TW202328116A - 含芳環類生物拮抗劑、其製備方法及應用 - Google Patents

含芳環類生物拮抗劑、其製備方法及應用 Download PDF

Info

Publication number
TW202328116A
TW202328116A TW111132297A TW111132297A TW202328116A TW 202328116 A TW202328116 A TW 202328116A TW 111132297 A TW111132297 A TW 111132297A TW 111132297 A TW111132297 A TW 111132297A TW 202328116 A TW202328116 A TW 202328116A
Authority
TW
Taiwan
Prior art keywords
alkyl
aryl
cycloalkyl
haloalkyl
alkenyl
Prior art date
Application number
TW111132297A
Other languages
English (en)
Chinese (zh)
Inventor
肖華玲
董加強
陸幸運
劉強
Original Assignee
大陸商上海翰森生物醫藥科技有限公司
大陸商江蘇豪森藥業集團有限公司
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 大陸商上海翰森生物醫藥科技有限公司, 大陸商江蘇豪森藥業集團有限公司 filed Critical 大陸商上海翰森生物醫藥科技有限公司
Publication of TW202328116A publication Critical patent/TW202328116A/zh

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not 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
    • A61K31/41—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
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic 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
    • A61K31/41—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
    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • 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
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW111132297A 2021-08-26 2022-08-26 含芳環類生物拮抗劑、其製備方法及應用 TW202328116A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN202110988568 2021-08-26
CN202110988568.9 2021-08-26
CN202210633028 2022-06-06
CN202210633028.3 2022-06-06

Publications (1)

Publication Number Publication Date
TW202328116A true TW202328116A (zh) 2023-07-16

Family

ID=85322470

Family Applications (1)

Application Number Title Priority Date Filing Date
TW111132297A TW202328116A (zh) 2021-08-26 2022-08-26 含芳環類生物拮抗劑、其製備方法及應用

Country Status (10)

Country Link
US (1) US20240368123A1 (https=)
EP (1) EP4393920A4 (https=)
JP (1) JP2024534111A (https=)
KR (1) KR20240051999A (https=)
CN (1) CN117836294A (https=)
AU (1) AU2022334402A1 (https=)
CA (1) CA3229397A1 (https=)
MX (1) MX2024002411A (https=)
TW (1) TW202328116A (https=)
WO (1) WO2023025277A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN118119617A (zh) * 2021-10-21 2024-05-31 年衍药业（上海）有限公司 一种双重拮抗剂及其用途
WO2025094214A1 (en) * 2023-11-02 2025-05-08 Msn Laboratories Private Limited, R&D Center Process for the preparation of 2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-(ethoxymethyl)phenyl]-N-(4,5-dimethyl-1,2-oxazol-3-yl) benzenesulfonamide and its intermediates thereof
IT202400000246A1 (it) * 2024-01-09 2025-07-09 Procos Spa Processo per la preparazione di sparsentan
WO2026021516A1 (zh) * 2024-07-25 2026-01-29 深圳信立泰药业股份有限公司 一种取代的血管紧张肽和内皮肽受体拮抗剂及其应用
WO2026067819A1 (zh) * 2024-09-30 2026-04-02 江苏豪森药业集团有限公司 含芳环类生物拮抗剂在制备治疗或预防肾脏疾病药物中的应用
CN119462631A (zh) * 2024-10-09 2025-02-18 广东莱佛士制药技术有限公司 一种司巴生坦中间体的合成方法

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2494792A (en) * 1991-08-19 1993-03-16 E.I. Du Pont De Nemours And Company Angiotensin ii receptor blocking imidazolinone derivatives
HUP0104634A3 (en) * 1998-07-06 2002-11-28 Bristol Myers Squibb Co Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists
US6638937B2 (en) * 1998-07-06 2003-10-28 Bristol-Myers Squibb Co. Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists
ATE339417T1 (de) * 1999-12-15 2006-10-15 Bristol Myers Squibb Co Biphenyl - sulfonamide als duale angiotensin - endothelin - rezeptor - antagonisten
ES2259909B1 (es) * 2005-02-28 2007-06-16 Inke, S.A. Procedimiento para la obtencion de un compuesto farmaceuticamente activo y de su intermedio de sintesis.
EP1996588A4 (en) * 2006-03-03 2011-10-05 Torrent Pharmaceuticals Ltd NEW DUAL ACTION RECEPTOR (DARA) ANTAGONISTS OF ATI AND ETA RECEPTORS
WO2007109456A2 (en) * 2006-03-16 2007-09-27 Pharmacopeia, Inc. Substituted biphenyl isoxazole sulfonamides as dual angiotensin endothelin receptor antagonists
US20080103312A1 (en) * 2006-08-29 2008-05-01 Kansal Vinod K Processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole
EP2297113A1 (en) * 2008-04-29 2011-03-23 Theravance, Inc. Dual-acting antihypertensive agents
WO2010114801A1 (en) * 2009-03-31 2010-10-07 Ligand Pharmaceuticals Inc. Oral formulations of diphenylsulfonamide endothelin and angiotensin ii receptor agonists to treat elevated blood pressure and diabetic nephropathy
WO2010135350A2 (en) 2009-05-20 2010-11-25 Pharmacopeia, Llc Biphenyl intermediate compounds and methods for the preparation of a dual angiotensin ii and endothelin a receptor antagonist
CN104761548B (zh) * 2015-04-27 2017-09-12 梯尔希（南京）药物研发有限公司 一种稳定同位素标记的二苯基磺酰胺类药物的制备方法
ES2984389T3 (es) * 2016-06-29 2024-10-29 Univ Montreal Heterociclos de biarilmetilo
CN117017985A (zh) 2016-10-13 2023-11-10 特拉维尔治疗公司 用于治疗肾脏疾病或病症的联苯磺酰胺化合物
CN112876424B (zh) * 2019-11-29 2023-06-30 上海拓界生物医药科技有限公司 血管紧张素ii受体及内皮素受体双重拮抗剂
CN118119617A (zh) * 2021-10-21 2024-05-31 年衍药业（上海）有限公司 一种双重拮抗剂及其用途
JP2024178482A (ja) * 2021-11-15 2024-12-25 株式会社アークメディスン 化合物、アンジオテンシンｉｉタイプ１受容体拮抗剤及び医薬組成物

Also Published As

Publication number Publication date
US20240368123A1 (en) 2024-11-07
EP4393920A1 (en) 2024-07-03
JP2024534111A (ja) 2024-09-18
KR20240051999A (ko) 2024-04-22
WO2023025277A1 (zh) 2023-03-02
AU2022334402A1 (en) 2024-02-22
CA3229397A1 (en) 2023-03-02
MX2024002411A (es) 2024-04-05
CN117836294A (zh) 2024-04-05
EP4393920A4 (en) 2025-12-24

Similar Documents

Publication Publication Date Title
TW202328116A (zh) 含芳環類生物拮抗劑、其製備方法及應用
CN102834382B (zh) 作为钙释放激活钙通道调节剂的吡唑衍生物
CN102271682B (zh) 用于治疗疼痛的p2x3受体拮抗剂
ES2314922T3 (es) N-arilpirrolidinas sustituidas como moduladores selectivos del receptor de androgenos.
CN102639500B (zh) 三环化合物、其制备方法及其在医药上的应用
JP2020023577A (ja) Ｇｐｒ１２０アゴニストとしてのビアリール誘導体
TW201835072A (zh) 新穎cyp11a1抑制劑
JP2022548028A (ja) Ｍａｇｌ阻害剤としての４，４ａ，５，７，８，８ａ－ヘキサピリド［４，３－ｂ］［１，４］オキサジン－３－オン化合物
CN105143206A (zh) 用于治疗癌症的嘧啶-2,4-二胺衍生物
TW201038586A (en) Sulfonamide derivatives
JP2006316054A (ja) 高コンダクタンス型カルシウム感受性ｋチャネル開口薬
WO2009058298A1 (en) P2x3, receptor antagonists for treatment of pain
TW201734001A (zh) ＲＯＲ－γ調節劑
JP2019508445A (ja) ピリミジンおよびそのバリアント、ならびにそのための使用
WO2012020820A1 (ja) ヘテロアリール－ピラゾール誘導体
CN111196804A (zh) TGF-βR1抑制剂及其应用
CA2938198A1 (en) Heterocyclic sulfonamide derivative and medicine comprising same
CN117794898A (zh) 3-吡咯基磺酰胺化合物作为gpr17拮抗剂
CN113727973B (zh) 可用作类法尼醇x受体调节剂的取代酰胺化合物
KR20150130413A (ko) 오렉신 수용체 길항제로서의 아제티딘 아미드 유도체
CN119798233A (zh) 一种at2r拮抗剂及其用途
TW202220990A (zh) 雜芳基取代的螺哌啶基衍生物及其藥物用途
EP1675585A2 (en) Large conductance calcium-activated k channel opener
CN116675684B (zh) 含炔基稠环类衍生物拮抗剂、其制备方法和应用
HUE026652T2 (en) Indole derivatives