CL2022003503A1 - Antagonistas del receptor de melanocortina y usos de estos. - Google Patents
Antagonistas del receptor de melanocortina y usos de estos.Info
- Publication number
- CL2022003503A1 CL2022003503A1 CL2022003503A CL2022003503A CL2022003503A1 CL 2022003503 A1 CL2022003503 A1 CL 2022003503A1 CL 2022003503 A CL2022003503 A CL 2022003503A CL 2022003503 A CL2022003503 A CL 2022003503A CL 2022003503 A1 CL2022003503 A1 CL 2022003503A1
- Authority
- CL
- Chile
- Prior art keywords
- compounds
- receptor antagonists
- salts
- melanocortin receptor
- anorexia
- Prior art date
Links
- 229940122534 Melanocortin receptor antagonist Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 150000003839 salts Chemical class 0.000 abstract 4
- 208000000103 Anorexia Nervosa Diseases 0.000 abstract 1
- 206010006895 Cachexia Diseases 0.000 abstract 1
- 101000978418 Homo sapiens Melanocortin receptor 4 Proteins 0.000 abstract 1
- 102100023724 Melanocortin receptor 4 Human genes 0.000 abstract 1
- 208000022531 anorexia Diseases 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 206010061428 decreased appetite Diseases 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/20—Spiro-condensed systems
-
- 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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Otolaryngology (AREA)
- Hospice & Palliative Care (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Described herein are compounds of Formula I and their pharmaceutically acceptable salts, wherein R1, R2, R3, X1, Y1, Y2, Y3, Y4 and Y5 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063036798P | 2020-06-09 | 2020-06-09 | |
| US202163167271P | 2021-03-29 | 2021-03-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2022003503A1 true CL2022003503A1 (es) | 2023-09-01 |
Family
ID=76422026
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2022003503A CL2022003503A1 (es) | 2020-06-09 | 2022-12-09 | Antagonistas del receptor de melanocortina y usos de estos. |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US11643412B2 (es) |
| EP (1) | EP4161927A1 (es) |
| JP (1) | JP7288554B1 (es) |
| KR (1) | KR20230011968A (es) |
| CN (1) | CN116113635A (es) |
| AU (1) | AU2021289169B2 (es) |
| BR (1) | BR112022024527A2 (es) |
| CA (1) | CA3186348A1 (es) |
| CL (1) | CL2022003503A1 (es) |
| CO (1) | CO2022017790A2 (es) |
| CR (1) | CR20220632A (es) |
| DO (1) | DOP2022000281A (es) |
| EC (1) | ECSP22093794A (es) |
| IL (1) | IL298891A (es) |
| MX (1) | MX2022015706A (es) |
| PE (1) | PE20231215A1 (es) |
| UY (1) | UY39260A (es) |
| WO (1) | WO2021250541A1 (es) |
| ZA (1) | ZA202213427B (es) |
Family Cites Families (38)
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|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| CA1146866A (en) | 1979-07-05 | 1983-05-24 | Yamanouchi Pharmaceutical Co. Ltd. | Process for the production of sustained release pharmaceutical composition of solid medical material |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| DE3438830A1 (de) | 1984-10-23 | 1986-04-30 | Rentschler Arzneimittel | Nifedipin enthaltende darreichungsform und verfahren zu ihrer herstellung |
| US5013556A (en) | 1989-10-20 | 1991-05-07 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
| WO1992018106A1 (en) | 1991-04-16 | 1992-10-29 | Nippon Shinyaku Co., Ltd. | Method of manufacturing solid dispersion |
| US5340591A (en) | 1992-01-24 | 1994-08-23 | Fujisawa Pharmaceutical Co., Ltd. | Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine |
| JP3265680B2 (ja) | 1992-03-12 | 2002-03-11 | 大正製薬株式会社 | 経口製剤用組成物 |
| US5612359A (en) | 1994-08-26 | 1997-03-18 | Bristol-Myers Squibb Company | Substituted biphenyl isoxazole sulfonamides |
| DE19504832A1 (de) | 1995-02-14 | 1996-08-22 | Basf Ag | Feste Wirkstoff-Zubereitungen |
| TW536540B (en) | 1997-01-30 | 2003-06-11 | Bristol Myers Squibb Co | Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe |
| ES2287971T3 (es) | 1997-08-11 | 2007-12-16 | Pfizer Products Inc. | Dispersiones farmaceuticas solidas con biodisponibilidad incrementada. |
| KR20010083092A (ko) | 1998-07-06 | 2001-08-31 | 스티븐 비. 데이비스 | 이중 안지오텐신 엔도텔린 수용체 길항제로서의 비페닐술폰아미드 |
| WO2004081643A1 (en) | 2002-12-20 | 2004-09-23 | Kaiser Aerospace & Electronics Corp. | Lenslet array with polarization conversion |
| EP1460073A1 (en) | 2003-03-20 | 2004-09-22 | MyoContract Ltd. | Substituted piperidine and piperazine derivatives as melanocortin-4 receptor modulators |
| EP1753748B1 (en) | 2004-05-12 | 2009-07-29 | Pfizer Products Inc. | Proline derivatives and their use as dipeptidyl peptidase iv inhibitors |
| JP4879988B2 (ja) * | 2005-09-29 | 2012-02-22 | メルク・シャープ・エンド・ドーム・コーポレイション | メラノコルチン−４受容体モジュレーターとしてのアシル化スピロピペリジン誘導体 |
| EA200801738A1 (ru) | 2006-02-23 | 2008-12-30 | Пфайзер Лимитед | Пиперидиноилпирролидиновые агонисты меланокортинового рецептора 4 типа |
| US8044068B2 (en) | 2006-04-04 | 2011-10-25 | Taisho Pharmaceutical Co., Ltd | Aminopyrrolidine compound |
| ES2487967T3 (es) | 2006-04-20 | 2014-08-25 | Pfizer Products Inc. | Compuestos amido heterocíclicos condensados con fenilo para la prevención y el tratamiento de enfermedades mediadas por la glucoquinasa |
| US20110130365A1 (en) | 2008-07-29 | 2011-06-02 | Benbow John W | Fluorinated Heteroaryls |
| AU2009286380B2 (en) | 2008-08-28 | 2011-09-15 | Pfizer Inc. | Dioxa-bicyclo[3.2.1.]octane-2,3,4-triol derivatives |
| FR2937868B1 (fr) | 2008-11-04 | 2010-11-05 | Galderma Res & Dev | Composes antagonistes des recepteurs de la melanocortine, leur procede de preparation et leur utilisation en medecine humaine ainsi qu'en cosmetique |
| EP2210885A1 (en) | 2009-01-14 | 2010-07-28 | Santhera Pharmaceuticals (Schweiz) AG | Substituted heteroarylpiperidine derivatives as melanocortin-4 receptor modulators |
| WO2010096854A1 (en) | 2009-02-27 | 2010-09-02 | Mimetica Pty Ltd | Methods of modulating the activity of the mc3 and/or mc4 receptors and treatment of conditions related to these receptors |
| US20110319379A1 (en) | 2009-03-11 | 2011-12-29 | Corbett Jeffrey W | Substituted Indazole Amides And Their Use As Glucokinase Activators |
| SI2406253T1 (sl) | 2009-03-11 | 2013-09-30 | Pfizer Inc. | Derivati benzofuranila, uporabljeni kot inhibitorji glukokinaze |
| EP2408780A2 (en) | 2009-03-20 | 2012-01-25 | Pfizer Inc. | 3-oxa-7-azabicycloý3.3.1¨nonanes |
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| CA2764021C (en) | 2009-06-05 | 2014-04-22 | Pfizer Inc. | Gpr 119 modulators |
| WO2011005611A1 (en) | 2009-07-09 | 2011-01-13 | Merck Sharp & Dohme Corp. | Neuromedin u receptor agonists and uses thereof |
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| AR109179A1 (es) | 2016-08-19 | 2018-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| TR201618240A2 (tr) | 2016-12-09 | 2017-01-23 | Ahmet Elibol | Aort kapak koruyucu kök replasman ameli̇yatlarinda kullanilan ölçüm ve si̇mülasyon terti̇bati |
| PE20191501A1 (es) | 2016-12-16 | 2019-10-22 | Pfizer | Agonistas receptores de glp-1 y sus usos de los mismos |
| NL2019545B1 (en) | 2017-09-14 | 2019-03-27 | Univ Delft Tech | Instrument for minimal invasive surgical operations, comprising a rod or catheter and a tip mounted on the rod or catheter with an elastically deformable element |
-
2021
- 2021-06-07 CN CN202180056466.1A patent/CN116113635A/zh active Pending
- 2021-06-07 JP JP2022575378A patent/JP7288554B1/ja active Active
- 2021-06-07 AU AU2021289169A patent/AU2021289169B2/en active Active
- 2021-06-07 EP EP21732126.4A patent/EP4161927A1/en active Pending
- 2021-06-07 KR KR1020227042755A patent/KR20230011968A/ko unknown
- 2021-06-07 CR CR20220632A patent/CR20220632A/es unknown
- 2021-06-07 IL IL298891A patent/IL298891A/en unknown
- 2021-06-07 CA CA3186348A patent/CA3186348A1/en active Pending
- 2021-06-07 MX MX2022015706A patent/MX2022015706A/es unknown
- 2021-06-07 PE PE2022002902A patent/PE20231215A1/es unknown
- 2021-06-07 WO PCT/IB2021/054970 patent/WO2021250541A1/en active Application Filing
- 2021-06-07 BR BR112022024527A patent/BR112022024527A2/pt unknown
- 2021-06-08 US US17/341,877 patent/US11643412B2/en active Active
- 2021-06-08 UY UY0001039260A patent/UY39260A/es unknown
-
2022
- 2022-12-07 CO CONC2022/0017790A patent/CO2022017790A2/es unknown
- 2022-12-08 DO DO2022000281A patent/DOP2022000281A/es unknown
- 2022-12-09 EC ECSENADI202293794A patent/ECSP22093794A/es unknown
- 2022-12-09 CL CL2022003503A patent/CL2022003503A1/es unknown
- 2022-12-12 ZA ZA2022/13427A patent/ZA202213427B/en unknown
-
2023
- 2023-01-31 US US18/162,052 patent/US20230174532A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP7288554B1 (ja) | 2023-06-07 |
| CR20220632A (es) | 2023-01-23 |
| DOP2022000281A (es) | 2023-01-15 |
| AU2021289169B2 (en) | 2024-01-04 |
| CA3186348A1 (en) | 2021-12-16 |
| CO2022017790A2 (es) | 2022-12-20 |
| PE20231215A1 (es) | 2023-08-17 |
| JP2023525394A (ja) | 2023-06-15 |
| AU2021289169A1 (en) | 2023-01-19 |
| BR112022024527A2 (pt) | 2022-12-27 |
| MX2022015706A (es) | 2023-01-24 |
| CN116113635A (zh) | 2023-05-12 |
| US20230174532A1 (en) | 2023-06-08 |
| WO2021250541A1 (en) | 2021-12-16 |
| IL298891A (en) | 2023-02-01 |
| UY39260A (es) | 2022-01-31 |
| TW202204357A (zh) | 2022-02-01 |
| ECSP22093794A (es) | 2023-01-31 |
| KR20230011968A (ko) | 2023-01-25 |
| EP4161927A1 (en) | 2023-04-12 |
| US11643412B2 (en) | 2023-05-09 |
| ZA202213427B (en) | 2023-07-26 |
| US20230019853A1 (en) | 2023-01-19 |
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