PE20030808A1 - Derivados triciclicos heterociclicos como antagonistas receptores de trombina - Google Patents
Derivados triciclicos heterociclicos como antagonistas receptores de trombinaInfo
- Publication number
- PE20030808A1 PE20030808A1 PE2002001022A PE2002001022A PE20030808A1 PE 20030808 A1 PE20030808 A1 PE 20030808A1 PE 2002001022 A PE2002001022 A PE 2002001022A PE 2002001022 A PE2002001022 A PE 2002001022A PE 20030808 A1 PE20030808 A1 PE 20030808A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- alcoxy
- heterocyclic
- receptor antagonists
- thrombin receptor
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- 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
- 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
- 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
- A61P19/02—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
- 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
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- 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
Abstract
SE REFIERE A DERIVADOS TRICICLICOS HETEROCICLICOS DE FORMULA I DONDE R ES H, ALQUILO C1-C5, HALOGENO, HIDROXI, AMINO, (C1-C6) ALQUILO-AMINO, (C1-C6)-DIALQUILAMINO, ALCOXI C1-C6, ENTRE OTROS; R1 Y R2 SON H, ALQUILO C1-C6, FLUOR(C1-C6)ALQUILO, DIFLUOR(C1-C6)ALQUILO, CICLOALQUILO C3-C6, ENTRE OTROS; R3 ES H, OH, ALCOXI C1-C6, ARILOXI, ARIL(C1-C6)ALQUILOXI, HETEROARILOXI, HETEROARIL(C1-C6)ALQUILOXI, ENTRE OTROS; n ES 1-4; n1 Y n2 SON 0-3; Het ES UN GRUPO HETEROAROMATICO MONO-BI, TRICICLICO DE 5 A 14 ATOMOS DE CARBONO; R4 Y R5 SON H, ALQUILO C1-C6, FENILO, BENCILO, CICLOALQUILO C3-C6; R4 Y R5 JUNTO A (CH2)3, (CH2)4 FORMAN UN ANILLO CON EL NITROGENO AL CUAL ESTAN ADHERIDOS; R7 ES H, ALQUILO C1-C6; R8, R10 Y R11 SON R1 Y -OR1; R9 ES H, OH, -NR4R5, ALCOXI C1-C6, HALOGENO, HALO (C1-C6)ALQUILO; B ES -(CH2)n3, ENTRE OTROS; R22 ES -COR23, ENTRE OTROS; R23 ES HALO(C1-C6)ALQUILO, ALQUENILO C2-C6, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. LOS COMPUESTOS DE FORMULA I SON ANTAGONISTAS DE RECEPTORES DE TROMBINA Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES ASOCIADAS A TROMBOSIS, ATEROESCLEROSIS, RESTENOSIS, HIPERTENSION
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US33035901P | 2001-10-18 | 2001-10-18 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20030808A1 true PE20030808A1 (es) | 2003-09-22 |
Family
ID=23289411
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2002001022A PE20030808A1 (es) | 2001-10-18 | 2002-10-16 | Derivados triciclicos heterociclicos como antagonistas receptores de trombina |
Country Status (23)
Country | Link |
---|---|
US (2) | US7037920B2 (es) |
EP (1) | EP1436298B1 (es) |
JP (2) | JP4307260B2 (es) |
KR (1) | KR100960170B1 (es) |
CN (1) | CN100369917C (es) |
AR (1) | AR036832A1 (es) |
AT (1) | ATE525378T1 (es) |
AU (1) | AU2002335031C1 (es) |
BR (1) | BR0213967A (es) |
CA (1) | CA2463628A1 (es) |
CO (1) | CO5570668A2 (es) |
EC (1) | ECSP045064A (es) |
HU (1) | HUP0500443A3 (es) |
IL (1) | IL160918A0 (es) |
MX (1) | MXPA04003610A (es) |
MY (1) | MY139335A (es) |
NO (1) | NO329349B1 (es) |
NZ (1) | NZ531869A (es) |
PE (1) | PE20030808A1 (es) |
PL (1) | PL371948A1 (es) |
RU (1) | RU2319704C9 (es) |
WO (1) | WO2003033501A1 (es) |
ZA (1) | ZA200402849B (es) |
Families Citing this family (46)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6346510B1 (en) | 1995-10-23 | 2002-02-12 | The Children's Medical Center Corporation | Therapeutic antiangiogenic endostatin compositions |
US7235567B2 (en) * | 2000-06-15 | 2007-06-26 | Schering Corporation | Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist |
US7488742B2 (en) * | 2000-06-15 | 2009-02-10 | Schering Corporation | Thrombin receptor antagonists |
ATE494284T1 (de) | 2002-04-16 | 2011-01-15 | Schering Corp | Tricyclischer thrombinrezeptorantagonist |
US20070243632A1 (en) * | 2003-07-08 | 2007-10-18 | Coller Barry S | Methods for measuring platelet reactivity of patients that have received drug eluting stents |
ATE536889T1 (de) | 2003-07-08 | 2011-12-15 | Accumetrics Inc | Kontrollierte thrombozyten-aktivierung zur überwachung der behandlung von adp-antagonisten |
DE602005009355D1 (de) * | 2004-05-28 | 2008-10-09 | Schering Corp | Gehinderte himbacinanaloga als thrombinrezeptorantagonisten |
EP1778652A2 (en) * | 2004-08-20 | 2007-05-02 | EntreMed, Inc. | Compositions and methods comprising proteinase activated receptor antagonists |
AU2005294265A1 (en) * | 2004-10-06 | 2006-04-20 | University Of Rochester | Treatment of pulmonary hypertension using an agent that inhibits a tissue factor pathway |
CA2582639A1 (en) * | 2004-10-08 | 2006-04-20 | Schering Corporation | Thrombin receptor antagonists |
DK1848705T3 (da) * | 2005-01-14 | 2010-06-14 | Schering Corp | EXO- og diastereoselektive synteser af himbacin-analoger |
CN101137636A (zh) * | 2005-01-14 | 2008-03-05 | 先灵公司 | Himbacine类似物的外型选择性合成 |
CN101137647A (zh) * | 2005-01-14 | 2008-03-05 | 先灵公司 | Himbacine类似物的合成 |
CA2601575A1 (en) * | 2005-03-31 | 2006-10-05 | Schering Corporation | Spirocyclic thrombin receptor antagonists |
US7595169B2 (en) * | 2005-04-27 | 2009-09-29 | Accumetrics, Inc. | Method for determining percent platelet aggregation |
WO2007075808A2 (en) * | 2005-12-20 | 2007-07-05 | Schering Corporation | Methods for preventing and/or treating a cell proliferative disorder |
CN101384590A (zh) * | 2005-12-22 | 2009-03-11 | 先灵公司 | 作为凝血酶受体拮抗剂的唑并异喹啉 |
JP2009521472A (ja) * | 2005-12-22 | 2009-06-04 | シェーリング コーポレイション | 心肺手術の合併症の予防としてのトロンビンレセプターアンタゴニスト |
CN101460463A (zh) * | 2006-03-29 | 2009-06-17 | 先灵公司 | 可作为凝血酶受体拮抗剂的单环和双环喜巴辛衍生物 |
EP2266976B1 (en) * | 2006-04-13 | 2013-07-31 | Merck Sharp & Dohme Corp. | Fused ring thrombin receptor antagonists |
KR20090031544A (ko) | 2006-06-29 | 2009-03-26 | 쉐링 코포레이션 | 치환된 비사이클릭 및 트리사이클릭 트롬빈 수용체 길항제 |
AR061727A1 (es) * | 2006-06-30 | 2008-09-17 | Schering Corp | Sintesis de dietil [[ 5- ( 3-fluorofenil) -piridin -2il] metil] fosfonato |
TWI367112B (en) * | 2006-06-30 | 2012-07-01 | Schering Corp | Immediate-release tablet formulations of a thrombin receptor antagonist |
TWI343262B (en) * | 2006-09-26 | 2011-06-11 | Schering Corp | Rapidly disintegrating lyophilized oral formulations of a thrombin receptor antagonist |
JP2010505842A (ja) | 2006-10-04 | 2010-02-25 | シェーリング コーポレイション | トロンビン受容体拮抗薬としての二環式誘導体および三環式誘導体 |
EP2078012A2 (en) * | 2006-10-04 | 2009-07-15 | Schering Corporation | Thrombin receptor antagonists based on the modified tricyclic unit of himbacine |
CA2673228A1 (en) * | 2006-12-22 | 2008-07-03 | Schering Corporation | Disintegration promoters in solid dose wet granulation formulations |
JP2010522169A (ja) * | 2007-03-23 | 2010-07-01 | シェーリング コーポレイション | トロンビン受容体アンタゴニストの使用による、経皮的インターベンション後の有害事象の低減 |
US20080299587A1 (en) * | 2007-05-03 | 2008-12-04 | Dennis Durbin | Methods of measuring inhibition of platelet aggregation by thrombin receptor antagonists |
MX2010008490A (es) | 2008-02-05 | 2010-08-18 | Sanofi Aventis | Triazolopiridazinas como inhibidores de par1, su produccion y su uso como medicamentos. |
US8148363B2 (en) | 2008-05-19 | 2012-04-03 | Schering Corporation | Heterocyclic compounds as factor IXA inhibitors |
JP5789256B2 (ja) | 2009-06-04 | 2015-10-07 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | トロンビン受容体アンタゴニストの活性代謝物 |
AU2010259003A1 (en) | 2009-06-08 | 2011-11-10 | Merck Sharp & Dohme Corp. | A thrombin receptor antagonist and clopidogrel fixed dose tablet |
TWI393716B (zh) | 2009-08-04 | 2013-04-21 | Merck Sharp & Dohme | 作為ixa因子抑制劑之雜環化合物 |
EP2822557B1 (en) | 2012-03-06 | 2017-08-23 | Merck Sharp & Dohme Corp. | Preparation and use of bicyclic himbacine derivatives as par-receptor antagonists |
US9808473B2 (en) | 2013-08-22 | 2017-11-07 | Merck Sharp & Dohme Corp. | Preparation and use of 3-pyridyl substituted-6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists |
EP3035930A4 (en) | 2013-08-22 | 2017-03-08 | Merck Sharp & Dohme Corp. | 7a-heterocycle substituted- 6, 6-difluoro bicyclic himbacine derivatives |
EP3035929A4 (en) | 2013-08-22 | 2017-03-15 | Merck Sharp & Dohme Corp. | 7a-amide substituted-6,6-difluoro bicyclic himbacine derivatives |
US9969724B2 (en) | 2014-04-16 | 2018-05-15 | Merck Sharp & Dohme Corp. | Factor IXa inhibitors |
CN104610330A (zh) * | 2015-02-25 | 2015-05-13 | 成都安斯利生物医药有限公司 | 一种制备(e)-3-丙烯酸乙酯频呐硼酸酯的方法 |
EP4185587A1 (en) | 2020-07-22 | 2023-05-31 | JANSSEN Pharmaceutica NV | Compounds useful as factor xia inhibitors |
US11814364B2 (en) | 2021-03-18 | 2023-11-14 | Janssen Pharmaceutica Nv | Pyridine N-oxide derivatives useful as factor XIa inhibitors |
US11845748B2 (en) | 2021-03-18 | 2023-12-19 | Janssen Pharmaceutica Nv | Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors |
US11919881B2 (en) | 2021-03-18 | 2024-03-05 | Janssen Pharmaceutica Nv | Substituted pyridine N-oxide derivatives useful as a factor XIa inhibitors |
US11897880B2 (en) | 2021-04-30 | 2024-02-13 | Janssen Pharmaceutica Nv | 7,8-dihydrobenzo[e]pyrido[3,4-c]azocine-2,5(3H,6H)-dione derivatives useful as a factor XIa inhibitors |
US11958856B2 (en) | 2021-07-22 | 2024-04-16 | Janssen Pharmaceutica Nv | Substituted 1,2,3,8,9,9a-hexahydro-5H-pyrrolo[1,2-a]azepin-5-ones as factor XIa inhibitors |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5716952A (en) * | 1992-03-18 | 1998-02-10 | Allergan | Method for reducing intraocular pressure in the mammalian eye by administration of muscarinic antagonists |
IL106197A (en) | 1992-07-30 | 1999-11-30 | Cor Therapeutics Inc | Agagonists for the rhombin receptors and pharmaceutical preparations containing them |
JP2000229961A (ja) * | 1998-12-11 | 2000-08-22 | Sagami Chem Res Center | ヒドロナフト[2,3−c]フラン誘導体およびその製造方法 |
US6063847A (en) * | 1997-11-25 | 2000-05-16 | Schering Corporation | Thrombin receptor antagonists |
DE19801636A1 (de) * | 1998-01-17 | 1999-07-22 | Bayer Ag | Substituierte bicyclische Lactone |
KR100604742B1 (ko) | 2000-06-15 | 2006-07-26 | 쉐링 코포레이션 | 트롬빈 수용체 길항제 |
-
2002
- 2002-10-16 EP EP02801732A patent/EP1436298B1/en not_active Expired - Lifetime
- 2002-10-16 CA CA002463628A patent/CA2463628A1/en not_active Abandoned
- 2002-10-16 RU RU2004115114/04A patent/RU2319704C9/ru not_active IP Right Cessation
- 2002-10-16 MY MYPI20023859A patent/MY139335A/en unknown
- 2002-10-16 US US10/271,715 patent/US7037920B2/en not_active Expired - Fee Related
- 2002-10-16 IL IL16091802A patent/IL160918A0/xx not_active IP Right Cessation
- 2002-10-16 MX MXPA04003610A patent/MXPA04003610A/es active IP Right Grant
- 2002-10-16 BR BR0213967-7A patent/BR0213967A/pt not_active IP Right Cessation
- 2002-10-16 JP JP2003536240A patent/JP4307260B2/ja not_active Expired - Fee Related
- 2002-10-16 KR KR1020047005435A patent/KR100960170B1/ko not_active IP Right Cessation
- 2002-10-16 AU AU2002335031A patent/AU2002335031C1/en not_active Ceased
- 2002-10-16 PE PE2002001022A patent/PE20030808A1/es not_active Application Discontinuation
- 2002-10-16 AR ARP020103876A patent/AR036832A1/es unknown
- 2002-10-16 PL PL02371948A patent/PL371948A1/xx not_active Application Discontinuation
- 2002-10-16 AT AT02801732T patent/ATE525378T1/de not_active IP Right Cessation
- 2002-10-16 CN CNB028206665A patent/CN100369917C/zh not_active Expired - Fee Related
- 2002-10-16 HU HU0500443A patent/HUP0500443A3/hu unknown
- 2002-10-16 NZ NZ531869A patent/NZ531869A/en not_active IP Right Cessation
- 2002-10-16 WO PCT/US2002/032936 patent/WO2003033501A1/en active IP Right Grant
-
2004
- 2004-04-15 EC EC2004005064A patent/ECSP045064A/es unknown
- 2004-04-15 ZA ZA200402849A patent/ZA200402849B/xx unknown
- 2004-04-16 CO CO04034781A patent/CO5570668A2/es not_active Application Discontinuation
- 2004-05-14 NO NO20042021A patent/NO329349B1/no not_active IP Right Cessation
-
2005
- 2005-12-19 US US11/311,083 patent/US20060106050A1/en not_active Abandoned
-
2008
- 2008-09-17 JP JP2008238716A patent/JP2009029820A/ja not_active Withdrawn
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