CN108602801A - 嘧啶组合物，超纯组合物及其盐，其制造方法，和其用于治疗组胺h4受体(h4)介导的疾病和病症的方法 - Google Patents

嘧啶组合物，超纯组合物及其盐，其制造方法，和其用于治疗组胺h4受体(h4)介导的疾病和病症的方法 Download PDF

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Publication number
CN108602801A
CN108602801A CN201680076200.2A CN201680076200A CN108602801A CN 108602801 A CN108602801 A CN 108602801A CN 201680076200 A CN201680076200 A CN 201680076200A CN 108602801 A CN108602801 A CN 108602801A
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CN
China
Prior art keywords
composition
dosage form
pyrimidine
methylamino
disease
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Pending
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CN201680076200.2A
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English (en)
Chinese (zh)
Inventor
Z·朱
H·巴克
M·伊登
W·刘
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Novartis AG
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Novartis AG
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Publication of CN108602801A publication Critical patent/CN108602801A/zh
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    • 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
    • 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
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61K9/2095—Tabletting processes
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pulmonology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201680076200.2A 2015-10-26 2016-10-25 嘧啶组合物，超纯组合物及其盐，其制造方法，和其用于治疗组胺h4受体(h4)介导的疾病和病症的方法 Pending CN108602801A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201562246482P 2015-10-26 2015-10-26
US62/246,482 2015-10-26
US201662329091P 2016-04-28 2016-04-28
US62/329,091 2016-04-28
US201662359066P 2016-07-06 2016-07-06
US62/359,066 2016-07-06
PCT/EP2016/075708 WO2017072131A1 (en) 2015-10-26 2016-10-25 Pyrimidine compositions, ultra-pure compositions and salts thereof, methods of making the same, and methods of using the same for treating histamine h4 receptor (h4) mediated diseases and conditions

Publications (1)

Publication Number Publication Date
CN108602801A true CN108602801A (zh) 2018-09-28

Family

ID=57200025

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680076200.2A Pending CN108602801A (zh) 2015-10-26 2016-10-25 嘧啶组合物，超纯组合物及其盐，其制造方法，和其用于治疗组胺h4受体(h4)介导的疾病和病症的方法

Country Status (21)

Country Link
US (2) US20170158671A1 (enExample)
EP (1) EP3368528A1 (enExample)
JP (1) JP2018531288A (enExample)
KR (1) KR20180067683A (enExample)
CN (1) CN108602801A (enExample)
AU (2) AU2016344627B9 (enExample)
BR (1) BR112018007765A2 (enExample)
CA (1) CA3001636A1 (enExample)
CL (1) CL2018001092A1 (enExample)
CO (1) CO2018004323A2 (enExample)
EC (1) ECSP18038867A (enExample)
HK (1) HK1252050A1 (enExample)
IL (1) IL258813A (enExample)
MX (1) MX2018005140A (enExample)
PE (1) PE20181364A1 (enExample)
PH (1) PH12018500822A1 (enExample)
RU (1) RU2018119104A (enExample)
SG (1) SG11201802676QA (enExample)
TW (1) TW201729810A (enExample)
WO (1) WO2017072131A1 (enExample)
ZA (1) ZA201802183B (enExample)

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Publication number Priority date Publication date Assignee Title
US10704021B2 (en) 2012-03-15 2020-07-07 Flodesign Sonics, Inc. Acoustic perfusion devices
CN105939767B (zh) 2014-01-08 2018-04-06 弗洛设计声能学公司 具有双声电泳腔的声电泳装置
US11377651B2 (en) 2016-10-19 2022-07-05 Flodesign Sonics, Inc. Cell therapy processes utilizing acoustophoresis
US11708572B2 (en) 2015-04-29 2023-07-25 Flodesign Sonics, Inc. Acoustic cell separation techniques and processes
US11214789B2 (en) 2016-05-03 2022-01-04 Flodesign Sonics, Inc. Concentration and washing of particles with acoustics
US10093731B2 (en) 2017-02-24 2018-10-09 Kindred Biosciences, Inc. Anti-IL31 antibodies for veterinary use
AU2018349284B2 (en) * 2017-10-09 2023-11-16 428 Pharma BV. New salt and solid state forms of escitalopram
CN114900773A (zh) 2017-12-14 2022-08-12 弗洛设计声能学公司 声泳系统及其操作方法、控制声换能器及声学系统的方法
JP7671275B2 (ja) 2019-08-29 2025-05-01 エランコ・ユーエス・インコーポレイテッド 動物用の抗ｉｌ３１抗体
US12102622B2 (en) 2021-02-10 2024-10-01 Iolyx Therapeutics, Inc. Methods for ophthalmic delivery of roflumilast
US12263160B2 (en) 2021-09-22 2025-04-01 Iolyx Therapeutics, Inc. Methods of treating ocular inflammatory diseases

Citations (2)

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CN101341134A (zh) * 2005-12-20 2009-01-07 辉瑞股份有限公司 嘧啶衍生物
WO2013182711A1 (en) * 2012-06-08 2013-12-12 Sensorion H4 receptor inhibitors for treating tinnitus

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Publication number Priority date Publication date Assignee Title
WO2002072548A2 (en) 2001-03-09 2002-09-19 Ortho-Mcneil Pharmaceutical, Inc. Heterocyclic compounds and their use as histamine h4 ligands.
AU2003272285A1 (en) 2002-09-06 2004-03-29 Janssen Pharmaceutica, N.V. Thienopyrrolyl and furanopyrrolyl compounds and their use as histamine h4 receptor ligands
KR101235116B1 (ko) * 2005-10-17 2013-02-20 에스케이케미칼주식회사 광학활성 암로디핀 겐티세이트 염의 제조방법
JP2008127359A (ja) * 2006-11-22 2008-06-05 Kowa Co アトピー性皮膚炎の予防及び／又は治療剤

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101341134A (zh) * 2005-12-20 2009-01-07 辉瑞股份有限公司 嘧啶衍生物
WO2013182711A1 (en) * 2012-06-08 2013-12-12 Sensorion H4 receptor inhibitors for treating tinnitus

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CHARLES E. MOWBRAY等: "Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: A novel histamine H4 receptor antagonist", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *

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Publication number Publication date
JP2018531288A (ja) 2018-10-25
US20170158671A1 (en) 2017-06-08
AU2016344627A1 (en) 2018-05-10
TW201729810A (zh) 2017-09-01
AU2020200840A1 (en) 2020-02-27
CL2018001092A1 (es) 2018-08-10
PH12018500822A1 (en) 2018-10-01
PE20181364A1 (es) 2018-08-27
ZA201802183B (en) 2019-02-27
HK1252050A1 (zh) 2019-05-10
RU2018119104A (ru) 2019-11-28
AU2016344627B9 (en) 2019-11-28
RU2018119104A3 (enExample) 2020-02-19
CA3001636A1 (en) 2017-05-04
KR20180067683A (ko) 2018-06-20
AU2016344627B2 (en) 2019-11-07
EP3368528A1 (en) 2018-09-05
WO2017072131A1 (en) 2017-05-04
CO2018004323A2 (es) 2018-07-19
MX2018005140A (es) 2018-05-07
US20190135787A1 (en) 2019-05-09
ECSP18038867A (es) 2018-05-31
BR112018007765A2 (pt) 2018-10-23
SG11201802676QA (en) 2018-05-30
IL258813A (en) 2018-06-28

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