US20040242566A1 - Dipeptidyl peptidase inhibitors - Google Patents

Dipeptidyl peptidase inhibitors Download PDF

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Publication number
US20040242566A1
US20040242566A1 US10/809,638 US80963804A US2004242566A1 US 20040242566 A1 US20040242566 A1 US 20040242566A1 US 80963804 A US80963804 A US 80963804A US 2004242566 A1 US2004242566 A1 US 2004242566A1
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United States
Prior art keywords
phenyl
group
alkyl
substituted
unsubstituted
Prior art date
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Abandoned
Application number
US10/809,638
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English (en)
Inventor
Jun Feng
Stephen Gwaltney
Stephen Kaldor
Jeffrey Stafford
Michael Wallace
Zhiyuan Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SYNX Inc
Takeda Pharmaceutical Co Ltd
Qualcomm Inc
Takeda California Inc
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Syrrx Inc
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Priority to US10/809,638 priority Critical patent/US20040242566A1/en
Assigned to SYNX, INC. reassignment SYNX, INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: FENG, JUN, ZHANG, ZHIYUAN, STAFFORD, JEFFREY A., GWALTNEY, STEPHEN L., KALDOR, STEPHEN W., WALLACE, MICHAEL B.
Assigned to QUALCOMM, INCORPORATED reassignment QUALCOMM, INCORPORATED ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: ARGAWAL, AVNEESH, NAGUIB, AYMAN FAWAY, SUTIVONG, ARAK
Publication of US20040242566A1 publication Critical patent/US20040242566A1/en
Assigned to TAKEDA PHARMACEUTICAL COMPANY LIMITED reassignment TAKEDA PHARMACEUTICAL COMPANY LIMITED ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: TAKEDA SAN DIEGO, INC.
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pregnancy & Childbirth (AREA)
  • AIDS & HIV (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
US10/809,638 2003-03-25 2004-03-24 Dipeptidyl peptidase inhibitors Abandoned US20040242566A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US10/809,638 US20040242566A1 (en) 2003-03-25 2004-03-24 Dipeptidyl peptidase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US45778503P 2003-03-25 2003-03-25
US10/809,638 US20040242566A1 (en) 2003-03-25 2004-03-24 Dipeptidyl peptidase inhibitors

Publications (1)

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US20040242566A1 true US20040242566A1 (en) 2004-12-02

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Family Applications (4)

Application Number Title Priority Date Filing Date
US10/809,636 Abandoned US20040242568A1 (en) 2003-03-25 2004-03-24 Dipeptidyl peptidase inhibitors
US10/809,637 Expired - Fee Related US7687625B2 (en) 2003-03-25 2004-03-24 Dipeptidyl peptidase inhibitors
US10/809,635 Expired - Fee Related US7550590B2 (en) 2003-03-25 2004-03-24 Dipeptidyl peptidase inhibitors
US10/809,638 Abandoned US20040242566A1 (en) 2003-03-25 2004-03-24 Dipeptidyl peptidase inhibitors

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Application Number Title Priority Date Filing Date
US10/809,636 Abandoned US20040242568A1 (en) 2003-03-25 2004-03-24 Dipeptidyl peptidase inhibitors
US10/809,637 Expired - Fee Related US7687625B2 (en) 2003-03-25 2004-03-24 Dipeptidyl peptidase inhibitors
US10/809,635 Expired - Fee Related US7550590B2 (en) 2003-03-25 2004-03-24 Dipeptidyl peptidase inhibitors

Country Status (7)

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US (4) US20040242568A1 (US20040242566A1-20041202-C00060.png)
EP (1) EP1608317B1 (US20040242566A1-20041202-C00060.png)
JP (1) JP4887139B2 (US20040242566A1-20041202-C00060.png)
KR (1) KR20050122220A (US20040242566A1-20041202-C00060.png)
CN (1) CN1894234A (US20040242566A1-20041202-C00060.png)
CA (1) CA2518465A1 (US20040242566A1-20041202-C00060.png)
WO (1) WO2004087053A2 (US20040242566A1-20041202-C00060.png)

Cited By (22)

* Cited by examiner, † Cited by third party
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US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US20080090845A1 (en) * 2006-08-23 2008-04-17 Neurogen Corporation Haloalkyl-substituted pyrimidinone derivatives
US20090069347A1 (en) * 2006-08-23 2009-03-12 Neurogen Corporation 2-phenoxy pyrimidinone analogues
US20090257979A1 (en) * 2008-04-15 2009-10-15 Intermune, Inc. Novel Inhibitors of Hepatitis C Virus Replication
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7687638B2 (en) 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7687625B2 (en) 2003-03-25 2010-03-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7723344B2 (en) 2003-08-13 2010-05-25 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7781584B2 (en) 2004-03-15 2010-08-24 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7790734B2 (en) 2003-09-08 2010-09-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7825242B2 (en) 2004-07-16 2010-11-02 Takeda Pharmaceutical Company Limted Dipeptidyl peptidase inhibitors
US7872124B2 (en) 2004-12-21 2011-01-18 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US20110110890A1 (en) * 2009-11-09 2011-05-12 Intermune, Inc. Novel Inhibitors of Hepatitis C Virus Replication
US7960384B2 (en) 2006-03-28 2011-06-14 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US8084605B2 (en) 2006-11-29 2011-12-27 Kelly Ron C Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
US8222411B2 (en) 2005-09-16 2012-07-17 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors
US10555929B2 (en) 2015-03-09 2020-02-11 Coherus Biosciences, Inc. Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
US11253508B2 (en) 2017-04-03 2022-02-22 Coherus Biosciences, Inc. PPARy agonist for treatment of progressive supranuclear palsy

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* Cited by examiner, † Cited by third party
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EP1911754B1 (en) * 2003-08-13 2013-10-09 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
AR051596A1 (es) 2004-10-26 2007-01-24 Irm Llc Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios
JP2008520744A (ja) 2004-11-19 2008-06-19 ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 抗炎症性ピラゾロピリミジン
AU2011201488B2 (en) * 2004-11-29 2011-11-17 Merck Sharp & Dohme Corp. Fused aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
WO2007024993A2 (en) 2005-08-26 2007-03-01 Merck & Co., Inc. Fused aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
DOP2006000008A (es) 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
EP2390264A1 (en) 2005-02-11 2011-11-30 Amylin Pharmaceuticals Inc. GIP analog and hybrid polypeptides with selectable propperties
US8686002B2 (en) 2005-08-21 2014-04-01 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as binding partners for 5-HT5 receptors
PL1931350T5 (pl) † 2005-09-14 2021-11-15 Takeda Pharmaceutical Company Limited Podanie inhibitorów dipeptydylo-peptydazy
JP2009520763A (ja) * 2005-12-23 2009-05-28 ノバルティス アクチエンゲゼルシャフト Ｄｐｐ−ｉｖ阻害剤として有用な縮合ヘテロ環式化合物
JP2009531456A (ja) * 2006-03-28 2009-09-03 武田薬品工業株式会社 （ｒ）−３−アミノピペリジン二塩酸塩の調製
CA2647391C (en) 2006-04-04 2015-12-29 The Regents Of The University Of California Kinase antagonists
PE20071221A1 (es) 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
JP2009533393A (ja) 2006-04-12 2009-09-17 プロビオドルグ エージー 酵素阻害薬
EP2079739A2 (en) 2006-10-04 2009-07-22 Pfizer Products Inc. Pyrido[4,3-d]pyrimidin-4(3h)-one derivatives as calcium receptor antagonists
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
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EP2143443B1 (en) 2007-04-03 2014-11-19 Mitsubishi Tanabe Pharma Corporation A combination of dipeptidyl peptidase iv inhibitor and sweetener for use in the treatment of obesity
DK2142514T3 (da) 2007-04-18 2015-03-23 Probiodrug Ag Thioureaderivater som glutaminylcyclase-inhibitorer
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EP2358720B1 (en) 2008-10-16 2016-03-02 The Regents of The University of California Fused ring heteroaryl kinase inhibitors
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
CN101817833B (zh) * 2009-02-26 2013-03-06 中国科学院广州生物医药与健康研究院 Dpp-iv抑制剂
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
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US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
RU2515541C2 (ru) 2009-11-12 2014-05-10 Ф.Хоффманн-Ля Рош Аг N-7 замещенные пурины и пиразолопиримидины, их композиции и способы применения
ME02186B (me) 2009-12-23 2016-02-20 Takeda Pharmaceuticals Co Fuzionisani heteroaromatski pirolidinoni kao syk inhibitori
US8648073B2 (en) 2009-12-30 2014-02-11 Fochon Pharma, Inc. Certain dipeptidyl peptidase inhibitors
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