AR040241A1 - Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia - Google Patents
Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemiaInfo
- Publication number
- AR040241A1 AR040241A1 ARP030101960A ARP030101960A AR040241A1 AR 040241 A1 AR040241 A1 AR 040241A1 AR P030101960 A ARP030101960 A AR P030101960A AR P030101960 A ARP030101960 A AR P030101960A AR 040241 A1 AR040241 A1 AR 040241A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- optionally substituted
- groups
- phenyl
- Prior art date
Links
- 208000008589 Obesity Diseases 0.000 title abstract 3
- 206010012601 diabetes mellitus Diseases 0.000 title abstract 3
- 235000020824 obesity Nutrition 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 26
- 125000000217 alkyl group Chemical group 0.000 abstract 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 16
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 13
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 11
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000001624 naphthyl group Chemical group 0.000 abstract 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 4
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 3
- 229910017711 NHRa Inorganic materials 0.000 abstract 3
- -1 ethylenedioxy Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 2
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 2
- 208000032928 Dyslipidaemia Diseases 0.000 abstract 2
- 208000017170 Lipid metabolism disease Diseases 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000002619 bicyclic group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- 102100036506 11-beta-hydroxysteroid dehydrogenase 1 Human genes 0.000 abstract 1
- 101710186107 11-beta-hydroxysteroid dehydrogenase 1 Proteins 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 206010022489 Insulin Resistance Diseases 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 201000001421 hyperglycemia Diseases 0.000 abstract 1
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical compound [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic 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
- A61P3/04—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
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Emergency Medicine (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Los compuestos son útiles para el tratamiento de la diabetes, tal como la diabetes no insulino dependiente (DMNID), hiperglicemia, obesidad, resistencia a la insulina, dislipidemia, hiperlipidemia, hipertensión, Síndrome X, y otros síntomas asociados con DMNID. Reivindicación 1: Inhibidores de la 11 beta hidroxiesteroide deshidrogenasa 1 para el tratamiento de la diabetes, obesidad y dislipidemia caracterizados porque comprenden una cantidad terapéuticamente efectiva de un compuesto representado por la fórmula (1), o por una sal o solvato del mismo farmacéuticamente aceptable, donde: A y B se pueden tomar separados o juntos: Cuando se toman separadamente, A representa halo, C1-6 alquil, O(C1-6)alquil o fenil, dicho alquil, fenil y la porción de alquil de O(C1-6)alquil siendo opcionalmente sustituidos con de 1 a 3 grupos halo; y B representa H, halo, C1-6 alquil, -O(C1-6)alquil, -S(C1-6)alquil, C2-6 alquenil, fenil o naftil, dicho alquil, alquenil, fenil, naftil, y las porciones de alquil de -O(C1-6)alquil y -S(C1-6)alquil siendo opcionalmente sustituidas con de 1 a 3 grupos seleccionados de halo, OH, CH3O, CF3 y OCF3; y cuando se toman juntos, A y B juntos representan (a) C1-4 alquileno opcionalmente sustituido con de 1 a 3 grupos halo, y de 1 a 2 grupos Ra donde, Ra representa C1-3 alquil, O(C1-3)alquil, (C6-10)ar(C1-6)alquileno o fenil opcionalmente sustituido con de 1 a 3 grupos halo, o (b) C2-5 alcanediil tal que forman un anillo de 3 a 6 miembros con el átomo de C al que están unidos, dicho anillo opcionalmente contiene un doble enlace o de 1 a 2 heteroátomos seleccionados de O, S, y N, dicho anillo de 3 a 6 miembros siendo opcionalmente sustituido con C1-4 alquileno, oxo, etilenedioxi o propilenedioxi, y siendo además opcionalmente sustituido con de 1 a 4 grupos seleccionados de halo, C1-4 alquil, halo(C1-4)alquil, (C1-3) acil, (C1-3) aciloxi, C1-3 alcoxi, (C1-6) alquil OC(O)-,C2-4 alquenil, C2-4 alquinil, (C1-3)alcoxi(C1-3)alquil; (C1-3)alcoxi(C1-3)alcoxi, fenil, CN, OH, D, NH2, NHRa y N(Ra)2 donde Ra es como previamente se definió; cada R1 representa H o es independientemente seleccionado del grupo consistente en: OH, halo, C1-10 alquil, C1-6 alcoxi y C6-10 aril, dicho C1-10 alquil, C6-10 aril y la porción de alquil de C1-6 alcoxi siendo opcionalmente sustituida con de 1 a 3 halo, OH, O(C1-3)alquil, grupos fenil o naftil, dicho fenil y naftil siendo opcionalmente sustituidos con de 1 a 3 sustituyentes independientemente seleccionados de halo, OCH3, OCF3, CH3, CF3 y fenil, donde dicho fenil está opcionalmente sustituido con de 1 a 3 grupos halo, o dos grupos R1 tomados juntos representan un fusionado C5-6 alquil o anillo aril, el cual puede ser opcionalmente sustituido con de 1 a 2 OH o grupos Ra, donde Ra es como se definió anteriormente; R2 y R3 son tomados juntos o separadamente. Cuando se toman juntos, R2 y R3 representan (a) un C3-8 alcanediil formando un anillo fusionado no aromático de 5 a 10 miembros opcionalmente interrumpido con de 1 a 2 enlaces dobles, y opcionalmente conteniendo de 1 a 2 heteroátomos seleccionados de O, S y N; o (b) un grupo monocíclico aromático fusionado de 6 a 10 miembros o un grupo bicíclico, dicho alcanediil y grupo monocíclico aromático o grupo bicíclico siendo opcionalmente sustituido con de 1 a 6 átomos halo, y de 1 a 4 de OH, C1-3 alquil, O(C1-3)alquil, halo(C1-3)alquil, halo(C1-3)alcoxi, y fenil, dicho fenil siendo opcionalmente sustituido con de 1 a 4 grupos independientemente seleccionados de halo, C1-3 alquil, O(C1-3)alquil, y dicho C1-3 alquil y la porción C1-3 alquil de O(C1-3)alquil siendo opcionalmente sustituido con de 1 a 3 grupos halo. Cuando se toman separadamente, R2 es seleccionado del grupo consistente en: (a) C1-14 alquil opcionalmente sustituido con de 1 a 6 grupos halo y de 1 a 3 sustituyentes seleccionados de OH, O(C1-3)alquil, y fenil, dicho fenil siendo opcionalmente sustituido con de 1 a 4 grupos independientemente seleccionados de halo, OCH3, OCF3, CH3, y CF3, y dicha porción C1-3 alquil de O(C1-3)alquil siendo opcionalmente sustituida con de 1 a 3 grupos halo; (b) fenil o piridil opcionalmente sustituida con de 1 a 3 halo, OH, o grupos Ra, con Ra como previamente se definió; (c) C2-10 alquenil, opcionalmente sustituido con de 1 a 3 sustituyentes independientemente seleccionados de halo, OH y O(C1-3)alquil, dicha porción C1-3 alquil de O(C1-3)alquil siendo opcionalmente sustituida con de 1 a 3 grupos halo; (d) CH2CO2H; (e) CH2CO2(C1-6)alquil; (f) CH2C(O)NHRa donde Ra es como previamente se definió; (g) NH2, NHRa y N(Ra)2 donde Ra es como previamente se definió; y R3 es seleccionado del grupo consistente en C1-14 alquil, C2-10 alquenil, S(C1-6)alquil, C6-10 aril, heterociclil y heteroaril, dicho alquil, alquenil, aril, heterociclil, heteroaril y la porción de alquil de S(C1-6)alquil siendo opcionalmente sustituido con (a) R, (b) de 1 a 6 grupos halo y (c) de 1 a 3 grupos elegidos de OH, NH2,NH(C1-4)alquil, N(C1-4 alquil)2, C1-4 alquil, O(C1-4)alquil, CN, (C1-4)alquilS(O)x- donde x es 0, 1, o 2, (C1-4)alquilSO2NH-,H2NSO2-, (C1-4)alquilNHSO2-y (C1-4 alquil)2NSO2-, dicho C1-4 alquil y las porciones C1-4 alquil de dichos grupos siendo opcionalmente sustituidas con fenil y de 1 a 3 grupos halo, y R es seleccionado de heterociclos, heteroaril y aril, dicho grupo siendo opcionalmente sustituido con de 1 a 4 grupos seleccionados de halo, C1-4 alquil, (C1-4)alquilS(O)x-, con x como previamente se definió, (C1-4)alquilSO2NH-, H2NSO2-, (C1-4)alquilNHSO2-, (C1-4 alquil)2NSO2-, CN, OH, O(C1-4)alquil, y dicho C1-4 alquil y las porciones de C1-4 alquil de dichos grupos siendo opcionalmente sustituidas con de 1 a 5 halo y 1 grupo seleccionado de OH y O(C1-3)alquil.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38738502P | 2002-06-10 | 2002-06-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR040241A1 true AR040241A1 (es) | 2005-03-23 |
Family
ID=29736306
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030101960A AR040241A1 (es) | 2002-06-10 | 2003-06-02 | Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US6730690B2 (es) |
| EP (1) | EP1532122B1 (es) |
| JP (1) | JP4405384B2 (es) |
| KR (1) | KR20050008805A (es) |
| CN (2) | CN1990474A (es) |
| AR (1) | AR040241A1 (es) |
| AT (1) | ATE537155T1 (es) |
| AU (2) | AU2003243420A1 (es) |
| BR (1) | BR0311137A (es) |
| CA (1) | CA2488592C (es) |
| EC (1) | ECSP045482A (es) |
| ES (1) | ES2377200T3 (es) |
| HR (1) | HRP20041180A2 (es) |
| IL (1) | IL165257A0 (es) |
| IS (1) | IS7519A (es) |
| JO (1) | JO2315B1 (es) |
| MA (1) | MA27317A1 (es) |
| MX (1) | MXPA04012381A (es) |
| MY (1) | MY134664A (es) |
| NO (1) | NO20050102L (es) |
| NZ (1) | NZ536188A (es) |
| PE (1) | PE20040726A1 (es) |
| PL (1) | PL373372A1 (es) |
| RU (1) | RU2319703C2 (es) |
| TW (1) | TWI324153B (es) |
| UA (1) | UA81417C2 (es) |
| WO (2) | WO2003104207A2 (es) |
| ZA (1) | ZA200408772B (es) |
Families Citing this family (175)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060148725A1 (en) * | 2001-12-21 | 2006-07-06 | The Miriam Hospital | Selective 11beta HSD inhibitors and methods of use thereof |
| US20030148987A1 (en) * | 2001-12-21 | 2003-08-07 | Morris David J. | Selective 11beta-HSD inhibitors and methods of use thereof |
| US7329683B2 (en) | 2002-02-01 | 2008-02-12 | Merck & Co., Inc. | 11-β-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia |
| JO2397B1 (en) * | 2002-12-20 | 2007-06-17 | ميرك شارب اند دوم كوربوريشن | Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors |
| KR101078098B1 (ko) | 2003-01-14 | 2011-10-28 | 아레나 파마슈티칼스, 인크. | 대사 조절제로서의 1,2,3-삼치환된 아릴 및 헤테로아릴유도체, 및 당뇨병 및 고혈당증을 비롯한 이에 관련된장애의 예방 및 치료 |
| US20040242568A1 (en) | 2003-03-25 | 2004-12-02 | Syrrx, Inc. | Dipeptidyl peptidase inhibitors |
| EP1624876A2 (en) * | 2003-04-29 | 2006-02-15 | The Miriam Hospital | Selective testicular 11beta-hsd inhibitors and methods of use thereof |
| WO2004103993A1 (en) | 2003-05-14 | 2004-12-02 | Syrrx, Inc. | Dipeptidyl peptidase inhibitors |
| US20070099884A1 (en) * | 2003-06-06 | 2007-05-03 | Erondu Ngozi E | Combination therapy for the treatment of diabetes |
| GB0315111D0 (en) | 2003-06-27 | 2003-07-30 | Cancer Rec Tech Ltd | Substituted 5-membered ring compounds and their use |
| EP1506967B1 (en) | 2003-08-13 | 2007-11-21 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| AU2004273610B2 (en) | 2003-09-22 | 2010-07-01 | Onepharm Research & Development Gmbh | Prevention and treatment of inflammation-induced and/or immune-mediated bone loss |
| CA2543602A1 (en) | 2003-10-28 | 2005-05-19 | Amgen Inc. | Triazole compounds and uses related thereto |
| WO2005060694A2 (en) * | 2003-12-18 | 2005-07-07 | Agy Therapeutics, Inc. | Treatment of neurologic disorders with inhibitors of 11beta-hsd1 |
| US7745630B2 (en) | 2003-12-22 | 2010-06-29 | Justin Stephen Bryans | Triazolyl piperidine arginine vasopressin receptor modulators |
| IN2012DN03023A (es) * | 2004-01-26 | 2015-07-31 | Merck Sharp & Dohme | |
| US7354938B2 (en) | 2004-03-23 | 2008-04-08 | Amgen Inc. | Pyrazole compounds and uses related thereto |
| WO2005097759A1 (en) | 2004-03-29 | 2005-10-20 | Merck & Co., Inc. | Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1 |
| US20050261302A1 (en) * | 2004-04-29 | 2005-11-24 | Hoff Ethan D | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their therapeutic application |
| PL1747198T3 (pl) * | 2004-05-07 | 2008-11-28 | Janssen Pharmaceutica Nv | Pochodne adamantylopirolidyn-2-onu jako inhibitory 11ß-dehydrogenazy hydroksysteroidowej |
| TWI350168B (en) | 2004-05-07 | 2011-10-11 | Incyte Corp | Amido compounds and their use as pharmaceuticals |
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| TW202123960A (zh) | 2019-08-30 | 2021-07-01 | 美商默沙東藥廠 | Pcsk9拮抗劑化合物 |
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| EP4225739B1 (en) | 2020-10-08 | 2026-01-21 | Merck Sharp & Dohme LLC | Preparation of benzimidazolone derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors |
| CR20230160A (es) | 2020-10-08 | 2023-06-02 | Merck Sharp & Dohme Llc | Preparación de derivados de oxindol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 |
| IL310851A (en) | 2021-08-19 | 2024-04-01 | Merck Sharp & Dohme Llc | Compounds for the treatment of diseases associated with PCSK9 activity |
| JP2025517334A (ja) | 2022-05-16 | 2025-06-05 | スパロー ファーマシューティカルズ,インコーポレーテッド | グルココルチコイド過剰を治療するための方法及び組成物 |
| CN116003279B (zh) * | 2022-06-13 | 2024-05-28 | 苏州大学 | 一种绿色的n-甲基酰胺化合物的制备方法 |
| US20230406885A1 (en) | 2022-06-15 | 2023-12-21 | Merck Sharp & Dohme Llc | Cyclic peptides for trapping interleukin-1 beta |
| AU2023400409A1 (en) | 2022-12-02 | 2025-06-26 | Merck Sharp & Dohme Llc | Preparation of fused azole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors |
| WO2025106386A1 (en) | 2023-11-14 | 2025-05-22 | Merck Sharp & Dohme Llc | A cyclic peptide for trapping interleukin-1 beta |
| TW202542176A (zh) | 2023-12-15 | 2025-11-01 | 美商默沙東有限責任公司 | 用於治療動脈粥樣硬化及發炎病症之環狀肽IL-1β捕捉劑 |
| US20260022125A1 (en) | 2024-07-19 | 2026-01-22 | Merck Sharp & Dohme Llc | Pyrrolopyridazine vegfr inhibitors |
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| TW226993B (es) * | 1992-05-29 | 1994-07-21 | Kumiai Chemical Industry Co | |
| TR200001645T2 (tr) | 1997-12-11 | 2000-12-21 | Janssen Pharmaceutica N.V. | Retinoyik asit taklidi anilürler. |
| US20030073850A1 (en) | 1998-08-07 | 2003-04-17 | Altenbach Robert J. | 4-Imidazole derivatives of benzyl and restricted benzyl sulfonamides, sulfamides, ureas, carbamates, and amides and their use |
| US6503935B1 (en) | 1998-08-07 | 2003-01-07 | Abbott Laboratories | Imidazoles and related compounds as α1A agonists |
| SE0001899D0 (sv) * | 2000-05-22 | 2000-05-22 | Pharmacia & Upjohn Ab | New compounds |
| WO2003004497A1 (en) | 2001-07-05 | 2003-01-16 | Sumitomo Pharmaceuticals Company, Limited | Novel heterocyclic compound |
| JO2397B1 (en) * | 2002-12-20 | 2007-06-17 | ميرك شارب اند دوم كوربوريشن | Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors |
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