AR082968A1 - Inhibidores biciclicos de notum pectinacetilesterasa y una composicion farmaceutica en base al compuesto - Google Patents
Inhibidores biciclicos de notum pectinacetilesterasa y una composicion farmaceutica en base al compuestoInfo
- Publication number
- AR082968A1 AR082968A1 ARP110103323A ARP110103323A AR082968A1 AR 082968 A1 AR082968 A1 AR 082968A1 AR P110103323 A ARP110103323 A AR P110103323A AR P110103323 A ARP110103323 A AR P110103323A AR 082968 A1 AR082968 A1 AR 082968A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- heterocycle
- aryl
- heteroalkyl
- hydrogen
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 8
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000001475 halogen functional group Chemical group 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 abstract 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 102000004251 pectinacetylesterase Human genes 0.000 abstract 1
- 108010072638 pectinacetylesterase Proteins 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
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Physical Education & Sports Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Se describen compuestos que se pueden utilizar para inhibir la Notum pectinacetilesterasa, como también composiciones que los comprenden. Estos compuestos son útiles para tratar las enfermedades y los trastornos que afectan a los huesos, en particular la osteoporosis.Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde: R1B es hidrógeno o alquilo, arilo, heteroalquilo o heterociclo opcionalmente sustituidos; R2 es hidrógeno, halo, -CO2R2A, -C(O)N(R2A)2, -SR2A, -OR2A o -N(R2A)2, alquilo, arilo, heteroalquilo o heterociclo, opcionalmente sustituidos; cada R2A es, de manera independiente, hidrógeno o alquilo, arilo, heteroalquilo, o heterociclo, opcionalmente sustituidos; R3 es hidrógeno, halo, ciano, -CO2R3A, -C(O)N(R3A)2, -SR3A, -OR3A, -N(R3A)2, o alquilo, arilo, heteroalquilo o heterociclo, opcionalmente sustituidos; cada R3A es, de manera independiente, hidrógeno, alquilo, arilo, heteroalquilo o heterociclo, opcionalmente sustituidos; R4 es hidrógeno, halo o alquilo, arilo, heteroalquilo o heterociclo, opcionalmente sustituidos; R5 es hidrógeno, halo, -CO2R5A, -C(O)N(R5A)2, -SR5A, -OR5A, -N(R5A)2 o arilo, heteroalquilo, o heterociclo, opcionalmente sustituidos; cada R5A es, de manera independiente, hidrógeno, alquilo, arilo, heteroalquilo, o heterociclo, opcionalmente sustituidos; y n es 0, 1 ó 2; en donde “opcionalmente sustituido” significa opcionalmente sustituido con uno o más de alcoxi, alquilo, amino (incluyendo alquilamino, dialquilamino), arilo, ácido carboxílico, ciano, halo, heterociclo o hidroxilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38252610P | 2010-09-14 | 2010-09-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR082968A1 true AR082968A1 (es) | 2013-01-23 |
Family
ID=44678054
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110103323A AR082968A1 (es) | 2010-09-14 | 2011-09-13 | Inhibidores biciclicos de notum pectinacetilesterasa y una composicion farmaceutica en base al compuesto |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US20120065200A1 (es) |
| EP (1) | EP2616471B1 (es) |
| JP (1) | JP2013537202A (es) |
| KR (1) | KR20130112888A (es) |
| CN (1) | CN103328481A (es) |
| AR (1) | AR082968A1 (es) |
| AU (1) | AU2011302225A1 (es) |
| BR (1) | BR112013006131A2 (es) |
| CA (1) | CA2811005A1 (es) |
| CL (1) | CL2013000682A1 (es) |
| CO (1) | CO6710916A2 (es) |
| DK (1) | DK2616471T3 (es) |
| ES (1) | ES2536078T3 (es) |
| MX (1) | MX2013002851A (es) |
| NZ (1) | NZ608031A (es) |
| PL (1) | PL2616471T3 (es) |
| PT (1) | PT2616471E (es) |
| RU (1) | RU2013116801A (es) |
| SG (1) | SG188530A1 (es) |
| TW (1) | TW201219401A (es) |
| WO (1) | WO2012037141A1 (es) |
| ZA (1) | ZA201301795B (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6042331B2 (ja) | 2010-07-23 | 2016-12-14 | プレジデント アンド フェローズ オブ ハーバード カレッジ | プロテアソーム活性を向上させる三環系化合物 |
| AR090037A1 (es) * | 2011-11-15 | 2014-10-15 | Xention Ltd | Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio |
| CA2861464C (en) | 2012-01-25 | 2018-03-06 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating tricyclic compounds |
| KR102590848B1 (ko) | 2016-12-28 | 2023-10-19 | 다트 뉴로사이언스, 엘엘씨 | Pde2 억제제로서 치환된 피라졸로피리미디논 화합물 |
| ES2902365T3 (es) | 2017-11-27 | 2022-03-28 | Dart Neuroscience Llc | Compuestos de furanopirimidina sustituidos como inhibidores de PDE1 |
| IL279977B2 (en) | 2018-07-09 | 2024-06-01 | Boehringer Ingelheim Animal Health Usa Inc | Heterocyclic anthelmintic compounds |
| GB201814151D0 (en) | 2018-08-31 | 2018-10-17 | Ucl Business Plc | Compounds |
| CN111171044B (zh) * | 2018-11-13 | 2022-06-24 | 沈阳化工研究院有限公司 | 一种噻吩并嘧啶类化合物及其医药用途 |
| CA3120858A1 (en) | 2018-11-21 | 2020-05-28 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase activity |
| JP7458406B2 (ja) | 2018-12-21 | 2024-03-29 | セルジーン コーポレーション | Ｒｉｐｋ２のチエノピリジン阻害剤 |
| US11560388B2 (en) | 2019-03-19 | 2023-01-24 | Boehringer Ingelheim Vetmedica Gmbh | Anthelmintic aza-benzothiophene and aza-benzofuran compounds |
| CA3183100A1 (en) | 2020-05-29 | 2021-12-02 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Anthelmintic heterocyclic compounds |
| TWI815475B (zh) * | 2021-05-27 | 2023-09-11 | 財團法人國家衛生研究院 | Ｃｄｇｓｈ鐵硫結構域２活化劑及其用途 |
| AR127495A1 (es) | 2021-11-01 | 2024-01-31 | Boehringer Ingelheim Vetmedica Gmbh | Compuestos de pirrolopiridazina como antihelmínticos |
| CN114984188A (zh) * | 2022-06-20 | 2022-09-02 | 重庆医科大学 | Notum与bmp9作为联合靶点在细胞成骨分化中的应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4008726A1 (de) | 1990-03-19 | 1991-09-26 | Basf Ag | Thieno(2,3-d)pyrimidinderivate |
| US6080576A (en) | 1998-03-27 | 2000-06-27 | Lexicon Genetics Incorporated | Vectors for gene trapping and gene activation |
| US6232320B1 (en) | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
| CA2654842A1 (en) * | 2006-06-12 | 2007-12-21 | Vertex Pharmaceuticals Incorporated | Thienopyrimidines useful as modulators of ion channels |
| WO2009001214A2 (en) * | 2007-06-28 | 2008-12-31 | Pfizer Products Inc. | Thieno[2,3-d]pyrimidin-4(3h)-one, isoxazolo[5,4-d]pyrimidin-4(5h)-one and isothiazolo[5,4-d]pyrimidin-4(5h)-one derivatives as calcium receptor antagonists |
-
2011
- 2011-09-08 TW TW100132460A patent/TW201219401A/zh unknown
- 2011-09-13 CN CN2011800442957A patent/CN103328481A/zh active Pending
- 2011-09-13 SG SG2013018700A patent/SG188530A1/en unknown
- 2011-09-13 BR BR112013006131A patent/BR112013006131A2/pt not_active IP Right Cessation
- 2011-09-13 US US13/231,653 patent/US20120065200A1/en not_active Abandoned
- 2011-09-13 JP JP2013528388A patent/JP2013537202A/ja not_active Withdrawn
- 2011-09-13 AR ARP110103323A patent/AR082968A1/es unknown
- 2011-09-13 KR KR1020137009332A patent/KR20130112888A/ko not_active Withdrawn
- 2011-09-13 EP EP11761206.9A patent/EP2616471B1/en not_active Not-in-force
- 2011-09-13 PT PT117612069T patent/PT2616471E/pt unknown
- 2011-09-13 WO PCT/US2011/051421 patent/WO2012037141A1/en not_active Ceased
- 2011-09-13 RU RU2013116801/04A patent/RU2013116801A/ru not_active Application Discontinuation
- 2011-09-13 AU AU2011302225A patent/AU2011302225A1/en not_active Abandoned
- 2011-09-13 DK DK11761206.9T patent/DK2616471T3/en active
- 2011-09-13 NZ NZ608031A patent/NZ608031A/en not_active IP Right Cessation
- 2011-09-13 ES ES11761206.9T patent/ES2536078T3/es active Active
- 2011-09-13 CA CA2811005A patent/CA2811005A1/en not_active Abandoned
- 2011-09-13 PL PL11761206T patent/PL2616471T3/pl unknown
- 2011-09-13 MX MX2013002851A patent/MX2013002851A/es not_active Application Discontinuation
-
2013
- 2013-03-08 ZA ZA2013/01795A patent/ZA201301795B/en unknown
- 2013-03-13 CL CL2013000682A patent/CL2013000682A1/es unknown
- 2013-04-12 CO CO13094694A patent/CO6710916A2/es not_active Application Discontinuation
-
2014
- 2014-06-10 US US14/300,281 patent/US20140288071A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| ES2536078T3 (es) | 2015-05-20 |
| KR20130112888A (ko) | 2013-10-14 |
| RU2013116801A (ru) | 2014-10-20 |
| CL2013000682A1 (es) | 2013-11-08 |
| US20120065200A1 (en) | 2012-03-15 |
| EP2616471A1 (en) | 2013-07-24 |
| JP2013537202A (ja) | 2013-09-30 |
| PL2616471T3 (pl) | 2015-07-31 |
| US20140288071A1 (en) | 2014-09-25 |
| BR112013006131A2 (pt) | 2016-06-07 |
| ZA201301795B (en) | 2014-05-28 |
| NZ608031A (en) | 2015-01-30 |
| SG188530A1 (en) | 2013-04-30 |
| CN103328481A (zh) | 2013-09-25 |
| MX2013002851A (es) | 2013-05-28 |
| CO6710916A2 (es) | 2013-07-15 |
| PT2616471E (pt) | 2015-04-20 |
| AU2011302225A1 (en) | 2013-03-21 |
| TW201219401A (en) | 2012-05-16 |
| DK2616471T3 (en) | 2015-04-07 |
| CA2811005A1 (en) | 2012-03-22 |
| WO2012037141A1 (en) | 2012-03-22 |
| EP2616471B1 (en) | 2014-12-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |