TR201618160A2 - SPECIAL DRUG MOLECULES SUITABLE FOR USE IN THE TREATMENT OF PARASITIC AND NEOPLASTIC DISEASES AND PROCEDURES FOR THE PREPARATION OF THEIR - Google Patents

SPECIAL DRUG MOLECULES SUITABLE FOR USE IN THE TREATMENT OF PARASITIC AND NEOPLASTIC DISEASES AND PROCEDURES FOR THE PREPARATION OF THEIR Download PDF

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TR201618160A2
TR201618160A2 TR2016/18160A TR201618160A TR201618160A2 TR 201618160 A2 TR201618160 A2 TR 201618160A2 TR 2016/18160 A TR2016/18160 A TR 2016/18160A TR 201618160 A TR201618160 A TR 201618160A TR 201618160 A2 TR201618160 A2 TR 201618160A2
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formula
disease
alkane
cancer
nhconh
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TR2016/18160A
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Hi̇kmet Üçişik Mehmet
Güzel Mustafa
Keski̇n Eli̇f
Onur Sucu Bi̇lgesu
Gölcük Aslihan
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T C Istanbul Medipol Ueniversitesi
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Priority to TR2016/18160A priority Critical patent/TR201618160A2/en
Priority to PCT/TR2017/000131 priority patent/WO2018106200A1/en
Publication of TR201618160A2 publication Critical patent/TR201618160A2/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/14—Aza-phenalenes, e.g. 1,8-naphthalimide
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

Mevcut buluş özgün ilaç moleküllerine, söz konusu ilaç moleküllerinin hazırlanmasında kullanılacak yeni bir üretim yöntemine ve söz konusu özgün ilaç moleküllerinin viral, bakteriyel ve neoplastik hastalıkların tedavisinde kullanılacak bir farmasötik bileşimin hazırlanmasında kullanılmasına ilişkindir.The present invention relates to specific drug molecules, a novel production method for the preparation of said drug molecules, and the use of said specific drug molecules in the preparation of a pharmaceutical composition for use in the treatment of viral, bacterial and neoplastic diseases.

Description

TARIFNAME PARAZITIK VE NEOPLASTIK HASTALIKLARIN TEDAVISINDE KULLANIMA UYGUN ÖZGÜN ILAÇ MOLEKÜLLERI VE BUNLARIN HAZIRLANMASINDA KULLANILACAK USULLER Teknik Alan Mevcut bulus Özgün ilaç moleküllerine, söz konusu ilaç moleküllerinin hazirlanmasinda kullanilacak yeni bir üretim yöntemine ve söz konusu özgün ilaç moleküllerinin viral, bakteriyel ve neoplastik hastaliklarin tedavisinde kullanilacak bir farmasötik bilesimin hazirlanmasinda kullanilmasina iliskindir. DESCRIPTION IN THE TREATMENT OF PARASITIC AND NEOPLASTIC DISEASES ORIGINAL DRUG MOLECULES SUITABLE FOR USE AND THEIR METHODS TO BE USED IN PREPARATION Technical Area The present invention relates to specific drug molecules, a new production method to be used in its preparation and the specific drug in question. molecules to be used in the treatment of viral, bacterial and neoplastic diseases. relates to its use in the preparation of a pharmaceutical composition.

Teknigin bilinen durumu Bakteriyel, viral ve neoplastik hastaliklar dünya popülasyonunun önemli kismini etkilemekte ve ortalama insan ömrü, yasam kalitesi v.b. parametrelerin belirlenmesinde önemli rol oynamaktadir. Bu tip hastaliklar hem is gücünde önemli kayiplara hem de tedavi masrafi nedeniyle ekonomik yüke neden olmaktadir. State of the art Bacterial, viral and neoplastic diseases constitute a significant portion of the world population. affects the average human lifespan, quality of life, etc. your parameters plays an important role in determining These types of diseases are important both in the workforce. It causes both losses and economic burden due to treatment costs.

Bilinen teknikte bakteriyel, Viral, parazitik ve neoplastik hastaliklarin tedavisi için ajanlar bulunmaktadir ancak yine de etkin tedavi saglayacak özgün ajanlara ve bunlarin üretiminde kullanilacak yüksek verimli üretim yöntemlerine ihtiyaç duyulmaktadir. For the treatment of bacterial, viral, parasitic and neoplastic diseases in the prior art agents exist, but still have specific agents and There is a need for highly efficient production methods to be used in their production. is heard.

Parazitik hastaliklarin yaygin türleri arasinda inalarya, trypaiiosoma gibi hastaliklar bulunmaktadir. Yine parazitlk bir hastalik olan Leishmaniasis, Leishmania sinifina ait protozoan parazitlerinin neden oldugu bir hastaliktir. Bu parazitlerin yayilmasinda disi tatarcik sinekleri rol oynar. Leishmaniasis hastaligi Cilt üzerinde, cilt altinda veya Viseral formda olabilir. Viseral türdeki leishmaniasis hastaligi cilt yaralariyla baslayip, ates, alyuvar sayisinda düsüklük ve safra kesesi ve karacigerde büyüme gibi etkiler gösterir. Among the common types of parasitic diseases are diseases such as inaria, trypaiiosoma. are available. Leishmaniasis, which is also a parasitic disease, belongs to the Leishmania class. It is a disease caused by protozoan parasites. In the spread of these parasites sandflies play a role. Leishmaniasis disease On the skin, under the skin or It can be in visceral form. Visceral type leishmaniasis disease starts with skin sores, effects such as fever, low red blood cell count, and enlargement of the gallbladder and liver shows.

Her yil yaklasik 2 milyon yeni leishmaniasis vakasi görülmekte olup bunlarin yaklasik 70000 adedi ölümle sonuçlanmaktadir. Leishinania türü parazitlerin sayica çok olmasi ve ayrica parazitin yayiliminda rol alan tatarcik sinegi türü sayisinin fazlaligi hastaligin bir çok alt türünün olusmasina neden olmustur, bu durum komplike bir tedavi uygulanmasini gerektirmektedir. Approximately 2 million new cases of leishmaniasis are seen each year, and these approximately 70000 of them result in death. The number of parasites of the Leishinania species and also the number of sandfly species involved in the spread of the parasite. Its excess has led to the formation of many subtypes of the disease, this situation requires complex treatment.

Leishmaniasis çogunlukla yoksulluk, keiitsellesme, orman tahribati ve yetersiz beslenmenin oldugu topluluklarda görülmektedir. Hastaligin engellenmesi için asi gelistirme çalismalari yapilmis olmakla beraber yapilan çalismalar sonucunda yeterli koruma saglayan güvenli bir asi gelistirilememistir. Leishmaniasis is mostly caused by poverty, keiitsellesme, deforestation and insufficient It is seen in communities where nutrition is available. To prevent the disease Although development studies have been carried out, sufficient A safe vaccine that provides protection has not been developed.

Dünya saglik örgütü tarafindan Leishmaniasis hastaliginin tedavisi için pentavalent antimon bilesikleri önerilmektedir. Bu tür bilesiklere örnek olarak sodyum stiboglukonat ve meglumin antimoniat verilebilir. Ancak bu ilaçlarin bir dezavantaji söz konusu ilaçlarin toksisitesinin yüksek olmasi nedeniyle medikal gözlem altinda parenteral uygulama ile tedavinin gerçeklestirilmesidir. Pentavalent for the treatment of Leishmaniasis by the World Health Organization antimony compounds are recommended. An example of such compounds is sodium. stibogluconate and meglumine antimoniate may be given. However, a disadvantage of these drugs Due to the high toxicity of the drugs in question, they are under medical observation. treatment with parenteral administration.

Ayrica, tedavi esnasinda hastalarda direnç gelismekte istenilen etkinin gön'jlebilmesi için dozun arttirilmasi ve tedavi süresinin uzatilmasi gerekmektedir. In addition, the desired effect can be achieved in the development of resistance in patients during the treatment. The dose needs to be increased and the duration of treatment extended.

Dünya saglik örgütü tarafindan önerilen diger Leishmaniasis ilaci ise pentamidindir. Önce pentavalent antimona karsi direnç gelistiren hastalarda etkili oldugu düsünülen bu ilacin zaman içerisinde etkinliginin düstügü görülmüstür. Bu durum bu ilaca karsi da direnç gelistigini düsündürmektedir. Ayrica, ilacin düsük tansiyon, kan sekeri düsüklügü, nefrotoksisite, geri dönüsü olmayan diabetes mellitus ve hatta ölüm gibi ciddi yan etkilerinin bulunmasi ilacin dünyanin bazi bölgelerinde kullaniminin tamamen durdurulmasina yol açmistir. Another Leishmaniasis drug recommended by the World Health Organization is pentamidine. It was first thought to be effective in patients who developed resistance to pentavalent antimony. It has been observed that the effectiveness of this drug decreases over time. This is against this drug. It also suggests that resistance is developing. In addition, the drug lowers blood pressure, blood sugar miscarriage, nephrotoxicity, irreversible diabetes mellitus and even death. The presence of serious side effects may prevent the use of the drug in some parts of the world. led to its complete cessation.

Antileishmania aktivitesi gösterdigi bilinen bir diger etken madde ise Amfoterisin B”dir. Bu etken madde de yukarida sayilan diger etken maddeler gibi toksik etki göstermesi nedeniyle medikal gözlem altinda hastalara verilmektedir. Another active ingredient known to show antileishmania activity is Amphotericin. is B. This active substance, like the other active substances mentioned above, has a toxic effect. It is given to patients under medical observation.

Leishmania tedavisinde kullanimi bilinen bir diger etken madde ise miltefosin'dir. Bu etken madde oral yoldan verilmeye olanak sagladigi için hastanin tedaviye adaptasyonunu saglama açisindan bilinen diger etken maddelere göre üstünlük göstermektedir. Ancak söz konusu ajanin teratojenik özellik göstermesi bu ilacin hamilelerde kullanimini imkansiz hale getirmektedir. Another active ingredient known to be used in the treatment of leishmania is miltefosine. This Since the active substance allows oral administration, the patient's treatment superiority over other known active substances in terms of ensuring its adaptation shows. However, because the agent in question has teratogenic properties, this drug makes it impossible to use in pregnant women.

Görüldügü üzere teknigin bilinen durumunda var olan ilaçlarin sayica az olmasi, uygulama yöntemlerinin medikal gözlem gerektirmesi ve ciddi yan etkilerinin olmasi bu hastaligin tedavisini zorlastirmaktadir bu durum yeni etken maddelerin gelistirilmesi ihtiyacini dogurmaktadir. basvuruda çesitli bisnaftalimidopropil türevleri açiklanmakta ve bunlarin Leishmaniasis ve bir neoplastik hastalik olan kanser tedavisindeki etkinlikleri gösterilmektedir. Ancak söz konusu moleküllerin çözünürlüklerinin düsük olmasi bu moleküllerin biyoyararlanimlarini düsürmektedir. Ayrica söz konusu moleküllerin sentez yöntemi fazla sayida ve karmasik adimlardan olustugu için ve verim düsük oldugu için büyük ölçekli endüstriyel üretimler için uygun degildir. As can be seen, the number of drugs available in the state of the art is low, application methods require medical observation and have serious side effects This complicates the treatment of this disease. raises the need for development. The application describes various bisnaphthalimidopropyl derivatives and their Their effectiveness in the treatment of leishmaniasis and cancer, a neoplastic disease. is shown. However, the low solubility of these molecules reduces the bioavailability of molecules. In addition, these molecules Since the synthesis method consists of many and complex steps and the yield is low It is not suitable for large scale industrial production.

Bulusun Amaci Bulus sahipleri bakteriyel, viral, parazitik ve neoplastik hastaliklarin tedavisinde kullanilabilecek alternatif etken maddeler gelistirmeyi amaçlamaktadir. Purpose of the Invention In the treatment of bacterial, viral, parasitic and neoplastic diseases It aims to develop alternative active ingredients that can be used.

Bulus sahipleri ayni zamanda ciddi yan etkileri olmadigi için kullaniini güvenli olan etken maddeler gelistirmeyi hedeflemektedirler. The inventors also consider it safe to use as it does not have serious side effects. They aim to develop active ingredients.

Bulusun bir diger amaci yüksek çözünürlüge sahip etken maddeler gelistirilmesidir. Another aim of the invention is to develop active substances with high solubility.

Bir diger açidan bulus sahipleri biyoyararlanimi yüksek etken maddeler gelistirmeyi hedef lemektedirler. On the other hand, inventors want to develop active substances with high bioavailability. they are targeting.

Bulus sahipleri ayni zamanda bakteriyel, viral, parazitik ve neoplastik hastaliklarin tedavisinde kullanima uygun moleküllerin sentezinde kullanilabilecek az sayida ve yüksek verimli adimlardan olusan bir üretim yöntemi gelistirmeyi amaçlamaktadir. The inventors are also responsible for bacterial, viral, parasitic and neoplastic diseases. There are few and many drugs that can be used in the synthesis of molecules suitable for use in therapy. aims to develop a production method consisting of highly efficient steps.

Bulus sahipleri bu sekilde söz konusu etken maddelerin üretim maliyetini düsürerek ilacin daha büyük kitlelere ulasmasini hedeflemektedir. In this way, the inventors can reduce the production cost of the said active substances. It aims to reach larger masses of the drug.

Bu amaçlar dogrultusunda çalismalar gerçeklestiren bulus sahipleri bakteriyel, viral, neoplastik ve L-eishmania gibi parazitik hastaliklarin tedavisinde kullanima uygun formül I ile gösterilen molekülleri ve söz konusu moleküllerin üretiminde kullanilabilecek bir üretiin yöntemini gelistirrnislerdir. Inventors who carry out studies in line with these purposes have bacterial, viral, Suitable for use in the treatment of neoplastic and parasitic diseases such as L-eishmania. the molecules represented by the formula I and in the production of said molecules They have developed a production method that can be used.

Bulusun Detayli Anlatimi Mevcut bulus Formül 1 ile gösterilen moleküllere iliskindir. Detailed Description of the Invention The present invention relates to molecules represented by Formula 1.

RA: Ci-Cs alkan, Ci-C5 alken veya C1 -C5 alkin X: Cl, F, Br veya I RB : -X, -NHZ, -COORS, -CHZCHNHZCOORg, -NRgRg ve L: R1, R2, R3, R4, R5, R6, RB = -H ve L=R1, R2, R3, R4, R5, R6 olup; R1: -OCOO-Rg-OOCO-; R2: -NHCONH-Rg-NHCONHg R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH- ve R8 ve R9 ise birbirinden bagimsiz olarak C1-C10 alkan, alken, alkin içerisinden seçilir. RA: Ci-Cs alkane, Ci-C5 alkene or C1-C5 alkyne X: Cl, F, Br or I RB : -X, -NHZ, -COORS, -CHZCHNHZCOORg, -NRgRg and L: R1, R2, R3, R4, R5, R6, RB = -H and L=R1, R2, R3, R4, R5, R6; R1: -OCOO-R8-OOCO-; R2: -NHCONH-Rg-NHCONHg R3: -OCOHN-R8-NHOCO-; R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH- and R8 and R9 are independently selected from C1-C10 alkane, alkene, alkyne.

Mevcut bulus kapsaminda kullanilan “alkan” terimi düz veya dallanmis doymus hidrokarbon Zincirlerini ifade etmektedir. The term "alkane" used in the present invention is straight or branched saturated stands for hydrocarbon chains.

Mevcut bulus kapsaminda kullanilan “alken” terimi en az bir karbon-karbon çift bagi içeren düz veya dallanmis hidrokarbon Zincirlerini ifade etmektedir. The term "alkene" as used in the present invention has at least one carbon-carbon double bond. It refers to straight or branched hydrocarbon chains containing

Mevcut bulus kapsaminda kullanilan “alkin” terimi en az bir karbon-karbon üçlü bagi içeren düz veya dallanmis hidrokarbon Zincirlerini ifade etmektedir. The term "alkyne" as used in the present invention has at least one carbon-carbon triple bond. It refers to straight or branched hydrocarbon chains containing

Bulusun bir uygulamasinda R3; C1 alkan, C2 alkan, C3 alkan, C4 alkan, C5 alkan, C6 alkan, C7 alkan, C3 alkan, C9 alkan veya C 10 alkandan olusan bir grubun içerisinden seçilir. In one embodiment of the invention, R3 is; C1 alkane, C2 alkane, C3 alkane, C4 alkane, C5 alkane, C6 alkane, C7 alkane, C3 alkane, C9 alkane, or C10 alkane is selected.

Bulusun bir uygulamasinda R9; C1 alkan, C2 alkan, C3 alkan, C4 alkan, C5 alkan, C6 alkan, C7 alkan, C3 alkan, C9 alkan veya Cm alkandan olusan bir grubun içerisinden seçilir. In one embodiment of the invention, R9; C1 alkane, C2 alkane, C3 alkane, C4 alkane, C5 alkane, C6 alkane, C7 alkane, C3 alkane, C9 alkane, or Cm alkane is selected.

Burada gösterilen sekliyle RB gösterildigi benzen halkasinin üzerinde herhangi bir karbona bagli olabilir. Ayrica her iki halkada da birbirinden farkli RB gruplari bu iki halka üzerindeki herhangi bir karbon atomuna bagli sekilde bulunabilir. Söz konusu çizim IUPAC tarafindan 2008 yilinda yayinlanan “Graphical representation standard for Chemical structure diagrams” baslikli yayinin GR 9.4. numarali bölümünde anlatilan kapsamdaki gibi, halka üzerindeki herhangi bir hidrojen atomunun burada tanimlanan RB grubu ile degistirebileeegini göstermektedir. Bulusun tercih edilen bir uygulamasinda mevcut bulusa uygun etken maddeler Formül 1 ile gösterilmekte olup RA: C3 alkan R1: -OCOO-Rg-OOCO-; R2: -NHCONH-Rg-NHCONHg R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R8: C i-C 10 alkandir, Bulusun tercih edilen bir diger uygulamasinda mevcut bulusa uygun etken maddeler Formül 1 ile gösterilmekte olup RA: C3 alkan R1: -OCOO-Rg-OOCO-g R2: -NHCONH-Rg-NHCONH-g R3: -OCOHN-Rg-NHOCO-g R4: -NHCOO-Rg-OOCNHj R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH R8: C i-C 10 alkandir. Any on the benzene ring as shown RB as shown here It may be due to carbon. In addition, different RB groups in both rings are present in these two rings. can be found attached to any carbon atom on the ring. Aforementioned The drawing was published in the “Graphical representation standard” published by IUPAC in 2008. For Chemical structure diagrams” GR 9.4. in section no. as in the scope described, where any hydrogen atom on the ring It shows that you can change it with the defined RB group. Invent a preferred The active ingredients in accordance with the invention available in the application are shown with Formula 1. RA: C3 alkane R1: -OCOO-R8-OOCO-; R2: -NHCONH-Rg-NHCONHg R3: -OCOHN-R8-NHOCO-; R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R8: C i-C 10 alkanes, In another preferred embodiment of the invention, the active ingredients according to the present invention It is represented by the formula 1 RA: C3 alkane R1: -OCOO-Rg-OOCO-g R2: -NHCONH-Rg-NHCONH-g R3: -OCOHN-Rg-NHOCO-g R4: -NHCOO-Rg-OOCNHj R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH R8 is C1-C10 alkane.

Bulusun tercih edilen bir diger uygulamasinda mevcut bulusa uygun etken maddeler Formül I ile gösterilmekte olup RA: C3 alkan R1: -OCOO-Rg-OOCO-g R2: -NHCONH-Rg-NHCONH-; R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH R3: Ci-C 10 alkandir. In another preferred embodiment of the invention, the active ingredients according to the present invention It is represented by the formula I. RA: C3 alkane R1: -OCOO-Rg-OOCO-g R2: -NHCONH-R8-NHCONH-; R3: -OCOHN-R8-NHOCO-; R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH R3 is C1-C10 alkane.

Bulusun tercih edilen bir diger uygulamasinda mevcut bulusa uygun etken maddeler Formül 1 ile gösterilmekte olup RA: C3 alkan RB = -CHzCHNHQCOORg R1: -OCOO-Rg-OOCO-; R2: -NHCONH-Rg-NHCONH-; R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH Rg: Ci-Cio alkandir. In another preferred embodiment of the invention, the active ingredients according to the present invention It is represented by the formula 1 RA: C3 alkane RB = -CHzCHNHQCOORg R1: -OCOO-Rg-OOCO-; R2: -NHCONH-R8-NHCONH-; R3: -OCOHN-R8-NHOCO-; R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH Rg: Ci-Cio alkane.

Bulusun tercih edilen bir diger uygulamasinda mevcut bulusa uygun etken maddeler Formül 1 ile gösterilmekte olup RA: C3 alkan R1= -OCOO-Rg-OOCO-; R2: -NHCONH-Rg-NHCONH-; R3: -OCOHN-Rg-NHOCO-g R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH R8: Ci-Cm alkan R9: C 1-C io alkandir. In another preferred embodiment of the invention, the active ingredients according to the present invention It is represented by the formula 1 RA: C3 alkane R1=-OCOO-R8-OOCO-; R2: -NHCONH-R8-NHCONH-; R3: -OCOHN-Rg-NHOCO-g R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH R8: Ci-Cm alkane R9: C 1-C10 alkane.

Bulusun tercih edilen bir uygulamasinda formül I ile gösterilen bilesik N1,N8-bis(3- gösterilmektedir. l-oimul I-.i Bulusun tercih edilen bir uygulamasinda formül I ile gösterilen bilesik 1,1'-(bütan- Ib ile gösterilmektedir. In a preferred embodiment of the invention, the compound represented by formula I is N1,N8-bis(3- is shown. l-oimul I-.i In a preferred embodiment of the invention, the compound represented by formula I is 1,1'-(butane- It is denoted by ib.

O Fni'miil Ih Bulusun tercih edilen bir uygulamasinda formül 1 ile gösterilen bilesik Butane-l,4-diil bis((3-(l ,3-di0kso-lH-ben20[de]isokiiiolin-2(3H)-il)pr0pil)karbamat) olup formül le ile gösterilmektedir. O Fni'miil Ih In a preferred embodiment of the invention, the compound represented by formula 1 is Butane-1,4-diyl. bis((3-(1,3-diOxo-1H-ben2O[de]isociiiolin-2(3H)-yl)propyl)carbamate) with the formula le is shown with.

O 0 lini'miil li: Bulusun tercih edilen bir uygulamasinda formül I ile gösterilen bilesik bis(3-(l,3- diokso-l H-benzo[de]isokin01in-2(3H)-il)pr0pil) bütane-I ,4-diildikarbamat olup 0 NMOÄNWNYOWN O Bulusun tercih edilen bir uygulamasinda formül I ile gösterilen bilesik bütane-l ,4-diil bis(3-(1,3-di0kso-lH-benzo[de]isokinolin-2(3H)-il)pr0pil) bis(karb0nat) olup formül le ile gösterilmektedir. o Q I-'oi'iiiiil lu 0 O Bulusun tercih edilen bir uygulamasinda formül I ile gösterilen bilesik N,N'-(oktan- l,8-dii1)bis(3-(l,3-di0kso-lH-benzo[de]isokinolin-Z(3H)-il)propanamid) olup formül O Formül [t Yukarida kimyasal yapilari ve spesifik kimyasal isimlendirmeleri verilen formül Ia-lf molekülleri bulusu açiklamak amaçli verilmis olup bulus kapsami bu moleküllerle sinirlandirilmamaktadir. O 0 lini'miil li: In a preferred embodiment of the invention, the compound represented by formula I is bis(3-(1,3-) dioxo-1H-benzo[de]isoquin01in-2(3H)-yl)propyl)butane-1,4-dididicarbamate 0 NMOÄNWNYOWN O In a preferred embodiment of the invention, the compound of formula I is butane-1,4-diyl The formula is bis(3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl) bis(carbonate) It is indicated with le. o Q I-'oi'iiiiii lu 0 O In a preferred embodiment of the invention, the compound represented by formula I is N,N'-(octane- 1,8-diyl1)bis(3-(1,3-dioxo-1H-benzo[de]isoquinolin-Z(3H)-yl)propanamide) with the formula O Formula [t Formula Ia-lf, whose chemical structures and specific chemical nomenclature are given above molecules are given to explain the invention and the scope of the invention is not limited to these molecules. not angered.

Mevcut bulus bir diger açidan, bulusa uygun formül I ile gösterilen moleküllerin hazirlanmasinda kullanilacak usullere yöneliktir. In another aspect, the present invention is concerned with the molecules represented by the formula I according to the invention. for the methods to be used in its preparation.

Bulusa uygun Formül 1 ile gösterilen etken maddelerin elde edilmesinde kullanilabilecek bir metot (Metot 1); i. Formül II ile gösterilen maddenin uygun bir çözücü varliginda CDI ile reaksiyona 1 5 sokulmasi, ii. Olusan ara ürünün Formül 111 ile gösterilen madde ile DIEA varliginda reaksiyona sokulmasi, ve Formül III iii. Son ürünün reaksiyon karisimindan izole edilmesi adimlarini içermekte olup burada verilen Rm ve R1] birbirinden bagimsiz olarak -OH ve -NH2 gruplari içerisinden; RB, -H, -X, -NHz, -COORg, -CHzCHNHzCOORg veya -NRgRg içerisinden; Rg ve R9 ise birbirinden bagimsiz olarak Ci-Cio alkan, alken, alkin içerisinden seçilir ve n ise 1-10 arasinda bir dogal sayidir. In obtaining the active substances indicated by Formula 1 according to the invention a method that can be used (Method 1); I. The substance represented by formula II can be reacted with CDI in the presence of a suitable solvent. 1 5 stings, ii. The intermediate product formed reacts with the substance indicated by Formula 111 in the presence of DIEA. insertion, and Formula III iii. Isolation of the final product from the reaction mixture Rm and R1] given herein are independently -OH and -NH2 groups; RB, -H, -X, -NHz, -COORg, -CHzCHNHzCOORg or from -NRgRg; Rg and R9 are independently Ci-Cio alkane, alkene, It is chosen from alkyne and n is a natural number from 1-10.

Bulusa uygun Formül 1 ile gösterilen etken maddelerin elde edilmesinde kullanilabilecek bir metot (Metot 11); i. Formül 11 ile gösterilen maddenin uygun bir çözücü içerisinde çözülmesi, RB Formül II ii. Reaksiyon karisimina formül IV ile gösterilen maddenin eklenmesi, Formül IV iii. Reaksiyon karisimina baz eklenmesi ve iv, Son ürünün reaksiyon karisimindan izole edilmesi Adiinlarini içermekte olup burada verilen Rio -OH ve -NH2 gruplari içerisinden, X ise -Cl, -Br, -1, -F içerisinden RB, -H, -X, -NH2, -COORg, -CH2CHNH2COOR3 veya -NRgRg içerisinden; R3 ve R9 ise birbirinden bagimsiz olarak C i-C 10 alkan, alken, alkin içerisinden seçilir ve n ise 1-10 arasinda bir dogal sayidir. In obtaining the active substances indicated by Formula 1 according to the invention a method that can be used (Method 11); I. Dissolving the substance represented by formula 11 in a suitable solvent, RB Formula II ii. Adding the substance represented by formula IV to the reaction mixture, Formula IV iii. Adding base to the reaction mixture and iv, Isolation of the final product from the reaction mixture Contains Adiinlarines, from the Rio -OH and -NH2 groups given here, X if -Cl, -Br, -1, -F out of RB, -H, -X, -NH2, -COORg, -CH2CHNH2COOR3 or from -NRgRg; R3 and R9 are independently C i-C 10 alkanes, alkenes, It is chosen from alkyne and n is a natural number from 1-10.

Burada bahsi geçen “baz” , K1/K2C03 , NaH, N,N-Diisopropylethylamine (DIEA), trietilamin (TEA)°dan olusan bir grubun içerisinden seçilebilir. The “base” mentioned here is K1/K2C03 , A group consisting of NaH, N,N-Diisopropylethylamine (DIEA), triethylamine (TEA) can be selected from.

Bulusa uygun Forinül I ile gösterilen etken maddelerin elde edilmesinde kullanilabilecek bir metot (Metot 111); i. Formül V ile gösterilen maddenin uygun bir çözücü içerisinde çözülmesi ve DCC ve HOBt varliginda reaksiyona sokulmasi, RB Formül V ii. Reaksiyon karisimina formül III ile gösterilen maddenin eklenmesi, Formül III iii. Son ürünün reaksiyon karisimindan izole edilmesi Adimlarini içermekte olup burada verilen RIO ve R1] bagimsiz olarak *OH ve *NHZ gruplari içerisinden; RB, -H, -X, -NHZ, -COORS, -CHZCHNHZCOORS veya -NRgRg içerisinden; R3 ve R9 ise birbirinden bagimsiz olarak Ci-Cio alkan, alken, alkin içerisinden seçilir, 11 ise 1-10 arasinda bir dogal sayidir. In the preparation of active substances indicated by Formula I according to the invention a method that can be used (Method 111); I. Dissolving the substance represented by formula V in a suitable solvent and DCC and reacting in the presence of HOBt, RB Formula V ii. Addition of the substance of formula III to the reaction mixture, Formula III iii. Isolation of the final product from the reaction mixture RIO and R1] given herein are independently *OH and *NHZ. among their groups; RB, -H, -X, -NHZ, -COORS, -CHZCHNHZCOORS or -NRgRg through; R3 and R9 are independently Ci-Cio alkane, alkene, alkyne. It is chosen from among, 11 is a natural number between 1-10.

Burada kullanilan “bir çözücü” terimi, reaksiyon esnasinda kullanilan reaktiflerin çözünmesini saglayacak herhangi bir organik solventi ifade etmektedir. The term “a solvent” as used herein refers to the reagents used during the reaction. It refers to any organic solvent that will dissolve it.

Söz konusu organik solvent asetik asit, aseton, asetonitril, benzen, l-butanol, 2- butaiiol, 2-butanon, t-butil alkol, karbon tetraklorür, klorobenzen, kloroform, siklohekzan, 1,2-dik10r0etan, dietileii glikol, dietileter, dietilen glikol dimetil eter, 1,2- dimetoksietan (DME), dimetilformamid (DMF), dimetilsülfoksit (DMSO), 1,4- dioksan, etanol, etil asetat, etilen glikol, gliserin, heptan, hekzametilfosforamid (HMPA), hekzametilfosforus triamid (HMPT), hekzan, metanol, metilt-bütil eter (MTBE), inetilen klorür (DCM), N-metil-Z-pirolidon (NMP), nitroinetan, pentan, petrol eteri, l-propanol, Z-propanol, piridin, tetrahidrofuran (THF), tolüen, trietil amiii, su, o-ksilen, m-ksilen, p-ksilen`den olusan bir grubun içerisinden seçilebilir. The organic solvent in question is acetic acid, acetone, acetonitrile, benzene, 1-butanol, 2- butaiiol, 2-butanone, t-butyl alcohol, carbon tetrachloride, chlorobenzene, chloroform, cyclohexane, 1,2-dichloroethane, diethylene glycol, diethylether, diethylene glycol dimethyl ether, 1,2- dimethoxyethane (DME), dimethylformamide (DMF), dimethylsulfoxide (DMSO), 1,4- dioxane, ethanol, ethyl acetate, ethylene glycol, glycerin, heptane, hexamethylphosphoramide (HMPA), hexamethylphosphorus triamide (HMPT), hexane, methanol, methylt-butyl ether (MTBE), inethylene chloride (DCM), N-methyl-Z-pyrrolidone (NMP), nitroinethane, pentane, petroleum ether, 1-propanol, Z-propanol, pyridine, tetrahydrofuran (THF), toluene, triethyl amiii, water, o-xylene, m-xylene, p-xylene.

Bulusun tercih edilen bir uygulamasinda Metot I”de solvent olarak DMF veya THF kullanilmaktadir. In a preferred embodiment of the invention, DMF or THF as solvent in Method I is used.

Bulusun tercih edilen bir uygulamasinda Metot Il”de solvent olarak DCM ve/veya DMF kullanilmaktadir. In a preferred embodiment of the invention, DCM and/or DCM as the solvent in Method II DMF is used.

Bulusun bir uygulamasinda Metot III'de solvent olarak THF kullanilmaktadir. In one embodiment of the invention, THF is used as the solvent in Method III.

Metot 1, II ve III ile gösterilen yöntemler oda sicakliginda veya 25-40 0C araliginda bir sicaklikta gerçeklestirilebilirler. Her bir metot içerisindeki adim bir digerinde farkli bir sicaklikta gerçeklestirlebilir. The methods shown in Methods 1, II, and III are kept at room temperature or in the range of 25-40 0C. can be carried out at one temperature. The step in each method is in another can be performed at a different temperature.

Bulusa uygun yöntemlerle elde edilen ürünler, filtrasyon, santrifüj, ekstrasyon, kristalizasyon, rekristalizasyon, kromatografi, distilasyon gibi yöntemlerle saflastirilabilir. Products obtained by methods according to the invention, filtration, centrifugation, extraction, methods such as crystallization, recrystallization, chromatography, distillation can be purified.

Burada bahsedilen kromatografi yöntemi; kolon kromatografisi, gaz kromatogratisi, sivi kromatografisi, ters fazli sivi kromatografisi içerisinden seçilebilir. The chromatography method mentioned here; column chromatography, gas chromatography, liquid chromatography can be selected from reversed phase liquid chromatography.

Bulusa uygun moleküllerin hazirlanmasina kullanilabilecek Metot I, Metot II ve Metot III isimli yöntemler hem sagladiklari reaksiyon verimi bakimindan hem de daha az sayida adim içermeleri bakimindan teknigin bilinen durumunda bu tip moleküllerin hazirlanmasi için kullanilan yöntemlere üstünlük göstermektedir. Methods I, Method II and Methods named Method III are both in terms of the reaction efficiency they provide and In the state of the art, these types of steps include fewer steps. It is superior to the methods used for the preparation of molecules.

Mevcut bulus kapsaminda tanimlanan Metot I, Metot II ve Metot III ile elde edilen moleküller asagida verilen formül I ile tanimlanmakta olup; RA: Ci-Cs alkan, Ci-Cs alken veya Ci-Cs alkin X: Cl, F, Br veya I RB : -H, -X, -NH2, -COORS, -CH2CHNH2COOR8, -NRgRg ve L: R1, R2, R3, R4, R5, R6, R7 olup; R1: -OCOO-Rg-OOCO-; R2: -N HCONH-Rg-N HCONH-; R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH- ve R8 ve R9 ise birbirinden bagimsiz olarak Ci-Cm alkan, alken, alkin içerisinden seçilir. Obtained by Method I, Method II and Method III described in the present invention molecules are defined by the formula I given below; RA: Ci-Cs alkane, Ci-Cs alkene or Ci-Cs alkyne X: Cl, F, Br or I RB : -H, -X, -NH2, -COORS, -CH2CHNH2COOR8, -NRgRg and L: R1, R2, R3, R4, R5, R6 is R7; R1: -OCOO-R8-OOCO-; R2: -N HCONH-R8-N HCONH-; R3: -OCOHN-R8-NHOCO-; R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH- and R8 and R9 are independently selected from Ci-C12 alkane, alkene, alkyne.

Bulus bir diger açidan Metot I, Metot II ve Metot III kullanilarak elde edilen formül I moleküllerine iliskindir RA: Ci-Cs alkan, Ci-Cs alken veya C1-C5 alkin X= C1, F, Br veya I RB : -H, -X, -NH2, -COORg, -CHgCHNl'bCOORg, -NRgRg VC L: R1, R2, R3, R4, R5, R6, R7 Olup; R2: -NHCONH-Rg-NHCONH-; R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH- ve R8 ve R9 ise birbirinden bagimsiz olarak Ci-Cio alkan, alken, alkin içerisinden seçilir. In another aspect of the invention, formula I obtained using Methods I, Method II and Method III relates to molecules RA: Ci-Cs alkane, Ci-Cs alkene or C1-C5 alkyne X= C1, F, Br or I RB : -H, -X, -NH2, -COORg, -CHgCHNl'bCOORg, -NRgRg VC L: R1, R2, R3, R4, R5, R6 is R7; R2: -NHCONH-R8-NHCONH-; R3: -OCOHN-R8-NHOCO-; R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH- and R8 and R9 are independently selected from Ci-Cio alkane, alkene, alkyne.

Mevcut bulusa uygun metot I, metot II ve metot [11 ile elde edilen, yukarida tanimlanan formül I bilesikleri daha az reaksiyon adimi kullanilarak ve daha yüksek verimle elde edilmektedir ayrica bu sekilde forinül I ile gösterilen moleküllerin daha kisa sürede elde edildigi de görülmüstür. Obtained by method I, method II and method [11, above, according to the present invention. compounds of formula I described using fewer reaction steps and higher It is obtained with efficiency, and in this way, the molecules indicated by forinule I are more It has also been seen that it is obtained in a short time.

Bulus bir diger açidan Formül 1 ile gösterilen bilesiklerin ilaç olarak kullanimini açiklamaktadir. Another aspect of the invention is the use of compounds of Formula 1 as drugs. explains.

Mevcut bulus bir açidan bulusa uygun Formül I ile gösterilen moleküllerin parazitik hastaliklarin tedavisinde kullanimina iliskindir. In one aspect, the present invention shows that the molecules represented by Formula I according to the invention are parasitic. related to its use in the treatment of diseases.

Burada kullanilan “parazitik hastaliklar” ifadesi bir parazitin neden oldugu veya bulastirdigi hastaliklari ifade etmektedir. The term “parasitic diseases” as used herein is caused by a parasite or refers to the diseases it transmits.

Burada bahsedilen parazitik hastaliklar sistozomiyaz, opistorsiyaz, klonorkiyaz, dikrosölyoz, fasioliyazis, paragonimiyaz, fasiolopsiyaz, ekinokokiyaz, tenyazis, sistiserkoz, difilobotrtyaz, sparganoz, himenolepiyaz, drakunkuliyaz, onkoserkiyazis, filaryaz, elefantiyazis, mansonelloz, trisinelozis, ankilostomiyaz, nekatoryaz, ankilostomyazis, askardiyoz, strongiloidiyaz, trisüriyaz, enterobiyazis, anisakiyaz, helmintiyazis, trikostronjiloz, anjiyostrongiloz, gnatostomiyaz, anjiyostrongiloz, singamiyaz, hirudiniyaz, akantosefallyaz, gongilonemiyaz, metastrongilyaz. telaziyaz, pediküloz, pithiriyaz, skabiyez, miyaz, tungiyaz, trombikuloz, skarabiazis, hirudiniyaz, linguatuloz, porosefaliyaz, leishmania, trypanosomiasis, plazmodyum falsiparum”un neden oldugu malarya, plazmodyum vivax”m neden oldugu malarya, plazmodyum malariae'nin neden oldugu malarya, chagas hastaligi, toksoplazma, pnömosistoz, babeziyoz, piroplazmoz, akantamebiyaz, naegleriyaz ve/veya mikrosporidioz olabilir. The parasitic diseases mentioned here are cystosomiasis, opistorciasis, clonorchiasis, dicrocoeliosis, fascioliasis, paragonimiasis, fasciolopsia, echinococciasis, tapeworm, cysticercosis, diphylobothriasis, sparganosis, hymenolepiiasis, dracunculiasis, onchocerciasis, filariasis, elephanthiasis, mansonellosis, tricinelosis, ankylostomiasis, necatoriasis, ankylostomiasis, ascardiosis, strongyloidiasis, trisuria, enterobiasis, anisakiasis, helminthiasis, trichostonyllosis, angiostrongylosis, gnatostomiasis, angiostrongilosis, syngamiasis, hirudiniasis, acanthosefalliasis, gongilonemiasis, metastrongiliasis. telasis, pediculosis, pithiriasis, scabies, myiasis, tungiasis, thrombiculosis, scarabiasis, hirudiniasis, linguatulose, porocephaliasis, leishmania, trypanosomiasis, plasmodium malaria caused by falciparum, malaria caused by plasmodium vivax, malaria caused by plasmodium malariae, chagas disease, toxoplasma, pneumocytosis, babesiosis, piroplasmosis, acanthamebiosis, naegleriosis and/or Could be microsporidiosis.

Bulusun tercih edilen bir uygulamasinda formül I ile gösterilen moleküller Leishmaniasis tedavisinde kullanilir. In a preferred embodiment of the invention, molecules of formula I It is used in the treatment of leishmaniasis.

Bulus, tercihen formül I ile gösterilen moleküllerin leishmaniasis tedavisinde kullanimina iliskindir. Burada bahsi geçen Leishmaniasis hastaligi kütanöz, mukokütanöz veya viseral Leishmaniasis olabilir. The invention preferably uses the molecules represented by formula I in the treatment of leishmaniasis. related to its use. The Leishmaniasis disease mentioned here is cutaneous, It may be mucocutaneous or visceral Leishmaniasis.

Bulus bir diger açidan L. Arabica, L. archibaldi, L. aristedesi, L. braziliensis, L. chagasi, L. colombiensis,L. Deanei, L. donovani, L. enrietii, L. equatorensis, L. forattinii, L. garnhami, L. gerbil, Lguyanensis, L. herreri, L. hertigi, L. infantum, L. killicki, L. lainsoni, L. major, L. Mexicana, L. naiffi, L. panamensis, L. peruviana, L. pifanoi, L. shaWi, L. tarentolae, L. tropica, L. turanica, L. venezuelensis türü parazitlerin neden oldugu enfeksiyonel hastaliklarin tedaivisinde mevcut bulusa uygun Formül 1 iler gösterilen moleküllerin kullanimina iliskindir. On the other hand, the invention is supported by L. Arabica, L. archibaldi, L. aristedesi, L. braziliensis, L. chagasi, L. colombiensis, L. Deanei, L. donovani, L. enrietii, L. equatorensis, L. forattinii, L. garnhami, L. gerbil, Lguyanensis, L. herreri, L. hertigi, L. infantum, L. killicki, L. lainsoni, L. major, L. Mexicana, L. naiffi, L. panamensis, L. peruviana, L. pifanoi, L. shaWi, L. tarentolae, L. tropica, L. turanica, L. venezuelensis sp. current invention in the treatment of infectious diseases caused by parasites Appropriate Formula 1 relates to the use of the above-mentioned molecules.

Mevcut bulus bir açidan bulusa uygun Formül I ile gösterilen moleküllerin bakteriyel hastaliklarin tedavisinde kullanimina iliskindir. In one aspect, the present invention shows that the molecules represented by Formula I according to the invention are bacterial related to its use in the treatment of diseases.

Burada kullanilan “bakteriyel hastaliklar” ifadesi patojenik bakterilein neden oldugu enfeksiyonlardan kaynaklanan hastaliklari ifade etmektedir. The expression “bacterial diseases” used here is caused by pathogenic bacteria. refers to diseases caused by infections.

Mevcut bulus kapsamindaki bakterilyel hastaliklar basili, bartonella, bordetella, borrelia, brusella, kampilobakter, kalamidya, kalamidofila, klostridyum, korinebakteryum, enterokokkus, eserya, fransiyella, hemofilus, helikobakter, lejyonella, leptospira, listeria, mikobakteryum, mikoplazma, nisserya, psödomonas, riketsiya, salmonella, sigella, stafilokokkus, streptokokkus, treponema, üreplazma, vibrio, yersinia, ana gruplarina mensup bakteriler nedeniyle olusan herhangi bir bakteriyel hastalik olabilir. Bacterial diseases within the scope of the present invention include bacillus, bartonella, bordetella, borrelia, brucella, campylobacter, calamidia, calamidophila, clostridium, corynebacterium, enterococcus, arachnid, francella, hemophilus, helicobacter, legionella, leptospira, listeria, mycobacterium, mycoplasma, nisseria, pseudomonas, rickettsia, salmonella, sigella, staphylococcus, streptococcus, treponema, ureaplasma, any disease caused by bacteria belonging to the main groups vibrio, yersinia, It could be a bacterial disease.

Söz konusu bakteriyel hastaliklar, örnegin bubonik veba, pnömonik veba, kolera, sifilis, konjenital sifilis, post streptokoksik glomerulonefrit, lohusa hummasi, impetigo, yilaiicik, atesli romatizma, kizil, streptokokkal faranjit, sepsis, akut bakteriyel pnömoni, menenjit, orta kulak iltihabi, endometrit, neonatal sepsis, neonatal menenjit, neonatal pnömoni, sistit, osteomiyelit, toksik sok sendromu, stafilokokkal gida zehirlenmesi, sigelloz, salmonella, paratifo, tifo, kayalik daglar lekeli hummasi, idrar yolu enfeksiyonlari, kornea enfeksiyonlari, pnömoni, endokardit, menenjit, bel soguklugu (gnore), pelvik enflamatuar hastaligi, tüberküloz, cüzzam, listeriyoz, leptospiroz, lejyoner hastaligi, peptik ülser, üst solunum yolu enfeksiyonlari, kronik gastrit, bronsit, septik artrit, tularemia, kanli diyare, idrar yolu enfeksiyonlari, endokardit, safra yolu enfeksiyonlari, difteri, tetanoz, papagan hummasi, trahom (trachoma), neonatal konjuktivit, üretrit, epididimit, prostatit, lenfogranülomatoz, atipik pnömoni, Guillain-Barre Sendromu, broselloz, malta huinmasi, lyme hastaligi olabilir. The bacterial diseases in question are, for example, bubonic plague, pneumonic plague, cholera, syphilis, congenital syphilis, post streptococcal glomerulonephritis, puerperal fever, impetigo, annuals, rheumatoid fever, scarlet fever, streptococcal pharyngitis, sepsis, acute bacterial pneumonia, meningitis, middle ear inflammation, endometritis, neonatal sepsis, neonatal meningitis, neonatal pneumonia, cystitis, osteomyelitis, toxic shock syndrome, staphylococcal food poisoning, sigellosis, salmonella, paratyphoid, typhoid, rocky mountains spotted fever, urinary tract infections, corneal infections, pneumonia, endocarditis, meningitis, gonorrhea, pelvic inflammatory disease, tuberculosis, leprosy, listeriosis, leptospirosis, legionnaires' disease, peptic ulcer, upper respiratory tract infections, chronic gastritis, bronchitis, septic arthritis, tularemia, bloody diarrhea, urinary tract infections, endocarditis, biliary tract infections, diphtheria, tetanus, parrot fever, trachoma (trachoma), neonatal conjunctivitis, urethritis, epididymitis, prostatitis, lymphogranulomatosis, atypical pneumonia, Guillain-Barre Syndrome, brocellosis, maltese fever, may be Lyme disease.

Mevcut bulus bir açidan bulusa uygun Formül 1 ile gösterilen moleküllerin viral hastaliklarin tedavisinde kullanimina iliskindir. In one aspect, the present invention shows that the molecules represented by Formula 1 according to the invention are viral. related to its use in the treatment of diseases.

Mevcut bulus kapsaminda kullanilan “viral hastaliklar” ifadesi patoj enik virüslerin ve bulasici virus partiküllerin (viron) kendilerini hürelere baglayip hücrelere giris yapmasiyla olusan hastaliklarin tamamini ifade etmektedir. The term “viral diseases” used in the present invention is the expression of pathogenic viruses and Infectious virus particles (virons) attach themselves to cells and enter cells. It refers to all of the diseases caused by doing it.

Bahsedilen viral hastaliklar adenoviridae, herpesviridae, papillomaviridae, polyomaviridae, poxviridae, heradnaviridae, parvoviridae, astroviridae, caliciviridae, picornaviridae, coronaviridae, flaviviridae, togaviridae, hepeviridae, retroviridae, ortomiksoviridae, arenaviridae, bunyaviridae, filoviridae, paramiksoviridae, rabdoviridae, reoviridae ana ailelerine mensup olan herhangi bir virüsün neden oldugu bir hastalik olabilir. Mentioned viral diseases are adenoviridae, herpesviridae, papillomaviridae, polyomaviridae, poxviridae, heradnaviridae, parvoviridae, astroviridae, caliciviridae, picornaviridae, coronaviridae, flaviviridae, togaviridae, hepeviridae, retroviridae, orthomyxoviridae, arenaviridae, bunyaviridae, filoviridae, paramyxoviridae, Caused by any virus belonging to the main families rabdoviridae, reoviridae It could be a disease.

Söz konusu viral hastaliklara ait özel örnekler, gasteroentirit, keratokonjuktivit, farenjit, krup, pnömoni, sistit, el-ayak-agiz hastaligi, pleurodnia, septik menenjit, perikadit, miyokardit, Burkitt”e Lenfoma, Hodgin`s lenfoma, nasafaranjiyel karsinom, akut hepatit, kronik hepatit, hepatic siroz, hepatoselüler karsinom, tonsilit, sitomegalik inklüzyon hastaligi, Kaposi sarkomu, castleman hastaligi, influenza, kizamik, reye sendromu, kabakulak, anogenital sigil, poliomiyellit, kuduz, konjenital rubella, kizamikçik, çiçek hastaligi, zona, konjenital su çiçegi sendromu olabilir. Specific examples of the viral diseases in question are gastroenteritis, keratoconjunctivitis, pharyngitis, croup, pneumonia, cystitis, hand-foot-mouth disease, pleurodnia, septic meningitis, pericaditis, myocarditis, Burkitt's lymphoma, Hodgin's lymphoma, nasopharyngeal carcinoma, acute hepatitis, chronic hepatitis, hepatic cirrhosis, hepatocellular carcinoma, tonsillitis, cytomegalic inclusion disease, Kaposi's sarcoma, Castleman's disease, influenza, measles, ray syndrome, mumps, anogenital wart, poliomyelitis, rabies, congenital rubella, may be rubella, smallpox, shingles, congenital varicella syndrome.

Mevcut bulus bir açidan bulusa uygun Formül 1 ile gösterilen moleküllerin neoplastik hastaliklarin tedavisinde kullanimina iliskindir. In one aspect of the present invention, the molecules represented by Formula 1 according to the invention are neoplastic related to its use in the treatment of diseases.

Mevcut bulus kapsaminda kullanilan “neoplastik hastaliklar” ifadesi habis (malign) tümörlere veya kontrolsüz hücre büyümesi ile karakterize olan bir fizyolojik duruma, örnegin kanser hastaligina isaret eder. Bulus kapsaininda “neoplastik hastalik” ve karsinoma, lenfoma, blastoma sarkoina ve lösemiyi içermekte olup bunlarla sinirli degildir. The expression “neoplastic diseases” used in the present invention is malignant. tumors or a physiological condition characterized by uncontrolled cell growth, For example, it refers to the disease of cancer. In the scope of the invention, “neoplastic disease” and includes, but is limited to, carcinoma, lymphoma, blastoma sarcoina, and leukemia is not.

Karsinoma, burada kullanildigi sekliyle, epitel hücrelerden olusan bir kanser türünü ifade etmektedir. Carcinoma, as used herein, is a type of cancer composed of epithelial cells. means.

Lenfoma, burada kullanildigi sekliyle, lenfositlerden gelisen bir kanser türünü anlatmaktadir. Lymphoma, as used herein, is a type of cancer that develops from lymphocytes. it tells.

Blastoma, burada kullanildigi sekliyle, blast hücre adiyla da bilinen öncü hücrelerden gelisen bir kanser türünü anlatmaktadir. Blastoma, as used herein, is one of the progenitor cells, also known as blast cells. describes a developing type of cancer.

Sarkoma, burada kullanildigi sekliyle, mezenkimal kökenli degismis hücrelerden kaynaklanan kanser türünü anlatmaktadir. Sarcoma, as used herein, consists of altered cells of mesenchymal origin. describes the type of cancer caused.

Lösemi, burada kullanildigi sekliyle, kemik iliginde baslayan ve yüksek sayida anormal akyuvar hücresi olusumuna neden olan kanser türünü ifade etmektedir. Leukemia, as used herein, is bone marrow-onset and high-number refers to the type of cancer that causes abnormal white blood cell formation.

Kanser türlerine ait daha özel örnekler meme kanseri, prostat kanseri, kolorektal kanser, deri kanseri, küçük hücreli akciger kanseri, küçük hücreli olmayan akciger kanseri, mezotelyom, gastrointestinal kanser, pankreas kanseri, gliyoblastom, vulva kanseri, rahim agzi kanseri, endometriyal karsinom, yumurtalik kanseri, karaciger kanseri, hepatom, mesane kanseri, böbrek kanseri, tükürük bezi karsinomu, tiroid kanseri ve çesitli bas ve boyun kanserlerini içerir. Bulus ayrica etken madde olarak bulusa uygun formül I ile gösterilen bilesikleri içeren bir farmasötik bilesime iliskindir. More specific examples of cancer types are breast cancer, prostate cancer, colorectal cancer, skin cancer, small cell lung cancer, non-small cell lung cancer, mesothelioma, gastrointestinal cancer, pancreatic cancer, glioblastoma, vulva cancer, cervical cancer, endometrial carcinoma, ovarian cancer, liver cancer, hepatoma, bladder cancer, kidney cancer, salivary gland carcinoma, thyroid cancer and various head and neck cancers. The invention is also used as an active ingredient. a pharmaceutical composition comprising the compounds of the formula I according to the invention. is related.

Söz konusu farmasötik bilesimler Formül 1 ile gösterilen bilesiklere ilave olarak en az bir diger etken madde içerebilir. Said pharmaceutical compositions, in addition to the compounds indicated by Formula 1, contain at least may contain another active ingredient.

Mevcut bulusun bir baska uygulamasinda formül I ile gösterilen bulusa uygun bilesikler diger antiparazitik, antibakteriyel, antiviral, antineoplastik ve/veya sitotoksik ve/veya antimetastatik etki gösteren bilinen aktif bilesiklerle veya bunlarin ikili/üçlü kombinasyonlariyla beraber kullanilabilir. Ikinci etken madde formül I ile gösterilen bilesiklerle beraber formüle edilebilecegi gibi formül l”e uygun bilesiklerden ayri sekilde formüle edilip beraber kullanima uygun paketlerde satisa sunulabilir› Bulusun tercih edilen bir uygulamasinda formül I ile gösterilen bilesikler en az bir adet antibakteriyel etki gösteren aktif bilesikle kombine edilir. In another embodiment of the present invention, in accordance with the invention represented by formula I other antiparasitic, antibacterial, antiviral, antineoplastic and/or with known active compounds or their Can be used with double/triple combinations. With the second active ingredient formula I It can be formulated with the compounds shown as well as conforming to formula I. It is formulated separately from the compounds and sold in packages suitable for use together. available› In a preferred embodiment of the invention, the compounds of formula I have at least one It is combined with an active compound with antibacterial effect.

Formül 1 ile gösterilen bilesiklerle kombine olarak kullanilabilecek antibakteriyel etki gösteren aktiI` bilesikler amikasin, gentamisin, kanamisin, neomisin, netilmisin, tobramisin, paromisin, streptomisin, spektinomisin, geldanainisiii, herbimisin, rifaksimin, lorakarbef, ertapenem, doripenem, imipenem, meropenem, sefadroksil, sefazolin, sefalotinj sefaleksin, sefaklor, sefamandol, sefoksitin, sefprozil, sefuroksimj sefiksim, sefdinir, sefditoren, sefoperazon, sefotaksim, sefpodoksim, seftazidim, seftibüten, seftizoksim, sefepim, seftarolin fosamil, seftobiprol, teikoplanin, vankomisin, televansin, dalbavansin, oritavansin, clindamisiii, linkomisin, daptomisin, azitromisin, klaritromisin, diritromisin, eritromisin, roksitromisin, troleandomisin, telitromisin, spiramisin, aztreonam, furazolidon, nitrofurantoin, linezolid, posizolid, radezolid, torezolid, amoksisilin, ampisilin, azlosilin, karbenisilin, kloksasilin, dikloksasilin, flukloksasilin, mezlosilin, metisilin, nafsilin, okzasilin, penisilin G, penisilin V, piperasilin, temosilin, tikarsilin, klavulanat, sulbaktam, tazobaktam, basitrasin, kolistin, poliniiksin B, siprotloksasin, enoksasin, gatifloksasin, gemifloksasin, levofloksasin, lomefloksasin, moksifloksasin, nalidinik asit, norfloksasin, ofloksasin, trovafloksasin, grepafloksasin, sparfloksasin, temafloksasin, mafenid, sulfasetamid, sulfadiazin, sülfadimetoksin, sülfametizol, sülfametoksazol, sulfanilimid, sülfasalazin, sülfisoksazol, trometoprim, demeklosiklin, doksisiklin, minosiklin, oksitetrasiklin, tetrasiklin, klofazimin, dapson, kapreoinisin, sikloserin, etambutol, isoriiyazid, pyrazinamid, rifampisin, rifabutin, rifapentin, streptomisiii, arsfenamin, kloramfenikol, fosfomisin, fusidik asit, metronidazol, mupirosin, platensimisin, kinupristin, dalfopristin, tiamfenikol, tigesiklin, tinidazol, trimetoprimî içeren grubun içerisinden veya burada sayilan ajanlarin ikili veya üçlü kombinasyonlari içerisinden seçilebilir. Antibacterial effect that can be used in combination with the compounds indicated by formula 1 active compounds showing amikacin, gentamicin, kanamycin, neomycin, netilmicin, tobramycin, paromycin, streptomycin, spectinomycin, geldanainisiiii, herbimycin, rifaximin, loracarbef, ertapenem, doripenem, imipenem, meropenem, cefadroxil, cefazolin, cephalotinj cephalexin, cefaclor, cefamandol, cefoxitin, cefprozil, cefuroxime cefixime, cefdinir, cefditoren, cefoperazone, cefotaxime, cefpodoxime, ceftazidime, ceftibuten, ceftizoxime, cefepime, ceftaroline fosamil, ceftobiprole, teicoplanin, vancomycin, televancin, dalbavancin, oritavancin, clindamycin, lincomycin, daptomycin, azithromycin, clarithromycin, dirithromycin, erythromycin, roxithromycin, troleandomycin, telithromycin, spiramycin, aztreonam, furazolidone, nitrofurantoin, linezolid, pozolid, radezolid, torezolide, amoxicillin, ampicillin, azlocillin, carbenicillin, cloxacillin, dicloxacillin, flucloxacillin, mezlocillin, methicillin, nafcillin, oxacillin, penicillin G, penicillin V, piperacillin, temosillin, ticarcillin, clavulanate, sulbactam, tazobactam, bacitracin, colistin, polynixin B, ciprotloxacin, enoxacin, gatifloxacin, gemifloxacin, levofloxacin, lomefloxacin, moxifloxacin, nalidinic acid, norfloxacin, ofloxacin, trovafloxacin, grepafloxacin, sparfloxacin, temafloxacin, mafenide, sulfacetamide, sulfadiazine, sulfadimethoxine, sulfamethizole, sulfamethoxazole, sulfanilimide, sulfasalazine, sulfisoxazole, tromethoprim, demeclocycline, doxycycline, minocycline, oxytetracycline, tetracycline, clofazimine, dapsone, capreoinicin, cycloserine, ethambutol, isoriazid, pyrazinamide, rifampicin, rifabutin, rifapentine, streptomycin, arsphenamine, chloramphenicol, fosfomycin, fusidic acid, metronidazole, mupirocin, platensimycin, quinupristin, dalfopristin, thiamphenicol, tigecycline, tinidazole, trimethoprimi from the group containing or of the agents listed herein, either double or triple can be selected from combinations.

Bulusun tercih edilen bir diger uygulamasinda formül I ile gösterilen bilesikler en az bir adet antiviral etki gösteren aktif bilesikle kombine edilir. In another preferred embodiment of the invention, the compounds of formula I are at least It is combined with an active compound with an antiviral effect.

Formül 1 ile gösterilen bilesiklerle kombine olarak kullanilabilecek antiviral etki gösteren aktif bilesikler abakaVir, asiklovir, adefovir, amantadin, amprenavir, ampligeii, arbidol, atazaiiavir, atripla, balavir, sidofovir, koinbivir, dolutegravir, darunavir, delavirdin, didanosin, dokosanol, eduksudin, efavirenz, emtrisitabin, enfuvirtid, entekavir, ekoliver, famsiklovir, fomivirsen, fosamprenavir, foskamet, fosfonet, gansiklovir, ibasitabin, imuiiovir, idoksuridin, imikuimod, iiidinavir, inosin, interferon tip I, interferon tip II, interferon tip III, interferon, lamivudin, lopinavir, lovirid, maravirok, moroksidin, metisazon, nelfinavir, nevirapin, neksavir, nitazoksanid, novir, oseltamivir, peginterferon alfa-Za, pensiklovir, peramivir, plekonaril, podofilotoksin, proteaz inhibitörü, nükleosit analoglari, ralgetavira ribavirin, rimantadin, ritonavir, piramidin, saquinavir, sofosbuvir, stavudin; telaprevir, tenofovir, tipranavir, trifliridine, trizivir, tromantadin, trovada, valasiklovir, valgansiklovir, Vidarabin, Viramidin, zalsitabin, zanamivir, Zidovudin°i içeren grubun içerisinden veya burada sayilan ajanlarin ikili veya üçlü kombinasyonlari içerisinden seçilebilir. Antiviral effect that can be used in combination with the compounds indicated by Formula 1 active compounds showing abacaVir, acyclovir, adefovir, amantadine, amprenavir, ampligeii, arbidol, atazaiiavir, atripla, balavir, cidofovir, koinbivir, dolutegravir, darunavir, delavirdine, didanosine, docosanol, eduksudin, efavirenz, emtricitabine, enfuvirtide, entecavir, ecoliver, famciclovir, fomivirsen, fosamprenavir, foskamet, phosphonet, ganciclovir, ibasitabine, imuiovir, idoxuridine, imiquimod, iiidinavir, inosine, interferon type I, interferon type II, interferon type III, interferon, lamivudine, lopinavir, loviride, maraviroc, moroxidine, metisazone, nelfinavir, nevirapine, nexavir, nitazoxanide, novir, oseltamivir, peginterferon alfa-Za, penciclovir, peramivir, pleconaril, podophyllotoxin, protease inhibitor, nucleoside analogues, ralgetavira ribavirin, rimantadine, ritonavir, pyramidin, saquinavir, sofosbuvir, stavudine; telaprevir, tenofovir, tipranavir, trifliridine, trizivir, tromantadine, trovada, valacyclovir, of the group containing valganciclovir, Vidarabine, Viramidin, zalcitabine, zanamivir, Zidovudine from or from binary or triple combinations of the agents listed herein. can be selected.

Bulusun tercih edilen bir diger uygulamasinda formül I ile gösterilen bilesikler en az bir adet antiparazitik etki gösteren aktif bilesikle kombine edilir. In another preferred embodiment of the invention, the compounds of formula I are at least It is combined with an active compound with an antiparasitic effect.

Formül I ile gösterilen bilesiklerle kombine olarak kullanilabilecek antiparazitik etki gösteren aktif bilesikler nitazoksanit, melarsoprol, eflomitin, metronidazol, tinidazol, miltefosin, mebendazol, pirantel pamoat, tiyabendazol, dietilkarbamazin, ivermektin, niklosamid, prazikuantel, albendazol, rifampin, amfoterisin B, fumagillin, furazolidon, nifursemizon, nitaksozanid, ornidazol, paramomisin sülfat, pentamidin, pirimetamine, tinidazol, albendazol, mebendazol, tiyabendazol, fenbendazol, triklabendazol, flubendazol, abamektin, dietilkarbamazin, ivermektin, suramin, pirantel pamoat, levamisol, niklosamid, nitasokzanid, oksiklonazd, monepantel, derquantel, amfoterisin B, üre stibamin, sodyum stiboglukonat, meglumin antimoniat, paromomisin, miltefosin, flukonazol, pentamidin”den olusan bir grubun içerisinden veya bunlarin ikili, üçlü kombinasyonlari içerisinden seçilebilir. Antiparasitic effect that can be used in combination with compounds of formula I active compounds showing nitazoxanide, melarsoprol, eflomitin, metronidazole, tinidazole, miltefosine, mebendazole, pyrantel pamoate, thiabendazole, diethylcarbamazine, ivermectin, niclosamide, praziquantel, albendazole, rifampin, amphotericin B, fumagillin, furazolidone, nifursemizon, nitaxozanide, ornidazole, paramomycin sulfate, pentamidine, pyrimethamine, tinidazole, albendazole, mebendazole, thiabendazole, fenbendazole, triclabendazole, flubendazole, abamectin, diethylcarbamazine, ivermectin, suramin, pyrantel pamoate, levamisole, niclosamide, nitasoxanide, oxyclonazd, monepantel, derquantel, amphotericin B, urea stibamine, sodium stibogluconate, meglumine antimoniate, from a group consisting of paromomycin, miltefosine, fluconazole, pentamidine or their double or triple combination.

Bulusun tercih edilen bir diger uygulamasinda formül I ile gösterilen bilesikler en az bir adet antineoplastik etki gösteren aktif bilesikle kombine edilir. In another preferred embodiment of the invention, the compounds of formula I are at least It is combined with an active compound with an antineoplastic effect.

Formül I ile gösterilen bilesiklerle kombine olarak kullanilabilecek antineoplastik etki gösteren aktif bilesikler siklofosfamid, ifosfamid, temozolomid, kapesitabin, 5-floro urasil, metotreksat, gemsitabin, pemetrekset, niitomisin, bleomisin, epirubisin, doksorubisin, etoposit, paklitaksel, irinotekan, dosetaksel, Vinkristin, karboplatin, cisplatin, okzaliplatin, bevacizumab, setuksimab, gefitinib, imatinib, trastuzumab, denosumab, rituksimab, sunitinib, zoledronat, abirateron, anastrozol, bikalutamid, eksemestan, goserelin, medroksiprogesteron, oktreotid, tamoksifen, bendamustin, karmustin, klorambusil, lomustin, melfalan, prokarbazin, streptozosin, fludarabin, raltitrexed, aktinomisin D, daktinomisin, doksorubisin, mitoksantron, eribulin, topotekan, vinblastin, vinorelbin, afatinib, aflibersept, krizotinib, dabrafenib, interferon, ipilimumab, lapatinib, nivolumab, panitumumab, pembrolizumab, pertuzumab, sorafenib, trastuzumab emtansin, temsorilimus, vemurafenib, ibandronik asit, pamidronat, bexarotan, buserelin, siproteron, degareliks, folinik asit, fulvestrant, lanreotid, lenalidomid, letrozole, leuprorelin, megestrol, mesna, talidomid°den olusan bir grubun içerisinden veya bunlarin ikili veya üçlü kombinasyonlari içerisinden seçilebilir. Antineoplastic effect that can be used in combination with compounds of Formula I Active compounds showing cyclophosphamide, ifosfamide, temozolomide, capecitabine, 5-fluoro uracil, methotrexate, gemcitabine, pemetrexed, niitomycin, bleomycin, epirubicin, doxorubicin, etoposide, paclitaxel, irinotecan, docetaxel, Vincristine, carboplatin, cisplatin, oxaliplatin, bevacizumab, cetuximab, gefitinib, imatinib, trastuzumab, denosumab, rituximab, sunitinib, zoledronate, abiraterone, anastrozole, bicalutamide, exemestane, goserelin, medroxyprogesterone, octreotide, tamoxifen, bendamustine, carmustine, chlorambucil, lomustine, melphalan, procarbazine, streptozocin, fludarabine, raltitrexed, actinomycin D, dactinomycin, doxorubicin, mitoxantrone, eribulin, topotecan, vinblastine, vinorelbine, afatinib, aflibercept, crizotinib, dabrafenib, interferon, ipilimumab, lapatinib, nivolumab, panitumumab, pembrolizumab, pertuzumab, sorafenib, trastuzumab emtansine, temsorilimus, vemurafenib, ibandronic acid, pamidronate, bexarotan, buserelin, cyproterone, degarelix, folinic acid, fulvestrant, consisting of lanreotide, lenalidomide, letrozole, leuprorelin, megestrol, mesna, thalidomide from within a group or their double or triple combination can be selected.

Bulusun bir diger uygulamasinda en az bir diger etken madde bulusa uygun formül l bilesikleriyle beraber veya ayri ayri formüle edilebilir ve söz konusu en az bir diger etken madde formül I bilesikleriyle ayni veya farkli dozaj formunda olabilir. In another application of the invention, at least one other active ingredient is in the formula I according to the invention. may be formulated separately or together with its compounds and said at least one other the active ingredient may be in the same or different dosage form as the compounds of formula I.

Bulusa uygun formül I bilesikleriyle beraber yukarida sayilan en az bir diger etken maddenin kullanilmasi durumunda söz konusu diger etken maddeler formül I”e uygun maddelerle ayni zamanda, birbirini takip eder sekilde sirali olarak veya birbirinden Bulusa uygun formülasyonlar formül I ile gösterilen etken maddelere ilaveten en az Bulusa uygun formül I ile gösterilen etken maddelerin kullanilabilecegi doz araligi hastanin ihtiyaçlari, hastaligin evresi ve kullanilacak etken maddeye göre belirlenir. At least one of the above-mentioned factors together with the compounds of formula I according to the invention If the substance is used, the other active substances in question are in accordance with formula I. at the same time as the items, sequentially or one after the other The formulations according to the invention, in addition to the active substances indicated by formula I, are at least Dosage range in which the active substances indicated by the formula I according to the invention can be used The needs of the patient are determined according to the stage of the disease and the active substance to be used.

Belirli bir duruma uygun dozun belirlenmesi teknigin bilinen durumunda yetkili kisilerce bilinmektedir. Determination of the appropriate dose for a particular situation is authorized by the state of the art. known to people.

Siindi bulus sadece örnek amaçli olan ve bu bulusun kapsamini herhangi bir sekilde kisitlar olarak yoruinlanmamasi gereken asagidaki örneklere atifta bulunularak açiklanacaktir. ÖRNEKLER: Örnek 1: 2-(3-aminopr0pil)-lH-benzo[de]izokinolin-l,3(2H)-dion (Formül Ha) sentez yöntemi 1,8-naftalik anhidrit (l mmol) ethanol suspensiyonu üstüne 1,4-diamin0pr0pan (1.25 mmol) eklendi. Reaksiyon gece boyunca 75°C”de reflüks birakildi. Reaksiyonun ilerleyisi ve kolon kromatogratisi yöntemi ile saflastirilmasi için etilasetat çözücü Sistemi kullanildi Analiz Verileri: LC-MS: hesaplanan : Örnek 2: 2-(3-hidroksipr0pil)-1H-benzo[de]izokinolin-l,3(2H)-di0n (Formül llb) sentez yöntemi 1,8-naftalik anhidrit (l mmol) DMF” de çözüldü. Ardindan ortama diaminopropan (1 ininol) ve DBU (1 inmol) eklendi. 4 saat boyunca reaksiyona ugratildi. Reaksiyonun ilerleyisi DCM/MeOH (40/1) çözücü sistemiyle kontrol edildi. Reaksiyon buzlu suda çöktürme ve süzme ile sonlandirilarak ürün saf olarak elde edildi. The present invention is for illustrative purposes only and does not in any way extend the scope of this invention. with reference to the following examples, which should not be construed as constraints. will be disclosed. EXAMPLES: Example 1: 2-(3-aminopropyl)-1H-benzo[de]isoquinolin-1,3(2H)-dione (Formula Ha) synthesis method 1,4-diaminopropan (1.25) on a 1,8-naphthalic anhydride (1 mmol) ethanol suspension mmol) was added. The reaction was allowed to reflux at 75°C overnight. Your reaction Ethylacetate solvent for further purification and purification by column chromatography. System used Analysis Data: LC-MS: calculated : Example 2: 2-(3-hydroxypropyl)-1H-benzo[de]isoquinolin-1,3(2H)-diOn (Formula IIb) synthesis method 1,8-naphthalic anhydride (1 mmol) was dissolved in DMF. Then medium diaminopropane (1 ininol) and DBU (1 inmol) were added. Reacted for 4 hours. Your reaction progress was checked with the DCM/MeOH (40/1) solvent system. reaction in ice water The product was obtained as pure after finishing with precipitation and filtration.

Analiz Verileri: LC -MS: hesaplanan = . Örnek 3: 3-(1,3-di0kzo-lH-benzo[de]izokinolin-2(3H)-il)propanoik asit (Formül Va) sentez yöntemi hiinîül \ .i Beta analin (l mmol) ACN ortaminda DIEA ile 700C de 1 saatlik süre boyunca reaksiyona ugratildi. Ardindan ortama 1,8-naftalik anhidrit (l mmol) eklenerek reaksiyonun 1 gün boyunca karismasi saglandi. Reaksiyonun ilerleyisi ve kolon kromatograiisi ile saflastirma islemi için DCM/ MeOH ( 20/1) çözücü sistemi kullanildi Analiz Verileri: LC-MS: hesaplanan : . Örnek 4: N 1 ,N8-bis(3-( 1 ,3-diokzo- 1 H-benzo[de]izokinolin-2(3H)-il)propil) oktandiainid (Formül la) sentez yöntemi O Formül In Suberik asit ( damla damla reaksiyon ortamina eklendi. 1-2 damla DMF eklenerek reaksiyon oda sicakligina getirildi. Reaksiyon oda sicakliginda 2 saat boyunca karistirildi. Ürün saf olarak elde edildi, Elde edilen Bu ürün DCM'de çözüldü ardindan Formül lla reaksiyon balonuna eklendi. Oda sicakliginda 10 dk. karistirildiktan sonra trietilainin (1.2 mmol) eklendi ve reaksiyon 2 saat boyunca oda sicakliginda karistirildi. Kolon kromatografisi ile saflastirma islemi için DCM/MeOH (40/1) çözücü sistemi kullanildi. Analysis Data: LC -MS: calculated = . Example 3: 3-(1,3-diOxo-1H-benzo[de]isoquinolin-2(3H)-yl)propanoic acid (Formula Va) synthesis method hiinîül \ .i Beta analine (1 mmol) in ACN medium with DIEA at 700C for 1 hour reacted. Then 1,8-naphthalic anhydride (1 mmol) was added to the medium. the reaction was allowed to stir for 1 day. Progression of the reaction and colon DCM/MeOH (20/1) solvent system for purification by chromatography used Analysis Data: LC-MS: calculated : . Example 4: N1,N8-bis(3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl) octandiainide (Formula la) synthesis method O Formula In Suberic acid ( drops drop was added to the reaction medium. Add 1-2 drops of DMF to the reaction chamber. brought to temperature. The reaction was stirred at room temperature for 2 hours. The product is pure Obtained This product was dissolved in DCM then Formula IIa added to the reaction bubble. 10 min at room temperature. triethylain after mixing (1.2 mmol) was added and the reaction stirred at room temperature for 2 hours. Colon DCM/MeOH (40/1) solvent system for purification by chromatography used.

Analiz Verileri: LC-MS: hesaplanan : . il)propil)üre) (Formül Ib) sentez yöntemi O NMNÄNWNHYNHWN Formül Ih Fomül Ha oda sicakliginda azot atmosferinde THF içerisinde çözüldükten sonra ortama CDI (3 mmol) ile reaksiyona ugratildi. Ardindan elde edilen ürün (4 mmol) ile 1,4- diamino bütan (l mmol) ve DIEA (2.2 mmol) THF ortaminda 16 saat boyunca reaksiyona ugratilmasi ile ürün elde edilmistir . Analysis Data: LC-MS: calculated : . il)propyl)urea) (Formula Ib) synthesis method O NMNÄNWNHYNHWN Formula Ih After Formula Ha is dissolved in THF at room temperature in a nitrogen atmosphere The medium was reacted with CDI (3 mmol). The resulting product (4 mmol) with 1,4-diamino butane (1 mmol) and DIEA (2.2 mmol) in THF medium for 16 hours The product was obtained by the reaction.

Analiz Verileri: LC-MS: hesaplanan : . Örnek 6: Butane-l ,4-diil bis((3-( 1 ,3-diokso- l H-benzo[de]isokinoli11-2(3H)- il)propil)karbamat) (Formül Ic) sentez yöntemi o 0 lioi'mii] lc Fomül Ila oda sicakliginda azot atmosferinde THF içerisinde çözüldükten sonra ortama CDI (3 mmol) ile reaksiyona ugratildi. Ardindan elde edilen ürün (4 mmol) ile 1,4-bütandiol (1 mmol) ve DIEA (2.2 mmol) THF ortaminda 16 saat boyunca reaksiyona ugratilmasi ile ürün elde edilmistir . 64.4 (06112), , Analiz verileri: LC-MS: hesaplanan : Örnek 7: bis(3-(1,3-diokso-1H-benzo[de]isokinolin-2(3H)-il)propil) bütane-'1,4- diildikarbama (Formül Id) sentez yöntemi NMOÄHWNTOWN O 0 Formül Id Fomül Hb oda sicakliginda azot atmosferinde THF içerisinde çözüldükten sonra ortama CDI (3 mmol) ile reaksiyona ugratildi. Ardindan elde edilen ürün (4 mmol) ile 1,4- diamino bütan (1 mmol) ve DIEA (2.2 mmol) THF ortaminda 16 saat boyunca reaksiyona ugratilmasi ile ürün elde edilmistir . Analysis Data: LC-MS: calculated : . Example 6: Butane-1,4-diyl bis((3-(1,3-dioxo-1H-benzo[de]isoquinolin11-2(3H)- il)propyl)carbamate) (Formula Ic) synthesis method o 0 lioi'mii] lc After Formula Ila has been dissolved in THF in a nitrogen atmosphere at room temperature The medium was reacted with CDI (3 mmol). The resulting product (4 mmol) with 1,4-butanediol (1 mmol) and DIEA (2.2 mmol) in THF medium for 16 hours The product was obtained by the reaction. 64.4 (06112), , Analysis data: LC-MS: calculated : Example 7: bis(3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl) butane-'1,4- dididicarbama (Formula Id) synthesis method NMOÄHWNTOWN O 0 Formula Id After the formula Hb is dissolved in THF in a nitrogen atmosphere at room temperature The medium was reacted with CDI (3 mmol). The resulting product (4 mmol) with 1,4-diamino butane (1 mmol) and DIEA (2.2 mmol) in THF medium for 16 hours The product was obtained by the reaction.

Analiz Verileri: IH NMR (, 2.03 (dd, .1 : , 4.33 - 4.04 (m, 4H, J = 7.1 Hz, 4H, ArH), ppm. Analysis Data: 1H NMR (, 2.03 (dd, .1 : , 4.33 - 4.04 (m, 4H, J = 7.1 Hz, 4H, ArH), ppm.

LC-MS: hesaplanan = bis(karbonat) (Formül le) sentez yöntemi O Q I-'oi'mul lu O 0 Fomül llb oda sicakliginda azot atmosferinde THF içerisinde çözüldükten sonra ortaina CDI (3 ininol) ile reaksiyona ugratildi. Ardindan elde edilen ürün (4 mmol) ile 1,4-bütandiol (l mmol) ve DIEA (2.2 mmol) DMF ortaminda 80 0C°de 5 gün boyunca reaksiyona ugratilmasi ile ürün elde edilmistir . LC-MS: calculated = bis(carbonate) (with formula) synthesis method O Q I-'oi'mul lu O 0 Formula IIb was dissolved in THF at room temperature in a nitrogen atmosphere. medium was reacted with CDI (3 ininol). The resulting product (4 mmol) with 1,4-butanediol (1 mmol) and DIEA (2.2 mmol) in DMF medium at 80 0C for 5 days The product was obtained by reacting during

LC-MS: hesaplanan = . Örnek 9: N,N'-(oktan- l ,8-diil)bis( 3-(1 ,3 -diokso- l H-benzo[de]isokinolin-2(3H)- il)propanamid) (Formül li) sentez yöntemi 0 Formül [1 Formül V (2.4mmol) azot atmosferinde THF de çözüldükten sonra ortama sirasiyla DCC ve HOBt (0.92 mmol) eklenerek OOCde 1 saat reaksiyona ugratildiktan sonra ortama 1,8-diamino oktan (0.92 mmol) ilave edildi ve 24 saat boyunca reaksiyona ugratildi. Elde edilen ürün kolon kromotografisi ile etilasetat/hegzan (8/1) sistemi ile saflastirildi. Örnek 10: N,N'-(0ktan-l ,8-diil)bis(3-(l ,3 -diokso-l H-benzo[de]isokiiiolin-2(3 H)- il)propanamid) (Formül If) sentez yöntemi 0 Formül [t Formül V DCM ortaminda çözüldükten sonra ortama ilave edilen oksalil klorid ile DMF (1,2 damla) katalizörlügünde reaksiyona ugratilarak elde edilen ürün (4mmol) ile 1,8-diamino oktan (lininol) ve DIEA (2.2mm01) DCM ortaminda 3 saat boyunca reaksiyona ugratilmasi sonucunda elde edilmistir. LC-MS: calculated = . Example 9: N,N'-(octane-1,8-diyl)bis( 3-(1,3-dioxo-1H-benzo[de]isoquinoline-2(3H)- il)propanamide) (Formula li) synthesis method 0 Formula [1 Formula V (2.4mmol) was dissolved in THF in nitrogen atmosphere, and then to the environment, respectively. After adding DCC and HOBt (0.92 mmol) and reacting in OOC for 1 hour 1,8-diamino octane (0.92 mmol) was added to the medium and reacted for 24 hours. was brought up. The obtained product was obtained by column chromatography with ethylacetate/hexane (8/1) system. purified. Example 10: N,N'-(Octan-1,8-diyl)bis(3-(1,3-dioxo-1H-benzo[de]isociiiolin-2(3H)- il)propanamide) (Formula If) synthesis method 0 Formula [t Formula V was dissolved in DCM medium and then added to the medium with oxalyl chloride. Product (4mmol) obtained by reacting with DMF (1.2 drops) catalysis with 1,8-diamino octane (lininol) and DIEA (2.2mm01) in DCM medium for 3 hours obtained as a result of the reaction.

Analiz Verileri; 13C NMR (, , LC-MS: hesaplanan = . Örnek 11: Bisnaftalimidopropildiaminooktan (BNIPDaoct) (formül lg) yeni sentez yöntemi O NME/*”dfßvjê Formüllg Formül Ha ile gösterilen bilesigin metanol içerisindeki çözeltisine baz ve 1,8- dibromooktan ilave edilerek, geri sogutucu altinda reflüks edildi. TLC ile takibi yapilarak 4 saat sonunda reaksiyon sonlandirildi. Analysis Data; 13C NMR (, , LC-MS: calculated = . Example 11: Bisnaphthalimidopropyldiaminooctane (BNIPDaoct) (formula lg) new synthesis method O NME/*”dfßvjê Formulalg The solution of the compound represented by formula I in methanol is mixed with base and 1,8- It was refluxed under reflux by adding dibromooctane. Follow up with TLC The reaction was terminated after 4 hours.

Reaksiyonda; DBU, KI/KQCO3, NaH, DIEA, TEA gibi çesitli bazlar denenmistir. In the reaction; Various bases such as DBU, KI/KQCO3, NaH, DIEA, TEA have been tried.

Kullanilan bazlar arasinda DBU ”nun etkinligi yüksek bulunmustur. Among the bases used, the effectiveness of DBU was found to be high.

Analiz Verileri: - , 3.04 - 2.97 (m, 4H, 2XNHCH2), , 8.51 - 8.38 13C NMR (, LC-MS: hesaplanan : Örnek 12: Bisnaftalimidopropildiaminononan (BNIPDanon) (formül Ih) yeni sentez yöntemi formül lh Formül IIa ile gösterilen bilesigin metanol içerisindeki çözeltisine DBU ve 1-9- dibromononan ilave edilerek, geri sogutucu altinda reflüks edildi. Reaksiyon, TLC ile takip edilerek 4 saat sonunda sonlandirildi. Analysis Data: - , 3.04 - 2.97 (m, 4H, 2XNHCH2), , 8.51 - 8.38 13C NMR (, LC-MS: calculated : Example 12: Bisnaphthalimidopropyldiaminononan (BNIPDanon) (formula Ih) new synthesis method formula lh The solution of the compound represented by formula IIa in methanol is mixed with DBU and 1-9- Dibromononan was added and refluxed under reflux. Reaction by TLC was followed and terminated after 4 hours.

Claims (2)

ISTEMLER 1. Formül 1 ile gösterilen moleküller olup burada RA: Ci-Cs alkan, C i-Cs alken veya Ci-Cs alkin 5 X= Cl, F, Br veya I RB : -X, -NHz, -COORg, -CH2CHNH2COOR8, 'NRSRQ VC L: R1, R2, R3, R4, R5, R6, R7 RB = -H ve L=R1, R2, R3, R4, R5, R6 olup; 10 R1: -OCOO-Rg-OOCO-; R2: -NHCONH-Rg-NHCONH-; R3: -OCOHN-Rg-NHOCO-g R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-CONH- 15 R6: -CONH-Rg-NHOC- R7: -NH-Rg-Nl-l ve R3 ve R9 ise birbirinden bagimsiz olarak C1-C10 alkan, alken, alkin içerisinden seçilir. CLAIM 1. Molecules of formula 1 wherein RA: Ci-C8 alkane, Ci-C8 alkene or Ci-C8 alkyne 5 X= Cl, F, Br or IRB : -X, -NHz, -COORg, -CH2CHNH2COOR8 , 'NRSRQ VC L: R1, R2, R3, R4, R5, R6, R7 RB = -H and L=R1, R2, R3, R4, R5, R6; 10 R1: -OCOO-Rg-OOCO-; R2: -NHCONH-R8-NHCONH-; R3: -OCOHN-Rg-NHOCO-g R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-CONH- 15 R6: -CONH-Rg-NHOC- R7: -NH-Rg-N1-1 and R3 and R9 are independently selected from C1-C10 alkane, alkene, alkyne. 2. Istem lie göre moleküller olup ; 20 R8 R8 RA : C3 alkan R1: -OCOO-Rg-OOCO-g R2: -NHCONH-Rg-NHCONH-; R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-OCNH- R6: -CONH-Rg-NHOC R8: Ci -Cio alkandir. . Istem l`e göre formül I ile gösterilen moleküller olup; RA = C3 alkan R1: -OCOO-Rg-OOCO-; R2: -NHCONH-Rg-NHCONH1 R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH1 R5: -NHCO-Rg-OCNH- R6: -CONH-Rg-NHOC R7: -NH-Rg-NH ve R8: C1 -C 1 0 alkandir. . Istem l“e göre formül I ile gösterilen moleküller olup RA = C3 alkan R3: -COORg R1: -OCOO-Rg-OOCO; R2: -NHCONH-Rg-NHCONH-; R3: -OCOHN-Rg-NHOCO-g R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-OCNH- R6: -CONH-Rg-NHOC R7: -NH-Rg-NH ve R8: C1 'C 1 0 alkandir. . Istem 1”e göre formül I ile gösterilen moleküller olup RA : C 3 alkan RB = -CHZCHNH2COOR3 R1: -OCOO-Rg-OOCO-; R2: -NHCONH-Rg-NHCONH-; R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-OCNH- R6: -CONH-Rg-NHOC R7: -NH-Rg-NH ve R8: Ci -Cio alkandir. 6. Istem lle göre formül I ile gösterilen moleküller olup RA = C3 alkan R1: -OCOO-Rg-OOCO-g R2: -NHCONH-Rg-NHCONH-g R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-OCNH- R6: -CONH-Rg-NHOC R7: -NH-Rg-NH ve R8: Ci-Cio alkan R9: Ci-Cio alkandir. 7. Istem lse göre bir molekül olup formül la ile gösterilemektedir. O Formül lu 8. Istem Ve göre bir molekül olup formül lb ile gösterilmektedir. N/VxNJLN/WNH NHWN o Furmiil II\ 9. Istem l'e göre bir molekül olup formül IC ile gösterilmektedir, O O 1501 111`ul Ic O 0 12. Istem lle göre bir molekül olup formül If ile gösterilmektedir 10 iii. O Formül [1' Formül 1 ile gösterilen etken maddelerin elde edilmesinde kullanilacak bir metot Formül 11 ile gösterilen maddenin uygun bir çözücü varliginda CDI ile reaksiyona sokulmasi, R5 Formül II Olusan ara ürünün Formül HI ile gösterilen madde ile DIEA varliginda reaksiyona sokulmasi, ve Formül III Son ürünün reaksiyon karisimindan izole edilmesi adimlarini içermekte olup, burada verilen RH) ve R” birbirinden bagimsiz olarak 7 OH ve -NH2 gruplari içerisinden; RB, -H, -X, -NHZ, -COORg, - CHZCHNHZCOORg veya -NRgRg içerisinden; R8 ve R9 ise birbirinden bagimsiz olarak C i-Cio alkan, alken, alkin içerisinden seçilir ve n ise 1-10 arasinda bir dogal sayidir. Formül 1 ile gösterilen etken maddelerin elde edilmesinde kullanilacak bir metot Formül 11 ile gösterilen maddenin bir çözücü içerisinde çözülmesi, RB Formül II Reaksiyon karisimina formül IV ile gösterilen maddenin eklenmesi, Formül IV Reaksiyon karisimina baz eklenmesi ve Son ürünün reaksiyon karisimindan izole edilmesi adimlarini içerrnekte olup burada verilen RIO *OH ve *NHZ gruplari içerisinden, X ise -Cl, -Br, -I, -F içerisinden RB, -H, -X, -NHZ, -COORS, -CHZCHNHZCOORS veya -NRgRg içerisinden; R8 ve R9 ise birbirinden bag1m51z olarak Ci-Cio alkan! alken, alkin içerisinden seçilir ve 11 ise 1-10 arasinda bir dogal sayidir. Istem 14`e göre bir metot olup baz l,8-diazabicyclo(, Kl/K, trietilamin (TEAYdan olusan bir grubun içerisinden seçilir. Formül 1 ile gösterilen etken maddelerin elde edilmesinde kullanilacak bir metot Formül V ile gösterilen maddenin bir çözücü içerisinde çözülmesi ve DCC ve HOBt varliginda reaksiyona sokulmasi, RB Formül V Reaksiyon karisimina formül [11 ile gösterilen maddenin eklenmesi, Formül III Son ürünün reaksiyon karisimindan izole edilmesi Adimlarini içermekte olup burada verilen Rio ve RH bagimsiz olarak -OH ve - NHZ gruplari içerisinden; RB, -H, -X, -NHZ, -COORg, -CHZCHNHZCOORg veya - NRgRg içerisinden; R8 ve R9 ise birbirinden bagimsiz olarak Ci-Cio alkan, alken, alkin içerisinden seçilir, n ise 1-10 arasinda bir dogal sayidir. Istem 13-16°daii herhangi birine göre bir metot olup çözücü bir organik solvent olup asetik asit, aseton, asetoiiitril, benzen, l-butaiiol, 2-butanol, 2-butanon, t-butil alkol, karbon tetraklorür, klorobenzen, kloroform, siklohekzan, 1,2-dikloroetan, dietilen glikol, dietileter, dietilen glikol dimetil eter, , dimetilformamid (DMF), dimetilsülfoksit (DMSO), 1,4-di0ksan, etanol, etil asetat, etilen glikol, gliserin, heptan, hekzametilfosforamid (HMPA), hekzametilfosforus triamid (HMPT), hekzan, metanol, metilt-bütil eter (MTBE), metilen klorür (DCM), N-metil-Z-pirolidon (NMP), nitrometan, pentan, petrol eteri, l-propanol, 2-pr0panol, piridin, tetrahidrofuran (THF), tolüen, trietil amin, su, o-ksilen, m-ksilen, p-ksilen7den olusan bir grubun içerisinden seçilir. Istein 13-16'dan herhangi `birine göre bir metot olup oda sicakliginda veya 25-40 0C araliginda bir sicaklikta gerçeklestirilir. Formül 1 ile gösterilen moleküller olup RA: Ci-Cs alkan, Ci-Cs alken veya Ci-Cs alkin X: C1, F, Br veya I RB : -H, -X, -NHZ, -COORg, -CHZCHNHZCOORg, -NRgRg VE: L: R1, R2, R3, R4, R5: R6: R7› R1: -OCOO-Rg-OOCO-; R2: -NHCONH-Rg-NHCONH-g R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH- Olarak belirlenmistir ve R8 ve R9 ise birbirinden bagimsiz olarak Ci-Cig alkan, alken, alkin içerisinden seçilmektedir, özelligi söz konusu moleküllerin istem 13- 16”ya göre metot I, metot H veya metot HPten herhangi biriyle hazirlanmasidir. Istem l”e göre formül I ile gösterilen etken maddelerin bakteriyel, Viral, parazitik ve neoplastik hastaliklarin tedavisinde ilaç olarak kullanimi. Istem 20°ye göre bir kullanim olup parazitik hastalik sistozomiyaz, opistorsiyaz, klonorkiyaz, dikrosölyoz, fasioliyazis, paragonimiyaz, fasiolopsiyaz, ekinokokiyaz, teiiyazis, sistiserkoz, difilobotrtyaz, sparganoz, himenolepiyaz, drakunkuliyaz, onkoserkiyazis, filaryaz, elefantiyazis, mansonelloz, trisinelozis, ankilostomiyaz, nekatoiyaz, ankilostomyazis, askardiyoz, strongiloidiyaz, trisüriyaz, enterobiyazis, anisakiyaz, helmintiyazis, trikostronjiloz, anjiyostrongiloz, gnatostomiyaz, anjiyostrongiloz, singamiyaz, hirudiniyaz, akantosefallyaz, gongilonemiyaz, metastrongilyaz, telaziyaz, pediküloz, pithiriyaz, skabiyez, miyaz, tungiyaz, troinbikuloz, skarabiazis, hirudiniyaz, linguatuloz, porosefaliyaz, leishmania, trypanosomiasis, plazmodyum falsiparum”un neden oldugu malarya, plazmodyum Vivax"1n neden oldugu malarya, plazmodyum malariaelnin neden oldugu malarya, ehagas hastaligi, toksoplazma, pnömosistoz, babeziyoz, piroplazmoz, akantamebiyaz, naegleriyaz ve/veya mikrosporidioz olabilir. Istem 21 ”e göre bir kullanim olup parazitik hastalik leishmaniasis”tir. Istem 22°ye göre bir kullanim olup parazitik hastalik L. Arabica, L. archibaldi, L. aristedesi, L. braziliensis, L. chagasi, L. colombiensis,L. Deanei, L. donovani, L. enrietii, L. equatorensis, L. forattinii, L. garnhami, L. gerbil, L.guyanensis, L. herreri, L. hertigi, L. infantuin, L. killicki, L. lainsoni, L. major, L. Mexicana, L. naiffi, L. panainensis, L. peruviana, L. pifanoi, L. shawi, L. tarentolae, L. tropica, L. turanica, L. venezuelensis türü parazitlerin neden oldugu bir hastaliktir. Istem 20”ye göre bir kullanim olup bakteriyel hastalik basili, bartonella, bordetella, borrelia, brusella, kampilobakter, kalamidya, kalamidofila, klostridyum, korinebakteryum, enterokokkus, eserya, fransiyella, hemofilus, helikobakter, lejyonella, leptospira, listeria, mikobakterwm, inikoplazma, nisserya, psödomonas, riketsiya, salmonella, sigella, stafilokokkus, streptokokkus, treponema, üreplazma, vibrio, yersinia, ana gruplarina mensup bakteriler nedeniyle olusan herhangi bir bakteriyel hastaliktir. Istem 24'e göre bir kullanim olup bakteriyel hastalik bubonie veba, pnömonik veba, kolera, sifilis, konjenital sifilis, post streptokoksik glomerulonefrit, lohusa hummasi, impetigo, yilancik, atesli romatizma, kizil, streptokokkal faranjit, sepsis, akut bakteriyel pnömoni, menenjit, orta kulak iltihabi, endometrit, neonatal sepsis, neonatal menenjit, neonatal pnömoni, sistit, osteomiyelit, toksik sok sendromu, statilokokkal gida zehirlenmesi, sigelloz, salmonella, paratifo, tifo, kayalik daglar lekeli hummasi, idrar yolu enfeksiyonlari, kornea enfeksiyonlari, pnömoni, endokardit, menenjit, gnore, pelvik enflamatuar hastaligi, tüberküloz, Cüzzam, listeriyoz, leptospiroz, lejyoner hastaligi, peptik ülser, üst solunum yolu enfeksiyonlari, kronik gastrit, bronsit, septik artrit, tularemia, kanli diyare, idrar yolu enfeksiyonlari, endokardit, safra yolu enfeksiyonlari, difteri, tetanoz, papagan hummasi, trachoma, neonatal konjuktivit, üretrit, epididimit, prostatit, lenfogranülomatoz, atipik pnömoni, Guillain-Barre Sendromu, broselloz, malta hummasi, lyrne hastaligi olabilir. Istem 20”ye göre bir kullanim olup viral hastalik adenoviridae, herpesviridae, papillomaviridae, polyomaviridae, poxviridae, heradnaviridae, parvoviridae, astroviridae, caliciviridae, picornaviridae, coronaviridae, flaviviridae, togaviridae, hepeviridae, retroviridae, ortomiksoviridae, arenaviridae, bunyaviridae, filoviridae, paramiksoviridae, rabdoviridae, reoviridae ana ailelerine mensup olan herhangi bir virüsün neden oldugu bir hastalik olabilir. Istem 265ya göre bir kullanim olup viral hastalik gasteroentirit, keratokonjuktivit, farenjit, krup, pnömoni, sistit, el-ayak-agiz hastaligi, pleurodnia, septik menenjit, perikadit, miyokardit, Burkitfe Lenfoma, Hodginas lenfoma, nasafaranjiyel karsinom, akut hepatit, kronik hepatit, hepatic siroz, hepatoselüler karsinom, tonsilit, sitomegalik inklüzyon hastaligi, Kaposi sarkomu, castleman hastaligi, influenza, kizamik, reye sendromu, kabakulak, anogenital sigil, poliomiyellit, kuduz, konjenital mbella, kizamikçik, çiçek hastaligi, zona, konjenital su çiçegi sendromuolabilir. Istem 20`ye göre bir kullanim olup neoplastic hastalik habis (malign) tümörlere veya kontrolsüz hücre büyümesi ile karakterize olan bir fizyolojik durumlardir. Istem 28°e göre bir kullanim olup neoplastik hastalik karsinoma, lenfoma, blastoma sarkoma veya lösemi olabilir. Istem 29”a göre bir kullaniin olup kanser hastaligi; meme kanseri, prostat kanseri, kolorektal kanser, deri kanseriî küçük hücreli akciger kanseri, küçük hücreli olinayan akciger kanseri, mezotelyom, gastrointestinal kanser, pankreas kanseri, gliyoblastom, vulva kanseri, rahim agzi kanseri, endoinetriyal karsinom, yumurtalik kanseri, karaciger kanseri, hepatom, mesane kanseri, böbrek kanseri, tükürük bezi karsinomu, tiroid kanseri ve çesitli bas ve boyun kanserleri olabilir. Istem 1”e uygun fonnül I ile gösterilen bilesikleri içeren farmasötik bilesimler Istem 31°e göre bir farmasötik bilesim olup form I ile gösterilen bilesiklere ilaveten en az bir diger etken madde içerir. Istem 32°ye göre bir farmasötik bilesim olup diger etken madde antiparazitik, antibakteriyel, antiviral, antineoplastik ve/Veya sitotoksik ve/Veya antiinetastatik etki gösteren bilinen aktif bilesiklerle veya bunlarin ikili, üçlü kombinasyonlari içerisinden seçilir. Istem 33°e göre bir farmasötik bilesim olup antibakteriyel etki gösteren aktif bilesik amikasin, gentamisin, kanamisin, neomisin, netilmisin, tobramisin, paromisin, streptomisin, spektinoinisin, geldanamisin, herbimisin, rifaksimin, lorakarbef, ertapenem, doripenem, imipenem, meropenem, sefadroksil, sefazolin, sefalotin, sefaleksin, sefaklor, sefamandol, sefoksitin, sefprozil, sefuroksim, sefiksim, sefdinir, sefditoren, sefoperazon, sefotaksim, sefpodoksim, seftazidim, seftibüten, seftizoksim, sefepim, seftarolin fosamil, seftobiprol, teikoplanin, vankomisin, televansin, dalbavansin, oritavansin, clindamisin, linkomisin, daptomisin, azitromisin, klaritromisin, diritromisin, eritromisin, roksitromisin, troleandomisin, telitromisin, spiramisin, aztreonam, furazolidon, nitrofurantoin, linezolid, posizolid, radezolid, torezolid, ainoksisilin, ampisilin, azlosilin, karbenisilin, kloksasilin, dikloksasilin, flukloksasilin, mezlosilin, metisilin, nafsilin, okzasilin, penisilin G, penisilin V, piperasilin, temosilin, tikarsilin, klavulanat, sulbaktam, tazobaktam, basitrasin, kolistin, polimiksin B, siproiloksasin, enoksasin, gatifloksasin, gemifloksasin, levofloksasin, lomefloksasin, moksifloksasin, nalidinik asit, norfloksasin, ofloksasin, trovafloksasin, grepafloksasin, spariloksasin, temafloksasin, inafenid, sulfasetamid, sulfadiazin, sülfadimetoksin, sülfametizol, sülfametoksazol, sulfanilimid, sülfasalazin, sülfisoksazol, trometoprim, demeklosiklin, doksisiklin, minosikliii, oksitetrasiklin, tetrasiklin, klofazimin, dapson, kapreomisin, sikloserin, etambutol, isoniyazid, pyrazinamid, rifampisin, rifabutin, rifapentin, streptomisin, arsfenamin, kloramfenikol, fosfomisin, fusidik asit, metronidazol, mupirosin, platensimisin, kinupristin, dalfopristin, tiamfenikol, tigesiklin, tinidazol, trimetoprim`i içeren grubun içerisinden veya burada sayilan ajanlarin ikili veya üçlü kombinasyonlari içerisinden seçilir. Istem 33”e göre bir farmasötik bilesim olup antiviral etki gösteren aktif bilesikler abakavir, asiklovir, adefovir, amantadin, amprenavir, ampligen, arbidol, atazanavir, atripla, balavir, sidofovir, kombivir, dolutegravir, darunavir, delavirdin, didanosin, dokosanol, eduksudin, efavirenz, emtrisitabin, enfuvirtid, entekavir, ekoliver, famsiklovir, fomivirsen, fosamprenavir, foskarnet, fosfonet, gansiklovir, ibasitabin, imunovir, idoksuridin, imikuimod, indinavir, inosin, interferon tip I, interferon tip II, interferon tip III, interferon, lamivudin, lopinavir, lovirid, maravirok, moroksidin, metisazon, nelfinavir, nevirapin, neksavir, nitazoksanid, novir, oseltamivir, peginterferon alfa-Za, pensiklovir, peramivir, plekonaril, podofilotoksin, proteaz inhibitörü, nükleosit analoglari, ralgetavir, ribavirin, rimantadin, ritonavir, piramidin, saquinavir, sofosbuvir, stavudin, telaprevir, tenofovir, tipranavir, trifliridine, trizivir, tromantadin, trovada, valasiklovir, valgansiklovir, Vidarabin, Viramidin, zalsitabin, zanamivir, zidovudin”i içeren grubun içerisinden veya burada sayilan ajanlarin ikili veya üçlü kombinasyonlari içerisinden seçilir. Istem 33,6 göre bir farmasötik bilesim olup antiparazitik etki gösteren aktif bilesikler nitazoksanit, melarsoprol, eflornitin, metronidazol, tinidazol, miltefosin, mebendazol, pirantel pamoat, tiyabendazol, dietilkarbamazin, ivermektin, niklosamid, prazikuantel, albendazol, rifampin, amfoterisin B, fumagillin, furazolidon, nifursemizon, nitaksozanid, ornidazol, paramomisin sülfat, pentamidin, pirimetamine, tinidazol, albendazol, mebendazol, tiyabendazol, fenbendazol, triklabendazol, flubendazol, abamektin, dietilkarbamazin, ivermektin, suramin, pirantel pamoat, levamisol, niklosamid, nitasokzanid, oksiklonazd, monepantel, derquantel, amfoterisin B, üre stibamin, sodyum stiboglukonat, meglumin antimoniat, paromomisin, miltefosin, flukonazol, pentamidin°den olusan bir grubun içerisinden veya bunlarin ikili, üçlü kombinasyonlari içerisinden seçilir. 37. Istem 33”e göre bir farmasötik bilesim olup antineoplastik etki gösteren aktif bilesikler siklofosfamidj ifosfamid, temozolomid, kapesitabin, 5-f'loro urasil, metotreksat, gemsitabin, peinetrekset, initomisin, bleomisin, epirubisin, doksorubisin, etoposit, paklitaksel, irinotekan, dosetaksel, vinkristin, karboplatin, cisplatin, okzaliplatin, bevacizumab, setuksimab, gefitinib, imatinib, trastuzumab, denosumab, rituksimab, sunitinib, zoledronat, abirateron, anastrozol, bikalutamid, eksemestan, goserelin, medroksiprogesteron, oktreotid, tamoksifen, bendamustin, karinustin, klorambusil, lomustin, inelfalan, prokarbazin, streptozosin, fludarabin, raltitrexed, aktinomisin D, daktinomisin, doksorubisin, mitoksantron, eribulin, topotekan, Vinblastin, vinorelbin, afatinib, aflibersept, krizotinib, dabrafenib, interferon, ipilimumab, lapatinib, nivolumab, panitumumab, pembrolizumab, pertuzumab, sorafenib, trastuzumab emtansin, temsorilimus, vemurafenib, ibandronik asit, pamidronat, bexarotan, buserelin, siproteron, degareliks, folinik asit, fulvestrant, lanreotid, lenalidomid, letrozole, leuprorelin, megestrol, mesna, talidomid”den olusan bir grubun içerisinden veya bunlarin ikili veya üçlü kombinasyonlari içerisinden seçilir. 38. Istem 31-37”ten herhangi birine göre bir farmasötik bilesim olup en az bir yardimci madde içerir.2. They are molecules according to claim; 20 R8 R8 RA : C3 alkane R1: -OCOO-Rg-OOCO-g R2: -NHCONH-Rg-NHCONH-; R3: -OCOHN-R8-NHOCO-; R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-OCNH- R6: -CONH-Rg-NHOC R8: C1 -Cio alkane. . Molecules shown with formula I according to claim 1; RA = C3 alkane R1: -OCOO-Rg-OOCO-; R2: -NHCONH-Rg-NHCONH1 R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-Rg-OOCNH1 R5: -NHCO-Rg-OCNH- R6: -CONH-Rg-NHOC R7: -NH-Rg-NH and R8: C1 -C10 alkane. . Molecules of formula I according to claim 1 wherein RA = C3 alkane R3: -COORg R1: -OCOO-Rg-OOCO; R2: -NHCONH-R8-NHCONH-; R3: -OCOHN-Rg-NHOCO-g R4: -NHCOO-Rg-OOCNH-; R5: -NHCO-Rg-OCNH- R6: -CONH-Rg-NHOC R7: -NH-Rg-NH and R8: C1'C10 alkane. . Molecules of formula I according to claim 1 wherein RA: C 3 alkane RB = -CHZCHNH2COOR3 R1: -OCOO-Rg-OOCO-; R2: -NHCONH-R8-NHCONH-; R3: -OCOHN-R8-NHOCO-; R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-OCNH- R6: -CONH-Rg-NHOC R7: -NH-Rg-NH and R8: C1 -Cio alkane. 6. Molecules of the formula I according to claim 11 wherein RA = C3 alkane R1: -OCOO-Rg-OOCO-g R2: -NHCONH-Rg-NHCONH-g R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-OCNH- R6: -CONH-Rg-NHOC R7: -NH-Rg-NH and R8: Ci-Cio alkane R9: Ci-Cio alkane. 7. A molecule according to claim 1, represented by the formula la. It is a molecule according to claim 8 of Formula 1 and is represented by formula lb. N/VxNJLN/WNH NHWN o Furmiil II\ 9. A molecule according to claim 1, indicated by formula IC, O O 1501 111`ul Ic O 0 12. A molecule according to claim 11, designated by formula If 10 iii. O Formula [1' A method to be used to obtain the active substances represented by Formula 1 Reacting the substance represented by Formula 11 with CDI in the presence of a suitable solvent, R5 Reacting the formed intermediate with the substance represented by Formula HI in the presence of DIEA, and Formula III It includes the steps of isolating the final product from the reaction mixture, wherein RH) and R” are independently of each other from 7 OH and -NH2 groups; RB, -H, -X, -NHZ, -COORg, -CHZCHNHZCOORg or -NRgRg; R8 and R9 are independently selected from C i-Cio alkane, alkene, alkyne and n is a natural number between 1-10. A method to be used to obtain the active substances represented by formula 1 includes the steps of dissolving the substance represented by formula 11 in a solvent, adding the substance indicated by formula IV to the RB Formula II reaction mixture, adding a base to the formula IV reaction mixture, and isolating the final product from the reaction mixture. given RIO from *OH and *NHZ groups, X from -Cl, -Br, -I, -F RB, -H, -X, -NHZ, -COORS, -CHZCHNHZCOORS or -NRgRg; R8 and R9 are Ci-Cio alkanes independently of each other! alkene is chosen from alkyne and 11 is a natural number from 1-10. A method according to claim 14, and the base is selected from a group consisting of 1,8-diazabicyclo(, K1/K, triethylamine (TEAY). A method to be used in obtaining the active substances indicated by formula 1 is to dissolve the substance indicated by formula V in a solvent and It includes the steps of reacting in the presence of DCC and HOBt, adding the substance indicated by formula [11 to the RB Formula V reaction mixture, isolating the Formula III final product from the reaction mixture. Rio and RH given here independently from the -OH and -NHZ groups; RB, -H , -X, -NHZ, -COORg, -CHZCHNHZCOORg or -NRgRg, R8 and R9 are independently selected from Ci-Cio alkane, alkene, alkyne, n is a natural number between 1-10. Claim 13-16° a method according to any of the following, the solvent being an organic solvent acetic acid, acetone, acetoitrile, benzene, 1-butaylol, 2-butanol, 2-butanone, t-butyl alcohol, carbon tetrachloride, chlorobenzene, chloroform, cyclohexane, 1,2 -dichloroethane, diethylene glycol, diethylether, diethylene glycol dimethyl ether, dimethylformamide (DMF), dimethylsulfoxide (DMSO), 1,4-dioxane, ethanol, ethyl acetate, ethylene glycol, glycerine, heptane, hexamethylphosphoramide (HMPA), hexamethylphosphorus triamide (HMPT), hexane, methanol, methylt-butyl ether (MTBE), methylene chloride (DCM), N-methyl-Z-pyrrolidone (NMP), nitromethane, pentane, petroleum ether, 1-propanol, 2-propanol, pyridine, tetrahydrofuran (THF) , toluene, triethyl amine, water, o-xylene, m-xylene, p-xylene. It is a method according to any of the request 13-16 and is carried out at room temperature or at a temperature in the range of 25-40 0C. Molecules represented by formula 1 are RA: Ci-Cs alkane, Ci-Cs alkene or Ci-Cs alkyne X: C1, F, Br or I RB : -H, -X, -NHZ, -COORg, -CHZCHNHZCOORg, -NRgRg AND: L: R1, R2, R3, R4, R5: R6: R7› R1: -OCOO-Rg-OOCO-; R2: -NHCONH-Rg-NHCONH-g R3: -OCOHN-Rg-NHOCO-; R4: -NHCOO-R8-OOCNH-; R5: -NHCO-Rg-CONH- R6: -CONH-Rg-NHOC- R7: -NH-Rg-NH- and R8 and R9 are independently selected from Ci-Cig alkane, alkene, alkyne. the preparation of the said molecules according to claims 13-16 with either method I, method H or method HP. The use of the active ingredients shown in formula I according to claim 1 as a drug in the treatment of bacterial, viral, parasitic and neoplastic diseases. It is a use according to claim 20 and the parasitic disease cystosomiasis, opistorciasis, clonorchiasis, dicrocoeliosis, fascioliasis, paragonimiasis, fasciolopsia, echinocochiasis, theiiasis, cysticercosis, diphylobothriasis, sparganosis, clonorchiasis, dichrocoeleosis, dracunolycosis, phyllocyscosis, echinocochiasis, theiiasis, cysticercosis, diaphylobottiasis, sparganosis, hymenolepiasis, elechonolepiosis, phyllocysciasis nekatoiiasis, ankylostomiasis, ascardiosis, strongyloidiasis, trisuria, enterobiasis, anisachia, helminthiasis, trichostrongylosis, angiostrongilosis, gnathostomiasis, angiostrongilosis, syngamyiasis, hirudiniasis, enterobiasis, anisachia, helminthiasis, tricostrongylosis, angiostrongilosis, gnathostomiasis, angiostrongilosis, syngamymiasis, hirudiniasis, acanthosis, enterobiasis, rheumatoid arthritis, pharyngitis hirudiniasis, linguatulose, porocephaliasis, leishmania, trypanosomiasis, malaria caused by plasmodium falciparum, malaria caused by plasmodium Vivax, malaria caused by plasmodium malariael, malaria caused by plasmodium malariael, ehagas disease, ehagas disease, aeganoplasmosis, aeganoplasmosis, psoriasis, toxoplasmosis, aeganoplasmosis, psoriasis be knows. It is a use according to claim 21 and the parasitic disease is leishmaniasis. A use according to claim 22 wherein the parasitic disease L. Arabica, L. archibaldi, L. aristedesi, L. braziliensis, L. chagasi, L. colombiensis, L. Deanei, L. donovani, L. enrietii, L. equatorensis, L. forattinii, L. garnhami, L. gerbil, L.guyanensis, L. herreri, L. hertigi, L. infantuin, L. killicki, L. lainsoni, It is a disease caused by parasites such as L. major, L. Mexicana, L. naiffi, L. panainensis, L. peruviana, L. pifanoi, L. shawi, L. tarentolae, L. tropica, L. turanica, L. venezuelensis. It is a use according to claim 20, bacterial disease bacillus, bartonella, bordetella, borrelia, brucella, campylobacter, chalamydia, calamidophila, clostridium, corynebacterium, enterococcus, arachnid, francella, hemophilus, helicobacter, legionella, listobacterioma, It is any bacterial disease caused by bacteria belonging to the main groups nisserya, pseudomonas, rickettsia, salmonella, sigella, staphylococcus, streptococcus, treponema, ureaplasma, vibrio, yersinia. A use according to claim 24 for bacterial disease bubony plague, pneumonic plague, cholera, syphilis, congenital syphilis, post streptococcal glomerulonephritis, puerperal fever, impetigo, stinging, febrile rheumatism, scarlet fever, streptococcal pharyngitis, acute bacterial pneumonitis, pharyngitis, middle ear inflammation, endometritis, neonatal sepsis, neonatal meningitis, neonatal pneumonia, cystitis, osteomyelitis, toxic shock syndrome, staticoccal food poisoning, sigellosis, salmonella, paratyphoid, typhoid fever, rocky mountain spotted fever, urinary tract infections, corneal infections, pneumonitis , meningitis, gnore, pelvic inflammatory disease, tuberculosis, leprosy, listeriosis, leptospirosis, legionnaires' disease, peptic ulcer, upper respiratory tract infections, chronic gastritis, bronchitis, septic arthritis, tularemia, bloody diarrhea, urinary tract infections, endocarditis, biliary tract infections , diphtheria, tetanus, parrot fever, trachoma, neonatal conjunctivitis, urethritis, epididymitis, prostatitis, lymphogranulomatosis, atypia It may be pneumonia, Guillain-Barre Syndrome, brocellosis, maltese fever, Lyrne disease. It is a use according to claim 20, viral disease adenoviridae, herpesviridae, papillomaviridae, polyomaviridae, poxviridae, heradnaviridae, parvoviridae, astroviridae, caliciviridae, picornaviridae, coronaviridae, flaviviridae, togaviridae, hepeviridae, papillomaviridae, polyomaviridae, filaviryaviridae, retroviridae, orthoviryaviridae, retroviridae, orthoviryaviridae may be a disease caused by any virus belonging to the main families rabdoviridae, reoviridae. A use according to claim 265, viral disease gastroenteritis, keratoconjunctivitis, pharyngitis, croup, pneumonia, cystitis, hand-foot-mouth disease, pleurodnia, septic meningitis, pericaditis, myocarditis, Burkitfe Lymphoma, Hodginas lymphoma, chronic hepatitis, nasopharyngeal carcinoma , hepatic cirrhosis, hepatocellular carcinoma, tonsillitis, cytomegalic inclusion disease, Kaposi's sarcoma, Castleman's disease, influenza, measles, Reye's syndrome, mumps, anogenital wart, poliomyelitis, rabies, congenital mbella, rubella, smallpox, shingles, congenital syndrome. The use according to claim 20, wherein neoplastic disease is malignant tumors or a physiological condition characterized by uncontrolled cell growth. A use according to claim 28 wherein the neoplastic disease may be carcinoma, lymphoma, blastoma sarcoma or leukemia. For a use according to claim 29, cancer disease; breast cancer, prostate cancer, colorectal cancer, skin cancer small cell lung cancer, non-small cell lung cancer, mesothelioma, gastrointestinal cancer, pancreatic cancer, glioblastoma, vulva cancer, cervical cancer, endoinetrial carcinoma, ovarian cancer, liver cancer, hepatoma, bladder cancer, kidney cancer, salivary gland carcinoma, thyroid cancer, and various head and neck cancers. Pharmaceutical compositions containing compounds represented by formula I according to claim 1 A pharmaceutical composition according to claim 31, containing at least one other active ingredient in addition to the compounds represented by form I. It is a pharmaceutical composition according to claim 32 and the other active ingredient is selected from known active compounds showing antiparasitic, antibacterial, antiviral, antineoplastic and/or cytotoxic and/or antiinetastatic effects, or their double or triple combinations. A pharmaceutical composition according to claim 33 and the active compound with antibacterial action is amikacin, gentamicin, kanamycin, neomycin, netilmicin, tobramycin, paromycin, streptomycin, spectinoinicin, geldanamycin, herbimycin, rifaximin, loracarbef, ertapenem, doripenem, dimenem, imipenem, Sefazolin, Sefalotin, Sefalexin, Sefaklor, Sefamandol, Sefoxide, Sefprozil, Sefuroxim, Sefiksim, Sefdinir, Sefditoren, Sefoperazone, Sefotaxim, Sefpodoxim, Seftazidim, Seftizoxim, Sefepim, Ceftarin Fosamil, Seftobiprol, Teybaninin, Dalbaninin, Dalbaninin , clindamycin, lincomycin, daptomycin, azithromycin, clarithromycin, dirithromycin, erythromycin, roxithromycin, troleandomycin, telithromycin, spiramycin, aztreonam, furazolidone, nitrofurantoin, linezolid, posizolid, dirithromycin, erythromycin, cycloxilicillin, cycloxilicillin, fluloxilicillin, amphibiancillin, , mezlocillin, methicillin, nafcillin, oxacillin, penicillin G, penicillin V, piperacillin, temocillin, ticarcillin, clavulanate, sulbactam, tazobactam, bacitracin, colistin, polymyxin B, ciproiloxacin, enoxacin, gatifloxacin, gemifloxacin, levofloxacin, lomefloxacin, moxifloxacin, moxifloxacin, moxifloxacin, nafloxacin, nafloxacin sulfacetamide, sulfadiazine, sulfadimethoxine, sulfametizole, sulfamethoxazole, sulfanilimide, sulfasalazine, sulfisoxazole, tromethoprim, demeclocycline, doxycycline, minocycline, oxytetracycline, tetracycline, clofamethoxazole, sulfanilimide, ethicocycline, doxycycline, minocycline, oxytetracycline, sulfamethoxazole, clophazinemycin, ethyl acetate, cyclophosphamide, chlorophyllium, are selected from the group consisting of arsphenamine, chloramphenicol, fosfomycin, fusidic acid, metronidazole, mupirocin, platensimycin, quinupristin, dalfopristin, thiamphenicol, tigecycline, tinidazole, trimethoprim, or from double or triple combinations of the agents listed here. A pharmaceutical composition according to claim 33 and active compounds with antiviral effects abacavir, acyclovir, adefovir, amantadine, amprenavir, ampligen, arbidol, atazanavir, atripla, balavir, cidofovir, combivir, dolutegravir, darunavir, delavirdine, didanosine, dokosupine efavirenz, emtricitabine, enfuvirtide, entecavir, ecoliver, famciclovir, fomivirsen, fosamprenavir, foskarnet, phosphonet, ganciclovir, ibasitabine, imunovir, idoxuridine, imiquimod, indinavir, inosin, interferon type II, interferon type II, interferon type II, interferon lopinavir, loviride, maraviroc, moroxidine, metisazone, nelfinavir, nevirapine, nexavir, nitazoxanide, novir, oseltamivir, peginterferon alfa-Za, penciclovir, peramivir, pleconaril, podophyllotoxin, protease inhibitor, ribavirintavirin, analogues of ribavirin, protease inhibitor, nucleo-pyramidinevirtamivir, nucleonaryl, podophyllotoxin, protease inhibitor, nucleo-pyramidinevirintavirin , saquinavir, sofosbuvir, stavudine, telaprevir, tenofovir, tipranavir, trifliridine, trizivir, tromantadine, trovada, valacyclovir, valganciclovir, Vida rabine, Viramidin, zalcitabine, zanamivir, zidovudine, or from double or triple combinations of the agents listed here. It is a pharmaceutical composition according to claim 33.6 and the active compounds with antiparasitic effect are nitazoxanide, melarsoprol, eflornithine, metronidazole, tinidazole, miltefosine, mebendazole, pyrantel pamoate, thiabendazole, diethylcarbamazine, ivermectin, metronidazole, pyrantel pamoate, thiabendazole, diethylcarbamazine, ivermectin, cyclonicindazole, ammonidazole, pyramidol, amphincindazol, amphicindazole furazolidone, nifursemison, nitaxozanide, ornidazole, paramomycin sulfate, pentamidine, pyrimethamine, tinidazole, albendazole, mebendazole, thiabendazole, fenbendazole, triclabendazole, flubendazole, abamectin, diethylcarbamazine, diethylcarbamazine, cyclopamide, occiclozapine derquantel is selected from a group consisting of amphotericin B, urea stibamine, sodium stibogluconate, meglumine antimoniate, paromomycin, miltefosine, fluconazole, pentamidine, or binary or triple combinations thereof. 37. A pharmaceutical composition according to claim 33 and the active compounds with antineoplastic effect are cyclophosphamide, ifosfamide, temozolomide, capecitabine, 5-fluorouracil, methotrexate, gemcitabine, peinetrexet, initomycin, bleomycin, epirubicin, doxorubicin, irispacinocin, e docetaxel, vincristine, carboplatin, cisplatin, oxaliplatin, bevacizumab, cetuximab, gefitinib, imatinib, trastuzumab, denosumab, rituximab, sunitinib, zoledronate, abiraterone, anastrozole, bicalutamide, exemestane, bicalutoxin, chlorineprogestin, octalutoxycin, oxregestrene, oxregestrene, bicalutoxin, oxregestrene, oxemetrazoline, octalutoxin, oxregesterone, chlorine, octalutoxycin, oxregesterone lomustine, inelphalan, procarbazine, streptozocin, fludarabine, raltitrexed, actinomycin D, dactinomycin, doxorubicin, mitoxantrone, eribulin, topotecan, Vinblastine, vinorelbine, afatinib, aflibercept, crizotinib, dabrafenib, crizotinab, peripliumab, peripolumab, umbanib, persimmon, afatinib, aflibercept, crizotinib , sorafenib, trastuzumab emtansine, temsorilimus, vemurafenib, ibandronic acid, pamidronate, bexarota n is selected from a group consisting of buserelin, cyproterone, degarelix, folinic acid, fulvestrant, lanreotide, lenalidomide, letrozole, leuprorelin, megestrol, mesna, thalidomide, or binary or triple combinations thereof. 38. A pharmaceutical composition according to any one of claims 31-37 comprising at least one excipient.
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