SG10201501936PA - Polymorphic forms st-246 and methods of preparation - Google Patents

Polymorphic forms st-246 and methods of preparation

Info

Publication number
SG10201501936PA
SG10201501936PA SG10201501936PA SG10201501936PA SG10201501936PA SG 10201501936P A SG10201501936P A SG 10201501936PA SG 10201501936P A SG10201501936P A SG 10201501936PA SG 10201501936P A SG10201501936P A SG 10201501936PA SG 10201501936P A SG10201501936P A SG 10201501936PA
Authority
SG
Singapore
Prior art keywords
preparation
methods
polymorphic forms
polymorphic
forms
Prior art date
Application number
SG10201501936PA
Other languages
English (en)
Inventor
Shanthakumar R Tyavanagimatt
Melialani A C L Stone
William C Weimers
Dylan Nelson
Tove C Bolken
Dennis E Hruby
Michael H O'neill
Gary Sweetapple
Kelley A Mccloughan
Original Assignee
Siga Technologies Inc
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 Siga Technologies Inc filed Critical Siga Technologies Inc
Publication of SG10201501936PA publication Critical patent/SG10201501936PA/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/58[b]- or [c]-condensed
    • C07D209/724,7-Endo-alkylene-iso-indoles
    • C07D209/764,7-Endo-alkylene-iso-indoles with oxygen atoms in positions 1 and 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035Isoindoles, e.g. phthalimide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/12Viral antigens
    • A61K39/275Poxviridae, e.g. avipoxvirus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/58[b]- or [c]-condensed
    • C07D209/70[b]- or [c]-condensed containing carbocyclic rings other than six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Mycology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Dermatology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Inorganic Chemistry (AREA)
SG10201501936PA 2010-03-23 2011-03-23 Polymorphic forms st-246 and methods of preparation SG10201501936PA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31674710P 2010-03-23 2010-03-23
US37303110P 2010-08-12 2010-08-12

Publications (1)

Publication Number Publication Date
SG10201501936PA true SG10201501936PA (en) 2015-05-28

Family

ID=44656766

Family Applications (2)

Application Number Title Priority Date Filing Date
SG2012070322A SG184201A1 (en) 2010-03-23 2011-03-23 Polymorphic forms st-246 and methods of preparation
SG10201501936PA SG10201501936PA (en) 2010-03-23 2011-03-23 Polymorphic forms st-246 and methods of preparation

Family Applications Before (1)

Application Number Title Priority Date Filing Date
SG2012070322A SG184201A1 (en) 2010-03-23 2011-03-23 Polymorphic forms st-246 and methods of preparation

Country Status (20)

Country Link
US (7) US9339466B2 (fr)
EP (1) EP2549871B1 (fr)
JP (3) JP6018041B2 (fr)
KR (6) KR20160062208A (fr)
CN (4) CN103068232B (fr)
AP (1) AP3221A (fr)
AU (1) AU2011232551B2 (fr)
BR (1) BR112012023743B1 (fr)
CA (2) CA3030671A1 (fr)
CL (1) CL2012002621A1 (fr)
DK (1) DK2549871T3 (fr)
FR (1) FR22C1023I2 (fr)
IL (4) IL221991B (fr)
MX (1) MX361428B (fr)
NZ (1) NZ602578A (fr)
PE (2) PE20130212A1 (fr)
RU (2) RU2015146899A (fr)
SG (2) SG184201A1 (fr)
WO (1) WO2011119698A1 (fr)
ZA (1) ZA201207141B (fr)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
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US8530509B2 (en) 2003-06-20 2013-09-10 Siga Technologies, Inc. Compounds, compositions and methods for treatment and prevention of orthopoxvirus infections and associated diseases
KR20160062208A (ko) * 2010-03-23 2016-06-01 시가 테크놀로지스, 인크. 다형체 형태 st―246 및 제조방법
AU2013302764B2 (en) * 2012-08-16 2017-12-21 Siga Technologies, Inc. Methods of preparing Tecovirimat
CN105307636A (zh) * 2013-07-19 2016-02-03 西佳技术公司 非晶形特考韦瑞制备
EP3043793B1 (fr) * 2013-11-19 2021-01-06 Siga Technologies Inc. Réhydratation de monohydrate de técovirimat micronisé
AU2015320358B2 (en) * 2014-09-26 2020-05-14 Millendo Therapeutics, Inc. Solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N'-((1-(4-(dimethylamino)phenyl)cyclopentyl) methyl)urea hydrochloride and compositions, methods and kits related thereto
EP3416637A4 (fr) 2016-02-16 2019-11-06 Siga Technologies, Inc. Formulations en suspension de st-246 (técovirimat monohydraté)
EP3605680A4 (fr) 2017-03-31 2021-01-13 Osaka Gas Co., Ltd. Élément électrochimique, module électrochimique, pile à combustible à oxyde solide et procédé de production
RU2716709C1 (ru) * 2019-08-20 2020-03-16 Федеральное бюджетное учреждение науки "Государственный научный центр вирусологии и биотехнологии "Вектор" Федеральной службы по надзору в сфере защиты прав потребителей и благополучия человека (ФБУН ГНЦ ВБ "Вектор" Роспотребнадзора) Пероральная лекарственная форма препарата в капсулах для лечения и профилактики заболеваний, вызываемых ортопоксвирусами
WO2023080188A1 (fr) * 2021-11-04 2023-05-11 興和株式会社 Capsule
WO2023080189A1 (fr) * 2021-11-04 2023-05-11 興和株式会社 Produit médicamenteux

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US4173646A (en) * 1974-10-04 1979-11-06 Merck & Co., Inc. Tricyclicdicarboximides
US4061763A (en) * 1975-05-09 1977-12-06 Merck & Co., Inc. Tricyclicdicarboximides
US5068356A (en) * 1990-02-20 1991-11-26 Atochem North America, Inc. Hindered phenolic n-(amido)imides
ZA939565B (en) 1993-12-21 1994-08-11 Applied Analytical Ind Inc Method for preparing low dose pharmaceutical products.
CA2396079A1 (fr) * 2000-01-07 2001-07-19 Transform Pharmaceuticals, Inc. Formation, identification et analyse a productivites elevees de formes solides diverses
AU2256702A (en) 2000-12-01 2002-06-11 Kyowa Hakko Kogyo Kk Composition improved in solubility or oral absorbability
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US7687641B2 (en) * 2003-06-20 2010-03-30 Siga Technologies, Inc. Chemicals, compositions, and methods for treatment and prevention of orthopoxvirus infections and associated diseases
US7737168B2 (en) 2003-06-20 2010-06-15 Siga Technologies, Inc. Compounds, compositions, and methods for treatment and prevention of orthopoxvirus infections and associated diseases
AU2004249250C1 (en) * 2003-06-20 2012-04-12 Siga Technologies, Inc. Compounds, compositions and methods for treatment and prevention of orthopoxvirus infections and associated diseases
US8530509B2 (en) 2003-06-20 2013-09-10 Siga Technologies, Inc. Compounds, compositions and methods for treatment and prevention of orthopoxvirus infections and associated diseases
US20070122471A1 (en) 2003-12-25 2007-05-31 Takeda Pharmaceutical Company Limited Method of improving suitability for granulation
DK1838670T3 (da) * 2004-12-09 2010-03-01 Zach System Spa Fremgangsmåde til fremstilling af carvedilol og dets enantiomere
US8642577B2 (en) * 2005-04-08 2014-02-04 Chimerix, Inc. Compounds, compositions and methods for the treatment of poxvirus infections
AP2267A (en) 2006-03-02 2011-08-02 Siga Technologies Inc Antiviral drugs for treatment of arenavirus infection.
EP3006425A1 (fr) 2007-04-23 2016-04-13 Siga Technologies, Inc. Composition pharmaceutique destinees au traitement et a la prévention d'une infection causée par des orthopoxvirus
CN101445478B (zh) * 2008-08-22 2011-04-06 中国人民解放军军事医学科学院生物工程研究所 含一个结晶水的化合物st-246及其晶体与制备方法
RU2412160C1 (ru) * 2009-09-25 2011-02-20 Федеральное государственное учреждение науки "Государственный научный центр вирусологии и биотехнологии "Вектор" Федеральной службы по надзору в сфере защиты прав потребителей и благополучия человека (ФГУН ГНЦ ВБ "Вектор" Роспотребнадзора) 7-[n'-(4-трифторметилбензоил)-гидразинокарбонил]-трицикло[3.2.2.02,4]нон-8-ен-6-карбоновая кислота, обладающая противовирусной активностью
KR20160062208A (ko) * 2010-03-23 2016-06-01 시가 테크놀로지스, 인크. 다형체 형태 st―246 및 제조방법

Also Published As

Publication number Publication date
US20240156782A1 (en) 2024-05-16
RU2015146899A (ru) 2019-01-11
MX361428B (es) 2018-12-06
KR20160028489A (ko) 2016-03-11
FR22C1023I1 (fr) 2022-07-22
US9744154B2 (en) 2017-08-29
US10045964B2 (en) 2018-08-14
CA2793533C (fr) 2019-02-26
CN103068232B (zh) 2015-08-26
KR20130018271A (ko) 2013-02-20
CN105111131A (zh) 2015-12-02
WO2011119698A9 (fr) 2013-01-31
SG184201A1 (en) 2012-10-30
AU2011232551B2 (en) 2014-11-13
FR22C1023I2 (fr) 2024-02-16
US20180193308A1 (en) 2018-07-12
US11890270B2 (en) 2024-02-06
CA2793533A1 (fr) 2011-09-29
US20210137885A1 (en) 2021-05-13
PE20170944A1 (es) 2017-07-13
AP3221A (en) 2015-04-30
EP2549871B1 (fr) 2018-08-22
IL258239A (en) 2018-05-31
CL2012002621A1 (es) 2013-10-11
US10406137B2 (en) 2019-09-10
US20110236434A1 (en) 2011-09-29
KR20150092354A (ko) 2015-08-12
WO2011119698A1 (fr) 2011-09-29
RU2012144818A (ru) 2014-04-27
EP2549871A4 (fr) 2016-03-09
EP2549871A1 (fr) 2013-01-30
US10933050B2 (en) 2021-03-02
MX2012010859A (es) 2013-04-29
US20160107993A1 (en) 2016-04-21
JP2016040323A (ja) 2016-03-24
CN103068232A (zh) 2013-04-24
US20180311213A1 (en) 2018-11-01
RU2578606C2 (ru) 2016-03-27
IL221991B (en) 2019-06-30
US20190343799A1 (en) 2019-11-14
CA3030671A1 (fr) 2011-09-29
IL241731A0 (en) 2015-11-30
JP2013522371A (ja) 2013-06-13
AP2012006514A0 (en) 2012-10-31
BR112012023743B1 (pt) 2020-02-18
JP2018012735A (ja) 2018-01-25
JP6018041B2 (ja) 2016-11-02
IL241730A0 (en) 2015-11-30
CN105111130A (zh) 2015-12-02
CN105175311A (zh) 2015-12-23
AU2011232551A1 (en) 2012-10-18
KR20150011016A (ko) 2015-01-29
KR20160062208A (ko) 2016-06-01
DK2549871T3 (en) 2018-12-10
PE20130212A1 (es) 2013-03-09
BR112012023743A2 (pt) 2015-09-15
ZA201207141B (en) 2016-06-29
KR20170102070A (ko) 2017-09-06
US9339466B2 (en) 2016-05-17
NZ602578A (en) 2014-08-29

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