AR080444A1 - Metodos para la utilizacion de cotransportadores de sodio-glucosa 1 y 2 - Google Patents
Metodos para la utilizacion de cotransportadores de sodio-glucosa 1 y 2Info
- Publication number
- AR080444A1 AR080444A1 ARP110100644A ARP110100644A AR080444A1 AR 080444 A1 AR080444 A1 AR 080444A1 AR P110100644 A ARP110100644 A AR P110100644A AR P110100644 A ARP110100644 A AR P110100644A AR 080444 A1 AR080444 A1 AR 080444A1
- Authority
- AR
- Argentina
- Prior art keywords
- heterocycle
- aryl
- alkyl
- agent
- inhibitor
- Prior art date
Links
- 102000000070 Sodium-Glucose Transport Proteins Human genes 0.000 title 1
- 108010080361 Sodium-Glucose Transport Proteins Proteins 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 108091006277 SLC5A1 Proteins 0.000 abstract 5
- 102000058090 Sodium-Glucose Transporter 1 Human genes 0.000 abstract 5
- 230000009977 dual effect Effects 0.000 abstract 5
- 239000003112 inhibitor Substances 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 239000003472 antidiabetic agent Substances 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 230000036996 cardiovascular health Effects 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 230000010034 metabolic health Effects 0.000 abstract 2
- 229940124597 therapeutic agent Drugs 0.000 abstract 2
- QKDRXGFQVGOQKS-CRSSMBPESA-N (2s,3r,4r,5s,6r)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-methylsulfanyloxane-3,4,5-triol Chemical group C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](SC)O2)O)=CC=C1Cl QKDRXGFQVGOQKS-CRSSMBPESA-N 0.000 abstract 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 239000000883 anti-obesity agent Substances 0.000 abstract 1
- 229940125708 antidiabetic agent Drugs 0.000 abstract 1
- 239000002220 antihypertensive agent Substances 0.000 abstract 1
- 229940030600 antihypertensive agent Drugs 0.000 abstract 1
- 229940125710 antiobesity agent Drugs 0.000 abstract 1
- 239000002830 appetite depressant Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000007423 decrease Effects 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 230000000055 hyoplipidemic effect Effects 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
-
- 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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/32—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
- Pyrane Compounds (AREA)
Abstract
Métodos para mejorar la salud cardiovascular y/o metabolica de pacientes, en particular de aquellos que padecen de diabetes de Tipo 2, así como compuestos y composiciones farmacéuticas utiles en los mismos. Reivindicacion 1: Una dosis de 300 mg/día o menor (por ejemplo 250, 200, 150, 100 o 50 mg/día o menor) de un inhibidor dual SGLT1/2 de la formula (1) o una sal farmacéuticamente aceptable del mismo, para ser utilizada en una mejora de la salud cardiovascular o metabolica de un paciente diabético o pre-diabético, en donde cada R1A es, de manera independiente, hidrogeno, alquilo, arilo o heterociclo; cada R6 es, de manera independiente, hidrogeno, hidroxilo, amino, alquilo, arilo, ciano, halogeno, heteroalquilo, heterociclo, nitro, C:::CR6A, OR6A, SR6A, SOR6A, SO2R6A, C(O)R6A, CO2R6A, CO2H, CON(R6A)(R6A), CONH(R6A), CONH2, NHC(O)R6A, o NHSO2R6A; cada R6A es, de manera independiente, alquilo, arilo o heterociclo; cada R7 es, de manera independiente, hidrogeno, hidroxilo, amino, alquilo, arilo, ciano, halogeno, heteroalquilo, heterociclo, nitro, C:::CR7a, OR7A, SR7A, SOR7A, SO2R7A, C(O)R7A, CO2R7A, CO2H, CON(R7A)(R7A), CONH(R7A), CONH2, NHC(O)R7A o NHSO2R7A; cada R7A es, de manera independiente, alquilo, arilo o heterociclo; m es 1-4; n es 1-3; p es 0-2; y en donde, de manera opcional, cada alquilo, arilo, heteroalquilo o heterociclo esta sustituido con uno o mas de alcoxi, amino, ciano, halo, hidroxilo o nitro. Reivindicacion 8: El uso de la reivindicacion 1, en donde el inhibidor dual de SGLT1/2 es de la formula (2). Reivindicacion 9: El uso de la reivindicacion 8, en donde el inhibidor dual de SGLT1/2 es de la formula (3). Reivindicacion 10: El uso de la reivindicacion 9, en donde el inhibidor dual de SGLT1/2 es de la formula (4). Reivindicacion 13: El uso de la reivindicacion 12, en donde el inhibidor dual de SGLT1/2 es el (2S,3R,4R,5S,6R)-2-(4-cloro-3-(4-etoxibencil)fenilo)-6-(metiltio)tetrahidro-2H-piran-3,4,5-triol. Reivindicacion 14: El uso de la reivindicacion 1, en donde el paciente ha tomado, o está tomando de manera concurrente, un segundo agente terapéutico, en donde dicho segundo agente terapéutico es un agente anti-diabético, un agente anti-hiperglicémico, un agente hipolipidémico/un agente que disminuye los lípidos, agentes anti-obesidad, un agente anti-hipertensivo o un supresor del apetito.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30959210P | 2010-03-02 | 2010-03-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080444A1 true AR080444A1 (es) | 2012-04-11 |
Family
ID=43795398
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100644A AR080444A1 (es) | 2010-03-02 | 2011-03-02 | Metodos para la utilizacion de cotransportadores de sodio-glucosa 1 y 2 |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US20110218159A1 (es) |
| EP (1) | EP2542236B1 (es) |
| JP (2) | JP6126383B2 (es) |
| KR (2) | KR20180051683A (es) |
| CN (1) | CN102821764A (es) |
| AR (1) | AR080444A1 (es) |
| AU (1) | AU2011223861B2 (es) |
| BR (1) | BR112012021771B1 (es) |
| CA (1) | CA2791300C (es) |
| CY (1) | CY1118611T1 (es) |
| DK (1) | DK2542236T3 (es) |
| ES (1) | ES2609104T3 (es) |
| HR (1) | HRP20170093T1 (es) |
| HU (1) | HUE031441T2 (es) |
| IL (1) | IL221372A0 (es) |
| LT (1) | LT2542236T (es) |
| MX (1) | MX342423B (es) |
| PL (1) | PL2542236T3 (es) |
| PT (1) | PT2542236T (es) |
| RS (1) | RS55620B1 (es) |
| RU (1) | RU2012141893A (es) |
| SI (1) | SI2542236T1 (es) |
| TW (1) | TWI562775B (es) |
| WO (1) | WO2011109333A1 (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| BRPI0711558A2 (pt) | 2006-05-04 | 2011-11-08 | Boeringer Ingelheim Internat Gmbh | polimorfos |
| PE20140960A1 (es) | 2008-04-03 | 2014-08-15 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| BRPI0916997A2 (pt) | 2008-08-06 | 2020-12-15 | Boehringer Ingelheim International Gmbh | Inibidor de dpp-4 e seu uso |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| EA034869B1 (ru) | 2009-11-27 | 2020-03-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Лечение генотипированных пациентов с диабетом ингибиторами дпп-4, такими как линаглиптин |
| US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| TWI631963B (zh) * | 2011-01-05 | 2018-08-11 | 雷西肯製藥股份有限公司 | 包含鈉－葡萄糖共同輸送體１與２之抑制劑的組合物與應用方法 |
| US20130303554A1 (en) | 2012-05-14 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Use of a dpp-4 inhibitor in sirs and/or sepsis |
| JP6224084B2 (ja) | 2012-05-14 | 2017-11-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 糸球体上皮細胞関連障害及び／又はネフローゼ症候群の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体 |
| TR201908247T4 (tr) * | 2012-11-20 | 2019-06-21 | Lexicon Pharmaceuticals Inc | Sodyum glikoz birlikte taşıyıcı 1 inhibitörleri. |
| KR102238860B1 (ko) * | 2013-06-14 | 2021-04-12 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 및 이의 합병증의 치료를 위한 dpp-4 억제제 |
| WO2014206349A1 (zh) * | 2013-06-28 | 2014-12-31 | 四川海思科制药有限公司 | 氧杂-硫杂-双环[3.2.1]辛烷衍生物、制备方法及其用途 |
| WO2015183794A1 (en) * | 2014-05-27 | 2015-12-03 | City Of Hope | Tgr5 agonist complexes for treating diabetes and cancer |
| JP6727419B2 (ja) * | 2016-05-25 | 2020-07-22 | クリスタル ファーマシューティカル（スーチョウ）カンパニー，リミテッド | ナトリウム−グルコース共輸送体阻害薬の新規な結晶形及びその製造方法並びに用途 |
| CN109310697A (zh) | 2016-06-10 | 2019-02-05 | 勃林格殷格翰国际有限公司 | 利格列汀和二甲双胍的组合 |
| CN110066302B (zh) | 2018-01-23 | 2022-12-27 | 广东东阳光药业有限公司 | 吡喃葡萄糖基衍生物及其用途 |
| US11186602B2 (en) | 2018-01-31 | 2021-11-30 | Sunshine Lake Pharma Co., Ltd. | Glucopyranosyl derivative and use thereof |
| CN112469407B (zh) * | 2018-03-28 | 2024-10-01 | 阿沃林特有限公司 | 用于治疗餐后低血糖症的方法 |
| CN108610385A (zh) * | 2018-04-23 | 2018-10-02 | 中国科学院成都生物研究所 | 一种钠-葡萄糖协同转运蛋白1抑制剂的药物用途 |
| CN110117300A (zh) * | 2018-04-23 | 2019-08-13 | 中国科学院成都生物研究所 | 包含钠-葡萄糖协同转运蛋白1抑制剂的药物用途 |
| CN110117304A (zh) * | 2018-04-23 | 2019-08-13 | 中国科学院成都生物研究所 | 一种钠-葡萄糖协同转运蛋白1和2抑制剂的药物用途 |
| CN110092768A (zh) * | 2018-04-23 | 2019-08-06 | 中国科学院成都生物研究所 | 包含钠-葡萄糖协同转运蛋白1抑制剂的组合物及使用方法 |
| KR20210065974A (ko) * | 2018-09-26 | 2021-06-04 | 렉시컨 파마슈티컬스 인코퍼레이티드 | N-(1-((2-(디메틸아미노)에틸)아미노)-2-메틸-1-옥소프로판-2-일)-4-(4-(2-메틸-5-((2s,3r,4r,5s,6r)-3,4,5-트리히드록시-6-(메틸티오)테트라히드로-2h-피란-2-일)벤질)페닐)부탄아미드의 결정질 형태 및 그의 합성 방법 |
| CA3145427A1 (en) | 2019-07-10 | 2021-01-14 | Sunshine Lake Pharma Co., Ltd. | Glucopyranosyl derivatives and their uses |
| CN114585387B (zh) * | 2019-09-04 | 2024-10-29 | 日本烟草产业株式会社 | 利用联用药物的糖尿病的治疗或预防方法 |
| WO2022105845A1 (zh) * | 2020-11-19 | 2022-05-27 | 北京盈科瑞创新药物研究有限公司 | 一种糖苷类衍生物及其制备方法和应用 |
Family Cites Families (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3674836A (en) | 1968-05-21 | 1972-07-04 | Parke Davis & Co | 2,2-dimethyl-{11 -aryloxy-alkanoic acids and salts and esters thereof |
| US4027009A (en) | 1973-06-11 | 1977-05-31 | Merck & Co., Inc. | Compositions and methods for depressing blood serum cholesterol |
| JPS5612114B2 (es) | 1974-06-07 | 1981-03-18 | ||
| US4231938A (en) | 1979-06-15 | 1980-11-04 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
| MX7065E (es) | 1980-06-06 | 1987-04-10 | Sankyo Co | Un procedimiento microbiologico para preparar derivados de ml-236b |
| US4450171A (en) | 1980-08-05 | 1984-05-22 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
| US4448784A (en) | 1982-04-12 | 1984-05-15 | Hoechst-Roussel Pharmaceuticals, Inc. | 1-(Aminoalkylphenyl and aminoalkylbenzyl)-indoles and indolines and analgesic method of use thereof |
| US5354772A (en) | 1982-11-22 | 1994-10-11 | Sandoz Pharm. Corp. | Indole analogs of mevalonolactone and derivatives thereof |
| US4499289A (en) | 1982-12-03 | 1985-02-12 | G. D. Searle & Co. | Octahydronapthalenes |
| CA1327360C (en) | 1983-11-14 | 1994-03-01 | William F. Hoffman | Oxo-analogs of mevinolin-like antihypercholesterolemic agents |
| US4613610A (en) | 1984-06-22 | 1986-09-23 | Sandoz Pharmaceuticals Corp. | Cholesterol biosynthesis inhibiting pyrazole analogs of mevalonolactone and its derivatives |
| US4686237A (en) | 1984-07-24 | 1987-08-11 | Sandoz Pharmaceuticals Corp. | Erythro-(E)-7-[3'-C1-3 alkyl-1'-(3",5"-dimethylphenyl)naphth-2'-yl]-3,5-dihydroxyhept-6-enoic acids and derivatives thereof |
| US4647576A (en) | 1984-09-24 | 1987-03-03 | Warner-Lambert Company | Trans-6-[2-(substitutedpyrrol-1-yl)alkyl]-pyran-2-one inhibitors of cholesterol synthesis |
| HU198005B (en) | 1984-12-04 | 1989-07-28 | Sandoz Ag | Process for producing mevqlolakton, derivatives, its indene-analogues and pharmaceutical compositions containing them |
| US4668794A (en) | 1985-05-22 | 1987-05-26 | Sandoz Pharm. Corp. | Intermediate imidazole acrolein analogs |
| AU598775B2 (en) | 1985-10-25 | 1990-07-05 | Sandoz Ag | Heterocyclic analogs of mevalonolactone |
| FR2596393B1 (fr) | 1986-04-01 | 1988-06-03 | Sanofi Sa | Derives de l'acide hydroxy-3 dihydroxyoxophosphorio-4 butanoique, leur procede de preparation, leur application comme medicament et les compositions les renfermant |
| US5614492A (en) | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
| US4681893A (en) | 1986-05-30 | 1987-07-21 | Warner-Lambert Company | Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis |
| DK277488A (da) | 1987-05-22 | 1988-11-23 | Squibb & Sons Inc | Phosporholdige hmg-coa-reduktaseinhibitorer, deres anvendelse og fremstilling samt mellemprodukter ved fremstillingen |
| US4759923A (en) | 1987-06-25 | 1988-07-26 | Hercules Incorporated | Process for lowering serum cholesterol using poly(diallylmethylamine) derivatives |
| JP2569746B2 (ja) | 1987-08-20 | 1997-01-08 | 日産化学工業株式会社 | キノリン系メバロノラクトン類 |
| US4924024A (en) | 1988-01-11 | 1990-05-08 | E. R. Squibb & Sons, Inc. | Phosphorus-containing squalene synthetase inhibitors, new intermediates and method |
| US4871721A (en) | 1988-01-11 | 1989-10-03 | E. R. Squibb & Sons, Inc. | Phosphorus-containing squalene synthetase inhibitors |
| NO177005C (no) | 1988-01-20 | 1995-07-05 | Bayer Ag | Analogifremgangsmåte for fremstilling av substituerte pyridiner, samt mellomprodukter til bruk ved fremstillingen |
| US5506219A (en) | 1988-08-29 | 1996-04-09 | E. R. Squibb & Sons, Inc. | Pyridine anchors for HMG-CoA reductase inhibitors |
| US5753675A (en) | 1989-03-03 | 1998-05-19 | Novartis Pharmaceuticals Corporation | Quinoline analogs of mevalonolactone and derivatives thereof |
| FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
| US5177080A (en) | 1990-12-14 | 1993-01-05 | Bayer Aktiengesellschaft | Substituted pyridyl-dihydroxy-heptenoic acid and its salts |
| JP2648897B2 (ja) | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | ピリミジン誘導体 |
| US5595872A (en) | 1992-03-06 | 1997-01-21 | Bristol-Myers Squibb Company | Nucleic acids encoding microsomal trigyceride transfer protein |
| US5470845A (en) | 1992-10-28 | 1995-11-28 | Bristol-Myers Squibb Company | Methods of using α-phosphonosulfonate squalene synthetase inhibitors including the treatment of atherosclerosis and hypercholesterolemia |
| US5594016A (en) | 1992-12-28 | 1997-01-14 | Mitsubishi Chemical Corporation | Naphthalene derivatives |
| ES2133158T3 (es) | 1993-01-19 | 1999-09-01 | Warner Lambert Co | Formulacion ci-981 oral, estable y proceso de preparacion del mismo. |
| US5739135A (en) | 1993-09-03 | 1998-04-14 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| US5776983A (en) | 1993-12-21 | 1998-07-07 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
| US5488064A (en) | 1994-05-02 | 1996-01-30 | Bristol-Myers Squibb Company | Benzo 1,3 dioxole derivatives |
| US5385929A (en) | 1994-05-04 | 1995-01-31 | Warner-Lambert Company | [(Hydroxyphenylamino) carbonyl] pyrroles |
| US5612359A (en) | 1994-08-26 | 1997-03-18 | Bristol-Myers Squibb Company | Substituted biphenyl isoxazole sulfonamides |
| US5491134A (en) | 1994-09-16 | 1996-02-13 | Bristol-Myers Squibb Company | Sulfonic, phosphonic or phosphiniic acid β3 agonist derivatives |
| US5541204A (en) | 1994-12-02 | 1996-07-30 | Bristol-Myers Squibb Company | Aryloxypropanolamine β 3 adrenergic agonists |
| US5620997A (en) | 1995-05-31 | 1997-04-15 | Warner-Lambert Company | Isothiazolones |
| WO1997012613A1 (en) | 1995-10-05 | 1997-04-10 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| JP2000502086A (ja) | 1995-12-13 | 2000-02-22 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 核レセプターのリガンドおよびリガンド結合ドメイン |
| US5770615A (en) | 1996-04-04 | 1998-06-23 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
| US5962440A (en) | 1996-05-09 | 1999-10-05 | Bristol-Myers Squibb Company | Cyclic phosphonate ester inhibitors of microsomal triglyceride transfer protein and method |
| US5885983A (en) | 1996-05-10 | 1999-03-23 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| US5827875A (en) | 1996-05-10 | 1998-10-27 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| US5760246A (en) | 1996-12-17 | 1998-06-02 | Biller; Scott A. | Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method |
| TW536540B (en) | 1997-01-30 | 2003-06-11 | Bristol Myers Squibb Co | Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe |
| GB9713739D0 (en) | 1997-06-27 | 1997-09-03 | Karobio Ab | Thyroid receptor ligands |
| EP1052994A2 (en) | 1998-02-02 | 2000-11-22 | Trustees Of Tufts College | Use of dipeptidylpetidase inhibitors to regulate glucose metabolism |
| EP1062222A1 (en) | 1998-03-09 | 2000-12-27 | Fondatech Benelux N.V. | Serine peptidase modulators |
| DE19823831A1 (de) | 1998-05-28 | 1999-12-02 | Probiodrug Ges Fuer Arzneim | Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen |
| DE19828113A1 (de) | 1998-06-24 | 2000-01-05 | Probiodrug Ges Fuer Arzneim | Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV |
| DE19828114A1 (de) | 1998-06-24 | 2000-01-27 | Probiodrug Ges Fuer Arzneim | Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV |
| ID26984A (id) | 1998-07-06 | 2001-02-22 | Bristol Myers Squibb Co | Senyawa-senyawa sulfonamida sebagai antagonis reseptor angiotensin endotelin ganda |
| TWI302149B (en) | 1999-09-22 | 2008-10-21 | Bristol Myers Squibb Co | Substituted acid derivatives useful as antiodiabetic and antiobesity agents and method |
| US6414002B1 (en) | 1999-09-22 | 2002-07-02 | Bristol-Myers Squibb Company | Substituted acid derivatives useful as antidiabetic and antiobesity agents and method |
| PH12000002657B1 (en) | 1999-10-12 | 2006-02-21 | Bristol Myers Squibb Co | C-aryl glucoside SGLT2 inhibitors |
| US6395767B2 (en) | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| US6555519B2 (en) | 2000-03-30 | 2003-04-29 | Bristol-Myers Squibb Company | O-glucosylated benzamide SGLT2 inhibitors and method |
| GEP20063908B (en) | 2001-10-18 | 2006-08-25 | Bristol Myers Squibb Co | Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions |
| US7393836B2 (en) | 2004-07-06 | 2008-07-01 | Boehringer Ingelheim International Gmbh | D-xylopyranosyl-substituted phenyl derivatives, medicaments containing such compounds, their use and process for their manufacture |
| PE20080251A1 (es) * | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| TWI499414B (zh) * | 2006-09-29 | 2015-09-11 | Lexicon Pharmaceuticals Inc | 鈉與葡萄糖第２型共同運輸體（ｃｏ-ｔｒａｎｓｐｏｒｔｅｒ ２）的抑制物與其應用方法 |
| US7846945B2 (en) | 2007-03-08 | 2010-12-07 | Lexicon Pharmaceuticals, Inc. | Piperdine-based inhibitors of sodium glucose co-transporter 2 and methods of their use |
| UA107175C2 (uk) * | 2007-07-26 | 2014-12-10 | Спосіб і сполука, призначені для одержання інгібіторів контранспортера натрій-глюкози 2 типу, варіанти | |
| CL2008002425A1 (es) * | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Composición farmacéutica que comprende un inhibidor de sglt2 y 1-(4-metil-quinazolin-2-il)metil-3metil-7-(-2-butin-1-il)-8-(3-(r)-amino-piperidin-1il)-xantina, un inhibidor de dpp iv y su uso para el tratamiento de la obesidad y de la diabetes tipo 1 y 2 y complicaciones de esta. |
| CL2008003653A1 (es) * | 2008-01-17 | 2010-03-05 | Mitsubishi Tanabe Pharma Corp | Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica. |
| TWI472521B (zh) * | 2008-07-17 | 2015-02-11 | Lexicon Pharmaceuticals Inc | （２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）－２－（４－氯－３－（４－乙氧苄基）苯基）－６－（甲硫）四氫－２ｈ－哌喃－３，４，５－三醇的固體形態與其使用方法 |
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- 2011-03-01 KR KR1020187013218A patent/KR20180051683A/ko not_active Ceased
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