WO2014049610A3 - Peptides as gip, glp-1 and glucagon receptors triple-agonist - Google Patents

Peptides as gip, glp-1 and glucagon receptors triple-agonist Download PDF

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Publication number
WO2014049610A3
WO2014049610A3 PCT/IN2013/000577 IN2013000577W WO2014049610A3 WO 2014049610 A3 WO2014049610 A3 WO 2014049610A3 IN 2013000577 W IN2013000577 W IN 2013000577W WO 2014049610 A3 WO2014049610 A3 WO 2014049610A3
Authority
WO
WIPO (PCT)
Prior art keywords
peptides
gip
glp
triple
agonist
Prior art date
Application number
PCT/IN2013/000577
Other languages
French (fr)
Other versions
WO2014049610A2 (en
Inventor
Rajesh Bahekar
Ranjit C. Desai
Original Assignee
Cadila Healthcare Limited
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 Cadila Healthcare Limited filed Critical Cadila Healthcare Limited
Publication of WO2014049610A2 publication Critical patent/WO2014049610A2/en
Publication of WO2014049610A3 publication Critical patent/WO2014049610A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/605—Glucagons
    • 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

Abstract

The present invention provides novel peptides, having the structural formula (I) showed GIP, GLP-1 & Glucagon-receptors triple-agonistic activity. These peptides exhibit increased stability to proteolytic cleavage, especially against DPP-IV (Dipeptidyl peptidase-IV) enzyme. These peptides can be delivered by parenteral routes of administration, for the treatment or prevention of diabetes, obesity and related metabolic disorders. The present invention thus discloses novel peptides as GIP, GLP-1 & Glucagon-receptors triple-agonist having the following structure (I) A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z12-Z13-Z14-Z15-Z16-Z17-Z18-Z19-Z20-Z21-Z22-Z23- Z24-Z25-Z26-Z27-Z28-Z29-B
PCT/IN2013/000577 2012-09-26 2013-09-26 Peptides as gip, glp-1 and glucagon receptors triple-agonist WO2014049610A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN2807/MUM/2012 2012-09-26
IN2807MU2012 2012-09-26

Publications (2)

Publication Number Publication Date
WO2014049610A2 WO2014049610A2 (en) 2014-04-03
WO2014049610A3 true WO2014049610A3 (en) 2014-10-02

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Application Number Title Priority Date Filing Date
PCT/IN2013/000577 WO2014049610A2 (en) 2012-09-26 2013-09-26 Peptides as gip, glp-1 and glucagon receptors triple-agonist

Country Status (2)

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AR (1) AR092873A1 (en)
WO (1) WO2014049610A2 (en)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA126465C2 (en) 2011-06-10 2022-10-12 Ханмі Сайенс Ко., Лтд. A peptide having oxyntomodulin activity and a pharmaceutical composition for the treatment of obesity containing it
EP3502129B1 (en) 2011-06-17 2021-04-07 Hanmi Science Co., Ltd. A conjugate comprising oxyntomodulin and an immunoglobulin fragment, and use thereof
KR101968344B1 (en) 2012-07-25 2019-04-12 한미약품 주식회사 A composition for treating hyperlipidemia comprising oxyntomodulin analog
UA116217C2 (en) 2012-10-09 2018-02-26 Санофі Exendin-4 derivatives as dual glp1/glucagon agonists
KR102311517B1 (en) 2012-11-06 2021-10-14 한미약품 주식회사 Liquid formulation of protein conjugate comprising the oxyntomodulin and an immunoglobulin fragment
KR101993393B1 (en) 2012-11-06 2019-10-01 한미약품 주식회사 A composition for treating diabetes or diabesity comprising oxyntomodulin analog
LT2934568T (en) 2012-12-21 2018-02-12 Sanofi Dual glp1/gip or trigonal glp1/gip/glucagon agonists
US20160318987A1 (en) * 2013-12-13 2016-11-03 Medimmune Limited Protease resistant peptides
MA39301A1 (en) 2014-01-20 2018-01-31 Hanmi Pharmaceutical Co Ltd Long-acting insulin and associated use
AR100639A1 (en) 2014-05-29 2016-10-19 Hanmi Pharm Ind Co Ltd COMPOSITION TO TREAT DIABETES THAT INCLUDES CONJUGATES OF PROLONGED INSULIN ANALOGS AND CONJUGATES OF PROLONGED INSULINOTROPIC PEPTIDES
TWI684458B (en) 2014-05-30 2020-02-11 南韓商韓美藥品股份有限公司 Composition for treating diabetes mellitus comprising insulin and a glp-1/glucagon dual agonist
TWI772252B (en) 2014-09-16 2022-08-01 南韓商韓美藥品股份有限公司 Use of a long acting glp-1/glucagon receptor dual agonist for the treatment of non-alcoholic fatty liver disease
WO2016077220A1 (en) * 2014-11-10 2016-05-19 Mb2 Llc Gip/glp-1 co-agonist peptides for human administration
EP3241841A4 (en) 2014-12-30 2018-10-17 Hanmi Pharm. Co., Ltd. Glucagon derivative having improved stability
KR102418477B1 (en) * 2014-12-30 2022-07-08 한미약품 주식회사 Gluagon Derivatives
AR105319A1 (en) 2015-06-05 2017-09-27 Sanofi Sa PROPHARMS THAT INCLUDE A DUAL AGONIST GLU-1 / GLUCAGON CONJUGATE HIALURONIC ACID CONNECTOR
TWI726889B (en) * 2015-06-10 2021-05-11 英商梅迪繆思有限公司 Protease-resistant lipidated peptides
TN2017000555A1 (en) 2015-06-30 2019-04-12 Hanmi Pharm Ind Co Ltd Glucagon derivative and a composition comprising a long acting conjugate of the same
UY36870A (en) 2015-08-28 2017-03-31 Hanmi Pharm Ind Co Ltd NEW INSULIN ANALOGS
CN108699125B (en) 2015-12-31 2022-10-28 韩美药品株式会社 glucagon/GLP-1/GIP receptor triple agonists
AU2017273857B2 (en) 2016-06-01 2021-08-19 Athira Pharma, Inc. Compounds
IL263934B2 (en) 2016-06-29 2023-10-01 Hanmi Pharm Ind Co Ltd Glucagon derivative, conjugate thereof, composition comprising same and therapeutic use thereof
EP3517544A4 (en) 2016-09-23 2020-06-03 Hanmi Pharm. Co., Ltd. Insulin analog having reduced binding force to insulin receptor, and use thereof
TW201833132A (en) 2016-12-02 2018-09-16 法商賽諾菲公司 New compounds as peptidic trigonal glp1/glucagon/gip receptor agonists
AR110301A1 (en) 2016-12-02 2019-03-13 Sanofi Sa COMPOUNDS AS GLP1 / GLUCAGÓN / GIP RECEPTING AGENISTS
CN110536899B (en) 2017-03-23 2023-12-12 韩美药品株式会社 Insulin analogue complex with reduced affinity for insulin receptor and uses thereof
TWI810937B (en) 2017-12-21 2023-08-01 美商美國禮來大藥廠 Incretin analogs and uses thereof
TWI744579B (en) 2017-12-21 2021-11-01 美商美國禮來大藥廠 Incretin analogs and uses thereof
SG11202010016QA (en) 2018-04-10 2020-11-27 Sanofi Aventis Deutschland Lixisenatide synthesis with capping
JP7434169B2 (en) 2018-04-10 2024-02-20 サノフィ－アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング Method for cleaving solid phase-bound peptides from solid phase
TW202015735A (en) 2018-05-30 2020-05-01 法商賽諾菲公司 Conjugates comprising an glp-1/glucagon/gip triple receptor agonist, a linker and hyaluronic acid
MA53382A (en) * 2018-07-23 2021-06-02 Lilly Co Eli GIP / GLP1 CO-AGONIST COMPOUNDS
MX2022002115A (en) 2019-08-19 2022-03-17 Lilly Co Eli Methods of making incretin analogs.
TWI795698B (en) 2019-12-18 2023-03-11 美商美國禮來大藥廠 Incretin analogs and uses thereof
EP4269425A1 (en) * 2020-12-24 2023-11-01 Hanmi Pharm. Co., Ltd. Novel triple activator that activates all of glucagon, glp-1 and gip receptors, and use thereof
WO2023228156A1 (en) * 2022-05-27 2023-11-30 D&D Pharmatech Inc. Peptide compositions and methods of use threof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009125424A2 (en) * 2007-12-11 2009-10-15 Cadila Healthcare Limited Peptidomimetics with glucagon antagonistic and glp-1 agonistic activities
WO2009155258A2 (en) * 2008-06-17 2009-12-23 Indiana University Research And Technology Corporation Glucagon/glp-1 receptor co-agonists
WO2010148089A1 (en) * 2009-06-16 2010-12-23 Indiana University Research And Technology Corporation Gip receptor-active glucagon compounds
WO2011048614A2 (en) * 2009-10-22 2011-04-28 Cadila Healthcare Limited Short chain peptidomimetics based orally active glp-1 agonist and glucagon receptor antagonist
WO2011088837A1 (en) * 2010-01-20 2011-07-28 Zealand Pharma A/S Treatment of cardiac conditions

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2204645A1 (en) 1994-11-07 1996-05-17 Keiichi Yano Novel oxyntomodulin
GB0121709D0 (en) 2001-09-07 2001-10-31 Imp College Innovations Ltd Food inhibition agent
JP4733922B2 (en) 2002-01-10 2011-07-27 インペリアル・イノベ−ションズ・リミテッド Correction of eating behavior
GB0300571D0 (en) 2003-01-10 2003-02-12 Imp College Innovations Ltd Modification of feeding behaviour
GB0511986D0 (en) 2005-06-13 2005-07-20 Imp College Innovations Ltd Novel compounds and their effects on feeding behaviour
ATE553124T1 (en) 2005-06-13 2012-04-15 Imp Innovations Ltd OXYNTOMODULIN ANALOGS AND THEIR EFFECTS ON EATING BEHAVIOR
US7928058B2 (en) 2006-02-22 2011-04-19 Merck Sharp & Dohme Corp. Pharmaceutical composition comprising oxyntomodulin derivatives and a method for reducing body weight using the composition
TWI428346B (en) 2006-12-13 2014-03-01 Imp Innovations Ltd Novel compounds and their effects on feeding behaviour
EP2124974B1 (en) 2007-01-05 2017-03-15 Indiana University Research and Technology Corporation Glucagon analogs exhibiting enhanced solubility in physiological ph buffers
AU2008216265B2 (en) 2007-02-15 2014-04-03 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
JP5385266B2 (en) 2007-06-15 2014-01-08 ジーランド ファーマ アクティーゼルスカブ Glucagon analog
ES2558155T3 (en) 2007-10-30 2016-02-02 Indiana University Research And Technology Corporation Compounds showing glucacon antagonist activity and GLP-1 agonist
EA020326B9 (en) 2008-06-17 2015-03-31 Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн Gip-based mixed agonists for treatment of metabolic disorders and obesity
DK2370462T3 (en) 2008-12-15 2014-09-08 Zealand Pharma As Glucagon-ANALOGS
DK2370461T3 (en) 2008-12-15 2013-12-16 Zealand Pharma As glucagon
EA020520B1 (en) 2008-12-15 2014-11-28 Зилэнд Фарма А/С Glucagon analogues
CN102282167B (en) 2008-12-15 2014-08-13 西兰制药公司 Glucagon analogues
WO2010096052A1 (en) 2009-02-19 2010-08-26 Merck Sharp & Dohme Corp. Oxyntomodulin analogs
SG177609A1 (en) 2009-07-13 2012-02-28 Zealand Pharma As Acylated glucagon analogues
US8703701B2 (en) 2009-12-18 2014-04-22 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
AR079345A1 (en) 2009-12-22 2012-01-18 Lilly Co Eli OXINTOMODULINE PEPTIDAL ANALOG
AR079344A1 (en) 2009-12-22 2012-01-18 Lilly Co Eli PEPTIDAL ANALOG OF OXINTOMODULIN, PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS AND USES TO PREPARE A USEFUL MEDICINAL PRODUCT TO TREAT NON-INSULINED INDEPENDENT DIABETES AND / OR OBESITY
JP6007417B2 (en) 2011-05-31 2016-10-12 レセプトス エルエルシー Novel GLP-1 receptor stabilizer and modulator
UA126465C2 (en) 2011-06-10 2022-10-12 Ханмі Сайенс Ко., Лтд. A peptide having oxyntomodulin activity and a pharmaceutical composition for the treatment of obesity containing it
EP3502129B1 (en) 2011-06-17 2021-04-07 Hanmi Science Co., Ltd. A conjugate comprising oxyntomodulin and an immunoglobulin fragment, and use thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009125424A2 (en) * 2007-12-11 2009-10-15 Cadila Healthcare Limited Peptidomimetics with glucagon antagonistic and glp-1 agonistic activities
WO2009155258A2 (en) * 2008-06-17 2009-12-23 Indiana University Research And Technology Corporation Glucagon/glp-1 receptor co-agonists
WO2010148089A1 (en) * 2009-06-16 2010-12-23 Indiana University Research And Technology Corporation Gip receptor-active glucagon compounds
WO2011048614A2 (en) * 2009-10-22 2011-04-28 Cadila Healthcare Limited Short chain peptidomimetics based orally active glp-1 agonist and glucagon receptor antagonist
WO2011088837A1 (en) * 2010-01-20 2011-07-28 Zealand Pharma A/S Treatment of cardiac conditions

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DAN DONNELLY: "The structure and function of the glucagon-like peptide-1 receptor and its ligands", BRITISH JOURNAL OF PHARMACOLOGY, vol. 166, no. 1, 1 May 2012 (2012-05-01), pages 27 - 41, XP055060540, ISSN: 0007-1188, DOI: 10.1111/j.1476-5381.2011.01687.x *
RUNGE S ET AL: "Different domains of the glucagon and glucagon-like peptide-1 receptors provide the critical determinants of ligand selectivity", BRITISH JOURNAL OF PHARMACOLOGY, NATURE PUBLISHING GROUP, BASINGSTOKE, HANTS; GB, vol. 138, no. 5, 1 March 2003 (2003-03-01), pages 787 - 794, XP002427759, ISSN: 0007-1188, DOI: 10.1038/SJ.BJP.0705120 *

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Publication number Publication date
WO2014049610A2 (en) 2014-04-03
AR092873A1 (en) 2015-05-06

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