CA2943874A1 - Substituted spirocyclic inhibitors of autotaxin - Google Patents

Substituted spirocyclic inhibitors of autotaxin Download PDF

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Publication number
CA2943874A1
CA2943874A1 CA2943874A CA2943874A CA2943874A1 CA 2943874 A1 CA2943874 A1 CA 2943874A1 CA 2943874 A CA2943874 A CA 2943874A CA 2943874 A CA2943874 A CA 2943874A CA 2943874 A1 CA2943874 A1 CA 2943874A1
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CA
Canada
Prior art keywords
methyl
triazaspiro
decan
oxobutan
fluoro
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.)
Abandoned
Application number
CA2943874A
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English (en)
French (fr)
Inventor
Lee BABISS
Matthew Clark
Anthony D. Keefe
Mark J. Mulvihill
Haihong Ni
Louis RENZETTI
Frank Ruebsam
Ce Wang
Zhifeng Xie
Ying Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
X-RX Inc
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 CA2943874A1 publication Critical patent/CA2943874A1/en
Abandoned legal-status Critical Current

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    • 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
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    • 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
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    • 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
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A—HUMAN NECESSITIES
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    • A61P17/04—Antipruritics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • 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
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • 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)
CA2943874A 2014-04-04 2015-04-03 Substituted spirocyclic inhibitors of autotaxin Abandoned CA2943874A1 (en)

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

Publications (1)

Publication Number Publication Date
CA2943874A1 true CA2943874A1 (en) 2015-10-08

Family

ID=54241341

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2943874A Abandoned CA2943874A1 (en) 2014-04-04 2015-04-03 Substituted spirocyclic inhibitors of autotaxin

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

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