PE20080271A1 - Compuestos heterociclicos como inhibidores del transportador de glicina-1 (glyt-1) - Google Patents

Compuestos heterociclicos como inhibidores del transportador de glicina-1 (glyt-1)

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Publication number
PE20080271A1
PE20080271A1 PE2007000843A PE2007000843A PE20080271A1 PE 20080271 A1 PE20080271 A1 PE 20080271A1 PE 2007000843 A PE2007000843 A PE 2007000843A PE 2007000843 A PE2007000843 A PE 2007000843A PE 20080271 A1 PE20080271 A1 PE 20080271A1
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PE
Peru
Prior art keywords
phenyl
glyt
inhibitors
piperazin
alkyl
Prior art date
Application number
PE2007000843A
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English (en)
Inventor
Stephen Hitchcock
Wenyuan Qian
Xiaoyang Xia
Scott S Harried
Albert Amegadzie
Original Assignee
Amgen Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38565553&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20080271(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of PE20080271A1 publication Critical patent/PE20080271A1/es

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    • C07D241/04Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
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    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
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    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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    • C07D333/14Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms

Abstract

SE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE n ES DE 1 A 3; R1 Y R2 SON CADA UNO H, ALQUILO(C1-C6), ALCOXI(C1-C6), CICLOALQUILO(C3-C10), ENTRE OTROS; R3, R4 Y R5 SON CADA UNO H, ALQUILO(C1-C6), FLUORO O FLUOROALQUILO(C1-C6); Ar1 Y Ar2 SON CADA UNO ARILO(C6-C10), HETEROARILO DE 5 A 10 MIEMBROS, CICLOALQUILO(C3-C10) O HETEROCICLILO DE 5 A 8 MIEMBROS OPCIONALMENTE SUSTITUIDOS CON Rg, Rh O Ri, DONDE Rg ES ALQUILO(C1-C6), HALO, HALOALQUILO(C1-C6), CN, ENTRE OTROS; Rh Y Ri SON CADA UNO ALQUILO(C1-C6), HALO, ALCOXI(C1-C6), CN, CARBOXI, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO (R)-2-(4-(FENIL(3-(TRIFLUOROMETIL)FENIL)METIL)PIPERAZIN-1-IL)ACETICO, ACIDO 2-(4-((3-BROMOFENIL)(FENIL)METIL)PIPERAZIN-1-IL)ACETICO, ACIDO 2-(4-((3,5-DICLOROFENIL)(FENIL)METIL)PIPERAZIN-1-IL)ACETICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DEL TRANSPORTADOR DE GLICINA-1 (GLYT-1) SIENDO UTILES EN EL TRATAMIENTO DE ESQUIZOFRENIA, TRASTORNO PSICOTICO
PE2007000843A 2006-06-28 2007-07-02 Compuestos heterociclicos como inhibidores del transportador de glicina-1 (glyt-1) PE20080271A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US81693606P 2006-06-28 2006-06-28
US85002706P 2006-10-06 2006-10-06

Publications (1)

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PE20080271A1 true PE20080271A1 (es) 2008-04-10

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ID=38565553

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PE2011002078A PE20120223A1 (es) 2006-06-28 2007-07-02 Compuestos heterociclicos como inhibidores del transportador de glicina-1 (glyt-1)
PE2007000843A PE20080271A1 (es) 2006-06-28 2007-07-02 Compuestos heterociclicos como inhibidores del transportador de glicina-1 (glyt-1)

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PE2011002078A PE20120223A1 (es) 2006-06-28 2007-07-02 Compuestos heterociclicos como inhibidores del transportador de glicina-1 (glyt-1)

Country Status (29)

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US (4) US7538114B2 (es)
EP (3) EP2565183A1 (es)
JP (1) JP5179486B2 (es)
KR (2) KR101086589B1 (es)
AR (1) AR077156A1 (es)
AU (1) AU2007265467C1 (es)
BR (1) BRPI0713381A2 (es)
CA (1) CA2655159C (es)
CR (1) CR10570A (es)
CY (1) CY1115119T1 (es)
DK (1) DK2041088T3 (es)
EA (1) EA014959B3 (es)
ES (1) ES2452822T3 (es)
HK (1) HK1126205A1 (es)
HR (1) HRP20140336T1 (es)
IL (1) IL195473A (es)
MX (1) MX2008015448A (es)
MY (1) MY153714A (es)
NO (1) NO20090402L (es)
NZ (1) NZ573129A (es)
PE (2) PE20120223A1 (es)
PL (1) PL2041088T3 (es)
PT (1) PT2041088E (es)
RS (1) RS53277B (es)
SG (1) SG172685A1 (es)
SI (1) SI2041088T1 (es)
TW (1) TWI429631B (es)
WO (1) WO2008002583A1 (es)
ZA (1) ZA201004216B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2655159C (en) 2006-06-28 2014-12-30 Amgen Inc. Glycine transporter-1 inhibitors
MX2010006045A (es) * 2007-12-12 2010-06-23 Amgen Inc Inhibidores de transportador de glicina-1.
CN103096893B (zh) * 2010-06-04 2016-05-04 阿尔巴尼分子研究公司 甘氨酸转运体-1抑制剂、其制备方法及其用途
US9012489B2 (en) 2011-08-03 2015-04-21 Boehringer Ingelheim International Gmbh Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament
JOP20130213B1 (ar) 2012-07-17 2021-08-17 Takeda Pharmaceuticals Co معارضات لمستقبلht3-5
EP3134406A1 (en) 2014-04-24 2017-03-01 Dart Neuroscience (Cayman) Ltd Substituted 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole and 4,5,6,7-tetrahydro-2h-pyrazolo [4,3-c]pyridine compounds as glyt1 inhibitors
PT3201203T (pt) 2014-09-29 2021-08-09 Takeda Pharmaceuticals Co Forma cristalina de 1-(1-metil-1h-pirazol-4-il)-n-((1r,5s,7s)-9-metil-3-oxa-9-azabiciclo[3.3.1]nonan-7-il)-1hindol-3-carboxamida
TWI601712B (zh) 2014-11-05 2017-10-11 達特神經科學(開曼)有限責任公司 作為glyt1抑制劑之經取代之氮雜環丁基化合物
KR101753617B1 (ko) * 2016-05-10 2017-07-11 주식회사 뉴로벤티 피페라진-1-카복사미딘 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 자폐 범주성 장애 예방 및 치료용 약학적 조성물

Family Cites Families (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3032556A (en) * 1962-05-01 Process for the preparation of new
GB817231A (en) * 1956-01-27 1959-07-29 Henri Morren New derivatives of n-mono-benzhydryl-piperazine and process for the preparation thereof
US3928356A (en) 1967-10-06 1975-12-23 Fujisawa Pharmaceutical Co 10-{8 4-({107 -Hydroxy alkyl)-1-piperazimyl{9 -dibenzo (h,f) oxofins and thiepins and acetyl esters thereof
FR2081579B1 (es) 1970-03-18 1973-04-06 Delalande Sa
US4107288A (en) 1974-09-18 1978-08-15 Pharmaceutical Society Of Victoria Injectable compositions, nanoparticles useful therein, and process of manufacturing same
GB1574822A (en) 1976-03-23 1980-09-10 Lafon Labor Acetohydroxamic acid derivatives and pharmaceutical compositions thereof
US4082755A (en) * 1977-02-14 1978-04-04 Janssen Pharmaceutica N.V. 1-[(Diarylmethyl)aminoalkyl]piperidimes
NO155805C (no) 1981-02-06 1987-06-10 Ucb Sa Analogifremgangsmaate for fremstilling av terapeutisk virksomme 2-(4-(difenylmethyl)-1-piperazinyl)-eddiksyrer og deres amider og ikke-toksiske salter.
US4929618A (en) 1988-03-25 1990-05-29 Ube Industries, Ltd. Piperdine and piperazine derivatives, and antihistaminic pharmaceutical compositions containing the same
CA2015949A1 (en) 1989-05-22 1990-11-22 Yasuo Ito Piperidine derivative, method for preparation thereof, and a pharmaceutical composition comprising the same
JPH03184963A (ja) 1989-12-13 1991-08-12 Hokuriku Seiyaku Co Ltd ジベンズオキサゼピン誘導体
JPH03246287A (ja) 1990-02-22 1991-11-01 Hokuriku Seiyaku Co Ltd ピペラジン誘導体
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
JP2767321B2 (ja) 1991-07-19 1998-06-18 ゼリア新薬工業株式会社 ピペラジン誘導体及びこれを含有する医薬
JPH05148234A (ja) 1991-10-02 1993-06-15 Hokuriku Seiyaku Co Ltd アルカン酸誘導体
GB9202238D0 (en) 1992-02-03 1992-03-18 Wellcome Found Compounds
US5807858A (en) 1996-06-05 1998-09-15 Delta Pharmaceutical, Inc. Compositions and methods for reducing respiratory depression
US5538973A (en) 1992-03-27 1996-07-23 Kyoto Pharmaceutical Industries, Ltd. Imidazole derivative, pharmaceutical use thereof, and intermediate therefor
JP3352184B2 (ja) 1993-11-12 2002-12-03 株式会社アズウェル ピペラジン不飽和脂肪酸誘導体
HU213107B (en) 1994-02-23 1997-02-28 Egyt Gyogyszervegyeszeti Gyar Process for producing acetic acid derivatives and pharmaceutical compositions containing them
AU3186395A (en) 1994-08-10 1996-03-07 British Biotech Pharmaceuticals Limited Imidazopyridine derivatives as dual histamine (h1) and platelet activating factor (paf) antagonists
US5700801A (en) 1994-12-23 1997-12-23 Karl Thomae, Gmbh Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
CA2207618A1 (en) 1994-12-23 1996-07-04 Helmut Pieper Piperazine derivatives, medicaments comprising these compounds, their use and processes for their preparation
UA54385C2 (uk) 1995-04-07 2003-03-17 Ново Нордіск А/С N-заміщені азагетероциклічні карбонові кислоти та їх ефіри, спосіб їх одержання, фармацевтична композиція та спосіб лікування
IL117798A (en) 1995-04-07 2001-11-25 Schering Plough Corp Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them
JP3246287B2 (ja) 1995-09-08 2002-01-15 株式会社大林組 既存建物のジャッキアップ工法
US6469009B1 (en) 1996-04-08 2002-10-22 Ucb, S.A. Pharmaceutical compositions for the treatment of rhinitis
AT403803B (de) 1996-04-19 1998-05-25 Sanochemia Ltd Neue benzazepinderivate, diese enthaltende arzneimittel und verwendung derselben zum herstellen von arzneimitteln
WO1997045115A1 (en) 1996-05-31 1997-12-04 Trophix Pharmaceuticals, Inc. Pharmaceutical for treatment of neurological and neuropsychiatric disorders
US6001854A (en) * 1996-05-31 1999-12-14 Allelix Neuroscience Inc. Pharmaceutical for treating of neurological and neuropsychiatric disorders
WO1997045423A1 (en) 1996-05-31 1997-12-04 Trophix Neuroscience Inc. Pharmaceutical for treating of neurological and neuropsychiatric disorders
TW416953B (en) * 1996-09-25 2001-01-01 Takeda Chemical Industries Ltd Tricyclic compounds for eliciting a prostaglandin I2 receptor agonistic effect, their production and use
CA2267500A1 (en) 1996-10-04 1998-04-16 Novo Nordisk A/S N-substituted azaheterocyclic compounds
TW486475B (en) 1996-12-26 2002-05-11 Ube Industries Acid addition salt of optically active piperidine compound and process for preparing the same
GB9709972D0 (en) * 1997-05-19 1997-07-09 Pfizer Ltd Tetrazoles
WO1998055459A1 (fr) * 1997-06-04 1998-12-10 Azwell Inc. Procede pour produire des derives de piperazinesulfonamide et leurs sels
EP0991633A1 (en) 1997-06-25 2000-04-12 Novo Nordisk A/S Novel heterocyclic compounds
GB9804734D0 (en) 1998-03-05 1998-04-29 Pfizer Ltd Compounds
CA2233763C (en) * 1998-03-31 2005-01-11 Teknion Furniture Systems Limited Electrical station
US6894059B1 (en) 1999-03-26 2005-05-17 Ucb S.A. Compounds and methods for treatment of asthma, allergy and inflammatory disorders
US6693099B2 (en) 2000-10-17 2004-02-17 The Procter & Gamble Company Substituted piperazine compounds optionally containing a quinolyl moiety for treating multidrug resistance
EP1632483B1 (en) 2001-02-16 2008-10-29 Aventis Pharmaceuticals Inc. Heterocyclic substituted carbonyl derivatives and their use as dopamine d3 receptor ligands
ES2376399T3 (es) 2001-08-24 2012-03-13 Yale University Compuestos de piperazinona como agentes antitumorales y anticancer�?genos.
PL369108A1 (en) * 2001-09-06 2005-04-18 Schering Corporation 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
US20040259912A1 (en) * 2001-09-28 2004-12-23 Takahiro Matsumoto Benzine derivatives, process for preparing the same and use thereof
DE10149370A1 (de) * 2001-10-06 2003-04-10 Merck Patent Gmbh Pyrazolderivate
WO2003032912A2 (en) * 2001-10-16 2003-04-24 Hypnion, Inc. Treatment of cns disorders using cns target modulators
US7355042B2 (en) 2001-10-16 2008-04-08 Hypnion, Inc. Treatment of CNS disorders using CNS target modulators
CN100500679C (zh) 2001-11-01 2009-06-17 中国人民解放军军事医学科学院毒物药物研究所 具有调节血管内皮细胞功能活性的化合物及其制备方法和用途
CN100486982C (zh) 2001-11-02 2009-05-13 中国人民解放军军事医学科学院毒物药物研究所 具有预防和治疗血栓性疾病功能的化合物,含它们的药物组合物和它们的医药用途
CN100486981C (zh) 2001-11-02 2009-05-13 中国人民解放军军事医学科学院毒物药物研究所 具有预防和治疗动脉粥样硬化功能的化合物及其在生物医药学中的应用
WO2003039255A1 (en) 2001-11-05 2003-05-15 Basf Aktiengesellschaft Use of substituted dibenzothiepine derivatives as insecticidal, acaricidal and nematicidal agents
TW200300757A (en) * 2001-11-16 2003-06-16 Schering Corp Azetidinyl diamines useful as ligands of the nociceptin receptor orl-1
DE60234278D1 (de) 2001-12-06 2009-12-17 Merck & Co Inc Mitotische kinesin-hemmer
AU2002363960B2 (en) 2001-12-06 2008-07-10 Merck Sharp & Dohme Corp. Mitotic kinesin inhibitors
US7378411B2 (en) 2001-12-06 2008-05-27 Merck & Co., Inc. Substituted thienopyrimidinones as a mitotic kinesin inhibitor
US20050107404A1 (en) 2001-12-06 2005-05-19 Fraley Mark E. Mitotic kinesin inhibitors
EP1465896A4 (en) 2001-12-06 2006-01-11 Merck & Co Inc MITOTIC INHIBITORS OF KINESIN
ES2280595T3 (es) * 2001-12-20 2007-09-16 H. Lundbeck A/S Derivados de ariloxifenilo y arilsulfanilfenilo.
JP4454314B2 (ja) 2002-03-27 2010-04-21 サン・ファーマ・アドバンスド・リサーチ・カンパニー・リミテッド 4−(ジアリールメチル)−1−ピペラジニル誘導体
US8476280B2 (en) 2002-05-09 2013-07-02 Versi Group, Llc Compositions and methods for combating lower urinary tract dysfunctions with delta opioid receptor agonists
WO2004004728A1 (en) 2002-07-02 2004-01-15 Ucb Farchim S.A. Diarylmethylpiperazines as prophylactic or therapeutic agents for viral myocarditis
SE0203303D0 (sv) 2002-11-07 2002-11-07 Astrazeneca Ab Novel Compounds
CA2534675C (en) 2003-08-11 2013-07-23 F. Hoffmann-La Roche Ag Piperazine with or-substituted phenyl group and their use as glyt1 inhibitors
SE0400027D0 (sv) 2004-01-09 2004-01-09 Astrazeneca Ab Diarylmethyl piperazine derivatives, preparations thereof and uses thereof
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
JPWO2006043691A1 (ja) 2004-10-18 2008-05-29 株式会社リバース・プロテオミクス研究所 創薬標的タンパク質及び標的遺伝子、並びにスクリーニング方法
CN1709870B (zh) * 2005-07-19 2011-07-06 中国科学院成都生物研究所 光学纯n′,n′-二取代脯氨酰肼化合物及其制备方法和应用
WO2007137417A1 (en) * 2006-05-26 2007-12-06 Neuromed Pharmaceuticals Ltd. Heterocyclic compounds as calcium channel blockers
CA2655159C (en) * 2006-06-28 2014-12-30 Amgen Inc. Glycine transporter-1 inhibitors
CN100506809C (zh) * 2006-11-28 2009-07-01 广西大学 手性二苯甲基哌嗪衍生物及其制备方法

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