AR064026A1 - Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasa - Google Patents
Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasaInfo
- Publication number
- AR064026A1 AR064026A1 ARP070105302A ARP070105302A AR064026A1 AR 064026 A1 AR064026 A1 AR 064026A1 AR P070105302 A ARP070105302 A AR P070105302A AR P070105302 A ARP070105302 A AR P070105302A AR 064026 A1 AR064026 A1 AR 064026A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- group
- heteroaryl
- independently
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 8
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 5
- 229910052731 fluorine Inorganic materials 0.000 abstract 5
- 239000011737 fluorine Substances 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001624 naphthyl group Chemical group 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 abstract 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000004930 Fatty Liver Diseases 0.000 abstract 1
- 206010022489 Insulin Resistance Diseases 0.000 abstract 1
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- -1 hydroxy, cyano, amino Chemical group 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 230000004060 metabolic process Effects 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- KIWSYRHAAPLJFJ-DNZSEPECSA-N n-[(e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enyl]pyridine-3-carboxamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/CNC(=O)C1=CC=CN=C1 KIWSYRHAAPLJFJ-DNZSEPECSA-N 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
Son de utilidad para la prevencion y tratamiento de afecciones relacionadas con la síntesis y metabolismo anormales de lípidos, incluidas enfermedades cardiovasculares, tales como aterosclerosis; obesidad; diabetes; enfermedad neurologica; síndrome metabolico; resistencia a insulina; y esteatosis hepática. Reivindicacion 1: Un compuesto de la formula estructural 1: o una sal farmacéuticamente aceptable de la misma; en la que: q es 0 o 1; r es 0 o 1; Z es O, S, o NR4; X-Y es N-C(O), N-CRaRb, CR14-O, CR14-S(O)0-2, o CR13-CRaRb; Ra y Rb son cada uno independientemente hidrogeno o alquilo C1-3, en los que el alquilo está opcionalmente sustituido con de uno a tres sustituyentes que se seleccionan independientemente a partir de fluor e hidroxi; W es heteroarilo que se selecciona del grupo constituido por el grupo de formulas (2); R1 es heteroarilo que se selecciona del grupo constituido por el grupo de formulas (3) en el que RC es -(CH2)mCO2H, -(CH2)mCO2alquilo C1-3, -(CH2)m-Z- (CH2)pCO2H, o -(CH2)m-Z-(CH2)pCO2alquilo C1-3; en el que cualquier átomo de carbono de los grupos metileno (CH2) de (CH2)m o (CH2)p está opcionalmente sustituido con un hidroxi, un amino o uno u dos átomos de fluor; y en el que dicho anillo heteroarilo R1 está opcionalmente sustituido con un sustituyente que se selecciona independientemente a partir del grupo constituido por ciano, halogeno, alquilo C1-4, alcoxi C1-4, alquiltio C1-4, alquilsulfonilo C1-4, y trifluorometilo; cada R2 se selecciona independientemente a partir del grupo constituido por: hidrogeno, halogeno, hidroxi, ciano, amino, nitro, alquilo C1-4, opcionalmente sustituido con de uno a cinco átomos de fluor, alcoxi C1-4, opcionalmente sustituido con de uno a cinco átomos de fluor, alquiltio C1-4, opcionalmente sustituido con de uno a cinco átomos de fluor, alquil C1-4 sulfonilo, carboxi, alquiloxi C1-4 carbonilo, y alquil C1-4 carbonilo; Ar es fenilo, naftilo, o heteroarilo opcionalmente sustituido con de uno a cinco sustituyentes R3; cada R3 se selecciona Independientemente a partir del grupo constituido por: alquilo C1-6, alquenilo C2-6, (CH2)n-fenilo, (CH2)n-naftilo, (CH2)n-heteroarilo, (CH2)n-heterociclilo, (CH2)n-cicloalquilo 3-7, halogeno, nitro, (CH2)nOR4, (CH2)nN(R4)2, (CH2)nC:::N, (CH2)nCO2R4, (CH2)NR4SO2R4, (CH2)nSO2N(R4)2, (CH2)nS(O)0-2R4, (CH2)nNR4C(O)N(R4)2, (CH2)nC(O)N(R4)2, (CH2)nNR4C(O)R4, (CH2)nNR4CO2R4, (CH2)nC(O)R4, O(CH2)nC(O)N(R4)2, (CH2)s-Z-(CH2)t-fenilo, (CH2)s-Z-(CH2)t- naftilo, (CH2)s-Z-(CH2)t-heteroarilo, (CH2)s-Z-(CH2)t-heterociclilo, (CH2)s-Z-(CH2)t-cicIoalquilo C3-7, (CH2)s-Z-(CH2)t-OR4, (CH2)s-Z-(CH2)t-N(R4)2, (CH2)s-Z-(CH2)t-NR4SO2R4, (CH2)s-Z-(CH2)t-C:::N, (CH2)s-Z-(CH2)t-CO2R4, (CH2)s-Z-(CH2)t-SO2N(R4)2, (CH2)s-Z-(CH2)t-S(O)0-2R4, (CH2)s-Z-(CH2)t-NR4C(O)N(R4)2, (CH2)s-Z-(CH2)t-C(O)N(R4)2, (CH2)s-Z-(CH2)t-NR4C(O)R4, (CH2)s-Z-(CH2)t-NR4CO2R4, (CH2)s-Z-(CH2)t-C(O)R4, CF3, CH2CF3, OCF3, y OCH2CF3; en el que fenilo, naftilo, heteroarilo, cicloalquilo, y heterociclilo están opcionalmente sustituidos con de uno a tres sustituyentes que se seleccionan independientemente a partir de halogeno, hidroxi, alquilo C1-4, trifluorometilo, y alcoxi C1-4, opcionalmente sustituido con de uno a cinco átomos de fluor y en el que cualquier átomo de carbono de un metileno (CH2) de R3 está opcionalmente sustituido con de uno a dos grupos que se seleccionan independientemente a partir de fluor, hidroxi, y alquilo C1-4; o dos sustituyentes cuando están en ci mismo grupo metileno (CH2) se toman conjuntamente con el átomo de carbono al que están unidos formando un grupo ciclopropilo; cada R4 se selecciona independientemente a partir del grupo constituido por hidrogeno, alquilo C1-6, (CH2)n-fenilo, (CH2)n- heteroarilo, (CH2)n-naftilo, y (CH2)ncicloalquilo C3-7, en el que alquilo, fenilo, heteroarilo, y cicloalquilo están opcionalmente sustituidos con de uno a tres grupos que se seleccionan independientemente a partir de halogeno, alquilo C1-4 y alcoxi C1-4, o dos grupos R4 junto con el átomo al que están unidos forman un sistema anular cíclico monociclico o bicíclico de 4 a 8 miembros que opcionalmente contiene un heteroátomo adicional que se selecciona a partir de O, S, NH, y Nalquilo C1-4; R5, R6, R7, R8, R9, R10, R11, y R12 son cada uno independientemente hidrogeno, fluor, o alquilo C1-3, en los que el alquilo está opcionalmente sustituido con de uno a tres sustituyentes que se seleccionan independientemente a partir de fluor e hidroxi; R13 es hidrogeno, alquilo C1-3, fluor, o hidroxi; cada R14 es hidrogeno o alquilo C1-3; cada m es independientemente un numero entero de 0 a 4; cada p es independientemente un numero entero de 1 a 3; cada n es independientemente un numero entero de 0 a 2; cada s es independientemente un numero entero de 1 a 3; y cada t es independientemente un numero entero de 1 a 3.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87221606P | 2006-12-01 | 2006-12-01 | |
| US89890007P | 2007-02-01 | 2007-02-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR064026A1 true AR064026A1 (es) | 2009-03-04 |
Family
ID=39467388
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070105302A AR064026A1 (es) | 2006-12-01 | 2007-11-29 | Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasa |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US8063224B2 (es) |
| EP (1) | EP2099793B1 (es) |
| JP (1) | JP5050061B2 (es) |
| KR (1) | KR20090086623A (es) |
| AR (1) | AR064026A1 (es) |
| AT (1) | ATE543816T1 (es) |
| AU (1) | AU2007327276B2 (es) |
| BR (1) | BRPI0719702A2 (es) |
| CA (1) | CA2670703C (es) |
| CL (1) | CL2007003440A1 (es) |
| CO (1) | CO6190521A2 (es) |
| CR (1) | CR10858A (es) |
| EA (1) | EA200970524A1 (es) |
| EC (1) | ECSP099375A (es) |
| GT (1) | GT200900144A (es) |
| IL (1) | IL198824A0 (es) |
| MA (1) | MA31017B1 (es) |
| MX (1) | MX2009005713A (es) |
| NO (1) | NO20092469L (es) |
| PE (1) | PE20081199A1 (es) |
| SV (1) | SV2009003275A (es) |
| TN (1) | TN2009000212A1 (es) |
| TW (1) | TW200826936A (es) |
| WO (1) | WO2008064474A1 (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2398940C (en) * | 2000-02-24 | 2012-02-21 | Xenon Genetics, Inc. | Methods and compositions using stearoyl-coa desaturase to identify triglyceride reducing therapeutic agents |
| JP2009537571A (ja) * | 2006-05-22 | 2009-10-29 | メルク フロスト カナダ リミテツド | ステアロイル−コエンザイムaデルタ−9デサチュラーゼのインヒビターとしての環状アミン誘導体 |
| WO2007143823A1 (en) * | 2006-06-12 | 2007-12-21 | Merck Frosst Canada Ltd. | Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| EP2032570A4 (en) | 2006-06-13 | 2010-10-27 | Merck Frosst Canada Ltd | AZACYCLOPENTATE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME-A-DELTA-9-DESATURASE |
| AU2007283401A1 (en) * | 2006-08-09 | 2008-02-14 | Merck Frosst Canada Ltd. | Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme A delta-9 desaturase |
| AR064965A1 (es) | 2007-01-26 | 2009-05-06 | Merck Frosst Canada Inc | Derivados de azacicloalcanos como inhibidores de estearoil - coenzima a delta -9 desaturasa |
| EP2148878A4 (en) * | 2007-04-20 | 2011-08-10 | Merck Canada Inc | NEW HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME-A-DELTA-9-DESATURASE |
| EP2152719A4 (en) * | 2007-05-23 | 2011-01-19 | Merck Frosst Canada Ltd | BICYCLIC HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME-A-DELTA-9-DESATURASE |
| WO2008157844A1 (en) | 2007-06-21 | 2008-12-24 | Forest Laboratories Holdings Limited | Novel piperazine derivatives as inhibitors of stearoyl-coa desaturase |
| JO3272B1 (ar) * | 2007-07-19 | 2018-09-16 | Takeda Pharmaceuticals Co | مستحضر صلب يشمل ألوجليبتين وميتفورمين هيدروكلوريد |
| CA2693290A1 (en) * | 2007-07-20 | 2009-01-29 | Merck Frosst Canada Ltd. | Bicyclic heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| JP2012501975A (ja) * | 2008-09-08 | 2012-01-26 | メルク カナダ インコーポレイテッド | ステアロイルコエンザイムAδ−9デサチュラーゼの阻害剤としての芳香族複素環化合物 |
| AU2010215035B2 (en) * | 2009-02-17 | 2014-06-12 | Merck Canada Inc. | Novel spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase |
| AU2010215041A1 (en) * | 2009-02-23 | 2011-07-28 | Merck Canada Inc. | Heterocyclic derivatives as inhibitors of stearoyl-coenzyme A delta-9 desaturase |
| WO2010108268A1 (en) * | 2009-03-23 | 2010-09-30 | Merck Frosst Canada Ltd. | Heterocyclic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| EP2459568A4 (en) | 2009-07-28 | 2013-02-27 | Merck Frosst Canada Ltd | NEW SPIRO COMPOUNDS AS AN INHIBITORS OF STEAROYL COENZYME A DELTA 9 DESATURASE |
| WO2011134969A1 (de) | 2010-04-28 | 2011-11-03 | Bayer Cropscience Ag | Ketoheteroarylpiperidin und -piperazin derivate als fungizide |
| PL2668182T3 (pl) * | 2011-01-28 | 2018-11-30 | Immunic Ag | Inhibitowanie IL17 i IFN-gamma do leczenia zapalenia autoimmunologicznego |
| EP2766000A2 (en) | 2011-10-15 | 2014-08-20 | F.Hoffmann-La Roche Ag | Scd1 antagonists for treating cancer |
| WO2013062882A1 (en) * | 2011-10-26 | 2013-05-02 | Merck Canada Inc. | Scd inhibitors for the treatment of hcv |
| WO2013134546A1 (en) | 2012-03-07 | 2013-09-12 | Mayo Foundation For Medical Education And Research | Methods and materials for treating cancer |
| JP6293127B2 (ja) | 2012-05-22 | 2018-03-14 | イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブリュー ユニバーシティー オブ エルサレム リミテッド | 未分化細胞の選択的阻害剤 |
| US10301273B2 (en) | 2014-08-07 | 2019-05-28 | Mayo Foundation For Medical Education And Research | Compounds and methods for treating cancer |
| US11970486B2 (en) | 2016-10-24 | 2024-04-30 | Janssen Pharmaceutica Nv | Compounds and uses thereof |
| JP2020514293A (ja) | 2017-01-06 | 2020-05-21 | ユマニティ セラピューティクス,インコーポレーテッド | 神経障害を治療する方法 |
| CA3083000A1 (en) | 2017-10-24 | 2019-05-02 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
| EP3768269B1 (en) | 2018-03-23 | 2025-08-20 | Janssen Pharmaceutica NV | Compounds and uses thereof |
| MX2021008903A (es) | 2019-01-24 | 2021-11-04 | Yumanity Therapeutics Inc | Compuestos y usos de los mismos. |
| EA202192047A1 (ru) | 2019-11-13 | 2021-12-08 | Юманити Терапьютикс, Инк. | Соединения и их применение |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1595923A1 (de) * | 1965-02-20 | 1969-11-27 | Merck Ag E | 1-Aralkyl-4-(thiazolyl-2)-piperazine und Verfahren zu ihrer Herstellung |
| JP4169368B2 (ja) | 1996-01-15 | 2008-10-22 | 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 | 脈管形成阻害性ピリダジンアミン |
| US20050119251A1 (en) | 2001-12-21 | 2005-06-02 | Jian-Min Fu | Nicotinamide derivatives and their use as therapeutic agents |
| US7754711B2 (en) | 2003-07-30 | 2010-07-13 | Xenon Pharmaceuticals Inc. | Pyridazine derivatives and their use as therapeutic agents |
| US7514436B2 (en) | 2003-07-30 | 2009-04-07 | Xenon Pharmaceuticals Inc. | Pyridazine derivatives and their use as therapeutic agents |
| US7345043B2 (en) | 2004-04-01 | 2008-03-18 | Miikana Therapeutics | Inhibitors of histone deacetylase |
| CN101084212A (zh) | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 杂环衍生物及其作为硬脂酰CoA去饱和酶介导剂的用途 |
| TW200626138A (en) | 2004-09-20 | 2006-08-01 | Xenon Pharmaceuticals Inc | Heterocyclic derivatives and their use as therapeutic agents |
| BRPI0515477A (pt) | 2004-09-20 | 2008-07-22 | Xenon Pharmaceuticals Inc | derivados heterocìclicos bicìclicos e o uso dos mesmos como inibidores de estaroil-coa-desaturase (scd) |
| CA2580857A1 (en) | 2004-09-20 | 2006-09-28 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| MX2007003319A (es) | 2004-09-20 | 2007-06-05 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como agentes terapeuticos. |
| CA2580855A1 (en) * | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| US8071603B2 (en) | 2004-09-20 | 2011-12-06 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors |
| MX2007003318A (es) * | 2004-09-20 | 2007-05-18 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como agentes terapeuticos. |
| GT200600046A (es) | 2005-02-09 | 2006-09-25 | Terapia de combinacion | |
| WO2006125181A2 (en) | 2005-05-19 | 2006-11-23 | Xenon Pharmaceuticals Inc. | Piperidine derivatives and their use as stearoyl-coa desaturase modulators |
| EP1902051A1 (en) * | 2005-06-09 | 2008-03-26 | Merck Frosst Canada Ltd. | Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| CA2615045A1 (en) | 2005-07-20 | 2007-01-25 | Merck Frosst Canada Ltd. | Heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| JP2009510132A (ja) | 2005-10-05 | 2009-03-12 | メルク フロスト カナダ リミテツド | ロイコトリエン生合成の阻害剤としての置換キノリン |
| EP1951731A4 (en) | 2005-11-15 | 2010-07-07 | Merck Frosst Canada Ltd | AZACYCLOHEXANDERIVATES AS INHIBITORS OF STEAROYL-COENZYME-A-DELTA-9-DESATURASE |
| EP1966183A4 (en) | 2005-12-20 | 2010-12-29 | Merck Frosst Canada Ltd | HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A-DELTA-9-DESATURASE |
| JP2009537571A (ja) | 2006-05-22 | 2009-10-29 | メルク フロスト カナダ リミテツド | ステアロイル−コエンザイムaデルタ−9デサチュラーゼのインヒビターとしての環状アミン誘導体 |
| WO2007143823A1 (en) | 2006-06-12 | 2007-12-21 | Merck Frosst Canada Ltd. | Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| EP2032570A4 (en) | 2006-06-13 | 2010-10-27 | Merck Frosst Canada Ltd | AZACYCLOPENTATE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME-A-DELTA-9-DESATURASE |
| AU2007283401A1 (en) | 2006-08-09 | 2008-02-14 | Merck Frosst Canada Ltd. | Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme A delta-9 desaturase |
| JP2010506859A (ja) | 2006-10-20 | 2010-03-04 | メルク フロスト カナダ リミテツド | ステアロイル−コエンザイムaデルタ−9デサチュラーゼの阻害剤としてのアザシクロアルカン誘導体 |
| AR064965A1 (es) | 2007-01-26 | 2009-05-06 | Merck Frosst Canada Inc | Derivados de azacicloalcanos como inhibidores de estearoil - coenzima a delta -9 desaturasa |
-
2007
- 2007-11-26 TW TW096144835A patent/TW200826936A/zh unknown
- 2007-11-28 WO PCT/CA2007/002139 patent/WO2008064474A1/en not_active Ceased
- 2007-11-28 EA EA200970524A patent/EA200970524A1/ru unknown
- 2007-11-28 JP JP2009538560A patent/JP5050061B2/ja not_active Expired - Fee Related
- 2007-11-28 BR BRPI0719702-0A patent/BRPI0719702A2/pt not_active IP Right Cessation
- 2007-11-28 AT AT07845603T patent/ATE543816T1/de active
- 2007-11-28 EP EP07845603A patent/EP2099793B1/en active Active
- 2007-11-28 KR KR1020097013826A patent/KR20090086623A/ko not_active Ceased
- 2007-11-28 MX MX2009005713A patent/MX2009005713A/es unknown
- 2007-11-28 CA CA2670703A patent/CA2670703C/en not_active Expired - Fee Related
- 2007-11-28 AU AU2007327276A patent/AU2007327276B2/en not_active Ceased
- 2007-11-29 CL CL200703440A patent/CL2007003440A1/es unknown
- 2007-11-29 AR ARP070105302A patent/AR064026A1/es not_active Application Discontinuation
- 2007-11-30 PE PE2007001699A patent/PE20081199A1/es not_active Application Discontinuation
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2009
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- 2009-05-27 SV SV2009003275A patent/SV2009003275A/es unknown
- 2009-05-28 CO CO09054946A patent/CO6190521A2/es not_active Application Discontinuation
- 2009-05-29 TN TNP2009000212A patent/TN2009000212A1/fr unknown
- 2009-06-01 EC EC2009009375A patent/ECSP099375A/es unknown
- 2009-06-10 CR CR10858A patent/CR10858A/es unknown
- 2009-06-22 MA MA32023A patent/MA31017B1/fr unknown
- 2009-06-30 NO NO20092469A patent/NO20092469L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CO6190521A2 (es) | 2010-08-19 |
| JP2010510993A (ja) | 2010-04-08 |
| EP2099793A1 (en) | 2009-09-16 |
| TN2009000212A1 (en) | 2010-10-18 |
| JP5050061B2 (ja) | 2012-10-17 |
| CA2670703C (en) | 2012-05-15 |
| GT200900144A (es) | 2011-06-23 |
| CL2007003440A1 (es) | 2008-04-04 |
| PE20081199A1 (es) | 2008-10-19 |
| US8063224B2 (en) | 2011-11-22 |
| ATE543816T1 (de) | 2012-02-15 |
| MA31017B1 (fr) | 2009-12-01 |
| AU2007327276A1 (en) | 2008-06-05 |
| TW200826936A (en) | 2008-07-01 |
| KR20090086623A (ko) | 2009-08-13 |
| BRPI0719702A2 (pt) | 2013-12-17 |
| EA200970524A1 (ru) | 2009-12-30 |
| SV2009003275A (es) | 2009-11-18 |
| EP2099793A4 (en) | 2010-12-29 |
| US20080132542A1 (en) | 2008-06-05 |
| WO2008064474A1 (en) | 2008-06-05 |
| CA2670703A1 (en) | 2008-06-05 |
| IL198824A0 (en) | 2010-02-17 |
| AU2007327276B2 (en) | 2011-06-09 |
| MX2009005713A (es) | 2009-06-08 |
| NO20092469L (no) | 2009-08-27 |
| EP2099793B1 (en) | 2012-02-01 |
| ECSP099375A (es) | 2009-07-31 |
| CR10858A (es) | 2009-06-25 |
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