CO6321274A2 - Compuestos de pirazol acetamida n-sustituida como activadores de glucoquinasa - Google Patents
Compuestos de pirazol acetamida n-sustituida como activadores de glucoquinasaInfo
- Publication number
- CO6321274A2 CO6321274A2 CO10154094A CO10154094A CO6321274A2 CO 6321274 A2 CO6321274 A2 CO 6321274A2 CO 10154094 A CO10154094 A CO 10154094A CO 10154094 A CO10154094 A CO 10154094A CO 6321274 A2 CO6321274 A2 CO 6321274A2
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- heterocycloalkyl
- carbonyl
- hydrogen
- group
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Reproductive Health (AREA)
- Child & Adolescent Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
1.- Un compuesto que tiene la fórmula: o un polimorfo, solvato, éster, lautómero, enantiómero, sal o prodroga del mismo aceptable para uso farmacéutico, donde R1 se selecciona del grupo integrado por heterocicloalquilo (C3-12), heterobicicicloalquilo (C3-12), heteroarilo, y heterobicicloarilo (C4-12), cada uno sustituido o no sustituido; R2 se selecciona del grupo integrado por hidrógeno y un sustituyente que puede convertirse a hidrógeno in vivo; R3 se selecciona del grupo integrado por hidrógeno, carbonilo, sulfonilo, sulfinilo, alquilo (C1-10), haloalquilo (C1-10), carbonilalquilo (C1-3), tiocarbonilalquilo (C1-3), sulfonilalquilo (C1-3), sulfinilalquilo (C1-3), aminoalquilo (C1-10), iminoalquilo (C1-3), cicloalquilo (C3-12)-alquilo (C1-5), heterocicloalquilo (C3-12)-alquilo (C1-5), arilalquilo (C1-10), heteroarilalquilo (C1-5), bicicloarilo (C9-12)-alquilo (C1-5), heterobicicloarilo (C8-12)-alquilo (C1-5), cicloalquilo (C3-12), heterocicloalquilo (C3-12), bicicloalquilo (C9-12), heterobicicicloalquilo (C3-12), arilo, heteroarilo, bicicloarilo (C9-12) y heterobicicloarilo (C4-12), cada uno sustituido o no sustituido, o R3 es -L-R18; R4 se selecciona del grupo integrado por hidrógeno, carbonilo, sulfonilo, sulfinilo, alquilo (C1-10), haloalquilo (C1-10), carbonilalquilo (C1-3), tiocarbonilalquilo (C1-3), sulfonilalquilo (C1-3), sulfinilalquilo (C1-3), aminoalquilo (C1-10), iminoalquilo (C1-3), cicloalquilo (C3-12)-alquilo (C1-5), heterocicloalquilo (C3-12)-alquilo (C1-5), arilalquilo (C1-10), heteroarilalquilo (C1-5), bicicloarilo (C9-12)-alquilo (C1-5), helerobicicloarilo (C8-12)-alquilo (C1-5), cicloalquilo (C3-12), heterocicloalquilo (C3-12), bicicloalquilo (C9-12), heterobicicicloalquilo (C3-12), arilo, heteroarilo, bicicloarilo (C9-12) y heterobicicloarilo (C4-12), cada uno sustituido o no sustituido, o R3 y R4 se toman juntos para formar un anillo sustituido o no sustituido; R5 se selecciona del grupo integrado por hidrógeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi (C1-10), ariloxi (C4-12), heteroariloxi (C1-10), carbonilo, oxicarbonilo, amido, amino, alquilamino (C1-10), sulfonamido, imino, sulfonilo, sulfinilo, ...
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US5405208P | 2008-05-16 | 2008-05-16 | |
US10837008P | 2008-10-24 | 2008-10-24 |
Publications (1)
Publication Number | Publication Date |
---|---|
CO6321274A2 true CO6321274A2 (es) | 2011-09-20 |
Family
ID=41076813
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CO10154094A CO6321274A2 (es) | 2008-05-16 | 2010-12-07 | Compuestos de pirazol acetamida n-sustituida como activadores de glucoquinasa |
Country Status (27)
Country | Link |
---|---|
US (4) | US8563730B2 (es) |
EP (1) | EP2294053B1 (es) |
JP (1) | JP5513492B2 (es) |
KR (1) | KR20110018366A (es) |
CN (1) | CN102105451B (es) |
AR (1) | AR071811A1 (es) |
AU (1) | AU2009246167B2 (es) |
BR (1) | BRPI0912802A2 (es) |
CA (1) | CA2724116A1 (es) |
CL (1) | CL2009001203A1 (es) |
CO (1) | CO6321274A2 (es) |
CR (1) | CR11827A (es) |
DO (1) | DOP2010000351A (es) |
EA (1) | EA018988B1 (es) |
EC (1) | ECSP10010688A (es) |
GE (1) | GEP20135783B (es) |
IL (1) | IL209062A (es) |
MA (1) | MA32391B1 (es) |
MX (1) | MX2010012298A (es) |
MY (1) | MY152749A (es) |
NZ (1) | NZ589084A (es) |
PE (2) | PE20091901A1 (es) |
SG (1) | SG190625A1 (es) |
TW (1) | TWI445707B (es) |
UY (1) | UY31830A (es) |
WO (1) | WO2009140624A2 (es) |
ZA (1) | ZA201007975B (es) |
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AU2008292238B2 (en) * | 2007-08-27 | 2014-06-12 | Basf Se | Pyrazole compounds for controlling invertebrate pests |
JP2011510986A (ja) * | 2008-02-05 | 2011-04-07 | メルク・シャープ・エンド・ドーム・コーポレイション | メトホルミン及びジペプチジルペプチダーゼ−iv阻害剤の併用医薬組成物 |
CN102105451B (zh) | 2008-05-16 | 2013-11-13 | 塔克达加利福尼亚股份有限公司 | 葡糖激酶活化剂 |
MY152008A (en) | 2008-08-27 | 2014-08-15 | Takeda Pharmaceutical | Pyrrole compounds |
CA2735184C (en) * | 2008-09-11 | 2013-05-28 | Pfizer Inc. | Heteroaryls amide derivatives and their use as glucokinase activators |
CN102224149B (zh) | 2008-09-24 | 2014-09-10 | 巴斯夫欧洲公司 | 防治无脊椎动物害虫的吡唑化合物 |
EP2451804B1 (en) | 2009-07-06 | 2014-04-30 | Basf Se | Pyridazine compounds for controlling invertebrate pests |
ES2461618T3 (es) | 2009-07-06 | 2014-05-20 | Basf Se | Compuestos de piridacina para el control de plagas de invertebrados |
CN102469785A (zh) | 2009-07-24 | 2012-05-23 | 巴斯夫欧洲公司 | 防治无脊椎动物害虫的吡啶衍生物 |
WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
AU2011235212B2 (en) | 2010-03-31 | 2014-07-31 | The Scripps Research Institute | Reprogramming cells |
JP5902676B2 (ja) | 2010-05-26 | 2016-04-13 | ブイティーブイ セラピューティクス リミティド ライアビリティ カンパニー | グルコキナーゼ活性化因子と組み合わせたメトホルミンの使用、及びメトホルミン及びグルコキナーゼ活性化因子を含む組成物 |
US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
US20130197229A1 (en) * | 2010-10-13 | 2013-08-01 | Christopher Matthews | Method of making azaindazole derivatives |
WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
JP6234443B2 (ja) | 2012-05-17 | 2017-11-22 | ブイティーブイ・セラピューティクス・エルエルシー | 糖尿病治療のためのグルコキナーゼ活性化因子組成物 |
CN105050585A (zh) * | 2013-03-04 | 2015-11-11 | Vtv治疗有限责任公司 | 稳定的葡萄糖激酶活化剂组合物 |
EP2878339A1 (en) | 2013-12-02 | 2015-06-03 | Siena Biotech S.p.A. | SIP3 antagonists |
TWI667233B (zh) | 2013-12-19 | 2019-08-01 | 德商拜耳製藥公司 | 新穎吲唑羧醯胺,其製備方法、含彼等之醫藥製劑及其製造醫藥之用途 |
EA201791390A1 (ru) * | 2014-12-19 | 2017-10-31 | Арагон Фармасьютикалз, Инк. | Способ получения соединения диарилтиогидантоина |
CN105092770B (zh) * | 2015-01-12 | 2017-03-29 | 上海中医药大学 | 一种筛选二肽基肽酶四抑制剂的方法 |
LT3307707T (lt) | 2015-06-15 | 2021-01-11 | Syngenta Crop Protection Ag | Halogeninti fenoksifenilamidinai ir jų naudojimas kaip fungicidų |
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GB201714777D0 (en) | 2017-09-14 | 2017-11-01 | Univ London Queen Mary | Agent |
CN114246950A (zh) * | 2018-05-31 | 2022-03-29 | 华领医药技术(上海)有限公司 | 含葡萄糖激酶激活剂和α-葡萄糖苷酶抑制剂的药物组合及其制备方法和用途 |
KR20210020866A (ko) | 2018-06-12 | 2021-02-24 | 브이티브이 테라퓨틱스 엘엘씨 | 인슐린 또는 인슐린 유사체와 조합된 글루코키나제 활성제의 치료적 용도 |
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