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公开(公告)号:US10689429B2
公开(公告)日:2020-06-23
申请号:US15301960
申请日:2015-04-07
申请人: Novo Nordisk A/S
发明人: Lars Linderoth , Jacob Kofoed , Jesper Lau , Paw Bloch , Patrick William Garibay , Janos Tibor Kodra
IPC分类号: C07K14/605 , C07C235/20 , A61K38/00
摘要: The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first Lys residue at a position corresponding to position 36 of GLP-1(7-37) (SEQ ID NO: 1), a second Lys residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of seven amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 1); which derivative comprises two protractors attached to said first and second Lys residue, respectively, each via a linker; wherein the protractor is selected from: HOOC—C6H4—O—(CH2)y—CO—*, and Chem. 1: HOOC—(CH2)x—CO—*, Chem. 2: wherein y is an integer in the range of 8-11, and x is 12; and the linker comprises at least one of: *—NH—CH(COOH)—(CH2)2—CO—*, Chem. 3: *—NH—CH((CH2)2—COOH)—CO—*, and/or Chem. 4: *—NH—(CH2)2—[O—(CH2)2]k—O—[CH2]n—CO—*, Chem. 5: wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical uses thereof, such as for the treatment of diabetes and obesity, as well as to the GLP-1 peptides forming part of these derivatives which have Lys residues at positions 36 and 37 and no other Lys residues, and the GLP-1(9-37) fragments thereof. The invention furthermore relates to an intermediate product comprising 3-carboxyphenoxy-nonanoic acid with a protection group at the carboxy group of the nonanoic acid, optionally via a linker. The derivatives have a very good potency and a long half-life which makes them potentially useful for, e.g., oral administration.
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公开(公告)号:US10604554B2
公开(公告)日:2020-03-31
申请号:US15966642
申请日:2018-04-30
申请人: Novo Nordisk A/S
IPC分类号: C07K14/605 , A61K38/26 , A61K38/00
摘要: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1: HOOC—(CH2)x—CO—*, and Chem. 2: HOOC—C6H4—O—(CH2)y—CO—*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, which is connected at its CO—* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptide and linker intermediates. The derivatives are potent, stable, protracted, and suitable for oral administration.
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公开(公告)号:US10603442B2
公开(公告)日:2020-03-31
申请号:US15505423
申请日:2015-08-25
申请人: Novo Nordisk A/S
摘要: A logging device adapted to be attached to a pen drug delivery device (210) and capture a property value related to the dose amount of drug expelled from the drug delivery device during an expelling event, the logging device comprising a bore in which a snap lock with a flexible wire portion is arranged circumferentially in the bore, the wire being adapted to be moved laterally by a projection on the pen device and subsequently snap inwardly when the pen device is inserted axially in the bore. In this way an axial snap lock is provided between the logging device and the drug delivery device.
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公开(公告)号:US10603437B2
公开(公告)日:2020-03-31
申请号:US15464968
申请日:2017-03-21
申请人: Novo Nordisk A/S
发明人: Henrik Bengtsson , Toke Folke Christensen , Louise Wagner Noergaard , Mads Schenstroem Stefansen
IPC分类号: A61M5/24 , G16H40/63 , G06F19/00 , A61B5/145 , A61M5/315 , A61M5/32 , G06Q50/22 , G16H10/65 , A61M5/172 , A61M5/31
摘要: A system for optimizing a patient's basal insulin dosage regimen over time, adapted to determine from blood glucose values whether and by how much to vary a patient's present recommended amount of the insulin-containing drug in order to maintain the patient's future blood glucose level measurements within a predefined range, and wherein a given blood glucose value is disregarded if no patient-actuated operation being indicative of the administration of a dose of an insulin containing drug has been detected in a pre-defined amount of time prior to the determination of the given blood glucose value.
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公开(公告)号:US10596328B2
公开(公告)日:2020-03-24
申请号:US15532579
申请日:2015-12-22
申请人: Novo Nordisk A/S
摘要: The present invention relates to a drug delivery device (100) comprising a housing (101), a threaded piston rod (102), a rotatable drive tube (103), a drive nut (104) in threaded engagement with the piston rod (102) and being rotationally locked but axially moveable relative to the drive tube (103), and a support member (105) arranged rotationally free on the piston rod (102), the support member (105) being axially locked relative to the housing (101) and arranged to allow the drive tube (103) to move axially. The device further comprises a compression drive spring (106) arranged between the piston rod (102) and the drive tube (103), the compression drive spring (106) being arranged axially between the drive nut (104) and the support member (105).
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公开(公告)号:US20200079829A1
公开(公告)日:2020-03-12
申请号:US16614454
申请日:2018-05-23
申请人: Novo Nordisk A/S
发明人: Xiang Gao , Xujia Zhang , Hongtao Guan , Henning Thoegersen , Kristian Sass-Oerum , Lars Fogh Iversen , Per Noergaard , Sebastian Beck Joergensen , Kristian Tage Hansen , Yi Wang , Kilian Waldemar Conde Frieboes , Birgit Wieczorek
IPC分类号: C07K14/495
摘要: The invention relates to MIC-1 compounds. More specifically it relates to compounds comprising a MIC-1 polypeptide with an N-terminal amino acid extension and a protractor wherein the amino acid extension comprises 3 to 36 amino acid residues and where the MIC-1 polypeptide and the N-terminal amino acid extension together have a calculated pI lower than 6.5. The compounds of the invention have MIC-1 activity. The invention also relates to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable excipients, as well as the medical use of the compounds.
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公开(公告)号:US10570184B2
公开(公告)日:2020-02-25
申请号:US15315985
申请日:2015-06-03
申请人: Novo Nordisk A/S
发明人: Ulrich Sensfuss , Jesper F. Lau , Thomas Kruse
摘要: The present invention relates to novel glucagon derivatives which are GLP-1/glucagon receptor co-agonists, and to the use of the glucagon derivatives in medicine, such as in the treatment of diabetes, obesity and related diseases and conditions.
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公开(公告)号:US10556066B2
公开(公告)日:2020-02-11
申请号:US15575864
申请日:2016-05-26
申请人: Novo Nordisk A/S
发明人: Andre Larsen
摘要: An assembly comprises an electric consumer, an electric voltage source adapted to power the electric consumer, and user operated actuation means. The electric voltage source is operatable between a first state in which a first voltage is generated and a second state in which a second higher voltage is generated. The user operated actuation means is operatable from a first to a second state and adapted to thereby operate the electric voltage source from the first to the second state, and operatable from the second state to the first state and adapted to thereby operate the electric voltage source from the second to the first state.
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公开(公告)号:US20200030542A1
公开(公告)日:2020-01-30
申请号:US16500991
申请日:2018-04-06
申请人: Novo Nordisk A/S
IPC分类号: A61M5/315
摘要: The present invention provides a drug injection device (1) for delivering multiple doses of drug, comprising: a housing (2) extending along a main axis, a dose expelling mechanism comprising a piston rod (60) configured to move relative to the housing (2) from a first position to a second position to cause ejection of a dose of drug, the piston rod (60) extending between a proximal piston rod end and a distal piston rod end and comprising a dosing track (63), the piston rod (60) further being movable relative to the housing (2) from an initial pre-use position to a final end stop position to cause accumulated ejection of a predefined total dose, a dosing track follower (17) fixed with respect to the housing (2) and adapted to travel the dosing track (63) during dose ejection, a dose setting mechanism operable to set the dose to be ejected by the dose expelling mechanism, electronic means (82, 90, 91, 92, 95) for registering a dose setting operation and for registering a dose size of an ejected dose, and a display (81) adapted to indicate a size of a current set dose, the electronic means (82, 90, 91, 92, 95) being configured to provide a first type of update of the display (81) responsive to dose changing operations of the dose setting mechanism, wherein the electronic means (82, 90, 91, 92, 95) is further configured to calculate a current accumulated dose from the dose sizes of registered ejected doses to thereby provide an updated value of a total amount of drug ejected, determine a current remaining dose by comparing the current accumulated dose and the predefined total dose, and provide a second type of update of the display (81) when during a dose increasing operation of the dose setting mechanism the current set dose exceeds the current remaining dose, the second type of update being different from the first type of update, and wherein the final end stop position is defined by a track end configuration of the dosing track (63) between the proximal piston rod end and the distal piston rod end.
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公开(公告)号:US20200030541A1
公开(公告)日:2020-01-30
申请号:US16589566
申请日:2019-10-01
申请人: Novo Nordisk A/S
摘要: The present invention relates to an injection device comprising a torsion spring operatively connected to a dose setting member being adapted to set a dose to be ejected from the injection device. A rotatably mounted display member adapted to display the dose to be ejected in accordance with a setting of the dose setting member is also provided. The rotatably mounted display member is adapted to be rotated over an angle corresponding to at least one revolution of the display member. The display member may be implemented as a dose indicator barrel having numerals arranged along a helical path on an outer surface thereof, or alternatively, as a counting device having two or more display wheels having numerals arranged on an outer surface thereof.
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