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PE20130212A1 - Formas polimorficas de st-246 y metodos de preparacion - Google Patents

Formas polimorficas de st-246 y metodos de preparacion

Info

Publication number
PE20130212A1
PE20130212A1 PE2012001623A PE2012001623A PE20130212A1 PE 20130212 A1 PE20130212 A1 PE 20130212A1 PE 2012001623 A PE2012001623 A PE 2012001623A PE 2012001623 A PE2012001623 A PE 2012001623A PE 20130212 A1 PE20130212 A1 PE 20130212A1
Authority
PE
Peru
Prior art keywords
polymorphic forms
preparation methods
polymorphic
polymorphic form
2teta
Prior art date
Application number
PE2012001623A
Other languages
English (en)
Inventor
Shanthakumar R Tyavanagimatt
Melialani A C L Stone
William C Weimers
Dyland 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44656766&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20130212(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Siga Technologies Inc filed Critical Siga Technologies Inc
Publication of PE20130212A1 publication Critical patent/PE20130212A1/es

Links

Classifications

    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/12—Viral antigens
    • A61K39/275—Poxviridae, e.g. avipoxvirus
    • 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
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • C07D209/72—4,7-Endo-alkylene-iso-indoles
    • C07D209/76—4,7-Endo-alkylene-iso-indoles with oxygen atoms in positions 1 and 3
    • 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)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Immunology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Biotechnology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Inorganic Chemistry (AREA)

Abstract

SE REFIERE A FORMAS POLIMORFICAS DEL COMPUESTO 4-TRIFLUOROMETIL-N-(3,3a,4,4a,5,5a,6,6a-OCTAHIDRO-1,3-DIOXO-4,6-ETENOCICLOPROP[f]ISOINDOL-2(1H)-IL)-BENZAMIDA O ST-246 TAL COMO: A) LA FORMA POLIMORFICA I QUE MUESTRA UN PATRON DE DIFRACCION DE RAYOS X EN POLVO QUE TIENE PICOS A LOS ANGULOS DE REFLEXION 2TETA DE 7.63, 10.04, 11.47, 14.73, 15.21, 15.47, 16.06, 16.67, 16.98, 18.93, 19.96, 20.52, 20.79, 22.80, 25.16, ENTRE OTROS; B) LA FORMA POLIMORFICA III QUE MUESTRA UN PATRON DE DIFRACCION DE RAYOS X EN POLVO QUE TIENE PICOS A LOS ANGULOS DE REFLEXION 2TETA DE 6.71, 9.05, 12.49, 13.03, 13.79, 14.87, 15.72, 16.26, 16.74, 18.10, 18.43, 19.94, 21.04, 21.51, 23.15, ENTRE OTROS; C) LA FORMA POLIMORFICA IV; ENTRE OTROS. TAMBIEN SE REFIERE A PROCEDIMIENTOS DE PREPARACION Y COMPOSICIONES FARMACEUTICAS DE DICHAS FORMAS POLIMORFICAS. EL COMPUESTO ST-246 INHIBE UNA PROTEINA DEL ORTOPOXVIRUS
PE2012001623A 2010-03-23 2011-03-23 Formas polimorficas de st-246 y metodos de preparacion PE20130212A1 (es)

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
PE20130212A1 true PE20130212A1 (es) 2013-03-09

Family

ID=44656766

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2017000752A PE20170944A1 (es) 2010-03-23 2011-03-23 Formas polimorficas de st-246 y metodos de preparacion
PE2012001623A PE20130212A1 (es) 2010-03-23 2011-03-23 Formas polimorficas de st-246 y metodos de preparacion

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2017000752A PE20170944A1 (es) 2010-03-23 2011-03-23 Formas polimorficas de st-246 y metodos de preparacion

Country Status (20)

Country Link
US (8) US9339466B2 (es)
EP (1) EP2549871B1 (es)
JP (3) JP6018041B2 (es)
KR (6) KR20160028489A (es)
CN (4) CN105111130A (es)
AP (1) AP3221A (es)
AU (1) AU2011232551B2 (es)
BR (1) BR112012023743B1 (es)
CA (2) CA2793533C (es)
CL (1) CL2012002621A1 (es)
DK (1) DK2549871T3 (es)
FR (1) FR22C1023I2 (es)
IL (4) IL221991B (es)
MX (1) MX361428B (es)
NZ (1) NZ602578A (es)
PE (2) PE20170944A1 (es)
RU (2) RU2015146899A (es)
SG (2) SG184201A1 (es)
WO (1) WO2011119698A1 (es)
ZA (1) ZA201207141B (es)

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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
DK2549871T3 (en) * 2010-03-23 2018-12-10 Siga Tech Inc Polymorphic form ST-246 and processes for its preparation
CN104540508B (zh) 2012-08-16 2017-06-20 西佳技术公司 制备特考韦瑞的方法
CA3128535C (en) * 2013-07-19 2024-10-15 Siga Technologies, Inc. PREPARATION OF AMORPHIC TECOVIRIMAT
CN105636585B (zh) * 2013-11-19 2020-02-07 西佳技术公司 微粉化特考韦瑞一水化物的再水化
EP3197435A1 (en) * 2014-09-26 2017-08-02 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
CN108430469A (zh) 2016-02-16 2018-08-21 西加技术公司 St-246(特考韦瑞一水合物)混悬制剂
WO2018181924A1 (ja) 2017-03-31 2018-10-04 大阪瓦斯株式会社 電気化学素子、電気化学モジュール、固体酸化物形燃料電池、および製造方法
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
JP2024178477A (ja) * 2021-11-04 2024-12-25 興和株式会社 カプセル剤
JP2024178478A (ja) * 2021-11-04 2024-12-25 興和株式会社 医薬品

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DK2549871T3 (en) * 2010-03-23 2018-12-10 Siga Tech Inc Polymorphic form ST-246 and processes for its preparation

Also Published As

Publication number Publication date
US20160107993A1 (en) 2016-04-21
PE20170944A1 (es) 2017-07-13
CL2012002621A1 (es) 2013-10-11
CA2793533C (en) 2019-02-26
CA3030671A1 (en) 2011-09-29
US11890270B2 (en) 2024-02-06
DK2549871T3 (en) 2018-12-10
CN103068232A (zh) 2013-04-24
US20210137885A1 (en) 2021-05-13
FR22C1023I2 (fr) 2024-02-16
IL221991B (en) 2019-06-30
US20190343799A1 (en) 2019-11-14
CN103068232B (zh) 2015-08-26
SG184201A1 (en) 2012-10-30
RU2012144818A (ru) 2014-04-27
EP2549871A1 (en) 2013-01-30
KR20160028489A (ko) 2016-03-11
KR20170102070A (ko) 2017-09-06
US9744154B2 (en) 2017-08-29
US20260000644A1 (en) 2026-01-01
MX2012010859A (es) 2013-04-29
KR20160062208A (ko) 2016-06-01
ZA201207141B (en) 2016-06-29
BR112012023743B1 (pt) 2020-02-18
EP2549871B1 (en) 2018-08-22
IL241731A0 (en) 2015-11-30
US20180311213A1 (en) 2018-11-01
US10406137B2 (en) 2019-09-10
FR22C1023I1 (fr) 2022-07-22
JP2016040323A (ja) 2016-03-24
CN105175311A (zh) 2015-12-23
AP3221A (en) 2015-04-30
SG10201501936PA (en) 2015-05-28
US20180193308A1 (en) 2018-07-12
JP2018012735A (ja) 2018-01-25
WO2011119698A9 (en) 2013-01-31
NZ602578A (en) 2014-08-29
AU2011232551A1 (en) 2012-10-18
WO2011119698A1 (en) 2011-09-29
BR112012023743A2 (pt) 2015-09-15
US10045964B2 (en) 2018-08-14
US12433868B2 (en) 2025-10-07
EP2549871A4 (en) 2016-03-09
US20240156782A1 (en) 2024-05-16
US20110236434A1 (en) 2011-09-29
US10933050B2 (en) 2021-03-02
KR20150011016A (ko) 2015-01-29
MX361428B (es) 2018-12-06
JP6018041B2 (ja) 2016-11-02
IL258239A (en) 2018-05-31
JP2013522371A (ja) 2013-06-13
KR20150092354A (ko) 2015-08-12
KR20130018271A (ko) 2013-02-20
CN105111130A (zh) 2015-12-02
AP2012006514A0 (en) 2012-10-31
RU2015146899A (ru) 2019-01-11
US9339466B2 (en) 2016-05-17
AU2011232551B2 (en) 2014-11-13
CN105111131A (zh) 2015-12-02
CA2793533A1 (en) 2011-09-29
RU2578606C2 (ru) 2016-03-27
IL241730A0 (en) 2015-11-30

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