JP4300108B2 - ジペプチジルペプチダーゼ阻害剤としてのピロリジン類 - Google Patents

ジペプチジルペプチダーゼ阻害剤としてのピロリジン類 Download PDF

Info

Publication number
JP4300108B2
JP4300108B2 JP2003508713A JP2003508713A JP4300108B2 JP 4300108 B2 JP4300108 B2 JP 4300108B2 JP 2003508713 A JP2003508713 A JP 2003508713A JP 2003508713 A JP2003508713 A JP 2003508713A JP 4300108 B2 JP4300108 B2 JP 4300108B2
Authority
JP
Japan
Prior art keywords
compound
mmol
dpp
added
solution
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.)
Expired - Fee Related
Application number
JP2003508713A
Other languages
English (en)
Japanese (ja)
Other versions
JP2005518337A (ja
JP2005518337A5 (enExample
Inventor
ハフナー,コート,デール
マクドウガルド,ダリル,リン
ランドハワ,アマージット,サブ
レイスター,スティーブン,マイケル
デアトン,デービッド,エヌ.
レンハード,ジェームス,マーティン
Original Assignee
スミスクライン ビーチャム コーポレーション
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 スミスクライン ビーチャム コーポレーション filed Critical スミスクライン ビーチャム コーポレーション
Publication of JP2005518337A publication Critical patent/JP2005518337A/ja
Publication of JP2005518337A5 publication Critical patent/JP2005518337A5/ja
Application granted granted Critical
Publication of JP4300108B2 publication Critical patent/JP4300108B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • C07D207/2732-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • 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
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06Antiabortive agents; Labour repressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • 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
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C07D207/48Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D277/06Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Gynecology & Obstetrics (AREA)
  • AIDS & HIV (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
JP2003508713A 2001-06-27 2002-06-26 ジペプチジルペプチダーゼ阻害剤としてのピロリジン類 Expired - Fee Related JP4300108B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30133301P 2001-06-27 2001-06-27
US38701102P 2002-06-06 2002-06-06
PCT/US2002/020466 WO2003002530A2 (en) 2001-06-27 2002-06-26 Pyrrolidines as dipeptidyl peptidase inhibitors

Publications (3)

Publication Number Publication Date
JP2005518337A JP2005518337A (ja) 2005-06-23
JP2005518337A5 JP2005518337A5 (enExample) 2005-12-22
JP4300108B2 true JP4300108B2 (ja) 2009-07-22

Family

ID=26972304

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2003508713A Expired - Fee Related JP4300108B2 (ja) 2001-06-27 2002-06-26 ジペプチジルペプチダーゼ阻害剤としてのピロリジン類

Country Status (8)

Country Link
US (1) US7196201B2 (enExample)
EP (1) EP1399420B1 (enExample)
JP (1) JP4300108B2 (enExample)
AT (1) ATE380175T1 (enExample)
AU (1) AU2002316437A1 (enExample)
DE (1) DE60223920T2 (enExample)
ES (1) ES2296962T3 (enExample)
WO (1) WO2003002530A2 (enExample)

Families Citing this family (156)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0010188D0 (en) * 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
DE60226723D1 (de) 2001-03-27 2008-07-03 Merck & Co Inc Dipeptidylpeptidase-hemmer für die behandlung oder prävention von diabetes
US20030199000A1 (en) * 2001-08-20 2003-10-23 Valkirs Gunars E. Diagnostic markers of stroke and cerebral injury and methods of use thereof
US20040176914A1 (en) * 2001-04-13 2004-09-09 Biosite Incorporated Methods and compositions for measuring biologically active natriuretic peptides and for improving their therapeutic potential
US20030219734A1 (en) * 2001-04-13 2003-11-27 Biosite Incorporated Polypeptides related to natriuretic peptides and methods of their identification and use
US7524635B2 (en) * 2003-04-17 2009-04-28 Biosite Incorporated Methods and compositions for measuring natriuretic peptides and uses thereof
CA2414073A1 (en) * 2001-05-04 2002-11-14 Gunars E. Valkirs Diagnostic markers of acute coronary syndromes and methods of use thereof
CN1990468A (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
US20040209307A1 (en) * 2001-08-20 2004-10-21 Biosite Incorporated Diagnostic markers of stroke and cerebral injury and methods of use thereof
US20040219509A1 (en) * 2001-08-20 2004-11-04 Biosite, Inc. Diagnostic markers of stroke and cerebral injury and methods of use thereof
US7608406B2 (en) * 2001-08-20 2009-10-27 Biosite, Inc. Diagnostic markers of stroke and cerebral injury and methods of use thereof
DE60233949D1 (de) * 2001-08-20 2009-11-19 Biosite Inc Diagnostische marker für schlaganfall und hirntrauma sowie verfahren zur verwendung davon
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
AU2003297564A1 (en) * 2002-12-04 2004-06-23 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
KR20050122220A (ko) 2003-03-25 2005-12-28 다케다 샌디에고, 인코포레이티드 디펩티딜 펩티다제 억제제
ATE464889T1 (de) 2003-05-05 2010-05-15 Probiodrug Ag Medizinische verwendung von hemmern von glutaminyl und glutamatcyclasen
DE602004026712D1 (de) 2003-05-05 2010-06-02 Probiodrug Ag Medizinische verwendung von hemmern von glutaminyl und glutamatcyclasen
ATE462432T1 (de) 2003-05-05 2010-04-15 Probiodrug Ag Glutaminylcyclase-hemmer
US7560455B2 (en) 2003-05-14 2009-07-14 Merck & Co., Inc. 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
EP1631679A2 (en) * 2003-05-21 2006-03-08 Bayer HealthCare AG Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase 7 (dpp7)
AU2004247068A1 (en) * 2003-06-06 2004-12-23 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US6995183B2 (en) 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
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
US7579357B2 (en) 2003-08-13 2009-08-25 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005026148A1 (en) 2003-09-08 2005-03-24 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
CA2551037A1 (en) 2003-09-22 2005-03-31 Banyu Pharmaceutical Co., Ltd. Novel piperidine derivative
WO2005033099A2 (en) * 2003-10-03 2005-04-14 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
NZ546322A (en) 2003-10-15 2008-11-28 Probiodrug Ag Use of effectors of glutaminyl and glutamate cyclases
ZA200603165B (en) 2003-11-03 2007-07-25 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
JP2007510651A (ja) * 2003-11-04 2007-04-26 メルク エンド カムパニー インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−iv阻害剤としての縮合フェニルアラニン誘導体
RU2385723C2 (ru) * 2003-11-17 2010-04-10 Новартис Аг Применение ингибиторов дипептидилпептидазы iv
KR20170104639A (ko) * 2003-11-17 2017-09-15 노파르티스 아게 디펩티딜 펩티다제 ⅳ 억제제의 용도
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
RS52163B (sr) * 2004-02-05 2012-08-31 Kyorin Pharmaceutical Co. Ltd. Derivati bicikloestra
CN1922139B (zh) * 2004-02-18 2010-12-29 杏林制药株式会社 双环酰胺衍生物
CA2557275C (en) * 2004-02-27 2012-06-05 Kyorin Pharmaceutical Co., Ltd. Bicyclo derivative
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
MXPA06010571A (es) 2004-03-15 2007-02-16 Takeda Pharmaceutical Inhibidores de dipeptidil peptidasa.
CA2560314A1 (en) 2004-03-29 2005-10-20 Merck & Co., Inc. Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
EP2305352A1 (en) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders
US7687638B2 (en) 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7842707B2 (en) * 2004-07-23 2010-11-30 Nuada, Llc Peptidase inhibitors
CA2575736A1 (en) 2004-08-06 2006-02-16 Merck & Co., Inc. Sulfonyl compounds as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
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
BRPI0608469A2 (pt) 2005-04-22 2010-01-05 Alantos Pharmaceuticals Holding Inc inibidores de dipeptidil peptidase-iv
EP1892241B1 (en) 2005-05-30 2016-03-30 Msd K.K. Novel piperidine derivative
MY152185A (en) 2005-06-10 2014-08-29 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
US7321055B2 (en) * 2005-08-04 2008-01-22 Ajinomoto Co., Inc. Production method of optically active dephenylalanine compounds
JPWO2007018248A1 (ja) 2005-08-10 2009-02-19 萬有製薬株式会社 ピリドン化合物
US7875633B2 (en) 2005-08-24 2011-01-25 Banyu Pharmaceutical Co., Ltd. Phenylpyridone derivative
JPWO2007029847A1 (ja) 2005-09-07 2009-03-19 萬有製薬株式会社 二環性芳香族置換ピリドン誘導体
PL1942898T5 (pl) 2005-09-14 2014-10-31 Takeda Pharmaceuticals Co Inhibitory peptydazy dipeptydylowej do leczenia cukrzycy
WO2007035629A2 (en) 2005-09-16 2007-03-29 Takeda Pharmaceutical Company Limited Process for the preparation of pyrimidinedione derivatives
WO2007041052A2 (en) 2005-09-29 2007-04-12 Merck & Co., Inc. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
JPWO2007049798A1 (ja) 2005-10-27 2009-04-30 萬有製薬株式会社 新規ベンゾオキサチイン誘導体
WO2007055418A1 (ja) 2005-11-10 2007-05-18 Banyu Pharmaceutical Co., Ltd. アザ置換スピロ誘導体
EP1801098A1 (en) 2005-12-16 2007-06-27 Merck Sante 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors
GB0526291D0 (en) 2005-12-23 2006-02-01 Prosidion Ltd Therapeutic method
CA2645154C (en) * 2006-03-08 2011-11-29 Kyorin Pharmaceutical Co., Ltd. Method for producing aminoacetylpyrrolidinecarbonitrile derivative and production intermediate thereof
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
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
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
EP2083831B1 (en) 2006-09-22 2013-12-25 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
WO2008038692A1 (en) 2006-09-28 2008-04-03 Banyu Pharmaceutical Co., Ltd. Diaryl ketimine derivative
JP2008115178A (ja) * 2006-11-03 2008-05-22 Ajinomoto Co Inc ジフェニルアラニン−Ni(II)錯体の製造方法
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
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
SI2091948T1 (sl) 2006-11-30 2012-07-31 Probiodrug Ag Novi inhibitorji glutaminil ciklaze
EP1935420A1 (en) 2006-12-21 2008-06-25 Merck Sante 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
JPWO2008114857A1 (ja) * 2007-03-22 2010-07-08 杏林製薬株式会社 アミノアセチルピロリジンカルボニトリル誘導体の製造方法
JP5319518B2 (ja) 2007-04-02 2013-10-16 Msd株式会社 インドールジオン誘導体
JP5616630B2 (ja) 2007-04-03 2014-10-29 田辺三菱製薬株式会社 ジペプチジルペプチダーゼ4阻害化合物と甘味料との併用
EP2142514B1 (en) 2007-04-18 2014-12-24 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
WO2008137105A1 (en) 2007-05-07 2008-11-13 Merck & Co., Inc. Method of treatment using fused aromatic compounds having anti-diabetic activity
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
DK2170930T3 (da) 2007-06-04 2012-11-05 Synergy Pharmaceuticals Inc Agonister af guanylatcyclase, anvendelige til behandlingen af gastrointestinale sygdomme, inflammation, cancer og andre sygdomme
CL2008003653A1 (es) 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica.
AU2009220605A1 (en) 2008-03-06 2009-09-11 Msd K.K. Alkylaminopyridine derivative
EP2272841A1 (en) 2008-03-28 2011-01-12 Banyu Pharmaceutical Co., Ltd. Diarylmethylamide derivative having antagonistic activity on melanin-concentrating hormone receptor
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
EP2328910B1 (en) 2008-06-04 2014-08-06 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
WO2009154132A1 (ja) 2008-06-19 2009-12-23 萬有製薬株式会社 スピロジアミン-ジアリールケトオキシム誘導体
ES2624828T3 (es) 2008-07-16 2017-07-17 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros
JPWO2010013595A1 (ja) 2008-07-30 2012-01-12 Msd株式会社 5員−5員又は5員−6員縮環シクロアルキルアミン誘導体
EP2322499A4 (en) * 2008-08-07 2011-12-21 Kyorin Seiyaku Kk PROCESS FOR PREPARING A BICYCLO [2,2,2] OCTYLAMINE DERIVATIVE
JPWO2010018866A1 (ja) * 2008-08-14 2012-01-26 杏林製薬株式会社 安定化された医薬組成物
US8410284B2 (en) 2008-10-22 2013-04-02 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
CN102272103B (zh) 2008-10-30 2015-10-21 默沙东公司 异烟酰胺食欲素受体拮抗剂
EP2362731B1 (en) 2008-10-31 2016-04-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2010056717A1 (en) 2008-11-17 2010-05-20 Merck Sharp & Dohme Corp. Substituted bicyclic amines for the treatment of diabetes
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011011508A1 (en) 2009-07-23 2011-01-27 Schering Corporation Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
CN102695546B (zh) 2009-09-11 2014-09-10 前体生物药物股份公司 作为谷氨酰胺酰环化酶抑制剂的杂环衍生物
JP2013510834A (ja) 2009-11-16 2013-03-28 メリテク [1,5]‐ジアゾシン誘導体
EP2521721B1 (en) 2009-12-30 2014-10-01 Shanghai Fochon Pharmaceutical Co. Ltd 3-(3-aminopiperidin-1-yl)-5-oxo-1,2,4-triazine derivates as dipeptidyl peptidase iv(dpp-iv) inhibitors
JP2013520502A (ja) 2010-02-25 2013-06-06 メルク・シャープ・エンド・ドーム・コーポレイション 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
SG183229A1 (en) 2010-03-10 2012-09-27 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
JP2013523819A (ja) 2010-04-06 2013-06-17 アリーナ ファーマシューティカルズ, インコーポレイテッド Gpr119レセプターのモジュレーターおよびそれに関連する障害の処置
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
WO2011146300A1 (en) * 2010-05-17 2011-11-24 Merck Sharp & Dohme Corp. Novel prolylcarboxypeptidase inhibitors
US20130156720A1 (en) 2010-08-27 2013-06-20 Ironwood Pharmaceuticals, Inc. Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
SG188548A1 (en) 2010-09-22 2013-04-30 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
SG192941A1 (en) 2011-02-25 2013-09-30 Merck Sharp & Dohme Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
JP6251038B2 (ja) 2011-03-01 2017-12-20 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼcアゴニストの調製方法
WO2012123563A1 (en) 2011-03-16 2012-09-20 Probiodrug Ag Benz imidazole 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
WO2012145604A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145603A1 (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
WO2013006738A1 (en) 2011-07-06 2013-01-10 Gilead Sciences, Inc. Compounds for the treatment of hiv
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
WO2014022528A1 (en) 2012-08-02 2014-02-06 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
JP2016516004A (ja) 2013-02-22 2016-06-02 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. 抗糖尿病二環式化合物
EP2970119B1 (en) 2013-03-14 2021-11-03 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
US9486494B2 (en) 2013-03-15 2016-11-08 Synergy Pharmaceuticals, Inc. Compositions useful for the treatment of gastrointestinal disorders
CA2905438A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
JP6606491B2 (ja) 2013-06-05 2019-11-13 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼcの超高純度アゴニスト、その作成および使用方法
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
BR112017003745A2 (pt) 2014-08-29 2017-12-05 Tes Pharma S R L inibidores de semialdeído descarboxilase de ácido alfa-amino-beta-carboximucônico
GB201415598D0 (en) 2014-09-03 2014-10-15 Univ Birmingham Elavated Itercranial Pressure Treatment
WO2016144862A1 (en) 2015-03-09 2016-09-15 Intekrin Therapeutics, Inc. Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
KR102180740B1 (ko) 2016-08-19 2020-11-20 길리애드 사이언시즈, 인코포레이티드 Hiv 바이러스 감염의 예방적 또는 치유적 치료에 유용한 치료 화합물
JP2020500838A (ja) 2016-10-14 2020-01-16 ティエエッセ ファルマ ソチエタ レスポンサビリタ リミタータ Α−アミノ−β−カルボキシムコン酸セミアルデヒドデカルボキシラーゼの阻害剤
WO2018106518A1 (en) 2016-12-06 2018-06-14 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
WO2018118670A1 (en) 2016-12-20 2018-06-28 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
KR20200036808A (ko) 2017-04-03 2020-04-07 코히러스 바이오사이언시스, 인크. 진행성 핵상 마비 치료를 위한 PPARγ 작용제
AR112412A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas de sal de colina de un inhibidor de la cápside del vih
TWI687415B (zh) 2017-08-17 2020-03-11 美商基利科學股份有限公司 Hiv蛋白質膜抑制劑之固體形式
DK3461819T3 (da) 2017-09-29 2020-08-10 Probiodrug Ag Inhibitorer af glutaminylcyklase
PL3752495T3 (pl) 2018-02-15 2024-01-15 Gilead Sciences, Inc. Pochodne pirydynowe i ich zastosowanie do leczenia infekcji hiv
CA3175384A1 (en) 2018-02-16 2019-08-22 Gilead Sciences, Inc. Methods and intermediates for preparing therapeutic compounds useful in the treatment of retroviridae viral infection
CN120053445A (zh) 2018-07-16 2025-05-30 吉利德科学公司 用于治疗hiv的衣壳抑制剂
KR20210111248A (ko) 2018-11-20 2021-09-10 테스 파마 에스.알.엘. α-아미노-β-카르복시뮤콘산 세미알데하이드 데카르복실라제의 저해제
US12331018B2 (en) 2019-02-13 2025-06-17 Merck Sharp & Dohme Llc Pyrrolidine orexin receptor agonists
WO2020167706A1 (en) 2019-02-13 2020-08-20 Merck Sharp & Dohme Corp. 5-alkyl pyrrolidine orexin receptor agonists
WO2021026047A1 (en) 2019-08-08 2021-02-11 Merck Sharp & Dohme Corp. Heteroaryl pyrrolidine and piperidine orexin receptor agonists
EP4643882A2 (en) 2019-11-26 2025-11-05 Gilead Sciences, Inc. Capsid inhibitors for the prevention of hiv
WO2021262990A1 (en) 2020-06-25 2021-12-30 Gilead Sciences, Inc. Capsid inhibitors for the treatment of hiv
CR20230089A (es) 2020-08-18 2023-04-11 Merck Sharp & Dohme Llc Agonistas de bicicloheptano pirrolidina de los receptores de orexina
EP4440702B1 (en) 2021-12-03 2025-05-21 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
JP7736929B2 (ja) 2021-12-03 2025-09-09 ギリアード サイエンシーズ, インコーポレイテッド Hivウイルス感染症のための治療化合物
US12084467B2 (en) 2021-12-03 2024-09-10 Gilead Sciences, Inc. Therapeutic compounds for HIV virus infection

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL111785A0 (en) * 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
US6090786A (en) 1994-06-10 2000-07-18 Fondatech Benelux N.V. Serine proteases, their activity and their synthetic inhibitors
KR100318804B1 (ko) * 1996-08-28 2002-01-04 시오노 요시히코 티아졸릴-알라닌 잔기를 갖는 신규한 펩티드 유도체
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
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
AU766219B2 (en) 1998-02-02 2003-10-09 1149336 Ontario Inc. Method of regulating glucose metabolism, and reagents related thereto
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
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
GB9906714D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for improving fertility
GB9906715D0 (en) * 1999-03-23 1999-05-19 Ferring Bv Compositions for promoting growth
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
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
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
AU2001233622A1 (en) 2000-02-25 2001-09-03 Novo-Nordisk A/S Inhibition of beta cell degeneration
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
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
DE10025464A1 (de) * 2000-05-23 2001-12-06 Inst Medizintechnologie Magdeb Kombinierte Verwendung von Enzyminhibitoren zur Therapie von Autoimmunerkrankungen, bei Transplantationen und Tumorerkrankungen sowie Kombinationen von Enzyminhibitoren umfassende pharmazeutische Zubereitungen
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
WO2002002560A2 (en) 2000-07-04 2002-01-10 Novo Nordisk A/S Purine-2,6-diones which are inhibitors of the enzyme dipeptidyl peptidase iv (dpp-iv)
NZ524974A (en) 2000-10-06 2005-10-28 Tanabe Seiyaku Co Aliphatic nitrogen-containing 5-membered ring compound
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
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
JP2002265439A (ja) * 2001-03-08 2002-09-18 Mitsubishi Pharma Corp シアノピロリジン誘導体およびその医薬用途
DE60226723D1 (de) 2001-03-27 2008-07-03 Merck & Co Inc Dipeptidylpeptidase-hemmer für die behandlung oder prävention von 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
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
WO2003000180A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
GB0125446D0 (en) 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
ATE349435T1 (de) * 2002-02-28 2007-01-15 Prosidion Ltd Dpiv-inhibitoren auf glutaminbasis
AU2003297564A1 (en) * 2002-12-04 2004-06-23 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

Also Published As

Publication number Publication date
US20040167341A1 (en) 2004-08-26
ES2296962T3 (es) 2008-05-01
JP2005518337A (ja) 2005-06-23
WO2003002530A3 (en) 2003-04-03
DE60223920T2 (de) 2008-11-13
ATE380175T1 (de) 2007-12-15
EP1399420B1 (en) 2007-12-05
WO2003002530A2 (en) 2003-01-09
US7196201B2 (en) 2007-03-27
EP1399420A2 (en) 2004-03-24
AU2002316437A1 (en) 2003-03-03
DE60223920D1 (en) 2008-01-17

Similar Documents

Publication Publication Date Title
JP4300108B2 (ja) ジペプチジルペプチダーゼ阻害剤としてのピロリジン類
JP4357293B2 (ja) ジペプチジルペプチダーゼ阻害剤としてのフルオロピロリジン類
US7132443B2 (en) Fluoropyrrolidines as dipeptidyl peptidase inhibitors
AU2002322344A1 (en) Fluoropyrrolidines as dipeptidyl peptidase inhibitors
KR100848491B1 (ko) 베타아미노기를 갖는 2-싸이아졸리딘 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법
ES2291966T3 (es) Inhibidores de dpp-iv.
KR20080094806A (ko) 치환된 이미다졸 유도체 및 이의 PTPase 억제제로서의 용도
CA2564264A1 (en) 1,2,4-oxadiazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
KR20080071476A (ko) 신규한 디펩티딜 펩티데이즈 iv(dpp-iv) 저해제
US20060264433A1 (en) Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
CA2560669C (en) Pyrrolidine-3,4-dicarboxamide derivatives
US20050192324A1 (en) Novel dipeptidyl peptidase IV inhibitors; processes for their preparation and compositions thereof
HK1111419A (en) Fluoropyrrolidines as dipeptidyl peptidase inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20050329

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20050329

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20081209

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20090306

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20090407

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20090420

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120424

Year of fee payment: 3

LAPS Cancellation because of no payment of annual fees