PE20090226A1 - PIRROLIDINAMIDAS SUSTITUIDAS COMO INHIBIDORES DEL FACTOR Xa Y SU PREPARACION - Google Patents
PIRROLIDINAMIDAS SUSTITUIDAS COMO INHIBIDORES DEL FACTOR Xa Y SU PREPARACIONInfo
- Publication number
- PE20090226A1 PE20090226A1 PE2008000536A PE2008000536A PE20090226A1 PE 20090226 A1 PE20090226 A1 PE 20090226A1 PE 2008000536 A PE2008000536 A PE 2008000536A PE 2008000536 A PE2008000536 A PE 2008000536A PE 20090226 A1 PE20090226 A1 PE 20090226A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- chloro
- thiofen
- pyrrolidin
- tetrahydro
- Prior art date
Links
- 108010074860 Factor Xa Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- -1 PYRROLIDINAMIDE COMPOUND Chemical class 0.000 abstract 4
- 239000002253 acid Substances 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003457 sulfones Chemical class 0.000 abstract 1
- 230000001732 thrombotic effect Effects 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
- C07D419/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
REFERIDA A UN COMPUESTO DE PIRROLIDINAMIDA DE FORMULA (I), DONDE D SE SELECCIONA DE (IIa), (IIb) Y (IIc); K1 Y K4 SON CH2, C(O), UN ENLACE, ENTRE OTROS; K2 Y K3 SON CH2, C(O), CHR8a, ENTRE OTROS; R8a ES ALQUILO C1-C5, HIDROXIALQUILO C1-C5, AMINOALQUILO C1-C5, ENTRE OTROS; X ES O, S, CF2, SULFONA, ENTRE OTROS; A1 ES N O CR10; A2 ES N O CR11; A3 ES N O CR12; A5 ES NH, S U O; R10, R11 Y R12 SON H, F, Cl, CF3, ALQUILO C1-C5, ENTRE OTROS; -L-E-G-J- ES -C-C-C-C OPCIONALMENTE SUSTITUIDO CON R4 Y R5; L1 ES C(O); R4 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R5 ES H, ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; L2 ES C(O); M ES FENILO, PIRIDILO, TIENILO, FURILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: [1-(3-METIL-2,3,4,5-TETRAHIDRO-1H-BENZO[d]AZEPIN-7-CARBONIL)-PIRROLIDIN-3-IL]-AMIDA DE ACIDO 5-CLORO-TIOFEN-2-CLORO-TIOFEN-2-CARBOXILICO, [1-(2-METIL-1,2,3,4-TETRAHIDRO-ISOQUINOLIN-6-CARBONIL)-PIRROLIDIN-3-IL]-AMIDA DEL ACIDO 5-CLORO-TIOFEN-2-CARBOXILICO, [4-HIDROXI-1-(2-METIL-1,2,3,4-TETRAHIDRO-ISOQUINOLIN-6-CARBONIL)-PIRROLIDIN-3-IL]-AMIDA DEL ACIDO (3SR,4SR)-5-CLORO-TIOFEN-2-CARBOXILICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DEL FACTOR Xa Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES TROMBOTICAS VENOSAS Y ARTERIALES
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07105053A EP1975165A1 (de) | 2007-03-27 | 2007-03-27 | Substituierte Pyrrolidinamide, deren Herstellung und deren Verwendung als Arzneimittel |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090226A1 true PE20090226A1 (es) | 2009-04-02 |
Family
ID=38599360
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008000536A PE20090226A1 (es) | 2007-03-27 | 2008-03-25 | PIRROLIDINAMIDAS SUSTITUIDAS COMO INHIBIDORES DEL FACTOR Xa Y SU PREPARACION |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8309542B2 (es) |
| EP (2) | EP1975165A1 (es) |
| JP (1) | JP5397959B2 (es) |
| AR (1) | AR065852A1 (es) |
| CA (1) | CA2682012A1 (es) |
| CL (1) | CL2008000873A1 (es) |
| PE (1) | PE20090226A1 (es) |
| TW (1) | TW200902022A (es) |
| UY (1) | UY30979A1 (es) |
| WO (1) | WO2008116881A1 (es) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2220079A2 (en) * | 2007-11-15 | 2010-08-25 | Boehringer Ingelheim International GmbH | Substituted amides, manufacturing and use thereof as medicaments |
| WO2009153179A1 (en) * | 2008-06-16 | 2009-12-23 | F. Hoffmann-La Roche Ag | Pyrrolidine derivatives as nk2 receptor antagonists |
| MX2012002827A (es) * | 2009-09-11 | 2012-04-10 | Sunovion Pharmaceuticals Inc | Agonistas inversos y antagonistas de histamina h3 y metodos para usar los mismos. |
| PT2861566T (pt) | 2012-06-13 | 2017-02-08 | Hoffmann La Roche | Novos diazaspirocicloalcanos e azaspirocicloalcanos |
| HRP20191937T1 (hr) | 2012-09-25 | 2020-01-10 | F. Hoffmann - La Roche Ag | Derivati heksahidropirolo [3,4-c]pirola i srodni spojevi kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za liječenje npr. bubrežnih bolesti |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| PL3074400T3 (pl) | 2013-11-26 | 2018-03-30 | F.Hoffmann-La Roche Ag | Pochodne oktahydrocyklobuta[1,2-c;3,4-c']dipirolu jako inhibitory autotaksyny |
| SG11201607845RA (en) | 2014-03-26 | 2016-10-28 | Hoffmann La Roche | Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| SG11201607839UA (en) | 2014-03-26 | 2016-10-28 | Hoffmann La Roche | Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| US20170247326A1 (en) * | 2014-09-10 | 2017-08-31 | Epizyme, Inc. | Substituted Pyrrolidine Carboxamide Compounds |
| EP3078378B1 (en) | 2015-04-08 | 2020-06-24 | Vaiomer | Use of factor xa inhibitors for regulating glycemia |
| KR20180043837A (ko) | 2015-09-04 | 2018-04-30 | 에프. 호프만-라 로슈 아게 | 페녹시메틸 유도체 |
| BR112017026682A2 (pt) | 2015-09-24 | 2018-08-14 | Hoffmann La Roche | novos compostos bicíclicos como inibidores de dupla ação de atx/ca |
| EP3353178B1 (en) | 2015-09-24 | 2021-07-14 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
| JP6876685B2 (ja) | 2015-09-24 | 2021-05-26 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Atx阻害剤としての二環式化合物 |
| EP3353180B1 (en) | 2015-09-24 | 2022-03-16 | F. Hoffmann-La Roche AG | Bicyclic compounds as atx inhibitors |
| CA3043938A1 (en) | 2016-12-21 | 2018-06-28 | Biotheryx, Inc. | Thienopyrrole derivatives for use in targeting proteins, compositions, methods, and uses thereof |
| JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ.ホフマン-ラ ロシュ アーゲー | Atxインヒビターとしての新規二環式化合物 |
| PE20191757A1 (es) | 2017-03-16 | 2019-12-12 | Hoffmann La Roche | Compuestos heterociclicos utiles como inhibidores dobles de atx/ca |
| US20220133740A1 (en) | 2019-02-08 | 2022-05-05 | Frequency Therapeutics, Inc. | Valproic acid compounds and wnt agonists for treating ear disorders |
| EP3962906A1 (en) * | 2019-04-30 | 2022-03-09 | Calico Life Sciences LLC | Substituted cycloalkyls as modulators of the integrated stress pathway |
| KR102333564B1 (ko) * | 2019-11-28 | 2021-12-01 | 동방에프티엘(주) | 광학 활성 다이아민 유도체 및 티아졸 유도체의 생산을 위한 새로운 합성경로 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE308540T1 (de) * | 2000-08-17 | 2005-11-15 | Lilly Co Eli | Antithrombosemittel |
| US7312214B2 (en) * | 2002-05-10 | 2007-12-25 | Bristol-Myers Squibb Company | 1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors |
| PL382706A1 (pl) * | 2002-08-26 | 2007-11-26 | Takeda Pharmaceutical Company Limited | Związek modulujący receptor wapnia i jego zastosowanie |
| US7205318B2 (en) * | 2003-03-18 | 2007-04-17 | Bristol-Myers Squibb Company | Lactam-containing cyclic diamines and derivatives as a factor Xa inhibitors |
| US20050119266A1 (en) * | 2003-10-01 | 2005-06-02 | Yan Shi | Pyrrolidine and piperidine derivatives as factor Xa inhibitors |
| US7820699B2 (en) | 2005-04-27 | 2010-10-26 | Hoffmann-La Roche Inc. | Cyclic amines |
| PE20070171A1 (es) | 2005-06-30 | 2007-03-08 | Boehringer Ingelheim Int | GLICINAMIDAS SUSTITUIDAS CON EFECTO ANTITROMBOTICO E INHIBIDOR DEL FACTOR Xa |
| US20070032473A1 (en) | 2005-07-19 | 2007-02-08 | Kai Gerlach | Substituted amides and their use as medicaments |
| EP1818330A1 (de) | 2006-02-14 | 2007-08-15 | Boehringer Ingelheim Pharma GmbH & Co.KG | Substituierte Prolinamide, deren Herstellung und deren Verwendung als Arzneimittel |
| JP5263686B2 (ja) | 2006-05-16 | 2013-08-14 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換プロリンアミド、その製造及び薬物としての使用 |
-
2007
- 2007-03-27 EP EP07105053A patent/EP1975165A1/de not_active Ceased
-
2008
- 2008-03-25 UY UY30979A patent/UY30979A1/es not_active Application Discontinuation
- 2008-03-25 PE PE2008000536A patent/PE20090226A1/es not_active Application Discontinuation
- 2008-03-26 JP JP2010500259A patent/JP5397959B2/ja not_active Expired - Fee Related
- 2008-03-26 EP EP08718234A patent/EP2132193B1/de not_active Not-in-force
- 2008-03-26 CL CL2008000873A patent/CL2008000873A1/es unknown
- 2008-03-26 WO PCT/EP2008/053568 patent/WO2008116881A1/de not_active Ceased
- 2008-03-26 US US12/531,343 patent/US8309542B2/en active Active
- 2008-03-26 AR ARP080101240A patent/AR065852A1/es unknown
- 2008-03-26 CA CA002682012A patent/CA2682012A1/en not_active Abandoned
- 2008-03-26 TW TW097110833A patent/TW200902022A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP1975165A1 (de) | 2008-10-01 |
| CL2008000873A1 (es) | 2009-03-27 |
| EP2132193A1 (de) | 2009-12-16 |
| UY30979A1 (es) | 2008-10-31 |
| JP2010522713A (ja) | 2010-07-08 |
| US8309542B2 (en) | 2012-11-13 |
| TW200902022A (en) | 2009-01-16 |
| JP5397959B2 (ja) | 2014-01-22 |
| CA2682012A1 (en) | 2008-10-02 |
| AR065852A1 (es) | 2009-07-08 |
| WO2008116881A1 (de) | 2008-10-02 |
| EP2132193B1 (de) | 2012-10-24 |
| US20100099664A1 (en) | 2010-04-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |