JP6845230B2 - デュアルatx/ca阻害剤としての新規な二環式化合物 - Google Patents
デュアルatx/ca阻害剤としての新規な二環式化合物 Download PDFInfo
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- JP6845230B2 JP6845230B2 JP2018515621A JP2018515621A JP6845230B2 JP 6845230 B2 JP6845230 B2 JP 6845230B2 JP 2018515621 A JP2018515621 A JP 2018515621A JP 2018515621 A JP2018515621 A JP 2018515621A JP 6845230 B2 JP6845230 B2 JP 6845230B2
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- Prior art keywords
- substituted
- alkyl
- alkoxy
- pyrrole
- trans
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Classifications
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Ophthalmology & Optometry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15186642.3 | 2015-09-24 | ||
| EP15186642 | 2015-09-24 | ||
| PCT/EP2016/072277 WO2017050747A1 (en) | 2015-09-24 | 2016-09-20 | New bicyclic compounds as dual atx/ca inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018528244A JP2018528244A (ja) | 2018-09-27 |
| JP2018528244A5 JP2018528244A5 (OSRAM) | 2019-10-24 |
| JP6845230B2 true JP6845230B2 (ja) | 2021-03-17 |
Family
ID=54199040
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018515621A Active JP6845230B2 (ja) | 2015-09-24 | 2016-09-20 | デュアルatx/ca阻害剤としての新規な二環式化合物 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US10738053B2 (OSRAM) |
| EP (1) | EP3353181B1 (OSRAM) |
| JP (1) | JP6845230B2 (OSRAM) |
| KR (1) | KR20180053408A (OSRAM) |
| CN (1) | CN107614505B (OSRAM) |
| AR (1) | AR106100A1 (OSRAM) |
| AU (1) | AU2016328365B2 (OSRAM) |
| BR (1) | BR112017026682A2 (OSRAM) |
| CA (1) | CA2984585A1 (OSRAM) |
| CL (1) | CL2018000649A1 (OSRAM) |
| CO (1) | CO2017011152A2 (OSRAM) |
| CR (1) | CR20180143A (OSRAM) |
| IL (1) | IL255511B (OSRAM) |
| MX (1) | MX2017015034A (OSRAM) |
| PE (1) | PE20180233A1 (OSRAM) |
| PH (1) | PH12018500409A1 (OSRAM) |
| RU (1) | RU2725138C2 (OSRAM) |
| TW (1) | TW201725206A (OSRAM) |
| WO (1) | WO2017050747A1 (OSRAM) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI633087B (zh) | 2012-06-13 | 2018-08-21 | 赫孚孟拉羅股份公司 | 新穎二氮雜螺環烷及氮雜螺環烷 |
| HRP20191937T1 (hr) | 2012-09-25 | 2020-01-10 | F. Hoffmann - La Roche Ag | Derivati heksahidropirolo [3,4-c]pirola i srodni spojevi kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za liječenje npr. bubrežnih bolesti |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| LT3074400T (lt) | 2013-11-26 | 2018-02-12 | F. Hoffmann-La Roche Ag | Oktahidro-ciklobuta [1,2-c;3,4-c`]dipirolo dariniai kaip autotaksino inhibitoriai |
| EA037928B1 (ru) | 2014-03-26 | 2021-06-08 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
| PE20161223A1 (es) | 2014-03-26 | 2016-11-12 | Hoffmann La Roche | Compuestos condensados de [1,4]diazepina como inhibidores de la produccion de autotaxina (atx) y acido lisofosfatidico (lpa) |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| MX377277B (es) | 2015-09-04 | 2025-03-07 | Hoffmann La Roche | Derivados de fenoximetilo. |
| CA2991615A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | Bicyclic compounds as atx inhibitors |
| AU2016328365B2 (en) | 2015-09-24 | 2020-04-23 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual ATX/CA inhibitors |
| EP3353178B1 (en) | 2015-09-24 | 2021-07-14 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
| AU2016328535A1 (en) | 2015-09-24 | 2017-11-09 | F. Hoffmann-La Roche Ag | Bicyclic compounds as ATX inhibitors |
| JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ.ホフマン-ラ ロシュ アーゲー | Atxインヒビターとしての新規二環式化合物 |
| BR112019019017A2 (pt) * | 2017-03-16 | 2020-04-14 | Hoffmann La Roche | compostos heterocíclicos de utilidade como inibidores duplos de atx/ca |
| CA3145960A1 (en) | 2019-07-22 | 2021-01-28 | Boehringer Ingelheim International Gmbh | N-methyl, n-(6-(methoxy)pyridazin-3-yl) amine derivatives as autotaxin (atx) modulators for the treatment of inflammatory airway or fibrotic diseases |
| WO2022149010A1 (en) | 2021-01-05 | 2022-07-14 | Cadila Healthcare Limited | Novel inhibitors of autotaxin |
Family Cites Families (140)
| 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 |
| PL342735A1 (en) | 1998-02-04 | 2001-07-02 | Banyu Pharma Co Ltd | N-acylic derivatives of acyclic amines |
| JP2001039950A (ja) | 1999-07-30 | 2001-02-13 | Banyu Pharmaceut Co Ltd | N−アシル環状アミン誘導体 |
| WO2001030780A2 (en) | 1999-10-27 | 2001-05-03 | Cor Therapeutics, Inc. | Pyridyl-containing spirocyclic compounds as inhibitors of fibrinogen-dependent platelet aggregation |
| WO2002070523A1 (en) | 2001-03-07 | 2002-09-12 | Pfizer Products Inc. | Modulators of chemokine receptor activity |
| EP1499306A4 (en) | 2002-04-12 | 2007-03-28 | Merck & Co Inc | BICYCLIC AMIDE |
| 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 |
| CA2558211C (en) | 2004-03-03 | 2013-09-03 | Chemocentryx, Inc. | Bicyclic and bridged nitrogen heterocycles |
| RU2006146608A (ru) | 2004-06-09 | 2008-07-20 | Ф.Хоффманн-Ля Рош Аг (Ch) | ОКТАГИДРОПИРРОЛО[3,4-с]-ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПРОТИВОВИРУСНЫХ АГЕНТОВ |
| ES2442857T3 (es) | 2004-08-10 | 2014-02-13 | Janssen Pharmaceutica Nv | Derivados de 1,2,4-triazin-6-ona inhibidores de VIH |
| 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 |
| CN101166736B (zh) | 2005-04-28 | 2013-02-06 | 惠氏公司 | 他那普戈特的多晶型ⅱ |
| 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 |
| WO2007049771A1 (ja) | 2005-10-28 | 2007-05-03 | Ono Pharmaceutical Co., Ltd. | 塩基性基を含有する化合物およびその用途 |
| WO2007058322A1 (ja) | 2005-11-18 | 2007-05-24 | Ono Pharmaceutical Co., Ltd. | 塩基性基を含有する化合物およびその用途 |
| 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 |
| 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 |
| JP2008001743A (ja) | 2006-06-20 | 2008-01-10 | Bridgestone Corp | トレッド用ゴム組成物及びそれを用いたタイヤ |
| 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 |
| CA2663500A1 (en) | 2006-09-15 | 2008-03-20 | Schering Corporation | Spiro-condensed azetidine derivatives useful in treating pain, diabetes and disorders of lipid metabolism |
| 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 |
| 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 |
| CA2682637A1 (en) | 2007-03-29 | 2008-10-09 | F. Hoffmann-La 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. |
| JP2010524987A (ja) | 2007-04-27 | 2010-07-22 | サノフィ−アベンティス | 2−ヘテロアリール−ピロロ[3,4−c]ピロール誘導体及びscd阻害剤としてのそれらの使用 |
| BRPI0812853A2 (pt) | 2007-08-07 | 2014-12-23 | Abbott Gmbh | Compostos de quinolina adequados para tratar distúrbios que respondem à modulação do receptor 5-ht6 de serotonina. |
| 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 |
| CA2727914A1 (en) | 2008-06-19 | 2009-12-23 | Banyu Pharmaceutical Co., Ltd. | Spirodiamine-diaryl ketoxime derivative technical field |
| EP2328898B1 (de) * | 2008-09-09 | 2014-12-24 | Sanofi | 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 |
| EP2358677B1 (en) | 2008-11-17 | 2014-01-08 | 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 |
| CA2745041C (en) | 2008-12-01 | 2017-08-22 | Kai Schiemann | 2, 5-diamino-substituted pyrido [4, 3-d] pyrimidines as autotaxin inhibitors against cancer |
| TW201035102A (en) | 2009-03-04 | 2010-10-01 | Gruenethal Gmbh | Sulfonylated tetrahydroazolopyrazines and their use as medicinal products |
| CA2754446A1 (en) | 2009-03-05 | 2010-09-10 | Daiichi Sankyo Company, Limited | Pyridine derivative |
| 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 |
| KR20120027177A (ko) | 2009-04-02 | 2012-03-21 | 메르크 파텐트 게엠베하 | 오토탁신 저해제로서의 피페리딘 및 피라진 유도체 |
| AU2010230646B2 (en) | 2009-04-02 | 2015-11-26 | Merck Patent Gmbh | Heterocyclic compounds as autotaxin inhibitors |
| EA201101396A1 (ru) | 2009-04-02 | 2012-09-28 | Мерк Патент Гмбх | Ингибиторы аутотаксина |
| FR2945534B1 (fr) | 2009-05-12 | 2012-11-16 | Sanofi Aventis | DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| US8648066B2 (en) | 2009-05-22 | 2014-02-11 | Exelixis, Inc. | Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture |
| 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 |
| JP2013501064A (ja) | 2009-08-04 | 2013-01-10 | 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 | リゾホスファチジン酸受容体アンタゴニストとしての化合物 |
| 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 |
| MX2012007935A (es) | 2010-01-07 | 2012-08-15 | Du Pont | Compuestos heterociclicos fungicidas. |
| WO2011115813A1 (en) | 2010-03-18 | 2011-09-22 | Abbott Laboratories | Lactam acetamides as calcium channel blockers |
| HUE025774T2 (en) | 2010-03-19 | 2016-05-30 | Pfizer | 2,3 dihydro-1h-inden-1-yl-2,7-diazaspiro[3.6]nonane derivatives and their use as antagonists or inverse agonists of the ghrelin receptor |
| 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 |
| 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 |
| US9000025B2 (en) | 2010-08-20 | 2015-04-07 | Amira Pharmaceuticals, Inc. | Autotaxin inhibitors and uses thereof |
| US8859775B2 (en) | 2010-09-02 | 2014-10-14 | Merck Patent Gmbh | Pyrazolopyridinone derivatives as LPA receptor antagonists |
| US8999985B2 (en) | 2010-12-02 | 2015-04-07 | Shanghai De Novo Pharmatech Co Ltd. | Substituted phthalazin-1(2H)-ones, preparation processes and medical uses thereof |
| JP5937102B2 (ja) | 2010-12-14 | 2016-06-22 | エレクトロフォレティクス リミテッド | カゼインキナーゼ1デルタ(ck1デルタ)阻害剤 |
| WO2012166415A1 (en) | 2011-05-27 | 2012-12-06 | Amira Pharmaceuticals, Inc. | Heterocyclic autotaxin inhibitors and uses thereof |
| US8664213B2 (en) | 2011-08-29 | 2014-03-04 | 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 |
| US9815851B2 (en) | 2011-12-02 | 2017-11-14 | Phenex Pharmaceuticals Ag | Pyrrolo carboxamides as modulators of orphan nuclear receptor RAR-related orphan receptor-gamma (RORγ, 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 |
| ES2984771T3 (es) | 2012-06-13 | 2024-10-31 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| TWI633087B (zh) | 2012-06-13 | 2018-08-21 | 赫孚孟拉羅股份公司 | 新穎二氮雜螺環烷及氮雜螺環烷 |
| RU2665462C2 (ru) | 2012-06-27 | 2018-08-30 | Ф. Хоффманн-Ля Рош Аг | Соединения 5-азаиндазола и способы их применения |
| 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 |
| EP2877166B1 (en) | 2012-07-27 | 2018-02-28 | Biogen MA Inc. | 1-[7-(cis-4-methyl-cyclohexyloxy)-8-trifluoromethyl-naphthalen-2-ylmethyl]-piperidine-4-carboxylic acid derivatives as autotaxin (ATX) modulators for treating inflammations and autoimmune disorders |
| AR092211A1 (es) * | 2012-09-24 | 2015-04-08 | Merck Patent Ges Mit Beschränkter Haftung | Derivados de hidropirrolopirrol |
| HRP20191937T1 (hr) | 2012-09-25 | 2020-01-10 | F. Hoffmann - La Roche Ag | Derivati heksahidropirolo [3,4-c]pirola i srodni spojevi kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za liječenje npr. bubrežnih bolesti |
| RS57875B1 (sr) | 2012-09-25 | 2018-12-31 | Bayer Pharma AG | Kombinacija regorafeniba i acetilsalicilne kiseline za lečenje kolorektalnog kancera |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| DK2912019T3 (da) | 2012-10-25 | 2021-05-25 | Tetra Discovery Partners Llc | Heteroarylhæmmere af pde4 |
| AU2013368842B2 (en) | 2012-12-31 | 2015-11-12 | Cadila Healthcare Limited | Substituted phthalazin-1 (2H)-one derivatives as selective inhibitors of poly (ADP-ribose) polymerase-1 |
| US20160002247A1 (en) | 2013-03-01 | 2016-01-07 | The University Of Tokyo | 8-substituted imidazopyrimidinone derivative having autotaxin inhibitory activity |
| HK1219943A1 (zh) | 2013-03-12 | 2017-04-21 | Acucela, Inc. | 用於治疗眼科疾病和障害的取代3-苯基丙胺衍生物 |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| JP6419735B2 (ja) | 2013-03-12 | 2018-11-07 | アッヴィ・インコーポレイテッド | 四環系ブロモドメイン阻害剤 |
| 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 |
| WO2014152725A1 (en) | 2013-03-15 | 2014-09-25 | Biogen Idec Ma Inc. | S1p and/or atx modulating agents |
| EP2991994B1 (en) | 2013-05-01 | 2018-08-15 | Vitae Pharmaceuticals, Inc. | Thiazolopyrrolidine inhibitors of ror-gamma |
| KR20160033726A (ko) | 2013-07-18 | 2016-03-28 | 노파르티스 아게 | 헤테로방향족 고리-벤질-아미드-사이클 코어를 포함하는 오토탁신 억제제 |
| CN105636958B (zh) | 2013-10-17 | 2018-01-05 | 沃泰克斯药物股份有限公司 | Dna‑pk抑制剂 |
| HRP20210957T1 (hr) | 2013-11-22 | 2021-09-17 | Sabre Therapeutics Llc | Spojevi inhibitori autotaksina |
| AR098475A1 (es) | 2013-11-26 | 2016-06-01 | Bayer Cropscience Ag | Compuestos pesticidas y usos |
| LT3074400T (lt) | 2013-11-26 | 2018-02-12 | F. Hoffmann-La Roche Ag | Oktahidro-ciklobuta [1,2-c;3,4-c`]dipirolo dariniai kaip autotaksino inhibitoriai |
| EA201691913A1 (ru) | 2014-03-26 | 2017-02-28 | Басф Се | Замещенные [1,2,4]триазольные и имидазольные соединения в качестве фунгицидов |
| PE20161223A1 (es) | 2014-03-26 | 2016-11-12 | Hoffmann La Roche | Compuestos condensados de [1,4]diazepina como inhibidores de la produccion de autotaxina (atx) y acido lisofosfatidico (lpa) |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| EA037928B1 (ru) * | 2014-03-26 | 2021-06-08 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
| SG11201607920RA (en) | 2014-04-04 | 2016-10-28 | X Rx Inc | Substituted spirocyclic inhibitors of autotaxin |
| WO2016031987A1 (ja) | 2014-08-29 | 2016-03-03 | 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ピリミジノン誘導体 |
| SI3207043T1 (sl) | 2014-10-14 | 2019-04-30 | Vitae Pharmaceuticals, Inc. | Dihidropirolopiridinovi inhibitorji za ROR-gama |
| BR112017017052A2 (pt) | 2015-02-15 | 2018-04-10 | F. Hoffmann-La Roche Ag | derivados de 1-(het)arilsulfonil-(pirrolidina ou piperidina)-2-carboxamida e seu 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 |
| MX377277B (es) | 2015-09-04 | 2025-03-07 | Hoffmann La Roche | Derivados de fenoximetilo. |
| PL415078A1 (pl) | 2015-09-04 | 2017-03-13 | Oncoarendi Therapeutics Spółka Z Ograniczoną Odpowiedzialnością | Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków |
| EP3353178B1 (en) * | 2015-09-24 | 2021-07-14 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
| EP3353328A4 (en) | 2015-09-24 | 2019-06-12 | Ionis Pharmaceuticals, Inc. | MODULATORS OF KRAS EXPRESSION |
| AU2016328365B2 (en) | 2015-09-24 | 2020-04-23 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual ATX/CA inhibitors |
| CA2991615A1 (en) * | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | Bicyclic compounds as atx inhibitors |
| AU2016328535A1 (en) * | 2015-09-24 | 2017-11-09 | F. Hoffmann-La Roche Ag | Bicyclic compounds as ATX inhibitors |
| WO2017087863A1 (en) * | 2015-11-20 | 2017-05-26 | 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 |
| AU2016362040B2 (en) | 2015-12-01 | 2019-10-10 | Nihon Nohyaku Co., Ltd. | 3H-pyrrolopyridine compound, N-oxide thereof or salt thereof, agricultural and horticultural insecticide comprising the compound and method for using the same |
| WO2017139978A1 (zh) | 2016-02-19 | 2017-08-24 | 吴伟东 | 手机app更新方法及系统 |
| JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ.ホフマン-ラ ロシュ アーゲー | Atxインヒビターとしての新規二環式化合物 |
| BR112019019017A2 (pt) | 2017-03-16 | 2020-04-14 | Hoffmann La Roche | compostos heterocíclicos de utilidade como inibidores duplos de atx/ca |
| US11014927B2 (en) | 2017-03-20 | 2021-05-25 | Forma Therapeutics, Inc. | Pyrrolopyrrole compositions as pyruvate kinase (PKR) activators |
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| CN107614505B (zh) | 2021-05-07 |
| US20200291038A1 (en) | 2020-09-17 |
| KR20180053408A (ko) | 2018-05-21 |
| US10889588B2 (en) | 2021-01-12 |
| CA2984585A1 (en) | 2017-03-30 |
| EP3353181A1 (en) | 2018-08-01 |
| WO2017050747A1 (en) | 2017-03-30 |
| RU2725138C2 (ru) | 2020-06-30 |
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| CL2018000649A1 (es) | 2018-08-17 |
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