PE20170206A1 - Inhibidores espirociclicos sustituidos de la autotaxina - Google Patents

Inhibidores espirociclicos sustituidos de la autotaxina

Info

Publication number
PE20170206A1
PE20170206A1 PE2016001885A PE2016001885A PE20170206A1 PE 20170206 A1 PE20170206 A1 PE 20170206A1 PE 2016001885 A PE2016001885 A PE 2016001885A PE 2016001885 A PE2016001885 A PE 2016001885A PE 20170206 A1 PE20170206 A1 PE 20170206A1
Authority
PE
Peru
Prior art keywords
alkyl
methyl
autotaxin
substitute
oxobutan
Prior art date
Application number
PE2016001885A
Other languages
English (en)
Inventor
Zhifeng Xie
Ce Wang
Frank Ruebsam
Louis Renzetti
Mark J Mulvihill
Anthony D Keefe
Matthew Clark
Lee Babiss
Ying Zhang
Haihong Ni
Original Assignee
X-Rx Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by X-Rx Inc filed Critical X-Rx Inc
Publication of PE20170206A1 publication Critical patent/PE20170206A1/es

Links

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
    • C07D471/10—Spiro-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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring 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
    • A61K31/69—Boron compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se refiere a inhibidores espirociclicos de formula (I) en donde X1 y X2 son alquilo C1-C2, C=O, entre otros; X3 es alquilo C1-C2, O, entre otros; m y n son 0, 1 o 2; R1, R2 y R2a son alquilo C0-C12, cicloalquilo C3-C12-alquilo C0-C12-, entre otros cada uno opcionalmente sustituido; R4 es alquilo C0-C12, heterocicloalquilo C3-C12- alquilo C0-C12-, entre otros, opcionalmente sustituido. Son compuestos preferidos: (R)-3-Fluoro-N-(3-metil-1-(3-metil-2,4-dioxo-1-fenil-1,3,8-triazaespiro[4.5]decan-8-il)-1-oxobutan-2-il)benzamida; (R)-2-Fluoro-3-metil-N-(3-metil-1-(3-metil-2,4-dioxo-1-fenil-1,3,8-triazaespiro[4.5]decan-8-il)-1-oxobutan-2-il)benzamida; entre otros. Tambien se refiere a una composicion. Dichos compuestos inhiben la actividad de la autotaxina (ATX) modulando el nivel del acido lisofosfatidico (LPA) y la senalizacion asociada siendo utiles como agentes de tratamiento o profilaxis de enfermedades como cancer, inflamacion cronica, dolor neuropatico, entre otros
PE2016001885A 2014-04-04 2015-04-03 Inhibidores espirociclicos sustituidos de la autotaxina PE20170206A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201461975123P 2014-04-04 2014-04-04

Publications (1)

Publication Number Publication Date
PE20170206A1 true PE20170206A1 (es) 2017-04-09

Family

ID=54241341

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001885A PE20170206A1 (es) 2014-04-04 2015-04-03 Inhibidores espirociclicos sustituidos de la autotaxina

Country Status (21)

Country Link
US (3) US10011601B2 (es)
EP (1) EP3125895A4 (es)
JP (2) JP6616821B2 (es)
KR (1) KR20160133004A (es)
CN (1) CN107106559A (es)
AP (1) AP2016009496A0 (es)
AU (2) AU2015240519B2 (es)
CA (1) CA2943874A1 (es)
CL (1) CL2016002516A1 (es)
CR (1) CR20160496A (es)
CU (1) CU24442B1 (es)
DO (1) DOP2016000270A (es)
EA (1) EA201691840A1 (es)
EC (1) ECSP16084293A (es)
IL (1) IL248050A0 (es)
MD (1) MD20160116A2 (es)
MX (1) MX2016013049A (es)
PE (1) PE20170206A1 (es)
PH (1) PH12016501922A1 (es)
SG (1) SG11201607920RA (es)
WO (1) WO2015154023A1 (es)

Families Citing this family (26)

* 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
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
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)
PE20170206A1 (es) 2014-04-04 2017-04-09 X-Rx Inc Inhibidores espirociclicos sustituidos de la autotaxina
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
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
EP3423057A1 (en) 2016-03-04 2019-01-09 Gilead Sciences, Inc. Compositions and combinations of autotaxin inhibitors
JOP20190107A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
CN108456208B (zh) * 2017-02-22 2021-04-16 广州市恒诺康医药科技有限公司 氮杂螺环类化合物及其制备方法和应用
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
US10961242B2 (en) 2017-05-17 2021-03-30 Legochem Biosciences, Inc. Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same
KR101798840B1 (ko) 2017-05-17 2017-11-17 주식회사 레고켐 바이오사이언스 신규 오토탁신 저해 화합물 및 이를 함유하는 약제학적 조성물
BR112020005720A2 (pt) * 2017-09-29 2020-10-20 Takeda Pharmaceutical Company Limited composto ou sal, medicamento, métodos para inibir monoacilglicerol lipase e para a profilaxia ou o tratamento de doença de alzheimer, doença de parkinson, doença de huntington, esclerose lateral amiotrófica, esclerose múltipla, distúrbio de ansiedade, dor, epilepsia ou depressão, e, uso do composto ou sal.
WO2020051230A1 (en) * 2018-09-04 2020-03-12 X-Rx, Inc. Amorphous pharmaceutical compositions and uses thereof
TW202229255A (zh) 2020-11-13 2022-08-01 丹麥商Ｈ 朗德貝克公司 Magl抑制劑
CN112675308B (zh) * 2020-12-09 2023-05-05 中国人民解放军军事科学院军事医学研究院 抑制enpp2基因和/或蛋白表达的物质在制备治疗多发性骨髓瘤的药物中的应用
KR20230128511A (ko) * 2021-01-05 2023-09-05 자이두스 라이프사이언시즈 리미티드 신규한 오토택신 억제제
WO2024073658A1 (en) * 2022-09-30 2024-04-04 Genentech, Inc. Hydantoin modulators of cholesterol biosynthesis and their use for promoting remyelination

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5877182A (en) 1996-09-13 1999-03-02 Merck & Co., Inc. Piperidines promote release of growth hormone
US6369077B1 (en) 1997-05-08 2002-04-09 Smithkline Beecham Corporation Protease inhibitors
GB0030303D0 (en) 2000-12-13 2001-01-24 Lilly Co Eli Compounds
JP2004532838A (ja) * 2001-03-02 2004-10-28 ブリストル−マイヤーズ スクイブ カンパニー メラノコルチン受容体のモデュレーターとして有用な化合物及びそれを含む製薬組成物
CA2439691A1 (en) 2001-03-02 2002-09-12 Bristol-Myers Squibb Company Co-administration of melanocortin receptor agonist and phosphodiesterase inhibitor for treatment of cyclic-amp associated disorders
ATE447565T1 (de) * 2001-10-01 2009-11-15 Bristol Myers Squibb Co Spiro-hydantoin-verbindungen, die sich als entzündungshemmende mittel eignen
US20040192674A1 (en) 2003-02-14 2004-09-30 Marquis Robert W. Cathepsin L inhibitors
CA2512886A1 (en) 2003-02-28 2004-09-10 Galderma Research & Development, S.N.C. Ligands that modulate lxr-type receptors
WO2005122379A2 (en) * 2004-05-27 2005-12-22 The Regents Of The University Of California Alpha-4 beta-1 integrin ligands for imaging and therapy
WO2006137465A1 (ja) 2005-06-24 2006-12-28 Shionogi & Co., Ltd. 含窒素複素環誘導体
US7601844B2 (en) 2006-01-27 2009-10-13 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
US8329159B2 (en) * 2006-08-11 2012-12-11 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8906859B2 (en) * 2006-11-10 2014-12-09 Cera Therapeutics, Inc. Uses of kappa opioid synthetic peptide amides
WO2008060621A2 (en) 2006-11-17 2008-05-22 Abbott Laboratories Aminopyrrolidines as chemokine receptor antagonists
US8378100B2 (en) 2008-01-09 2013-02-19 University Of Virginia Patent Foundation Phosphonate derivatives as autotaxin inhibitors
MX2010010241A (es) 2008-03-20 2010-12-06 Forest Lab Holdings Ltd Derivados de piperidina novedosos como inhibidores de estearoil-coa desaturasa.
WO2009151644A2 (en) 2008-06-13 2009-12-17 Yale University Small molecule inhibitors of autotaxin methods of use
WO2010037081A1 (en) * 2008-09-29 2010-04-01 Palatin Technologies, Inc. Melanocortin receptor-specific spiro-piperidine compounds
EA201100879A1 (ru) 2008-12-01 2012-01-30 Мерк Патент Гмбх Производные пиридопиримидина в качестве ингибиторов аутотаксина
US8329907B2 (en) 2009-04-02 2012-12-11 Merck Patent Gmbh Autotaxin inhibitors
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
DK2455376T3 (en) 2009-06-11 2015-03-02 Abbvie Bahamas Ltd Heterocyclic compounds as inhibitors of hepatitis C virus (HCV)
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
KR101184115B1 (ko) * 2009-08-31 2012-09-18 일동제약주식회사 신규 펩티드 데포르밀라제 저해제 화합물 및 그 제조방법
US8497371B2 (en) 2009-10-26 2013-07-30 University Of Memphis Research Foundation Pipemidic acid derivative autotaxin inhibitors
US8518945B2 (en) 2010-03-22 2013-08-27 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
EP2552914B1 (de) 2010-03-26 2015-11-11 Merck Patent GmbH Benzonaphthyridinamine als autotaxin-inhibitoren
JP2011219368A (ja) 2010-04-02 2011-11-04 Daiichi Sankyo Co Ltd Ｎ−サリチルアミノ酸誘導体
ES2646834T3 (es) 2010-08-20 2017-12-18 Amira Pharmaceuticals, Inc. Inhibidores de autotaxina y usos de los mismos
US8546416B2 (en) * 2011-05-27 2013-10-01 Novartis Ag 3-spirocyclic piperidine derivatives as ghrelin receptor agonists
US9260416B2 (en) 2011-05-27 2016-02-16 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
US9273011B2 (en) 2011-10-28 2016-03-01 Inhibitaxin Limited Substituted pyridazines for the treatment of pain
EA201492223A1 (ru) 2012-06-13 2015-03-31 Ф. Хоффманн-Ля Рош Аг Новые диазаспироциклоалканы и азаспироциклоалканы
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
TW201500356A (zh) 2013-04-12 2015-01-01 Lilly Co Eli 二氫吡啶并嘧啶化合物
EP3022201A1 (en) 2013-07-18 2016-05-25 Novartis AG Autotaxin inhibitors
AU2014291711B2 (en) 2013-07-18 2017-02-02 Novartis Ag Autotaxin inhibitors comprising a heteroaromatic ring-benzyl-amide-cycle core
WO2015042052A1 (en) 2013-09-17 2015-03-26 Pharmakea, Inc. Heterocyclic vinyl autotaxin inhibitor compounds
US9714240B2 (en) 2013-09-17 2017-07-25 Pharmakea, Inc. Vinyl autotaxin inhibitor compounds
US9850203B2 (en) 2013-09-26 2017-12-26 Pharmakea, Inc. Autotaxin inhibitor compounds
PE20170206A1 (es) 2014-04-04 2017-04-09 X-Rx Inc Inhibidores espirociclicos sustituidos de la autotaxina
EP3134079A4 (en) 2014-04-23 2017-12-20 X-RX Discovery, Inc. Substituted n-(2-(amino)-2-oxoethyl)benzamide inhibitors of autotaxin and their preparation and use in the treatment of lpa-dependent or lpa-mediated diseases

Also Published As

Publication number Publication date
CR20160496A (es) 2017-01-02
US20170166568A1 (en) 2017-06-15
US10233182B2 (en) 2019-03-19
AU2015240519B2 (en) 2019-08-15
EP3125895A1 (en) 2017-02-08
WO2015154023A1 (en) 2015-10-08
JP2017513932A (ja) 2017-06-01
CN107106559A (zh) 2017-08-29
PH12016501922A1 (en) 2016-12-19
IL248050A0 (en) 2016-11-30
MX2016013049A (es) 2017-04-27
MD20160116A2 (ro) 2017-04-30
CL2016002516A1 (es) 2017-05-12
DOP2016000270A (es) 2016-12-15
US20190225611A1 (en) 2019-07-25
JP2020040960A (ja) 2020-03-19
EP3125895A4 (en) 2017-08-30
EA201691840A1 (ru) 2017-03-31
AP2016009496A0 (en) 2016-10-31
US20180282332A1 (en) 2018-10-04
SG11201607920RA (en) 2016-10-28
CU20160150A7 (es) 2017-02-02
CA2943874A1 (en) 2015-10-08
US10011601B2 (en) 2018-07-03
ECSP16084293A (es) 2017-01-31
KR20160133004A (ko) 2016-11-21
CU24442B1 (es) 2019-09-04
JP6616821B2 (ja) 2019-12-04
AU2015240519A1 (en) 2016-10-20
AU2019264641A1 (en) 2019-12-05

Similar Documents

Publication Publication Date Title
PE20170206A1 (es) Inhibidores espirociclicos sustituidos de la autotaxina
PE20180117A1 (es) Inhibidores de indolamina-2,3-dioxigenasa para el tratamiento de cancer
DOP2017000066A (es) Compuestos y composiciones como inhibidores de quinasa raf
ECSP17073191A (es) Compuestos heterocíclicos como inhibidores de lsd1
PH12016502382A1 (en) Substituted indazole compounds as irak4 inhibitors
DOP2016000085A (es) Amino-heteroaril-benzamidas como inhibidores de cinasa
ECSP16076566A (es) Compuestos de heteroarilo o arilo biciclicos fusionados y su aplicación a inhibidores de irak4
DOP2020000249A (es) N-benzisoxazolilo bencenosulfonamidas como inhibidores de kat
CU20160180A7 (es) Compuestos de dihidroisoquinolinona sustituida
PE20181145A1 (es) Compuestos de piridina
PE20180461A1 (es) Nuevos compuestos biciclicos como inhibidores de la atx
PE20200387A1 (es) Proceso novedoso para la elaboracion de compuestos para su uso en el tratamiento del cancer
EA201692143A1 (ru) Производные аминопиразина в качестве ингибиторов фосфатидилинозитол-3-киназы
AR089781A1 (es) Fluorometil-5,6-dihidro-4h-[1,3]oxazinas
GT201400167A (es) Nuevos derivados de bencil sulfonamida utiles como inhibidores de mogat-2
PE20181319A1 (es) Compuestos de isoindol
MX2016015467A (es) Derivados de carbonitrilo como moduladores selectivos del receptor de androgenos.
EA201791396A1 (ru) ПРОИЗВОДНЫЕ ИМИДАЗОПИРИДАЗИНА В КАЧЕСТВЕ ИНГИБИТОРОВ PI3Kβ
UY35785A (es) Derivados de piperazina sustituidos como moduladores del transportador de la glicina-1 (glyt1)
EA201692139A1 (ru) Производные пиразина в качестве ингибиторов фосфатидилинозитол 3-киназы
PE20161226A1 (es) Acido (s)-3'-metil-abscisico y esteres del mismo
AR091402A1 (es) Profarmacos de acido fosforadimico
EA201791397A1 (ru) СВЯЗАННЫЕ С ГЕТЕРОЦИКЛИЛАМИ ПРОИЗВОДНЫЕ ИМИДАЗОПИРИДАЗИНА В КАЧЕСТВЕ ИНГИБИТОРОВ PI3Kβ
NZ707087A (en) Novel flavonoid compounds and uses thereof
UY36023A (es) “derivados cristalinos de (s)-1-((2r,3r,4s,5s)-5-alil-3-metoxi-4-(tosilmetil) tetrahidrofuran-2-il)-3-aminopropan-2-ol “.