JP6616821B2 - オートタキシンの置換スピロ環式阻害剤 - Google Patents

オートタキシンの置換スピロ環式阻害剤 Download PDF

Info

Publication number
JP6616821B2
JP6616821B2 JP2017503794A JP2017503794A JP6616821B2 JP 6616821 B2 JP6616821 B2 JP 6616821B2 JP 2017503794 A JP2017503794 A JP 2017503794A JP 2017503794 A JP2017503794 A JP 2017503794A JP 6616821 B2 JP6616821 B2 JP 6616821B2
Authority
JP
Japan
Prior art keywords
methyl
triazaspiro
decan
fluoro
oxobutan
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2017503794A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017513932A5 (https=
JP2017513932A (ja
Inventor
リー バビス,
マシュー クラーク,
アントニー ディー. キーフ,
マーク ジェイ. マルビヒル,
ハイホン ニ,
ルイス レンゼッティ,
フランク ルーブサム,
ツェ ワン,
ジフェン シエ,
イン ザン,
Original Assignee
エックス−アールエックス, インコーポレイテッド
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 エックス−アールエックス, インコーポレイテッド filed Critical エックス−アールエックス, インコーポレイテッド
Publication of JP2017513932A publication Critical patent/JP2017513932A/ja
Publication of JP2017513932A5 publication Critical patent/JP2017513932A5/ja
Application granted granted Critical
Publication of JP6616821B2 publication Critical patent/JP6616821B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (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)
JP2017503794A 2014-04-04 2015-04-03 オートタキシンの置換スピロ環式阻害剤 Expired - Fee Related JP6616821B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461975123P 2014-04-04 2014-04-04
US61/975,123 2014-04-04
PCT/US2015/024338 WO2015154023A1 (en) 2014-04-04 2015-04-03 Substituted spirocydic inhibitors of autotaxin

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2019203023A Division JP2020040960A (ja) 2014-04-04 2019-11-08 オートタキシンの置換スピロ環式阻害剤

Publications (3)

Publication Number Publication Date
JP2017513932A JP2017513932A (ja) 2017-06-01
JP2017513932A5 JP2017513932A5 (https=) 2018-05-17
JP6616821B2 true JP6616821B2 (ja) 2019-12-04

Family

ID=54241341

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2017503794A Expired - Fee Related JP6616821B2 (ja) 2014-04-04 2015-04-03 オートタキシンの置換スピロ環式阻害剤
JP2019203023A Pending JP2020040960A (ja) 2014-04-04 2019-11-08 オートタキシンの置換スピロ環式阻害剤

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2019203023A Pending JP2020040960A (ja) 2014-04-04 2019-11-08 オートタキシンの置換スピロ環式阻害剤

Country Status (21)

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

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2014DN09346A (https=) 2012-06-13 2015-07-17 Hoffmann La Roche
KR102179599B1 (ko) 2012-09-25 2020-11-19 에프. 호프만-라 로슈 아게 이환형 유도체
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
CN105764905B (zh) 2013-11-26 2019-06-07 豪夫迈·罗氏有限公司 新的八氢-环丁二烯并[1,2-c;3,4-c’]二吡咯-2基
WO2015144609A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
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
MX2016013049A (es) 2014-04-04 2017-04-27 X-Rx Inc Inhibidores de autotaxina espirociclicos sustituidos.
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
CA2992889A1 (en) 2015-09-04 2017-03-09 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
KR20180054830A (ko) 2015-09-24 2018-05-24 에프. 호프만-라 로슈 아게 오토탁신(atx) 억제제로서의 이환형 화합물
AU2016328365B2 (en) 2015-09-24 2020-04-23 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
RU2018112230A (ru) 2015-09-24 2019-10-30 Ф. Хоффманн-Ля Рош Аг Бициклические соединения в качестве ингибиторов atx
CR20180057A (es) 2015-09-24 2018-04-02 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca.
AU2017228371A1 (en) 2016-03-04 2018-09-13 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
SG11201908560SA (en) 2017-03-16 2019-10-30 Hoffmann La Roche Heterocyclic compounds useful as dual atx/ca inhibitors
WO2018167113A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag New bicyclic compounds as atx inhibitors
KR101798840B1 (ko) 2017-05-17 2017-11-17 주식회사 레고켐 바이오사이언스 신규 오토탁신 저해 화합물 및 이를 함유하는 약제학적 조성물
US10961242B2 (en) 2017-05-17 2021-03-30 Legochem Biosciences, Inc. Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same
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
US12383547B2 (en) 2020-07-01 2025-08-12 Vanderbilt University Methods of treatment for a kidney disease
MX2023001725A (es) * 2020-08-14 2023-02-22 Novartis Ag Derivados de espiropiperidinilo sustituidos con heteroarilo y usos farmaceuticos de los mismos.
TWI904281B (zh) 2020-11-13 2025-11-11 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
US20240327407A1 (en) 2021-01-05 2024-10-03 Cadila Heal Thcare Limited Novel inhibitors of autotaxin
KR20250005229A (ko) 2022-05-04 2025-01-09 하. 룬드벡 아크티에셀스카브 모노아실글리세롤 리파제 억제제로서 1,1,1,3,3,3-헥사플루오로프로판-2-일 (s)-1-(피리다진-3-일카르바모일)-6 아자스피로[2.5]옥탄-6-카르복실레이트의 결정질 형태
JP2025534402A (ja) * 2022-09-30 2025-10-15 ジェネンテック, インコーポレイテッド コレステロール生合成のヒダントインモジュレーターおよび再髄鞘形成を促進するためのその使用

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
WO1998050534A1 (en) 1997-05-08 1998-11-12 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
JP2005506286A (ja) 2001-03-02 2005-03-03 ブリストル−マイヤーズ スクイブ カンパニー サイクリック−amp関連疾患の治療を目的としたメラノコルチン受容体アゴニストおよびホスホジエステラーゼ阻害剤の併用投与
CA2462112A1 (en) * 2001-10-01 2003-04-10 Bristol-Myers Squibb Company Spiro-hydantoin compounds useful as anti-inflammatory agents
US20040192674A1 (en) 2003-02-14 2004-09-30 Marquis Robert W. Cathepsin L inhibitors
EP1599447A1 (en) 2003-02-28 2005-11-30 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
CA2669917A1 (en) 2006-11-17 2008-05-22 Dawn M. George Aminopyrrolidines as chemokine receptor antagonists
US8378100B2 (en) 2008-01-09 2013-02-19 University Of Virginia Patent Foundation Phosphonate derivatives as autotaxin inhibitors
BRPI0909183A2 (pt) 2008-03-20 2015-08-25 Forest Lab Holdings Ltd Composto, composição farmacêutica e método de tratamento de condição que responde a inibidor de estearoil-coa dessaturase
US20110110886A1 (en) 2008-06-13 2011-05-12 Yale University Small molecule inhibitors of autotaxin and methods of use
WO2010037081A1 (en) * 2008-09-29 2010-04-01 Palatin Technologies, Inc. Melanocortin receptor-specific spiro-piperidine compounds
WO2010063352A1 (en) 2008-12-01 2010-06-10 Merck Patent Gmbh 2, 5-diamino-substituted pyrido [4, 3-d] pyrimidines as autotaxin inhibitors against cancer
BRPI1009800A2 (pt) 2009-04-02 2016-03-15 Merck Patent Gmbh compostos heterocíclicos como inibidores de autotaxina
KR20120027177A (ko) 2009-04-02 2012-03-21 메르크 파텐트 게엠베하 오토탁신 저해제로서의 피페리딘 및 피라진 유도체
MX2011010218A (es) 2009-04-02 2011-10-10 Merck Patent Gmbh Inhibidores de autotaxina.
UA118080C2 (uk) * 2009-06-11 2018-11-26 Еббві Айрленд Анлімітед Компані Противірусні сполуки
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
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
CN102822171B (zh) 2010-03-26 2015-09-02 默克专利有限公司 作为自分泌运动因子抑制剂的苯并萘啶胺类
JP2011219368A (ja) 2010-04-02 2011-11-04 Daiichi Sankyo Co Ltd N−サリチルアミノ酸誘導体
US9000025B2 (en) 2010-08-20 2015-04-07 Amira Pharmaceuticals, Inc. Autotaxin inhibitors and uses thereof
AR086554A1 (es) * 2011-05-27 2014-01-08 Novartis Ag Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina
US9260416B2 (en) 2011-05-27 2016-02-16 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
ES2748656T3 (es) 2011-10-28 2020-03-17 Inhibitaxin Ltd Derivados de piridazina útiles en terapia
IN2014DN09346A (https=) 2012-06-13 2015-07-17 Hoffmann La Roche
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
MX368059B (es) 2013-07-18 2019-09-18 Novartis Ag Inhibidores de autotaxina que comprenden un núcleo de anillo heteroaromático de bencil-amida cíclica.
US20160168119A1 (en) 2013-07-18 2016-06-16 Novartis Ag Autotaxin inhibitors
US9714240B2 (en) 2013-09-17 2017-07-25 Pharmakea, Inc. Vinyl autotaxin inhibitor compounds
JP2016530210A (ja) 2013-09-17 2016-09-29 ファーマケア,インク. ヘテロ環式ビニルオートタキシン阻害剤化合物
JP2016531874A (ja) 2013-09-26 2016-10-13 ファーマケア,インク. オートタキシン阻害剤化合物
MX2016013049A (es) 2014-04-04 2017-04-27 X-Rx Inc Inhibidores de autotaxina espirociclicos sustituidos.
CN107205972A (zh) 2014-04-23 2017-09-26 X-Rx股份有限公司 自分泌运动因子的取代的n‑(2‑(氨基)‑2‑氧代乙基)苯甲酰胺抑制剂及它们的制备和在治疗lpa‑依赖的或lpa‑介导的疾病中的用途

Also Published As

Publication number Publication date
JP2020040960A (ja) 2020-03-19
US20180282332A1 (en) 2018-10-04
MD20160116A2 (ro) 2017-04-30
US20190225611A1 (en) 2019-07-25
KR20160133004A (ko) 2016-11-21
CA2943874A1 (en) 2015-10-08
CL2016002516A1 (es) 2017-05-12
AU2015240519A1 (en) 2016-10-20
EP3125895A4 (en) 2017-08-30
EA201691840A1 (ru) 2017-03-31
US10011601B2 (en) 2018-07-03
EP3125895A1 (en) 2017-02-08
CR20160496A (es) 2017-01-02
US10233182B2 (en) 2019-03-19
DOP2016000270A (es) 2016-12-15
JP2017513932A (ja) 2017-06-01
MX2016013049A (es) 2017-04-27
PE20170206A1 (es) 2017-04-09
AP2016009496A0 (en) 2016-10-31
US20170166568A1 (en) 2017-06-15
CN107106559A (zh) 2017-08-29
AU2015240519B2 (en) 2019-08-15
CU20160150A7 (es) 2017-02-02
ECSP16084293A (es) 2017-01-31
PH12016501922A1 (en) 2016-12-19
AU2019264641A1 (en) 2019-12-05
IL248050A0 (en) 2016-11-30
SG11201607920RA (en) 2016-10-28
CU24442B1 (es) 2019-09-04
WO2015154023A1 (en) 2015-10-08

Similar Documents

Publication Publication Date Title
JP6616821B2 (ja) オートタキシンの置換スピロ環式阻害剤
JP6592008B2 (ja) オートタキシンの置換n−(2−アミノ)−2−オキソエチルベンズアミド阻害剤およびそれらの調製、ならびにlpa依存性またはlpa媒介性疾患の処置における使用
CN111655682B (zh) 一种高活性sting蛋白激动剂化合物
AU2019326368B2 (en) Inhibitors of KEAP1-Nrf2 protein-protein interaction
CA3219215A1 (en) Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
ES3010513T3 (en) Substituted pyrrolopyrimidine and pyrazolopyrimidine as bruton's tyrosine kinase (btk) degraders
CA2859578A1 (en) Dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders.
UA114323C2 (uk) Інгібітори nampt
JP7584802B2 (ja) 高活性stingタンパク質アゴニスト
CA3164963A1 (en) Furoindazole derivatives
TW202122382A (zh) 乙內醯脲衍生物
JP6322275B2 (ja) ヤヌスキナーゼ阻害剤としてのn−(2−シアノヘテロシクリル)ピラゾロピリドン
CA2891725A1 (en) Substituted pyridopyrazines as syk inhibitors
TW202146384A (zh) 取代的氮雜五元環類化合物及其在藥物中的應用
OA18996A (en) Substituted Spirocyclic Inhibitors of Autotaxin
WO2024086094A1 (en) Alkylamine-containing small molecule degraders of bcl6
HK40054771A (en) Inhibitors of keap1-nrf2 protein-protein interaction
HK40054771B (en) Inhibitors of keap1-nrf2 protein-protein interaction
EA041386B1 (ru) Спироциклические соединения и способы их получения и применения
NZ787918A (en) Pyridopyrimdinone CDK2/4/6 inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180330

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180330

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20181108

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20181128

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20190225

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20190424

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190528

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20190912

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20191010

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20191108

R150 Certificate of patent or registration of utility model

Ref document number: 6616821

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees