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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 NOVEL AMIDINE COMPOUNDS FOR TREATING MICROBIAL INFECTIONS PCT/US2003/027963 2003-09-05 WO2005033065A1 2005-04-14 TIDWELL, Richard, R.; BOYKIN, David; BRUN, Reto; STEPHENS, Chad, E.; KUMAR, Arvind

Novel amidine and diamidine compounds are useful in the treatment of microbial infections, including mycobacterial, fungal and protozoal infections. Pharmaceutical formulations comprising these compounds can be used in methods of treating microbial infections.

42 AMIDINES AND DERIVATIVES THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM PCT/EP2004/052201 2004-09-16 WO2005028425A2 2005-03-31 ALLEGRETTI, Marcello; CESTA, Maria, Candida; NANO, Giuseppe; BERTINI, Riccardo; BIZZARRI, Cinzia; COLOTTA, Francesco

Amidines and derivatives thereof of formula (I) are described. The process for their preparation and pharmaceutical compositions thereof are also described. The amidines of the invention are useful in the inhibition of chemotaxis of neutrophils induced by IL- 8. The compounds of the invention are used in the treatement of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

43 이노시톨 또는 트리할로스 유도체 및 이를 함유하는 퇴행성뇌신경계 질환 치료용 약학 조성물 KR1020080071383 2008-07-22 KR101021078B1 2011-03-14 정성기; 이우설; 김보람; 임정균; 서브해쉬씨.고쉬
본 발명은 혈뇌장벽(blood-brain barrier)에 대한 투과성이 우수한 이노시톨 또는 트리할로스 유도체에 관한 것으로, 이노시톨 또는 트리할로스 골격구조에 구아니딘기를 도입하여 제조된 본 발명의 화합물은 혈뇌장벽에 대한 투과성이 높아 뇌신경계로의 전달이 용이하므로 알츠하이머병 또는 헌팅턴병과 같은 퇴행성 뇌신경계 질환의 치료에 유용하게 활용될 수 있다. 이노시톨 유도체, 트리할로스 유도체, 혈뇌장벽 투과, 알츠하이머병, 헌팅턴병
44 카르보디이미드및그의제조방법 KR1019990007212 1999-03-05 KR1019990077603A 1999-10-25 코켈,니콜라스; 헤베를레,칼; 크라우스,루퍼트
카르보디이미드구조가비방향족탄소원자에결합되어있는, 카르보디이미드구조및 우레탄및(또는) 우레아구조를함유하며, 25 ℃에서고체인카르보디이미드.
45 아미디노 프로테아제 억제제 KR1019980704943 1996-12-20 KR1019990076817A 1999-10-15 티안바우루; 브루스이.톰주크; 칼,일릭; 리차드엠.솔
본 발명은 하기 화학식 I의 화합물을 비롯한 아미디노 화합물과 벤즈아미디노 화합물 뿐만 아니라 이의 수화물, 이의 용매화물 또는 이의 약학적으로 허용가능한 염에 관한 것으로서, 이 화합물은 여러 단백질 분해 효소를 억제한다. 또한 본 발명은 화학식 I의 화합물을 제조하는 방법에 관한 것이다. 화학식 I 상기 식에서 R 1 내지 R 4 , R 6 내지 R 9 , Y, Z, n 및 m은 명세서에 기술한 바와 같다.
46 신규한 포름아미딘 화합물 KR1019950016208 1995-06-19 KR1019970001314A 1997-01-24 엄현섭; 정동석; 곽광주
본발명은하기일반식(I)의자외선안정제로사용되는포름아미딘화합물및 그의제조방법에관한것이다. (상기식에서 R은탄소수 1~5의알킬기, R는탄소수 2~8의알킬기이고, n은 1~20의정수를나타낸다.)
47 Method for purifying residues containing isocyanates US12067104 2006-09-21 US09061971B2 2015-06-23 Andreas Wölfert; Carsten Knösche; Matthias Klötzer; Hermann Ascherl; Eckhard Stroefer; Heinrich-Josef Blankertz; Michael Schönherr; Martin Karches; Christian Benz
The present invention comprises a process for purifying isocyanate-comprising residues.
48 Process for the preparation of dispersions of cross-linking agents in water US12278275 2007-01-10 US08969471B2 2015-03-03 Laurentius Cornelis Josephus Hesselmans; Marthe Hesselmans; Andries Johannes Derksen
A process for the preparation of stable aqueous polycarbodiimide dispersions to be used as cross-linking agents, in which initially an isocyanate functional polycarbodiimide is prepared from a polyisocyanate and a mono- or polyisocyanate which contains a hydrophobic group. Thereafter the polycarbodiimide chain is capped and/or extended by reaction of the isocyanate functions or a part thereof with a hydrophilic amine- or hydroxy functional compound and of the remaining isocyanate functions with an amine- or hydroxy functional compound which contains hydrophobic groups, after which the obtained product is dispersed in water and the pH is adjusted to 9-14. The hydrophobic groups are hydrocarbons with 4-25 carbon atoms, fluorinated hydrocarbons, silicone functional hydrocarbons or polysilicones. Further, the invention relates to a coating mixture in which the polycarbodiimide dispersion is used as cross-linking agent and to the cured material obtained with the coating mixture.
49 Amino acid derivatives used as pharmaceutical substances US12847544 2010-07-30 US08658826B2 2014-02-25 Bernd Clement; Christiane Wolter-Reeh; Helen Schenk
The invention relates to a method for improving bioavailability of pharmaceutical substances and for allowing the pharmaceutical substances to permeate the blood-brain barrier, the pharmaceutical substances having at least one or more amidine, guanidine, N-hydroxyamidine (amidoxime) or N-hydroxyguanidine functions. The invention also relates to medicaments containing the correspondingly modified pharmaceutical substances.
50 S1P3 receptor antagonist US12088861 2006-10-11 US08546452B2 2013-10-01 Shin-ya Ohnuma; Takeshi Hasegawa; Tomoyuki Sada
The present invention relates to arylamidrazone derivatives having an antagonistic action against S1P3 receptors represented by the following formula (1) or a pharmaceutically acceptable salt thereof:
51 Method for producing colorless isocyanurates of diisocyanates US12530469 2008-03-27 US08373004B2 2013-02-12 Harald Schaefer; Carl Jokisch; Horst Binder; Matthias Kroner; Alexander Bayer
The present invention relates to a novel process for preparing colorless, isocyanurate group-comprising polyisocyanates of (cyclo)aliphatic diisocyanates.
52 Substituted phenylamidines and the use thereof as fungicides US12530566 2008-03-08 US08334237B2 2012-12-18 Thomas Seitz; Klaus Kunz; Wahed Ahmed Moradi; Jörg Nico Greul; Darren James Mansfield; Urlich Heinemann; Amos Mattes; Oswald Ort; Jean-Pierre Vors; Peter Dahem; Ulrike Wachendorff-Neumann; Arnd Voerste
The present invention relates to oxime ether-, hydrazone- or azomethine-substituted phenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the amidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.
53 PROCESS 738 US13264217 2010-04-22 US20120108814A1 2012-05-03 Kay Alison Boardman; Oliver Robert Cunningham; William Robert Fraser Goundry; David Dermot Patrick Laffan
Processes for the preparation of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline, salts thereof, and the intermediates used in the process are described.
54 Iminium salts and methods of preparing electron deficient olefins using such novel iminium salts US12424198 2009-04-15 US08022251B2 2011-09-20 Ciaran B. McArdle; Ligang Zhao
This invention relates to novel iminium salts, which may be in the form of ionic liquids, and a process for producing electron deficient olefins, such as 2-cyanoacrylates, using such an iminium salt, for instance in the form of an ionic liquid.
55 ACETYL MIMIC COMPOUNDS FOR THE INHIBITION OF ISOPRENYL-S-CYSTEINYL METHYLTRANSFERASE US12867796 2009-02-13 US20110053901A1 2011-03-03 Seung-Yub Lee; Michael Voronkov; Peter Wolanin
Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g., Parkinson's disease).
56 Phenylazo-acetoacetanilide derivatives with a polymerizable functional group and related compounds as monomers for preparing polymeric pigment dispersants for inkjet inks US11995329 2006-07-04 US07812113B2 2010-10-12 Geert Deroover; Wojciech Jaunky; Lambertus Groenendaal; Johan Loccufier
A monomer with a chromophore group represented by Formula (I): wherein AR1 represents a substituted or unsubstituted aromatic group; AR2 represents a substituted or unsubstituted aromatic group or a substituted or unsubstituted alkyl group; and R represents a substituted or unsubstituted alkyl group, with the proviso that one of R, AR1, and AR2 has a substituent with a polymerizable functional group. The monomer can be advantageously used to prepare polymeric dispersants for pigment dispersion, especially inkjet inks.
57 BIARYL AND BIHETEROARYL COMPOUNDS USEFUL IN TREATING IRON DISORDERS US12051741 2008-03-19 US20080234384A1 2008-09-25 Mikhail Chafeev; Nagasree Chakka; Jean-Jacques Cadieux; Jianmin Fu; Rajender Kamboj; Vishnumurthy Kodumuru; Jonathan Langille; Shifeng Liu; Jianyu Sun; Serguei Sviridov; Zaihui Zhang
This invention is directed to compounds of formula (I): wherein m, n, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.
58 Fermentation and purification of migrastatin and analog US10838895 2004-05-03 US07375230B2 2008-05-20 Chaitan Khosla; Peter J. Licari; John R. Carney
Migrastatin and a migrastatin analog can be produced by fermentation of Streptomyces platensis NRRL 18993 and used in pharmaceutical formulations to treat cancer and/or inhibit metastasis of cancer cells.
59 Multistage continuous preparation of cycloaliphatic diisocyanates US11185776 2005-07-21 US07371891B2 2008-05-13 Stephan Kohlstruk; Manfred Kreczinski; Hans-Werner Michalczak
The invention relates to a multistage process for continuous and phosgene-free preparation of cycloaliphatic diisocyanates.
60 Bisaminophenyl-based curatives and amidine-based curatives and cure accelerators for perfluoroelastomeric compositions US10768839 2004-01-29 US20050020859A1 2005-01-27 Carl Aufdermarsh; Harshad Amin; Anestis Logothetis; Victor Gubanov; Margarita Volkova; Lioudmila Karmanova; Alexandr Kollar; Polina Troichanskaia; Gennady Emelianov; Vsevolod Berenblit
Novel monoamidine, monoamidoxime and bisamidine curatives, co-curatives and cure accelerators are provided for use with perfluoroelastomeric compositions as well as novel synthesis methods for making monoamidine- and monoamidoxime-based curatives, co-curatives and cure accelerators. Also provided are diphenyl-based curatives, co-curatives and cure accelerators having sufficiently high molecular weight such that the melting temperature of the curatives, co-curatives and cure accelerators is no greater than about 240° C., and more preferably no greater than about 230° C.
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