AR074109A1 - Pirrolidinas heterociclicas agonistas de receptores de la melanocortina, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de la obesidad, diabetes y disfuncion erectil. - Google Patents
Pirrolidinas heterociclicas agonistas de receptores de la melanocortina, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de la obesidad, diabetes y disfuncion erectil.Info
- Publication number
- AR074109A1 AR074109A1 ARP090104355A ARP090104355A AR074109A1 AR 074109 A1 AR074109 A1 AR 074109A1 AR P090104355 A ARP090104355 A AR P090104355A AR P090104355 A ARP090104355 A AR P090104355A AR 074109 A1 AR074109 A1 AR 074109A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- unsubstituted
- hydroxy
- group
- trifluoromethyl
- Prior art date
Links
- 208000010228 Erectile Dysfunction Diseases 0.000 title 1
- 208000008589 Obesity Diseases 0.000 title 1
- 239000000556 agonist Substances 0.000 title 1
- 206010012601 diabetes mellitus Diseases 0.000 title 1
- 201000001881 impotence Diseases 0.000 title 1
- 235000020824 obesity Nutrition 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 125000005843 halogen group Chemical group 0.000 abstract 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- -1 hydroxy, mercapto Chemical group 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P3/08—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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Reproductive Health (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Hydrogenated Pyridines (AREA)
- Pyrrole Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto de la formula (1) caracterizado porque: R1 representa H, o representa alquilo C1-10, cicloalquilo C3-7, arilo C6-10, un heterociclo o un heteroarilo, cada uno de los cuales es insustituido o sustituido con por lo menos un sustituyente seleccionado entre el grupo que consiste en halogeno, amino, alquilo C1-4, trifluorometilo, hidroxi, alcoxi C1-4, ciano y oxo; R2 representa fenilo o un heteroarilo de 6 miembros, cada uno de los cuales es insustituido o mono- o disustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halogeno, hidroxi, alquilo C1-4, alcoxi C1-4, ciano y amino; R3 representa H, o representa alquilo C1-6 o cicloalquilo C3-7, cada uno de los cuales es insustituido o sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halogeno, metilo, trifluorometilo, hidroxi y amino; R4 representa cicloalquilo C4-7 o un heterociclo monocíclico, cada uno de los cuales es insustituido o mono- o poli-sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halogeno, hidroxi, alquilo C1-4, trifluorometilo, alcoxi C1-4 y oxo; o representa fenilo o un heteroarilo de seis miembros, cada uno de los cuales es insustituido o mono- o di-sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halogeno, hidroxi, alquilo C1-4, trifluorometilo, alcoxi C1-4 y amino; y R5 representa alquilo C1-6, difluorometilo, trifluorometilo, cicloalquilo C3-6, amino, alquilamino C1-4, di-alquilo C1-4amino, fenilo, un heteroarilo monocíclico o un heterociclo monocíclico en donde el alquilo es insustituido o sustituido con por lo menos un sustituyente seleccionado entre el grupo que consiste en fluoro, hidroxi, mercapto, alcoxi C1-4, acetoxi, amino, acetilamino, ciano, carbamoilo, dimetil carbamoilo y oxo y fenilo o el heteroarilo es insustituido o mono- o di- sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halogeno, hidroxi, metilo, trifluorometilo, metoxi y amino, o una sal farmacéuticamente aceptable o un isomero del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR20080112403 | 2008-11-12 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR074109A1 true AR074109A1 (es) | 2010-12-22 |
Family
ID=42165801
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090104355A AR074109A1 (es) | 2008-11-12 | 2009-11-11 | Pirrolidinas heterociclicas agonistas de receptores de la melanocortina, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de la obesidad, diabetes y disfuncion erectil. |
Country Status (26)
Country | Link |
---|---|
US (4) | US8288386B2 (es) |
EP (1) | EP2350060B1 (es) |
JP (1) | JP5399506B2 (es) |
KR (1) | KR101141976B1 (es) |
CN (1) | CN102282141B (es) |
AR (1) | AR074109A1 (es) |
AU (1) | AU2009314827B2 (es) |
BR (1) | BRPI0921063B8 (es) |
CA (1) | CA2742248C (es) |
CL (1) | CL2011001073A1 (es) |
CO (1) | CO6362006A2 (es) |
CR (1) | CR20110250A (es) |
EA (1) | EA019146B1 (es) |
EC (1) | ECSP11011026A (es) |
GE (1) | GEP20135850B (es) |
IL (1) | IL212468A0 (es) |
MA (1) | MA32774B1 (es) |
MX (1) | MX2011004583A (es) |
NZ (1) | NZ592512A (es) |
PE (1) | PE20110684A1 (es) |
TN (1) | TN2011000222A1 (es) |
TW (1) | TWI389903B (es) |
UA (1) | UA99555C2 (es) |
UY (1) | UY32238A (es) |
WO (1) | WO2010056022A2 (es) |
ZA (1) | ZA201103154B (es) |
Families Citing this family (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UA99555C2 (en) * | 2008-11-12 | 2012-08-27 | Элджи Лайф Саенсез Лтд. | Melanocortin receptor agonists |
US9018395B2 (en) | 2011-01-27 | 2015-04-28 | Université de Montréal | Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators |
PL3539551T3 (pl) | 2011-12-29 | 2022-02-21 | Rhythm Pharmaceuticals, Inc. | Sposób leczenia zaburzeń związanych z receptorem melanokortyny 4 u heterozygotycznych nosicieli |
JP6235560B2 (ja) | 2012-04-25 | 2017-11-22 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | (3,4−ジクロロ−フェニル)−((s)−3−プロピル−ピロリジン−3−イル)−メタノン塩酸塩及び製造方法 |
CN103420981A (zh) * | 2012-05-21 | 2013-12-04 | 中国医学科学院药物研究所 | 含有取代吡咯烷基的硫代吗啉类化合物 |
CA3000670A1 (en) | 2015-09-30 | 2017-04-06 | Rhythm Pharmaceuticals, Inc. | Method of treating melanocortin-4 receptor pathway-associated disorders |
WO2019195756A1 (en) | 2018-04-06 | 2019-10-10 | Rhythm Pharmaceuticals, Inc. | Compositions for treating kidney disease |
ES2970510T3 (es) * | 2019-11-07 | 2024-05-29 | Lg Chemical Ltd | Agonistas del receptor de melanocortina-4 |
IL302425A (en) * | 2020-10-29 | 2023-06-01 | Lg Chemical Ltd | An amorphous form of a melanocortin receptor agonist and a method for its preparation |
MX2023004656A (es) * | 2020-10-29 | 2023-05-18 | Lg Chemical Ltd | Forma cristalina ii del compuesto agonista de receptor de melanocortina y metodo de preparacion para la misma. |
JP2023548327A (ja) | 2020-10-29 | 2023-11-16 | エルジー・ケム・リミテッド | メラノコルチン受容体アゴニスト化合物の結晶形iおよびその製造方法 |
WO2022092913A1 (ko) * | 2020-10-29 | 2022-05-05 | 주식회사 엘지화학 | 멜라노코르틴 수용체 작용제 화합물의 결정형 ⅲ 및 이의 제조방법 |
WO2022092914A1 (ko) | 2020-10-29 | 2022-05-05 | 주식회사 엘지화학 | 멜라노코르틴 수용체 작용제 화합물의 결정형 ⅳ 및 이의 제조방법 |
WO2022139444A1 (ko) * | 2020-12-22 | 2022-06-30 | 주식회사 엘지화학 | 멜라노코르틴 수용체 작용제 화합물의 결정형 ⅱ 및 이의 제조방법 |
TWI832128B (zh) * | 2020-12-22 | 2024-02-11 | 南韓商Lg化學股份有限公司 | 使用作為黑皮質素-4受體選擇性促效劑 |
JP2024501829A (ja) * | 2020-12-22 | 2024-01-16 | エルジー・ケム・リミテッド | メラノコルチン受容体アゴニスト化合物の結晶形iiiおよびその製造方法 |
US20240043407A1 (en) * | 2020-12-22 | 2024-02-08 | Lg Chem, Ltd. | Crystalline form i of melanocortin receptor agonist compound and method for preparing same |
US20240059652A1 (en) | 2020-12-22 | 2024-02-22 | Lg Chem, Ltd. | Amorphous melanocortin receptor agonist and method for preparing same |
AU2022209657A1 (en) * | 2021-01-21 | 2023-07-20 | Lg Chem, Ltd. | Uses of melanocortin-4 receptor agonist |
JP2024508469A (ja) * | 2021-02-26 | 2024-02-27 | エルジー・ケム・リミテッド | メラノコルチン-4受容体アゴニスト |
MX2023013042A (es) | 2021-05-06 | 2023-11-15 | Lg Chemical Ltd | Forma cristalina vii de un compuesto agonista del receptor de melanocortina, y metodo para preparar la misma. |
MX2023013044A (es) | 2021-05-06 | 2023-11-15 | Lg Chemical Ltd | Forma cristalina v del compuesto agonista del receptor de melanocortina y metodo para preparar la misma. |
AU2022271120A1 (en) | 2021-05-07 | 2023-11-09 | Lg Chem, Ltd. | Crystal form iv of organic acid salts of melanocortin receptor agonist compound, and preparation method thereof |
WO2022235103A1 (ko) * | 2021-05-07 | 2022-11-10 | 주식회사 엘지화학 | 멜라노코르틴 수용체 작용제 화합물의 황산염의 결정형 및 이의 제조방법 |
JP2024516739A (ja) | 2021-05-07 | 2024-04-16 | エルジー・ケム・リミテッド | メラノコルチン受容体アゴニスト化合物とバニリンの共結晶およびその製造方法 |
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