KR102058853B1 - 지질화 펩타이드의 수용성 염과 이의 제조 방법 및 용도 - Google Patents

지질화 펩타이드의 수용성 염과 이의 제조 방법 및 용도 Download PDF

Info

Publication number
KR102058853B1
KR102058853B1 KR1020190023508A KR20190023508A KR102058853B1 KR 102058853 B1 KR102058853 B1 KR 102058853B1 KR 1020190023508 A KR1020190023508 A KR 1020190023508A KR 20190023508 A KR20190023508 A KR 20190023508A KR 102058853 B1 KR102058853 B1 KR 102058853B1
Authority
KR
South Korea
Prior art keywords
compound
acid
amorphous
formula
pharmaceutical composition
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.)
Active
Application number
KR1020190023508A
Other languages
English (en)
Korean (ko)
Other versions
KR20190103986A (ko
Inventor
강상욱
Original Assignee
브릿지바이오테라퓨틱스(주)
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 브릿지바이오테라퓨틱스(주) filed Critical 브릿지바이오테라퓨틱스(주)
Publication of KR20190103986A publication Critical patent/KR20190103986A/ko
Application granted granted Critical
Publication of KR102058853B1 publication Critical patent/KR102058853B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4891—Coated capsules; Multilayered drug free capsule shells
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846—Poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/02—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K19/00—Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C07K5/0823—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp and Pro-amino acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Analytical Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Immunology (AREA)
KR1020190023508A 2018-02-28 2019-02-27 지질화 펩타이드의 수용성 염과 이의 제조 방법 및 용도 Active KR102058853B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862636552P 2018-02-28 2018-02-28
US62/636,552 2018-02-28

Publications (2)

Publication Number Publication Date
KR20190103986A KR20190103986A (ko) 2019-09-05
KR102058853B1 true KR102058853B1 (ko) 2019-12-24

Family

ID=67684306

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020190023508A Active KR102058853B1 (ko) 2018-02-28 2019-02-27 지질화 펩타이드의 수용성 염과 이의 제조 방법 및 용도

Country Status (10)

Country Link
US (1) US11739120B2 (enExample)
EP (1) EP3759070A4 (enExample)
JP (2) JP7104141B2 (enExample)
KR (1) KR102058853B1 (enExample)
CN (1) CN110959002A (enExample)
MY (1) MY200470A (enExample)
PH (1) PH12020551233A1 (enExample)
SG (1) SG11202007544RA (enExample)
TW (2) TWI811767B (enExample)
WO (1) WO2019168357A1 (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102104507B1 (ko) * 2019-08-23 2020-04-24 브릿지바이오테라퓨틱스(주) 팔미토일-l-프롤릴-l-프롤릴-글리실-l-타이로신 나트륨을 포함하는 약제학적 제제 및 이의 제조방법
CN111297905B (zh) * 2020-03-18 2022-11-04 四川大学华西医院 一种基于皮肤前体细胞的提取物及其制备方法和用途

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1195762B (it) * 1980-10-13 1988-10-27 Reiner Alberto Real Sas Derivati idrosolubili della cefalexina e procedimento per la loro produzione
DE3839127A1 (de) 1988-11-19 1990-05-23 Hoechst Ag Pyrrolidon-2-carbonsaeure-derivate mit psychotroper wirkung
AUPM906594A0 (en) 1994-10-26 1994-11-17 Peptide Technology Limited Synthetic polyunsaturated fatty acid analogues
NZ332585A (en) 1996-05-01 2000-04-28 Ortho Mcneil Pharm Inc Carboxamide derivatives of pyrrolidine, piperidine and hexahydroazepine for the treatment of thrombosis disorders
ES2213985T3 (es) 1998-11-05 2004-09-01 Pfizer Products Inc. Derivados de hidroxiamida de acido 5-oxo-pirrolidin-2-carboxilico.
WO2003007876A2 (en) 2001-06-25 2003-01-30 University Of Massachusetts N-fatty acid-amino acid conjugates and therapeutic uses
WO2006113942A2 (en) 2005-04-20 2006-10-26 Schering Corporation Method of inhibiting cathepsin activity
US7842662B2 (en) 2006-11-10 2010-11-30 Cara Therapeutics, Inc. Synthetic peptide amide dimers
MX2010002300A (es) * 2007-08-29 2010-03-18 Pfizer Prod Inc Polimorfos de sal sodica del acido (3-(((4-terc-butil-bencil)-(pir idin-3-sulfonil)-amino)-metil)-fenoxi)-acetico o un hidrato de los mismos y procedimientos para fabricar los mismos.
WO2010059922A1 (en) * 2008-11-21 2010-05-27 Ligand Pharmaceuticals Incorporated Pyrrolidine carboxamide compounds
KR101151878B1 (ko) 2010-06-08 2012-05-31 미원상사주식회사 지방산 트리펩타이드염 및 이를 함유하는 항균 조성물
KR101348284B1 (ko) 2010-09-09 2014-01-03 주식회사 나이벡 인간 유래 세포 투과성 펩타이드와 생리활성 펩타이드 결합체 및 그 용도
KR20120048864A (ko) 2010-11-08 2012-05-16 주식회사 네오디엠 트리 펩타이드 유도체를 함유한 아토피 피부염 예방 및 치료용 조성물과 그 제조방법
KR20130038426A (ko) 2011-10-07 2013-04-18 성균관대학교산학협력단 지방산이 결합된 항당뇨 펩티드가 소수성 결합된 글리콜 키토산 히드로겔 및 이를 포함하는 당뇨병 예방 또는 치료용 약학적 조성물
KR101359886B1 (ko) 2011-12-28 2014-02-12 성균관대학교산학협력단 스매드 6번(Ｓｍａｄ６)으로부터 유래된 펩타이드를 유효성분으로 포함하는 패혈증 또는 패혈성 쇼크의 치료용 조성물
US20150368197A1 (en) * 2012-06-21 2015-12-24 Radikal Therapeutics Ins. Compositions and methods for treatment of inflammatory diseases of the lung
CN103724204B (zh) * 2013-11-27 2016-05-11 北京化工大学 一种水溶性引发剂及制备
NZ735250A (en) * 2015-07-08 2020-08-28 Research & Business Found Sungkyunkwan Univ Pyrrolidine carboxamido derivatives and methods for preparing and using the same

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
A. Serajuddin 등, Advanced Drug Delivery Reviews Vol.59, p.603-616 (2007.)*

Also Published As

Publication number Publication date
US20190263859A1 (en) 2019-08-29
TWI811767B (zh) 2023-08-11
MY200470A (en) 2023-12-27
KR20190103986A (ko) 2019-09-05
SG11202007544RA (en) 2020-09-29
EP3759070A1 (en) 2021-01-06
JP7104141B2 (ja) 2022-07-20
CN110959002A (zh) 2020-04-03
US11739120B2 (en) 2023-08-29
EP3759070A4 (en) 2021-12-08
TWI762770B (zh) 2022-05-01
JP2022106788A (ja) 2022-07-20
JP2020529435A (ja) 2020-10-08
PH12020551233A1 (en) 2021-05-17
TW202222818A (zh) 2022-06-16
WO2019168357A1 (en) 2019-09-06
TW201936577A (zh) 2019-09-16

Similar Documents

Publication Publication Date Title
KR102890565B1 (ko) 2-(3,5-디클로로-4-((5-이소프로필-6-옥소-1,6-디히드로피리다진-3-일)옥시)페닐)-3,5-디옥소-2,3,4,5-테트라히드로-1,2,4-트리아진-6-카르보니트릴의 고체 형태
JP5008777B2 (ja) （Ｒ）−５−［３−クロロ−４−（２，３−ジヒドロキシ−プロポキシ）−ベンズ［Ｚ］イリデン］−２−（［Ｚ］−プロピルイミノ）−３−ｏ−トリル−チアゾリジン−４−オンの結晶
AU2018281617A1 (en) Novel peptide and pharmaceutical composition for treatment of eye diseases comprising same novel peptide as active ingredient
EP3080141A1 (en) Solid form of abiraterone acetate
TW202432170A (zh) 相對於ｈｒａｓ及ｎｒａｓ具有選擇性之ｋｒａｓ抑制作用的環狀化合物
KR102058853B1 (ko) 지질화 펩타이드의 수용성 염과 이의 제조 방법 및 용도
WO2021233133A1 (zh) 用作ret激酶抑制剂的化合物及其应用
US11466008B2 (en) Co-crystals of neflamapimod (VX-745)
WO2023193563A1 (zh) 一种噻吩并吡啶化合物的晶型a、制备方法及其药物组合物
HK40025156A (en) Water soluble salts of lipidated peptides and methods for preparing and using the same
US11440908B2 (en) Crystalline forms of dasatinib
JP6392330B2 (ja) ポリペプチドワクチンの塩及びその製造方法と該塩を含有する医薬製品
EP3476843A1 (en) Pyrimidine compound, chloride salt thereof, and manufacturing and application of same
JP7517705B2 (ja) フロピリミジン化合物の塩および結晶形ならびにその医薬用途
HK40086425A (zh) 秋水仙碱衍生物的制备方法及其用途
JP2024545530A (ja) 縮合環誘導体の結晶形、その製造方法、及びその使用
KR20250139359A (ko) 인터류킨-23 수용체의 결정질 펩티드 억제제의 제조 방법
AU2025200217A1 (en) Systems and methods for preparing tailored radioactive isotope solutions
JP2023524622A (ja) ６－クロロ－７－（４－（４－クロロベンジル）ピペラジン－１－イル）－２－（１，３－ジメチル－１Ｈ－ピラゾール－４－イル）－３Ｈ－イミダゾ［４，５－ｂ］ピリジンの塩及び多形体
US20200016076A1 (en) Composition for the treatment of duchenne muscular dystrophy
EP4069674A1 (en) Crystalline form i of bucillamine
WO2019070698A1 (en) Novel forms of ibrutinib

Legal Events

Date Code Title Description
PA0109 Patent application

Patent event code: PA01091R01D

Comment text: Patent Application

Patent event date: 20190227

A201 Request for examination
A302 Request for accelerated examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20190425

Comment text: Request for Examination of Application

Patent event code: PA02011R01I

Patent event date: 20190227

Comment text: Patent Application

PA0302 Request for accelerated examination

Patent event date: 20190425

Patent event code: PA03022R01D

Comment text: Request for Accelerated Examination

Patent event date: 20190227

Patent event code: PA03021R01I

Comment text: Patent Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20190820

Patent event code: PE09021S01D

PG1501 Laying open of application
E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20191216

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20191218

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20191218

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
PR1001 Payment of annual fee

Payment date: 20221220

Start annual number: 4

End annual number: 4