TWI657076B - 經取代磺醯胺化合物 - Google Patents

經取代磺醯胺化合物 Download PDF

Info

Publication number
TWI657076B
TWI657076B TW103135249A TW103135249A TWI657076B TW I657076 B TWI657076 B TW I657076B TW 103135249 A TW103135249 A TW 103135249A TW 103135249 A TW103135249 A TW 103135249A TW I657076 B TWI657076 B TW I657076B
Authority
TW
Taiwan
Prior art keywords
alkyl
haloalkyl
compound
group
phenyl
Prior art date
Application number
TW103135249A
Other languages
English (en)
Chinese (zh)
Other versions
TW201605795A (zh
Inventor
慧芬 陳
初燕燕
史蒂芬 多
安東尼 艾斯達
白華 胡
亞力山德 柯利斯尼卡瓦
林星雨
喬瑟夫P 萊多斯
丹尼爾 蕭爾
維雪爾 維瑪
蘭 王
國生 吳
保偉 袁
Original Assignee
赫孚孟拉羅股份公司
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 赫孚孟拉羅股份公司 filed Critical 赫孚孟拉羅股份公司
Publication of TW201605795A publication Critical patent/TW201605795A/zh
Application granted granted Critical
Publication of TWI657076B publication Critical patent/TWI657076B/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C07D207/48—Sulfur atoms
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/41—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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P1/04—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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P11/14—Antitussive agents
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P27/16—Otologicals
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
TW103135249A 2013-10-11 2014-10-09 經取代磺醯胺化合物 TWI657076B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361890127P 2013-10-11 2013-10-11
US61/890,127 2013-10-11
CN2014086380 2014-09-12
??PCT/CN2014/086380 2014-09-12

Publications (2)

Publication Number Publication Date
TW201605795A TW201605795A (zh) 2016-02-16
TWI657076B true TWI657076B (zh) 2019-04-21

Family

ID=51794850

Family Applications (1)

Application Number Title Priority Date Filing Date
TW103135249A TWI657076B (zh) 2013-10-11 2014-10-09 經取代磺醯胺化合物

Country Status (22)

Country Link
US (4) US20160221945A1 (enExample)
EP (1) EP3055302B1 (enExample)
JP (2) JP2016532673A (enExample)
KR (1) KR20160064230A (enExample)
CN (1) CN105612153B (enExample)
BR (1) BR112016002012A2 (enExample)
CA (1) CA2917193A1 (enExample)
DK (1) DK3055302T3 (enExample)
ES (1) ES2713323T3 (enExample)
HR (1) HRP20190329T1 (enExample)
HU (1) HUE041652T2 (enExample)
LT (1) LT3055302T (enExample)
MX (1) MX363457B (enExample)
PL (1) PL3055302T3 (enExample)
PT (1) PT3055302T (enExample)
RS (1) RS58376B1 (enExample)
RU (1) RU2675792C2 (enExample)
SG (1) SG11201609411SA (enExample)
SI (1) SI3055302T1 (enExample)
TR (1) TR201902249T4 (enExample)
TW (1) TWI657076B (enExample)
WO (1) WO2015052264A1 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2975196A1 (en) * 2015-02-15 2016-08-18 F. Hoffmann-La Roche Ag 1-(het)arylsulfonyl-(pyrrolidine or piperidine)-2-carboxamide derivatives and their use as trpa1 antagonists
EP3259264B1 (en) 2015-02-20 2022-07-27 Rigel Pharmaceuticals, Inc. Gdf-8 inhibitors
JP2018519292A (ja) * 2015-07-01 2018-07-19 ファーマケア,インク. リシルオキシダーゼ様2阻害剤およびその使用
CA3012812A1 (en) * 2016-02-05 2017-08-10 Ea Pharma Co., Ltd. Heterocyclic sulfonamide derivative and medicine containing same
TW201808906A (zh) 2016-03-16 2018-03-16 拜耳作物科學股份有限公司 作為殺蟲劑之經取代吡啶化合物
CN109476640B (zh) * 2016-07-20 2022-02-25 豪夫迈·罗氏有限公司 双环脯氨酸化合物
EP3487849A1 (en) * 2016-07-20 2019-05-29 H. Hoffnabb-La Roche Ag Sulfonylcycloalkyl carboxamide compounds as trpa1 modulators
CN109803964A (zh) 2016-08-12 2019-05-24 豪夫迈·罗氏有限公司 磺酰基吡啶基trp抑制剂
EP3929194B1 (en) 2017-06-01 2024-04-17 Bristol-Myers Squibb Company Substituted nitrogen containing compounds
JP2019019124A (ja) * 2017-07-19 2019-02-07 日本化薬株式会社 ピラジン化合物
KR102716244B1 (ko) * 2017-12-08 2024-10-14 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유증 막횡단 전도 조절자의 조정제의 제조 방법
TW202000201A (zh) * 2018-02-20 2020-01-01 瑞士商赫孚孟拉羅股份公司 製備1-芳基磺醯基-吡咯啶-2-甲醯胺瞬時受體電位通道拮抗劑化合物及其結晶型式之方法
KR102006157B1 (ko) 2018-03-22 2019-08-01 (주)에스더블유엠 자율주행 차량의 주행 유도선 제공 방법 및 장치
KR102006158B1 (ko) 2018-03-27 2019-08-01 (주)에스더블유엠 차량 주행유도 장치 및 방법
KR102068473B1 (ko) 2018-03-30 2020-02-11 (주)에스더블유엠 차량 시뮬레이션 방법 및 장치
KR102798291B1 (ko) 2019-03-28 2025-04-18 스미토모 겐키 가부시키가이샤 쇼벨 및 시공시스템
CN111116456B (zh) * 2019-12-26 2022-01-28 南通华祥医药科技有限公司 一种4,4-二氟哌啶盐酸盐的制备方法
FR3114235A1 (fr) 2020-09-18 2022-03-25 Université Grenoble Alpes Inhibition du canal trpa1 astrocytaire comme nouvelle cible therapeutique neuroprotectrice dans les phases prodromales de la maladie d’alzheimer
CN112624966B (zh) * 2020-12-25 2022-12-23 杭州澳赛诺生物科技有限公司 一种2-氨甲基-4-甲基-5-吡啶羧酸的合成方法
IT202100015098A1 (it) 2021-06-09 2022-12-09 Flonext S R L Composto antagonista del canale trpa1 per uso in patologie degenerative della retina
CN116478076A (zh) * 2023-04-26 2023-07-25 南京优氟医药科技有限公司 一种(2s,4s)-1-叔丁氧羰基-2-(二氟甲基)-4-羟基吡咯烷的制备方法
WO2025132542A1 (en) 2023-12-19 2025-06-26 Idorsia Pharmaceuticals Ltd Macrocyclic orexin agonists
WO2025162472A1 (en) 2024-01-31 2025-08-07 Insmed Incorporated Linear dipeptidyl peptidase 1 inhibitors and uses thereof
WO2025259779A1 (en) * 2024-06-12 2025-12-18 Insmed Incorporated Uses of certain carboxamides as dpp1 inhibitors
CN119019440A (zh) * 2024-10-24 2024-11-26 浙江雅辰药物科技股份有限公司 一种6-环丙基吡啶-3-硼酸频那醇酯的制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013108857A1 (ja) * 2012-01-17 2013-07-25 味の素株式会社 複素環アミド誘導体及びそれを含有する医薬

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
EP0102324A3 (de) 1982-07-29 1984-11-07 Ciba-Geigy Ag Lipide und Tenside in wässriger Phase
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
HUT35524A (en) 1983-08-02 1985-07-29 Hoechst Ag Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance
US5004697A (en) 1987-08-17 1991-04-02 Univ. Of Ca Cationized antibodies for delivery through the blood-brain barrier
US5268164A (en) 1990-04-23 1993-12-07 Alkermes, Inc. Increasing blood-brain barrier permeability with permeabilizer peptides
US5112596A (en) 1990-04-23 1992-05-12 Alkermes, Inc. Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability
AU677216B2 (en) 1992-07-27 1997-04-17 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The Targeting of liposomes to the blood-brain barrier
GB9826174D0 (en) * 1998-11-30 1999-01-20 Celltech Therapeutics Ltd Chemical compounds
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
AU2001286930A1 (en) 2000-08-30 2002-03-13 The Board Of Trustees Of The Leland Stanford Junior University Glucocorticoid blocking agents for increasing blood-brain barrier permeability
US7034036B2 (en) 2000-10-30 2006-04-25 Pain Therapeutics, Inc. Inhibitors of ABC drug transporters at the blood-brain barrier
DE10121982B4 (de) 2001-05-05 2008-01-24 Lts Lohmann Therapie-Systeme Ag Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung
CA2450073C (en) 2001-07-25 2017-08-29 Biomarin Pharmaceutical Inc. Compositions and methods for modulating blood-brain barrier transport
US20030162695A1 (en) 2002-02-27 2003-08-28 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
JP4995423B2 (ja) 2002-12-03 2012-08-08 ブランシェット・ロックフェラー・ニューロサイエンスィズ・インスティテュート 物質を血液−脳関門を渡って輸送するための人工低密度リポタンパク質キャリア
WO2005025511A2 (en) 2003-09-10 2005-03-24 Cedars-Sinai Medical Center Potassium channel mediated delivery of agents through the blood-brain barrier
JP2009096764A (ja) * 2007-10-17 2009-05-07 Japan Tobacco Inc ピペリジン化合物及びそのhcvポリメラーゼ阻害剤としての利用
WO2010141805A1 (en) * 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of trpa1
JP2013028537A (ja) * 2009-11-11 2013-02-07 Dainippon Sumitomo Pharma Co Ltd N−ベンジルアミド誘導体およびそれを含有する医薬組成物
EP2520566A1 (en) * 2011-05-06 2012-11-07 Orion Corporation New Pharmaceutical Compounds
RU2603770C2 (ru) * 2014-11-28 2016-11-27 Федеральное государственное автономное образовательное учреждение высшего образования "Белгородский государственный национальный исследовательский университет" (НИУ "БелГУ") Замещенные пиразинопиримидиноны как блокаторы trpa1 каналов, фармацевтическая композиция, способы их получения и применения

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013108857A1 (ja) * 2012-01-17 2013-07-25 味の素株式会社 複素環アミド誘導体及びそれを含有する医薬

Also Published As

Publication number Publication date
RU2675792C2 (ru) 2018-12-25
PL3055302T3 (pl) 2019-05-31
US20160221945A1 (en) 2016-08-04
JP6735330B2 (ja) 2020-08-05
US20180118680A1 (en) 2018-05-03
US20200048197A1 (en) 2020-02-13
MX2016002368A (es) 2016-05-18
DK3055302T3 (en) 2019-03-18
PT3055302T (pt) 2019-02-26
ES2713323T3 (es) 2019-05-21
HRP20190329T1 (hr) 2019-04-19
SG11201609411SA (en) 2016-12-29
RU2016115868A (ru) 2017-11-17
EP3055302B1 (en) 2018-12-26
US11236046B2 (en) 2022-02-01
MX363457B (es) 2019-03-25
CN105612153A (zh) 2016-05-25
JP2016532673A (ja) 2016-10-20
BR112016002012A2 (pt) 2017-08-01
WO2015052264A1 (en) 2015-04-16
TR201902249T4 (tr) 2019-03-21
CA2917193A1 (en) 2015-04-16
EP3055302A1 (en) 2016-08-17
CN105612153B (zh) 2018-09-14
RS58376B1 (sr) 2019-04-30
RU2016115868A3 (enExample) 2018-06-25
HK1219478A1 (zh) 2017-04-07
JP2019065022A (ja) 2019-04-25
US20180282272A1 (en) 2018-10-04
TW201605795A (zh) 2016-02-16
KR20160064230A (ko) 2016-06-07
LT3055302T (lt) 2019-03-12
HUE041652T2 (hu) 2019-05-28
SI3055302T1 (sl) 2019-04-30

Similar Documents

Publication Publication Date Title
JP6735330B2 (ja) Trpa1調節因子として有用な置換複素環式スルホンアミド化合物
CN107922392B (zh) 1-(杂)芳基磺酰基-(吡咯烷或哌啶)-2-甲酰胺衍生物及其用途
JP2020500207A (ja) カルパインモジュレーター及びそれらの治療上の使用
CN105745209B (zh) 三唑并吡啶化合物、组合物及其使用方法
CN104619709A (zh) 作为tnf活性调节剂的咪唑并吡啶衍生物
WO2021139595A1 (zh) RORγt抑制剂及其制备方法和用途
TW202039474A (zh) 吡唑基-氨基-嘧啶基衍生物的苯甲醯胺及其組合物和方法
TW201211053A (en) Spiro compound and drug for activating adiponectin receptor
KR20240053589A (ko) 이중 기능성 키메라 헤테로 고리 화합물 및 이의 안드로겐 수용체 분해제로서의 용도
TW201734020A (zh) 布魯頓氏酪胺酸激酶抑制劑及其使用方法
CN117042769A (zh) 作为布鲁顿酪氨酸激酶(btk)降解剂的取代的吡咯并嘧啶和吡唑并嘧啶
KR20230123471A (ko) 화합물, 조성물 및 방법
CN108026105A (zh) TGFβ受体拮抗剂
CN112513021A (zh) RORγ拮抗剂及其在药物中的应用
CN115667259A (zh) 抑制h-pgds的稠环化合物
WO2021139599A1 (zh) RORγt抑制剂及其制备方法和用途
CN116917279A (zh) Btk抑制剂
HK1219478B (en) Substituted heterocyclic sulfonamide compounds useful as trpa1 modulators
HK40096088A (en) Heterocyclic compounds
HK40098678A (en) Substituted 1-aryl-1&#39;-heteroaryl compounds, substituted 1,1&#39;-biheteroaryl compounds, and methods using same
HK1251815B (en) 1-(het)arylsulfonyl-(pyrrolidine or piperidine)-2-carboxamide derivatives and their use

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees