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 (enExample
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

    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Diabetes (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 (enExample) 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 (enExample)
EP (1) EP3125895A4 (enExample)
JP (2) JP6616821B2 (enExample)
KR (1) KR20160133004A (enExample)
CN (1) CN107106559A (enExample)
AP (1) AP2016009496A0 (enExample)
AU (2) AU2015240519B2 (enExample)
CA (1) CA2943874A1 (enExample)
CL (1) CL2016002516A1 (enExample)
CR (1) CR20160496A (enExample)
CU (1) CU24442B1 (enExample)
DO (1) DOP2016000270A (enExample)
EA (1) EA201691840A1 (enExample)
EC (1) ECSP16084293A (enExample)
IL (1) IL248050A0 (enExample)
MD (1) MD20160116A2 (enExample)
MX (1) MX2016013049A (enExample)
PE (1) PE20170206A1 (enExample)
PH (1) PH12016501922A1 (enExample)
SG (1) SG11201607920RA (enExample)
WO (1) WO2015154023A1 (enExample)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2861566T (pt) 2012-06-13 2017-02-08 Hoffmann La Roche Novos diazaspirocicloalcanos e azaspirocicloalcanos
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
AU2014356583B2 (en) 2013-11-26 2019-02-28 F. Hoffmann-La Roche Ag New octahydro-cyclobuta (1,2-c;3,4-c')dipyrrol-2-yl
AU2015238537B2 (en) 2014-03-26 2019-08-01 F. Hoffmann-La Roche Ag Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors
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
CR20160496A (es) 2014-04-04 2017-01-02 X-Rx Inc Inhibidores espirocíclicos sustituidos de la autotaxina
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
UA123362C2 (uk) 2015-09-04 2021-03-24 Ф. Хоффманн-Ля Рош Аг Феноксиметильні похідні
CR20180057A (es) 2015-09-24 2018-04-02 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca.
AU2016328535A1 (en) 2015-09-24 2017-11-09 F. Hoffmann-La Roche Ag Bicyclic compounds as ATX inhibitors
KR20180053408A (ko) 2015-09-24 2018-05-21 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서의 신규한 이환형 화합물
CR20180072A (es) 2015-09-24 2018-02-26 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores de atx
CA3016081A1 (en) 2016-03-04 2017-09-08 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
SG11201908560SA (en) 2017-03-16 2019-10-30 Hoffmann La Roche Heterocyclic compounds useful as dual atx/ca 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
CA3076477A1 (en) 2017-09-29 2019-04-04 Takeda Pharmaceutical Company Limited Heterocyclic compound
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
KR20230051227A (ko) * 2020-08-14 2023-04-17 노파르티스 아게 헤테로아릴 치환된 스피로피페리디닐 유도체 및 이의 제약 용도
US11434222B2 (en) 2020-11-13 2022-09-06 H. Lundbeck A/S MAGL inhibitors
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
WO2022149010A1 (en) * 2021-01-05 2022-07-14 Cadila Healthcare Limited Novel inhibitors of autotaxin
CN119137114A (zh) 2022-05-04 2024-12-13 H.隆德贝克有限公司 作为单酰基甘油脂肪酶抑制剂的(s)-1-(哒嗪-3-基氨基甲酰基)-6-氮杂螺[2.5]辛烷-6-甲酸1,1,1,3,3,3-六氟丙-2-酯的结晶形式
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
HUP0001285A3 (en) 1997-05-08 2000-10-30 Smithkline Beecham Corp Philap Pyrrolidine derivatives as protease inhibitors, process for producing them and pharmaceutical compositions containing them
GB0030303D0 (en) 2000-12-13 2001-01-24 Lilly Co Eli Compounds
HUP0600103A2 (en) * 2001-03-02 2006-06-28 Bristol Myers Squibb Co Co-administration of melanocortin receptor agonist and phosphodiesterase inhibitor for treatment of cyclic-amp associated disorders
JP2005511475A (ja) * 2001-03-02 2005-04-28 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ジ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
AR036663A1 (es) * 2001-10-01 2004-09-22 Bristol Myers Squibb Co Compuestos de espiro-hidantoina utiles como agentes anti-inflamatorios, las composiciones farmaceuticas que las contienen y los intermediarios para preparar dichos compuestos
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
CN101534824A (zh) 2006-11-17 2009-09-16 艾博特公司 作为化学活素受体拮抗剂的氨基吡咯烷
US8378100B2 (en) 2008-01-09 2013-02-19 University Of Virginia Patent Foundation Phosphonate derivatives as autotaxin inhibitors
EP2268143A4 (en) 2008-03-20 2012-06-27 Forest Lab Holdings Ltd NEW PIPERIDINE DERIVATIVES AS INHIBITORS OF THE STEAROYL COA DESATURASE
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
SG171809A1 (en) 2008-12-01 2011-07-28 Merck Patent Gmbh 2, 5-diamino-substituted pyrido [4, 3-d] pyrimidines as autotaxin inhibitors against cancer
ES2547124T3 (es) 2009-04-02 2015-10-01 Merck Patent Gmbh Inhibidores de autotaxina
JP5767205B2 (ja) 2009-04-02 2015-08-19 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 オートタキシン阻害剤としての複素環式化合物
MX2011010203A (es) 2009-04-02 2011-10-14 Merck Patent Gmbh Derivados de piperidina y piperazina como inhibidores de autotaxina.
DK2368890T3 (da) * 2009-06-11 2013-07-22 Abbvie Bahamas Ltd Hepatitis C-virusinhibitorer
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
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
JP2013536200A (ja) 2010-08-20 2013-09-19 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 オートタキシン阻害剤およびその使用
EP2714680B1 (en) 2011-05-27 2015-11-25 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
UY34094A (es) * 2011-05-27 2013-01-03 Novartis Ag Derivados de la piperidina 3-espirocíclica como agonistas de receptores de la ghrelina
EP2771325B1 (en) 2011-10-28 2017-06-28 Inhibitaxin Limited Pyridazine derivatives useful in therapy
PT2861566T (pt) * 2012-06-13 2017-02-08 Hoffmann La Roche Novos diazaspirocicloalcanos e azaspirocicloalcanos
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
SG11201600241RA (en) 2013-07-18 2016-02-26 Novartis Ag Autotaxin inhibitors comprising a heteroaromatic ring-benzyl-amide-cycle core
EP3022201A1 (en) 2013-07-18 2016-05-25 Novartis AG Autotaxin inhibitors
US9951026B2 (en) 2013-09-17 2018-04-24 Pharmakea, Inc. Heterocyclic vinyl autotaxin inhibitor compounds
WO2015042053A1 (en) 2013-09-17 2015-03-26 Pharmakea, Inc. Vinyl autotaxin inhibitor compounds
US9850203B2 (en) 2013-09-26 2017-12-26 Pharmakea, Inc. Autotaxin inhibitor compounds
CR20160496A (es) 2014-04-04 2017-01-02 X-Rx Inc Inhibidores espirocíclicos sustituidos de la autotaxina
JP6592008B2 (ja) 2014-04-23 2019-10-16 エックス−アールエックス， インコーポレイテッド 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

Also Published As

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

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
CA2859578C (en) Dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders.
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
ES3010513T3 (en) Substituted pyrrolopyrimidine and pyrazolopyrimidine as bruton's tyrosine kinase (btk) degraders
UA114323C2 (uk) Інгібітори nampt
CA3219215A1 (en) Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
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
HK40054771B (en) Inhibitors of keap1-nrf2 protein-protein interaction
HK40054771A (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