CA2736361C - Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor - Google Patents

Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor Download PDF

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Publication number
CA2736361C
CA2736361C CA2736361A CA2736361A CA2736361C CA 2736361 C CA2736361 C CA 2736361C CA 2736361 A CA2736361 A CA 2736361A CA 2736361 A CA2736361 A CA 2736361A CA 2736361 C CA2736361 C CA 2736361C
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Prior art keywords
treatment
pharmaceutically acceptable
acceptable salt
mtor
combination
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Expired - Fee Related
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CA2736361A
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English (en)
French (fr)
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CA2736361A1 (en
Inventor
Carlos Garcia-Echeverria
Sauveur-Michel Maira
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Novartis AG
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Novartis AG
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    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA2736361A 2008-10-31 2009-10-29 Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor Expired - Fee Related CA2736361C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08168044.9 2008-10-31
EP08168044 2008-10-31
PCT/EP2009/064274 WO2010049481A1 (en) 2008-10-31 2009-10-29 Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor

Publications (2)

Publication Number Publication Date
CA2736361A1 CA2736361A1 (en) 2010-05-06
CA2736361C true CA2736361C (en) 2017-10-10

Family

ID=40332588

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2736361A Expired - Fee Related CA2736361C (en) 2008-10-31 2009-10-29 Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor

Country Status (12)

Country Link
US (3) US20110195966A1 (enExample)
EP (1) EP2349275B1 (enExample)
JP (4) JP2012506898A (enExample)
KR (1) KR20110090911A (enExample)
CN (2) CN102202668A (enExample)
AU (1) AU2009309616B2 (enExample)
BR (1) BRPI0921802A8 (enExample)
CA (1) CA2736361C (enExample)
ES (1) ES2627677T3 (enExample)
MX (1) MX2011004585A (enExample)
RU (2) RU2538683C2 (enExample)
WO (1) WO2010049481A1 (enExample)

Families Citing this family (32)

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US20100048524A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
US8476282B2 (en) * 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
PT2365802T (pt) 2008-11-11 2017-11-14 Univ Texas Microcápsulas de rapamicina e utilização para o tratamento de cancro
WO2010091306A1 (en) 2009-02-05 2010-08-12 Tokai Pharmaceuticals Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
US9283211B1 (en) 2009-11-11 2016-03-15 Rapamycin Holdings, Llc Oral rapamycin preparation and use for stomatitis
GB2478556A (en) * 2010-03-09 2011-09-14 Myrovlytis Technology Ventures Ltd A composition for use in the treatment of Birt-Hogg-Dubô sydrome
EP2675450B1 (en) * 2011-02-16 2016-02-10 Novartis AG Combinations of therapeutic agents for use in the treatment of neurodegenerative diseases
JP6130305B2 (ja) 2011-02-23 2017-05-17 インテリカイン, エルエルシー キナーゼ阻害剤の組み合わせおよびそれらの使用
US9127074B2 (en) * 2011-03-07 2015-09-08 Fondazione Telethon TFEB variants and uses thereof
US20140066474A1 (en) * 2011-04-25 2014-03-06 Novartis Ag Combination of phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor
ES2618489T3 (es) 2011-05-04 2017-06-21 Intellikine, Llc Composiciones farmacéuticas combinadas y usos de las mismas
AU2012313888B2 (en) 2011-09-27 2016-03-31 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
CN106924741A (zh) * 2011-11-08 2017-07-07 因特利凯有限责任公司 使用多种药剂的治疗方案
US20130209543A1 (en) * 2011-11-23 2013-08-15 Intellikine Llc Enhanced treatment regimens using mtor inhibitors
UY34632A (es) * 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
RU2012112128A (ru) * 2012-03-29 2013-10-10 Холин Максим Николаевич ИНГИБИТОРЫ СИГНАЛЬНОГО ПУТИ PI3K/AKT/IKK/NF-kB, ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ И СОДЕРЖАЩИЕ ИХ КОМПОЗИЦИИ ДЛЯ ПРОФИЛАКТИКИ И ЛЕЧЕНИЯ ВИРУСНЫХ ЗАБОЛЕВАНИЙ
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
WO2014160328A1 (en) 2013-03-13 2014-10-02 The Board Of Regents Of The University Of Texas System Mtor inhibitors for prevention of intestinal polyp growth
EP2968370A4 (en) 2013-03-14 2016-09-21 Univ Maryland AGENT FOR ANDROGEN RECEPTOR DOWNWARD CONTROL AND USES THEREOF
KR20150131224A (ko) 2013-03-14 2015-11-24 노파르티스 아게 돌연변이 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온
RU2015143437A (ru) 2013-03-15 2017-04-27 Дженентек, Инк. Способы лечения рака и предотвращения устойчивости к лекарственным препаратам для лечения рака
PE20161063A1 (es) 2013-05-01 2016-10-22 Hoffmann La Roche Compuestos de biheteroarilo y usos de los mismos
EP3033088A4 (en) 2013-08-12 2017-03-08 Tokai Pharmaceuticals, Inc. Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
CN103483345B (zh) * 2013-09-25 2016-07-06 中山大学 Pi3k激酶抑制剂、包含其的药物组合物及其应用
AU2014373683B2 (en) 2013-12-31 2020-05-07 Rapamycin Holdings, Llc Oral rapamycin nanoparticle preparations and use
US9700544B2 (en) 2013-12-31 2017-07-11 Neal K Vail Oral rapamycin nanoparticle preparations
WO2016168658A1 (en) 2015-04-15 2016-10-20 University Of Massachusetts Compositions and methods for xi chromosome reactivation
EP3297629A1 (en) 2015-05-20 2018-03-28 Novartis AG Pharmaceutical combination of everolimus with dactolisib
BR112019010470A2 (pt) 2016-11-23 2019-09-10 Novartis Ag métodos de realce de resposta imune com everolimo, dactolisib ou ambos
US10596165B2 (en) 2018-02-12 2020-03-24 resTORbio, Inc. Combination therapies
KR20210158019A (ko) 2020-06-23 2021-12-30 주식회사 온코빅스 포스파티딜이노시톨 3-키나제(pi3k) 억제제로써 pten 과오종 증후군에 의한 종양 세포의 성장 또는 증식을 억제하는데 유용한 신규한 피리미딘 유도체 및 이의 약제학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 약제학적 조성물
CN112294967A (zh) * 2020-09-30 2021-02-02 四川大学 一种mTOR抑制剂与抗癌药物的用途

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Publication number Priority date Publication date Assignee Title
IL153474A0 (en) * 2000-06-26 2003-07-06 Stressgen Biotechnologies Corp Human papilloma virus treatment
CN101039952A (zh) * 2004-10-13 2007-09-19 惠氏公司 作为pi3k抑制剂的17-羟基渥曼青霉素类似物
WO2007010012A2 (en) * 2005-07-20 2007-01-25 Novartis Ag Combination of a pyrimidylaminobenzamide and an mtor kinase inhibitor
KR101464384B1 (ko) * 2005-11-22 2014-11-21 쿠도스 파마슈티칼스 리미티드 mTOR 억제제로서 피리도피리미딘, 피라조피리미딘 및피리미도피리미딘 유도체
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
US7659274B2 (en) * 2006-01-25 2010-02-09 Osi Pharmaceuticals, Inc. Unsaturated mTOR inhibitors
WO2007120897A2 (en) * 2006-04-13 2007-10-25 The Trustees Of Columbia University In The City Of New York Compositions and intraluminal devices for inhibiting vascular stenosis
AU2008213808B2 (en) * 2007-02-06 2011-11-10 Novartis Ag PI 3-kinase inhibitors and methods of their use
RU2478387C2 (ru) * 2007-02-20 2013-04-10 Новартис Аг ИМИДАЗОХИНОЛИНЫ В КАЧЕСТВЕ ДВОЙНЫХ ИНГИБИТОРОВ ЛИПИДКИНАЗЫ И mTOR
CN101896177A (zh) * 2007-12-13 2010-11-24 诺瓦提斯公司 用于治疗癌症的治疗剂的组合

Also Published As

Publication number Publication date
JP2017002058A (ja) 2017-01-05
CN102202668A (zh) 2011-09-28
RU2014115188A (ru) 2015-10-20
JP2018197243A (ja) 2018-12-13
WO2010049481A1 (en) 2010-05-06
CN105030784A (zh) 2015-11-11
US20180133226A1 (en) 2018-05-17
EP2349275A1 (en) 2011-08-03
JP2012506898A (ja) 2012-03-22
JP2015013883A (ja) 2015-01-22
AU2009309616A1 (en) 2010-05-06
RU2011121508A (ru) 2012-12-10
ES2627677T3 (es) 2017-07-31
AU2009309616B2 (en) 2014-02-13
RU2538683C2 (ru) 2015-01-10
AU2009309616A2 (en) 2011-07-07
BRPI0921802A8 (pt) 2018-03-13
US20160136175A1 (en) 2016-05-19
EP2349275B1 (en) 2017-03-08
KR20110090911A (ko) 2011-08-10
CA2736361A1 (en) 2010-05-06
BRPI0921802A2 (pt) 2016-09-27
US20110195966A1 (en) 2011-08-11
MX2011004585A (es) 2011-06-01

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