AU2016344627B9 - 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 - Google Patents

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 Download PDF

Info

Publication number
AU2016344627B9
AU2016344627B9 AU2016344627A AU2016344627A AU2016344627B9 AU 2016344627 B9 AU2016344627 B9 AU 2016344627B9 AU 2016344627 A AU2016344627 A AU 2016344627A AU 2016344627 A AU2016344627 A AU 2016344627A AU 2016344627 B9 AU2016344627 B9 AU 2016344627B9
Authority
AU
Australia
Prior art keywords
methylamino
pyrimidine
pyrrolidin
cyclopropylmethyl
compound
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.)
Ceased
Application number
AU2016344627A
Other languages
English (en)
Other versions
AU2016344627A1 (en
AU2016344627B2 (en
Inventor
Helen BARKER
Wai Liu
Michael Yeadon
Zhijian Zhu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of AU2016344627A1 publication Critical patent/AU2016344627A1/en
Application granted granted Critical
Publication of AU2016344627B2 publication Critical patent/AU2016344627B2/en
Publication of AU2016344627B9 publication Critical patent/AU2016344627B9/en
Priority to AU2020200840A priority Critical patent/AU2020200840A1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • 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)
AU2016344627A 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 Ceased AU2016344627B9 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2020200840A AU2020200840A1 (en) 2015-10-26 2020-02-06 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

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2020200840A Division AU2020200840A1 (en) 2015-10-26 2020-02-06 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 (3)

Publication Number Publication Date
AU2016344627A1 AU2016344627A1 (en) 2018-05-10
AU2016344627B2 AU2016344627B2 (en) 2019-11-07
AU2016344627B9 true AU2016344627B9 (en) 2019-11-28

Family

ID=57200025

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2016344627A Ceased AU2016344627B9 (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
AU2020200840A Abandoned AU2020200840A1 (en) 2015-10-26 2020-02-06 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

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2020200840A Abandoned AU2020200840A1 (en) 2015-10-26 2020-02-06 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

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)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007072163A2 (en) * 2005-12-20 2007-06-28 Pfizer Limited Pyrimidine derivatives
WO2013182711A1 (en) * 2012-06-08 2013-12-12 Sensorion H4 receptor inhibitors for treating tinnitus

Family Cites Families (4)

* Cited by examiner, † Cited by third party
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
WO2007072163A2 (en) * 2005-12-20 2007-06-28 Pfizer Limited Pyrimidine derivatives
WO2013182711A1 (en) * 2012-06-08 2013-12-12 Sensorion H4 receptor inhibitors for treating tinnitus

Also Published As

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
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
CN108602801A (zh) 2018-09-28
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

Similar Documents

Publication Publication Date Title
AU2016344627B2 (en) 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
US11155533B2 (en) Crystalline forms and compositions of CFTR modulators
JP2018531288A6 (ja) ピリミジン組成物、超高純度組成物およびその塩、それを作成する方法、ならびにヒスタミンｈ４受容体（ｈ４）によって媒介される疾患および状態を治療するためにそれを用いる方法
EP2935249B1 (en) Autotaxin inhibitors
RU2526038C2 (ru) Тозилатная соль производного 5-пиразолил-2-пиридона, полезная в лечении copd
US9139570B2 (en) Solid forms of an antiviral compound
TW202229274A (zh) 用於治療發炎疾病之新穎塩類及其醫藥組合物
HUP0004586A2 (hu) Nyújtott hatóanyag-leadású tablettakészítmény Parkinson-kór kezelésére
JP2009531465A (ja) 中枢神経系障害の治療のための（２ｓ）−（４ｅ）−ｎ−メチル−５−［３−（５−イソプロポキシピリジン）イル］−４−ペンテン−２−アミンの多形形態
TW201305143A (zh) 光學活性吡唑基胺基喹唑啉及其醫藥組合物及使用方法
KR20260042158A (ko) 메닌 억제제를 포함하는 약학적 조성물
TWI875727B (zh) 有機化合物之結晶形及鹽型及其醫藥組合物
EP3999499B1 (en) Prodrugs in the modulation of interleukin
JP2013521289A (ja) フルオロウラシル誘導体
CN117043149A (zh) 促生长素抑制素调节剂的结晶形式
EP3849977B1 (en) Improved method for the manufacture of 3-[(1s)-1-imidazo[1,2-a]pyridin-6-ylethyl]-5-(1-methylpyrazol-4-yl)triazolo[4,5-b]pyrazine and polymorphic forms thereof
JP2026507424A (ja) 炎症性障害の治療のためのフマル酸塩を有する化合物１の薬学的組成物及び固体形態
EP3849970B1 (en) Crystalline (r)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl) piperazine-1-carboxylate, compositions and methods of use thereof
CN102666528A (zh) 晶体cdc7 抑制剂盐
EP4696689A1 (en) Salt form and crystal form of chiral heterocyclic compound having hedgehog pathway antagonist activity
WO2025147497A1 (en) Solid forms comprising (5r,6s)-10,11-difluoro-12-((2-fluoro-4-iodophenyl)amino)-5,6-dihydroxy-4,5,6,7-tetrahydro-1h-spiro[benzo[b][1,5,4]oxathiazecine-3,1'-cyclopropane] 2,2-dioxide, and compositions comprising and methods of using the same
HK40127025A (en) Parp1 inhibitors and uses thereof
HK40117292B (en) Parp1 inhibitors and uses thereof
HK40117292A (en) Parp1 inhibitors and uses thereof
HK40103623A (en) Kinase inhibitors and uses thereof

Legal Events

Date Code Title Description
SREP Specification republished
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired