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AR129504A2 - Hidrato de diclorhidrato de omecamtiv mecarbil, formas cristalinas, y composiciones farmacéuticas - Google Patents

Hidrato de diclorhidrato de omecamtiv mecarbil, formas cristalinas, y composiciones farmacéuticas

Info

Publication number
AR129504A2
AR129504A2 ARP230101396A ARP230101396A AR129504A2 AR 129504 A2 AR129504 A2 AR 129504A2 AR P230101396 A ARP230101396 A AR P230101396A AR P230101396 A ARP230101396 A AR P230101396A AR 129504 A2 AR129504 A2 AR 129504A2
Authority
AR
Argentina
Prior art keywords
dihydrochloride hydrate
omecamtiv mecarbil
mecarbil dihydrochloride
omecamtiv
crystalline form
Prior art date
Application number
ARP230101396A
Other languages
English (en)
Inventor
Mingda Bi
Robert Kuehl
Original Assignee
Amgen Inc
Cytokinetics 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=50549466&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR129504(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Amgen Inc, Cytokinetics Inc filed Critical Amgen Inc
Publication of AR129504A2 publication Critical patent/AR129504A2/es

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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Inorganic Chemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicación 1: Hidrato de diclorhidrato de omecamtiv mecarbil. Reivindicación 2: El hidrato de diclorhidrato de omecamtiv mecarbil de la reivindicación 1, caracterizado porque el hidrato de diclorhidrato de omecamtiv mecarbil es un monohidrato. Reivindicación 3: Una forma cristalina del hidrato de diclorhidrato de omecamtiv mecarbil de la reivindicación 1, caracterizada porque la forma cristalina se caracteriza por un patrón de difracción en polvo de rayos X que comprende picos en 6,6, 14,9, 20,1, 21,4, y 26,8 ± 0,2º 2q utilizando radiación Cu Ka. Reivindicación 7: Una forma cristalina del hidrato de diclorhidrato de omecamtiv mecarbil de la reivindicación 1, caracterizada porque el hidrato de diclorhidrato de omecamtiv mecarbil se caracteriza por un patrón de difracción en polvo de rayos X que comprende picos en 6,6, 8,4, 14,9, 15,4 y 26,8 ± 0,2º 2q utilizando radiación Cu Ka. Reivindicación 10: Una forma cristalina del hidrato de diclorhidrato de omecamtiv mecarbil de la reivindicación 1, caracterizada porque el hidrato de diclorhidrato de omecamtiv mecarbil se caracteriza por un patrón de difracción en polvo de rayos X que comprende picos en 6,6, 14,9, 16,3, 19,5 y 26,8 ± 0,2º 2q utilizando radiación Cu Ka. Reivindicación 12: Una composición farmacéutica caracterizada porque comprende el hidrato de diclorhidrato de omecamtiv mecarbil de la reivindicación 1 o 2, o la forma cristalina del hidrato de diclorhidrato de omecamtiv mecarbil de conformidad con cualquiera de las reivindicaciones 3 - 11. Reivindicación 13: Una composición farmacéutica caracterizada porque comprende: 6,13 - 18,37% p/p de un hidrato de diclorhidrato de omecamtiv mecarbil; 25 - 30% p/p de un agente de liberación de control, en donde el agente de liberación de control es hidroxipropilmetilcelulosa; 7,66 - 18,37% p/p de un agente de modificación de pH que es ácido fumárico; y 32,27 - 60,21% p/p de un relleno, en donde el relleno es una combinación de celulosa microcristalina y monohidrato de lactosa. Reivindicación 14: La composición farmacéutica de conformidad con la reivindicación 13, caracterizada porque tiene una relación en peso del agente modificador del pH al hidrato de diclorhidrato de omecamtiv mecarbil de menos de 2:1 a 1:1.
ARP230101396A 2013-03-14 2023-06-01 Hidrato de diclorhidrato de omecamtiv mecarbil, formas cristalinas, y composiciones farmacéuticas AR129504A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361785763P 2013-03-14 2013-03-14

Publications (1)

Publication Number Publication Date
AR129504A2 true AR129504A2 (es) 2024-09-04

Family

ID=50549466

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP140101155A AR095542A1 (es) 2013-03-14 2014-03-14 Compuestos heterocíclicos y sus usos
ARP230101396A AR129504A2 (es) 2013-03-14 2023-06-01 Hidrato de diclorhidrato de omecamtiv mecarbil, formas cristalinas, y composiciones farmacéuticas

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP140101155A AR095542A1 (es) 2013-03-14 2014-03-14 Compuestos heterocíclicos y sus usos

Country Status (42)

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US (16) US9951015B2 (es)
EP (3) EP2968173B1 (es)
JP (5) JP6498658B2 (es)
KR (2) KR102474467B1 (es)
CN (3) CN105209437B (es)
AP (1) AP2015008789A0 (es)
AR (2) AR095542A1 (es)
AU (2) AU2014240049C1 (es)
BR (2) BR112015023417B1 (es)
CA (2) CA3147180C (es)
CL (1) CL2015002708A1 (es)
CR (1) CR20150549A (es)
CY (2) CY1122695T1 (es)
DK (2) DK2968173T3 (es)
EA (1) EA031185B1 (es)
ES (2) ES2837038T3 (es)
HK (1) HK1218080A1 (es)
HR (2) HRP20191728T1 (es)
HU (2) HUE052355T2 (es)
IL (2) IL240788B (es)
JO (1) JOP20140114B1 (es)
LT (2) LT2970123T (es)
MA (2) MA44637B1 (es)
ME (1) ME03566B (es)
MX (3) MX2015012429A (es)
MY (2) MY186048A (es)
NZ (1) NZ711225A (es)
PE (1) PE20151786A1 (es)
PH (2) PH12019500176B1 (es)
PL (2) PL2968173T3 (es)
PT (2) PT2968173T (es)
RS (2) RS59536B1 (es)
RU (1) RU2663663C2 (es)
SA (1) SA515361088B1 (es)
SG (2) SG11201507258PA (es)
SI (2) SI2968173T1 (es)
SM (2) SMT201900563T1 (es)
TN (1) TN2015000380A1 (es)
TW (1) TWI667026B (es)
UA (1) UA117011C2 (es)
UY (1) UY35449A (es)
WO (2) WO2014152236A1 (es)

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WO2022177927A1 (en) 2021-02-16 2022-08-25 Assia Chemical Industries Ltd Unhydrous crystalline form of omecamtiv mecarbil dihydrobromide salt
CA3212491A1 (en) 2021-03-10 2022-09-15 Sebastien Caille Synthesis of omecamtiv mecarbil
US11986474B1 (en) 2023-06-27 2024-05-21 Cytokinetics, Incorporated Methods for treating heart failure by administering cardiac sarcomere activators

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US20220298114A1 (en) 2022-09-22
HRP20201967T1 (hr) 2021-03-05
MA44637A1 (fr) 2019-08-30
US20180312469A1 (en) 2018-11-01
EP2970123B1 (en) 2019-08-14
IL240788A0 (en) 2015-10-29
AU2014239995B2 (en) 2018-07-26
UA117011C2 (uk) 2018-06-11
US20200079736A1 (en) 2020-03-12
JOP20140114B1 (ar) 2021-08-17
KR20220045014A (ko) 2022-04-12
JP2016519071A (ja) 2016-06-30
JP2022023891A (ja) 2022-02-08
PE20151786A1 (es) 2015-12-11
US20250243163A1 (en) 2025-07-31
SG11201507258PA (en) 2015-10-29
MA38399A1 (fr) 2017-01-31
US12221417B2 (en) 2025-02-11
IL240788B (en) 2020-09-30
CA3147180C (en) 2024-04-23
PH12015501998B1 (en) 2016-01-11
EP2968173B1 (en) 2020-10-14
HK1218080A1 (zh) 2017-02-03
LT2970123T (lt) 2019-11-11
AU2014239995A1 (en) 2015-09-10
RU2663663C2 (ru) 2018-08-08
NZ750950A (en) 2020-09-25
SA515361088B1 (ar) 2018-07-22
US10421726B2 (en) 2019-09-24
WO2014152270A1 (en) 2014-09-25
LT2968173T (lt) 2021-03-25
DK2970123T3 (da) 2019-10-21
CA2902646C (en) 2022-08-16
US20240217933A1 (en) 2024-07-04
TWI667026B (zh) 2019-08-01
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US11958809B2 (en) 2024-04-16
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EA201591728A1 (ru) 2016-01-29
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US20200399221A1 (en) 2020-12-24
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