CN1894234A - 二肽基肽酶抑制剂 - Google Patents

二肽基肽酶抑制剂 Download PDF

Info

Publication number
CN1894234A
CN1894234A CNA2004800119000A CN200480011900A CN1894234A CN 1894234 A CN1894234 A CN 1894234A CN A2004800119000 A CNA2004800119000 A CN A2004800119000A CN 200480011900 A CN200480011900 A CN 200480011900A CN 1894234 A CN1894234 A CN 1894234A
Authority
CN
China
Prior art keywords
compound
alkyl
aryl
phenyl
unsubstituted
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CNA2004800119000A
Other languages
English (en)
Chinese (zh)
Inventor
冯军
S·L·戈瓦尔特尼
S·W·卡尔多
J·A·斯塔弗德
M·B·瓦拉斯
张志远
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.)
Takeda Pharmaceutical Co Ltd
Takeda California Inc
Original Assignee
Takeda Chemical Industries Ltd
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
Application filed by Takeda Chemical Industries Ltd filed Critical Takeda Chemical Industries Ltd
Publication of CN1894234A publication Critical patent/CN1894234A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
CNA2004800119000A 2003-03-25 2004-03-24 二肽基肽酶抑制剂 Pending CN1894234A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US45778503P 2003-03-25 2003-03-25
US60/457,785 2003-03-25

Publications (1)

Publication Number Publication Date
CN1894234A true CN1894234A (zh) 2007-01-10

Family

ID=33131718

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA2004800119000A Pending CN1894234A (zh) 2003-03-25 2004-03-24 二肽基肽酶抑制剂

Country Status (7)

Country Link
US (4) US7550590B2 (US20040242566A1-20041202-C00021.png)
EP (1) EP1608317B1 (US20040242566A1-20041202-C00021.png)
JP (1) JP4887139B2 (US20040242566A1-20041202-C00021.png)
KR (1) KR20050122220A (US20040242566A1-20041202-C00021.png)
CN (1) CN1894234A (US20040242566A1-20041202-C00021.png)
CA (1) CA2518465A1 (US20040242566A1-20041202-C00021.png)
WO (1) WO2004087053A2 (US20040242566A1-20041202-C00021.png)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102311447A (zh) * 2010-07-07 2012-01-11 中国科学院广州生物医药与健康研究院 杂环并嘧啶酮类dpp-iv抑制剂
CN102311448A (zh) * 2010-07-07 2012-01-11 中国科学院广州生物医药与健康研究院 噻吩并嘧啶酮类dpp-iv抑制剂
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
CN103130819A (zh) * 2011-12-01 2013-06-05 中国科学院上海药物研究所 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途
CN106045922A (zh) * 2016-06-12 2016-10-26 湘潭大学 2‑(氨基)甲基喹唑啉‑4(3h)‑酮类化合物及其制备方法和用途

Families Citing this family (127)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4887139B2 (ja) 2003-03-25 2012-02-29 武田薬品工業株式会社 ジペプチジルペプチダーゼインヒビター
EP1911754B1 (en) * 2003-08-13 2013-10-09 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
ZA200602051B (en) 2003-08-13 2007-10-31 Takeda Pharmaceutical 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7790734B2 (en) 2003-09-08 2010-09-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
GEP20094679B (en) 2004-03-15 2009-05-10 Takeda Pharmaceuticals Co Dipeptidyl peptidase inhibitors
JP2008501714A (ja) 2004-06-04 2008-01-24 武田薬品工業株式会社 ジペプチジルペプチダーゼインヒビター
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. 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
WO2006068760A2 (en) 2004-11-19 2006-06-29 The Regents Of The University Of California Anti-inflammatory pyrazolopyrimidines
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
EP1828192B1 (en) * 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
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
WO2006086769A2 (en) 2005-02-11 2006-08-17 Amylin Pharmaceuticals, Inc. Gip analog and hybrid polypeptides with selectable properties
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
JP5075125B2 (ja) 2005-08-26 2012-11-14 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療又は予防用ジペプチジルペプチダーゼｉｖ阻害剤としての縮合アミノピペリジン
RS52110B2 (sr) 2005-09-14 2018-05-31 Takeda Pharmaceuticals Co Inhibitori dipeptidil peptidaze za lečenje dijabetesa
US20070060528A1 (en) † 2005-09-14 2007-03-15 Christopher Ronald J Administration of dipeptidyl peptidase inhibitors
JP5122462B2 (ja) * 2005-09-16 2013-01-16 武田薬品工業株式会社 ジペプチジルペプチダーゼ阻害剤
WO2007071738A1 (en) * 2005-12-23 2007-06-28 Novartis Ag Condensed heterocyclic compounds useful as dpp-iv inhibitors
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
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
US7728146B2 (en) 2006-04-12 2010-06-01 Probiodrug Ag Enzyme inhibitors
CN101563349A (zh) * 2006-08-23 2009-10-21 神经能质公司 经卤烷基取代的嘧啶酮衍生物
EA200900330A1 (ru) * 2006-08-23 2009-08-28 Ньюроджен Корпорейшн Аналоги 2-феноксипиримидинона
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
EP2079739A2 (en) 2006-10-04 2009-07-22 Pfizer Products Inc. Pyrido[4,3-d]pyrimidin-4(3h)-one derivatives as calcium receptor antagonists
EP2089383B1 (en) 2006-11-09 2015-09-16 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
TW200838536A (en) * 2006-11-29 2008-10-01 Takeda Pharmaceutical 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
EP2091948B1 (en) 2006-11-30 2012-04-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
KR101361427B1 (ko) 2007-04-03 2014-02-10 미쓰비시 타나베 파마 코퍼레이션 디펩티딜 펩티다아제 4 저해 화합물과 감미료와의 병용
ES2533484T3 (es) 2007-04-18 2015-04-10 Probiodrug Ag Derivados de tiourea como inhibidores de la glutaminil ciclasa
ME00954B (me) 2007-05-11 2012-06-20 Pfizer Aminoheterociklični spojevi
GB2467670B (en) 2007-10-04 2012-08-01 Intellikine Inc Chemical entities and therapeutic uses thereof
EP3613743B1 (en) 2008-01-04 2022-03-16 Intellikine, LLC Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
US8637542B2 (en) 2008-03-14 2014-01-28 Intellikine, Inc. Kinase inhibitors and methods of use
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
BRPI0911259A2 (pt) * 2008-04-15 2015-10-06 Intermune Inc composto, composição farmacêutica, método de inibição da atividade da polimerase de ns5b in vitro e usos de compostos
CN102124009B (zh) 2008-07-08 2014-07-23 因特利凯公司 激酶抑制剂及其使用方法
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
US20100029371A1 (en) * 2008-08-01 2010-02-04 Gennady Medvinsky Personal Game Services Commerce System (PGSCS)
EP2346508B1 (en) 2008-09-26 2016-08-24 Intellikine, LLC Heterocyclic kinase inhibitors
CA2740885C (en) 2008-10-16 2018-04-03 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
CA2760791C (en) 2009-05-07 2017-06-20 Intellikine, Inc. Heterocyclic compounds and uses thereof
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
ES2548913T3 (es) 2009-09-11 2015-10-21 Probiodrug Ag Derivados heterocíclicos como inhibidores de glutaminil ciclasa
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
TW201121968A (en) * 2009-11-09 2011-07-01 Intermune Inc Novel inhibitors of hepatitis C virus replication
US8828990B2 (en) 2009-11-12 2014-09-09 Genentech, Inc. N-7 substituted purine and pyrazolopyrimine compounds, compositions and methods of use
MX2012007402A (es) 2009-12-23 2012-08-23 Takeda Pharmaceutical Pirrolidinonas heteroaromaticas fusionadas como inhibidores de tirosina cinasa esplenica (syk).
CA2784799C (en) 2009-12-30 2014-06-10 Shanghai Fochon Pharmaceutical Co Ltd Certain dipeptidyl peptidase inhibtors
US9181233B2 (en) 2010-03-03 2015-11-10 Probiodrug Ag Inhibitors of glutaminyl cyclase
EA022420B1 (ru) 2010-03-10 2015-12-30 Пробиодруг Аг Гетероциклические ингибиторы глутаминилциклазы (qc, ec 2.3.2.5)
US20130023494A1 (en) 2010-04-06 2013-01-24 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
US8604032B2 (en) 2010-05-21 2013-12-10 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
BR112013008100A2 (pt) 2010-09-22 2016-08-09 Arena Pharm Inc "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles."
WO2012064973A2 (en) 2010-11-10 2012-05-18 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
TWI674262B (zh) 2011-01-10 2019-10-11 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
CA2828483A1 (en) 2011-02-23 2012-11-01 Intellikine, Llc Combination of kinase inhibitors and uses thereof
WO2012118945A2 (en) * 2011-03-03 2012-09-07 Merck Sharp & Dohme Corp. Fused bicyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors
DK2686313T3 (en) 2011-03-16 2016-05-02 Probiodrug Ag Benzimidazole derivatives as inhibitors of glutaminyl cyclase
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140066369A1 (en) 2011-04-19 2014-03-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US20140038889A1 (en) 2011-04-22 2014-02-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012145604A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012177714A1 (en) 2011-06-22 2012-12-27 Takeda Pharmaceutical Company Limited Substituted 6-aza-isoindolin-1-one derivatives
AU2012284088B2 (en) 2011-07-19 2015-10-08 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
KR20140063605A (ko) 2011-07-19 2014-05-27 인피니티 파마슈티칼스, 인코포레이티드 헤테로사이클릭 화합물 및 그의 용도
EP3392252B1 (en) 2011-08-23 2023-10-04 Libertas Bio, Inc. Pyrimido- pyridazinone compounds and use thereof
RU2014111823A (ru) 2011-08-29 2015-10-10 Инфинити Фармасьютикалз, Инк. Гетероциклические соединения и их применения
MX370814B (es) 2011-09-02 2020-01-08 Univ California Pirazolo[3,4-d]pirimidinas sustituidas y usos de las mismas.
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
AU2013287176C1 (en) 2012-06-13 2023-01-19 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
CA2886240A1 (en) 2012-09-26 2014-04-03 The Regents Of The University Of California Modulation of ire1
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
UA120087C2 (uk) 2013-04-19 2019-10-10 Інсайт Холдинґс Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
HUE057734T2 (hu) 2013-10-04 2022-06-28 Infinity Pharmaceuticals Inc Heterociklusos vegyületek és alkalmazásuk
WO2015053023A1 (ja) * 2013-10-08 2015-04-16 シャープ株式会社 画像表示装置
CN106456628A (zh) 2014-03-19 2017-02-22 无限药品股份有限公司 用于治疗PI3K‑γ介导的障碍的杂环化合物
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
KR101739003B1 (ko) * 2014-07-11 2017-05-23 에스티팜 주식회사 신규한 트리아졸로피리미디논 또는 트리아졸로피리디논 유도체, 및 이들의 용도
GB201415598D0 (en) 2014-09-03 2014-10-15 Univ Birmingham Elavated Itercranial Pressure Treatment
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
ES2751669T3 (es) 2015-02-20 2020-04-01 Incyte Corp Heterociclos bicíclicos como inhibidores FGFR
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
KR20180006881A (ko) 2015-03-09 2018-01-19 인테크린 테라퓨틱스, 아이엔씨. 비알코올성 지방간 질환 및/또는 지방이영양증의 치료 방법
EP3350183A1 (en) 2015-09-14 2018-07-25 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
KR101730790B1 (ko) 2015-12-24 2017-04-28 한국과학기술연구원 세로토닌 5-ｈｔ6 저해 활성을 갖는 5,6,7,8-테트라하이드로퀴나졸린-2-아민 화합물
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
SG10201912456RA (en) 2016-06-24 2020-02-27 Infinity Pharmaceuticals Inc Combination therapies
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
AU2018249822A1 (en) 2017-04-03 2019-10-31 Coherus Biosciences Inc. PPArgamma agonist for treatment of progressive supranuclear palsy
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
CA3099116A1 (en) 2018-05-04 2019-11-07 Incyte Corporation Salts of an fgfr inhibitor
JP2021523121A (ja) 2018-05-04 2021-09-02 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｆｇｆｒ阻害剤の固体形態及びその調製プロセス
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US20230054782A1 (en) * 2019-12-18 2023-02-23 Merck Sharp & Dohme Llc Bicyclic heterocycle compounds methods of use thereof for the treatment of herpes viruses
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr

Family Cites Families (308)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US114141A (en) * 1871-04-25 Improvement in steam-traps
US150344A (en) * 1874-04-28 Improvement in fluid-meters
US150353A (en) * 1874-04-28 Improvement in bearing-bars for furnace-grates
US150343A (en) * 1874-04-28 Ezra milleb
CH317122A (de) * 1952-09-03 1956-11-15 Basf Ag Verfahren zur Herstellung von Küpenfarbstoffen
DE1249281B (US20040242566A1-20041202-C00021.png) 1963-05-18
DE1670912C3 (de) 1967-08-18 1981-06-11 Bayer Ag, 5090 Leverkusen Herbizide Mittel auf Basis von 1,2,4-Triazin-5-onen
GB1377642A (en) * 1971-01-14 1974-12-18 Koninklijke Gist Spiritus Penicillanic and cephalosporanic acid derivatives
US3960949A (en) * 1971-04-02 1976-06-01 Schering Aktiengesellschaft 1,2-Biguanides
DE2150686A1 (de) 1971-10-12 1973-04-19 Basf Ag 6-amino-uracil-5-carbonsaeurethioamide
AU5996573A (en) 1972-09-11 1975-03-06 Commonwealth Scientific And Industrial Research Organisation Pyridinium salts
US3823135A (en) * 1972-12-26 1974-07-09 Shell Oil Co Pyrimidone herbicides
GB1464248A (en) 1973-11-01 1977-02-09 Ici Ltd Substituted triazinediones their preparation and use as herbicides
DE2361551A1 (de) 1973-12-11 1975-06-19 Basf Ag Wasserloesliche azofarbstoffe
DE2500024A1 (de) 1975-01-02 1976-07-08 Basf Ag Wasserloesliche azofarbstoffe
JPS535180A (en) 1976-07-01 1978-01-18 Sumitomo Chem Co Ltd Preparation of 3,4-dihydro-2 (1h) quinazoline derivatives
DE2720085A1 (de) 1977-05-05 1978-11-16 Hoechst Ag Pyrimido(6,1-a)isochinolin-2-on- derivate
US4494978A (en) * 1976-12-30 1985-01-22 Chevron Research Company Herbicidal N-(N'-hydrocarbyloxycarbamylalkyl)-2,6-dialkyl-alpha-haloacetanilides
CH657851A5 (de) 1983-06-28 1986-09-30 Ciba Geigy Ag Chromogene chinazolonverbindungen.
AR240698A1 (es) 1985-01-19 1990-09-28 Takeda Chemical Industries Ltd Procedimiento para preparar compuestos de 5-(4-(2-(5-etil-2-piridil)-etoxi)benzil)-2,4-tiazolidindiona y sus sales
US5614492A (en) 1986-05-05 1997-03-25 The General Hospital Corporation Insulinotropic hormone GLP-1 (7-36) and uses thereof
EP0306228B1 (en) 1987-09-04 1999-11-17 Beecham Group Plc Substituted thiazolidinedione derivatives
US4935493A (en) * 1987-10-06 1990-06-19 E. I. Du Pont De Nemours And Company Protease inhibitors
GB8900382D0 (en) 1989-01-09 1989-03-08 Janssen Pharmaceutica Nv 2-aminopyrimidinone derivatives
US5433955A (en) 1989-01-23 1995-07-18 Akzo N.V. Site specific in vivo activation of therapeutic drugs
IE63502B1 (en) 1989-04-21 1995-05-03 Zeneca Ltd Aminopyrimidine derivatives useful for treating cardiovascular disorders
US5366862A (en) 1990-02-14 1994-11-22 Receptor Laboratories, Inc. Method for generating and screening useful peptides
US5814460A (en) 1990-02-14 1998-09-29 Diatide, Inc. Method for generating and screening useful peptides
DE69129998T2 (de) 1990-02-15 1998-12-24 Takeda Chemical Industries Ltd Pyrimidindionderivate, deren Herstellung und Verwendung
US5462928A (en) 1990-04-14 1995-10-31 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type IV
DE4110019C2 (de) 1991-03-27 2000-04-13 Merck Patent Gmbh Imidazopyridine, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Zubereitungen
US5387512A (en) * 1991-06-07 1995-02-07 Merck & Co. Inc. Preparation of 3-[z-benzoxazol-2-yl)ethyl]-5-(1-hydroxyethyl)-6-methyl-2-(1H)-pyridinone by biotransformation
US6825169B1 (en) 1991-10-22 2004-11-30 Trustees Of Tufts College Inhibitors of dipeptidyl-aminopeptidase type IV
JPH07504158A (ja) 1991-10-22 1995-05-11 ニュー　イングランド　メディカル　センター　ホスピタルズ　インク ジペプチジル−アミノペプチダーゼｉｖ型のインヒビタ
US5350752A (en) 1991-12-16 1994-09-27 E. R. Squibb & Sons, Inc. Dihydropyrimidine derivatives
DE4141788A1 (de) 1991-12-18 1993-06-24 Merck Patent Gmbh Imidazopyridine
CA2129337A1 (en) * 1992-02-19 1993-09-02 Jotham W. Coe Heterocyclic compounds for enhancing antitumor activity
DE4305602A1 (de) 1992-06-17 1993-12-23 Merck Patent Gmbh Imidazopyridine
EP0915090A1 (en) 1992-09-10 1999-05-12 Eli Lilly And Company Compounds useful as hypoglycemic agents and for treating Alzheimer's disease
IL106998A0 (en) 1992-09-17 1993-12-28 Univ Florida Brain-enhanced delivery of neuroactive peptides by sequential metabolism
US5811281A (en) 1993-07-12 1998-09-22 Cornell Research Foundation, Inc. Immortalized intestinal epithelial cell lines
IL111785A0 (en) * 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
DE4341453A1 (de) 1993-12-06 1995-06-08 Merck Patent Gmbh Imidazopyridine
CA2184891C (en) 1994-03-08 2000-09-26 Yasuhisa Kuroki Phosphonic diester derivative
US5580979A (en) 1994-03-15 1996-12-03 Trustees Of Tufts University Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions
US5543396A (en) 1994-04-28 1996-08-06 Georgia Tech Research Corp. Proline phosphonate derivatives
AU2790895A (en) 1994-06-10 1996-01-05 Universitaire Instelling Antwerpen Purification of serine protease and synthetic inhibitors thereof
US5601986A (en) * 1994-07-14 1997-02-11 Amgen Inc. Assays and devices for the detection of extrahepatic biliary atresia
DE4432860A1 (de) 1994-09-15 1996-03-21 Merck Patent Gmbh Imidazopyridine
US5512549A (en) 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
US5717533A (en) * 1995-01-13 1998-02-10 Methode Electronics Inc. Removable optoelectronic module
US5879173A (en) * 1995-01-13 1999-03-09 Methode Electronics, Inc. Removable transceiver module and receptacle
US5864468A (en) * 1995-01-13 1999-01-26 Methode Electronics, Inc. Removable optoelectronic module with grounding means
US5734558A (en) * 1995-01-13 1998-03-31 Poplawski; Daniel S. Removable optoelectronic module
US5614379A (en) * 1995-04-26 1997-03-25 Eli Lilly And Company Process for preparing anti-obesity protein
JP2002515724A (ja) 1995-06-01 2002-05-28 ダナ−ファーバー キャンサー インスティテュート インコーポレイテッド ヒト血清中に見出されたジペプチジルペプチダーゼｉｖ（ｃｄ２６）の新規形態、その抗体および利用法
US6325989B1 (en) 1995-06-01 2001-12-04 Dana-Farber Cancer Institute, Inc. Form of dipeptidylpeptidase IV (CD26) found in human serum
DK0748800T3 (da) 1995-06-09 2001-08-27 Hoffmann La Roche Pyrimidindion-, pyrimidintrion- og triazindionderivater som alfa-1-adrenergiske receptorantagonister
JPH0928376A (ja) 1995-07-21 1997-02-04 Ajinomoto Co Inc 新規ジペプチジルペプチダーゼｉｖとその製造方法
TW445263B (en) * 1996-02-29 2001-07-11 Janssen Pharmaceutica Nv Novel esters of 1,4-disubstituted piperidine derivatives
US20020006899A1 (en) * 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
DE19616486C5 (de) 1996-04-25 2016-06-30 Royalty Pharma Collection Trust Verfahren zur Senkung des Blutglukosespiegels in Säugern
US5965532A (en) 1996-06-28 1999-10-12 Trustees Of Tufts College Multivalent compounds for crosslinking receptors and uses thereof
BR9711098B1 (pt) 1996-07-01 2011-10-04 compostos heterocìclicos, processo para sua preparação e composições farmacêuticas contendo os mesmos e seu uso no tratamento de diabetes e doenças relacionadas.
US5885997A (en) 1996-07-01 1999-03-23 Dr. Reddy's Research Foundation Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them and their use in the treatment of diabetes and related diseases
US6006753A (en) 1996-08-30 1999-12-28 Eli Lilly And Company Use of GLP-1 or analogs to abolish catabolic changes after surgery
US6458924B2 (en) 1996-08-30 2002-10-01 Novo Nordisk A/S Derivatives of GLP-1 analogs
US7235627B2 (en) 1996-08-30 2007-06-26 Novo Nordisk A/S Derivatives of GLP-1 analogs
US6011155A (en) 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
GB9702701D0 (en) 1997-02-01 1997-04-02 Univ Newcastle Ventures Ltd Quinazolinone compounds
JP3468007B2 (ja) * 1997-02-05 2003-11-17 住友電装株式会社 レバー式コネクタ
US20030060434A1 (en) * 1997-02-18 2003-03-27 Loretta Nielsen Combined tumor suppressor gene therapy and chemotherapy in the treatment of neoplasms
US6100234A (en) 1997-05-07 2000-08-08 Tufts University Treatment of HIV
AU7381098A (en) 1997-05-16 1998-12-08 Novo Nordisk Biotech, Inc. Polypeptides having prolyl pipeptidyl aminopeptidase activity and nucleic acids encoding same
EP0897012A1 (en) 1997-07-05 1999-02-17 Societe Des Produits Nestle S.A. Cloning of the prolyl-dipeptidyl-peptidase from aspergillus oryzae
US6235493B1 (en) * 1997-08-06 2001-05-22 The Regents Of The University Of California Amino acid substituted-cresyl violet, synthetic fluorogenic substrates for the analysis of agents in individual in vivo cells or tissue
IL125950A0 (en) * 1997-09-05 1999-04-11 Pfizer Prod Inc Methods of administering ampa receptor antagonists to treat dyskinesias associated with dopamine agonist therapy
US6258597B1 (en) 1997-09-29 2001-07-10 Point Therapeutics, Inc. Stimulation of hematopoietic cells in vitro
US6485955B1 (en) * 1997-10-06 2002-11-26 The Trustees Of Tufts University Quiescent cell dipeptidyl peptidase: a novel cytoplasmic serine protease
US6342611B1 (en) 1997-10-10 2002-01-29 Cytovia, Inc. Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for capsases and other enzymes and the use thereof
WO1999025719A1 (fr) 1997-11-18 1999-05-27 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Substance physiologiquement active, la sulphostine, procede de fabrication et utilisation
FR2771004B1 (fr) * 1997-11-19 2000-02-18 Inst Curie Utilisation de derives de benzhydryl sulfinyle pour la fabrication de medicaments ayant un effet eveillant dans des situations de troubles de la vigilance d'origine medicamenteuse
CN1247777C (zh) * 1997-12-16 2006-03-29 诺沃奇梅兹有限公司 具有氨肽酶活性的多肽及其编码核酸
US6380357B2 (en) * 1997-12-16 2002-04-30 Eli Lilly And Company Glucagon-like peptide-1 crystals
EP2574336A1 (en) 1998-02-02 2013-04-03 Trustees Of Tufts College Use of dipeptidylpeptidase inhibitors to regulate glucose metabolism
US20020061839A1 (en) * 1998-03-09 2002-05-23 Scharpe Simon Lodewijk Serine peptidase modulators
FR2777283B1 (fr) 1998-04-10 2000-11-24 Adir Nouveaux composes peptidiques analogues du glucagon-peptide- 1 (7-37), leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
BR9910907A (pt) 1998-06-05 2002-02-13 Point Therapeutics Inc Compostos cìclicos de boroprolina
DE19828114A1 (de) 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
US6129911A (en) 1998-07-10 2000-10-10 Rhode Island Hospital, A Lifespan Partner Liver stem cell
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
DE19844693A1 (de) * 1998-09-29 2000-03-30 Delphi Automotive Systems Gmbh Zweiteiliger elektrischer Verbinder
US20030176357A1 (en) 1998-10-06 2003-09-18 Pospisilik Andrew J. Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
GB9906715D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for promoting growth
US6548529B1 (en) * 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
EP1171438A1 (en) 1999-04-20 2002-01-16 Novo Nordisk A/S Compounds, their preparation and use
US6329336B1 (en) 1999-05-17 2001-12-11 Conjuchem, Inc. Long lasting insulinotropic peptides
DE19926233C1 (de) 1999-06-10 2000-10-19 Probiodrug Ges Fuer Arzneim Verfahren zur Herstellung von Thiazolidin
US6107317A (en) 1999-06-24 2000-08-22 Novartis Ag N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6110949A (en) 1999-06-24 2000-08-29 Novartis Ag N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6172081B1 (en) 1999-06-24 2001-01-09 Novartis Ag Tetrahydroisoquinoline 3-carboxamide derivatives
US6528486B1 (en) 1999-07-12 2003-03-04 Zealand Pharma A/S Peptide agonists of GLP-1 activity
US6617340B1 (en) 1999-07-29 2003-09-09 Novartis Ag N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
EP1216232B1 (en) * 1999-08-27 2006-10-11 ChemoCentryx Inc Heterocyclic compounds and methods for modulating cxcr3 function
ES2234662T3 (es) * 1999-09-16 2005-07-01 Curis, Inc. Mediadores de rutas de señalizacion hedgehog, composiciones y usos relacionados con los mismos.
US6559188B1 (en) * 1999-09-17 2003-05-06 Novartis Ag Method of treating metabolic disorders especially diabetes, or a disease or condition associated with diabetes
US6414002B1 (en) * 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
WO2001023364A1 (en) 1999-09-28 2001-04-05 Merck Patent Gmbh Quinazolinones
US6447772B1 (en) 1999-10-01 2002-09-10 Klaire Laboratories, Inc. Compositions and methods relating to reduction of symptoms of autism
US6251391B1 (en) * 1999-10-01 2001-06-26 Klaire Laboratories, Inc. Compositions containing dipepitidyl peptidase IV and tyrosinase or phenylalaninase for reducing opioid-related symptons
JP2001172257A (ja) * 1999-10-05 2001-06-26 Fujisawa Pharmaceut Co Ltd 有機スルホンアミド化合物
CA2392209A1 (en) 1999-10-08 2001-04-19 Kazuyuki Fujishima M-substituted benzoic acid derivatives having integrin .alpha.v.beta.3 antagonistic activity
US6261794B1 (en) * 1999-10-14 2001-07-17 Saint Louis University Methods for identifying inhibitors of methionine aminopeptidases
US7230000B1 (en) * 1999-10-27 2007-06-12 Cytokinetics, Incorporated Methods and compositions utilizing quinazolinones
CA2388646C (en) * 1999-10-27 2009-01-27 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US20040152745A1 (en) 1999-11-12 2004-08-05 Guilford Pharmaceuticals, Inc. Dipeptidyl peptidase IV inhibitors and methods of making and using dipeptidyl peptidase IV inhibitors
WO2001034594A1 (en) 1999-11-12 2001-05-17 Guilford Pharmaceuticals, Inc. Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
GB9928330D0 (en) * 1999-11-30 2000-01-26 Ferring Bv Novel antidiabetic agents
US6517382B2 (en) * 1999-12-01 2003-02-11 Tyco Electronics Corporation Pluggable module and receptacle
WO2001041779A2 (en) * 1999-12-08 2001-06-14 1149336 Ontario Inc. Combined use of glp-2 receptor agonist and chemotherapeutic agent in treatment
US6380398B2 (en) 2000-01-04 2002-04-30 Novo Nordisk A/S Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
JP2003520226A (ja) * 2000-01-21 2003-07-02 ノバルティス アクチエンゲゼルシャフト ジペプチジルペプチダーゼ−ｉｖ阻害剤および抗糖尿病薬剤を含む組合せ物
WO2001055213A2 (en) * 2000-01-27 2001-08-02 Eli Lilly And Company Process for solubilizing glucagon-like peptide 1 (glp-1) compounds
US6569901B2 (en) 2000-01-28 2003-05-27 Novo Nordisk A/S Alkynyl-substituted propionic acid derivatives, their preparation and use
US7217722B2 (en) 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
US6448045B1 (en) 2000-03-10 2002-09-10 The Regents Of The University Of California Inducing insulin gene expression in pancreas cells expressing recombinant PDX-1
US6395767B2 (en) * 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
US6608038B2 (en) 2000-03-15 2003-08-19 Novartis Ag Methods and compositions for treatment of diabetes and related conditions via gene therapy
EP1136482A1 (en) 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-Amino-3-(alkyl)-pyrimidone derivatives as GSK3beta inhibitors
US6555519B2 (en) 2000-03-30 2003-04-29 Bristol-Myers Squibb Company O-glucosylated benzamide SGLT2 inhibitors and method
ATE419036T1 (de) 2000-03-31 2009-01-15 Prosidion Ltd Verbesserung der aktivität der inselzellen bei diabetes mellitus und dessen prävention
US6573096B1 (en) 2000-04-01 2003-06-03 The Research Foundation At State University Of New York Compositions and methods for inhibition of cancer invasion and angiogenesis
US6545170B2 (en) 2000-04-13 2003-04-08 Pharmacia Corporation 2-amino-5, 6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors
PT3029041T (pt) * 2000-04-25 2020-05-13 Icos Corp Inibidores de fosfatidil-inositol 3-quinase delta humana
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
GB0010188D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
US6783757B2 (en) 2000-06-01 2004-08-31 Kirkman Group, Inc. Composition and method for increasing exorphin catabolism to treat autism
TW583185B (en) 2000-06-13 2004-04-11 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same
US6432969B1 (en) 2000-06-13 2002-08-13 Novartis Ag N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6627636B2 (en) 2000-06-15 2003-09-30 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
US6620821B2 (en) 2000-06-15 2003-09-16 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
GB0014969D0 (en) 2000-06-19 2000-08-09 Smithkline Beecham Plc Novel method of treatment
US7078397B2 (en) 2000-06-19 2006-07-18 Smithkline Beecham Corporation Combinations of dipeptidyl peptidase IV inhibitors and other antidiabetic agents for the treatment of diabetes mellitus
AU2001268958B2 (en) 2000-07-04 2006-03-09 Novo Nordisk A/S Heterocyclic compounds, which are inhibitors of the enzyme dpp-iv
JP2002042960A (ja) * 2000-07-25 2002-02-08 Yazaki Corp コネクタ支持機構
AU2001281083A1 (en) 2000-08-01 2002-02-13 Pharmacia Corporation Hexahydro-7-1h-azepin-2-yl-haxanoic acid derivatives as inhibitors of inducible nitric oxide synthase
US7022711B2 (en) 2000-08-04 2006-04-04 Warner-Lambert Company 2-(4-Pyridyl)amino-6-dialkoxyphenyl-pyrido[2,3-d]pyrimidin-7-ones
EP1950199B1 (en) 2000-08-10 2009-12-02 Mitsubishi Tanabe Pharma Corporation Proline derivatives and use thereof as drugs
US20020165237A1 (en) 2000-08-11 2002-11-07 Fryburg David Albert Treatment of the insulin resistance syndrome
US20020037829A1 (en) 2000-08-23 2002-03-28 Aronson Peter S. Use of DPPIV inhibitors as diuretic and anti-hypertensive agents
US6900226B2 (en) * 2000-09-06 2005-05-31 Hoffman-La Roche Inc. Neuropeptide Y antagonists
WO2002026729A2 (en) * 2000-09-27 2002-04-04 Merck & Co., Inc. Benzopyrancarboxylic acid derivatives for the treatment of diabetes and lipid disorders
US20020064736A1 (en) 2000-09-27 2002-05-30 Fuji Photo Film Co., Ltd. Dye-forming coupler, silver halide photographic light-sensitive material, and method for producing an azomethine dye
IL154893A0 (en) * 2000-10-06 2003-10-31 Tanabe Seiyaku Co Aliphatic nitrogen-containing cyclic compounds, methods for the preparation thereof and pharmaceutical compositions containing the same
PL366005A1 (en) 2000-10-12 2005-01-24 Ferring Bv Novel serine protease genes related to dppiv
AUPR107800A0 (en) * 2000-10-27 2000-11-23 University Of Sydney, The Peptide and nucleic acid molecule ii
RU2003115614A (ru) 2000-10-27 2004-10-27 Пробиодруг Аг (De) Способ лечения неврологических и нейропсихологических нарушений
US6686337B2 (en) * 2000-10-30 2004-02-03 Ortho-Mcneil Pharmaceutical, Inc. Combination therapy comprising anti-diabetic and anticonvulsant agents
AU2002246568A1 (en) 2000-10-31 2002-08-06 Vanderbilt University Biological markers and diagnostic tests for angiotensin converting enzyme inhibitor- and vasopeptidase inhibitor-associated angioedema
WO2002060434A2 (en) 2000-10-31 2002-08-08 Merck & Co., Inc. Benzopyrancarboxylic acid derivatives for the treatment of diabetes and lipid disorders
AU2002225954A1 (en) 2000-11-08 2002-05-21 The University Of Georgia Research Foundation, Inc. Dipeptidylpeptidases and methods of use
US20030055052A1 (en) * 2000-11-10 2003-03-20 Stefan Peters FAP-activated anti-tumor compounds
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
US20020155565A1 (en) 2000-11-10 2002-10-24 Pilar Garin-Chesa FAP-activated anti-tumor compounds
US20030203946A1 (en) 2000-11-17 2003-10-30 Carsten Behrens Glucagon antagonists/inverse agonists
EP1343763A1 (en) * 2000-11-20 2003-09-17 Bristol-Myers Squibb Company Pyrodone derivatives as ap2 inhibitors
HUP0500880A2 (en) 2000-12-11 2006-05-29 Tularik Inc Cxcr3 antagonists and pharmaceutical compositions thereof
US20040180925A1 (en) 2000-12-27 2004-09-16 Kenji Matsuno Dipeptidylpeptidase-IV inhibitor
DE10100053A1 (de) 2001-01-02 2002-08-22 Keyneurotek Ag I G Verwendung von Enzyminhibitoren der Dipeptidylpeptidase IV sowie der Aminopeptidase N und pharmazeutischen Zubereitungen daraus zur Prävention und/oder Therapie Ischämie-bedingter akuter und chronischer neurodegenerativer Prozesse und Erkrankungen
CZ20032321A3 (en) 2001-02-02 2004-03-17 Takeda Chemical Industries, Ltd. Fused heterocyclic compounds
WO2002062798A2 (en) * 2001-02-05 2002-08-15 Dr. Reddy's Laboratories Ltd. Salts of pyrimidine derivatives for use against coronary heart disease and atherosclerose
TWI255817B (en) 2001-02-14 2006-06-01 Kissei Pharmaceutical Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof
PT1953162E (pt) * 2001-02-24 2012-07-13 Boehringer Ingelheim Pharma Derivados de xantina, sua preparação e sua utilização como produto farmacêutico
US6337069B1 (en) * 2001-02-28 2002-01-08 B.M.R.A. Corporation B.V. Method of treating rhinitis or sinusitis by intranasally administering a peptidase
US6371787B1 (en) * 2001-03-07 2002-04-16 International Business Machines Corporation Pull-to-release type latch mechanism for removable small form factor electronic modules
EP1372650B1 (en) * 2001-03-19 2008-11-19 Novartis AG Combinations comprising an antidiarrheal agent and an epothilone or an epothilone derivative
EP1385508B1 (en) * 2001-03-27 2008-05-21 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
FR2822826B1 (fr) 2001-03-28 2003-05-09 Servier Lab Nouveaux derives sulfonyles d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE10115921A1 (de) 2001-03-30 2002-10-02 Boehringer Ingelheim Pharma Verfahren zur Herstellung von 4,6-Diaminopyrimido[5,4-d]pyrimidinen
US6890905B2 (en) * 2001-04-02 2005-05-10 Prosidion Limited Methods for improving islet signaling in diabetes mellitus and for its prevention
GB0109146D0 (en) 2001-04-11 2001-05-30 Ferring Bv Treatment of type 2 diabetes
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
PE20021080A1 (es) * 2001-04-12 2003-02-12 Boehringer Ingelheim Int Un anticuerpo especifico fapo bibh1 en el tratamiento del cancer
FR2824825B1 (fr) 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US20030060494A1 (en) 2001-05-18 2003-03-27 Nobuyuki Yasuda Pharmaceutical use of N-carbamoylazole derivatives
US7105556B2 (en) 2001-05-30 2006-09-12 Bristol-Myers Squibb Company Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
US6794379B2 (en) 2001-06-06 2004-09-21 Tularik Inc. CXCR3 antagonists
KR100490048B1 (ko) * 2001-06-19 2005-05-17 삼성전자주식회사 액정 표시 장치 제조용 인라인 시스템 및 이를 이용하는 액정 표시 장치의 제조 방법
CA2450475A1 (en) 2001-06-20 2003-01-03 Linda Brockunier Dipeptidyl peptidase inhibitors for the treatment of diabetes
WO2003000180A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
CN1990469A (zh) 2001-06-27 2007-07-04 史密丝克莱恩比彻姆公司 作为二肽酶抑制剂的氟代吡咯烷
US20030135023A1 (en) * 2001-06-27 2003-07-17 Hans-Ulrich Demuth Peptide structures useful for competitive modulation of dipeptidyl peptidase IV catalysis
WO2003002593A2 (en) 2001-06-27 2003-01-09 Probiodrug Ag Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
US7368421B2 (en) 2001-06-27 2008-05-06 Probiodrug Ag Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
US20030130199A1 (en) 2001-06-27 2003-07-10 Von Hoersten Stephan Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
WO2003002553A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
DE60223920T2 (de) 2001-06-27 2008-11-13 Smithkline Beecham Corp. Pyrrolidine als dipeptidyl-peptidase-inhibitoren
WO2003072556A1 (en) 2001-06-27 2003-09-04 Prosidion Ltd. Glutaminyl based dpiv inhibitors
DE10150203A1 (de) 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
US6869947B2 (en) * 2001-07-03 2005-03-22 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
US20030144350A1 (en) 2001-07-20 2003-07-31 Adipogenix, Inc. Fat accumulation-modulation compounds
EP1285922A1 (en) 2001-08-13 2003-02-26 Warner-Lambert Company 1-Alkyl or 1-cycloalkyltriazolo[4,3-a]quinazolin-5-ones as phosphodiesterase inhibitors
JP2005508891A (ja) 2001-08-13 2005-04-07 プロバイオドラッグ アーゲー レグマインの不可逆性システインプロテアーゼ阻害剤
US6844316B2 (en) * 2001-09-06 2005-01-18 Probiodrug Ag Inhibitors of dipeptidyl peptidase I
DE10143840A1 (de) 2001-09-06 2003-03-27 Probiodrug Ag Neue Inhibitoren der Dipeptidylpeptidase I
US20030186963A1 (en) 2001-09-14 2003-10-02 Dorwald Florencio Zaragoza Substituted piperidines
KR20040033048A (ko) 2001-09-14 2004-04-17 미츠비시 웰파마 가부시키가이샤 티아졸리딘 유도체 및 이의 약학적 용도
US6673829B2 (en) * 2001-09-14 2004-01-06 Novo Nordisk A/S Aminoazetidine,-pyrrolidine and -piperidine derivatives
EP1463727A2 (en) 2001-09-19 2004-10-06 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
BRPI0212726B8 (pt) 2001-09-21 2021-05-25 Bristol Myers Squibb Co compostos contendo lactamas, e derivados dos mesmos, composição farmacêutica que os compreende e seus usos
ATE312827T1 (de) 2001-09-21 2005-12-15 Mitsubishi Pharma Corp 3-substituierte-4-pyrimidonderivate
AU2002337499B2 (en) 2001-09-21 2007-08-23 Mitsubishi Pharma Corporation 3-substituted-4-pyrimidone derivatives
US7019010B2 (en) * 2001-09-27 2006-03-28 Novertis Ag Combinations
HUP0402338A3 (en) * 2001-10-01 2008-10-28 Bristol Myers Squibb Co Spiro-hydantoin compounds, their use as anti-inflammatory agents, pharmaceutical compositions containing them and intermediates for preparing them
WO2003030946A1 (en) 2001-10-09 2003-04-17 Novartis Ag Regulation of insulin production
US7064135B2 (en) 2001-10-12 2006-06-20 Novo Nordisk Inc. Substituted piperidines
TWI301834B (en) 2001-10-22 2008-10-11 Eisai R&D Man Co Ltd Pyrimidone compound and pharmaceutical composition including the same
GB0125445D0 (en) 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
US6861440B2 (en) * 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
EP1442028A4 (en) 2001-11-06 2009-11-04 Bristol Myers Squibb Co SUBSTITUTED ACID DERIVATIVES, WHICH APPRECIATE AS ANTIDIBILICS AND AGENTS AGAINST OBESITAS, AND METHODS
AU2002363429B2 (en) * 2001-11-07 2008-05-08 Merck & Co., Inc. Mitotic kinesin inhibitors
US20030125304A1 (en) * 2001-11-09 2003-07-03 Hans-Ulrich Demuth Substituted amino ketone compounds
US20030089935A1 (en) 2001-11-13 2003-05-15 Macronix International Co., Ltd. Non-volatile semiconductor memory device with multi-layer gate insulating structure
EP2769715A3 (en) 2001-11-26 2014-09-17 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
MXPA04004956A (es) 2001-11-26 2004-08-11 Schering Corp Antagonistas de la hormona concentradora de melanina basados en la piperidina para tratamiento de la obesidad y de trastornos del sistema nervioso central.
CA2468192A1 (en) 2001-11-26 2003-06-05 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
WO2003048081A2 (en) 2001-12-04 2003-06-12 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
ES2291543T3 (es) * 2001-12-06 2008-03-01 MERCK & CO., INC. Inhibicion de kinesina mitotica.
JP2005518377A (ja) 2001-12-14 2005-06-23 ノボ　ノルディスク　アクティーゼルスカブ ホルモン感受性リパーゼの活性を低下させるための化合物の使用
TW200301698A (en) 2001-12-21 2003-07-16 Bristol Myers Squibb Co Acridone inhibitors of IMPDH enzyme
KR101018318B1 (ko) 2001-12-21 2011-03-04 노보 노르디스크 에이/에스 Ｇｋ 활성제로서의 아미드 유도체
US6727261B2 (en) * 2001-12-27 2004-04-27 Hoffman-La Roche Inc. Pyrido[2,1-A]Isoquinoline derivatives
AU2002351753A1 (en) * 2001-12-29 2003-07-30 Novo Nordisk A/S Combined use of a glp-1 compound and a modulator of diabetic late complications
AU2003201274A1 (en) 2002-01-11 2003-07-24 Novo Nordisk A/S Compositions comprising inhibitors of dpp-iv and nep enzymes for the treatment of diabetes
US7101898B2 (en) 2002-02-01 2006-09-05 Novo Nordisk A/S Amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes
AU2003218969A1 (en) 2002-02-01 2003-09-02 Probiodrug Ag Modulation of t lymphocytes using dp iv inhibitors
AU2003206834B2 (en) 2002-02-13 2006-10-19 F. Hoffmann-La Roche Ag Novel pyridine- and quinoline-derivatives
CA2474578C (en) * 2002-02-13 2009-08-25 F. Hoffmann-La Roche Ag Novel pyridin- and pyrimidin-derivatives
DE60301491T2 (de) 2002-02-27 2006-05-18 Pfizer Products Inc., Groton Acc-hemmer
SI1480961T1 (sl) 2002-02-28 2007-06-30 Prosidion Ltd Inhibitorji dpiv na osnovi glutaminila
AU2003228283A1 (en) 2002-03-07 2003-09-22 X-Ceptor Therapeutics, Inc. Quinazolinone modulators of nuclear receptors
US20030232761A1 (en) 2002-03-28 2003-12-18 Hinke Simon A. Novel analogues of glucose-dependent insulinotropic polypeptide
US20040106802A1 (en) * 2002-04-08 2004-06-03 Torrent Pharmaceuticals Ltd. Novel compounds and therapeutic uses thereof
CN1633420A (zh) 2002-04-08 2005-06-29 托伦脱药品有限公司 噻唑烷－4－腈和类似物以及它们作为二肽基－肽酶抑制剂的用途
JP2003300977A (ja) 2002-04-10 2003-10-21 Sumitomo Pharmaceut Co Ltd キサンチン誘導体
CA2484551A1 (en) 2002-04-30 2003-11-13 Trustees Of Tufts College Smart pro-drugs of serine protease inhibitors
TW200307667A (en) 2002-05-06 2003-12-16 Bristol Myers Squibb Co Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
US7057046B2 (en) 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
MXPA04011557A (es) 2002-05-23 2005-07-05 Chiron Corp Compuestos de quinazolinona sustituida.
GB0212412D0 (en) 2002-05-29 2002-07-10 Novartis Ag Combination of organic compounds
US6710040B1 (en) * 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
AU2003233010A1 (en) 2002-06-04 2003-12-19 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
BR0311697A (pt) * 2002-06-06 2005-03-22 Eisai Co Ltd Novos derivados condensados de imidazol
US20040009972A1 (en) * 2002-06-17 2004-01-15 Ding Charles Z. Benzodiazepine inhibitors of mitochondial F1F0 ATP hydrolase and methods of inhibiting F1F0 ATP hydrolase
WO2003106416A2 (en) 2002-06-17 2003-12-24 Smithkline Beecham Corporation Chemical process
SE0201976D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
US20040054171A1 (en) * 2002-07-04 2004-03-18 Jensen Anette Frost Polymorphic forms of a 4H-thieno[3,2-E]-1,2,4-thiadiazine 1,1-dioxide derivative
DK1528931T3 (da) 2002-08-09 2008-09-08 Prosidion Ltd Dipeptidylpeptidase-IV-inhibitorer til reduktion af hastigheden af kronisk vægtforögelse
US20040048853A1 (en) * 2002-08-21 2004-03-11 Gustave Bergnes Compounds, compositions, and methods
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
US7495005B2 (en) 2002-08-22 2009-02-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, their preparation and their use in pharmaceutical compositions
DE10238477A1 (de) * 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel
US6998502B1 (en) 2002-09-05 2006-02-14 Sabinsa Corporation Convenient process of manufacture for difluoromethylornithine and related compounds
EP1407774A1 (en) * 2002-09-10 2004-04-14 LION Bioscience AG 2-Amino-4-quinazolinones as LXR nuclear receptor binding compounds
EP1398032A1 (en) 2002-09-10 2004-03-17 PheneX Pharmaceuticals AG 4-Oxo-quinazolines as LXR nuclear receptor binding compounds
JP2004123738A (ja) 2002-09-11 2004-04-22 Takeda Chem Ind Ltd 徐放性製剤
ATE461212T1 (de) 2002-09-18 2010-04-15 Prosidion Ltd Sekundäre bindungsstelle von dipeptidylpeptidase iv (dp iv)
US20040058876A1 (en) 2002-09-18 2004-03-25 Torsten Hoffmann Secondary binding site of dipeptidyl peptidase IV (DP IV)
US7262207B2 (en) 2002-09-19 2007-08-28 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
US6869966B2 (en) * 2002-09-30 2005-03-22 Banyu Pharmaceutical Co., Ltd. N-substituted-2-oxodihydropyridine derivatives
NZ538897A (en) 2002-10-18 2007-02-23 Merck & Co Inc Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004037176A2 (en) 2002-10-21 2004-05-06 Bristol-Myers Squibb Company Quinazolinones and derivatives thereof as factor xa inhibitors
AU2003282983A1 (en) 2002-10-23 2004-05-13 Bristol-Myers Squibb Company Glycinenitrile-based inhibitors of dipeptidyl peptidase iv and methods
US7482337B2 (en) 2002-11-08 2009-01-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
MXPA05005260A (es) * 2002-11-18 2005-07-25 Pfizer Prod Inc Amidas ciclicas fluoradas que inhiben la dipeptidil peptidasa iv.
DE10254304A1 (de) 2002-11-21 2004-06-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
UY28103A1 (es) * 2002-12-03 2004-06-30 Boehringer Ingelheim Pharma Nuevas imidazo-piridinonas sustituidas, su preparación y su empleo como medicacmentos
DE10256264A1 (de) 2002-12-03 2004-06-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Imidazo-pyridinone und Imidazo-pyridazinone, ihre Herstellung und ihre Verwendung als Arzneimittel
US7109192B2 (en) 2002-12-03 2006-09-19 Boehringer Ingelheim Pharma Gmbh & Co Kg Substituted imidazo-pyridinones and imidazo-pyridazinones, the preparation thereof and their use as pharmaceutical compositions
US7135467B2 (en) 2003-01-13 2006-11-14 Bristol-Myers Squibb Company HIV integrase inhibitors
US7148246B2 (en) 2003-02-27 2006-12-12 Sanofi-Aventis Deutschland Gmbh Cycloalkyl derivatives having bioisosteric carboxylic acid groups, processes for their preparation and their use as pharmaceuticals
US20060270689A1 (en) * 2003-03-07 2006-11-30 Astrazeneca Ab Novel Fused Heterocycles and Uses Thereof
US20050014732A1 (en) * 2003-03-14 2005-01-20 Pharmacia Corporation Combination of an aldosterone receptor antagonist and an anti-diabetic agent
JP4887139B2 (ja) 2003-03-25 2012-02-29 武田薬品工業株式会社 ジペプチジルペプチダーゼインヒビター
TWI357408B (en) 2003-03-26 2012-02-01 Mitsubishi Tanabe Pharma Corp 3-substituted-4-pyrimidone derivatives
US7371871B2 (en) 2003-05-05 2008-05-13 Probiodrug Ag Inhibitors of glutaminyl cyclase
US7381537B2 (en) 2003-05-05 2008-06-03 Probiodrug Ag Use of inhibitors of glutaminyl cyclases for treatment and prevention of disease
EP1622870A2 (en) 2003-05-05 2006-02-08 Prosidion Ltd. Glutaminyl based dp iv-inhibitors
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7566707B2 (en) 2003-06-18 2009-07-28 Boehringer Ingelheim International Gmbh Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions
ES2355105T3 (es) 2003-06-20 2011-03-22 F. Hoffmann-La Roche Ag Pirido(2,1-a)isoquinolina como inhibidores de la dpp-iv.
RU2339636C2 (ru) 2003-06-20 2008-11-27 Ф.Хоффманн-Ля Рош Аг Гексагидропиридоизохинолины в качестве ингибиторов дипептидилпептидазы iv (dpp-iv)
JO2625B1 (en) * 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salts of dipeptidyl betidase inhibitor 4
US6995183B2 (en) * 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
ZA200602051B (en) 2003-08-13 2007-10-31 Takeda Pharmaceutical 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors
WO2005019168A2 (en) 2003-08-20 2005-03-03 Pfizer Products Inc. Fluorinated lysine derivatives as dipeptidyl peptidase iv inhibitors
US20050065144A1 (en) 2003-09-08 2005-03-24 Syrrx, Inc. Dipeptidyl peptidase inhibitors
US7790734B2 (en) 2003-09-08 2010-09-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7368453B2 (en) * 2003-11-19 2008-05-06 Chiron Corporation Quinazolinone compounds with reduced bioaccumulation
CN1918131B (zh) 2004-02-05 2011-05-04 前体生物药物股份公司 谷氨酰胺酰基环化酶抑制剂
GEP20094679B (en) 2004-03-15 2009-05-10 Takeda Pharmaceuticals Co Dipeptidyl peptidase inhibitors
EP1828192B1 (en) 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN102311447A (zh) * 2010-07-07 2012-01-11 中国科学院广州生物医药与健康研究院 杂环并嘧啶酮类dpp-iv抑制剂
CN102311448A (zh) * 2010-07-07 2012-01-11 中国科学院广州生物医药与健康研究院 噻吩并嘧啶酮类dpp-iv抑制剂
CN102329325A (zh) * 2010-07-07 2012-01-25 中国科学院广州生物医药与健康研究院 吡咯并嘧啶酮类dpp-iv抑制剂
CN102329325B (zh) * 2010-07-07 2013-11-27 中国科学院广州生物医药与健康研究院 吡咯并嘧啶酮类dpp-iv抑制剂
CN103130819A (zh) * 2011-12-01 2013-06-05 中国科学院上海药物研究所 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途
US9045491B2 (en) 2011-12-01 2015-06-02 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Thienyl [3,2-D] pyrimidin-4-one compounds, preparation method, pharmaceutical compositions and use thereof
CN103130819B (zh) * 2011-12-01 2016-01-20 中国科学院上海药物研究所 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途
CN106045922A (zh) * 2016-06-12 2016-10-26 湘潭大学 2‑(氨基)甲基喹唑啉‑4(3h)‑酮类化合物及其制备方法和用途

Also Published As

Publication number Publication date
US7687625B2 (en) 2010-03-30
WO2004087053A3 (en) 2006-08-31
EP1608317A4 (en) 2006-12-27
EP1608317A2 (en) 2005-12-28
WO2004087053A2 (en) 2004-10-14
EP1608317B1 (en) 2012-09-26
US7550590B2 (en) 2009-06-23
US20040242568A1 (en) 2004-12-02
JP4887139B2 (ja) 2012-02-29
KR20050122220A (ko) 2005-12-28
US20040259870A1 (en) 2004-12-23
CA2518465A1 (en) 2004-10-14
US20040242566A1 (en) 2004-12-02
US20050004117A1 (en) 2005-01-06
WO2004087053A9 (en) 2004-11-11
JP2007524600A (ja) 2007-08-30

Similar Documents

Publication Publication Date Title
CN1894234A (zh) 二肽基肽酶抑制剂
CN100340559C (zh) 作为凝血因子xa抑制剂的含氮杂双环
CN1867560A (zh) 4－嘧啶酮衍生物及其作为肽基肽酶抑制剂的用途
CN1926128A (zh) 二肽基肽酶抑制剂
CN1882591A (zh) 具有PDE－5抑制活性的5,7－二氨基吡唑并[4,3－d]嘧啶
CN1280291C (zh) 用作磷酸二酯酶抑制剂的取代的吡咯并吡啶酮衍生物
CN1596253A (zh) 用作抗炎药的螺－乙内酰脲化合物
CN1407985A (zh) 用作钾通道抑制剂的杂环二氢嘧啶
CN1622946A (zh) 治疗与p38激酶有关的症状的方法以及用作激酶抑制剂的吡咯并三嗪化合物
CN1871240A (zh) 吡咯并嘧啶酮衍生物
CN1599734A (zh) 作为cxc趋化因子受体拮抗剂的3,4－二取代的马来酰亚胺化合物
CN1768061A (zh) 作为大麻素受体配体的吡唑并[1,5－a][1,3,5]三嗪衍生物
CN1071164A (zh) 含氮杂环化合物
CN1922182A (zh) 作为激酶抑制剂的吡咯并三嗪化合物
CN1639165A (zh) 作为激酶抑制剂的嘌呤衍生物
CN1662509A (zh) 可用作激酶抑制剂的吡咯并三嗪苯胺化合物
CN101031560A (zh) 用作酪氨酸激酶抑制剂的环状二芳基脲
CN1205335A (zh) 三环二氮杂䓬加压素拮抗剂和催产素拮抗剂
CN1040755C (zh) 杂环化合物的制备方法
CN1829709A (zh) 对抗黄病毒的双环咪唑衍生物
CN1156995A (zh) 玻璃体结合蛋白受体拮抗剂
CN1553909A (zh) 作为gaba受体配体的苯并咪唑和吡啶并咪唑衍生物
CN1646499A (zh) 稠合哒嗪衍生物化合物和含这些化合物作为活性成分的药物
CN1922174A (zh) 病毒聚合酶抑制剂
CN1809565A (zh) 用于治疗癌症的吡咯并二氢异喹啉

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication