US20040058935A1 - Low hygroscopic aripiprazole drug substance and processes for the preparation thereof - Google Patents

Low hygroscopic aripiprazole drug substance and processes for the preparation thereof Download PDF

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Publication number
US20040058935A1
US20040058935A1 US10/333,244 US33324403A US2004058935A1 US 20040058935 A1 US20040058935 A1 US 20040058935A1 US 33324403 A US33324403 A US 33324403A US 2004058935 A1 US2004058935 A1 US 2004058935A1
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Prior art keywords
aripiprazole anhydride
aripiprazole
anhydride crystals
crystals
solid oral
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Abandoned
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US10/333,244
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English (en)
Inventor
Takuji Bando
Satoshi Aoki
Junichi Kawasaki
Makoto Ishigami
Youichi Taniguchi
Tsuyoshi Yabuuchi
Kiyoshi Fujimoto
Yoshihiro Nishioka
Noriyuki Kobayashi
Tsutomu Fujimura
Masanori Takahashi
Kaoru Abe
Tomonori Nakagawa
Koichi Shinhama
Naoto Utsumi
Michiaki Tominaga
Yoshihiro Ooi
Shohei Yamada
Kenji Tomikawa
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Otsuka Pharmaceutical Co Ltd
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Otsuka Pharmaceutical Co Ltd
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27171631&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=US20040058935(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from CA 2379005 external-priority patent/CA2379005A1/en
Application filed by Otsuka Pharmaceutical Co Ltd filed Critical Otsuka Pharmaceutical Co Ltd
Assigned to OTSUKA PHARMACEUTICAL CO., LTD. reassignment OTSUKA PHARMACEUTICAL CO., LTD. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: ABE, KAORU, AOKI, SATOSHI, BANDO, TAKUJI, FUJIMOTO, KIYOSHI, FUJIMURA, TSUTOMU, ISHIGAMI, MAKOTO, KAWASAKI, JUNICHI, KOBAYASHI, NORIYUKI, NAKAGAWA, TOMONORI, NISHIOKA, YOSHIHIRO, OOI, YOSHIHIRO, SHINHAMA, KOICHI, TAKAHASHI, MASANORI, TANIGUCHI, YOUICHI, TOMIKAWA, KENJI, TOMINAGA, MICHIAKI, UTSUMI, NAOTO, YABUUCHI, TSUYOSHI, YAMADA, SHOEHI
Publication of US20040058935A1 publication Critical patent/US20040058935A1/en
Priority to US11/790,604 priority Critical patent/US8399469B2/en
Priority to US11/790,606 priority patent/US7910589B2/en
Priority to US11/790,603 priority patent/US20070213343A1/en
Priority to US11/790,605 priority patent/US8017615B2/en
Priority to US11/797,024 priority patent/US20070203151A1/en
Priority to US11/797,019 priority patent/US20070203150A1/en
Priority to US11/797,030 priority patent/US20070203152A1/en
Priority to US13/067,750 priority patent/US8642760B2/en
Priority to US13/067,838 priority patent/US8901303B2/en
Priority to US13/217,636 priority patent/US8703772B2/en
Priority to US13/350,117 priority patent/US8580796B2/en
Priority to US13/476,773 priority patent/US8703773B2/en
Priority to US13/476,758 priority patent/US8901130B2/en
Priority to US13/749,753 priority patent/US8993761B2/en
Priority to US14/049,777 priority patent/US9359302B2/en
Priority to US14/624,595 priority patent/US10150735B2/en
Priority to US15/149,522 priority patent/US20160251315A1/en
Priority to US16/169,255 priority patent/US20190225584A1/en
Priority to US16/718,281 priority patent/US20200123110A1/en
Priority to US17/160,716 priority patent/US20210395204A1/en
Abandoned 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
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • 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
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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    • A—HUMAN NECESSITIES
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    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T428/00—Stock material or miscellaneous articles
    • Y10T428/29—Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
    • Y10T428/2982—Particulate matter [e.g., sphere, flake, etc.]

Definitions

  • FIG. 13 shows a thermogravimetric/differential thermal analysis endothermic curve of the type D crystals of aripiprazole anhydride obtained in Example 12 or Example 13.
  • FIG. 21 shows an IR spectrum of the type E crystals of aripiprazole anhydride obtained in Example 14.
  • Hydrate A defined according to one or more of the embodiments described herein wherein said Hydrate is made by a process as described herein.
  • aripiprazole drug substance of low hygroscopicity is provided.
  • aripiprazole drug substance of low hygroscopicity wherein said drug substance is Aripiprazole Anhydride Crystals B and will not substantially convert to a hydrous form of aripiprazole when properly stored even for an extended period.
  • said Aripiprazole Anhydride Crystals B can be stored under a relative humidity (RH) of 60% and at a temperature of 25° C., even for a period not less than 4 years.
  • the mean particle size of the Aripiprazole Hydrate A obtained by milling should normally be 50 ⁇ m or less, preferably 30 ⁇ m or less. Mean particle size can be ascertained by the particle size measurement method described hereinafter.
  • the Aripiprazole Anhydride Crystals B of the present invention can be prepared with certainty by heating Aripiprazole Hydrate A for about 18 hours at 100° C., and then heating it for about 3 hours at 120° C.
  • the Aripiprazole Anhydride Crystals B of the present invention can also be obtained if the heating time is extended still further, but this may not be economical.
  • Aripiprazole Anhydride Crystal B can be also obtained the following process.
  • the present invention relates to aripiprazole anhydride crystals (hereinafter referred to as “type E crystals of aripiprazole anhydride”) having the following physicochemical properties (11) to (14):
  • the present invention relates a process for preparing aripiprazole anhydride crystals stated in the aforementioned item 2, characterized by recrystallizing from toluene.
  • the present invention relates to a process for preparing aripiprazole anhydride crystals stated in the aforementioned item 4, characterized by heating a suspension of aripiprazole anhydride crystals in acetone.
  • the present invention relates to a pharmaceutical solid oral preparation obtained by drying a pharmaceutical solid oral preparation comprising conventional Aripiprazole Hydrate Crystals and one or more pharmaceutically acceptable carriers at 70 to 100° C., and the pharmaceutical solid oral preparation has at least one dissolution rate selected from the group consisting 60% or more at pH 4.5 after 30 minutes, 70% or more at pH 4.5 after 60 minutes, and 55% or more at pH 5.0 after 60 minutes.
  • Type C crystals of aripiprazole anhydride of the present invention have the following physicochemical properties (1) to (5):
  • Aripiprazole anhydride used as the raw material may be conventional aripiprazole anhydride crystals, for example, type-I crystals of aripiprazole anhydride, type-II crystals of aripiprazole anhydride crystals and the like, and these anhydrides may be either purified products or crude materials.
  • Type D crystals of aripiprazole anhydride of the present invention is prepared, for example, by recrystallization of aripiprazole anhydride from toluene. Specifically, an aripiprazole anhydride is added to toluene, further heated and dissolved, then thus obtained solution is cooled. By such procedures, type D crystals of aripiprazole anhydride of the present invention is separated out as crystals in toluene.
  • type D crystals of aripiprazole may be added as a seed crystal to said solution. Further, the seed crystal may be formed by cooling gradually said solution being obtained by heating and dissolving. In the presence of the seed crystal, type D crystals of aripiprazole anhydride may be separated out.
  • type B crystals of aripiprazole anhydride, type C crystals of aripiprazole anhydride, type D crystals of aripiprazole anhydride, type E crystals of aripiprazole anhydride, or type G crystals of aripiprazole anhydride prepared in the present invention can be used as the raw materials for aripiprazole anhydrides.
  • aripiprazole anhydrides can be used singly or in combination of at least 2 kinds thereof.
  • Aripiprazole anhydride used as the raw material may be well-known aripiprazole anhydride crystals, for example, any one of type-I crystals of aripiprazole anhydride and type-II crystals of aripiprazole anhydride and the like, and these anhydrides may be either purified products or crude materials.
  • aripiprazole anhydride crystals which are the raw material for preparing the Aripiprazole Anhydride Crystals B to G of the present invention are prepared for example by Method a or b below.
  • the powder x-ray diffraction pattern was measured at room temperature using a Cu Ka filled tube (35 kV 20 mA) as the x-ray source with a wide-angle goniometer, a 1° scattering slit, an 0.15 mm light-intercepting slit, a graphite secondary monochromator and a scintillation counter. Data collection was done in 2 ⁇ continuous scan mode at a scan speed of 5°/minute in scan steps of 0.02° in the range of 3° to 40°.
  • TOSS method (TOSS is a program name of the apparatus) among CP/MAS method.
  • Test tube made of zirconia, having the outside diameter of 7.5 mm, and inside capacity of 0.8 ml
  • the Aripiprazole Hydrate A (powder) obtained above had infrared absorption bands at 2951, 2822, 1692, 1577, 1447, 1378, 1187, 963 and 784 cm ⁇ 1 on the IR (KBr) spectrum.
  • the Aripiprazole Hydrate A (powder) obtained above had a weak peak at 71.3° C. in thermogravimetric/differential thermal analysis and a broad endothermic peak (weight loss observed corresponding to one water molecule) between 60-120° C.—clearly different from the endothermic curve of unmilled aripiprazole hydrate (see FIG. 6).
  • the Aripiprazole Anhydride Crystals B obtained above had remarkable infrared absorption bands at 2945, 2812, 1678, 1627, 1448, 1377, 1173, 960 and 779 cm ⁇ 1 on the IR (KBr) spectrum.
  • the Aripiprazole Anhydride Crystals B obtained in this way did not exhibit hygroscopicity of more than 0.4% even when left for 24 hours in a dessicator set at humidity 100%, temperature 60° C. (see Table 1 below).
  • the Aripiprazole Anhydride Crystals B obtained in this way did not exhibit hygroscopicity of more than 0.4% even when left for 24 hours in a dessicator set at humidity 100%, temperature 60° C. (see Table 1 below).
  • the Aripiprazole Anhydride Crystals B obtained in this way did not exhibit hygroscopicity of more than 0.4% even when left for 24 hours in a dessicator set at humidity 100%, temperature 60° C. (see Table 1 below).
  • the type D crystals of aripiprazole anhydride obtained above had an IR spectrum which was substantially identical to the IR (KBr) spectrum shown in FIG. 16. Specifically, it had characteristic infrared absorption bands at 2946, 1681, 1375, 1273, 1175 and 862 cm ⁇ 1 .
  • test solutions obtained respectively from 10 minutes, 20 minutes, 30 minutes, 45 minutes and 60 minutes after the start of test are named as T10, T20, T30, T45 and T60.
  • Example 19-a Tablet (30 mg) of — 79.8%
  • Example 19-b Tablet (30 mg) of — 85.9%
  • the intragranulation was placed in the blender and the Avicel® PH 200 and crospovidone added thereto and blended for five minutes. The magnesium stearate was then added and the mixture blended for an additional three minutes to form the final blend. Tablets compressed therefrom had a breaking force of 2.3 kP (3.5 SCU) and disintegrated in 10 seconds in 5 ml of water. The final blend formulation demonstrated excellent flow and was free of other problems such as chipping, capping and sticking. It has been found that utilizing Avicel® PH 102 for the intragranulation and Avicel® PH 200 for the extragranulation ingredient enhanced the quality of the resultant tablets.
  • Intragranulation Mg. per Ingredient Percent w/w tablet Xylitol (300) Xylisorb 26 52 Avicel ® PH 102 12 24 Calcium Silicate (crystalline, alpha 33.35 66.7 triclinic) Hubersorb 600 NF 10 20 (amorphous calcium silicate) Crospovidone 3 6 Amorphous silica 2 4 Aspartame 2 4 Wild cherry flavor 0.15 0.3 Tartaric acid 2 4 Acesulfame K 2 4 Magnesium stearate 0.25 0.5 Total weight 92.75 185.5

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US10/333,244 2001-09-25 2002-09-25 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof Abandoned US20040058935A1 (en)

Priority Applications (20)

Application Number Priority Date Filing Date Title
US11/790,605 US8017615B2 (en) 2001-09-25 2007-04-26 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/790,603 US20070213343A1 (en) 2001-09-25 2007-04-26 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/790,606 US7910589B2 (en) 2001-09-25 2007-04-26 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/790,604 US8399469B2 (en) 2001-09-25 2007-04-26 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/797,030 US20070203152A1 (en) 2001-09-25 2007-04-30 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/797,024 US20070203151A1 (en) 2001-09-25 2007-04-30 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/797,019 US20070203150A1 (en) 2001-09-25 2007-04-30 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US13/067,750 US8642760B2 (en) 2001-09-25 2011-06-23 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US13/067,838 US8901303B2 (en) 2001-09-25 2011-06-29 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US13/217,636 US8703772B2 (en) 2001-09-25 2011-08-25 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US13/350,117 US8580796B2 (en) 2001-09-25 2012-01-13 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US13/476,773 US8703773B2 (en) 2001-09-25 2012-05-21 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US13/476,758 US8901130B2 (en) 2001-09-25 2012-05-21 Low hygroscopic aripiprazole drug substance and processes for the preparation
US13/749,753 US8993761B2 (en) 2001-09-25 2013-01-25 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US14/049,777 US9359302B2 (en) 2001-09-25 2013-10-09 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US14/624,595 US10150735B2 (en) 2001-09-25 2015-02-18 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US15/149,522 US20160251315A1 (en) 2001-09-25 2016-05-09 Low hygroscopic aripiprazole drug substance and proce3sses for the preparation thereof
US16/169,255 US20190225584A1 (en) 2001-09-25 2018-10-24 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US16/718,281 US20200123110A1 (en) 2001-09-25 2019-12-18 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US17/160,716 US20210395204A1 (en) 2001-09-25 2021-01-28 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof

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US11/790,603 Division US20070213343A1 (en) 2001-09-25 2007-04-26 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/790,606 Division US7910589B2 (en) 2001-09-25 2007-04-26 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/797,030 Division US20070203152A1 (en) 2001-09-25 2007-04-30 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/797,024 Division US20070203151A1 (en) 2001-09-25 2007-04-30 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/797,019 Division US20070203150A1 (en) 2001-09-25 2007-04-30 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
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US11/790,603 Abandoned US20070213343A1 (en) 2001-09-25 2007-04-26 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/790,606 Expired - Lifetime US7910589B2 (en) 2001-09-25 2007-04-26 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
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US11/790,606 Expired - Lifetime US7910589B2 (en) 2001-09-25 2007-04-26 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/790,604 Expired - Lifetime US8399469B2 (en) 2001-09-25 2007-04-26 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
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US11/797,024 Abandoned US20070203151A1 (en) 2001-09-25 2007-04-30 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US11/797,030 Abandoned US20070203152A1 (en) 2001-09-25 2007-04-30 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
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US13/749,753 Expired - Fee Related US8993761B2 (en) 2001-09-25 2013-01-25 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US14/049,777 Expired - Lifetime US9359302B2 (en) 2001-09-25 2013-10-09 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US14/624,595 Expired - Fee Related US10150735B2 (en) 2001-09-25 2015-02-18 Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
US15/149,522 Abandoned US20160251315A1 (en) 2001-09-25 2016-05-09 Low hygroscopic aripiprazole drug substance and proce3sses for the preparation thereof
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PT1927357E (pt) 2010-06-08
CA2688915C (en) 2011-02-01
EP1419776A2 (en) 2004-05-19
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CA2426921C (en) 2011-03-15
EP1419776B1 (en) 2010-04-14
ES2343602T3 (es) 2010-08-04
ES2343220T3 (es) 2010-07-26
SI1419776T2 (sl) 2017-12-29
US20070203152A1 (en) 2007-08-30
US8642760B2 (en) 2014-02-04
CN101574347A (zh) 2009-11-11
EP1925308B1 (en) 2016-08-31
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US8993761B2 (en) 2015-03-31
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NO336262B1 (no) 2015-07-06
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EP1330249A1 (en) 2003-07-30
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US9359302B2 (en) 2016-06-07
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US20120315302A1 (en) 2012-12-13
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US20070203150A1 (en) 2007-08-30
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US20160251315A1 (en) 2016-09-01
US8703773B2 (en) 2014-04-22
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US20210395204A1 (en) 2021-12-23
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