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)
- Chemical Kinetics & Catalysis (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Neurology (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (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) | CN1312137C (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 (174)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003059267A2 (en) * | 2001-12-21 | 2003-07-24 | Rhode Island Hospital | SELECTIVE 11β-HSD INHIBITORS AND METHODS FOR USE THEREOF |
| US20060148725A1 (en) * | 2001-12-21 | 2006-07-06 | The Miriam Hospital | Selective 11beta HSD inhibitors and methods of use thereof |
| EP1474139B1 (en) | 2002-02-01 | 2007-11-21 | Merck & Co., Inc. | 11-beta-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 |
| ES2295816T3 (es) | 2003-01-14 | 2008-04-16 | Arena Pharmaceuticals, Inc. | Derivados arilo y heteroarilo 1,2,3-trisustituidos como moduladores del metabolismo, y profilaxis y tratamiento de transtornos relacionados con los mismos, tales como la diabetes y la hiperglucemia. |
| US20040242566A1 (en) | 2003-03-25 | 2004-12-02 | Syrrx, Inc. | Dipeptidyl peptidase inhibitors |
| US20050020550A1 (en) * | 2003-04-29 | 2005-01-27 | Morris David J. | Selective testicular 11beta-HSD inhibitors and methods of use thereof |
| EP1625122A1 (en) | 2003-05-14 | 2006-02-15 | Takeda San Diego, 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 |
| CA2535619A1 (en) | 2003-08-13 | 2005-02-24 | Takeda Pharmaceutical Company Limited | 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors |
| PL1663185T3 (pl) | 2003-09-22 | 2009-06-30 | Onepharm Res & Development Gmbh | Zapobieganie i leczenie utraty kości wywołanej przez zapalenie i/lub za pośrednictwem układu odpornościowego |
| WO2005044192A2 (en) * | 2003-10-28 | 2005-05-19 | Amgen Inc. | Triazole compounds and uses related thereto |
| US20050137209A1 (en) * | 2003-12-18 | 2005-06-23 | 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 |
| JP2007519726A (ja) * | 2004-01-26 | 2007-07-19 | メルク エンド カムパニー インコーポレーテッド | 11−ベータ−ヒドロキシステロイドデヒドロゲナーゼ1型の阻害剤の、新規結晶形態 |
| 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 |
| TWI350168B (en) | 2004-05-07 | 2011-10-11 | Incyte Corp | Amido compounds and their use as pharmaceuticals |
| WO2005108361A1 (en) * | 2004-05-07 | 2005-11-17 | Janssen Pharmaceutica N.V. | Adamantyl pyrrolidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors |
| NZ551077A (en) | 2004-05-07 | 2009-05-31 | Janssen Pharmaceutica Nv | Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors |
| WO2005121132A1 (ja) * | 2004-06-11 | 2005-12-22 | Shionogi & Co., Ltd. | 抗hcv作用を有する縮合ヘテロ環化合物 |
| US20060025445A1 (en) * | 2004-08-02 | 2006-02-02 | Xiang Jason S | 11-Beta HSD1 inhibitors |
| GB0418877D0 (en) * | 2004-08-24 | 2004-09-29 | Univ Edinburgh | Heart |
| DE602005017159D1 (de) | 2004-08-30 | 2009-11-26 | Janssen Pharmaceutica Nv | Oxysteroid-dehydrogenase-inhibitoren |
| WO2006024628A1 (en) | 2004-08-30 | 2006-03-09 | Janssen Pharmaceutica N.V. | Tricyclic lactam derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors |
| JP5208505B2 (ja) | 2004-08-30 | 2013-06-12 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 11−ベータヒドロキシステロイドデヒドロゲナーゼ阻害剤としてのn−2アダマンタニル−2−フェノキシ−アセトアミド誘導体 |
| KR101214665B1 (ko) * | 2004-09-16 | 2012-12-21 | 아스텔라스세이야쿠 가부시키가이샤 | 트리아졸 유도체 또는 그의 염 |
| JP5140577B2 (ja) | 2005-03-31 | 2013-02-06 | タケダ カリフォルニア インコーポレイテッド | ヒドロキシステロイドデヒドロゲナーゼ阻害剤 |
| AU2006232660B2 (en) | 2005-04-05 | 2010-03-25 | F. Hoffmann-La Roche Ag | 1H-Pyrazole 4-Carboxylamides, their preparation and their use as 11Beta-hydroxysteroid dehydrogenase |
| US7737155B2 (en) | 2005-05-17 | 2010-06-15 | Schering Corporation | Nitrogen-containing heterocyclic compounds and methods of use thereof |
| EP1894919B1 (en) * | 2005-06-07 | 2012-03-28 | Shionogi & Co., Ltd. | Heterocyclic compound having type i 11 beta hydroxysteroid dehydrogenase inhibitory activity |
| US7579360B2 (en) | 2005-06-09 | 2009-08-25 | Bristol-Myers Squibb Company | Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| US7572807B2 (en) | 2005-06-09 | 2009-08-11 | Bristol-Myers Squibb Company | Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors |
| US7622492B2 (en) | 2005-08-31 | 2009-11-24 | Hoffmann-La Roche Inc. | Pyrazolones as inhibitors of 11β-hydroxysteroid dehydrogenase |
| ME02005B (me) | 2005-09-14 | 2012-08-31 | Takeda Pharmaceuticals Co | Inhibitori dipeptidil peptidaze za lečenje dijabetesa |
| CN101360723A (zh) | 2005-09-16 | 2009-02-04 | 武田药品工业株式会社 | 制备嘧啶二酮衍生物的方法 |
| RU2302066C1 (ru) * | 2005-09-22 | 2007-06-27 | Научный центр волоконной оптики при Институте общей физики им. А.М. Прохорова Российской академии наук | Волоконный световод для оптического усиления излучения на длине волны в диапазоне 1000-1700 нм, способы его изготовления и волоконный лазер |
| CN101277960A (zh) | 2005-09-29 | 2008-10-01 | 默克公司 | 作为黑皮质素-4受体调节剂的酰化螺哌啶衍生物 |
| EP1953145B1 (en) * | 2005-11-21 | 2015-11-04 | Shionogi & Co., Ltd. | Heterocyclic compound having inhibitory activity on 11-b-hydroxysteroid dehydrogenase type i |
| US7998959B2 (en) | 2006-01-12 | 2011-08-16 | Incyte Corporation | Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same |
| EP1979335A2 (en) | 2006-01-18 | 2008-10-15 | F.Hoffmann-La Roche Ag | Thiazoles as 11 beta-hsd1 inhibitors |
| WO2007088895A1 (ja) * | 2006-01-31 | 2007-08-09 | Mochida Pharmaceutical Co., Ltd. | 3-アリールアミノ-1,2,4-トリアゾール誘導体 |
| US7834178B2 (en) | 2006-03-01 | 2010-11-16 | Bristol-Myers Squibb Company | Triazine 11-beta hydroxysteroid dehydrogenase type 1 inhibitors |
| CA2645712A1 (en) | 2006-03-16 | 2007-09-20 | Astellas Pharma Inc. | Triazole derivative or salt thereof |
| WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| JP2010500300A (ja) | 2006-08-08 | 2010-01-07 | サノフィ−アベンティス | アリールアミノアリール−アルキル−置換イミダゾリジン−2,4−ジオン、それらの製造法、それらの化合物を含有する薬剤、およびそれらの使用 |
| DK2054049T3 (en) | 2006-08-24 | 2016-08-01 | Univ Tennessee Res Found | SUBSTITUTED ACYLANILIDES AND PROCEDURES FOR USING THEREOF |
| US8324383B2 (en) | 2006-09-13 | 2012-12-04 | Takeda Pharmaceutical Company Limited | Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile |
| EP2698157B1 (en) | 2006-09-22 | 2015-05-20 | Merck Sharp & Dohme Corp. | Method of treatment using fatty acid synthesis inhibitors |
| TW200838536A (en) | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| TW200843794A (en) * | 2006-12-21 | 2008-11-16 | Centocor Inc | Use of long-acting GLP-1 receptor agonists to improve insulin sensitivity and lipid profiles |
| DE102007005045B4 (de) | 2007-01-26 | 2008-12-18 | Sanofi-Aventis | Phenothiazin Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| US8093236B2 (en) | 2007-03-13 | 2012-01-10 | Takeda Pharmaceuticals Company Limited | Weekly administration of dipeptidyl peptidase inhibitors |
| JP5319518B2 (ja) | 2007-04-02 | 2013-10-16 | Msd株式会社 | インドールジオン誘導体 |
| EP2163543B1 (en) | 2007-05-18 | 2015-03-04 | Shionogi&Co., Ltd. | Nitrogen-containing heterocyclic derivative having 11 beta-hydroxysteroid dehydrogenase type i inhibitory activity |
| EP2172453A4 (en) | 2007-06-27 | 2010-12-22 | Taisho Pharmaceutical Co Ltd | CONNECTION WITH 11-β-HSD1 INHIBITING ACTIVITY |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| US8119658B2 (en) | 2007-10-01 | 2012-02-21 | Bristol-Myers Squibb Company | Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| WO2009126861A2 (en) * | 2008-04-11 | 2009-10-15 | Bristol-Myers Squibb Company | Triazolopyridine compounds useful as dgat1 inhibitors |
| WO2009126624A1 (en) * | 2008-04-11 | 2009-10-15 | Bristol-Myers Squibb Company | Triazolo compounds useful as dgat1 inhibitors |
| EP2298747B1 (en) * | 2008-07-03 | 2016-12-28 | Astellas Pharma Inc. | Triazole derivative or salt thereof |
| WO2010003624A2 (en) | 2008-07-09 | 2010-01-14 | Sanofi-Aventis | Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof |
| AU2009308980B2 (en) | 2008-10-30 | 2013-02-28 | Merck Sharp & Dohme Corp. | Isonicotinamide orexin receptor antagonists |
| JO2870B1 (en) | 2008-11-13 | 2015-03-15 | ميرك شارب اند دوهم كورب | Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes |
| AU2009314200B2 (en) | 2008-11-17 | 2011-11-17 | Merck Sharp & Dohme Corp. | Substituted bicyclic amines for the treatment of diabetes |
| WO2010068601A1 (en) | 2008-12-08 | 2010-06-17 | Sanofi-Aventis | A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof |
| KR20110119790A (ko) * | 2009-02-12 | 2011-11-02 | 엑셀리시스, 인코포레이티드 | 당뇨병 및 비만을 치료하는데 tgr5 효능제로서 사용되는 트리아졸 및 이미다졸 유도체 |
| ES2350077B1 (es) | 2009-06-04 | 2011-11-04 | Laboratorios Salvat, S.A. | Compuestos inhibidores de 11beta-hidroxiesteroide deshidrogenasa de tipo 1. |
| WO2011011506A1 (en) | 2009-07-23 | 2011-01-27 | Schering Corporation | Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors |
| WO2011011508A1 (en) | 2009-07-23 | 2011-01-27 | Schering Corporation | Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors |
| US8552022B2 (en) | 2009-08-13 | 2013-10-08 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
| KR20120060207A (ko) | 2009-08-26 | 2012-06-11 | 사노피 | 신규한 결정성 헤테로방향족 플루오로글리코시드 수화물, 이들 화합물을 포함하는 약제 및 이들의 용도 |
| JP5734981B2 (ja) | 2009-09-02 | 2015-06-17 | メルク・シャープ・エンド・ドーム・コーポレイション | 糖尿病の治療又は予防のためのジペプチジルペプチダーゼiv阻害剤としてのアミノテトラヒドロピラン |
| WO2011071957A1 (en) | 2009-12-07 | 2011-06-16 | Sea Lane Biotechnologies, Llc | Conjugates comprising an antibody surrogate scaffold with improved pharmacokinetic properties |
| WO2011071565A1 (en) * | 2009-12-11 | 2011-06-16 | Exelixis, Inc. | Tgr5 agonists |
| US8853212B2 (en) | 2010-02-22 | 2014-10-07 | Merck Sharp & Dohme Corp | Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2011146358A1 (en) | 2010-05-21 | 2011-11-24 | Merck Sharp & Dohme Corp. | Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes |
| WO2011157827A1 (de) | 2010-06-18 | 2011-12-22 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
| 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 |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| 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 |
| US8742110B2 (en) | 2010-08-18 | 2014-06-03 | Merck Sharp & Dohme Corp. | Spiroxazolidinone compounds |
| UA112418C2 (uk) | 2010-09-07 | 2016-09-12 | Астеллас Фарма Інк. | Терапевтичний болезаспокійливий засіб |
| EP2619198A1 (en) | 2010-09-22 | 2013-07-31 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| EP2766349B1 (de) | 2011-03-08 | 2016-06-01 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2012120056A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683702B1 (de) | 2011-03-08 | 2014-12-24 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2012120057A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| US8828995B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| US8828994B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| EP2683701B1 (de) | 2011-03-08 | 2014-12-24 | Sanofi | Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| WO2012120051A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit adamantan- oder noradamantan substituierte benzyl-oxathiazinderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2012120055A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| AU2012240122B2 (en) | 2011-04-08 | 2016-08-25 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
| WO2012144478A1 (ja) * | 2011-04-19 | 2012-10-26 | 第一三共株式会社 | テトラヒドロチアゼピン誘導体 |
| CN103687855A (zh) | 2011-06-02 | 2014-03-26 | 英特维特国际股份有限公司 | 咪唑衍生物 |
| WO2012173917A1 (en) | 2011-06-16 | 2012-12-20 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment |
| 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 |
| EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US9422266B2 (en) | 2011-09-30 | 2016-08-23 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
| AR088352A1 (es) | 2011-10-19 | 2014-05-28 | Merck Sharp & Dohme | Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina |
| US9018200B2 (en) | 2011-10-24 | 2015-04-28 | Merck Sharp & Dohme Corp. | Substituted piperidinyl compounds useful as GPR119 agonists |
| WO2013068328A1 (en) | 2011-11-07 | 2013-05-16 | Intervet International B.V. | Bicyclo [2.2.2] octan-1-ylcarboxylic acid compounds as dgat-1 inhibitors |
| WO2013068439A1 (en) | 2011-11-09 | 2013-05-16 | Intervet International B.V. | 4-amino-5-oxo-7,8-dihydropyrimido[5, 4 -f] [1, 4] oxazepine compounds as dgat1 inhibitors |
| AU2012339870B2 (en) | 2011-11-15 | 2017-06-29 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds useful as GPR119 agonists |
| US9073930B2 (en) | 2012-02-17 | 2015-07-07 | Merck Sharp & Dohme | Dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| US20150057220A1 (en) | 2012-04-16 | 2015-02-26 | Kaneq Pharma Inc. | Fused aromatic phosphonate derivatives as precursors to ptp-1b inhibitors |
| US10987334B2 (en) | 2012-07-13 | 2021-04-27 | University Of Tennessee Research Foundation | Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs) |
| US9744149B2 (en) | 2012-07-13 | 2017-08-29 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| KR102122941B1 (ko) | 2012-07-13 | 2020-06-15 | 지티엑스, 인코포레이티드 | 선택적 안드로겐 수용체 조절자(sarms)를 이용한 안드로겐 수용체(ar) 양성 유방암의 치료 방법 |
| US9622992B2 (en) | 2012-07-13 | 2017-04-18 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| US9969683B2 (en) | 2012-07-13 | 2018-05-15 | Gtx, Inc. | Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS) |
| US10258596B2 (en) | 2012-07-13 | 2019-04-16 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| WO2014018350A1 (en) | 2012-07-23 | 2014-01-30 | Merck Sharp & Dohme Corp. | Treating diabetes with dipeptidyl peptidase-iv inhibitors |
| US9527875B2 (en) | 2012-08-02 | 2016-12-27 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| EP2931734B1 (en) | 2012-12-17 | 2020-12-02 | Merck Sharp & Dohme Corp. | Novel glucokinase activator compounds, compositions containing such compounds, and methods of treatment |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| WO2015089809A1 (en) | 2013-12-19 | 2015-06-25 | Merck Sharp & Dohme Corp. | Antidiabetic substituted heteroaryl compounds |
| WO2015112465A1 (en) | 2014-01-24 | 2015-07-30 | Merck Sharp & Dohme Corp. | Isoquinoline derivatives as mgat2 inhibitors |
| WO2015176267A1 (en) | 2014-05-22 | 2015-11-26 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| CA2950357A1 (en) | 2014-06-12 | 2015-12-17 | Universite De Lille 2 Droit Et Sante | Imidazol- or 1,2,4-triazol-derivatives and their use |
| EP3177287B1 (en) | 2014-08-08 | 2022-02-23 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| WO2016022448A1 (en) | 2014-08-08 | 2016-02-11 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| US10100042B2 (en) | 2014-08-08 | 2018-10-16 | Merck Sharp & Dohme Corp. | [5,6]—fused bicyclic antidiabetic compounds |
| MX382408B (es) | 2014-10-24 | 2025-03-13 | Merck Sharp & Dohme Llc | Coagonistas de los receptores de glucagón y de glp-1. |
| DK3212226T3 (da) | 2014-10-31 | 2020-06-15 | Ngm Biopharmaceuticals Inc | Sammensætninger og anvendelsesfremgangsmåder til behandling af metaboliske lidelser |
| TW201625635A (zh) | 2014-11-21 | 2016-07-16 | 默沙東藥廠 | 作為可溶性鳥苷酸環化酶活化劑之三唑并吡基衍生物 |
| PL3242666T3 (pl) | 2015-01-06 | 2025-02-17 | Arena Pharmaceuticals, Inc. | Związek do zastosowania w leczeniu dolegliwości związanych z receptorem s1p1 |
| US10245264B2 (en) | 2015-05-27 | 2019-04-02 | Merck Sharp & Dohme Corp. | Substituted imidazo[1,2-a]pyrazines as soluble guanylate cyclase activators |
| US10213429B2 (en) | 2015-05-28 | 2019-02-26 | Merck Sharp & Dohme Corp. | Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators |
| JP6838744B2 (ja) | 2015-06-22 | 2021-03-03 | アリーナ ファーマシューティカルズ, インコーポレイテッド | S1P1レセプター関連障害における使用のための(R)−2−(7−(4−シクロペンチル−3−(トリフルオロメチル)ベンジルオキシ)−1,2,3,4−テトラヒドロシクロペンタ[b]インドール−3−イル)酢酸(化合物1)の結晶性L−アルギニン塩 |
| EP3359191A4 (en) | 2015-10-05 | 2019-05-29 | Merck Sharp & Dohme Corp. | ANTIBODY PEPTIDE CONJUGATES WITH AGONISTEACTIVITY ON GLUCAGON RECEPTORS AND GLUCAGON-LIKE PEPTIDE-1 |
| WO2017107052A1 (en) | 2015-12-22 | 2017-06-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase stimulators |
| US10000458B2 (en) * | 2016-03-31 | 2018-06-19 | Sumitomo Chemical Company, Limited | Production method of 1, 2, 4-triazole compound |
| EP3235813A1 (en) | 2016-04-19 | 2017-10-25 | Cidqo 2012, S.L. | Aza-tetra-cyclo derivatives |
| WO2017197555A1 (en) | 2016-05-16 | 2017-11-23 | Merck Sharp & Dohme Corp. | Fused pyrazine derivatives useful as soluble guanylate cyclase stimulators |
| WO2017201683A1 (en) | 2016-05-25 | 2017-11-30 | Merck Sharp & Dohme Corp. | Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists |
| EP3496715B1 (en) | 2016-08-15 | 2021-11-03 | Merck Sharp & Dohme Corp. | Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease |
| WO2018034918A1 (en) | 2016-08-15 | 2018-02-22 | Merck Sharp & Dohme Corp. | Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease |
| WO2018057409A1 (en) | 2016-09-20 | 2018-03-29 | Merck Sharp & Dohme Corp. | Substituted 1-methyl-1,2,3,4-tetrahydroisoquinoline molecules as pcsk9 allosteric binders |
| KR20190078646A (ko) | 2016-11-18 | 2019-07-04 | 머크 샤프 앤드 돔 코포레이션 | 디아실글리세리드 o-아실트랜스퍼라제 2의 억제제로서 유용한 인다졸 유도체 |
| MX2019005679A (es) | 2016-11-18 | 2019-08-14 | Merck Sharp & Dohme | Derivados de indol de utilidad como inhibidores de diacilglicerido o-aciltransferasa 2. |
| WO2018107415A1 (en) | 2016-12-15 | 2018-06-21 | Merck Sharp & Dohme Corp. | Hydroxy isoxazole compounds useful as gpr120 agonists |
| AU2018220521A1 (en) | 2017-02-16 | 2019-09-05 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
| KR102859841B1 (ko) | 2018-06-06 | 2025-09-12 | 아레나 파마슈티칼스, 인크. | S1p1 수용체와 관련된 병태의 치료 방법 |
| JOP20190150A1 (ar) | 2018-06-21 | 2019-12-21 | Merck Sharp & Dohme | مركبات مناهضة لـ pcsk9 |
| US12220412B2 (en) | 2018-11-20 | 2025-02-11 | Sparrow Pharmaceuticals, Inc. | Methods for administering corticosteroids |
| US12331018B2 (en) | 2019-02-13 | 2025-06-17 | Merck Sharp & Dohme Llc | Pyrrolidine orexin receptor agonists |
| US11098029B2 (en) | 2019-02-13 | 2021-08-24 | Merck Sharp & Dohme Corp. | 5-alkyl pyrrolidine orexin receptor agonists |
| US12281109B2 (en) | 2019-04-04 | 2025-04-22 | Merck Sharp & Dohme Llc | Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes |
| WO2021026047A1 (en) | 2019-08-08 | 2021-02-11 | Merck Sharp & Dohme Corp. | Heteroaryl pyrrolidine and piperidine orexin receptor agonists |
| TW202123960A (zh) | 2019-08-30 | 2021-07-01 | 美商默沙東藥廠 | Pcsk9拮抗劑化合物 |
| EP3842060A1 (en) | 2019-12-23 | 2021-06-30 | Merck Sharp & Dohme Corp. | Stapled lactam co-agonists of the glucagon and glp-1 receptors |
| EP3842449A1 (en) | 2019-12-23 | 2021-06-30 | Merck Sharp & Dohme Corp. | Stapled olefin co-agonists of the glucagon and glp-1 receptors |
| EP3842061A1 (en) | 2019-12-23 | 2021-06-30 | Merck Sharp & Dohme Corp. | Stapled triazole co-agonists of the glucagon and glp-1 receptors |
| EP4153596A4 (en) | 2020-05-18 | 2024-08-14 | Merck Sharp & Dohme LLC | NOVEL DIACYLGLYCERIDE O-ACYLTRANSFERASE 2 INHIBITORS |
| MX2023001840A (es) | 2020-08-18 | 2023-03-13 | Merck Sharp & Dohme Llc | Agonistas de bicicloheptano pirrolidina de los receptores de orexina. |
| KR102445638B1 (ko) | 2020-09-03 | 2022-09-20 | 충남대학교산학협력단 | 11 알파 하이드록시프로게스테론을 포함하는 당뇨병 예방 또는 치료용 조성물 |
| PE20240217A1 (es) | 2020-10-08 | 2024-02-16 | Merck Sharp And Dohme Llc | Preparacion de derivados de oxindol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 |
| TW202229243A (zh) | 2020-10-08 | 2022-08-01 | 美商默沙東藥廠 | 作為新穎二醯基甘油酯o-醯基轉移酶2抑制劑之苯并咪唑酮衍生物的製備 |
| AU2022330007A1 (en) | 2021-08-19 | 2024-02-15 | Merck Sharp & Dohme Llc | Compounds for treating conditions related to pcsk9 activity |
| EP4525983A4 (en) | 2022-05-16 | 2025-09-03 | Sparrow Pharmaceuticals Inc | METHODS AND COMPOSITIONS FOR TREATING GLUCOCORTICOID EXCESS |
| 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 |
| CN119866342A (zh) | 2022-06-15 | 2025-04-22 | 默沙东有限责任公司 | 用于捕获白介素-1β的环肽 |
| IL321166A (en) | 2022-12-02 | 2025-07-01 | Merck Sharp & Dohme Llc | Preparation of fused azole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors |
| TW202540146A (zh) | 2023-11-14 | 2025-10-16 | 美商默沙東有限責任公司 | 用於捕捉介白素-1 β之環狀肽 |
| 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 |
| WO2026019977A1 (en) | 2024-07-19 | 2026-01-22 | Merck Sharp & Dohme Llc | Pyrrolopyridazine vegfr inhibitors |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW226993B (es) * | 1992-05-29 | 1994-07-21 | Kumiai Chemical Industry Co | |
| DE69824885T2 (de) | 1997-12-11 | 2005-07-21 | Janssen Pharmaceutica N.V. | Anilide als vitamin-a-säure-mimetika |
| 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 |
-
2003
- 2003-06-02 AR ARP030101960A patent/AR040241A1/es unknown
- 2003-06-03 MY MYPI20032060A patent/MY134664A/en unknown
- 2003-06-05 PE PE2003000565A patent/PE20040726A1/es not_active Application Discontinuation
- 2003-06-06 AU AU2003243420A patent/AU2003243420A1/en not_active Abandoned
- 2003-06-06 RU RU2004139063/04A patent/RU2319703C2/ru not_active IP Right Cessation
- 2003-06-06 PL PL03373372A patent/PL373372A1/xx not_active Application Discontinuation
- 2003-06-06 CA CA2488592A patent/CA2488592C/en not_active Expired - Fee Related
- 2003-06-06 UA UAA200500167A patent/UA81417C2/xx unknown
- 2003-06-06 AT AT03757385T patent/ATE537155T1/de active
- 2003-06-06 TW TW092115417A patent/TWI324153B/zh not_active IP Right Cessation
- 2003-06-06 NZ NZ536188A patent/NZ536188A/en not_active IP Right Cessation
- 2003-06-06 IL IL16525703A patent/IL165257A0/xx unknown
- 2003-06-06 BR BR0311137-7A patent/BR0311137A/pt not_active IP Right Cessation
- 2003-06-06 CN CNB03813392XA patent/CN1312137C/zh not_active Expired - Fee Related
- 2003-06-06 WO PCT/US2003/017898 patent/WO2003104207A2/en not_active Ceased
- 2003-06-06 KR KR10-2004-7019926A patent/KR20050008805A/ko not_active Ceased
- 2003-06-06 ES ES03757385T patent/ES2377200T3/es not_active Expired - Lifetime
- 2003-06-06 HR HR20041180A patent/HRP20041180A2/xx not_active Application Discontinuation
- 2003-06-06 CN CNA2007100037701A patent/CN1990474A/zh active Pending
- 2003-06-06 AU AU2003251410A patent/AU2003251410B2/en not_active Ceased
- 2003-06-06 JP JP2004511277A patent/JP4405384B2/ja not_active Expired - Fee Related
- 2003-06-06 WO PCT/US2003/017890 patent/WO2003104208A1/en not_active Ceased
- 2003-06-06 MX MXPA04012381A patent/MXPA04012381A/es not_active Application Discontinuation
- 2003-06-06 EP EP03757385A patent/EP1532122B1/en not_active Expired - Lifetime
- 2003-06-08 JO JO200365A patent/JO2315B1/en active
- 2003-06-09 US US10/457,682 patent/US6730690B2/en not_active Expired - Lifetime
- 2003-10-30 US US10/697,547 patent/US7179802B2/en not_active Expired - Lifetime
-
2004
- 2004-10-29 ZA ZA200408772A patent/ZA200408772B/xx unknown
- 2004-10-29 IS IS7519A patent/IS7519A/is unknown
- 2004-12-09 EC EC2004005482A patent/ECSP045482A/es unknown
-
2005
- 2005-01-05 MA MA28033A patent/MA27317A1/fr unknown
- 2005-01-07 NO NO20050102A patent/NO20050102L/no not_active Application Discontinuation
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR040241A1 (es) | Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia | |
| AR033306A1 (es) | Compuestos | |
| PE20030226A1 (es) | Compuestos arilicos sustituidos con quinuclidinas para el tratamiento de enfermedades | |
| NZ244429A (en) | Benzoxazole and benzothiazole derivatives, preparation and pharmaceutical compositions thereof | |
| PE20110598A1 (es) | Inhibidores de las enzimas de proteina cinasa activadas por mitogeno p38 | |
| RU2010126105A (ru) | Производные пиридина, замещенные гетероциклическим кольцом и фосфоноксиметильной группой, и содержащие их противогрибковые средства | |
| RU2009118602A (ru) | Производное индола | |
| AR072171A1 (es) | Derivados de nicotinamida, composicion farmaceutica que los comprende y su uso en combinaciones y en la preparacion de un medicamento para el tratamiento del asma. | |
| PE20080061A1 (es) | Compuestos derivados de amida como inhibidores de los canales de potasio task-1 y task-3 | |
| EP1243582A4 (en) | CHINOLINE AND CHINAZOLINE DERIVATIVES AND MEDICATIONS CONTAINING THEM | |
| BRPI0409110A (pt) | derivados de 4-(4-heterociclilalcoxi)fenil-1-(heterociclil-carboni l)piridina e compostos relacionados como antagonistas de histamina h3 para o tratamento de doenças neurológicas tais como alzheimer | |
| AR042469A1 (es) | Derivados de triazol como inhibidores de 11- beta - hidroxiesteroide deshidrogenasa - 1 | |
| AR035260A1 (es) | Derivados de piperidina amino sustituidas, composiciones farmaceuticas y el uso de dichos derivados para la preparacion de medicamentos como inhibidores de la gama secretasa, y para el tratamiento de la enfermedad de alzheimer | |
| RU2006146070A (ru) | Циннамидное соединение | |
| PE20060076A1 (es) | Antagonistas del receptor de acetilcolina muscarinico | |
| RU2008112691A (ru) | Азотсодержащее гетероциклическое соединение и его фармацевтическое применение | |
| PE20081782A1 (es) | Agonistas de adrenoreceptores alfa2c | |
| AR062299A1 (es) | Derivados de bencimidazol | |
| AR031526A1 (es) | Nuevas fenilpiperazinas, composiciones farmaceuticas que las contienen, metodos para preparar los compuestos y las composiciones y uso de los compuestos en la preparacion de un medicamento. | |
| AR074128A1 (es) | Derivados de 4-[2-(2-fluorofenoximetil)fenil] piperidina, composiciones farmaceuticas que los contienen, metodo de preparacion, compuestos intermediarios de dicho proceso y uso de los mismos para el tratamiento de dolores neuropaticos, mal de alzheimer y otras enfermedades relacionadas con el snc. | |
| RU2011108008A (ru) | Производные трициклического алкиламинометилоксазолидинона | |
| AR005279A1 (es) | Derivados 1-(piperidinil 1,2-disustituido)-4-(bencimidazolil e imidazopiridinil)-piperidina, proceso para su preparacion, composicion farmaceutica, y proceso para preparar dicha composicion | |
| PE20070212A1 (es) | Heterociclos de 1,4-dihidropiridina-condensados, procesos para preparar los mismos, uso y composiciones que los contienen | |
| RU2007128080A (ru) | Производные пирролидиния в качестве мускариновых рецепторов мз | |
| AR048319A1 (es) | Derivados de n-piperidina como moduladores de ccr3 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |