| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 41 | 作为血管加压素激动剂的吡咯并[2,1－c][1,4]苯并二氮杂庚因 | CN200380109593.5 | 2003-12-16 | CN1745083A | 2006-03-08 | A·J·莫利纳里; E·J·特里布尔斯基 |
| 新型的式(I)化合物及其药物可接受盐，以及包含这种化合物的组合物，它们在治疗夜间遗尿症、夜间尿急和/或类似疾病中用作抗利尿剂。 | ||||||
| 42 | 新的二氮杂双环芳基衍生物 | CN200480002423.1 | 2004-02-04 | CN1738820A | 2006-02-22 | D·彼得斯; G·M·奥尔森; E·O·尼尔森; T·D·约恩森; P·K·阿林 |
| 本发明涉及被发现为烟碱乙酰胆碱受体的胆碱能配体的新的二氮杂双环芳基衍生物。由于它们的药理学性质，本发明的化合物可以用于治疗与中枢神经系统(CNS)的胆碱能系统、外周神经系统(PNS)相关的各种疾病或障碍，与平滑肌收缩相关的疾病或障碍，内分泌疾病或障碍，与神经－变性相关的疾病或障碍，与炎症相关的疾病或病症，疼痛，和终止化学物质滥用引起的脱瘾症状。 | ||||||
| 43 | 펩타이드 구조물용 아미노산 대체물 | KR1020087026716 | 2007-03-30 | KR101393715B1 | 2014-05-13 | 샤르마셔브디.; 바스토스마가리타; 양웨이; 카이후이-지 |
| 하기 화학식 I의 고리-구속형 아미노산 대체물 (식 중, R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 및 y는 명세서 중에서 정의된 바와 같다), 화학식 I의 고리-구속형 아미노산 대체물의 합성 방법, 및, 화학식 I의 고리-구속형 아미노산 대체물 하나 이상과 복수개의 아미노산 잔기를 포함하는 선형 또는 사이클릭 화합물 및 화학식 I의 고리-구속형 아미노산 대체물 하나 이상과 복수개의 아미노산 잔기를 포함하는 선형 또는 사이클릭 화합물에서 사용하는 것을 포함하는 화학식 I의 고리-구속형 아미노산 대체물의 사용 방법. 고리-구속형 아미노산 대체물, 아미노산 잔기 | ||||||
| 44 | 모노아실화 디아민 중간체를 거친 비대칭 고리형 우레아의제조 방법 | KR1020007003637 | 1998-10-06 | KR1020010024403A | 2001-03-26 | 스톤,벤자민,알.,피.; 앤잴론,루이지; 포투나크,조셉,엠.; 해리스,그레고리,디.; 밸비스,요아니스,아이.; 월터마이어,로버트,이. |
| 본발명은비대칭고리형우레아의개선된제조방법및 비대칭고리형우레아의제조에있어서의중간체에관한것이다. 제조방법에서, 화학식 I-a의디아민을선택적으로모노아실화하여비대칭모노아실화디아민을수득하고, 이것을비대칭중간체로전환할수 있다. 비대칭중간체를더욱알킬화, 고리화및/또는변형시켜, HIV 감염의치료를위한 HIV 프로테아제억제제로서유용한화합물을수득할수 있다. 본발명은다양한종류의비대칭고리형우레아를대량으로제조할수 있다. <화학식Ⅰ-a> | ||||||
| 45 | 6-아릴-치환된-4H-티에노[2,3-e][1,2,4]트리아졸로 [3,4-c][1,4] 디아제핀 | KR1019890005190 | 1989-04-20 | KR1019900016221A | 1990-11-12 | 전성훈; 윌리암조셉홀리한 |
| 내용 없음. | ||||||
| 46 | 벤조 디아제핀의 제조 방법 | KR1019810002855 | 1981-08-06 | KR1019830009056A | 1983-12-17 | 앙리드마른 |
| 내용없음 | ||||||
| 47 | 펩타이드 구조물용 아미노산 대체물 | KR1020087026716 | 2007-03-30 | KR1020090008310A | 2009-01-21 | 샤르마셔브디.; 바스토스마가리타; 양웨이; 카이후이-지 |
| Ring-constrained amino acid surrogates of formula I where R1, R2, R3, R4, R5, R6a, R6b, R7, and y are as defined in the specification, methods for synthesizing ring-constrained amino acid surrogates of formula I, methods of use of ring-constrained amino acid surrogates of formula I, including use in linear or cyclic compounds which include a plurality of amino acid residues and one or more ring-constrained amino acid surrogates of formula I and linear or cyclic compounds which include a plurality of amino acid residues and one or more ring-constrained amino acid surrogates of formula I. | ||||||
| 48 | ２-메틸-４-(４-메틸-１-피페라지닐)-１０Ｈ-티에노[２,３-ｂ][１,５]벤조디아제핀의 순수하고 안정적인 형태를 생성하는 방법 | KR1020087024239 | 2006-03-14 | KR1020090008205A | 2009-01-21 | 판차사라,디네쉬; 굽타,푸르비; 카우쉬크,기테쉬; 두베이,수쉴,쿠마르 |
| Disclosed is an improved process for producing pure and thermally color stable crystalline Form I of 2-methyl-4-(4-methyl-l-piperazinyl)-10H-thieno[2,3-b][l,5] benzodiazepine and product thereof. The process comprises of reacting 2-(2-aminoanilino)-5-methylthiophene-3-carbonitrile with N-methyl piperazine in conjunction with N-methylpiperazine acid salt, to produce 2-methyl-4-(4-methyl-l-piperazinyl)-10H-thieno[2,3-b][l,5] benzodiazepine. Also disclosed is a process for obtaining the Polymorphic Form I of 2-methyl-4-(4-methyl-l-piperazinyl)-10H-thieno[2,3-b][l,5J benzodiazepine by crystallizing the crude 2-methyl-4-(4-methyl-l-piperazinyl)-10H-thieno [2,3-b][l,5] benzodiazepine in a mixture of solvents. Further the invention also provides a new polymorph of Olanzapine, dihydrate Form Ji and process for its preparation and a new hydrate Form J2 of Olanzapine having moisture content 1-3% and process for its preparation. | ||||||
| 49 | 신규한 1,4-디아자바이사이클로알칸 유도체, 이의 제법 및용도 | KR1020057005508 | 2003-09-29 | KR1020050062575A | 2005-06-23 | 페터스단; 올센군나르엠; 닐센엘제베트외스테르가아트; 외르겐센티노다이링; 아링필립케이 |
| This invention relates to novel 1,4- diazabicycloalkane derivatives of formula (I): any of its enantiomers or any mixture of its enantiomers, or a pharmaceutically-acceptable addition salt thereof, or an N-oxide thereof, and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | ||||||
| 50 | PHOSPHOR- UND SCHWEFEL-SUBSTITUIERTE BENZODIAZEPIN-DERIVATE | PCT/EP2016/065756 | 2016-07-05 | WO2017005711A1 | 2017-01-12 | SIEGEL, Stephan; HAENDLER, Bernard; TER LAAK, Antonius; FERNANDEZ-MONTALVAN, Amaury Ernesto; STÖCKIGT, Detlef; SCHMEES, Norbert |
Es werden Bromodomänen-proteininhibitorische, insbesondere BET-proteininhibitorische sowie bevorzugt BRD4-inhibitorische Phosphor- und Schwefel-substituierte Benzodiazepin-Derivate der allgemeinen Formel (I) in der R1, R2, R3, R4 und R5 die in der Beschreibung angegebenen Bedeutungen haben, pharmazeutische Mittel enthaltend die erfindungsgemäßen Verbindungen sowie deren prophylaktische und therapeutische Verwendung bei hyperproliferativen Erkrankungen, insbesondere bei Tumorerkrankungen beschrieben. Des weiteren wird die Verwendung von BET- Proteininhibitoren bei benignen Hyperplasien, atherosklerotische Erkrankungen, Sepsis, Autoimmunerkrankungen, Gefäßerkrankungen, viralen Infektionen, HIV-assoziierten Nierenerkrankungen, neurodegenerativen Erkrankungen, inflammatorischen Erkrankungen, atherosklerotischen Erkrankungen, Herzinsuffizienz, Muskeldystrophien wie zum Beispiel die fazioskapulohumerale Muskeldystrophie und bei der männlichen Fertilitätskontrolle beschrieben. |
||||||
| 51 | STABLE COMPOSITION FOR A PHARMACEUTICAL FORMULATION CONTAINING OLANZAPINE | PCT/IB2006/003937 | 2006-10-27 | WO2007052167A3 | 2007-05-10 | STEFANSSON, Stefan, Einar |
This invention relates to a stable pharmaceutical formulation containing olanzapine. The composition comprises olanzapine or a pharmaceutically acceptable salt thereof, one or more suitable pharmaceutical excipients and a compound of formula (I) and/or a compound of formula (II): or a pharmaceutically acceptable salt thereof. |
||||||
| 52 | BENZOXAZINYL-AMIDOCYCLOPENTYL-HETEROCYCLIC MODULATORS OF CHEMOKINE RECEPTORS | PCT/US2004011281 | 2004-04-09 | WO2004092124A3 | 2005-04-14 | GOBLE STEPHEN D; MILLS SANDER G; YANG LIHU; PASTERNAK ALEXANDER |
| Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula (I): which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions. | ||||||
| 53 | BIS-ARYLSULFONES | PCT/US2001/010848 | 2001-06-08 | WO01098279A2 | 2001-12-27 | |
| The present invention provides pharmaceutically active compounds useful for the treatment of diseases or disorders of the central nervous system. | ||||||
| 54 | VASOPRESSIN ANTAGONIST AND DIURETIC COMBINATION | PCT/US2000/026370 | 2000-09-26 | WO01023366A2 | 2001-04-05 | |
| This invention provides methods of increasing urine flow in humans while minimizing the loss of electrolytes or ions, the methods comprising administering to a human in need thereof a combination of N-[4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)ylcarbonyl)-3-chlorophenyl]-5-fluoro-2-methylbenzamide (or a pharmaceutically acceptable salt thereof), also known as VPA-985, and one or more diuretic agents, as well as pharmaceutical compositions and kits or packages for such combinations. | ||||||
| 55 | NEW 2,3-BENZODIAZEPINE DERIVATIVES | PCT/HU2000/000074 | 2000-07-04 | WO01004122A2 | 2001-01-18 | |
| The invention relates to new 2,3-benzodiazepine derivatives of general Formula (I), (wherein R<1> stands for methyl, formyl, carboxy, cyano, -CH=NOH, -CH=NNHCONH2 or -NR<5>R<6>, wherein R<5> and R<6> independently from each other represent hydrogen or lower alkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R<2> is nitro or amino; R<3> stands for hydrogen, lower alkanoyl or CO-NR<7>R<8>, wherein R<7> and R<8> independently from each other stand for hydrogen, lower alkoxy, lower alkyl or lower cycloalkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R<4> is hydrogen or lower alkyl; the dotted lines have the following meaning: if R<3> and R<4> are not present, the bond between positions C<8> and C<9> is a single bond and the bond between positions C<8> and N<7> is a double bond; if R<3> and R<4> are present, the bonds between positions C<8> and C<9> and between position C<8> and N<7> are single bonds; and if R<3> is present and R<4> is missing, the bond between positions C<8> and C<9> is a double bond and the bond between positions C<8> and N<7> is a single bond) and salts thereof. The invention compounds have neuroprotective effect. | ||||||
| 56 | AMIDE DERIVATIVES | PCT/GB2000/000912 | 2000-03-13 | WO00055153A1 | 2000-09-21 | |
| The invention concerns amide derivatives of Formula (Ia) wherein X is - NHCO- or -CONH-; m is 0-3; R<1> is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-2; R<2> is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino and carboxy; R<3> is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino and N-(1-6C)alkyl-arylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines. | ||||||
| 57 | TRICYCLIC INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASES | PCT/US2000/000411 | 2000-01-10 | WO00042040A1 | 2000-07-20 | |
| Compounds of formula (I) are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation. | ||||||
| 58 | BENZOXAZOLE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT | PCT/JP1999/006491 | 1999-11-19 | WO00031073A1 | 2000-06-02 | |
| Compounds represented by general formula (1) or salts thereof which are useful as the active ingredient of drugs for preventing and/or treating irritable bowel syndrome, systemic functional disorder of digestive tract or diarrhea, wherein R<1> represents halogeno; R<2> represents hydrogen or lower alkyl; and R<3> represents hydrogen, lower alkyl, lower alkoxy, hydroxy(lower alkyl), halogeno or amino optionally having a substituent selected from the group consisting of lower alkyl, lower alkenyl, lower alkylcarbony and amino-protective groups. | ||||||
| 59 | 2-METHYL-THIENO-BENZODIAZEPINE FORMULATION | PCT/US1999/006417 | 1999-03-24 | WO00018408A1 | 2000-04-06 | |
| The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof. | ||||||
| 60 | OXAZOLIDINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS | PCT/US1998/022639 | 1998-10-30 | WO99024428A1 | 1999-05-20 | |
| A compound of Formula (I) or a pharmaceutically acceptable salt thereof, which is antimicrobial agents, effective against various human and veterinary pathogens, including gram positive aerobic organisms, gram negative organisms, and anaerobic organisms. | ||||||
QQ群二维码
意见反馈
意见反馈