PE20191757A1 - Compuestos heterociclicos utiles como inhibidores dobles de atx/ca - Google Patents

Compuestos heterociclicos utiles como inhibidores dobles de atx/ca

Info

Publication number
PE20191757A1
PE20191757A1 PE2019001583A PE2019001583A PE20191757A1 PE 20191757 A1 PE20191757 A1 PE 20191757A1 PE 2019001583 A PE2019001583 A PE 2019001583A PE 2019001583 A PE2019001583 A PE 2019001583A PE 20191757 A1 PE20191757 A1 PE 20191757A1
Authority
PE
Peru
Prior art keywords
substituted
methyl
atx
inhibitors
helpful
Prior art date
Application number
PE2019001583A
Other languages
English (en)
Inventor
Patrizio Mattei
Jerôme Hert
Daniel Hunziker
Markus Rudolph
Petra Schmitz
Giorgio Patrick Di
Justin Gomme
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 PE20191757A1 publication Critical patent/PE20191757A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/10—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 linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

Referido a un compuesto de formula (I), en donde R1 se selecciona de i) fenilo sustituido con R3, R4 y R5, ii) piridinilo sustituido con R3, R4 y R5, y iii) tiofenilo sustituido con R3, R4 y R5; X se selecciona de i) N, y ii) CH; Y se selecciona de i) -CH2-OC(O)-, ii) -(CH2)qC(O)-, entre otros; W se selecciona de i) -(CR9R10)p-, ii) -(CR9R10)p-C(O), entre otros; R2 se selecciona de i) fenilo sustituido, ii) piridinilo sustituido, entre otros. Son compuestos preferidos: 2-((5-metil-2H-tetrazol-2-il) metil)-4-(trifluorometil) bencil 4-(2-fluoro-4-sulfamoilfenil)piperazina-1-carboxilato; [2-ciclopropil-6- (oxan-4-ilmetoxi)piridin-4-il]metil 4-[(4-sulfamoilfenil)metil]piperidin-1-carboxilato; entre otros. Dichos compuestos son inhibidores de ATX/CA (autotaxina/anhidrasa carbonica) siendo utiles en el tratamiento o la profilaxis de afecciones oculares. Tambien se refiere a una composicion farmaceutica que comprende dicho compuesto.
PE2019001583A 2017-03-16 2018-03-13 Compuestos heterociclicos utiles como inhibidores dobles de atx/ca PE20191757A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP17161249 2017-03-16
PCT/EP2018/056140 WO2018167001A1 (en) 2017-03-16 2018-03-13 Heterocyclic compounds useful as dual atx/ca inhibitors

Publications (1)

Publication Number Publication Date
PE20191757A1 true PE20191757A1 (es) 2019-12-12

Family

ID=58347248

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2019001583A PE20191757A1 (es) 2017-03-16 2018-03-13 Compuestos heterociclicos utiles como inhibidores dobles de atx/ca

Country Status (21)

Country Link
US (1) US11059794B2 (es)
EP (1) EP3596059B1 (es)
JP (1) JP7157755B2 (es)
KR (1) KR20190129924A (es)
CN (1) CN110392679B (es)
AR (1) AR111279A1 (es)
AU (1) AU2018233079B9 (es)
BR (1) BR112019019017A2 (es)
CA (1) CA3053329A1 (es)
CL (1) CL2019002609A1 (es)
CO (1) CO2019009373A2 (es)
CR (1) CR20190423A (es)
IL (1) IL269188B (es)
MA (1) MA49879A (es)
MX (1) MX2019010772A (es)
PE (1) PE20191757A1 (es)
PH (1) PH12019502118A1 (es)
RU (1) RU2019132254A (es)
SG (1) SG11201908560SA (es)
TW (1) TW201838982A (es)
WO (1) WO2018167001A1 (es)

Families Citing this family (17)

* 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
AU2013322838B2 (en) 2012-09-25 2018-02-01 F. Hoffmann-La Roche Ag New bicyclic derivatives
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
UA118201C2 (uk) 2013-11-26 2018-12-10 Ф. Хоффманн-Ля Рош Аг НОВИЙ ОКТАГІДРОЦИКЛОБУТА[1,2-c;3,4-c']ДИПІРОЛ-2-ІЛ
EA032357B1 (ru) 2014-03-26 2019-05-31 Ф. Хоффманн-Ля Рош Аг Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
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)
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
MX2020004504A (es) 2015-09-04 2021-11-10 Hoffmann La Roche Derivados de fenoximetilo.
PE20180552A1 (es) 2015-09-24 2018-04-02 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca
MA42919A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
EP3353181B1 (en) 2015-09-24 2021-08-11 F. Hoffmann-La Roche AG Bicyclic compounds as dual atx/ca inhibitors
MA42918A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
EP3596060B1 (en) 2017-03-16 2023-09-20 F. Hoffmann-La Roche AG New bicyclic compounds as atx inhibitors
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
US20210363152A1 (en) * 2018-12-11 2021-11-25 Hoffmann-La Roche Inc. Aminoazine amides
WO2020119896A1 (en) * 2018-12-11 2020-06-18 F. Hoffmann-La Roche Ag Heterocyclic inhibitors of atx
CN110746450A (zh) * 2019-09-17 2020-02-04 济南康和医药科技有限公司 一种贝前列素钠关键中间体的合成方法

Family Cites Families (141)

* 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
WO2001030780A2 (en) 1999-10-27 2001-05-03 Cor Therapeutics, Inc. Pyridyl-containing spirocyclic compounds as inhibitors of fibrinogen-dependent platelet aggregation
AU1400401A (en) 1999-11-09 2001-06-06 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Product inhibiting transduction of G heterotrimeric protein signals combined with another anti-cancer agent for therapeutic use in cancer treatment
MXPA03008109A (es) 2001-03-07 2003-12-12 Pfizer Prod Inc Moduladores de la actividad de receptores de quimiocinas.
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
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
WO2005121145A2 (en) 2004-06-09 2005-12-22 F. Hoffmann-La Roche Ag Octahydro-pyrrolo[3,4-c] derivatives and their use as antiviral compounds
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
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
EP2657235A1 (en) 2005-10-28 2013-10-30 Ono Pharmaceutical Co., Ltd. Compound containing basic group and use thereof
ES2407115T3 (es) 2005-11-18 2013-06-11 Ono Pharmaceutical Co., Ltd. Compuesto que contiene un grupo básico y uso del mismo
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
CA2663161C (en) 2006-09-11 2014-10-28 N.V. Organon Quinazolinone and isoquinolinone acetamide derivatives
JP2010503675A (ja) 2006-09-15 2010-02-04 シェーリング コーポレイション 疼痛、糖尿病および脂質代謝の障害の治療に有用なスピロ縮合アゼチジン誘導体
US8735411B2 (en) 2006-10-02 2014-05-27 Abbvie Inc. Macrocyclic benzofused pyrimidine derivatives
TWI454262B (zh) 2006-11-02 2014-10-01 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
WO2008059026A1 (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
JP2010522706A (ja) 2007-03-29 2010-07-08 エフ．ホフマン−ラ ロシュ アーゲー 非ヌクレオシド逆転写酵素阻害剤
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.
BRPI0810858A2 (pt) 2007-04-27 2014-10-29 Sanofi Aventis Derivados de 2-heteroaril-pirrolo[3,4-c] pirrol e seus usos como inibidores de scd
RU2483068C2 (ru) 2007-08-07 2013-05-27 Эбботт Гмбх Унд Ко.Кг Соединения хинолина, пригодные для лечения нарушений, являющихся ответом на модуляцию рецептора 5-ht6 серотонина
DE102007047737A1 (de) 2007-10-05 2009-04-30 Merck Patent Gmbh Piperidin- und Piperazinderivate
MX2010004281A (es) 2007-10-19 2010-09-10 Sarcode Corp Composiciones y metodos para el tratamiento de la retinopatia diabetica.
US7935725B2 (en) 2007-10-31 2011-05-03 Janssen Pharmaceutica Nv Aryl-substituted bridged or fused diamines as modulators of leukotriene A4 hydrolase
DE102007054156A1 (de) 2007-11-12 2009-05-14 Ventech Gmbh Verfahren zum Feststellen des Druckes und der Profiltiefe bei einem Fahrzeugreifen
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
AU2009261248A1 (en) 2008-06-19 2009-12-23 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
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
JP5697601B2 (ja) 2008-12-01 2015-04-08 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ 癌に対するオータキシン阻害剤としての２，５−ジアミノ−置換ピリド［４，３−ｄ］ピリミジン
TW201035102A (en) 2009-03-04 2010-10-01 Gruenethal Gmbh Sulfonylated tetrahydroazolopyrazines and their use as medicinal products
EP2404918B1 (en) 2009-03-05 2016-11-30 Daiichi Sankyo Company, Limited Pyridine derivative as ppary inhibitor
US20120010186A1 (en) 2009-03-23 2012-01-12 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
ES2527788T3 (es) 2009-04-02 2015-01-30 Merck Patent Gmbh Compuestos heterocíclicos como inhibidores de autotaxina
WO2010112124A1 (en) 2009-04-02 2010-10-07 Merck Patent Gmbh Autotaxin inhibitors
ES2422718T3 (es) 2009-04-02 2013-09-13 Merck Patent Gmbh Derivados de piperidina y piperazina como inhibidores de la autotaxina
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
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
WO2011017350A2 (en) 2009-08-04 2011-02-10 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
ES2534516T3 (es) 2010-01-07 2015-04-23 E.I. Du Pont De Nemours And Company Compuestos heterocíclicos fungicidas
US8815869B2 (en) 2010-03-18 2014-08-26 Abbvie Inc. Lactam acetamides as calcium channel blockers
DK2547679T3 (en) 2010-03-19 2016-01-11 Pfizer 2,3 dihydro-1H-inden-1-yl-2,7-diazaspiro [3.6] nonane derivatives and their use as antagonists or inverse agonists of ghrelin receptor
ES2562183T3 (es) 2010-03-26 2016-03-02 Merck Patent Gmbh Benzonaftiridinaminas como inhibidores de la autotaxina
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
CN103189378B (zh) 2010-09-02 2016-03-02 默克专利股份公司 作为lpa受体拮抗剂的吡唑并吡啶酮衍生物
EP2646428B1 (en) 2010-12-02 2016-06-01 Shanghai De Novo Pharmatech Co Ltd. Heterocyclic derivatives, preparation processes and medical uses thereof
DK2835131T3 (en) 2010-12-14 2017-12-04 Electrophoretics Ltd Casein kinase 1 delta inhibitors (CK1 delta)
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
ME03300B (me) 2012-06-13 2019-07-20 Incyte Holdings Corp Supsтituisana triciklična jedinjenja као inhibiтori fgfr
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
ES2671194T3 (es) 2012-07-27 2018-06-05 Biogen Ma Inc. Compuestos que son agentes moduladores de S1P y/o agentes moduladores de ATX
US9522889B2 (en) 2012-07-27 2016-12-20 Biogen Ma Inc. ATX modulating agents
AR092211A1 (es) 2012-09-24 2015-04-08 Merck Patent Ges Mit Beschränkter Haftung Derivados de hidropirrolopirrol
AU2013322838B2 (en) 2012-09-25 2018-02-01 F. Hoffmann-La Roche Ag New bicyclic derivatives
DK2900269T3 (en) 2012-09-25 2018-10-01 Bayer Pharma AG COMBINATION OF REGORAFENIB AND ACETYLSALICYLIC ACID FOR TREATMENT OF COLORECTAL CANCER.
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
PT2938598T (pt) 2012-12-31 2017-02-07 Cadila Healthcare Ltd Derivados de ftalazin-1-(2h)-ona substituídos como inibidores seletivos da poli (adp-ribose) polimerase-1
US20160002247A1 (en) 2013-03-01 2016-01-07 The University Of Tokyo 8-substituted imidazopyrimidinone derivative having autotaxin inhibitory activity
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
KR102224992B1 (ko) 2013-03-12 2021-03-10 애브비 인코포레이티드 테트라사이클릭 브로모도메인 억제제
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
EP2970099A4 (en) 2013-03-12 2016-12-21 Acucela Inc SUBSTITUTED 3-PHENYLPROPYLAMINE DERIVATIVES FOR THE TREATMENT OF EYE DISEASES AND DRESSES
EP2970302A1 (en) 2013-03-15 2016-01-20 Biogen MA Inc. S1p and/or atx modulating agents
WO2014179564A1 (en) 2013-05-01 2014-11-06 Vitae Pharmaceuticals, Inc. Thiazalopyrrolidine inhibitors of ror-gamma
AU2014291711B2 (en) 2013-07-18 2017-02-02 Novartis Ag Autotaxin inhibitors comprising a heteroaromatic ring-benzyl-amide-cycle core
PL3057959T3 (pl) 2013-10-17 2018-08-31 Vertex Pharmaceuticals Incorporated Inhibitory DNA-PK
MX2016006623A (es) 2013-11-22 2017-03-10 Pharmakea Inc Compuestos de inhibidor de autotaxina.
AR098475A1 (es) 2013-11-26 2016-06-01 Bayer Cropscience Ag Compuestos pesticidas y usos
UA118201C2 (uk) 2013-11-26 2018-12-10 Ф. Хоффманн-Ля Рош Аг НОВИЙ ОКТАГІДРОЦИКЛОБУТА[1,2-c;3,4-c']ДИПІРОЛ-2-ІЛ
EA032357B1 (ru) 2014-03-26 2019-05-31 Ф. Хоффманн-Ля Рош Аг Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
AU2015238666B2 (en) 2014-03-26 2018-11-15 Basf Se Substituted [1,2,4]triazole and imidazole compounds as fungicides
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)
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
CN107106559A (zh) 2014-04-04 2017-08-29 X-Rx股份有限公司 自分泌运动因子的取代的螺环抑制剂
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
JP6564029B2 (ja) 2014-10-14 2019-08-21 ヴァイティー ファーマシューティカルズ，エルエルシー Ｒｏｒ−ガンマのジヒドロピロロピリジン阻害剤
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
WO2016181408A2 (en) 2015-05-11 2016-11-17 Cadila Healthcare Limited NOVEL SHORT-CHAIN PEPTIDES AS KAPPA (κ) OPIOID RECEPTORS (KOR) AGONIST
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
MX2020004504A (es) 2015-09-04 2021-11-10 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
MA42918A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
MA42919A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
US20180273577A1 (en) 2015-09-24 2018-09-27 Ionis Pharmaceuticals, Inc. Modulators of kras expression
PE20180552A1 (es) 2015-09-24 2018-04-02 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca
EP3353181B1 (en) 2015-09-24 2021-08-11 F. Hoffmann-La Roche AG Bicyclic compounds as dual atx/ca inhibitors
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
MX2018006499A (es) 2015-11-25 2018-08-01 Dana Farber Cancer Inst Inc Inhibidores de bromodominio bivalentes y usos de los mismos.
CN108290858B (zh) 2015-12-01 2021-07-06 日本农药株式会社 3h-吡咯并吡啶化合物或其n-氧化物、或它们的盐类及含有该化合物的农业园艺用杀虫剂及其使用方法
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
EP3596060B1 (en) 2017-03-16 2023-09-20 F. Hoffmann-La Roche AG New bicyclic compounds as atx inhibitors
MD3448859T2 (ro) 2017-03-20 2020-03-31 Forma Therapeutics Inc Compoziții de pirolopirol în calitate de activatori ai piruvatkinazei (PKR)

Also Published As

Publication number Publication date
IL269188A (en) 2019-11-28
AR111279A1 (es) 2019-06-26
US11059794B2 (en) 2021-07-13
AU2018233079B9 (en) 2021-07-22
BR112019019017A2 (pt) 2020-04-14
AU2018233079B2 (en) 2021-06-24
KR20190129924A (ko) 2019-11-20
AU2018233079A1 (en) 2019-08-29
RU2019132254A3 (es) 2021-06-04
IL269188B (en) 2021-12-01
CO2019009373A2 (es) 2019-09-09
SG11201908560SA (en) 2019-10-30
CR20190423A (es) 2019-11-01
WO2018167001A1 (en) 2018-09-20
CA3053329A1 (en) 2018-09-20
CN110392679A (zh) 2019-10-29
MA49879A (fr) 2020-06-24
MX2019010772A (es) 2019-12-16
RU2019132254A (ru) 2021-04-16
EP3596059C0 (en) 2024-04-24
EP3596059B1 (en) 2024-04-24
TW201838982A (zh) 2018-11-01
JP2020514355A (ja) 2020-05-21
PH12019502118A1 (en) 2020-07-06
CL2019002609A1 (es) 2020-02-14
JP7157755B2 (ja) 2022-10-20
US20200002297A1 (en) 2020-01-02
CN110392679B (zh) 2023-04-07
EP3596059A1 (en) 2020-01-22

Similar Documents

Publication Publication Date Title
PE20191757A1 (es) Compuestos heterociclicos utiles como inhibidores dobles de atx/ca
PE20141681A1 (es) Inhibidores de btk
PE20120321A1 (es) Indazoles sustituidos con oxazol como inhibidores de pi3-quinasa
PE20131377A1 (es) Triazina-oxadiazoles
PE20190913A1 (es) Derivados aromaticos de sulfonamida
PE20090717A1 (es) Derivados de quinolina como inhibidores de la pi3 quinasa
PE20090974A1 (es) Mezclas fungicidas
PE20180227A1 (es) Benzamidas sustituidas con 1,3-tiazol-2-ilo
PE20180177A1 (es) Derivados de 1-(het) arilsulfonil-(pirrolidin o piperidin)-2-carboxamida y su uso como antagonistas de trpa1
PE20081532A1 (es) Compuestos novedosos
PE20131153A1 (es) Inhibidores de la tirosina-quinasa de bruton
PE20110136A1 (es) Compuestos organicos
PE20141361A1 (es) Compuesto heterociclico dihidroxi aromatico
PE20061436A1 (es) Derivados de amida sustituida como inhibidores de proteina quinasa
PE20161400A1 (es) Derivados de isoindolin-1-ona con actividad positiva del modulador alosterico del receptor colinergico muscarinico m1 para el tratamiento de la enfermedad de alzheimer
PE20161225A1 (es) 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer
PE20142099A1 (es) Derivados de sulfonamida
PE20121510A1 (es) Isoquinolinonas y quinazolinonas sustituidas
PE20110298A1 (es) Derivados de picolinamida como inhibidores de cinasa
PE20081845A1 (es) Nuevos derivados de aminopirimidina como inhibidores de plk1
PE20120690A1 (es) Derivados de 5-fluoropirimidinona
AR055563A1 (es) Compuestos de piridil acido acetico, agente farmaceutico y utilizacion del compuesto para preparar dicho agente
PE20130382A1 (es) Derivados de n-(imidazopirimidin-7-il)-heteroarilamida y su uso como inhibidores de pde10a
PE20110906A1 (es) Compuestos de arilo con sustituyentes heterociclicos como inhibidores hif
PE20141120A1 (es) Compuestos heterociclicos