|Technical composition and developments of patents regarding Liraglutide
|HUANG Jia1, WANG Jun2
|  杨文英.人GLP-1类似物利拉鲁肽的最新研究进展[J].中华内分泌代谢杂志, 2010, 26(9): 840-843.Yang Wenying.Review on the human GLP-1 analogues[J].Chinese Journal of Endocrinology and Metabolism, 2010, 26(9): 840-843.
 杨铁军.产业专利分析报告-糖尿病药物.北京: 知识产权出版社, 2016.Yang Tiejun.Industrial analysis report on Diabetes medicine.Beijing: Intellectual Property Publishing House, 2016.
 Novo Nordisk.Acylating amino group of peptide or protein, for reduc-ing in vivo clearance rate, by reacting with alkanoyl carboxylate ester acylating agent and saponifying acylated peptide ester: WO, 0055119A1[P].2000-09-21.
 Novo Nordisk.Ion exchange chromatographic separation process for sep-arating glucagon like peptide-1, its analog or derivative from a mixture containing the peptide and other related impurities, comprises use of a organic modifier for elution: WO, 0055203A1[P].2000-09-21.
 Novo Nordisk..Preparation of N-acylated peptides involves reacting a peptide having free amino groups with a reactive ester or N-hydroxy im-ide ester of an aminoacid derivative under basic conditions in an aque-ous mixture: WO, 2004029077A2[P].2004-04-08.
 Novo Nordisk..New glucagon-like peptide-1(GLP-1) derivative com-prising modified GLP-1(7-37) sequence having derivatized with an al-bumin binding residue, is albumin binder, useful e.g.for treating or pre-venting hyperglycemia and type 2 diabetes: WO, 2009030738A1[P].2009-03-12.
 Novo Nordisk.Use of a glucagon-like peptide-1 receptor agonist for treating type 1 diabetes and reducing e.g.the number of hypoglycemias or hypoglycemic episodes and the amount of exogenous glucose needed for recovering from the episodes: WO, 2014202780A1[P].2014-12-24.
 Hybio Pharm Co.Ltd..Method for solid phase synthesizing liraglutide, involves coupling solid phase vector of resin with glycine, and perform-ing solid-phase synthesis process by coupling amino acid with N-termi-nal-fluorenylmethyloxycarbonyl protection: WO, 2013037266A1[P].2013-03-21.
 Hybio Pharm Co.Ltd..Synthesizing liraglutide, by synthesizing five polypeptide fragments of e.g.amino acid: CN, 102875665A[P].2013-01-16.
 Hybio Pharm Co.Ltd..Synthesizing liraglutide, involves bonding first polypeptide fragment, second polypeptide fragment, third polypeptide fragment, and fourth polypeptide fragment with resin, and subjecting obtained peptide resin to e.g.purification: CN, 104045705A[P].2014-09-17.
 Hybio Pharm Co.Ltd..Synthesizing liraglutide peptide involves com-bining dipeptide fragment and/or tripeptide fragment to obtain Gly-res-in: CN, 104045706A[P].2014-09-17.
 Hybio Pharm Co.Ltd..Preparing liraglutide peptide comprises e.g.pre-paring glycine-resin, carrying out primary successive coupling to ob-tain polypeptide segment-resin, carrying out side chain modification, secondary successive coupling, and cracking: CN, 103288951A[P].2013-09-11.
 Hybio Pharm Co.Ltd..Solid phase preparation of liraglutide, by cleav-ing second peptide fragment-second resin, coupling second polypep-tide fragment with first polypeptide fragment-first resin and purifying remaining coupled liraglutide amino acids: CN, 103304659A[P].2013-09-18.
 Hybio Pharm Co.Ltd..Purifying solid-phase synthesized liraglutide coarse peptide, comprises e.g.dissolving solid-phase synthesized pep-tide in acetonitrile water solution, and performing first high-perfor?mance liquid chromatography purification: WO, 2013117135A1[P].2013-08-15.
 Novo Nordisk.Pharmaceutical composition useful for treatment of e.g.hyperglycemia comprises insulinotropic peptide, meal-related insulin peptide and preservative: WO, 2005046716A1[P].2005-05-26.
 Novo Nordisk.Composition useful for treating hyperglycemia compris-es insulinotropic peptide, insulin peptide, and ligand for the HisB10 anion site which improves stability by blocking an interaction between the two peptides: WO, 2006029634[P].2006-03-23.
 Novo Nordisk.Soluble pharmaceutical composition for treating type 2 diabetes, comprises insulinotropic glucagon-like peptide-1 compound, basal insulin peptide, additives and zinc: WO, 2009063072A2[P].2009-05-22.
 Novo Nordisk.Particle used as pharmaceutical composition or medica-ment for treating metabolic diseases chosen from diabetes mellitus and obesity, comprises glucagon-like peptide-1 compound, divalent metal and polycationic compound: WO, 2012098188A1.2012-07-26.
 Novo Nordisk.New pulmonary liquid or dry formulation comprises a GLP-1 compound to which a lipophilic substituent is attached, option-ally via a spacer, useful in a pulmonary delivery device: WO, 0151071A2.2001-07-19.
 Novo Nordisk.Composition useful for treating diabetes such as type 2 diabetes, comprises glucagon-like peptide-1 compound, divalent met-al and polycationic compound: WO, 2012098187A1.2012-07-26.
 Novozymes Biopharma.Highly purified albumin composition, used to reduce formation of insulin fibrils in zinc ion free formulation and to reduce formation of peptide fibrils, comprises peptide, albumin, and optionally octanoate or polysorbate 80: WO, 2014096440A2[P].2014-06-26.
 Hoechst Marion Roussel, Sanofi-Aventis.Aqueous pharmaceutical for-mulation, useful for treating diabetes mellitus, comprises an insulin an-alog, zinc, a preservative and an isotonic agent: WO, 2011003823A1[P].2011-01-13.
 Sanofi-Aventis.Medicated module for drug delivery device to deliver human insulin through single dose setter to patient, has output needle portion whose distal end partially pierces fluid seal that is positioned at base of needle cover: WO, 2012059449A1[P].2012-05-10.
 Sanofi-Aventis.Medicated module for use with drug delivery device by healthcare professional to deliver e.g.medicament, to patient, has engagement needle and output needle which are primed with medica-ment when module is attached to drug delivery device: WO, 2012059455A1.2012-05-10.
 Sanofi-Aventis.Medicated module for use with pen injector that is uti-lized for delivering e.g.A21-Gly human insulin from separate reser-voirs to patient to treat diabetes mellitus, has shroud compressing res-ervoir to dispense medicament: WO, 2012059457A1.2012-05-10.
 Sanofi-Aventis.Medicated module for attaching drug delivery device of drug delivery system for use by healthcare professional to deliver e.g.drug agents to patient, has lockout feature preventing module from being reconnected to drug delivery device: WO, 2012059459A1[P].2012-05-10.
 Sanofi-Aventis.Medicated module for drug delivery system to deliver medicaments e.g.human insulin, to patient for treating diabetes, has needle in fluid communication with reservoir of drug delivery device after module is attached to delivery device: WO, 2012059453A1[P].2012-05-10.
 Agouron Pharma.New benzofuranyl derivatives useful for treating obe-sity and obesity-related disorders and Type 2 diabetes and diabetesrelated disorders e.g.diabetic neuropathy, diabetic retinopathy, diabet-ic cardiomyopathy, anorexia nervosa: WO, 2010103437A1[P].2010-09-16.
 Agouron Pharma.New L-(piperidin-4-yl)-pyrazole derivatives are Gprotein coupled receptor modulators useful to treat e.g.diabetes, coro-nary heart disease, ischemic stroke, peripheral vascular disease, inter-mittent claudication and myocardial infarction: WO, 2010140092A1[P].2010-12-09.
 Agouron Pharma.New pyrazole compounds useful for treating e.g.dia-betes, hyperlipidemia, coronary heart: WO, 2012069948A1[P].2012-05-31.
 Agouron Pharma.New substituted pyrazolospiroketone compounds used for treating e.g.obesity, diabetes-related disorders, nonalcoholic fatty liver disease, hyperglycemia and metabolic syndrome; and in drug and substrate tissue distribution assay: WO, 2012056372A1[P].2012-05-03.
 Agouron Pharma.New substituted 2,3-dihydro-1H-inden-1-yl-2,7-diazaspiro(3.5)nonane derivatives are ghrelin receptor modulators, use-ful to e.g.treat obesity, type Ⅱ diabetes and their related disorders (e.g.impaired glucose tolerance) in animals: WO, 2011114271A1[P].2011-09-22.
 Pfizer Inc.New pyrazolospiroketone compounds useful for treating dis-ease treated by inhibiting acetyl-coenzyme A carboxylase e.g.obesity, diabetes, hepatic insulin resistance and nonalcoholic fatty liver dis-ease: WO, 2009144554A1[P].2009-12-03.
 Pfizer Inc.New substituted 3-oxa-7-azabicyclononane compounds are G-protein-coupled receptor-119 agonists, useful to treat e.g.diabetes, metabolic disorder e.g.hyperlipidemia, myocardial infarction, arthritis, obesity, osteoporosis and hypertension: WO, 2010106457A2[P].2010-09-23.
 Pfizer Inc.New pyrimidin-4-yl-tetrahydro-pyrrolo(3,4-c)pyrazole compounds are G-protein-coupled: WO, 2011036576A1[P].2011-03-31.
 Pfizer Inc.New imidazo-pyrazole derivatives are G-protein-coupled receptor inhibitors, useful for treatment of e.g.hyperlipidemia, diabe-tes, coronary heart disease, or ischemic stroke: WO, 2011061679A1[P].2011-05-26.
 Pfizer Inc.New 4-amino-5-oxo-7,8-dihydropyrimido(5,4-f)(1,4) oxaz-epin-6(5H)-yl-phenyl compounds are diacyl-glycerol O-acyltransfer-ase 1 inhibitors, useful to treat e.g.diabetic nephropathy, hyperten-sion, diabetic nephropathy and skin cancer: WO, 2010086820A1[P].2010-08-05.
 Pfizer Inc.New (4-(4-(4-amino-5-oxo-7,8-dihydro-5H-pyrido(4,3-d) pyrimidin-6-yl)-phenyl)-cyclohexyl)-acetic acid derivatives are diacylglycerol acyltransferase-1 inhibitors useful e.g.for treating obesi-ty and type 2 diabetes: WO, 2010089685A1[P].2010-08-12.
 Pfizer Inc.New 4-amino-7,8-dihydropyrido(4,3-d) pyrimidin-5(6H)-one derivative useful for treating Type 2 diabetes, diabetes-related disorders, obesity and obesity-related disorders in animals: US, 2010197591A1[P].2010-08-05.
 Pfizer Inc.New fused pyrrolidine compounds are G-protein coupled re-ceptor 119 modulators, useful for treating e.g.diabetes, coronary heart disease, ischemic stroke, peripheral vascular disease, hypertension and congestive heart failure: WO, 2010128414A1[P].2010-11-11.
 Pfizer Inc.New pyrimidine compound useful for treating e.g.coronary heart disease, intermittent claudication, myocardial infarction, osteopo-rosis, hypertension, congestive heart failure, chronic renal failure, dia-betic neuropathy, metabolic syndrome: WO, 2010128425A1[P].2010-11-11.
 Pfizer Inc.New pyrrolidinyl-pyrimidine compounds are G-protein cou-pled receptor 119 modulators, useful for treating e.g.diabetes, coro-nary heart disease, ischemic stroke, peripheral vascular disease, hyper-tension and congestive heart failure: US, 2010285145A1[P].2010-11-11.
 Pfizer Inc.New dioxa-bicyclo(3.2.1) octane-2,3,4-triol derivatives are sodium-glucose co-transporter-2 inhibitors, useful for treating obesi-ty and type 2 diabetes and diabetes-related disorders e.g.impaired glucose tolerance and hyperinsulinemia: WO, 2011051864A1[P].2011-05-05.
 Pfizer Inc.New 1-methylcyclopropyl-3-fluoro-4-((5-methyl-6-((2-methylpyridin-3-yl) oxy) pyrimidin-4-yl)oxy)piperidine-1-carboxyl-ate is G-protein-coupled receptor modulator, useful for treating e.g.hyperlipidemia, diabetes and Alzheimers disease: WO, 2013011402A1[P].2013-01-24.
 Pfizer Inc.New substituted 3H-imidazo(4,5-b) pyridine compounds are diacylglycerol acyltransferase 2 modulator, useful for treating e.g.diabetes, obesity, ketosis, hyperlipidemia, chronic renal failure and en-dothelial dysfunction: WO, 2013150416A1[P].2013-10-10.
 Pfizer Inc.New 2-tert-butyl-1-(1H-indazol-5-ylcarbonyl)-2H-spiro (piperidine-4,5-pyrano(3,2-c)pyrazol)-7(6H)-one for treating dis-ease treated by inhibiting acetyl-coenzyme A carboxylase e.g.obesity, diabetes and nonalcoholic fatty liver disease: WO, 2009144555A1[P].2009-12-03.
 Cure DM Group Holdings LLC.New optimized proislet peptide, useful for treating a pathology associated with impaired pancreatic function, e.g.type 1 diabetes, metabolic syndrome/dysmetabolic syndrome, over-weightness, obesity, and hyperlipidemia: WO, 2009029847A1[P].2009-03-05.
 Cure DM Inc.Treatment of type 1 diabetes mellitus involves co-ad-ministration of agent that stimulates pancreatic islet cell regeneration and/or transformation and agent that specifically inhibits the activity autoimmune cells: US, 2006198839A1.2006-09-07.
 Cure DM Group Holdings LLC.New isolated human proislet, useful e.g.to increase insulin production, induce pancreatic islet neogenesis, and to treat pathology associated with impaired pancreatic function e.g.pre-diabetes and latent autoimmune diabetes in humans: EP, 2295066A1[P].2011-03-16.
 Cure DM Group Holdings LLC.New proislet peptide, e.g.huntingtin interacting protein peptides, and human regenerating islet-derived pep-tides, with an optimization modification, useful for stimulating islet neogenesis or stimulating pancreatic islet cell regeneration: EP, 2559700A2[P].2013-02-20.
 Cure DM Group Holdings LLC.Treating a pathology associated with impaired pancreatic function comprises administering to the subject a human proislet peptide: US, 2011280833A1[P].2011-11-17.
 Cure DM Group Holdings LLC.Treating pathology associated with im-paired pancreatic function including prediabetes, type 2 diabetes hy-perglycemia and latent autoimmune diabetes, comprises administering human pro-islet peptide comprising specific amino acid sequences: US, 2013190233A1.2013-07-25.
 Cure DM Group Holdings LLC, Curedm Inc.Treating pathology associ-ated with impaired pancreatic function including type 2 diabetes, la-tent autoimmune diabetes or hyperglycemia in subject e.g.human, in-volves administering human proislet peptide: US, 2010093605A1.2010-04-15.
 Cure DM Group Holdings LLC.Stimulating islet cell neogenesis in a subject comprises administering to the subject an amount of HIP2, use-ful for treating a disease or condition associated with impaired pancre-atic function, e.g.type I diabetes, and bulimia: WO, 2008064306A2[P].2008-05-29.
 CureDM Inc.Use of islet neogenesis agent for treating newly diag-nosed or pre-existing type 1 diabetes, treating newly diagnosed or preexisting type 2 diabetes, and treating a pathology associated with im-paired pancreatic function: US, 2009142338A1[P].2009-06-04.
 CureDM Inc.New human proIslet peptide which stimulates pancreatic islet cell regeneration, useful for treating diseases or disorders having impaired pancreatic function, e.g.type 1 diabetes, type 2 diabetes, and latent autoimmune diabetes: US, 2008300190A1[P].2008-12-04.
 Boehringer Ingelheim Int.Co.Ltd.Method for slowing progression of, delaying or treating of pre-diabetes in a patient diagnosed of being overweight or obese, comprises administering one or more antiobesity drugs: WO, 2013139777A1[P].2013-09-26.
 Boehringer Ingelheim Int.Co.Ltd.Pharmaceutical combination, com-position or kit useful for e.g.treating obesity, comprises dipeptidyl pep-tidase-4 inhibitor, preferably linagliptin, and glucagon-like peptide-1(GLP-1) analog having short half life e.g.exendin-4: WO, 2013098372A1[P].2013-07-04.
 Boehringer Ingelheim Int.Composition, useful e.g.to treat and prevent hyperuricemia, kidney stones and hyponatremia, comprises a sodiumdependent glucose cotransporter-2 inhibitor, a dipeptidyl peptidaseIV inhibitor, and an antidiabetic agent e.g.biguanides: WO, 2010092125A1.2010-08-19.
 Boehringer Ingelheim Int.Pharmaceutical compound, composition or combination used for preventing and/or treating metabolic disorder e.g.type 1 diabetes mellitus, comprises dipeptidyl peptidase-4 inhibitor,like peptide 1 receptor agonists useful to treat type I diabetes, type Ⅱ diabetes, gestational diabetes, obesity, excessive appetite, insufficient satiety or metabolic disorder: WO, 2013090454A2.2013-06-20.
 Boehm M.F.New substituted heterocyclic compound useful for treat-ing malcondition e.g.type I diabetes, type Ⅱ diabetes, gestational dia-betes, obesity, excessive appetite, insufficient satiety or metabolic dis-order in a patient: WO, 2014201172A1[P].2014-12-18
 Boehm M.F.New substituted aryl compounds are glucagon-like pep-tide agonists useful to treat malconditon comprising type I diabetes, type Ⅱ diabetes, gestational diabetes, obesity, excessive appetite, insuf-ficient satiety and metabolic disorder: WO, 2012166951A1[P].2012-12-06.
 Lilly&Co Eli.Treating gastroparesis, e.g.a delay in gastric emptying time, in a patient with type 2 diabetes comprising administering to a patient a GLP-1 compound: WO, 03087139A2[P].2003-10-23.
 Novo Nordisk.Preventing or treating alcoholism or drug addiction, comprises administering an amount of a glucagon-like peptide-1(GLP-1) (I) agonist to a subject: WO, 2013083826A2[P].2013-06-13.
 Novo Nordisk.Use of glucagon like peptide-1 agonist for e.g.reduc-ing food intake; treating binge eating disorder, bulimia nervosa, crav-ing for food, obesity; changing the snack preference; and lowering the snack intake: WO, 2005056036A2[P].2005-06-23.
 Amylin Pharm Inc.Use of glucagon like peptide 1(GLP-1) receptor agonist compound or a pharmaceutical composition comprising a GLP-1 receptor agonist compound for treating, e.g.non-rapid eye move-ment sleep disorder, sleepwalking disorder, or sleep bruxism: WO, 2010138671A1[P].2010-12-02.
 Amylin Pharm Inc.Method for treating e.g.pancreatitis, diabetes and their associated symptoms or reducing plasma amylase and plasma li-pase concentrations in human involves administering exenatide or glu-cagon-like peptide-1 receptor agonist to human: WO, 2011156407A2[P].2011-12-15.
 Amylin Pharm Inc.Treating obstructive sleep apnea in a patient in-volves administering to the patient glucagon-like protein-1 receptor agonist compound or pharmaceutical composition comprising glucagonlike protein-1 receptor agonist compound: WO, 2011056713A2[P].2011-05-12.and optionally antidiabetic agents: WO, 2011064352A1[P].2011-06-03.
 Boehringer Ingelheim Int.Composition, useful e.g.to treat e.g.im-paired glucose tolerance and metabolic syndrome, comprises 6-(2-hy-droxy-2-methylpropyl)-3-(1-(1-methyl-2-oxo-1, 2-dihydropyridin-4-yl) phenyl-ethyl)-6-phenyl-1, 3-oxazinan-2-one and therapeutic agent: WO, 2012059416.2012-05-10.
 Boehringer Ingelheim Int.Composition, useful for e.g.treating diabe-tes mellitus, hypoglycemia, postprandial hyperglycemia, myocardial in-farction, and heart failure, comprises sodium glucose cotransporter in-hibitor, and glucagon-like peptide receptor agonist: WO, 2012107476A1[P].2012-08-16.
 Boehringer Ingelheim Int.Combination, useful for e.g.treating hyper-glycemia, overweight, obesity, hyperlipidemia, hypertension and athero-sclerosis, comprises a glucagon-like peptide-1 receptor agonist and a dipeptidyl peptidase-4 inhibitor i.e.linagliptin: WO, 2011138421A1[P].2011-11-10.
 Boehringer Ingelheim Int.Pharmaceutical composition used for, e.g.preventing type 1 diabetes mellitus, comprises dipeptidyl peptidase-4 inhibitor: WO, 2010092163A2[P].2010-08-19.
 Boehm M.F.New substituted phenyl keto compounds are glucagon-like peptide 1 receptor agonists useful to treat type I diabetes, type Ⅱ diabetes, gestational diabetes, obesity, excessive appetite, insufficient satiety or metabolic disorder: WO, 2013090454A2. 2013-06-20.
 Boehm M. F. New substituted heterocyclic compound useful for treating malcondition e.g. type I diabetes, type Ⅱ diabetes, gestational diabetes, obesity, excessive appetite, insufficient satiety or metabolic disorder in a patient: WO, 2014201172A1[P]. 2014-12-18
 Boehm M. F. New substituted aryl compounds are glucagon-like peptide agonists useful to treat malconditon comprising type I diabetes, type Ⅱ diabetes, gestational diabetes, obesity, excessive appetite, insufficient satiety and metabolic disorder: WO, 2012166951A1[P]. 2012-12-06.
 Lilly&Co Eli. Treating gastroparesis, e.g. a delay in gastric emptying time, in a patient with type 2 diabetes comprising administering to a patient a GLP-1 compound: WO, 03087139A2[P]. 2003-10-23.
 Novo Nordisk. Preventing or treating alcoholism or drug addiction, comprises administering an amount of a glucagon-like peptide-1(GLP-1) (I) agonist to a subject: WO, 2013083826A2[P]. 2013-06-13.
 Novo Nordisk. Use of glucagon like peptide-1 agonist for e.g. reducing food intake; treating binge eating disorder, bulimia nervosa, craving for food, obesity; changing the snack preference; and lowering the snack intake: WO, 2005056036A2[P]. 2005-06-23.
 Amylin Pharm Inc. Use of glucagon like peptide 1(GLP-1) receptor agonist compound or a pharmaceutical composition comprising a GLP-1 receptor agonist compound for treating, e.g. non-rapid eye movement sleep disorder, sleepwalking disorder, or sleep bruxism: WO, 2010138671A1[P]. 2010-12-02.
 Amylin Pharm Inc. Method for treating e.g. pancreatitis, diabetes and their associated symptoms or reducing plasma amylase and plasma lipase concentrations in human involves administering exenatide or glucagon-like peptide-1 receptor agonist to human: WO, 2011156407A2[P]. 2011-12-15.
 Amylin Pharm Inc. Treating obstructive sleep apnea in a patient involves administering to the patient glucagon-like protein-1 receptor agonist compound or pharmaceutical composition comprising glucagonlike protein-1 receptor agonist compound: WO, 2011056713A2[P]. 2011-05-12.
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