ES2116583T3 - Compuestos azaciclicos, composiciones que los contienen y su uso como antagonistas de taquicininas. - Google Patents
Compuestos azaciclicos, composiciones que los contienen y su uso como antagonistas de taquicininas.Info
- Publication number
- ES2116583T3 ES2116583T3 ES94907565T ES94907565T ES2116583T3 ES 2116583 T3 ES2116583 T3 ES 2116583T3 ES 94907565 T ES94907565 T ES 94907565T ES 94907565 T ES94907565 T ES 94907565T ES 2116583 T3 ES2116583 T3 ES 2116583T3
- Authority
- ES
- Spain
- Prior art keywords
- sup
- sub
- compounds
- replaced
- rent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000005557 antagonist Substances 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- SLRMQYXOBQWXCR-UHFFFAOYSA-N 2154-56-5 Chemical class [CH2]C1=CC=CC=C1 SLRMQYXOBQWXCR-UHFFFAOYSA-N 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 206010047700 Vomiting Diseases 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/40—Oxygen atoms
- C07D211/42—Oxygen atoms attached in position 3 or 5
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Anesthesiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
- Pyrrole Compounds (AREA)
Abstract
EL PRESENTE INVENTO SE REFIERE A COMPUESTOS DE LA FORMULA (I), Y SALES Y PRODROGAS DE LOS MISMOS, EN LA QUE N ES 1, 2 O 3 Y DONDE ALGUN ATOMO DE CARBONO DE (CH{SUB,2}){SUB,N} PUEDE SER SUSTITUIDO POR R{SUP,4} Y/O R{SUP,5}; X REPRESENTA O O S; R{SUP,1} REPRESENTA FENILO (CH{SUB,2}){SUB,Q} OPCIONALMENTE SUSTITUIDO, ARILO, HETEROARILO, BENCIHIDRILO O BENCILO; R{SUP,4} Y R{SUP,5} CADA UNO REPRESENTA INDEPENDIENTEMENTE H, HALO, ALQUILOC{SUB,1-6}, OXO, CO{SUB,2}R{SUP,A} O CONR{SUP,A}R{SUP,B}, R{SUP,6} REPRESENTA H O ALQUILOC{SUB,1-6}; R{SUP,7} REPRESENTA ALQUILOC{SUB,1-6} O FENILO OPCIONALMENTE SUSTITUIDO; R{SUP,8} REPRESENTA H, COR{SUP,A}, CO{SUB,2}R{SUP,A}, COCONR{SUP,A}R{SUP,B}, COCO{SUB,2}R{SUP,A}, ALQUILO C{SUB,1-6} OPCIONALMENTE SUSTITUIDO POR UNA VARIEDAD DE SUSTITUYENTES, O ALQUILOC{SUB,1-6} OPCIONALMENTE SUSTITUIDO POR OXO, SUSTITUIDO POR UN HETREOCICLO AROMATICO OPCIONALMENTE SUSTITUIDO. LOS COMPUESTOS SON ANTAGONISTAS DE LA TACIQUININA UTILES PARA EL TRATAMIENTO DEL DOLOR O LA INFLAMACION, MIGRAÑA O EMESIS.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB939303243A GB9303243D0 (en) | 1993-02-18 | 1993-02-18 | Therapeutic agents |
| GB939322150A GB9322150D0 (en) | 1993-10-27 | 1993-10-27 | Therapeutic agents |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2116583T3 true ES2116583T3 (es) | 1998-07-16 |
Family
ID=26302480
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES94907565T Expired - Lifetime ES2116583T3 (es) | 1993-02-18 | 1994-02-10 | Compuestos azaciclicos, composiciones que los contienen y su uso como antagonistas de taquicininas. |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US5633266A (es) |
| EP (1) | EP0683767B1 (es) |
| JP (1) | JPH08506823A (es) |
| AT (1) | ATE166867T1 (es) |
| AU (1) | AU679207B2 (es) |
| CA (1) | CA2152925A1 (es) |
| DE (1) | DE69410784T2 (es) |
| ES (1) | ES2116583T3 (es) |
| WO (1) | WO1994019323A1 (es) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL111960A (en) * | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| ATE170174T1 (de) * | 1994-01-13 | 1998-09-15 | Merck Sharp & Dohme | Gem-bissubstituierte azazyclische tachykinin- antagonisten |
| GB9402688D0 (en) * | 1994-02-11 | 1994-04-06 | Merck Sharp & Dohme | Therapeutic agents |
| JPH10500944A (ja) * | 1994-05-05 | 1998-01-27 | メルク シヤープ エンド ドーム リミテツド | モルホリン誘導体及びタキキニンのアンタゴニストとしてのそれらの使用 |
| DE19504627A1 (de) * | 1995-02-13 | 1996-08-14 | Bayer Ag | Verfahren und neue Zwischenprodukte zur Herstellung von Triazolinonen |
| GB9513117D0 (en) * | 1995-06-28 | 1995-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| GB9513121D0 (en) * | 1995-06-28 | 1995-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| US6013631A (en) | 1998-06-19 | 2000-01-11 | Xoma Corporation | Bactericidal/permeability-increasing protein (BPI) deletion analogs |
| KR100885986B1 (ko) | 1999-11-03 | 2009-03-03 | 에이엠알 테크놀로지, 인크. | 노르에피네프린, 도파민 및 세로토닌의 재흡수를 방지하기위한 아릴 및 헤테로아릴 치환된테트라하이드로이소퀴놀린 및 이들의 용도 |
| US7163949B1 (en) | 1999-11-03 | 2007-01-16 | Amr Technology, Inc. | 4-phenyl substituted tetrahydroisoquinolines and use thereof |
| WO2001095904A1 (en) * | 2000-06-12 | 2001-12-20 | University Of Rochester | Method of treating symptoms of hormonal variation, including hot flashes, using tachykinin receptor antagonist |
| CA2415532C (en) | 2000-07-11 | 2010-05-11 | Albany Molecular Research, Inc. | Novel 4-phenyl substituted tetrahydroisoquinolines therapeutic use thereof |
| US7407480B2 (en) * | 2001-07-27 | 2008-08-05 | Ams Research Corporation | Method and apparatus for correction of urinary and gynecological pathologies, including treatment of incontinence cystocele |
| WO2003101459A1 (en) * | 2002-05-29 | 2003-12-11 | The Regents Of The University Of California | Antagonizing nk1 receptors inhibits consumption of substances of abuse |
| KR101389246B1 (ko) | 2004-07-15 | 2014-04-24 | 브리스톨-마이어스스퀴브컴파니 | 아릴- 및 헤테로아릴-치환된 테트라히드로이소퀴놀린, 및 이것의 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도 |
| JPWO2006030975A1 (ja) * | 2004-09-17 | 2008-05-15 | 武田薬品工業株式会社 | ピペリジン誘導体およびその用途 |
| WO2006115285A1 (ja) * | 2005-04-21 | 2006-11-02 | Takeda Pharmaceutical Company Limited | 医薬組成物 |
| EP1888050B1 (en) | 2005-05-17 | 2012-03-21 | Merck Sharp & Dohme Ltd. | cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid for the treatment of cancer |
| ZA200800440B (en) | 2005-07-15 | 2009-12-30 | Amr Technology Inc | Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin |
| US8293900B2 (en) | 2005-09-29 | 2012-10-23 | Merck Sharp & Dohme Corp | Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators |
| GB0603041D0 (en) | 2006-02-15 | 2006-03-29 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| EP2698157B1 (en) | 2006-09-22 | 2015-05-20 | Merck Sharp & Dohme Corp. | Method of treatment using fatty acid synthesis inhibitors |
| US20110218176A1 (en) | 2006-11-01 | 2011-09-08 | Barbara Brooke Jennings-Spring | Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development |
| EP2805945B1 (en) | 2007-01-10 | 2019-04-03 | MSD Italia S.r.l. | Amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors |
| US8106086B2 (en) | 2007-04-02 | 2012-01-31 | Msd K.K. | Indoledione derivative |
| US8389553B2 (en) | 2007-06-27 | 2013-03-05 | Merck Sharp & Dohme Corp. | 4-carboxybenzylamino derivatives as histone deacetylase inhibitors |
| US8258306B2 (en) * | 2007-12-12 | 2012-09-04 | Amgen Inc. | Glycine transporter-1 inhibitors |
| KR20100126467A (ko) | 2008-03-03 | 2010-12-01 | 타이거 파마테크 | 티로신 키나아제 억제제 |
| US9156812B2 (en) | 2008-06-04 | 2015-10-13 | Bristol-Myers Squibb Company | Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine |
| US8691825B2 (en) | 2009-04-01 | 2014-04-08 | Merck Sharp & Dohme Corp. | Inhibitors of AKT activity |
| KR101830447B1 (ko) | 2009-05-12 | 2018-02-20 | 알바니 몰레큘라 리써치, 인크. | 7-([1,2,4]트리아졸로[1,5-α]피리딘-6-일)-4-(3,4-디클로로페닐)-1,2,3,4-테트라하이드로이소퀴놀린 및 이의 용도 |
| CN102638982B (zh) | 2009-05-12 | 2015-07-08 | 百时美施贵宝公司 | (S)-7-([1,2,4]三唑并[1,5-a]吡啶-6-基)-4-(3,4-二氯苯基)-1,2,3,4-四氢异喹啉的晶型及其用途 |
| EP2429295B1 (en) | 2009-05-12 | 2013-12-25 | Albany Molecular Research, Inc. | Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof |
| EP2488028B1 (en) | 2009-10-14 | 2020-08-19 | Merck Sharp & Dohme Corp. | Substituted piperidines that increase p53 activity and the uses thereof |
| WO2011163330A1 (en) | 2010-06-24 | 2011-12-29 | Merck Sharp & Dohme Corp. | Novel heterocyclic compounds as erk inhibitors |
| CN107090456B (zh) | 2010-08-02 | 2022-01-18 | 瑟纳治疗公司 | 使用短干扰核酸的RNA干扰介导的联蛋白(钙粘蛋白关联蛋白质),β1基因表达的抑制 |
| JP2013537423A (ja) | 2010-08-17 | 2013-10-03 | メルク・シャープ・エンド・ドーム・コーポレイション | 低分子干渉核酸(siNA)を用いたB型肝炎ウイルス(HBV)遺伝子発現のRNA干渉媒介性阻害 |
| US8883801B2 (en) | 2010-08-23 | 2014-11-11 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors |
| WO2012030685A2 (en) | 2010-09-01 | 2012-03-08 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| EP2615916B1 (en) | 2010-09-16 | 2017-01-04 | Merck Sharp & Dohme Corp. | Fused pyrazole derivatives as novel erk inhibitors |
| DK2632472T3 (en) | 2010-10-29 | 2018-03-19 | Sirna Therapeutics Inc | RNA INTERFERENCE-MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERRING NUCLEIC ACIDS (SINA) |
| WO2012087772A1 (en) | 2010-12-21 | 2012-06-28 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| EP2699568A1 (en) | 2011-04-21 | 2014-02-26 | Piramal Enterprises Limited | A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation |
| WO2013063214A1 (en) | 2011-10-27 | 2013-05-02 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| EP2844261B1 (en) | 2012-05-02 | 2018-10-17 | Sirna Therapeutics, Inc. | SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS |
| CN105050598B (zh) | 2012-09-28 | 2018-04-27 | 默沙东公司 | 作为erk抑制剂的新型化合物 |
| RS56680B1 (sr) | 2012-11-28 | 2018-03-30 | Merck Sharp & Dohme | Kompozicije i postupci za lečenje kancera |
| US8846657B2 (en) | 2012-12-20 | 2014-09-30 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as HDM2 inhibitors |
| WO2014120748A1 (en) | 2013-01-30 | 2014-08-07 | Merck Sharp & Dohme Corp. | 2,6,7,8 substituted purines as hdm2 inhibitors |
| EP3041938A1 (en) | 2013-09-03 | 2016-07-13 | Moderna Therapeutics, Inc. | Circular polynucleotides |
| US10975084B2 (en) | 2016-10-12 | 2021-04-13 | Merck Sharp & Dohme Corp. | KDM5 inhibitors |
| US11098059B2 (en) | 2017-11-08 | 2021-08-24 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
| EP3706742B1 (en) | 2017-11-08 | 2023-03-15 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| EP3833667B1 (en) | 2018-08-07 | 2024-03-13 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| CA3108388A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| EP3833668B1 (en) | 2018-08-07 | 2025-03-19 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| WO2025008409A2 (en) | 2023-07-03 | 2025-01-09 | Preeti Jha | Substituted 2-phenylpiperidine compounds for use in the diagnosis, treatment and/or prevention of cancer |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6033439B2 (ja) * | 1980-03-07 | 1985-08-02 | 財団法人相模中央化学研究所 | ジペプチドの製造方法 |
| UA41251C2 (uk) * | 1990-01-04 | 2001-09-17 | Пфайзер, Інк. | Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі |
| EP0499313B1 (en) * | 1991-02-11 | 1997-06-11 | MERCK SHARP & DOHME LTD. | Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy |
| CA2112397A1 (en) * | 1991-08-20 | 1993-03-04 | Raymond Baker | Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them |
| AU675786B2 (en) * | 1992-04-15 | 1997-02-20 | Merck Sharp & Dohme Limited | Azacyclic compounds |
| US5444074A (en) * | 1992-04-15 | 1995-08-22 | Merck Sharp & Dohme Limited | Piperidine tachykinin receptor antagonists |
| US5496833A (en) * | 1993-04-13 | 1996-03-05 | Merck Sharp & Dohme Limited | Piperidine tachykinin receptor antagonists |
-
1994
- 1994-02-10 DE DE69410784T patent/DE69410784T2/de not_active Expired - Fee Related
- 1994-02-10 AT AT94907565T patent/ATE166867T1/de not_active IP Right Cessation
- 1994-02-10 CA CA002152925A patent/CA2152925A1/en not_active Abandoned
- 1994-02-10 EP EP94907565A patent/EP0683767B1/en not_active Expired - Lifetime
- 1994-02-10 WO PCT/EP1994/000412 patent/WO1994019323A1/en not_active Ceased
- 1994-02-10 AU AU61093/94A patent/AU679207B2/en not_active Ceased
- 1994-02-10 US US08/495,429 patent/US5633266A/en not_active Expired - Fee Related
- 1994-02-10 JP JP6518622A patent/JPH08506823A/ja not_active Ceased
- 1994-02-10 ES ES94907565T patent/ES2116583T3/es not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| WO1994019323A1 (en) | 1994-09-01 |
| CA2152925A1 (en) | 1994-09-01 |
| AU679207B2 (en) | 1997-06-26 |
| DE69410784D1 (de) | 1998-07-09 |
| JPH08506823A (ja) | 1996-07-23 |
| DE69410784T2 (de) | 1999-01-14 |
| AU6109394A (en) | 1994-09-14 |
| ATE166867T1 (de) | 1998-06-15 |
| US5633266A (en) | 1997-05-27 |
| EP0683767A1 (en) | 1995-11-29 |
| EP0683767B1 (en) | 1998-06-03 |
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