-13 Incyte Corporation MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
JP2008031064A (ja) * 2006-07-27 2008-02-14 Astellas Pharma Inc ジアシルピペラジン誘導体
WO2008033764A2 (en) 2006-09-11 2008-03-20 N.V. Organon Quinazolinone and isoquinolinone acetamide derivatives
AR062790A1 (es) 2006-09-15 2008-12-03 Schering Corp Derivados de azetidina utiles en el tratamiento del dolor, diabetes y trastornos del metabolismo de los lipidos
US8735411B2 (en) 2006-10-02 2014-05-27 Abbvie Inc. Macrocyclic benzofused pyrimidine derivatives
TWI404532B (zh) 2006-11-02 2013-08-11 Targacept Inc 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺
ATE523497T1 (de) 2006-11-15 2011-09-15 High Point Pharmaceuticals Llc Neue 2-(2-hydroxyphenyl)benzimidazole, die sich für die behandlung von obesitas und diabetes eignen
TW200831085A (en) 2006-12-13 2008-08-01 Merck & Co Inc Non-nucleoside reverse transcriptase inhibitors
EP1975165A1 (de) 2007-03-27 2008-10-01 Boehringer Ingelheim Pharma GmbH & Co. KG Substituierte Pyrrolidinamide, deren Herstellung und deren Verwendung als Arzneimittel
MX2009009920A (es) 2007-03-29 2009-10-19 Hoffmann La Roche Inhibidores no nucleosidos de transcriptasa inversa.
CL2008001002A1 (es) 2007-04-11 2008-10-17 Actelion Pharmaceuticals Ltd Compuestos derivados de oxazolidinona; composicion farmaceutica que comprende a dichos compuestos; y su uso para preparar un medicamento para tratar una infeccion bacteriana.
AU2008248996A1 (en) 2007-04-27 2008-11-13 Sanofi-Aventis 2 -heteroaryl- pyrrolo [3, 4-C] pyrrole derivatives and their use as SCD inhibitors
UA99626C2 (ru) 2007-08-07 2012-09-10 Эбботт Гмбх Унд Ко. Кг Соединения хинолина, пригодные для лечения нарушений, реагирующих на модуляцию рецептора 5-нт6 серотонина
DE102007047737A1 (de) 2007-10-05 2009-04-30 Merck Patent Gmbh Piperidin- und Piperazinderivate
CA2702984C (en) 2007-10-19 2017-04-11 Sarcode Corporation Compositions and methods for treatment of diabetic retinopathy
AR069126A1 (es) 2007-10-31 2009-12-30 Janssen Pharmaceutica Nv Diaminas en puente o fusionadas sustituidas con arilo como moduladores de leucotrieno a4 hidrolasa
JP2009161449A (ja) 2007-12-28 2009-07-23 Lion Corp Ppar活性促進剤並びに美容用飲食品、皮膚外用剤及び医薬
WO2009154132A1 (ja) 2008-06-19 2009-12-23 萬有製薬株式会社 スピロジアミン-ジアリールケトオキシム誘導体
US8673917B2 (en) 2008-09-09 2014-03-18 Sanofi 2-heteroaryl-pyrrolo [3,4-C]pyrrole derivatives, and use thereof as SCD inhibitors
TW201020247A (en) 2008-11-06 2010-06-01 Gruenenthal Gmbh Substituierte disulfonamide
US8188090B2 (en) 2008-11-17 2012-05-29 Hoffman-La Roche Inc. Naphthylacetic acids
DE102008059578A1 (de) 2008-11-28 2010-06-10 Merck Patent Gmbh Benzo-Naphtyridin Verbindungen
EA201100879A1 (ru) * 2008-12-01 2012-01-30 Мерк Патент Гмбх Производные пиридопиримидина в качестве ингибиторов аутотаксина
TW201035102A (en) 2009-03-04 2010-10-01 Gruenethal Gmbh Sulfonylated tetrahydroazolopyrazines and their use as medicinal products
CN102341386A (zh) 2009-03-05 2012-02-01 第一三共株式会社 吡啶衍生物
WO2010108268A1 (en) 2009-03-23 2010-09-30 Merck Frosst Canada Ltd. Heterocyclic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
TW201038572A (en) 2009-03-25 2010-11-01 Gruenenthal Gmbh Substituted spiro-amide compounds
US8841324B2 (en) 2009-04-02 2014-09-23 Merck Patent Gmbh Heterocyclic compounds as autotaxin inhibitors
EA201101396A1 (ru) 2009-04-02 2012-09-28 Мерк Патент Гмбх Ингибиторы аутотаксина
EP2414330B1 (en) 2009-04-02 2013-05-01 Merck Patent GmbH Piperidine and piperazine derivatives as autotaxin inhibitors
FR2945534B1 (fr) * 2009-05-12 2012-11-16 Sanofi Aventis DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
AU2010249790A1 (en) 2009-05-22 2011-12-08 Exelixis, Inc. Benzoxazepines based P13K/mT0R inhibitors against proliferative diseases
US20120083476A1 (en) 2009-06-05 2012-04-05 Janssen Pharmaceutica Nv Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase
DE102009033392A1 (de) 2009-07-16 2011-01-20 Merck Patent Gmbh Heterocyclische Verbindungen als Autotaxin-Inhibitoren II
US8592402B2 (en) * 2009-08-04 2013-11-26 Amira Pharmaceuticals, Inc. Compounds as lysophosphatidic acid receptor antagonists
UA107360C2 (en) 2009-08-05 2014-12-25 Biogen Idec Inc Bicyclic aryl sphingosine 1-phosphate analogs
AR079022A1 (es) 2009-11-02 2011-12-21 Sanofi Aventis Derivados de acido carboxilico ciclico sustituidos con acilamino, su uso como productos farmaceuticos, composicion farmaceutica y metodo de preparacion
AU2011204323B2 (en) 2010-01-07 2013-12-12 E. I. Du Pont De Nemours And Company Fungicidal heterocyclic compounds
WO2011115813A1 (en) 2010-03-18 2011-09-22 Abbott Laboratories Lactam acetamides as calcium channel blockers
RS54383B1 (en) 2010-03-19 2016-04-28 Pfizer Inc. 2,3-DIHYDRO-1H-INDEN-1-IL-2,7-DIAZASPIRO DERIVATIVES [3.6] NONANES AND THEIR USE AS ANTAGONISTS OR INVERNING AGELISTS OF GRELIN RECEPTORS
AU2011232058B2 (en) 2010-03-26 2016-09-08 Merck Patent Gmbh Benzonaphthyridinamines as autotaxin inhibitors
GB201008005D0 (en) 2010-05-13 2010-06-30 Sentinel Oncology Ltd Pharmaceutical compounds
EP2575794A2 (en) 2010-06-04 2013-04-10 B.S.R.C. "Alexander Fleming" Autotaxin pathway modulation and uses thereof
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
JP2013536200A (ja) * 2010-08-20 2013-09-19 アミラ ファーマシューティカルス,インコーポレーテッド オートタキシン阻害剤およびその使用
EP2611808B1 (en) 2010-09-02 2014-11-12 Merck Patent GmbH Pyrazolopyridinone derivatives as lpa receptor antagonists
WO2012071684A1 (en) 2010-12-02 2012-06-07 Shanghai De Novo Pharmatech Co Ltd. Heterocyclic derivates,preparation processes and medical uses thereof
CN104906103B (zh) 2010-12-14 2018-05-18 电泳有限公司 酪蛋白激酶1δ(CK1δ)抑制剂
WO2012166415A1 (en) * 2011-05-27 2012-12-06 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
EP2751118B1 (en) 2011-08-29 2016-10-12 Bristol-Myers Squibb Company Spiro bicyclic diamine derivatives as hiv attachment inhibitors
WO2013054185A1 (en) 2011-10-13 2013-04-18 Pfizer, Inc. Pyrimidine and pyridine derivatives useful in therapy
JPWO2013065712A1 (ja) 2011-10-31 2015-04-02 東レ株式会社 ジアザスピロウレア誘導体及びその医薬用途
US8809552B2 (en) 2011-11-01 2014-08-19 Hoffmann-La Roche Inc. Azetidine compounds, compositions and methods of use
WO2013079223A1 (en) 2011-12-02 2013-06-06 Phenex Pharmaceuticals Ag Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rorϒ, nr1f3) activity and for the treatment of chronic inflammatory and autoimmune diseases
TWI638802B (zh) 2012-05-24 2018-10-21 芬蘭商奧利安公司 兒茶酚o-甲基轉移酶活性抑制化合物
IL289834B1 (en) 2012-06-13 2024-03-01 Incyte Holdings Corp Conversion of tricyclic compounds as FGFR inhibitors
JP6258928B2 (ja) 2012-06-13 2018-01-10 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 新規ジアザスピロシクロアルカンおよびアザスピロシクロアルカン
EP2867232B1 (en) 2012-06-27 2018-08-08 F.Hoffmann-La Roche Ag 5-azaindazole compounds and methods of use
JP6324380B2 (ja) 2012-07-27 2018-05-16 バイオジェン・エムエイ・インコーポレイテッドBiogen MA Inc. S1p調節剤および/またはatx調節剤である化合物
JP6391571B2 (ja) 2012-07-27 2018-09-19 バイオジェン・エムエイ・インコーポレイテッドBiogen MA Inc. Atx調節剤
AR092211A1 (es) 2012-09-24 2015-04-08 Merck Patent Ges Mit Beschränkter Haftung Derivados de hidropirrolopirrol
PT2900669T (pt) 2012-09-25 2019-10-29 Hoffmann La Roche Derivados de hexahidropirrolo[3,4−c]pirrol e compostos relacionados enquanto inibidores da autotaxina (atx) e enquanto inibidores da produção de ácido lisofosfatídico (lpa) para o tratamento de, por exemplo, doenças renais
PL2900269T3 (pl) 2012-09-25 2019-02-28 Bayer Pharma Aktiengesellschaft Połączenie regorafenibu i kwasu acetylosalicylowego do leczenia raka jelita grubego
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
PL2912019T3 (pl) 2012-10-25 2021-11-02 Tetra Discovery Partners Llc Heteroarylowe inhibitory pde4
AP2015008439A0 (en) 2012-12-31 2015-05-31 Cadila Healthcare Ltd Substituted phthalazin-1(2H)-one derivatives as selective inhibitors of poly (adp-ribose) polymerase-1
WO2014133112A1 (ja) 2013-03-01 2014-09-04 国立大学法人東京大学 オートタキシン阻害活性を有する8-置換イミダゾピリミジノン誘導体
TWI593692B (zh) 2013-03-12 2017-08-01 美國禮來大藥廠 四氫吡咯并噻嗪化合物
EP3539962A1 (en) 2013-03-12 2019-09-18 AbbVie Inc. Tetracyclic bromodomain inhibitors
JP2016512528A (ja) 2013-03-12 2016-04-28 アクセラ インコーポレイテッド 眼疾患及び眼障害を治療するための置換された3−フェニルプロピルアミン誘導体
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
US20160039825A1 (en) 2013-03-15 2016-02-11 Biogen Ma Inc. S1p and/or atx modulating agents
AU2014291711B2 (en) 2013-07-18 2017-02-02 Novartis Ag Autotaxin inhibitors comprising a heteroaromatic ring-benzyl-amide-cycle core
LT3057959T (lt) 2013-10-17 2018-06-11 Vertex Pharmaceuticals Incorporated Dnr-pk inhibitoriai
SI3071561T1 (sl) 2013-11-22 2021-11-30 Sabre Therapeutics Llc Spojine, ki inhibirajo avtotaksin
AR098475A1 (es) 2013-11-26 2016-06-01 Bayer Cropscience Ag Compuestos pesticidas y usos
WO2015078803A1 (en) 2013-11-26 2015-06-04 F. Hoffmann-La Roche Ag NEW OCTAHYDRO-CYCLOBUTA [1,2-c;3,4-c']DIPYRROL-2-YL
ES2671452T3 (es) 2014-03-26 2018-06-06 Basf Se Compuestos de [1,2,4]triazol e imidazol sustituidos como fungicidas
SI3122750T1 (sl) 2014-03-26 2019-12-31 F. Hoffmann-La Roche Ag Biciklične spojine kot zaviralci proizvodnje avtotaksina (ATX) in lizofosfatidne kisline (LPA)
CN106029667B (zh) 2014-03-26 2019-08-23 豪夫迈·罗氏有限公司 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的稠合[1,4]二氮杂*化合物
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
KR20160133004A (ko) 2014-04-04 2016-11-21 엑스-알엑스, 인크. 오토탁신의 치환된 스피로시클릭 억제제
EP3187492A4 (en) 2014-08-29 2018-05-09 The University of Tokyo Pyrimidinone derivative having autotaxin-inhibitory activity
PT3207043T (pt) 2014-10-14 2019-03-25 Vitae Pharmaceuticals Llc Inibidores de di-hidropirrolopiridina de ror-gama
CR20170367A (es) 2015-02-15 2017-09-12 Hoffmann La Roche Derivados de 1-(het)arilsulfonil-(pirrolidin o piperidin)-2-carboxamida y su uso como antagonistas de trpa1
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
CN104927727B (zh) 2015-07-06 2017-01-11 香山红叶建设有限公司 一种玻璃幕墙用结构密封胶及其制备方法
PL415078A1 (pl) 2015-09-04 2017-03-13 Oncoarendi Therapeutics Spółka Z Ograniczoną Odpowiedzialnością Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków
UA123362C2 (uk) 2015-09-04 2021-03-24 Ф. Хоффманн-Ля Рош Аг Феноксиметильні похідні
MX2017015034A (es) 2015-09-24 2018-04-13 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca).
CN107922415B (zh) 2015-09-24 2022-04-15 豪夫迈·罗氏有限公司 新的作为双重atx/ca抑制剂的二环化合物
JP6876685B2 (ja) 2015-09-24 2021-05-26 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Atx阻害剤としての二環式化合物
TW201723176A (zh) 2015-09-24 2017-07-01 Ionis製藥公司 Kras表現之調節劑
MA42918A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
US10323038B2 (en) 2015-11-20 2019-06-18 Abide Therapeutics, Inc. Pyrazole compounds and methods of making and using same
US10385057B2 (en) 2015-11-20 2019-08-20 Lundbeck La Jolla Research Center, Inc. Pyrazole compounds and methods of making and using same
RU2742035C2 (ru) 2015-11-25 2021-02-01 Дана-Фарбер Кэнсер Инститьют, Инк. Бивалентные ингибиторы бромодоменов и пути их применения
KR102070746B1 (ko) 2015-12-01 2020-01-29 니혼노야쿠가부시키가이샤 3h-피롤로피리딘 화합물 또는 그의 n-옥사이드, 또는 그들의 염류 및 상기 화합물을 함유하는 농원예용 살충제 및 그의 사용 방법
WO2017139978A1 (zh) 2016-02-19 2017-08-24 吴伟东 手机app更新方法及***
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
CA3053329A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag Heterocyclic compounds useful as dual atx/ca inhibitors
BR112018075312A2 (pt) 2017-03-20 2019-10-01 Forma Therapeutics Inc composições de pirrolopirrol como ativadores da piruvato quinase (pkr)

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