JP2013523619A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013523619A5 JP2013523619A5 JP2013500535A JP2013500535A JP2013523619A5 JP 2013523619 A5 JP2013523619 A5 JP 2013523619A5 JP 2013500535 A JP2013500535 A JP 2013500535A JP 2013500535 A JP2013500535 A JP 2013500535A JP 2013523619 A5 JP2013523619 A5 JP 2013523619A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- ethoxy
- carboxy
- butanoyl
- acetyl
- 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.)
- Granted
Links
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 174
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 127
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 102
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 87
- 125000003277 amino group Chemical compound 0.000 claims 81
- -1 18-hydroxy-18-oxooctadecanoyl Chemical group 0.000 claims 49
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 45
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 38
- 108060003199 Glucagon Proteins 0.000 claims 27
- 229960004666 Glucagon Drugs 0.000 claims 26
- MASNOZXLGMXCHN-ZLPAWPGGSA-N Glucagonum Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 25
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- 206010020993 Hypoglycaemia Diseases 0.000 claims 10
- 230000002218 hypoglycaemic Effects 0.000 claims 10
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 7
- 150000001413 amino acids Chemical group 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 208000001072 Type 2 Diabetes Mellitus Diseases 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 208000002705 Glucose Intolerance Diseases 0.000 claims 4
- 239000004472 Lysine Substances 0.000 claims 4
- 206010012601 Diabetes mellitus Diseases 0.000 claims 3
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 229960003104 Ornithine Drugs 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Substances N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 206010033307 Overweight Diseases 0.000 claims 2
- 230000002496 gastric Effects 0.000 claims 2
- 235000020825 overweight Nutrition 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 206010004716 Binge eating Diseases 0.000 claims 1
- 206010006550 Bulimia nervosa Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- 208000004981 Coronary Disease Diseases 0.000 claims 1
- 206010012335 Dependence Diseases 0.000 claims 1
- 206010061818 Disease progression Diseases 0.000 claims 1
- 206010058108 Dyslipidaemia Diseases 0.000 claims 1
- 102100003818 GCG Human genes 0.000 claims 1
- 101710042131 GCG Proteins 0.000 claims 1
- 101700071595 GRZ1 Proteins 0.000 claims 1
- 210000001035 Gastrointestinal Tract Anatomy 0.000 claims 1
- 206010018464 Glycogen storage disease type I Diseases 0.000 claims 1
- 206010019708 Hepatic steatosis Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010022498 Insulinoma Diseases 0.000 claims 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 1
- 206010061227 Lipid metabolism disease Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 101700078733 ZGLP1 Proteins 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 235000021407 appetite control Nutrition 0.000 claims 1
- 201000001320 atherosclerosis Diseases 0.000 claims 1
- 239000002876 beta blocker Substances 0.000 claims 1
- 230000037396 body weight Effects 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 201000008739 coronary artery disease Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 238000005516 engineering process Methods 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 235000020828 fasting Nutrition 0.000 claims 1
- 230000037406 food intake Effects 0.000 claims 1
- 235000012631 food intake Nutrition 0.000 claims 1
- 201000004541 glycogen storage disease I Diseases 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000007689 inspection Methods 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 230000004899 motility Effects 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000035935 pregnancy Effects 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrugs Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000036186 satiety Effects 0.000 claims 1
- 235000019627 satiety Nutrition 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000004584 weight gain Effects 0.000 claims 1
- 235000019786 weight gain Nutrition 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
- WTNGPLGFFGCYMU-ZQWQDMLBSA-N CC([C@H](CCCCNC(CC[C@@H](C(O)=O)NC(CC[C@@H](C(O)=O)NC(COCCOCCNC(CC[C@@H](C(O)=O)NC(CCCCCCCCCCCCCCCCC(O)=O)=O)=O)=O)=O)=O)NC)=O Chemical compound CC([C@H](CCCCNC(CC[C@@H](C(O)=O)NC(CC[C@@H](C(O)=O)NC(COCCOCCNC(CC[C@@H](C(O)=O)NC(CCCCCCCCCCCCCCCCC(O)=O)=O)=O)=O)=O)=O)NC)=O WTNGPLGFFGCYMU-ZQWQDMLBSA-N 0.000 description 1
- RUKXKBJQLHBSJS-KDHDBVBQSA-N CN[C@@H](CCCCNC(CC[C@@H](C(O)=O)NC(CCC(C(O)=O)NC(COCCOCCNC(COCCOCCNC(CC[C@@H](C(O)=O)NC(CCCCCCCCCOc(cc1)ccc1C(O)=O)=O)=O)=O)=O)=O)=O)C(C=C)=O Chemical compound CN[C@@H](CCCCNC(CC[C@@H](C(O)=O)NC(CCC(C(O)=O)NC(COCCOCCNC(COCCOCCNC(CC[C@@H](C(O)=O)NC(CCCCCCCCCOc(cc1)ccc1C(O)=O)=O)=O)=O)=O)=O)=O)C(C=C)=O RUKXKBJQLHBSJS-KDHDBVBQSA-N 0.000 description 1
- 0 CN[C@@](CCCCNC(CC[C@@](C(O)=O)NC(CCC(CO)NC(COCCOCCNC(COCCOCCNC(CC[C@@](*(O)=O)NC(CCCCCCCCCCCCCCCCC(O)=O)=O)=O)=O)=O)=O)=O)C(*)=O Chemical compound CN[C@@](CCCCNC(CC[C@@](C(O)=O)NC(CCC(CO)NC(COCCOCCNC(COCCOCCNC(CC[C@@](*(O)=O)NC(CCCCCCCCCCCCCCCCC(O)=O)=O)=O)=O)=O)=O)=O)C(*)=O 0.000 description 1
Claims (17)
- グルカゴンペプチドであって、配列番号 1と、前記グルカゴンペプチドにおける7個までのアミノ酸置換と、3個以上の負に荷電している部分を含む置換基(前記負に荷電している部分のうちの1個は、親油性部分から遠位にあり、前記置換基は、前記グルカゴンペプチドの次のアミノ酸位置:X10、X12、X16、X17、X18、X20、X21、X24、X25、X27、X28、X29および/またはX30のうちの1個または複数中のLysのイプシロン位か、Ornのデルタ位か、またはCysの硫黄に結合している)とを含むグルカゴンペプチドまたは薬学的に許容されるその塩、アミド、酸もしくはプロドラッグ。
- 前記置換が前記グルカゴンペプチドの次の位置: X2、X4、X9、X10、X12、X16、X17、X18、X20、X21、X24、X25、X27、X28、X29および/またはX30に存在する、請求項1に記載のグルカゴンペプチド。
- 前記置換基が式IIを有する、請求項1から2のいずれかに記載のグルカゴンペプチド:
Z1-Z2-Z3-Z4 [II]
[式中、
Z1は、式IIa、IIbまたはIIcの1つによる構造を表し;
式IIc中のmは5〜11であり、
式IIc中のCOOH基は、フェニル環上の2、3または4位に結合していてよく、式IIa、IIbおよびIIc中の記号*は、Z2中の窒素への結合点を表し;Z2が存在しない場合、Z1は記号*でZ3上の窒素に結合し;Z2およびZ3が存在しない場合、Z1は記号*でZ4上の窒素に結合している)
Z2は存在しないか、または式IId、IIe、IIf、IIg、IIh、IIi、IIjもしくはIIkの1つによる構造を表し;
Z2は、*で示されている炭素原子を介して、*で示されているZ3の窒素に結合しており;Z3が存在しない場合、Z2は、*で示されている炭素原子を介して、*で示されているZ4の窒素に結合しており、かつZ3およびZ4が存在しない場合、Z2は、*で示されている炭素を介して、グルカゴンペプチドのリシンのイプシロン窒素またはオルニチンのデルタ窒素に結合している)
Z3は存在しないか、または式IIm、IIn、IIoまたはIIpの1つによる構造を表し;
Z4は存在しないか、または式IId、IIe、IIf、IIg、IIh、IIi、IIjもしくはIIkの1つによる構造を表し;ここで、各アミノ酸部分は独立に、LまたはDのいずれかであり、Z4は、記号*で示されている炭素を介して、グルカゴンペプチドのリシンのイプシロン窒素またはオルニチンのデルタ窒素に結合している]。 - 前記置換基が式IIIa、IIIb、IIIc、IIId、IIIe、IIIf、IIIg、IIIh、IIIi、IIIj、IIIk、IIIl、IIIm、IIInまたはIIIoの1つによる構造を表す、請求項1から3のいずれかに記載のグルカゴンペプチド:
- 前記置換基が前記グルカゴンペプチドの次のアミノ酸位置:X12、X16、X20、X24、X25、X28、X29および/またはX30のうちの1つまたは複数に存在する、請求項1から4のいずれかに記載のグルカゴンペプチド。
- 前記置換基が前記グルカゴンペプチドの次のアミノ酸位置:X16、X24および/またはX28のうちの1つまたは複数に存在する、請求項1から5のいずれかに記載のグルカゴンペプチド。
- 前記置換基が前記グルカゴンペプチドのアミノ酸位置X24に存在する、請求項1から6のいずれかに記載のグルカゴンペプチド。
- 下記からなる群から選択される、請求項1から7のいずれか一項に記載のグルカゴンペプチド。
Nε24-([(4S)-5-ヒドロキシ-4-[[(4S)-5-ヒドロキシ-4-[[2-[2-[2-[[2-[2-[2-[[(4S)-5-ヒドロキシ-4-[(18-ヒドロキシ-18-オキソオクタデカノイル)アミノ]-5-オキソペンタノイル]アミノ]エトキシ]エトキシ]アセチル]アミノ]エトキシ]エトキシ]アセチル]アミノ]-5-オキソペンタノイル]アミノ]-5-オキソペンタノイル])[Lys24,Leu27]グルカゴン
- 請求項1から8のいずれか一項に記載のグルカゴンペプチドを含む医薬組成物。
- 1種または複数の追加の治療活性化合物または物質をさらに含む、請求項9に記載の医薬組成物。
- GLP-1化合物をさらに含む、請求項9から10のいずれか一項に記載の医薬組成物。
- インスリン化合物をさらに含む、請求項9から11のいずれか一項に記載の医薬組成物。
- 非経口投与に適している、請求項9から12のいずれか一項に記載の医薬組成物。
- 療法で使用するための、請求項1から8のいずれか一項に記載のグルカゴンペプチドを含む医薬組成物。
- 高血糖、2型糖尿病、耐糖能障害、1型糖尿病および肥満を治療または予防するための医薬品を調製するための、請求項1から8のいずれか一項に記載のグルカゴンペプチドを含む医薬品。
- 2型糖尿病における疾患進行を遅延または予防するための、肥満を治療するための、または過体重を予防するための、食物摂取量を低下させるための、エネルギー消費を増大させるための、体重を減少させるための、耐糖能障害(IGT)から2型糖尿病への進行を遅延させるための;2型糖尿病からインスリン要求性糖尿病への進行を遅延させるための;食欲を制御するための;満腹を誘発するための;体重減少の成功後に体重再増加を予防するための;過体重または肥満に関連する疾患または状態を治療するための;大食症を治療するための;暴食を治療するための;アテローム硬化症、高血圧、2型糖尿病、IGT、脂質異常症、冠状動脈性心疾患、肝脂肪症を治療するための、ベータ遮断薬中毒を治療するための、X線、CT-およびNMR走査などの技術を使用する胃腸管の検査に関連して有用な胃腸管の運動性の阻害のために使用するための、請求項1から８のいずれか一項に記載のグルカゴンペプチドを含む医薬品。
- 低血糖、インスリン誘発性低血糖、反応性低血糖、糖尿病性低血糖、非糖尿病性低血糖、空腹時低血糖、薬物誘発性低血糖、胃バイパス誘発性低血糖、妊娠時低血糖、アルコール誘発性低血糖、インスリノーマおよびフォン・ギールケ病を治療または予防するための医薬品を調製するための、請求項1から8のいずれか一項に記載のグルカゴンペプチドを含む医薬品。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10157901.9 | 2010-03-26 | ||
| EP10157901 | 2010-03-26 | ||
| US31999410P | 2010-04-01 | 2010-04-01 | |
| US61/319,994 | 2010-04-01 | ||
| PCT/EP2011/054714 WO2011117416A1 (en) | 2010-03-26 | 2011-03-28 | Novel glucagon analogues |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016141243A Division JP2016183192A (ja) | 2010-03-26 | 2016-07-19 | 新規のグルカゴンアナログ |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013523619A JP2013523619A (ja) | 2013-06-17 |
| JP2013523619A5 true JP2013523619A5 (ja) | 2014-05-22 |
| JP6026993B2 JP6026993B2 (ja) | 2016-11-16 |
Family
ID=42710766
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013500534A Expired - Fee Related JP6054861B2 (ja) | 2010-03-26 | 2011-03-28 | 新規のグルカゴン類似体 |
| JP2013500535A Expired - Fee Related JP6026993B2 (ja) | 2010-03-26 | 2011-03-28 | 新規のグルカゴンアナログ |
| JP2016141243A Withdrawn JP2016183192A (ja) | 2010-03-26 | 2016-07-19 | 新規のグルカゴンアナログ |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013500534A Expired - Fee Related JP6054861B2 (ja) | 2010-03-26 | 2011-03-28 | 新規のグルカゴン類似体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016141243A Withdrawn JP2016183192A (ja) | 2010-03-26 | 2016-07-19 | 新規のグルカゴンアナログ |
Country Status (12)
| Country | Link |
|---|---|
| US (8) | US20130143798A1 (ja) |
| EP (2) | EP2552951A1 (ja) |
| JP (3) | JP6054861B2 (ja) |
| KR (1) | KR20130018410A (ja) |
| CN (2) | CN102918056B (ja) |
| AU (1) | AU2011231503C1 (ja) |
| BR (1) | BR112012024379A2 (ja) |
| CA (1) | CA2792663A1 (ja) |
| MX (1) | MX336412B (ja) |
| RU (1) | RU2559320C2 (ja) |
| WO (2) | WO2011117416A1 (ja) |
| ZA (1) | ZA201206838B (ja) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2830974A1 (en) * | 2011-03-28 | 2012-10-04 | Jesper F. Lau | Novel glucagon analogues |
| DK3878859T5 (da) | 2011-06-10 | 2024-06-10 | Hanmi Science Co Ltd | Hidtil ukendte oxyntomodulinderivater og farmaceutisk præparat til behandling af fedme omfattende disse |
| CN109306015B (zh) | 2011-06-17 | 2022-04-26 | 韩美科学株式会社 | 包括泌酸调节肽和免疫球蛋白片段的结合物以及其应用 |
| AU2012311484B2 (en) | 2011-09-23 | 2017-04-13 | Novo Nordisk A/S | Novel glucagon analogues |
| MX2014015423A (es) * | 2012-06-14 | 2015-04-09 | Sanofi Sa | Analogos de peptido de exedina-4. |
| DK2875043T3 (en) | 2012-07-23 | 2017-03-27 | Zealand Pharma As | glucagon |
| KR101968344B1 (ko) | 2012-07-25 | 2019-04-12 | 한미약품 주식회사 | 옥신토모듈린 유도체를 포함하는 고지혈증 치료용 조성물 |
| TWI608013B (zh) | 2012-09-17 | 2017-12-11 | 西蘭製藥公司 | 升糖素類似物 |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| KR101993393B1 (ko) | 2012-11-06 | 2019-10-01 | 한미약품 주식회사 | 옥신토모듈린 유도체를 포함하는 당뇨병 또는 비만성 당뇨병 치료용 조성물 |
| DK2916819T3 (da) | 2012-11-06 | 2019-10-14 | Hanmi Pharm Ind Co Ltd | Væskeformig formulering af proteinkonjugat omfattende oxyntomodulinet og et immunoglobulin-fragment |
| CN118324870A (zh) * | 2012-11-20 | 2024-07-12 | 梅德瑞斯糖尿病有限责任公司 | 用于胰岛素抗性的改良的肽药物 |
| PE20151239A1 (es) | 2012-12-21 | 2015-09-08 | Sanofi Sa | Derivados de exendina-4 funcionalizada |
| CA2907454C (en) | 2013-03-21 | 2021-05-04 | Sanofi-Aventis Deutschland Gmbh | Synthesis of hydantoin containing peptide products |
| DK2976325T3 (en) | 2013-03-21 | 2017-06-06 | Sanofi Aventis Deutschland | SYNTHESIS OF PEPTIDE PRODUCTS CONTAINING CYCLIC IMID |
| AR095986A1 (es) | 2013-04-03 | 2015-11-25 | Sanofi Sa | Proteínas modificadas que regulan glucosa en sangre con perfil alterado de actividad farmacológica y preparación de las mismas |
| MX362275B (es) * | 2013-04-18 | 2019-01-10 | Novo Nordisk As | Co-agonista de peptido similar a glucagon tipo 1 (glp-1) receptor de glucagon de larga duracion, estables para uso medico. |
| DK2986313T3 (da) * | 2013-04-18 | 2019-08-12 | Novo Nordisk As | Stabile, protraherendede glp-1/glucagonreceptor-co-agonister til medicinsk anvendelse |
| EP3010546B1 (en) | 2013-06-20 | 2017-08-09 | Novo Nordisk A/S | Glp-1 derivatives and uses thereof |
| GB201315335D0 (en) * | 2013-08-29 | 2013-10-09 | Of Singapore | Amino diacids containing peptide modifiers |
| US9988429B2 (en) | 2013-10-17 | 2018-06-05 | Zealand Pharma A/S | Glucagon analogues |
| DK3057984T3 (en) | 2013-10-17 | 2018-10-08 | Zealand Pharma As | ACYLED GLUCAGON ANALOGS |
| CN105829339B (zh) * | 2013-11-06 | 2021-03-12 | 西兰制药公司 | 胰高血糖素-glp-1-gip三重激动剂化合物 |
| JP6682432B2 (ja) | 2013-11-06 | 2020-04-15 | ジーランド ファーマ アクティーゼルスカブ | Ｇｉｐ−ｇｌｐ−１デュアルアゴニスト化合物及び方法 |
| TW201609795A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 作為雙重ｇｌｐ－１／ｇｉｐ受體促效劑的艾塞那肽－４（ｅｘｅｎｄｉｎ－４）胜肽類似物 |
| TW201609797A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 雙重ｇｌｐ－１／升糖素受體促效劑 |
| EP3080154B1 (en) | 2013-12-13 | 2018-02-07 | Sanofi | Dual glp-1/gip receptor agonists |
| WO2015086731A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Exendin-4 peptide analogues as dual glp-1/glucagon receptor agonists |
| TW201609796A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 非醯化之艾塞那肽－４（ｅｘｅｎｄｉｎ－４）胜肽類似物 |
| AR098616A1 (es) * | 2013-12-18 | 2016-06-01 | Lilly Co Eli | Péptido para el tratamiento de hipoglicemia severa |
| US9963496B2 (en) | 2014-02-18 | 2018-05-08 | Novo Nordisk A/S | Stable glucagon analogues and use for treatment of hypoglycaemia |
| TW201625668A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 作為胜肽性雙重ｇｌｐ－１／昇糖素受體激動劑之艾塞那肽－４衍生物 |
| TW201625669A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自艾塞那肽－４（Ｅｘｅｎｄｉｎ－４）之肽類雙重ＧＬＰ－１／升糖素受體促效劑 |
| TW201625670A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自ｅｘｅｎｄｉｎ－４之雙重ｇｌｐ－１／升糖素受體促效劑 |
| EP3151852A1 (en) * | 2014-06-04 | 2017-04-12 | Novo Nordisk A/S | Glp-1/glucagon receptor co-agonists for medical use |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| TWI802396B (zh) | 2014-09-16 | 2023-05-11 | 南韓商韓美藥品股份有限公司 | 長效glp-1/高血糖素受體雙促效劑治療非酒精性脂肝疾病之用途 |
| WO2016055610A1 (en) * | 2014-10-10 | 2016-04-14 | Novo Nordisk A/S | Stable glp-1 based glp-1/glucagon receptor co-agonists |
| EP3212218B1 (en) | 2014-10-29 | 2021-06-30 | Zealand Pharma A/S | Gip agonist compounds and methods |
| ES2739289T3 (es) | 2014-11-27 | 2020-01-30 | Novo Nordisk As | Derivados de GLP-1 y sus usos |
| CN107108714B (zh) | 2014-12-17 | 2022-02-08 | 诺和诺德股份有限公司 | Glp-1衍生物及其用途 |
| KR102418477B1 (ko) | 2014-12-30 | 2022-07-08 | 한미약품 주식회사 | 글루카곤 유도체 |
| PE20230304A1 (es) * | 2014-12-30 | 2023-02-13 | Hanmi Pharm Ind Co Ltd | Derivados de glucagon como agentes hipoglucemicos y antiobesidad |
| CA2980978A1 (en) | 2015-04-16 | 2016-10-20 | Zealand Pharma A/S | Acylated glucagon analogue |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| WO2016198628A1 (en) | 2015-06-12 | 2016-12-15 | Sanofi | Non-acylated exendin-4 derivatives as dual glp-1/glucagon receptor agonists |
| WO2016198624A1 (en) | 2015-06-12 | 2016-12-15 | Sanofi | Exendin-4 derivatives as trigonal glp-1/glucagon/gip receptor agonists |
| HUE066226T2 (hu) | 2015-06-30 | 2024-07-28 | Hanmi Pharmaceutical Co Ltd | Glükagon származék és annak hosszú hatású konjugátumát tartalmazó készítmény |
| AR105284A1 (es) | 2015-07-10 | 2017-09-20 | Sanofi Sa | Derivados de exendina-4 como agonistas peptídicos duales específicos de los receptores de glp-1 / glucagón |
| TWI622596B (zh) | 2015-10-26 | 2018-05-01 | 美國禮來大藥廠 | 升糖素受體促效劑 |
| EP4442314A2 (en) * | 2015-10-28 | 2024-10-09 | Tufts University | Novel polypeptides with improved proteolytic stability, and methods of preparing and using same |
| CA3010265A1 (en) | 2015-12-31 | 2017-07-06 | Hanmi Pharm. Co., Ltd. | Long-acting conjugate of triple glucagon/glp-1/gip receptor agonist |
| IL263934B2 (en) * | 2016-06-29 | 2023-10-01 | Hanmi Pharm Ind Co Ltd | A derivative of glucagon, its conjugate, a preparation containing it and its medical use |
| AR110299A1 (es) | 2016-12-02 | 2019-03-13 | Sanofi Sa | Conjugados que comprenden un agonista dual de glp-1 / glucagón, un conector y ácido hialurónico |
| CN108261391B (zh) * | 2016-12-30 | 2022-03-01 | 江苏太平洋美诺克生物药业有限公司 | 稳定的包含cd147单克隆抗体的药物制剂 |
| CN108261544B (zh) * | 2016-12-30 | 2023-05-05 | 江苏太平洋美诺克生物药业股份有限公司 | 稳定的包含cd147单克隆抗体的药物制剂 |
| RS65380B1 (sr) | 2017-08-24 | 2024-04-30 | Novo Nordisk As | Glp-1 kompozicije i njihova upotreba |
| KR20210109552A (ko) | 2018-12-21 | 2021-09-06 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 이중특이적 단백질 |
| CN113396156A (zh) * | 2019-02-05 | 2021-09-14 | 伊莱利利公司 | 胰高血糖素类似物激动剂及其使用方法 |
| JP7425855B2 (ja) * | 2019-08-13 | 2024-01-31 | エニジェン カンパニー．，リミテッド． | エキセナチド類似体及びその用途 |
| US20230093542A1 (en) | 2020-02-18 | 2023-03-23 | Novo Nordisk A/S | Glp-1 compositions and uses thereof |
| CN114075275A (zh) * | 2020-08-17 | 2022-02-22 | 成都奥达生物科技有限公司 | 一种长效胰岛素类似物 |
| JP2023554693A (ja) | 2021-01-20 | 2023-12-28 | バイキング・セラピューティクス・インコーポレイテッド | 代謝及び肝臓障害の処置のための組成物及び方法 |
| CN118234743A (zh) * | 2021-11-19 | 2024-06-21 | 深圳市康哲生物科技有限公司 | 含订合钉的多肽及其应用 |
Family Cites Families (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL93173A0 (en) * | 1989-02-01 | 1990-11-05 | Shionogi & Co | Production of glucagon |
| US5408037A (en) * | 1991-01-17 | 1995-04-18 | Zymogenetics, Inc. | Methods for detecting glucagon antagonists |
| US5424286A (en) | 1993-05-24 | 1995-06-13 | Eng; John | Exendin-3 and exendin-4 polypeptides, and pharmaceutical compositions comprising same |
| US5869602A (en) | 1995-03-17 | 1999-02-09 | Novo Nordisk A/S | Peptide derivatives |
| JP3043430B2 (ja) | 1995-09-08 | 2000-05-22 | ノボ ノルディスク アクティーゼルスカブ | ２−アルキルピロリジン類 |
| CZ220498A3 (cs) | 1996-01-17 | 1998-11-11 | Novo Nordisk A/S | Deriváty 1,2,4-thiadiazinu a 1,4-thiazinu, příprava a použití |
| WO1997041120A1 (en) | 1996-07-26 | 1997-11-06 | Dr. Reddy's Research Foundation | Thiazolidinedione compounds having antidiabetic, hypolipidaemic, antihypertensive properties, process for their preparation and pharmaceutical compositions thereof |
| PT944648E (pt) | 1996-08-30 | 2007-06-26 | Novo Nordisk As | Derivados do glp-1. |
| IL127296A (en) | 1996-12-31 | 2003-01-12 | Reddy Research Foundation | Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them |
| WO1997041119A1 (en) | 1997-05-02 | 1997-11-06 | Dr. Reddy's Research Foundation | Novel antidiabetic compounds having hypolipidaemic, antihypertensive properties, process for their preparation and pharmaceutical compositions containing them |
| BR9810378A (pt) | 1997-07-01 | 2000-08-29 | Novo Nordisk As | Composto,uso do mesmo, composição farmacêutica, e, processos de tratar a diabete do tipo i ou do tipo ii, de tratar a hiperglicemia, e de diminuir a glicose do sangue em um mamìfero |
| US6613942B1 (en) | 1997-07-01 | 2003-09-02 | Novo Nordisk A/S | Glucagon antagonists/inverse agonists |
| RU2215004C2 (ru) | 1997-07-16 | 2003-10-27 | Ново Нордиск А/С | Конденсированное производное 1,2,4-тиадиазина, фармацевтическая композиция и способ получения лекарственного препарата |
| WO1999019313A1 (en) | 1997-10-27 | 1999-04-22 | Dr. Reddy's Research Foundation | Novel tricyclic compounds and their use in medicine; process for their preparation and pharmaceutical compositions containing them |
| US6440961B1 (en) | 1997-10-27 | 2002-08-27 | Dr. Reddy's Research Foundation | Tricyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them |
| EP0971917B1 (en) | 1997-12-02 | 2002-02-06 | Dr. Reddy's Research Foundation | Thiazolidinedione and oxazolidinedione derivatives having antidiabetic, hypolipidaemic and antihypertensive properties |
| EP1123292A1 (en) | 1998-10-21 | 2001-08-16 | Novo Nordisk A/S | New compounds, their preparation and use |
| AU6325699A (en) | 1998-10-21 | 2000-05-08 | Dr. Reddy's Research Foundation | New compounds, their preparation and use |
| WO2000023417A1 (en) | 1998-10-21 | 2000-04-27 | Novo Nordisk A/S | New compounds, their preparation and use |
| AU6190199A (en) | 1998-10-21 | 2000-05-08 | Dr. Reddy's Research Foundation | New compounds, their preparation and use |
| WO2000023425A1 (en) | 1998-10-21 | 2000-04-27 | Novo Nordisk A/S | New compounds, their preparation and use |
| JP2002527520A (ja) | 1998-10-21 | 2002-08-27 | ノボ ノルディスク アクティーゼルスカブ | 新規化合物、その製造及び使用 |
| PL348237A1 (en) | 1998-12-18 | 2002-05-20 | Novo Nordisk As | Fused 1,2,4-thiadiazine derivatives, their preparation and use |
| WO2000041121A1 (en) | 1999-01-07 | 2000-07-13 | Ccrewards.Com | Method and arrangement for issuance and management of digital coupons and sales offers |
| EP1147094A1 (en) | 1999-01-15 | 2001-10-24 | Novo Nordisk A/S | Non-peptide glp-1 agonists |
| JP2002534511A (ja) | 1999-01-18 | 2002-10-15 | ノボ ノルディスク アクティーゼルスカブ | 置換型イミダゾール、それらの調製及び使用 |
| AU3957800A (en) | 1999-04-16 | 2000-11-02 | Dr. Reddy's Research Foundation | Crystalline r- guanidines, arginine or (l) -arginine (2(s)) -2- ethoxy -3-(4- (2-(10(h) -phenoxazin -10-yl)ethoxy}phenyl)propanoate |
| WO2000063191A1 (en) | 1999-04-16 | 2000-10-26 | Dr. Reddy's Research Foundation | Novel polymorphic forms of an antidiabetic agent: process for their preparation and a pharmaceutical composition containing them |
| TR200103851T2 (tr) | 1999-04-16 | 2002-04-22 | Dr. Reddy' S Research Foundation | Bir antidiyabetik maddenin yeni polimorfik formları, bunların hazırlanması için işlem ve bunları farmasötik bileşimler |
| JP2002542245A (ja) | 1999-04-16 | 2002-12-10 | ノボ ノルディスク アクティーゼルスカブ | 置換イミダゾール、それらの製造および使用 |
| CZ20013558A3 (cs) | 1999-04-20 | 2002-05-15 | Novo Nordisk A/S | Sloučenina, farmaceutický prostředek, způsob léčby, jejich příprava a vyuľití |
| JP2002542237A (ja) | 1999-04-20 | 2002-12-10 | ノボ ノルディスク アクティーゼルスカブ | 新規な化合物、それらの製造及び使用 |
| AU3958200A (en) | 1999-04-20 | 2000-11-02 | Novo Nordisk A/S | New compounds, their preparation and use |
| EP1171438A1 (en) | 1999-04-20 | 2002-01-16 | Novo Nordisk A/S | Compounds, their preparation and use |
| AU3957600A (en) | 1999-04-26 | 2000-11-10 | Boehringer Ingelheim International Gmbh | Piperidyl-imidazole derivatives, their preparations and therapeutic uses |
| CA2505617A1 (en) * | 1999-05-17 | 2000-11-23 | Conjuchem Inc. | Modified secretin and method of synthesizing thereof |
| WO2000069911A1 (en) * | 1999-05-17 | 2000-11-23 | Conjuchem, Inc. | Long lasting insulinotropic peptides |
| KR100556323B1 (ko) | 2000-07-20 | 2006-03-03 | 에프. 호프만-라 로슈 아게 | 알파-아실 및 알파-헤테로원자-치환된 벤젠 아세트아미드글루코키나제 활성화제 |
| US6953787B2 (en) | 2002-04-12 | 2005-10-11 | Arena Pharmaceuticals, Inc. | 5HT2C receptor modulators |
| US7314859B2 (en) | 2002-12-27 | 2008-01-01 | Diobex, Inc. | Compositions and methods for the prevention and control of insulin-induced hypoglycemia |
| BRPI0414539B8 (pt) * | 2003-09-19 | 2021-05-25 | Novo Nordisk As | composto, composição farmacêutica, e, uso de um composto |
| CN101380476A (zh) * | 2003-09-19 | 2009-03-11 | 诺沃挪第克公司 | 治疗肽的清蛋白结合型衍生物 |
| TWI372629B (en) | 2005-03-18 | 2012-09-21 | Novo Nordisk As | Acylated glp-1 compounds |
| CA2913805A1 (en) * | 2005-11-07 | 2007-05-18 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| TWI428346B (zh) * | 2006-12-13 | 2014-03-01 | Imp Innovations Ltd | 新穎化合物及其等對進食行為影響 |
| WO2008086086A2 (en) | 2007-01-05 | 2008-07-17 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting enhanced solubility in physiological ph buffers |
| WO2008101017A2 (en) | 2007-02-15 | 2008-08-21 | Indiana Unversity Research And Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| WO2008152403A1 (en) | 2007-06-15 | 2008-12-18 | Zealand Pharma A/S | Glucagon analogues |
| US8895694B2 (en) * | 2007-09-05 | 2014-11-25 | Novo Nordisk A/S | Glucagon-Like Peptide-1 derivatives and their pharmaceutical use |
| WO2009030771A1 (en) | 2007-09-05 | 2009-03-12 | Novo Nordisk A/S | Peptides derivatized with a-b-c-d- and their therapeutical use |
| US20100317057A1 (en) * | 2007-12-28 | 2010-12-16 | Novo Nordisk A/S | Semi-recombinant preparation of glp-1 analogues |
| KR101074010B1 (ko) * | 2009-09-04 | 2011-10-17 | (주)이스트소프트 | 블록 단위 데이터 압축 및 복원 방법 및 그 장치 |
-
2011
- 2011-03-28 CN CN201180025883.6A patent/CN102918056B/zh not_active Expired - Fee Related
- 2011-03-28 KR KR1020127027952A patent/KR20130018410A/ko active Search and Examination
- 2011-03-28 RU RU2012144289/04A patent/RU2559320C2/ru not_active IP Right Cessation
- 2011-03-28 AU AU2011231503A patent/AU2011231503C1/en not_active Ceased
- 2011-03-28 WO PCT/EP2011/054714 patent/WO2011117416A1/en active Application Filing
- 2011-03-28 BR BR112012024379A patent/BR112012024379A2/pt not_active Application Discontinuation
- 2011-03-28 WO PCT/EP2011/054712 patent/WO2011117415A1/en active Application Filing
- 2011-03-28 EP EP11710504A patent/EP2552951A1/en not_active Withdrawn
- 2011-03-28 EP EP11710218A patent/EP2552950A1/en not_active Withdrawn
- 2011-03-28 CA CA2792663A patent/CA2792663A1/en not_active Withdrawn
- 2011-03-28 US US13/637,522 patent/US20130143798A1/en not_active Abandoned
- 2011-03-28 MX MX2012010881A patent/MX336412B/es unknown
- 2011-03-28 US US13/637,454 patent/US20130035285A1/en not_active Abandoned
- 2011-03-28 JP JP2013500534A patent/JP6054861B2/ja not_active Expired - Fee Related
- 2011-03-28 JP JP2013500535A patent/JP6026993B2/ja not_active Expired - Fee Related
- 2011-03-28 CN CN201180025875.1A patent/CN102918055B/zh not_active Expired - Fee Related
-
2012
- 2012-09-12 ZA ZA2012/06838A patent/ZA201206838B/en unknown
-
2015
- 2015-06-15 US US14/739,614 patent/US20150274801A1/en not_active Abandoned
- 2015-08-17 US US14/827,539 patent/US20160002311A1/en not_active Abandoned
-
2016
- 2016-05-16 US US15/155,541 patent/US20160271263A1/en not_active Abandoned
- 2016-07-19 JP JP2016141243A patent/JP2016183192A/ja not_active Withdrawn
- 2016-09-12 US US15/262,450 patent/US20170051034A1/en not_active Abandoned
-
2017
- 2017-03-13 US US15/456,912 patent/US20170190757A1/en not_active Abandoned
- 2017-07-26 US US15/660,458 patent/US20180016319A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013523619A5 (ja) | ||
| JP2013523618A5 (ja) | ||
| JP2014527975A5 (ja) | ||
| RU2012144289A (ru) | Новые аналоги глюкагона | |
| RU2014114434A (ru) | Новые аналоги глюкагона | |
| JP2014510739A5 (ja) | ||
| CA2786934A1 (en) | Treatment of cardiac conditions | |
| AU2011247824B2 (en) | Glucagon-like peptide-1 analogue and use thereof | |
| RU2006144821A (ru) | Пролонгирующие метки полипептидов, содержащие тетразольную группировку | |
| JP2014504597A (ja) | アシル化グルカゴン類似体とインスリン類似体の組合せ物 | |
| EP2773377B1 (en) | Glp-1 receptor agonist peptide gastrin conjugates | |
| CN105745222A (zh) | 酰化胰高血糖素类似物 | |
| CA2747197A1 (en) | Glucagon analogues | |
| KR20150116912A (ko) | 글루카곤 유사체 | |
| MX2014013319A (es) | Análogos de péptido-2 tipo glucagón (glp-2). | |
| JP2012532898A (ja) | アシル化グルカゴン類似体 | |
| CN111132690A (zh) | 胰高血糖素和glp-1受体的长效共激动剂 | |
| CN115490760B (zh) | 一种glp-1受体和gcg受体共激动多肽衍生物 | |
| KR20230008846A (ko) | 이중 수용체 아고니즘 작용을 갖는 폴리펩티드 유도체 및 그 용도 | |
| CA3222051A1 (en) | Polypeptide derivative having effect of dual targeted activation of glp-1r and gipr, preparation method therefor, and use thereof | |
| JP7350851B2 (ja) | グルカゴン由来ペプチド及びその用途 | |
| JP2015517458A5 (ja) | ||
| JPWO2020115048A5 (ja) | ||
| JP2014500244A5 (ja) | ||
| KR20230125802A (ko) | 신규 화합물 |