KR101752124B1 - 선택적인 스핑고신 1 포스페이트 수용체 조절자 및 카이랄 합성 방법 - Google Patents

선택적인 스핑고신 1 포스페이트 수용체 조절자 및 카이랄 합성 방법 Download PDF

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KR101752124B1
KR101752124B1 KR1020167035297A KR20167035297A KR101752124B1 KR 101752124 B1 KR101752124 B1 KR 101752124B1 KR 1020167035297 A KR1020167035297 A KR 1020167035297A KR 20167035297 A KR20167035297 A KR 20167035297A KR 101752124 B1 KR101752124 B1 KR 101752124B1
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compound
dihydro
inden
chiral
cyano
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KR20160149317A (ko
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에스더 마틴보로우
마르쿠스 에프. 보헴
아담 리차드 예거
준코 타미야
리밍 황
이누구르티 브라마카리
마니샤 무르자니
그레그 알란 티모니
제니퍼 엘. 브룩스
로버트 피치
피오나 로레인 스콧
마이클 알렌 한슨
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레셉토스,엘엘씨
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/74—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,3
    • A01N43/78—1,3-Thiazoles; Hydrogenated 1,3-thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
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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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07C245/12—Diazo compounds, i.e. compounds having the free valencies of >N2 groups attached to the same carbon atom
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    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
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    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
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  • Wood Science & Technology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020167035297A 2009-11-13 2010-11-15 선택적인 스핑고신 1 포스페이트 수용체 조절자 및 카이랄 합성 방법 Active KR101752124B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US26130109P 2009-11-13 2009-11-13
US61/261,301 2009-11-13
US26247409P 2009-11-18 2009-11-18
US61/262,474 2009-11-18
PCT/US2010/056760 WO2011060392A1 (en) 2009-11-13 2010-11-15 Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis

Related Parent Applications (1)

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KR1020127015292A Division KR101721716B1 (ko) 2009-11-13 2010-11-15 선택적인 스핑고신 1 포스페이트 수용체 조절자 및 카이랄 합성 방법

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KR20160149317A KR20160149317A (ko) 2016-12-27
KR101752124B1 true KR101752124B1 (ko) 2017-06-28

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KR1020167035297A Active KR101752124B1 (ko) 2009-11-13 2010-11-15 선택적인 스핑고신 1 포스페이트 수용체 조절자 및 카이랄 합성 방법
KR1020127015292A Active KR101721716B1 (ko) 2009-11-13 2010-11-15 선택적인 스핑고신 1 포스페이트 수용체 조절자 및 카이랄 합성 방법

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US (4) US8362048B2 (enExample)
EP (3) EP3868377A1 (enExample)
JP (3) JP5650233B2 (enExample)
KR (2) KR101752124B1 (enExample)
CN (2) CN105061350B (enExample)
AU (1) AU2010319983B2 (enExample)
BR (2) BR112012011427B8 (enExample)
CA (2) CA2780772C (enExample)
CY (3) CY1120338T1 (enExample)
DK (2) DK2498610T4 (enExample)
EA (2) EA024801B1 (enExample)
ES (2) ES2858337T3 (enExample)
FI (1) FI2498610T4 (enExample)
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HR (2) HRP20180874T4 (enExample)
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IL (2) IL219691B (enExample)
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MX (1) MX2012005560A (enExample)
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PH (2) PH12012500939A1 (enExample)
PL (2) PL2498610T5 (enExample)
PT (2) PT3406142T (enExample)
RS (2) RS57253B2 (enExample)
SG (1) SG10201407357PA (enExample)
SI (2) SI3406142T1 (enExample)
SM (2) SMT201800288T1 (enExample)
TR (1) TR201807912T4 (enExample)
WO (1) WO2011060392A1 (enExample)

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ES2665461T3 (es) * 2009-11-13 2018-04-25 Celgene International Ii Sàrl Moduladores del receptor esfingosina 1-fosfato y métodos de síntesis quiral
JP5650233B2 (ja) 2009-11-13 2015-01-07 レセプトス インコーポレイテッドＲｅｃｅｐｔｏｓ， Ｉｎｃ． 選択的スフィンゴシン−１−リン酸受容体変調因子および不斉合成方法
WO2012158550A2 (en) 2011-05-13 2012-11-22 Receptos, Inc. Selective heterocyclic sphingosine 1 phosphate receptor modulators
KR101951519B1 (ko) * 2012-06-21 2019-02-22 에자이 알앤드디 매니지먼트 가부시키가이샤 신규한 인단설파미드 유도체
WO2014158302A1 (en) * 2013-03-25 2014-10-02 Swenson Rolf Eric Novel sphingosine 1-phosphate receptor antagonists
WO2015066515A1 (en) * 2013-11-01 2015-05-07 Receptos, Inc. Selective sphingosine 1 phosphate receptor modulators and combination therapy therewith
AU2016246398A1 (en) 2015-04-06 2017-10-26 Auspex Pharmaceuticals, Inc. Deuterium-substituted oxadiazoles
WO2017215617A1 (zh) 2016-06-14 2017-12-21 苏州科睿思制药有限公司 奥扎莫德的晶型、其盐酸盐的晶型及其制备方法
US11192886B2 (en) 2016-07-22 2021-12-07 Medshine Discovery Inc. S1P1 agonist and application thereof
EP3502100A1 (en) * 2016-08-19 2019-06-26 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal forms of ozanimod and preparation method therefor
US10882830B2 (en) 2016-09-14 2021-01-05 Receptos Llc Crystal form of ozanimod hydrochloride and processes for preparation therefor
US11117875B2 (en) 2016-09-14 2021-09-14 Hangzhou Solipharma Co., Ltd. Crystalline forms, preparation methods and pharmaceutical compositions of ozanimod
WO2018064356A1 (en) 2016-09-29 2018-04-05 Celgene International Ii Sarl Compounds and methods for treating lupus
JP7123956B2 (ja) * 2017-02-28 2022-08-23 ヘリオイースト・ファーマシューティカル・カンパニー・リミテッド スピロ化合物およびその使用
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CN108727291A (zh) * 2017-04-21 2018-11-02 宁波爱诺医药科技有限公司 奥扎莫德及其中间体的制备方法
CN108727292A (zh) * 2017-04-21 2018-11-02 宁波爱诺医药科技有限公司 一种奥扎莫德及其中间体的制备方法
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