Hua Xun Intellectual Property: The State Intellectual Property Office has determined that the patent rights of Selepa I are all invalid.

2023Year06Month30On the same day, the State Intellectual Property Office issued No.562524No. Invalidation Request Review Decision, Declaration Involved.“Crystalbody”Invention patent right (patent number:ZL201080028176.8) (hereinafter referred to as the patent in question) are all invalid.This caseRequesterYesNanjing Huaxun Intellectual Property Consultants Co., Ltd.,The patentee isJapan New Medicine Co., Ltd..The patents involvedDrugsSelensipa(Selexipag)is a selective prostacyclinIPreceptor agonists, currently in60Several countries are licensed for pulmonary hypertension (PAH) of oral treatment.This caseAll invalidThe legal basis isPatent Law No.22Article3Creativity under paragraph.

【Decision Points]]

The preparation of medicinal compounds into medicinal crystal forms is a common pursuit in this field. The key to judging whether the crystal forms of known medicinal compounds are creative lies in determining whether they produce unexpected technical effects. If those skilled in the art cannot determine that the technical effects recorded in the patent specification must be brought about by crystals, they cannot determine which technical effects the crystals themselves produce, furthermore, it is not certain that the patented crystals produce unexpected technical effects relative to the prior art.

[CaseBackground]]

RequesterViewpoint:Claim1RelativeEvidence1and common knowledge(Evidence2,3)The combination is not creative.Patent involvedand evidence1The difference is the evidence.1UndisclosedSelensipafor crystals,Patent involvedrelative to the evidence1The technical problem actually solved is only to provide a specific crystal form. Different crystals have different physical and chemical properties, such as stability, particle size, etc., and those skilled in the art can try to obtain different crystals by using conventional crystallization techniques in the field of industrial crystallization.

PatenteeViewpoint:Patent involvedcrystal formIUnexpected technical effects are obtained, as shown in the grain size.Large so that the filter is good,High impurity removal rateandHigh purity.PatenteeAlsoIndicates that the particle size is an inherent property of the crystal, and there is only one particle size distribution, with small deviation; the effect of residual solvent and impurity removal is related to the crystal itself, as well as the preparation process and preparation process.

The focus of dispute between the two sides:Patent involvedcrystal formIHas an unexpected technical effect been achieved.

Facts checked:Patent involvedThe aim is to provide a new crystal with excellent efficacy, which is a high quality product and easy to handle in industry (seePatent involvedInstruction No.2Page[0006]-[0019]paragraph). For the technical effect of crystals,Patent involvedThree test cases were recorded: Test example1DeterminationParticle size; test example2Determination of the concentration of residual solvents contained in crystals; test examples3The impurity removal effect of recrystallization was determined.

【Claims]]

1. Claim1Protection2-{4-[N-(5,6-diphenyl pyrazine-2-Base)-N-isopropyl amino]butoxy}-N -(methylsulfonyl)acetamide (hereinafter referred toSelensipa)Itype crystal, and defines the powderXX-ray diffraction pattern.
2. Claim2-6and8All protection contains crystal formIComposition as active ingredient.
3. Claim7protection crystal formIThe preparation method.

【InvalidReasons for the decision and its conclusions]]

Evidence1(CN1516690A)made publicSelensipaThe preparation method.InvolvedPatentClaim1crystal formIand evidence1The differenceTechnical featureslies in: Claims1for crystal formIwhich has a specific powderXX-ray diffraction patterns, while the evidence1UndisclosedTheForm of the compound.

It is known in the art that the particle size is not only related to the crystal itself, but also related to the preparation method of the crystal, the size of the particle size is mainly affected by the crystal nucleation and growth process, so the crystal preparation process of a variety of process parameters will affect the particle size obtained, even for the same crystal type, the use of different preparation methods.AlsoCrystals with different particle sizes can be obtained; the concentration of residual solvent in the crystal, the purity of the crystal and the removal rate of impurities all represent the purity of the crystal, and it is known in the art that the performance is not only related to the nature of the crystal itself, but also related to the preparation method of the crystal, and the purity of the same crystal obtained by different preparation methods, the residual amount of solvent, etc. are also different.. Therefore, the technical effects recorded in the patent specification in question do not represent the technical effects of the crystal itself, I .e. the patent specification in question does not record the crystal form.Iper se, the specific technical effect, which is relative to the evidence1It is even more impossible to talk about the unexpected technical effect, so the claim.1relative to the evidence1Only a specific crystal form of a known compound is obtained.

Evidence3The study of drug polymorphism is an indispensable and important part of new drug development and production process control and preparation design. Evidence2It is disclosed that the preparation of drug polymorphs includes a recrystallization method, and different crystal forms can be obtained by selecting different solvents under certain conditions.

Accordingly, the claims1in evidence1and evidence2,3The basis of the combination does not have the patent law.22Article3The creativity of the provisions.

Claim2-6and8Additional technical featuresalreadycompared document1discloses or gives technical teaching,Claim7The additional technical features arecan passObtained regular technical means in the field.,InClaim1Without the premise of creativity, the claim2-9Nor does the Patent Act No.22Article3The creativity of the provisions.

counter-evidence1-4Creativity-related documents. counter-evidence1Used to prove evidence1The product obtained is not the crystal form of the patent involved.IBut the crystal form described in the patent specification involved.III. counter-evidence2Used to demonstrate that the larger the particle size, the better the filtration and drying performance. counter-evidence3Control limits for demonstrating impurity levels.counter-evidence4Used to prove the crystal formIRelative to crystal formIIIThe purity is higher and the impurity removal effect is better.counter-evidence1,4It is a supporting document related to the experiment. As Dao Hao Si did not appear in court for questioning, the authenticity of the two pieces of evidence cannot be confirmed. In addition, those skilled in the art cannot be sure that the technical effect recorded in the patent specification in question is a crystal form.Iproduced by itself, disproved2-4The technical effect embodied is not only determined by the nature of the crystal itself, so the crystal form cannot be determined.IThe technical effect of the crystal form cannot be proved.IUnexpected technical results were achieved.

Based on the above facts and reasons, the State Intellectual Property Office declared201080028176.8All patent rights for the invention are invalid.