HRP20120078T1 - Pirazolinski spojevi kao antagonisti mineralokortikoidnih receptora - Google Patents

Pirazolinski spojevi kao antagonisti mineralokortikoidnih receptora Download PDF

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HRP20120078T1
HRP20120078T1 HR20120078T HRP20120078T HRP20120078T1 HR P20120078 T1 HRP20120078 T1 HR P20120078T1 HR 20120078 T HR20120078 T HR 20120078T HR P20120078 T HRP20120078 T HR P20120078T HR P20120078 T1 HRP20120078 T1 HR P20120078T1
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cyclopentyl
benzo
tetrahydro
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Jay Meyers Marvin
Barbieri Arhancet Graciela
Chen Xiangyang
Landis Hockerman Susan
Allen Long Scott
William Mahoney Matthew
Bruce Reitz David
Gerace Rico Joseph
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Pfizer Products Inc.
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Abstract

Spoj, ili farmaceutski prihvatljiva sol tog spoja, naznačen time što ima strukturu Formule II: gdje: X se bira iz skupine koju čine -CH2- i -O-;Z se bira iz skupine koju čine -C(R81)- i -N-;R1 se bira iz skupine koju čine ciklopentil, ciklobutil i fenil; gdje R1 ciklopentilni, ciklobutilni i fenilni supstituenti mogu izborno biti supstituirani s jednim ili više supstituenata, koje se neovisno bira iz skupine koju čine klor, fluor, metil, etil, propil, klormetil, diklormetil, triklormetil, fluormetil, difluormetil i trifluormetil; R2 se bira iz skupine koju čine vodik ili (C1-C4)-alkil; R5 se bira iz skupine koju čine-(CH2)mOR50, -(CH2)mC(O)OR50, te -(CH2)mC(O)NR51R52; gdje: m je 0, 1, 2 ili 3; R50 se bira iz skupine koju čine vodik i (C1-C6)-alkil; R51 i R52 se neovisno bira iz skupine koju čine vodik i (C1-C6)-alkil; gdje R50, R51 i R52 (C1-C6)-alkilni supstituenti mogu neovisno i izborno biti supstituirani s jednim ili više supstituenata, koje se bira iz skupine koju čine halogen, -OR53, -C(O)R53, -C(O)OR53, -C(O)NR54R55, -NR54R55, -N(R56)C(O)R53; -S(O)pR53, te -S(O)pNR54R55;p je 0, 1 ili 2; R53 se bira iz skupine koju čine vodik, (C1-C6)-alkil, halogen-(C1-C6)-alkil, hidroksi-(C1-C6)-alkil, te karboksi-(C1-C6)-alkil; R54 i R55 se neovisno bira iz skupine koju čine vodik, (C1-C6)-alkil, halogen-(C1-C6)-alkil, hidroksi-(C1-C6)-alkil, te karboksi-(C1-C6)-alkil; iR81, R82, R83, R84 i R85 se neovisno bira iz skupine koju čine vodik, klor, fluor, cijano, hidroksi, karboksi, metil, etil, triklormetil, trifluormetil, cijanometil, hidroksimtil, karboksimtil, metoksi, amino, metilamino, te dimetilamino. Patent sadrži još 19 patentnih zahtjeva.

Claims (20)

1. Spoj, ili farmaceutski prihvatljiva sol tog spoja, naznačen time što ima strukturu Formule II: [image] gdje: X se bira iz skupine koju čine -CH2- i -O-; Z se bira iz skupine koju čine -C(R81)- i -N-; R1 se bira iz skupine koju čine ciklopentil, ciklobutil i fenil; gdje R1 ciklopentilni, ciklobutilni i fenilni supstituenti mogu izborno biti supstituirani s jednim ili više supstituenata, koje se neovisno bira iz skupine koju čine klor, fluor, metil, etil, propil, klormetil, diklormetil, triklormetil, fluormetil, difluormetil i trifluormetil; R2 se bira iz skupine koju čine vodik ili (C1-C4)-alkil; R5 se bira iz skupine koju čine-(CH2)mOR50, -(CH2)mC(O)OR50, te -(CH2)mC(O)NR51R52; gdje: m je 0, 1, 2 ili 3; R50 se bira iz skupine koju čine vodik i (C1-C6)-alkil; R51 i R52 se neovisno bira iz skupine koju čine vodik i (C1-C6)-alkil; gdje R50, R51 i R52 (C1-C6)-alkilni supstituenti mogu neovisno i izborno biti supstituirani s jednim ili više supstituenata, koje se bira iz skupine koju čine halogen, -OR53, -C(O)R53, -C(O)OR53, -C(O)NR54R55, -NR54R55, -N(R56)C(O)R53; -S(O)pR53, te -S(O)pNR54R55; p je 0, 1 ili 2; R53 se bira iz skupine koju čine vodik, (C1-C6)-alkil, halogen-(C1-C6)-alkil, hidroksi-(C1-C6)-alkil, te karboksi-(C1-C6)-alkil; R54 i R55 se neovisno bira iz skupine koju čine vodik, (C1-C6)-alkil, halogen-(C1-C6)-alkil, hidroksi-(C1-C6)-alkil, te karboksi-(C1-C6)-alkil; i R81, R82, R83, R84 i R85 se neovisno bira iz skupine koju čine vodik, klor, fluor, cijano, hidroksi, karboksi, metil, etil, triklormetil, trifluormetil, cijanometil, hidroksimtil, karboksimtil, metoksi, amino, metilamino, te dimetilamino.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R2 je vodik.
3. Spoj u skladu s patentnim zahtjevom 2, naznačen time što: R5 je -(CH2)mC(O)OR50; gdje: m je 0, 1, 2 ili 3; R50 se bira iz skupine koju čine vodik i (C1-C6)-alkil; gdje R50 (C1-C6)-alkilni supstituent može neovisno i izborno biti supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine halogen, -OR53, -C(O)R53, -C(O)OR53, -C(O)NR54R55, -NR54R55, -N(R56)C(O)R53; -S(O)pR53, te -S(O)pNR54R55; p je 0, 1 ili 2; R53 se bira iz skupine koju čine vodik, (C1-C6)-alkil, halogen-(C1-C6)-alkil, hidroksi-(C1-C6)-alkil, te karboksi-(C1-C6)-alkil; i R54 i R55 se neovisno bira iz skupine koju čine vodik, (C1-C6)-alkil, halogen-(C1-C6)-alkil, hidroksi-(C1-C6)-alkil, te karboksi-(C1-C6)-alkil.
4. Spoj u skladu s patentnim zahtjevom 2, naznačen time što: X je -CH2-; Z je -C(R81)- R1 se bira iz skupine koju čine ciklopentil, ciklobutil i fenil; gdje R1 fenilni supstituent može izborno biti supstituiran s fluorom; R5 je -(CH2)mC(O)OR50; gdje: m je 0; R50 je vodik; svaki od R81, R84 i R85 je vodik; i R82 i R83 se neovisno bira iz skupine koju čine klor, cijano, te metil.
5. Spoj u skladu s patentnim zahtjevom 4, naznačen time što R82 je klor, a R83 je cijano.
6. Spoj u skladu s patentnim zahtjevom 4, naznačen time što R1 je ciklopentil.
7. Spoj u skladu s patentnim zahtjevom 4, naznačen time što R1 je fenil; gdje R1 fenilni supstituent može izborno biti supstituiran s fluorom.
8. Spoj u skladu s patentnim zahtjevom 2, naznačen time što: X je -O-; Z je -C(R81)-; R1 se bira iz skupine koju čine ciklopentil, ciklobutil i fenil; gdje R1 fenilni supstituent može izborno biti supstituiran s fluorom; R5 je -(CH2)mC(O)OR50; gdje: m je 0; R50 je vodik; svaki od R81, R84 i R85 je vodik; i R82 i R83 se neovisno bira iz skupine koju čine klor, cijano, te metil.
9. Spoj u skladu s patentnim zahtjevom 2, naznačen time što: X je -CH2-; Z je -N-; R1 se bira iz skupine koju čine ciklopentil, ciklobutil i fenil; gdje R1 fenilni supstituent može izborno biti supstituiran s fluorom; R5 je -(CH2)mC(O)OR50; gdje: m je 0; R50 je vodik; svaki od R81, R84 i R85 je vodik; i R82 i R83 se neovisno bira iz skupine koju čine klor, cijano, te metil.
10. Spoj u skladu s patentnim zahtjevom 2, naznačen time što: X je -O-; Z je -N-; R1 se bira iz skupine koju čine ciklopentil, ciklobutil i fenil; gdje R1 fenilni supstituent može izborno biti supstituiran s fluorom; R5 je -(CH2)mC(O)OR50; gdje: m je 0; R50 je vodik; svaki od R81, R84 i R85 je vodik; i R82 i R83 se neovisno bira iz skupine koju čine klor, cijano, te metil.
11. Spoj u skladu s patentnim zahtjevom 2, naznačen time što ga se bira iz skupine koju čine: 2-(3-klor-4-cijanofenil)-3-(4-fluorfenil)-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 3-(4-fluorfenil)-7-hidroksi-3,3a,4,5-tetrahidrobenzo[g]indazol-2-il)-2-metilbenzonitril; 3-(4-fluorfenil)-7-hidroksi-3,3a,4,5-tetrahidrobenzo[g]indazol-2-il)-2-(trifluormetil)benzonitril; 2-klor-4-(3-(4-fiuorfenil)-7-hidroksi-3,3a,4,5-tetrahidrobenzo[g]indazol-2-il)benzonitril; 2-(3-klor-4-cijanofenil)-3-(4-fluorfenil)-N-(2-(metilsulfonil)etil)-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksamid; 2-(3-klor-4-cijanofenil)-3-ciklopentil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(4-cijanofenil)-3-ciklopentil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(4-cijano-3-metilfenil)-3-ciklopentil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(5-cijano-6-metilpiridin-2-il)-3-ciklopentil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(4-cijano-3-metoksifenil)-3-ciklopentil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; N-(-2-(3-klor-4-cijanofenil)-3-ciklopentil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-il)acetamid; metil-2-(3-klor-4-cijanofenil)-3-ciklopentil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilat; 2-(3-klor-4-cijanofenil)-3-ciklopentil-3a-metil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(3-klor-4-cijanofenil)-3-ciklopentil-N-(2-(metilsulfonil)etil)-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksamid; 2-(3-klor-4-cijanofenil)-3-ciklopentil-N-(2-hidroksietil)-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksamid; 2-(4-cijano-3-metilfenil)-3-ciklopentil-2,3,3a,4-tetrahidrokromeno[4,3-c]pirazol-7-karboksilna kiselina; 2-(3-klor-4-cijanofenil)-3-ciklobutil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(3-klor-4-cijanofenil)-3-ciklopentenil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(4-cijano-3-metilfenil)-3-ciklopentenil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(3-klor-4-cijanofenil)-3-(5-metil-2-furil)-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(3-klor-4-cijanofenil)-3-(3-furil)-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(3-klor-4cijanofenil)-3-(5-metil-2-furil)-N-[2-(metilsulfonil)etil]-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksamid; 2-(3-klor-4-cijanofenil)-N-[2-(metilsulfonil)etil]-3-(2-metil-1,3-tiazol-5-il)-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksamid; 2-(3-klor-4-cijanofenil)-3-ciklopentil-2,3,3a,4-tetrahidrokromeno[4,3-c]pirazol-7-karboksilna kiselina; 2-[4-cijano-3-(trifluormetil)fenil]-3-ciklopentil-2,3,3a,4-tetrahidrokromeno[4,3-c]pirazol-7-karboksilna kiselina; 2-(4-cijano-3-metilfenil)-3-ciklopentenil-2,3,3a,4-tetrahidrokromeno[4,3-c]pirazol-7-karboksilna kiselina; i 2-(3-klor-4-cijanofenil)-3-ciklopentenil-2,3,3a,4-tetrahidrokromeno[4,3-c]pirazol-7-karboksilna kiselina; ili njihove farmaceutski prihvatljive soli.
12. Spoj u skladu s patentnim zahtjevom 2, naznačen time što ga se bira iz skupine koju čine: 2-(3-klor-4-cijanofenil)-3-ciklopentil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; 2-(4-cijano-3-metilfenil)-3-ciklopentil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; i 2-(4-cijano-3-metoksifenil)-3-ciklopentil-3,3a,4,5-tetrahidro-2H-benzo[g]indazol-7-karboksilna kiselina; ili njihove farmaceutski prihvatljive soli.
13. Spoj u skladu s patentnim zahtjevom 2, naznačen time što ima formulu [image] ili njegova farmaceutski prihvatljiva sol.
14. Spoj u skladu s patentnim zahtjevom 2, naznačen time što ima formulu [image] ili njegova farmaceutski prihvatljiva sol.
15. Spoj u skladu s patentnim zahtjevom 2, naznačen time što ima formulu [image] ili njegova farmaceutski prihvatljiva sol.
16. Spoj u skladu s patentnim zahtjevom 2, naznačen time što ima formulu [image]
17. Farmaceutski pripravak, naznačen time što sadrži terapijski djelotvornu količinu spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 16, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljivu podlogu.
18. Pripravak u skladu s patentnim zahtjevom 17, naznačen time što dodatno sadrži terapijski djelotvornu količinu jednog ili više spojeva, koje se bira iz skupine koju čine diuretici, inhibitori angiotenzin-konvertirajućeg enzima, blokatori receptora angiotenzina II, blokatori kalcijskih kanala, β-blokatori, α-blokatori, α,β-blokatori, antagonisti aldosteronskog receptora i inhibitori renina.
19. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 16, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi kao medikament.
20. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 16, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju stanja koje se bira između kardiovaskularnih stanja, stanja bubrega, stanja jetre, vaskularnih stanja, upalnih stanja, boli, retinopatije, neuropatije, inzulinopatije, edema, disfunkcije endotela i disfunkcije baroreceptora.
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Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI431010B (zh) 2007-12-19 2014-03-21 Lilly Co Eli 礦皮質素受體拮抗劑及使用方法
MX336881B (es) * 2009-10-29 2016-02-04 Bristol Myers Squibb Co Compuestos heterociclicos triciclicos.
WO2011141456A1 (en) 2010-05-10 2011-11-17 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for the treatment of fluid accumulation in and/ or under the retina
EP2569310A1 (en) 2010-05-11 2013-03-20 Pfizer Inc Morpholine compounds as mineralocorticoid receptor antagonists
US9241944B2 (en) 2010-06-16 2016-01-26 Institut National De La Santé Et De La Recherche Médicale (Inserm) Methods and compositions for stimulating reepithelialisation during wound healing
CN102372710A (zh) * 2010-08-18 2012-03-14 山东轩竹医药科技有限公司 作为盐皮质激素受体拮抗剂的并环类化合物
WO2012048022A2 (en) * 2010-10-05 2012-04-12 Nova Southeastern University Methods and compositions for therapeutic modulation of aldosterone levels in heart disease
EA029518B1 (ru) 2014-06-30 2018-04-30 Астразенека Аб Бензоксазиноновые амиды в качестве модуляторов минералокортикоидного рецептора
ES2846835T3 (es) 2015-10-13 2021-07-29 Inst Nat Sante Rech Med Métodos y composiciones farmacéuticas para el tratamiento de la neovascularización coroidea
WO2018019843A1 (en) 2016-07-26 2018-02-01 INSERM (Institut National de la Santé et de la Recherche Médicale) Antagonist of mineralocorticoid receptor for the treatment of osteoarthritis
KR102482825B1 (ko) 2016-09-02 2022-12-29 브리스톨-마이어스 스큅 컴퍼니 치환된 트리시클릭 헤테로시클릭 화합물
US11046646B2 (en) 2017-08-09 2021-06-29 Bristol-Myers Squibb Company Alkylphenyl compounds
US11059784B2 (en) 2017-08-09 2021-07-13 Bristol-Myers Squibb Company Oxime ether compounds
CN109051490B (zh) 2018-09-18 2024-07-23 深圳市鲸仓科技有限公司 可移动式密集存拣装置
WO2021180818A1 (en) 2020-03-11 2021-09-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of determining whether a subject has or is at risk of having a central serous chorioretinopathy
EP4395785A1 (en) 2021-08-31 2024-07-10 Inserm (Institut National de la Santé et de la Recherche Scientifique) Methods for the treatment of ocular rosacea
CN113679716B (zh) 2021-10-13 2024-03-26 史大永 溴酚-吡唑啉化合物在治疗猫冠状病毒疾病中的应用
CN114230457B (zh) * 2022-01-04 2023-06-09 中山大学 一类2-亚苄基四氢萘酮衍生物及其制备方法和应用

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1086068A (en) * 1964-09-02 1967-10-04 Ici Ltd Process for the whitening of polymeric materials and nitrogen-containing polycyclic compounds for use therein
BE789948A (fr) * 1971-10-13 1973-04-11 Sandoz Sa Nouveaux derives du pyrazole, leur preparation et leur application comme medicaments
US3816438A (en) * 1972-12-22 1974-06-11 Sandoz Ag 2h(1)-benzothiepino(5,4-c)-pyrazoles and(1)-benzothiopyrano(4,3-c)-pyrazoles
US3843666A (en) * 1973-05-29 1974-10-22 Sandoz Ag Process for preparing substituted indeno,naphtho and cyclohepta pyrazoles
US4866025A (en) * 1988-09-30 1989-09-12 Eastman Kodak Company Thermally-transferable fluorescent diphenylpyrazolines
WO1993015066A1 (en) * 1992-01-23 1993-08-05 Pfizer Inc. Benzopyran and related ltb4 antagonists
GB9318691D0 (en) 1993-09-09 1993-10-27 Merck Sharp & Dohme Therapeutic agents
AR006520A1 (es) 1996-03-20 1999-09-08 Astra Pharma Prod Derivados de 2-arilpirazolisoquinolina y cinolinona y procedimiento para su preparacion.
WO1998009969A1 (en) * 1996-09-05 1998-03-12 Astra Pharmaceuticals Ltd. Novel aryl-pyridazines
JPH10273467A (ja) * 1997-01-29 1998-10-13 Snow Brand Milk Prod Co Ltd 新規テトラロン又はベンゾピラノン誘導体及びその製造方法
IT1292092B1 (it) 1997-06-05 1999-01-25 Geange Ltd Impiego di derivati eterociclici aromatici azotati nel trattamento topico di affezioni di tessuti epiteliali
DE69918542T2 (de) 1998-04-30 2005-08-18 Abbott Gmbh & Co. Kg Substituierte trizyklische pyrazolderivate mit protein kinase aktivität
US6432974B1 (en) * 2000-02-04 2002-08-13 Wyeth Pyrrolo-isoquinoline and tetra-hydropyrrolo-isoquinoline derivatives and their use as mediators of the 5-HT7 receptor
DE60329990D1 (de) 2002-03-08 2009-12-24 Merck & Co Inc Mitotische kinesin-hemmer
JP2006508893A (ja) 2002-03-15 2006-03-16 イーライ・リリー・アンド・カンパニー ステロイドホルモン核内レセプターモジュレーターとしてのジヒドロインドール−２−オン誘導体
TW200400816A (en) 2002-06-26 2004-01-16 Lilly Co Eli Tricyclic steroid hormone nuclear receptor modulators
NZ538426A (en) 2002-08-02 2007-05-31 Vertex Pharma Pyrazole compositions useful as inhibitors of glycogen synthase kinase-3 (GSK-3)
WO2004026306A2 (en) 2002-09-18 2004-04-01 Pfizer Products Inc. Pyrazole derivatives as transforming growth factor (tgf) inhibitors
BRPI0406883A (pt) 2003-01-22 2006-01-03 Lilly Co Eli Composto, composição farmacêutica, método de tratar um distúrbio, e, uso de um composto
ES2308296T3 (es) * 2003-12-19 2008-12-01 Eli Lilly And Company Modulares del receptor nuclear de hormonas esteroideas triciclicas.
JP2007230869A (ja) 2004-04-05 2007-09-13 Takeda Chem Ind Ltd アルドステロン受容体拮抗剤
WO2006010142A2 (en) 2004-07-14 2006-01-26 Ligand Pharmaceuticals, Inc. Mineralocorticoid receptor modulator compounds, processes for their preparation, and their use
PL1773768T3 (pl) 2004-07-30 2019-03-29 Exelixis, Inc. Pochodne pirolu jako środki farmaceutyczne
AU2006205220B2 (en) 2005-01-10 2012-09-13 Exelixis, Inc. Heterocyclic carboxamide compounds as steroid nuclear receptors ligands
EP1844768A1 (en) 2005-01-19 2007-10-17 Dainippon Sumitomo Pharma Co., Ltd. Aromatic sulfone compound as aldosterone receptor modulator
JP2008530094A (ja) 2005-02-10 2008-08-07 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害剤

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