JP5122446B2 - 大環状グレリン受容体アンタゴニストおよびインバースアゴニストならびにその使用方法 - Google Patents

大環状グレリン受容体アンタゴニストおよびインバースアゴニストならびにその使用方法

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Publication number
JP5122446B2
JP5122446B2 JP2008515697A JP2008515697A JP5122446B2 JP 5122446 B2 JP5122446 B2 JP 5122446B2 JP 2008515697 A JP2008515697 A JP 2008515697A JP 2008515697 A JP2008515697 A JP 2008515697A JP 5122446 B2 JP5122446 B2 JP 5122446B2
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Japan
Prior art keywords
compound
ghrelin
compounds
group
receptor
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JP2008515697A
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English (en)
Japanese (ja)
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JP2009508805A (ja
Inventor
フレイザー，グレアム
ホヴェイダ，ハミド
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トランザイム・ファーマ，インコーポレイテッド
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Priority claimed from PCT/US2005/020887 external-priority patent/WO2006046977A1/en
Application filed by トランザイム・ファーマ，インコーポレイテッド filed Critical トランザイム・ファーマ，インコーポレイテッド
Publication of JP2009508805A publication Critical patent/JP2009508805A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A61P5/08—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nutrition Science (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2008515697A 2005-06-13 2006-04-26 大環状グレリン受容体アンタゴニストおよびインバースアゴニストならびにその使用方法 Expired - Fee Related JP5122446B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
USPCT/US2005/020887 2005-06-13
PCT/US2005/020887 WO2006046977A1 (en) 2004-10-26 2005-06-13 Macrocyclic ghrelin receptor antagonists and methods of using the same
PCT/US2006/015698 WO2006137974A2 (en) 2005-06-13 2006-04-26 Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same

Publications (2)

Publication Number Publication Date
JP2009508805A JP2009508805A (ja) 2009-03-05
JP5122446B2 true JP5122446B2 (ja) 2013-01-16

Family

ID=37570927

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2008515697A Expired - Fee Related JP5122446B2 (ja) 2005-06-13 2006-04-26 大環状グレリン受容体アンタゴニストおよびインバースアゴニストならびにその使用方法

Country Status (4)

Country Link
EP (1) EP1891090A2 (de)
JP (1) JP5122446B2 (de)
CA (1) CA2583345A1 (de)
WO (1) WO2006137974A2 (de)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2054429B1 (de) 2006-09-11 2013-11-06 Tranzyme Pharma, Inc. Makrozyklische motilinrezeptor antagonisten zur behandlung von gastro-intestinaler störungen
US8889632B2 (en) 2007-01-31 2014-11-18 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
AU2008241532A1 (en) 2007-02-09 2008-10-30 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor modulators and methods of using the same
KR101623985B1 (ko) 2007-03-28 2016-05-25 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 스티칭된 폴리펩티드
CN102812037A (zh) * 2009-10-30 2012-12-05 特兰齐姆制药公司 大环生长素释放肽受体拮抗剂和反向激动剂及其使用方法
JP2013535514A (ja) 2010-08-13 2013-09-12 エイルロン セラピューティクス，インコーポレイテッド ペプチド模倣大環状分子
JP6342808B2 (ja) 2011-10-18 2018-06-13 エイルロン セラピューティクス，インコーポレイテッド ペプチドミメティック大環状化合物
AU2013221433B2 (en) 2012-02-15 2018-01-18 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
BR112014020103A2 (pt) 2012-02-15 2018-10-09 Aileron Therapeutics, Inc. macrociclos peptidomiméticos
BR112015009470A2 (pt) 2012-11-01 2019-12-17 Aileron Therapeutics Inc aminoácidos dissubstituídos e seus métodos de preparação e uso
CN107106642B (zh) 2014-09-24 2021-02-26 艾瑞朗医疗公司 拟肽大环化合物及其制剂
SG11201702223UA (en) 2014-09-24 2017-04-27 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof
CA2979847A1 (en) 2015-03-20 2016-09-29 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10023613B2 (en) 2015-09-10 2018-07-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles as modulators of MCL-1

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2284459C (en) * 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
EP2210612B1 (de) * 2003-06-18 2016-10-05 Ocera Therapeutics, Inc. Makrozyklische Motilin Rezeptorantagonisten
US7491695B2 (en) * 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
US7476653B2 (en) * 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
CA2533818C (en) * 2003-07-31 2015-03-17 Tranzyme Pharma, Inc. Spatially-defined macrocyclic compounds useful for drug discovery
US7550431B2 (en) * 2003-07-31 2009-06-23 Tranzyme Pharma Inc. Spatially-defined macrocycles incorporating peptide bond surrogates
WO2006046977A1 (en) * 2004-10-26 2006-05-04 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor antagonists and methods of using the same

Also Published As

Publication number Publication date
WO2006137974A3 (en) 2007-04-12
WO2006137974A2 (en) 2006-12-28
EP1891090A2 (de) 2008-02-27
CA2583345A1 (en) 2006-12-28
JP2009508805A (ja) 2009-03-05

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