AR092645A1 - Derivados biciclicos inhibidores de autotaxina (atx) - Google Patents

Derivados biciclicos inhibidores de autotaxina (atx)

Info

Publication number
AR092645A1
AR092645A1 ARP130103396A ARP130103396A AR092645A1 AR 092645 A1 AR092645 A1 AR 092645A1 AR P130103396 A ARP130103396 A AR P130103396A AR P130103396 A ARP130103396 A AR P130103396A AR 092645 A1 AR092645 A1 AR 092645A1
Authority
AR
Argentina
Prior art keywords
substituted
thiophenyl
quinoline
alkyl
cycloalkyl
Prior art date
Application number
ARP130103396A
Other languages
English (en)
Inventor
Hunziker Daniel
Hert Jerme
Mauser Harald
Tang Guozhi
Wang Lisha
Mattei Patrizio
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 AR092645A1 publication Critical patent/AR092645A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epidemiology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Composiciones que contienen los compuestos y métodos de uso de dichos compuestos. Reivindicación 1: Compuestos de la fórmula (1) en la que: R¹ es alquilo, haloalquilo, cicloalquilo sustituido, cicloalquilalquilo sustituido, piperazinilo sustituido, piperidinilo sustituido, indaniloxialquilo sustituido, fenilo sustituido, fenilalquilo sustituido, fenoxialquilo sustituido, fenilcicloalquilo sustituido, fenilalquenilo sustituido, fenilalquinilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridinilalquenilo sustituido, piridinilalquinilo sustituido, tiofenilo sustituido, tiofenilalquilo sustituido, tiofenilalquenilo sustituido, tiofenilalquinilo sustituido, naftilo, naftilo sustituido, quinolilo, quinolinilo sustituido, isoquinolilo sustituido, isoquinolinilo sustituido, 2,3-dihidro-1H-isoindol-2-ilo sustituido, 1H-indol-2-ilo sustituido o benzofuran-2-ilo sustituido, dichos cicloalquilo sustituido, cicloalquilalquilo sustituido, piperazinilo sustituido, piperidinilo sustituido, indaniloxialquilo sustituido, fenilo sustituido, fenilalquilo sustituido, fenilalquinilo sustituido, fenoxialquilo sustituido, fenilcicloalquilo sustituido, fenilalquenilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridinilalquenilo sustituido, piridinilalquinilo sustituido, tiofenilo sustituido, tiofenilalquilo sustituido, tiofenilalquenilo sustituido, tiofenilalquinilo sustituido, naftilo sustituido, quinolinilo sustituido, isoquinolinilo sustituido, 2,3-dihidro-1H-isoindol-2-ilo sustituido, 1H-indol-2-ilo sustituido y benzofuran-2-ilo sustituido están sustituidos por R⁸, R⁹ y R¹⁰; Y es -OC(O)-, -NR⁷C(O)-, -C(O)-, -S(O)₂-, un resto de fórmula (2) ó (3); A es -N- o CR⁵-; W es -O-, -S-, -NR⁶-, -C(O)-, -S(O)₂-, -C(O)-NR⁶- o -CR³R⁴-; R³ y R⁴ se eligen con independencia entre H, halógeno, alquilo y cicloalquilo; R⁵, R⁶ y R⁷ se eligen con independencia entre H, alquilo y cicloalquilo; R⁸, R⁹ y R¹⁰ se eligen con independencia entre H, alquilo, hidroxialquilo, haloalquilo, hidroxihaloalquilo, cicloalquilo, cicloalquilalquilo, cicloalquilalcoxi, cicloalcoxi, cicloalcoxialquilo, cicloalquilalcoxialquilo, alcoxi, alcoxialquilo, haloalcoxi, alcoxihaloalquilo, alcoxialcoxi, alcoxialcoxialquilo, fenilo, fenilo sustituido, piridinilo, piridinilo sustituido, pirrolilo, pirrolilo sustituido, pirrolidinilo, pirrolidinilo sustituido, tetrahidrofuranilo, tetrahidrofuranilo sustituido, halógeno, hidroxi, ciano, alquilsulfanilo, haloalquilsulfanilo, cicloalquilsulfanilo, alquilsulfinilo, haloalquilsulfinilo, cicloalquilsulfinilo, alquilcarbonilo, haloalquilcarbonilo, cicloalquilcarbonilo, alquilsulfonilo, haloalquilsulfonilo, cicloalquilsulfonilo, aminosulfonilo sustituido, amino sustituido y aminoalquilo sustituido, dichos aminosulfonilo sustituido, amino sustituido y aminoalquilo sustituido están sustituidos sobre el átomo de nitrógeno por uno o dos sustituyentes elegidos con independencia entre H, alquilo, cicloalquilo, cicloalquilalquilo, hidroxialquilo, alcoxialquilo, alquilcarbonilo y cicloalquilcarbonilo, y dichos fenilo sustituido, pirrolilo sustituido, pirrolidinilo sustituido, tetrahidrofuranilo sustituido y piridinilo sustituido están sustituidos de una a tres veces por sustituyentes elegidos con independencia entre alquilo, halógeno, haloalquilo, alcoxi y haloalcoxi; m, n, p y q se eligen con independencia entre 1 y 2; R¹¹ es H, alquilo, haloalquilo o cicloalquilo; R¹² es alquilo, halógeno, haloalquilo y alcoxi; R² se elige entre los sistemas de anillos del grupo de fórmulas (4); y sus sales farmacéuticamente aceptables.
ARP130103396A 2012-09-25 2013-09-23 Derivados biciclicos inhibidores de autotaxina (atx) AR092645A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12185941 2012-09-25

Publications (1)

Publication Number Publication Date
AR092645A1 true AR092645A1 (es) 2015-04-29

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Family Applications (1)

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ARP130103396A AR092645A1 (es) 2012-09-25 2013-09-23 Derivados biciclicos inhibidores de autotaxina (atx)

Country Status (33)

Country Link
US (4) US20150353559A1 (es)
EP (2) EP2900669B1 (es)
JP (1) JP6285444B2 (es)
KR (1) KR102179599B1 (es)
CN (1) CN104684915B (es)
AR (1) AR092645A1 (es)
AU (1) AU2013322838B2 (es)
BR (1) BR112015004111A2 (es)
CA (1) CA2878442A1 (es)
CL (1) CL2015000706A1 (es)
CR (1) CR20150120A (es)
DK (1) DK2900669T3 (es)
EA (1) EA036630B1 (es)
ES (1) ES2753163T3 (es)
HK (1) HK1206722A1 (es)
HR (1) HRP20191937T1 (es)
HU (1) HUE045797T2 (es)
IL (1) IL237126A (es)
IN (1) IN2015DN00960A (es)
LT (1) LT2900669T (es)
MA (1) MA37940B1 (es)
MX (1) MX368615B (es)
PE (1) PE20150758A1 (es)
PH (1) PH12015500263B1 (es)
PL (1) PL2900669T3 (es)
PT (1) PT2900669T (es)
RS (1) RS59512B1 (es)
SG (1) SG11201500572YA (es)
SI (1) SI2900669T1 (es)
TW (1) TWI609018B (es)
UA (1) UA116547C2 (es)
WO (1) WO2014048865A1 (es)
ZA (1) ZA201500345B (es)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA201492223A1 (ru) 2012-06-13 2015-03-31 Ф. Хоффманн-Ля Рош Аг Новые диазаспироциклоалканы и азаспироциклоалканы
EP2900669B1 (en) 2012-09-25 2019-09-04 F.Hoffmann-La Roche Ag Hexahydropyrrolo[3,4-c]pyrrole derivatives and related compounds as autotaxin (atx) inhibitors and as inhibitors of the lysophosphatidic acid (lpa) production for treating e.g. renal diseases
US9409895B2 (en) 2012-12-19 2016-08-09 Novartis Ag Autotaxin inhibitors
JP6363616B2 (ja) 2012-12-19 2018-07-25 ノバルティス アーゲー オートタキシン阻害剤
AR095079A1 (es) * 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
CA2917050A1 (en) * 2013-07-03 2015-01-08 Todd K. Jones Pyrrolo-pyrrole carbamate and related organic compounds, pharmaceutical compositions, and medical uses thereof
WO2015048507A1 (en) 2013-09-26 2015-04-02 Mnemosyne Pharmaceuticals, Inc. Selective octahydro-cyclopenta[c] pyrrole negative modulators of nr2b
CA2930737C (en) 2013-11-22 2023-02-21 Pharmakea, Inc. Autotaxin inhibitor compounds
KR20160087900A (ko) 2013-11-26 2016-07-22 에프. 호프만-라 로슈 아게 신규한 옥타하이드로-사이클로부타[1,2-c；3,4-c'']다이피롤-2-일
CN106103446B (zh) * 2014-03-26 2019-07-30 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)生产抑制剂的二环化合物
UA119347C2 (uk) 2014-03-26 2019-06-10 Ф. Хоффманн-Ля Рош Аг Конденсовані [1,4]діазепінові сполуки як інгібітори продукції аутотаксину (atх) та лізофосфатидилової кислоти (lpa)
US9051320B1 (en) 2014-08-18 2015-06-09 Pharmakea, Inc. Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor
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
KR20240060887A (ko) 2015-05-27 2024-05-08 사브레 테라퓨틱스 엘엘씨 오토탁신 억제제 및 이의 용도
CA2988306A1 (en) 2015-06-05 2016-12-08 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
AU2016316717B2 (en) 2015-09-04 2021-02-18 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
KR20180053408A (ko) * 2015-09-24 2018-05-21 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서의 신규한 이환형 화합물
MX2018001430A (es) 2015-09-24 2018-04-20 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca).
EP3353180B1 (en) 2015-09-24 2022-03-16 F. Hoffmann-La Roche AG Bicyclic compounds as atx inhibitors
WO2017050792A1 (en) * 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
CN106986789B (zh) * 2016-01-20 2019-07-16 中国人民解放军军事医学科学院生物医学分析中心 对苯二酚类化合物及其制备方法与在抗肿瘤或免疫调节中的应用
WO2017197192A1 (en) 2016-05-12 2017-11-16 Abide Therapeutics, Inc. Spirocycle compounds and methods of making and using same
JOP20190107A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles 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
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
EP3555101A2 (en) 2016-12-19 2019-10-23 Bayer Pharma Aktiengesellschaft [(phenylsulfonyl)octahydro-epiminoisoindol-yl](1h-1,2,3-triazol-5-yl)methanones
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
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
NZ763766A (en) 2017-03-20 2023-07-28 Novo Nordisk Healthcare Ag Pyrrolopyrrole compositions as pyruvate kinase (pkr) activators
ES2952332T3 (es) 2017-08-29 2023-10-30 H Lundbeck As Compuestos espirocíclicos y sus métodos de preparación y uso
BR112020003946A2 (pt) 2017-08-29 2020-09-08 Lundbeck La Jolla Research Center, Inc. compostos de espirociclo e métodos para produzir e usar os mesmos
WO2019076358A1 (en) 2017-10-19 2019-04-25 Js Innopharm (Shanghai) Ltd HETEROCYCLIC COMPOUNDS, COMPOSITIONS COMPRISING THE HETEROCYCLIC COMPOUND, AND METHODS OF USE THEREOF
TWI780281B (zh) * 2017-12-14 2022-10-11 丹麥商Ｎｍｄ藥品公司 用於治療神經肌肉病症的化合物
BR112021005188A2 (pt) 2018-09-19 2021-06-08 Forma Therapeutics, Inc. tratamento de anemia falciforme com um composto de ativação de piruvato cinase r
EP3852791B1 (en) 2018-09-19 2024-07-03 Novo Nordisk Health Care AG Activating pyruvate kinase r
CN111620866A (zh) * 2019-02-27 2020-09-04 南京药石科技股份有限公司 一种顺式-7,7-二氟-六氢-1H 吡咯并[3,4-c]吡啶衍生物及其制备方法
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
TW202229255A (zh) 2020-11-13 2022-08-01 丹麥商Ｈ 朗德貝克公司 Magl抑制劑
CN113214111A (zh) * 2021-04-30 2021-08-06 上海立科化学科技有限公司 3-（2-氰基苯基）丙酸及4-氰基-1-茚满酮的制备方法
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors

Family Cites Families (125)

* 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
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
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
CZ20021550A3 (cs) 1999-11-09 2003-02-12 Societe De Conseils De Recherches Et D'application Produkt zahrnující inhibitor transdukce signálů heterotrimerického G proteinu kombinovaný s jiným protirakovinným činidlem pro terapeutické použití v léčbě rakoviny
EP1368354A1 (en) 2001-03-07 2003-12-10 Pfizer Products Inc. Modulators of chemokine receptor activity
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
US7435831B2 (en) * 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
EP1720545B1 (en) 2004-03-03 2014-10-29 ChemoCentryx, Inc. Bicyclic and bridged nitrogen heterocycles
EP1761542B1 (en) 2004-06-09 2008-01-02 F.Hoffmann-La Roche Ag Octahydropyrrolo[3,4-c]pyrrole derivatives an their use as antiviral agents
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
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
JP5251127B2 (ja) 2005-10-28 2013-07-31 小野薬品工業株式会社 塩基性基を含有する化合物およびその用途
JP5412113B2 (ja) * 2005-11-14 2014-02-12 パーデュー・リサーチ・ファウンデーション Ｎ置換インデノイソキノリン及びその合成
PT1961744E (pt) 2005-11-18 2013-05-15 Ono Pharmaceutical Co Composto que contém um grupo básico e sua utilização
US20070208001A1 (en) 2006-03-03 2007-09-06 Jincong Zhuo Modulators of 11- beta 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
RU2009113612A (ru) 2006-09-11 2010-10-20 Н.В. Органон (Nl) Ацетамидные производные хиназолинона и изохинолинона
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
CA2669884A1 (en) 2006-11-15 2008-05-22 High Point Pharmaceuticals, Llc Novel 2-(2-hydroxyphenyl)benzimidazoles useful for treating obesity and diabetes
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
EP2142520A1 (en) 2007-03-29 2010-01-13 F. Hoffmann-Roche AG Non-nucleoside reverse transcriptase inhibitors
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.
EP2152711B1 (de) 2007-04-27 2010-11-24 Sanofi-Aventis 2 -heteroaryl- pyrrolo [3, 4-c]pyrrol- derivate und deren verwendung als scd inhibitoren
DE102007047737A1 (de) 2007-10-05 2009-04-30 Merck Patent Gmbh Piperidin- und Piperazinderivate
US20090155176A1 (en) 2007-10-19 2009-06-18 Sarcode Corporation Compositions and methods for treatment of diabetic retinopathy
PA8802501A1 (es) * 2007-10-31 2009-06-23 Janssen Pharmaceutica Nv Diaminas en puente o fusionadas sustituidas con arilo como moduladores de leucotrieno, 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
EP2301936A1 (en) 2008-06-19 2011-03-30 Banyu Pharmaceutical Co., Ltd. Spirodiamine-diarylketoxime derivative
WO2010028761A1 (de) 2008-09-09 2010-03-18 Sanofi-Aventis 2-heteroaryl-pyrrolo[3, 4-c]pyrrol-derivate und ihre verwendung als scd inhibitoren
TW201020247A (en) 2008-11-06 2010-06-01 Gruenenthal Gmbh Substituierte disulfonamide
WO2010055006A1 (en) 2008-11-17 2010-05-20 F. Hoffmann-La Roche Ag Naphthylacetic acids used as crth2 antagonists or partial agonists
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
TW201038572A (en) 2009-03-25 2010-11-01 Gruenenthal Gmbh Substituted spiro-amide compounds
EP2414327B1 (de) * 2009-04-02 2014-11-19 Merck Patent GmbH Heterocyclische verbindungen als autotaxin-inhibitoren
KR20120027177A (ko) 2009-04-02 2012-03-21 메르크 파텐트 게엠베하 오토탁신 저해제로서의 피페리딘 및 피라진 유도체
US8329907B2 (en) 2009-04-02 2012-12-11 Merck Patent Gmbh 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
JP2012527474A (ja) 2009-05-22 2012-11-08 エクセリクシス， インク． 増殖性疾患に対するベンゾキサゼピンベースのｐｉ３ｋ／ｍｔ０ｒ阻害剤
WO2010141817A1 (en) 2009-06-05 2010-12-09 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
EP2462128B1 (en) 2009-08-04 2016-09-21 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
US8835427B2 (en) * 2010-01-07 2014-09-16 E I Du Pont De Nemours And Company Fungicidal heterocyclic compounds
US8815869B2 (en) 2010-03-18 2014-08-26 Abbvie Inc. Lactam acetamides as calcium channel blockers
PT2547679E (pt) 2010-03-19 2016-01-27 Pfizer Derivados de 2,3-di-hidro-1h-indeno-1-il-2,7-diazaspiro[3.6]nonano e sua utilização como antagonistas ou agonistas inversos do receptor de grelina
EP2552914B1 (de) 2010-03-26 2015-11-11 Merck Patent GmbH Benzonaphthyridinamine als autotaxin-inhibitoren
GB201008005D0 (en) 2010-05-13 2010-06-30 Sentinel Oncology Ltd Pharmaceutical compounds
WO2011151461A2 (en) 2010-06-04 2011-12-08 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
ES2646834T3 (es) * 2010-08-20 2017-12-18 Amira Pharmaceuticals, Inc. Inhibidores de autotaxina y usos de los mismos
WO2012028243A1 (en) * 2010-09-02 2012-03-08 Merck Patent Gmbh Pyrazolopyridinone derivatives as lpa receptor antagonists
CA2818903C (en) 2010-12-14 2021-03-23 Electrophoretics Limited 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor
US9260416B2 (en) 2011-05-27 2016-02-16 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
EP2800745B1 (en) 2011-12-02 2020-02-12 Phenex Pharmaceuticals AG Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rory, 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
EA201492223A1 (ru) 2012-06-13 2015-03-31 Ф. Хоффманн-Ля Рош Аг Новые диазаспироциклоалканы и азаспироциклоалканы
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
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
NZ703852A (en) 2012-07-27 2018-03-23 Biogen Ma Inc Atx modulating agents
MX357035B (es) 2012-09-25 2018-06-25 Bayer Pharma AG Combinacion de regorafenib y acido acetilsalicilico para el tratamiento del cancer.
EP2900669B1 (en) 2012-09-25 2019-09-04 F.Hoffmann-La Roche Ag Hexahydropyrrolo[3,4-c]pyrrole derivatives and related compounds as autotaxin (atx) inhibitors and as inhibitors of the lysophosphatidic acid (lpa) production for treating e.g. renal diseases
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
ES2871821T3 (es) 2012-10-25 2021-11-02 Tetra Discovery Partners Llc Inhibidores de heteroarilo de PDE4
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
CN105209428A (zh) 2013-03-12 2015-12-30 奥克塞拉有限公司 用于治疗眼科疾病和病症的取代的3-苯基丙胺衍生物
CN105026403B (zh) 2013-03-12 2018-05-18 艾伯维公司 四环布罗莫结构域抑制剂
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
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
TW201446768A (zh) 2013-03-15 2014-12-16 Biogen Idec Inc S1p及/或atx調節劑
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
CA2930737C (en) 2013-11-22 2023-02-21 Pharmakea, Inc. Autotaxin inhibitor compounds
AR098475A1 (es) 2013-11-26 2016-06-01 Bayer Cropscience Ag Compuestos pesticidas y usos
KR20160087900A (ko) 2013-11-26 2016-07-22 에프. 호프만-라 로슈 아게 신규한 옥타하이드로-사이클로부타[1,2-c；3,4-c'']다이피롤-2-일
AU2015238666B2 (en) 2014-03-26 2018-11-15 Basf Se Substituted [1,2,4]triazole and imidazole compounds as fungicides
UA119347C2 (uk) 2014-03-26 2019-06-10 Ф. Хоффманн-Ля Рош Аг Конденсовані [1,4]діазепінові сполуки як інгібітори продукції аутотаксину (atх) та лізофосфатидилової кислоти (lpa)
CN106103446B (zh) 2014-03-26 2019-07-30 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)生产抑制剂的二环化合物
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
PE20170206A1 (es) 2014-04-04 2017-04-09 X-Rx Inc Inhibidores espirociclicos sustituidos de la autotaxina
UA118989C2 (uk) 2014-10-14 2019-04-10 Вітае Фармасьютікалс, Інк. Дигідропіролопіридинові інгібітори ror-гамма
JP6700291B2 (ja) 2015-02-15 2020-05-27 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ １−（ｈｅｔ）アリールスルホニル−（ピロリジン又はピペリジン）−２−カルボキサミド誘導体、及びｔｒｐａ１拮抗薬としてのそれらの使用
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
AU2016316717B2 (en) 2015-09-04 2021-02-18 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
TW201723176A (zh) 2015-09-24 2017-07-01 Ｉｏｎｉｓ製藥公司 Ｋｒａｓ表現之調節劑
WO2017050792A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
KR20180053408A (ko) 2015-09-24 2018-05-21 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서의 신규한 이환형 화합물
MX2018001430A (es) 2015-09-24 2018-04-20 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca).
EP3353180B1 (en) 2015-09-24 2022-03-16 F. Hoffmann-La Roche AG Bicyclic compounds as atx inhibitors
CR20180336A (es) 2015-11-25 2018-08-06 Dana Farber Cancer Inst Inc Inhibidores de bromodominio bivalentes y usos de los mismos
EP3385261A4 (en) 2015-12-01 2019-04-24 Nihon Nohyaku Co., Ltd. 3H-PYRROLOPYRIDINE COMPOUND OR ITS N-OXIDE, OR SALTS THEREOF, AGRICULTURAL INSECTICIDE AND HORTICULTURAL CONTAINING THE SAME, AND USE THEREOF
WO2017139978A1 (zh) 2016-02-19 2017-08-24 吴伟东 手机app更新方法及系统
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
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
NZ763766A (en) 2017-03-20 2023-07-28 Novo Nordisk Healthcare Ag Pyrrolopyrrole compositions as pyruvate kinase (pkr) activators

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