CN116637077A - 包含sGC刺激剂的固体分散体 - Google Patents

包含sGC刺激剂的固体分散体 Download PDF

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Publication number
CN116637077A
CN116637077A CN202310714725.6A CN202310714725A CN116637077A CN 116637077 A CN116637077 A CN 116637077A CN 202310714725 A CN202310714725 A CN 202310714725A CN 116637077 A CN116637077 A CN 116637077A
Authority
CN
China
Prior art keywords
compound
dispersion
solid dispersion
disease
amorphous
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.)
Pending
Application number
CN202310714725.6A
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English (en)
Chinese (zh)
Inventor
C·A·顿巴尔
V·塞瑟拉曼
A·哈沙什
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.)
Cyclone Therapy Co ltd
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Cyclone Therapy Co ltd
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Filing date
Publication date
Application filed by Cyclone Therapy Co ltd filed Critical Cyclone Therapy Co ltd
Publication of CN116637077A publication Critical patent/CN116637077A/zh
Pending legal-status Critical Current

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    • 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
    • A61K9/14—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
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • 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
    • A61K9/14—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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202310714725.6A 2015-11-30 2016-11-22 包含sGC刺激剂的固体分散体 Pending CN116637077A (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201562260910P 2015-11-30 2015-11-30
US62/260,910 2015-11-30
US201662359440P 2016-07-07 2016-07-07
US62/359,440 2016-07-07
PCT/US2016/063312 WO2017095697A1 (en) 2015-11-30 2016-11-22 Solid dispersions comprising a sgc stimulator
CN201680077389.7A CN108883071A (zh) 2015-11-30 2016-11-22 包含sGC刺激剂的固体分散体

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201680077389.7A Division CN108883071A (zh) 2015-11-30 2016-11-22 包含sGC刺激剂的固体分散体

Publications (1)

Publication Number Publication Date
CN116637077A true CN116637077A (zh) 2023-08-25

Family

ID=57590822

Family Applications (4)

Application Number Title Priority Date Filing Date
CN202310714725.6A Pending CN116637077A (zh) 2015-11-30 2016-11-22 包含sGC刺激剂的固体分散体
CN201680077389.7A Pending CN108883071A (zh) 2015-11-30 2016-11-22 包含sGC刺激剂的固体分散体
CN202310714714.8A Pending CN116942616A (zh) 2015-11-30 2016-11-22 包含sGC刺激剂的固体分散体
CN202310714716.7A Pending CN116637076A (zh) 2015-11-30 2016-11-22 包含sGC刺激剂的固体分散体

Family Applications After (3)

Application Number Title Priority Date Filing Date
CN201680077389.7A Pending CN108883071A (zh) 2015-11-30 2016-11-22 包含sGC刺激剂的固体分散体
CN202310714714.8A Pending CN116942616A (zh) 2015-11-30 2016-11-22 包含sGC刺激剂的固体分散体
CN202310714716.7A Pending CN116637076A (zh) 2015-11-30 2016-11-22 包含sGC刺激剂的固体分散体

Country Status (12)

Country Link
US (4) US20190269619A1 (enExample)
EP (1) EP3383372B1 (enExample)
JP (3) JP6952707B2 (enExample)
KR (1) KR102841419B1 (enExample)
CN (4) CN116637077A (enExample)
AU (1) AU2016364976B2 (enExample)
BR (1) BR112018011154B1 (enExample)
CA (1) CA3006746C (enExample)
EA (1) EA201891315A1 (enExample)
IL (2) IL259493B (enExample)
MX (3) MX389961B (enExample)
WO (1) WO2017095697A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3012001A1 (en) 2016-02-01 2017-08-10 Ironwood Pharmaceuticals, Inc. Use of sgc stimulators for the treatment of nonalcoholic steatohepatitis (nash)
SG10202100168XA (en) * 2016-07-07 2021-02-25 Cyclerion Therapeutics Inc Novel processes for preparation of soluble guanylate cyclase stimulators
ES2963563T3 (es) * 2016-07-07 2024-03-27 Cyclerion Therapeutics Inc Procesos novedosos para preparar estimuladores de guanilato ciclasa soluble
WO2019055859A1 (en) 2017-09-14 2019-03-21 Ironwood Pharmaceuticals, Inc. TREATMENT OF METABOLIC SYNDROME BY SGC STIMULATOR
WO2019161534A1 (en) * 2018-02-22 2019-08-29 Ironwood Pharmaceuticals, Inc. Novel processes and intermediates for preparation of soluble guanylate cyclase stimulators
EP4249469A3 (en) * 2018-01-10 2023-12-27 Cyclerion Therapeutics, Inc. Novel processes and intermediates for the preparation of soluble guanylate cyclase stimulators
WO2019172420A1 (ja) * 2018-03-09 2019-09-12 協和発酵キリン株式会社 医薬組成物
JP7503781B2 (ja) * 2018-07-30 2024-06-21 株式会社リコー 粒子の製造方法、並びに、それにより製造された粒子及び医薬
WO2020027030A1 (en) * 2018-07-30 2020-02-06 Ricoh Company, Ltd. Method for producing particle, and particle produced by the method and medicament
WO2021056048A1 (en) * 2019-09-23 2021-04-01 Bionomics Limited Therapeutic formulations and uses thereof
JP7730810B2 (ja) 2019-10-29 2025-08-28 サイクレリオン・セラピューティクス，インコーポレーテッド ｓＧＣ刺激剤による糖尿病性腎症の処置
US20240000769A1 (en) * 2020-12-18 2024-01-04 UCB Biopharma SRL Amorphous solid dispersions
US20240366596A1 (en) 2021-07-28 2024-11-07 Cyclerion Therapeutics, Inc. Treatment of hfpef in post-menopausal women with an sgc stimulator

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014144100A2 (en) * 2013-03-15 2014-09-18 Takashi Nakai Sgc stimulators

Family Cites Families (5)

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DK0901786T3 (da) * 1997-08-11 2007-10-08 Pfizer Prod Inc Faste farmaceutiske dispersioner med foröget biotilgængelighed
EP1027886B1 (en) * 1999-02-10 2008-07-09 Pfizer Products Inc. Pharmaceutical solid dispersions
EP2654726A1 (en) * 2011-03-08 2013-10-30 Zalicus Pharmaceuticals Ltd. Solid dispersion formulations and methods of use thereof
US9309235B2 (en) * 2012-09-18 2016-04-12 Ironwood Pharmaceuticals, Inc. SGC stimulators
EP3094327A1 (en) * 2014-01-13 2016-11-23 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2014144100A2 (en) * 2013-03-15 2014-09-18 Takashi Nakai Sgc stimulators

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
FRIESEN D.T.等: "Hydroxypropyl Methylcellulose Acetate Succinate-Based Spray-Dried Dispersions: An Overview", MOLECULAR PHARMACEUTICS, vol. 5, no. 6, 1 December 2008 (2008-12-01), pages 1003 - 1019 *
LEUNER, C等: "Improving drug solubility for oral delivery using solid dispersions", EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTIC, vol. 50, no. 1, 3 July 2000 (2000-07-03), pages 47 - 60 *

Also Published As

Publication number Publication date
AU2016364976A1 (en) 2018-06-14
US20250017862A1 (en) 2025-01-16
EA201891315A1 (ru) 2018-12-28
MX389961B (es) 2025-03-20
IL290338B2 (en) 2023-05-01
JP7641320B2 (ja) 2025-03-06
AU2016364976B2 (en) 2022-08-25
BR112018011154B1 (pt) 2023-09-26
CN116942616A (zh) 2023-10-27
US20190269619A1 (en) 2019-09-05
US20240293324A1 (en) 2024-09-05
EP3383372B1 (en) 2023-11-01
CA3006746A1 (en) 2017-06-08
MX2022001655A (es) 2022-03-11
JP2023100851A (ja) 2023-07-19
MX2022001656A (es) 2022-03-11
WO2017095697A1 (en) 2017-06-08
CN116637076A (zh) 2023-08-25
IL290338A (en) 2022-04-01
EP3383372A1 (en) 2018-10-10
JP2019501216A (ja) 2019-01-17
JP7277534B2 (ja) 2023-05-19
CN108883071A (zh) 2018-11-23
KR102841419B1 (ko) 2025-08-01
CA3006746C (en) 2024-01-30
JP2022000464A (ja) 2022-01-04
IL259493A (en) 2018-07-31
KR20180086497A (ko) 2018-07-31
IL259493B (en) 2022-03-01
JP6952707B2 (ja) 2021-10-20
BR112018011154A2 (pt) 2018-11-21
IL290338B1 (en) 2023-01-01
US20250255821A1 (en) 2025-08-14

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