PE20231948A1 - Compuestos aromaticos que contienen boro y analogos de insulina - Google Patents
Compuestos aromaticos que contienen boro y analogos de insulinaInfo
- Publication number
- PE20231948A1 PE20231948A1 PE2023001666A PE2023001666A PE20231948A1 PE 20231948 A1 PE20231948 A1 PE 20231948A1 PE 2023001666 A PE2023001666 A PE 2023001666A PE 2023001666 A PE2023001666 A PE 2023001666A PE 20231948 A1 PE20231948 A1 PE 20231948A1
- Authority
- PE
- Peru
- Prior art keywords
- amine
- covalently conjugated
- diabetes
- compound
- compounds containing
- Prior art date
Links
- 150000001491 aromatic compounds Chemical class 0.000 title 1
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical class 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 title 1
- 150000001412 amines Chemical class 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000008186 active pharmaceutical agent Substances 0.000 abstract 2
- 229940088679 drug related substance Drugs 0.000 abstract 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 2
- MJUVRTYWUMPBTR-MRXNPFEDSA-N 1-(2,2-difluoro-1,3-benzodioxol-5-yl)-n-[1-[(2r)-2,3-dihydroxypropyl]-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)indol-5-yl]cyclopropane-1-carboxamide Chemical compound FC=1C=C2N(C[C@@H](O)CO)C(C(C)(CO)C)=CC2=CC=1NC(=O)C1(C=2C=C3OC(F)(F)OC3=CC=2)CC1 MJUVRTYWUMPBTR-MRXNPFEDSA-N 0.000 abstract 1
- ZOXJGFHDIHLPTG-UHFFFAOYSA-N Boron Chemical compound [B] ZOXJGFHDIHLPTG-UHFFFAOYSA-N 0.000 abstract 1
- 208000002705 Glucose Intolerance Diseases 0.000 abstract 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 abstract 1
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract 1
- 208000019022 Mood disease Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 abstract 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 229910052796 boron Inorganic materials 0.000 abstract 1
- 201000001421 hyperglycemia Diseases 0.000 abstract 1
- PBGKTOXHQIOBKM-FHFVDXKLSA-N insulin (human) Chemical class C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3C=CC(O)=CC=3)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3NC=NC=3)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(=O)N[C@@H](CC(N)=O)C(O)=O)=O)CSSC[C@@H](C(N2)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C=CC=CC=1)C(C)C)C1=CN=CN1 PBGKTOXHQIOBKM-FHFVDXKLSA-N 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
-
- 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
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- 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
- C07K14/62—Insulins
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Diabetes (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Toxicology (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
Abstract
La presente invencion se refiere a un compuesto que comprende X1 y uno o mas Z1c, un tautomero, estereoisomero o una mezcla de estereoisomeros, o una sal o hidrato aceptable desde el punto de vista farmaceutico, en donde: X1 comprende: i. NH2 u OH; ii. Una sustancia farmacologica que comprende una amina; iii) una sustancia farmacologica conjugada de manera covalente con un ligador que contiene amina; o iv) una amina configurada para conjugarse de manera covalente con una sustancia farmacologica, en donde cada Z1c se selecciona de las formulas FFF1 a FF224; en donde cada Z1c se conjuga de manera covalente con una amina en X1 o con OH cuando X1 es OH, donde cada B1 a B6 son independientemente un grupo aromatico que contiene boro y X represente un punto de union covalente a una amina en X1 o con OH cuando X1 es OH. Tambien se refiere a un analogo de insulina humana y a composiciones farmaceuticas. Son compuestos especificos los compuestos ejemplo 315, 318, entre otros. Dicho compuesto es util en la prevencion y tratamiento de la hiperglucemia, diabetes tipo 2, intolerancia a la glucosa, diabetes tipo 1, obesidad, sindrome metabolico X o dislipidemia, diabetes durante el embarazo, prediabetes, enfermedad de Alzheimer, diabetes MODY 1, MODY 2 o MODY 3, trastornos del estado de animo y trastornos psiquiatricos.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063116050P | 2020-11-19 | 2020-11-19 | |
| US202063122338P | 2020-12-07 | 2020-12-07 | |
| US202163210968P | 2021-06-15 | 2021-06-15 | |
| US202163249868P | 2021-09-29 | 2021-09-29 | |
| PCT/US2021/059802 WO2022109078A1 (en) | 2020-11-19 | 2021-11-18 | Aromatic boron-containing compounds and insulin analogs |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20231948A1 true PE20231948A1 (es) | 2023-12-05 |
Family
ID=79024395
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023001666A PE20231948A1 (es) | 2020-11-19 | 2021-11-18 | Compuestos aromaticos que contienen boro y analogos de insulina |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP4247429A1 (es) |
| JP (1) | JP2024500284A (es) |
| KR (1) | KR20230110505A (es) |
| AU (1) | AU2021382599A1 (es) |
| CA (1) | CA3198757A1 (es) |
| CO (1) | CO2023006369A2 (es) |
| DO (1) | DOP2023000097A (es) |
| EC (1) | ECSP23036608A (es) |
| IL (1) | IL302775A (es) |
| MX (1) | MX2023005935A (es) |
| PE (1) | PE20231948A1 (es) |
| TW (1) | TW202237188A (es) |
| WO (1) | WO2022109078A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202409070A (zh) * | 2022-05-18 | 2024-03-01 | 美商普羅托莫科技公司 | 芳族含硼化合物及相關胰島素類似物 |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US906028A (en) | 1908-03-27 | 1908-12-08 | Herbert E Jennison | Adjustable foot-block for radiators. |
| US4421685A (en) | 1980-03-27 | 1983-12-20 | Eli Lilly And Company | Process for producing an insulin |
| NZ273285A (en) | 1993-09-17 | 1997-10-24 | Novo Nordisk As | Insulin derivatives and compositions thereof |
| US6011007A (en) | 1993-09-17 | 2000-01-04 | Novo Nordisk A/S | Acylated insulin |
| US6869930B1 (en) | 1993-09-17 | 2005-03-22 | Novo Nordisk A/S | Acylated insulin |
| US5474978A (en) | 1994-06-16 | 1995-12-12 | Eli Lilly And Company | Insulin analog formulations |
| US5461031A (en) | 1994-06-16 | 1995-10-24 | Eli Lilly And Company | Monomeric insulin analog formulations |
| US5504188A (en) | 1994-06-16 | 1996-04-02 | Eli Lilly And Company | Preparation of stable zinc insulin analog crystals |
| US5547929A (en) | 1994-09-12 | 1996-08-20 | Eli Lilly And Company | Insulin analog formulations |
| US5693609A (en) | 1994-11-17 | 1997-12-02 | Eli Lilly And Company | Acylated insulin analogs |
| YU18596A (sh) | 1995-03-31 | 1998-07-10 | Eli Lilly And Company | Analogne formulacije monomernog insulina |
| US5866538A (en) | 1996-06-20 | 1999-02-02 | Novo Nordisk A/S | Insulin preparations containing NaCl |
| ZA984697B (en) | 1997-06-13 | 1999-12-01 | Lilly Co Eli | Stable insulin formulations. |
| CA2306905A1 (en) | 1997-10-24 | 1999-05-06 | Eli Lilly And Company | Fatty acid-acylated insulin analogs |
| US6444641B1 (en) | 1997-10-24 | 2002-09-03 | Eli Lilly Company | Fatty acid-acylated insulin analogs |
| ZA989744B (en) | 1997-10-31 | 2000-04-26 | Lilly Co Eli | Method for administering acylated insulin. |
| ATE290877T1 (de) | 1998-01-09 | 2005-04-15 | Novo Nordisk As | Stabilisierte insulin-zubereitungen |
| US6586207B2 (en) | 2000-05-26 | 2003-07-01 | California Institute Of Technology | Overexpression of aminoacyl-tRNA synthetases for efficient production of engineered proteins containing amino acid analogues |
| AU2002349295A1 (en) * | 2001-12-02 | 2003-06-17 | Novo Nordisk A/S | Glucose dependant release of insulin from glucose sensing insulin derivatives |
| WO2003073238A2 (en) | 2002-02-27 | 2003-09-04 | California Institute Of Technology | Computational method for designing enzymes for incorporation of amino acid analogs into proteins |
| AU2003236201A1 (en) | 2002-05-07 | 2003-11-11 | Novo Nordisk A/S | Soluble formulations comprising monomeric insulin and acylated insulin |
| AU2005208748A1 (en) | 2004-01-23 | 2005-08-11 | California Institute Of Technology | Engineered proteins, and methods of making and using |
| AU2005211385B2 (en) | 2004-02-02 | 2008-12-11 | Ambrx, Inc. | Modified human growth hormone polypeptides and their uses |
| US7816320B2 (en) | 2004-12-22 | 2010-10-19 | Ambrx, Inc. | Formulations of human growth hormone comprising a non-naturally encoded amino acid at position 35 |
| BRPI0519568C8 (pt) | 2004-12-22 | 2022-06-14 | Ambrx Inc | Aminoacil-trna sintetase (rs), composições que compreendem a dita aminoacil-trna sintetase, célula de levedura, célula fúngica, célula não eucariótica, vetor que codifica uma rs, polinucleotídeo e ainda método para produzir um polipeptídeo em uma célula com um aminoácido selecionado em uma posição especificada |
| US20100247433A1 (en) | 2005-10-14 | 2010-09-30 | California Institute Of Technology | Use of non-canonical amino acids as metabolic markers for rapidly-dividing cells |
| PT1999259E (pt) | 2006-03-03 | 2014-09-24 | California Inst Of Techn | Incorporação sítio-específica de aminoácidos em moléculas |
| WO2007130453A2 (en) | 2006-05-02 | 2007-11-15 | Allozyne, Inc. | Non-natural amino acid substituted polypeptides |
| US20080096819A1 (en) | 2006-05-02 | 2008-04-24 | Allozyne, Inc. | Amino acid substituted molecules |
| JP5552046B2 (ja) | 2007-06-13 | 2014-07-16 | ノボ・ノルデイスク・エー／エス | インスリン誘導体を含有する薬学的製剤 |
| CN101918026B (zh) | 2007-11-20 | 2016-03-02 | Ambrx公司 | 经修饰胰岛素多肽和其用途 |
| US9996862B2 (en) | 2012-07-23 | 2018-06-12 | @Pay Ip Holdings Llc | Point of sale email-based e-commerce |
| WO2014093696A2 (en) * | 2012-12-12 | 2014-06-19 | Massachusetts Institute Of Technology | Insulin derivatives for diabetes treatment |
| JP2017522282A (ja) | 2014-06-10 | 2017-08-10 | カリフォルニア インスティチュート オブ テクノロジー | 非標準的インスリンおよびそれらの使用 |
| WO2017070617A1 (en) * | 2015-10-21 | 2017-04-27 | Case Western Reserve University | Diol-modified insulin analogues containing a glucose-regulated conformational switch |
| US11186595B2 (en) * | 2017-11-09 | 2021-11-30 | Novo Nordisk A/S | Glucose-sensitive albumin-binding derivatives |
| AU2019255611A1 (en) * | 2018-04-16 | 2020-11-12 | University Of Utah Research Foundation | Glucose-responsive insulin |
| CN113646329A (zh) * | 2019-03-29 | 2021-11-12 | 诺和诺德股份有限公司 | 葡萄糖敏感性胰岛素衍生物 |
| WO2021022116A1 (en) * | 2019-07-31 | 2021-02-04 | Thermalin Inc. | Insulin analogues with glucose regulated conformational switch |
| CR20220555A (es) * | 2020-03-31 | 2023-01-23 | Protomer Tech Inc | Conjugados para reactividad selectiva a dioles vecinales |
-
2021
- 2021-11-18 PE PE2023001666A patent/PE20231948A1/es unknown
- 2021-11-18 KR KR1020237015641A patent/KR20230110505A/ko unknown
- 2021-11-18 MX MX2023005935A patent/MX2023005935A/es unknown
- 2021-11-18 CA CA3198757A patent/CA3198757A1/en active Pending
- 2021-11-18 JP JP2023530242A patent/JP2024500284A/ja active Pending
- 2021-11-18 EP EP21827270.6A patent/EP4247429A1/en active Pending
- 2021-11-18 AU AU2021382599A patent/AU2021382599A1/en active Pending
- 2021-11-18 IL IL302775A patent/IL302775A/en unknown
- 2021-11-18 WO PCT/US2021/059802 patent/WO2022109078A1/en active Application Filing
- 2021-11-18 TW TW110143044A patent/TW202237188A/zh unknown
-
2023
- 2023-05-16 CO CONC2023/0006369A patent/CO2023006369A2/es unknown
- 2023-05-17 DO DO2023000097A patent/DOP2023000097A/es unknown
- 2023-05-18 EC ECSENADI202336608A patent/ECSP23036608A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3198757A1 (en) | 2022-05-27 |
| CO2023006369A2 (es) | 2023-05-19 |
| EP4247429A1 (en) | 2023-09-27 |
| JP2024500284A (ja) | 2024-01-09 |
| WO2022109078A1 (en) | 2022-05-27 |
| AU2021382599A1 (en) | 2023-06-22 |
| DOP2023000097A (es) | 2023-09-29 |
| MX2023005935A (es) | 2023-05-29 |
| TW202237188A (zh) | 2022-10-01 |
| KR20230110505A (ko) | 2023-07-24 |
| IL302775A (en) | 2023-07-01 |
| ECSP23036608A (es) | 2023-06-30 |
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